Download as pdf or txt
Download as pdf or txt
You are on page 1of 165

A Tex t B o o k o î

P HA RM ACOLOGY ı
" .

l b u s P re
ı s c r ib e d fo r B P h a rm a c y
S tr ic tly A s p e r S y a
,

h rm a c y C o u n c il o f In d ia , N e w D e ıhi
S e m e s te r IV b y P a

D r M a d a n K a u s hik

P e e V e e (R e g d )

Scanned by CamScanner
CO N T EN T S

C h a p te r 4 Phm a c o lo fD
gy o ru g a A c tin g o n C en tr a l N e rv o u a S y ıte m I 206 296

\ 飞
u b n o h ađion t o w o ı o g y 3 , 1 2 H is to r iç a 1 ıa n d m a r k s o f p h m a I 4 0 N
am
e u ro hu m o r a l tr m
m is s io n in e n tr a i n e r v o s s y s te m 2
in o b u ty r ic a c id (G A B A ) 2 0 8 4 2 G iu ta m a te n e u r o tr a n s m itte r (G L I J)
4 1 G am m a

£ tu m a c o Ao g y 6 , 1 4 N a tu r e a n d s o u r c e o f d r u g s 9 ,
g \ u S co pe o P
,

zg 2 1 1 , 4 3 G l c in e 2 1 3 4 4 D
y o p a ın in e rg ic p a th w a y s 2 1 5 , 4 5 S e r o to n in 2 1 9,
U Ëņ c o n c e p t 1 1 1 6 R o u te s o t d r u g a d m in is tr a tio n 1 2 , 1 7
,
\ r 4 6 G e n e r a l a n e s th e tic s W 4 6 1 】 n h a la tio n a l g e n e r a l a n a e s th e tic s 2 2 4 , 4 7
1 5 , 1 8 A d d ic tio n 1 8 , 1 9 T o le r a n 1 9 , 1 10 D
ı? Ķ ce ru
g ¥ [J T C H y p n o tic s , s e d a tiv e ś 2 4 1 4 8 C e n tr a ll a c tin
, y g m u s c le r e la x a n ts 2 5 5 , 4 9
d e ıt e A \ \\ T a c c p h y 21 , 1 12 Id io s y n c ra sy 2 2 , 1 1 3 A lle r a
g y Y f aT A n ti e p ile p tic d r u s 2 6 2 4 1 0 A lc o h o l 2 7 0 4 1 1 D is u lf】r a m 2 7 5 4 1 2 M e th a
g , , ,

1 H m s 2 5 1 15 E m ry m e in d u c tio n en z w e in h ib itio n o ili


= , , n , in o l 2 7 7
O t d 33

C h a p te r 5 P h a tm ln B y fD
acn o ru g i A c tin g on C en tr a l N e rv o u ı S y a te m U 297 380
G e = a ıT b t m a co ı
o gr n 45 99 e e 己垂
5 1 A n tip s y c h o tic d r u g s 2 9 8 , 5 2 A n tid e p r e s s a n t d r u g s 3 0 8, 5 3 A n ti a n x i
U » m h n 2 2 ī T in c ip le o f d r u g a c tio n 4 7 , 2 2 1 M e c h a n is m o f ln m e ty d r u g s 3 2 0 , 5 4 A n ti m a n ie s o r m o o d s ta b liz e r s 3 2 5 , 5 6 H a llu c in o g e n s
&agartim 2 3 D n ıg r e c e p to r in te r a c tio n 5 0 , 2 3 1 R e c e p to r th e o r ie s a g iT a 3 2 8 , 5 7 A n tip a r k in s o n s d r u s 3 3 1 , 5 7 A n tia L z h e im e r s a e n ts 3 3 8 , 5 8
g g
X ZL ı i m o t r e c e p to t s 5 3 , 2 4 1 T ra n sd u cń o n m echa n is m 53, O p io id a n a lg e s ics a n d a n ta g o n is ı s 3 4 3 , 5 8 1 N a r c o tic a n a lg e s ic s 3 4 3 , 5 8 2

25 D « e ıd ıū o n s h ip 59 , 2 5 1 T h e r a p e u tic in d e x 6 1 , 2 6 C o m q n n O p io id a n ta g o n is ts p h a r m a c o lo g y 3 5 6 , 5 9 C N S S U l a n t s a n d n o o tr o p ic s
m d i d bA ł 358
P 61 2 7 F a c to rs m o d ify in g d r u g a c tio n 64, 2 8 A d
m & q 69 , L 9 m ıg in tm c o n s 7 5 , 2 10 D
ū n ıg d is c o v e ry an d bmi \ In d e x (i) (iii)
« ım o E n ew m 8p 7 8 , 2 1 1 p h a r m a co v ig ila n ce 80

h \ h m a a o(D m Ĉ 0S O
» A c tin g on p e ń ph e ra l N e rv o u s s y s te m 1oo 20 5
3 ı0 ı = a io n a n d lrm c ı H
E n io n o f p e r ip h e r a l n e r v o u s s y s te m 101, 3 2 N eu rJ u

U««mi=i=il0c 3 1 1 s te p s im v o lv e d in n e u ro hu m o ra ıtr a n s
n in im 10 5, 3 2 2 C
u n
i m n n itte r 1 0 6 , 3 2 3 C 1a s s ifıc a tio n o f n e u ro tr a n s
m , 33
\ h o r n iın e tĵc
pa ı s s y s te m d d r u gs 1 09 , 3 3 1 c h o ı in
aAnū c
an

Ħ 圳 ,
h o d ru i
g s 1 1 8 , 3 4 p a r a s p n p a th o ly t c

Scanned by CamScanner
Scanned by CamScanner
rä]l A Te x t B o o k o f P ha r
m a c o l
g (V °
y
j G e n e ľ a ıP h a r m a c o lo w t
LA N D M A R K S O F p H A R M A c o
l ĺ 2 H IS T O R IC A L LB §Iı
u s
q b d is co m id e r e d th e fa th e r o fA ın e r ic a n
f M ic h ig a n in 1 8 9 1 an
i o f th e s p e c ie s , p e o p le h a v e tr e a te d p a in a n d d is e a s e w i d ep a r tm t a t th e u n iv e r s ity o
sin c e th e b e gin n n g
en

t a n im a ls , a n d m in e r a ls H o w e v e r Th e s c ie n c e o f
th s
uBÉáces
d e riv e d fro m p la n s , p h a r m a c o lo g y is l ha is m by w h ic h
d e r s ta n d th e m ec n s
g y is to
e ss
a c o lo u n
ld u s h e re d in b y th e a b ility to is o la h ? p ıır e c o m p hase 7 ħe g o a l o f p h a rm
th a n 15o ye a r s o p o u n d s ijbthe )ıl i uiıent r a tio n a l u se o f e ffe c tiv e a g en ts in th e
to a b le th e
f 1h e s d m tißc m e th o d H is to r ic a lly th e s e le c t io n a n d U S e o f s y s te m s en
Jd in te r a c t ith b io lo g ic le d to
a b lis h m e n t o
w
e sı
dr ıs ífere w hi ta s k h as a n
f d is e a s e f p h a r m a c o lo g y in t s
T he su cce ss o
)
bX
lia g p °s is d tr e a tm en t o
)f
an
t 5 0 e a rs T w e n tie th c e n t u r y
:4 9
l l i th e p a s y
d r u g d e v e lo p m e n t p a r tic u a r y
n
d e x p lo s io n o f n e w o f
, m g n o x io fo r d ia b e te s th e d is c o v e r y
二 ニア葛 歹苁二碡钰
ıl s a ge .

二 职 賺 。. . 石ぶ 蒯
。 p a ぷ 剧。
ġ
ri ęH q p p m e n ts in c lu d e th e is o la tio n a n d u s e
o f in s u lin

dv en t o f m o d em p y
s c h o p h a r m a c o lo g y
? c r o b ia l a n d a n tin e o p
la s tic d r u g s a n d th e a

Řtimi c
ec u l ar b i ol og y , e n e t i s ,
ń d dr ug d e s i gn s u g e
g s t t ha t n e w d r u g


t ad v a n c e s i n m o l ill v id e e v e n g r e a te r a d v a n c e s
in th e
lo ie in n o v a o t i n s w p r o

¥$lopment a n d p h a r m a c o g
S e co n d Irı e se c o n d p ha se f d r u g u s a e E x e r ie n
感 tr e atm e n t o f m e d ic a l d is o r d e r s
in th is c e n tu r y


o
g p c e e n a b le d
ÞĒō ĦĖ too
u n d e rs m d w M d ı s u b s ta n c e s w e r e a c tu a lly beneicial in j
qosc C O LO G Y
r e lie v in
g p a r tic ııla r d i e a s e N O B E L P R IZ E P H A R M A
ģ ĥ 9İ b
s ym p 加m &
1heß rstedirredrugs w e r e p r o b a b ly s im p le exte rnal p r e p a r a t io n s s u h
c as co o l
y in p h a m lo g y
m ud or a s o o g W th e e a d ie s t 】 03 eß ıi N Y e ar A w a rd s ig n iĦc a ııt d is c o v u a co
o n o w ıı r e s c r i tio n s fr o m 2 1 o o B C E o e l pe ıs o n
p p a
includelves
b

« m la in in g ? O v e r m a n y o e n h ir ie s
w p e o p le learned th e th e r a p e u tic v a lu e o Ê
n a ural 190 8 F iis t a n tiın ic r o b ia l druce (m g ic b u lle t)
p r o du d s thro u g h trial a n d e n D r B 1 5 00 B C E E i T q ı
iıylMetchnikofi P a u l E i u lic h
y g y p tia n p r e s a ip tio n s c a lle d f o r c a s to o il
o p iu m ļ a n d 0 c hn
g i lh a t a r e s ta l u s e d to d a y In c h in a a
l
n c ie n t s c r o 丑s fr o m
lis te d
P fo r 】 ıa b a l medicines f
a Į l
tim e
o r m o r e th a n 5 o d is
aı m y su r e o n w ħ h
e ases D io s c o r id e s ' d r e e k
g o e d in th e ls t c e n h
n y d e s c r ib e d m o
r e th a n 6 0 o m e d ic in
c o lJe d e d a n d ħ a l p la t ħe
s u d ie d a s lr
e b a ire le d w ith
th e R o m a n a r m
d e sa ibe d ı ħe p r y S u s r u ta a H in d u p h y s iþ j
w ķ o í A y ım e d jc m e d c n e in th a n

Is la m ic e 5 th c e n tu ı
P y Midbrï Ąges,
D u r in g th e

靆 Ĥ e u se o f h b
rr a l
o s t la Jn o u s l A v i
y c a u ia » a n d c h i
r s t ia n m o n k s c u lti
v a te d a n d ie d

Z 9 J T lo a

Scanned by CamScanner
į łŁl ť t 囪L

'
, .

RĮ ţ iy TjA
,
Te x tB ' " ofph
ì
. '" ' "


N O B E L P R IZ E P H A R M A C O L O G ' "
h

Y z

N o b e lP e n on s S ig n ific a n t d lı
co v e ry 니
S ir )a q Es BlacJ
G e ıtr u d e E lto n G e o ıg e ü 一
H H c ħin gs 概
蚓 -
fr e d G ih
Aı an
ı Ada r tin R o d b e lJ 199 4 ı
Jis c o v e z f G p r o te in
y
a コ
o
s a n d th e J,
v o lm ıte e rs in th e la b o r a to r y
ce lı
s ił

l d itio n s o f u se
RobeıtFunh80 o u is
【 ı
gn a rm F e r id li 199 8 R e c o g n itio n d u c ts (2 ) T h e o p tim a co n
' " s a fe f th e n e w p ro

gn d
'
ffic a c y ty o
. ' ' " " To d e te r m in e th e e an
.i

lly , b y p a re n te ra lro u te
To b d m in is te r e d o ra
f d ru g i e e a
te ) o f a d m in is tr a tio
P a u l G in e e n ga r d E r ic 2 0 00 n o
C a rlsso n R o le o i d o p a m in e in M e th o d (r o u
'

K än d e l tr a n s d u c lio n in th e n
sc h iz o p h r e n ia 'p iė h
e rv o u s sy '
" m g r ëi
m ay h a rm th e concerned ndividual
□ sc o PE o F
PHARMACOĹo
:ln
h r m a c o lo g ie s h l d y a n d
d r e q u ir e s r ig o r o u s p a
Th e p h n m a c o lo th e s iz e d o r in v e n te
gy is a n e x p e r im e n ta l s c ie n c e a n d o n e o f th e o u T ħe p ro d u c t syn
n ew
tic u s e s to x ic ity e tc
T h e s tu d y o f
th e b a s ic m e d ic a l sciences Tħe s c o p e o f
y n ge st
)o f discipı
ine¢bHłæh jo n to d e te r m in e its m e c
e y ą Įp a ł
h a n is m o f a c tio n th e r a p e u
a r e m a d e in
p h a r m a c o lo g y js c o n s ta n tl t d T h e cl n ca
i i l t r ia ı
s
y enĮ ġ jN f th e d r u g is m u s t to b e c o n d u c e
COntribution to m e d id ru l th e r a
p y h a s m a d e its p o s it io n in th e m d
Jts miĤ ųqfism a n d e x c r e tio n o
medicines , o f g r e a te r im p o r ta n c e Its r e ı
e íc a ] fiëR ln & Ĥ đ i
tb ę d a ţ Atory im a ls a n d o n h u m a n v o lu n te e r s
o n a n
a tio n s h i
8
p to th e o th e r m e d ic a l s c ie n c e s is i t
th a t e n a ble s m e đc a ıs h ıd e n ts to tın d e n e r e s tin
r s ta n d th e b e tte r g
p o s itio n o f th is s c ie n c e
W ħe n th e r e is a n ĵ m b a la n æ in th e R e q p ir a to ı) P h i
n o r m a l b o d il
y p r o c e s s a p a th o lo g ic a l c o n d itio n (illn e o v a sc u ıa r P h a rm a c q ı
o gy
s s ) is lĺ í) n C a rd ı
p e se n t Th e n a d r u g o r p h a r m a c e u tic a l a e n t * Ðn
(c h e m ıc a ıp r o d u c t) is a d m in is te r e d t

e
g
su Ħ e r e r b c u r e th e d is e
a s e d c o n d itio n T ħe a c ti

P a th o g e n ic s ta te is s h z d e d b th e h a r
o n o f th e d r u
g
o
in tr o d u c e d in th e b o d to c u r e
y
th ė
in
o J bT 9

o J bo r
r
y p m a c o Jo
g y p ħa r m a c o ı o g y u s e s c h e m ic a l s u b s ta n c e s t z ıJ ırn Ja dJ
o
P r o d u c e c h a n g e in fu n c tio n a n d m
o rp h o lo
g y h th e Jiv ín g s y s te m (m e n & a n im a ls )
Jt is Ja ıo v m b
y g o in g th r o u g h th e a s t M s to r P h. aco ı
oa r
y o f r e s e a r c h a n d in v e n tió n s T 1ì e tlt a lk a lo id
rm
p Vıï ßlßJa į i
m o tp M n e w a i
s s o la te d fr o
n ı la n t o itım b y th e G e r m a n A o th e c a r
p p
1807 ı n 1828 w o h p y s:ee rrhh lım e r in th e y e a r
e r s Jm th e s iz e d
u re a ı ro m a m m o n iu m c y a n a tE

N Į Ī4 0 C N
N H 2C O N H 2
A m m o n iu m c y a n a te U re a
m a d e u re
a w ith o u t a k id
n qy
the
y e a r 19o o A b e l
an d M s a s s o c ia d u lı
te s is o la te d d ren ) fr o m th e a
o r a dr e
n a l la n d
g s
a a in (e p jn
ı e p h r in e m e

h the e a
y r 1901 R e id
H u n t is o la t d Ja r g e
num be r o fn e a c e ty Jc h o Jin e fr o m th e a d re n a l g la n d s s in ce th e n a
ew d ru U ĵ İ l Ŕ iliJ
g s h a v e b e e n s n th i th e s e ie ic łie Jd
tiı
y es z e d a n d
p re p a re d e v e ry y e a r ín n

Ħq 1 2 A dı
a o ra m re p re s e n tı
n o th e a c o p e o f p ha rm a c o lo Ĥ v

Scanned by CamScanner
妇 區
・ 區
lm r đ
Ieral pha rm a c o

T o x ic o d y n a m ic s
d e s a rib e s th e h a r m fu l
a s s e s th e a b s o r p
tio
e

n
ffe c ts th a t th e
d is tr ib u tio n
P
s n e x i
b io tr a n s

T o x ic o k in e tic s e n c o m p
n ıd y
i o f ge n e tic a lly
d d e a ls w ith th e s
is r e la tiv ly n ew fie ld a n
p h a rm a c o tic s m s a e
gn e
h ic h d e a ls w ith th e
is th e d iv is io n w
ľ C lin ic a l p h a r m a c o lo g y
lo g y
Cl c ph a rm a co
i f a t io n a b o u t th e u s e ħıln e s s
id e s n o r m
a c o lo g ic a l e ffe c ts o
f d r u g s in m a n It p r o v
p h a rm i ° r ta n c e fo r
th e e ffe c tiv e a n d
to x ic ity o f n e w d r u g s in
h u ın a n s It is o f g r e a t m p
pomjpand
SafQiçbf d r u g s in m an

□ NATU ? A N D SO U R C E O F D R
ly k n
Th ààrg "
j
" h e
p r e s e n te d b y t r e
n am e. . H ic h is c o n u n o n o w n a s

s o u rc e s o f d ru gs
u u n i ag

ï
ŢŢ iiT
' "

Ť
R C E O F


eJiluq«
y d t Jb n ìĥ
ıt S y n t h e tic 寧
X ı S e m i s W t h e tic 礬
M ic r o o r g a n ı
s m 薛
D NA R e co m bı n a n tTe c h n o ı
In J ilJ n T q o gy

ï ri J in i łm
F ig 1 3 o r ig in n f th e d r u g ħo d iffe
m re n t so lu c e s
u rll ı
frĵr
P la n t S o u rc e T h e d r u g s a r e o b ta in e d fr o m p la n t o r ig in p la n ts c a n b e u se d a s th e r a p e u tic
OjtĮ çęi in
rę§ s e v e ra l w a y s It c a n b e u se d as h e r b a l te a s o r o th e r h o m e m a de rem e d ie s w h en
thoıq r g jc o n s id e r e d a s m e d ic in a l
p la n ts T h e y c a n b e u se d a s c ru d
e e x tr a c ts o r s ta n d a rd
e n r ic h e d fr a c tio n s in p h a r m a c e u tic a l r
p e p a r a tio n s s u c h a s tin c tu r e s flu id e x tr a c ts der
P¥fsñ n ca p s u le s w h e n th e
y a r e c o n s id e r e d as p h y to p h a r m tic a l p
p o w

哼fles F in a lly
a ceu
p a r a tio n s o r h e r b a l
re
\ p la n ts c a n b e s u b je c te d to s u c c e i
ss e v tr a c tio n a n d
p u r ific a tio n
ex
P
$gw iĵ w e s to is o la te th e c o m p o u n d s o f in te r e s t w h ic h c a n th e m s e lv e s b e a c tiv e a n d u s d
a
ke a d r u g e x a m p le s b e in g q u in in e d ig o x in a n d e r o t
ŕifï 'aļ ı e

g a m in e

Scanned by CamScanner

e ra l P h a rm a c o ı
o gw
G e rı

M ic ro b io ıo g i◆ l S o ıtr c e s
M a n y life s a v in g d r u g s a re o b ta in e d fr o ń in g i
m m o u ld s an d
b a c te r a e g p e n
i iď li h P e n ic illiu m c h lo r a m
n o m n o ta h ım
p h e n ic o l fr o m S tr e p to m
y c es
v en e z u e ı
ae g r is o ń rlv in fa n a n ti fu n g a l d r u g ) fr o m P e n ic iu iu m g ń s e o fu lv u m n e o m )lc in ħo m
S tr e p to m y c e s fr a d ia e a n d ept omy cin fr o m S tr e p to m y c e s g r is e u s

s H n & y n M t t ic S o » n ce « So m e tim es semiynthetic p r o c e s s e s a re u se d to p re p a re d ru Þ


- w hen
th e s jm th e s is o f d r u g s fc o m p le x o le c u le s ) ın a
m y b e d ifó c u lt e x p e n s iv e a n d u n eco n c m ŕ ic a l o r
h e n th e lso
w n a tu r a u rc e s n ı
ay yß e ld im p u r e c o 呷 o u n d s In th e s e s itu a t io n th is m e b d s p la y
th
im p o r ta n t ro le F o r
an exam p le s a r e semiynthetic h u m a n in su lin a n d 6 a m in o p e ilic ilĮ a n ic
a c id d e ń v a tiv e s T h e s e a re p r e p a re d b y che m ic a lly m o d ify in g su b s ta n ces th a t a r e a v a ila b le
fr o m a h tr a
īı l s o u r c e im r o v to im p its p
p e ro v e o te n c y e ific a c y a n d a ls o r e du c e s id e e ffe c ts
: ĥ ı{J ĺ J Z
ntial D " t "
W j
iS ĥ ír rO
r【 "

F ig 1 4 B a s ic co n ce p to fe ss e n tia l d ru gs
? b io y Jł
ao

e ss en tia l m e d ic in e lis t con ta in s lim ite d co s t e ffe c tiv e an d s a fe m e d ic in e s, w h ile th e o pen


ßn i t ßt l r
l p h a rm a ce u tic a l m a rke t is flo o d e d w ith a la r g e n u m ber o f m e d ic in es m an y o f w h ic h a re o f

Scanned by CamScanner

L
.
ız

. T' h e' c t t. o'


" o np c e p f" n s s e nt
e t
í
l íI □
ial lm medicines
ia
A T

edicines h ha as
e x t B

b
o o

p ne e n
k o fP h ' '" " a' c"
a
o lo
ı
Wi v Vf°q
i
d o u b d id rra lu e sh w o r ld w id e a

§ıU a l R o u te
d d e r th e to e su cke d T h is te is d
m l
rKĝ ta b le ts a r e p la ce u n n gu ro u u se

J
YI o J I
m R O U T E S O F D R U G A D M IN IS T R A
W 1 sJ In tJ j
e
h a in r o u tw f a d m in is tr a tio s n u li
Rou k o f a d m in is tr a tio n a re vo m o n o f d r u s (1 ) E
g a s t】
hm n
n te r a l H
ou te (2
P a l R o u te )
Aa?äiı
ges
3 n 0 t a c tio is q u ic k
ı E n ie n ıR o u te (1 ) O n se
n

(B y
ŕ. X e H y
U e
ı e n te ra l r o u te includes o ra l ro u te m o u th ) n a sa l ro u te b lin g u a l
su
tio in th liv er is
m u te a n d ıe c r o u , îginal .' ' " m a M '' " m e. . ' " . ' " _ c n e

O n l R o u te (B y M on th ) io v íi id e d (p r e v en tėd )
av o

t llo d to sw a llo w o r c hew th e ta b le t is k e p t b e lo w to n gu e


T h is is a ı
u h 】r a l r o u t o f a d m in is tr a tio f d r u g s Ti
n o n e d r u g s in th e fo a re n o a w e
rm w w w
c a p s u le s po w d e rs m ù? u res e a le a dm in is te r e d th r o u h th is r o u te
g
o r s y s te m ic e ffe c t
cal C 1o tr im a z o le v a g in a l
a罗
」, T h is ro u te is a ls o u se d to p r o d u c e lo
d h i o f rulvo g in a l C a n d id ia s is O th e r ın e d ic in e s 1ĵ k e
A d r a n ta g e Ŕiİ ĉ ūqq s u p p o s ito
ńes are u se case v a

le e tc a r e a ls o a dm in is te r e d b y th is r o u te
1 M is ıo u is th e m o s t c o n v e n ie n tro u te o fdru g d m in is tr a t io
J s ßn o ] iı
M ic o n a z o le k e to co n a z o
a n
J R e c ta ıR o u te
Z P a tie n t c a n th e p r e s c r ib e d m e d ic in es M m se lf
i n to p r o d u c e
3 T he n js
S l iT th d r u g s th r o u g h th is r o u te in th e fo r m o f s u p p o s ito r y o r e n e m a a r e g v e
e
no p a in b th e p a tie n t th is ro u te is v e ry c o n v e n ie t d h u gh th is r o u te
n e co n o m ic a l 1o ¡
ß3 o l lo c a l o r s y s te m c e i ff e c t G lu c o s e P a r a ld ih y d e c a n b e a d m in is te r e d t r o
D is a d マ至此妇魯區
it ń e s a r e m e d ic in e s
o 7 닥・o h 厂 C h lo r p r o m a z in e s u p p o s ito ń e s a r e g iv e n fa r v o m itin g c o n tr o l S u p p o s o
1 T h e e ffe đ o f
d r u g m b y o r a l r o u te is d e la y e d 570 qT 0t ' in c o r p o r a te d in w a x y b a s e w h ic h m e lts a t b o d y te m p e r a tu r e T h e ın e
d ic a te d s u p p o s ito ń e s
It is no ta n e m e e n c r j s T o Ja t d i f i t
rg y o u te 9 Īĥ a r e s o r e n r e r g e r a o r

3 T he in ila n t d r u
gs ca n n o tbe g iv th r o o b n l In d o e th a c in su p p o s ito ń e s a re a d m in is te r e d fo r rh e u m a to id ar th r itis a m in o p h y u in
g h th is
en m
u ro u te
4 T h js ro u te (z n n o t b e u s e d in c a s e f ) lİ e o qq u e su p p o s ito r y fo r b ro n c h ia l a s th m a En em a is liq u id p r e p a r a tio n in tr o d u c e d in th e c o lo n
o u n c o n s c io u s a n d
5 C e r ta in d r u
n o n « o o
p e r a t iv e p a tie n ţ b ßu EVacuatėn e n e m d fo e ffe c t R e te n tio n e n e m a is m e a n t fo r a d m in is tr a tio n
gs c an n o t b e g iv e n th r o
. V Ī a is u se r p u r g a tio n
u g h th is To u te as th e y d e s tr o y e d b?gaótric fłmg t hr o u g h thi s e
for loc a l us x le co r ū s o n e i s g i ve n
a re
e n z ym e s ó do r sy s t em i c as we l l as e. a mp ro u t

C ar e sh o u ld b in u lc e r a tiv e co liū s
e taJce n th t
a s u ffic ie n t
dru to
g P r e v e n t s tic ki q u a n tity o f w a te r s h o u ld b e g iv e n to p a tie n t w i tA iđv á n td Ëe s o f r e c ta l ro u te
n g o f dr u
g in o e s o p h a g ııs a n d to d e c r e a s i it
e m a n t e fe c t o f
w e d ic in e s ŁĴ rwÐitaūon o f g a s tr ic m u co sa is av o id e d b y th is ro u te

-
Xx=X ° ty h '" ' " h . sh' ' " , g iv e. ' ' " c in e s h h qu i į .. ' ' " e b im
(2 ) T h e
o t
itd m
d ru gs
in is te r e d b y th is
w h ic h a re

ro u te
d e s tr o y e d by g a s tr ic en z ym es g a s tr ic ac id ity can b e

T (3 ) t h e d ic in d e s tr o y e d d u r in g th e fir s t p a s s
N ıııı«
o ıte
m e es w h ic h a re th r o u g h liv er can b e


C e r ta i
n d ru p s
c
ps) "
XPOd T
-
nth , '" lo c " ' "ect . N d g iv e . In th , f. R m o f ' " a l g u tta e (n a s a l
忒に慧鞣
."
' " ' 。 。, 。。
g s . ' " '" .
' ' 一 d ' ''。 叩
诊デ
' " ' " '
P ıie o ńne a r e a d m in i
s te r e d in th e fo r m
o f n a s a l dris
自由自 q ń ió JT j)

Scanned by CamScanner
Scanned by CamScanner
s b io lo g "
iı a l e ffe c t D e Ħn itio it is
p ro d u
n a
a b i】
i v to ce p ro p e r ty o f th e d
bo u n d to th e re c e
p to r a n d e
ru g
ffic a c y d
n o

e te
t th

r n ıin e s
e rec
ep
dru g is b o d w h.
o n c e th e
u n
ha p p e n s

D if¢ e ren t dru g s


th a t b in d to th e s a m e r e c e p to r a n d p r o d u c e th e s a m e t
yp e o f re s
p o n se w
d iff f e a c h o th e r in te r m s o f th e ir a ffin ity f o te n c jjj
i
typ c y a ll e r ro m
p y ) an d /o r e tftc a
a c o m p a r a tiv e te r m fo r d is tin g u is h in
cy Th e
te rn ıp o te m y js u s e d a s g w h ic h a o n i g s t h a s a h ig h e r
r e c e p to r The dru g h ic h
a ffin iy fo r a g iv e n w ca n p ro d u ce an e ffe c t a t lo w druer
c o n c e n tr a tio n s įs m o re Į x ) te n t (in Fig uri 5 D r u g A is th e m o s tp o te n t a d D
g
n ru g D is th e
e a s t p o te n t)
ı

:
'

Im

0 1 10 10 100 0 1 1 0 10 100
A is m
peūū n ta go n
șD ţ (n M Æ ) (s e iı e)
s c a ı F ig 1 6 C p e titiv e an d n o n co m ve
ło m M U LŁ
g ł¢ (s e m ū o g s ¢d e ) ru g m o g o m

Ħ& = S cb r m a lic ū lï ıs h a tio n o


f th e doseresponse c u r v e s f o r a s e d e s o f a o n is ts (A B C
g an d D ) th a t
h ar e & e s a m e e fó c «
J b ııt d iH E r in t - ・ o f th e ir
p o te n c y T h e m o s t p o te n t d r u g (D r u g A ) h a s th e lo w es t
Fm T a ln q an d is a p p m « im a te l 2 0 3 0 fo ld m o r e o tm t th
y p a n D ru g D

Jių iv ÐrIT

zJeirı
o

Scanned by CamScanner
sse n gef
ith th e c
h e m ic a l m e
f l o d in g it w b le m gh
d c ir c u it b y
o le a s u r a
th e b r a in .
Re w a r
s e s th e
in t e n s e ly p
t d u g s a ffe c t d c ir c u it c a u
g do se do e s p r o d u c e a n y a d d itio n a l r e s p M os r
th e d r u n ot
u la ū o n o
f th e r e w a r
ħ? th e r im ıe a s e jn o n se w hen T h is o v e r s tim
ll th e r e c e p to r s a r e n o t o c d o p a m in e M g h th a t t
h e p erso n
r e c e p to rs
to p r o d u c e th e r e s p o n se a
cu p ie d to p r o d u d u c e s th e
on
i w h ic h r e k n o w n a s
ce n e fe c t
th ė s d o p a
t b a n ef
ll m
by a 6 0 1 a g o n is t i e e a ch ce or tis s u e h as so m to th e e x c e s
m a x im a l re s p
o n se e re ce
p to b r a in a d ju s ts k in g th e
hiđ n øy b e c a lle d sp a r e r e c e p to r s
rs u n
occupi o v e r tim e th e
h th e y f e lt w h e n n« īr bs t t a iiiilaiı
w d to th e h ig
fe e ls c o m p a r e
M a x im u m r e s p o n se is p m du
They
ced by
are n o t
a go n
M dden
is t a t a c o n c e n tr a tio n th a t d o e s n
ila b le W n e n th e a
o t re
q u ir e to le r a n ce
X S o c ı
a
! e n v ı
e n
:"
t

x c u p a n c y o ft e r e p
h c e to r o r rm av a
ı

be c o u p le d to r e s p o n s e
T he y d o n o t? fe r fr o m th e n o n s a r e
p
y re
p to r
o ccu
p ie d th e
y T ra u m a
& a b u s e 19 ļ ) G e n e tic s


ca n re ce

M ax R es po n se e th n ic ı
ty @ キ

c 5 l? g e n d e r

A d d ヒ划ö れ

t a b le fa m ily æ ボ
l s k iı
ls u n s
p p o o r s o c ia
"
pe e r p re s s u re = ? M e n t a ıiıınes

ï> ,

ĝ Z iv in th dru g a d d ic tio n

\
in e s e
F ig 1 8 A m a jo r f a c to r v o

b bu se d o r ca u se ċun g
f d ru g can e a
S pın , d d ic tio in fo rm a tio n in d ic a t e s a n y ty p e o
D ru g a n
bacco d lc o h o l a s w e ll
r u g s lik e t o an
d a
i
n D r u g a d d ic t o n
d d ic tio in v o lv e s e a s ily a c c e s s ib le
li a p p e a r to b e
a

d lik i e a n d h e r o in S o m e d r u g a d d ic tio n s Ľ k e a lc o h o s m
l l
a s i ega l r u g s e c o c a n
D d d ic tio n in fo
ıtmnnlblıc o n c e n b a u o n ı h t m in e a d d ic tio n is o n th e r is e ru g a
s 1o o h ı
g h th e s p a re r= c ÐĦo rs a re o c c u
pı d e c lin in g w h ile o th e r s lik e m e th a m p e a
andma=bnaı
msponselsdimı
nihed'Reprentedfn D & E
ed
l
d r u g s a n d d r u g ty p e s a r e c o m m o n y a s s o c ia t e d w ith 山 n g a d d ic tio n
) įj in d ic a te s th e fo llo w in g
Fi 1 7 E ffe c t o f S a r e
p p to
re ce rs
d dru g ith 2 0 % f b eco m in g d e p en den t o n it a t so m e
1o
3 A lc o h o ı m o st w id e ly a bu se w o u s e rs
SP a r e rece
P to «sy b e d e m o n s tr a te d b u s in i
nu
m a 9o n js t b
a v a i】
a b le r e c e to
y g rr ev
p r s T h e s p a r e r e c e to r
e r s ib le a n ta g o n is t to p r e v en t bindiģ o f Po īŢ

dru g d d ic tio is
s u b s ta n deń d fr o th e p iu th e o s t c o īn m n
4 L
m n s?
p ro d t« e a n u n d i i
m n is h e d m
p co n ce
p t can be sh o w n w h e n th e agiİiist O p ia te s ces v e m o m poppy m o n a

a x im l th a t o f h e r o in
a re sp o n se in p re se n ce o f An ir r e v e i ėib le
W by
addiof b x i (c u r
are )
n T h is to x in
C ò Ła in e cra ck u p to 10 % o fu se rs go o n to h e a v y dru g u se
o ccu
p ie s a t le a s t 5 0 % f r e c e p to B t ș tiJ1 A p h e ta m in e s
o Ilk e
\ 11u t thie
rs u m c r y s ta lm e th u se o n th e r is e in ru r a l co m m u n itie s
yw a enoE
re
q u ir e d fo r H à11u c in o g e n s lik e P C P L S D d j
a riu a n a fte n b in d ith
a co m
p le te ly n o rm a l tw itc h o fA ch
an m o co m e w o th er d r u gs
P r e s c r ip tio n m e d ic a tio n su ch a s o x
yco do n e an d m o rp h in e
ddktio i s a
c him
O tìīe r c h e m ic a ls lik e to b a c c o s te r o id s an d o th e r s
m p u s iv e
DI ū c dis
W
. ea se c h a r a c te r i
b zed by d ru
co n tr o k in g
Xd in V
an
c
g Es tha t o
6cc uw ove
Ļ d e sp ite h
m h co n
g
se qu e n c e s
see an d u se th a t is
□ T O LER AN
in ter r tim
e e w ith d r u
g u se cha lle n e T h e to le r a n ce m ay b e đe fiï t e cl
g d d ic te d u n u s u a l r e s is ta n c e
d r itg
an a as to th e d in
p e rs o n s sen co n tr o l
c o n tin u o u s d
oT a ry do s e o f a ıh i
a n re g u la r u se f d r u gs m a
o
y ca u se to le It
c o n s ta n tu f d ru g
ra n ce m y be
a a c q u ir e d
se o o r it m a y b e co n
g e n ita l R e p e a te d a d m in is tr a tio n o f d ru g pro du l


Scanned by CamScanner
rĺŕp
i ". 2 i; ı

T .
lG e n e ra l Pharmacolo
38
n rıa l ıb e s s
d fa ile d t, o re sp o n d '"
rugconcentrationswhich 4 r R E s u LT
-x
ce a l

蠶 £
唱寓俨
th e d r u g p £b e '" 饨
. "
c e llu la r a c c lim
tiz a tio to th e p r e s e n
e ffe c tiv e
Th e a n ce o f a d r u g ís tr u
e to l eranc
" in a
ru
y 驟 鸾騾 黨
" '
对 병阳 園 踊 贸 可 ˜

D ru g D ep e n d e n c e
c ld y
da n Be f q u ı
lı d th a re d u e lle n ı
n re s p o to th e d
T oļ« ıa n c ıc a n b ı d ı m
as n se fte
ru g a r re peaı
e d dm ı
a n is tr a u o ns

(A )
M ec t lh a t w a s o n c e o

N o d tu l
M a ïn a d a

(日)
ta ı
o w er dos

Fırstdl
: e la m a
ı
,

(c ) = "
(D )
= ł - .
s la n a ll ħo m lh e a y a s a
s a n ae s m a c h

Hean
n d n M er
M a b ra in d n w ly

ratedropıTW g e n
ywlessanergldnB e u
Ĺ , ı
ı
ı

in g ls
r o v e rh e a ı
seı
000
a rı
sk

t W I " ' " trate s p e e d . u ood


p Bı

.
参熟 S M ï llo n W th d r w I
. . .

T le ra e
F ig 1 1 o A d ia g r a m s h o w s th e e f fe c t o f dru g dep e n de n ce

= = = = X o f5
==i '" n" " ・' " q e p e a te d u s e r re q u ir d a ey er lh Dr D įi f h e r o in depen den ce a ls o o ccu rs It d e v e lo ps w h en th e n e u r o n s a d a p t to
W ith re p e a te d u s e o

d o n ly fu n c ū o n n o rm a lly in th e p r e s e n c e o f th e dru g W n en
r e p e a te d d r u g su r e a n
Ħg 1 9 F u n dam en ta l c o n c e t o f T o l
th e ex po
p e ra n c e
ith d r a w e r a l p h y s io lo g ie re a c tio n s o cc u r T h e se c an b e m ild (e g fo r
th e d r u g is w n sev
W tie iı the dr u i life th r e a te n in g (e g fo a lc o ) T h is
hoı is lc n n as th e w ith d r a w a l
g s d is c o n tin u e d th e To l c a ffe in e ) o r ev en r o w
e ra n c e
d le n ic a 1 G l c n l d th b iM th
y y tr in itr a te is u s e d i d s yn d ro m e In th e c a s e o f h e r o in w ith ? aw a l can b e v e r y s e r io u s a n e a u s e r w u se e
fa c to ń e s w h n y n a m ite fa c to r ie s T h e n e w w
e n in h a le v a o r k e r s ín d n a d ii d ru g id th e ith d r a w lsyn d r o
p o u r s o f G iy c e r y l tr in itr a t y te a g a in to av o w a m e
e c a u s e ħe a d a h
c e T ħe w o r k e r s f o T he s ig n s a n d sy m p to m s d is p la y e d M o s t a g e n ts c a u s e a c h a n g e in th e le v e ıo f c o n s c io u s n e s s

J i s l o s t a n d if th e u su a lly a d e c r e a s e in r e s p o n s iv e n e s s S u p p r e s s io n o f b r a in a c tiv ity c a n b e s o s e v e r e th a t th e


y r g tu m to w o r k th p erso n m a y s to p b r e a th in g w h ic h can c a u s e d e a th
e y a g a in ex p e r ie n c e hea da che
: j A 1be m a ly th e u s e r m a y b e a ita te d a n r
tiv e io d b le to s le e
g g y an x u s an u n a p Hallutions
a re p o s s iÞ
1e A b n o r m a l v ita l s i n s (te m
g p e r a tu r e p u ls e te r e s p ir a to te b ı
o o d p re s su
ra ry ra re )
s s ib le a n d
ąr e p o can b e life t
y ・a te n in g
c h e s t p a in is
po
A b d o m in a ı a in
s s ib le är id can b e ca u se d b y heart o r 1g da m a ge f r o , d . Ĥ iju
°
se
p n a u se a v o mitin g a n d d ia r r h e a a r e s s ib le V itin g b lo
po o ın o d o r b lo o d in
bo w e l m o v e m e n ts can be ı
ife th r e a te n in
g W ith d r a w a l s y ind r o m es a re v a r ia b le d e p e n d in g
th e a
on
g e n t b u t c a n b e life th r e a te n in g

@ 1 T A C C P H s I
T he re
p e a te d d m in is tr a tio
a n o f d ru gs t s h o r t in te r v a ls
a
ta c c p h la x is t
y o The Ephedń p r o d u c e s le s s e ffe c t is c a lle d
n e 50 ın i]lig r a m sh o w s e r e d u c in
ca n n o tb e a h
c ie v e g e a n d th e s a m e e « e c t
d by a d m in is tr a tio f th e
n o sa m e do se
T he cu rv e fo r th e a c tio n o f 5o m g an d 3o m f e p h e d r in
g o e a t e r e d to a p a tie n t

Scanned by CamScanner
Scanned by CamScanner
lı r? iA Te x tB o o k o fP ha rm a c o ı

Y J
°
L
d e ffe c t Th e regu la r in ta k e o f a lc o h ls
th e re q u ir e o o p iu m
p r o d u ce
m lp h ilıe
R E s u LT H H !
p sB=ss
d to d r u g M ū iid y w o n t
ce an d fa ile d to re sp o n co n cen tr a tio n s w h ic h o c c u rs
a
th e d ru g p n se n a re o r d in a r il R E s u LT : Th e bo dy ca n t
y

'
its e w Oerheaı
ing ls a rls k

IA ) Iio a = (B ) nrstdg
ıx p o s u Ħ
(c ) (D ) S'"nddrug
in th e
H e u t ıa le d ro p s le a v g =
.. .
BX po su c

参粼磉 移
«s io f [u i$ In ia c d o n s ris e s A Ll e e
to m u s c le s
L v nu a ' " '
ı ho b
M e s s age s
K wm h d « ū a
o b
ūı an« w
tm o w w e lt
. , le g s c a n
. ..

ff e c t f dru g dep en den ce


sh o w th e e o
F ig 1 1 o A d ia g r a m s

= 班◆◆' " U" " P'" , d '" " q u lr e d . " " lhu n d. D o i w ith p e a te d u s e
re o f h e r o in depen d en c e a ls o o ccu rs It d ev e lo p s w h e n th e n eu ro n s a d a p t to

a lly in th re se n ce f th e d r u g W n e n
o
d o n ly ń in c tio n n o rm e p
r e p e a te d d r u g
y o su re a n
l ig L 9 F u dam th e e x p
n en ta l c o n c ep t fT le r a n ū Th c a n b e m ild (e g fo r
o o ce
d r u g is ith ? aw n se v era l p h y s io lo g ie re a c o n s o ccu r e se
th e w
W M the d r u life th r e a te n in g (e g fo r a lc o h o l) T h is is ı
m o w n a s th e w ith d r a w a l
c a ffe in e ) o r
n
g is d ix on tin u e d th e to le r a n
ev en
ce u su a lly d is a d th e b iu th
pp e a rs a ft e r a tim e The d ro m e In th e case o f h e r o in w ith d r a w a l can b e v e r y s e r io u s a n a u s er w u se e
s )m
la đo r ie s he n in ha le
w
v a po u rs o 山u g a g a in to a v o id th e w ith d r a w a l\ d ro m e
f G iy c e r l tr ir i
y ıtr a te ca u se ħe a d a c h e The w o r ke rs f d s y m p to d is p la y e d M o s t a g e n ts c a u s e h a n g e in th e le v e l o f c o n s c io u s n e s s
he a d a o T he s ig n s a n m s a c
w tm ū ey
a c tiv ity c a n b e s o s e v e r e th a t th e
ar e a w a fr o m th e fa t S u p p r e s s io n o f b
y u su a lly a d e c r e a s e in r e s p o n s iv e n e s s r a in
c or
y fo r a lo n g
p e r io d f tim
o th
e e a c
q u ir e d p e rso n m a y s to p b r e a th in g w h ic h can c a u s e d e a th

A 1te tiv e ı
y th e u s e r m a y b e a
m a
g ita te d an gry an x io u s an d u n ab ı
e to s le e p Hallutions
are poss1e A bn o rm alv ita l s ig n s (te m p e r a h u e p u ls e ra te re s p ir a to r y ra te b lo o d p r e s s u r e )
a re po s s ib le a n d can b e life th r e a te n in g
c h e s t p a jn iß p o s s ib le d Ca' b e c au se d Heat' . IUg d a ń a fro g iiuse
ge
A b d o m in a l a in itin g a n d d ia r r h e a a r e
p n a u se a v o m
p o s s ib le v itin g b lo d b lo d in
wof th
bk o ın
p p in g the o o r o
bo w e lm o v em en ts b e life th r e a te n in
e d ru
g ca n re sl it
can
g w ith d r a w a l s y in d r o m es are v a r ia b le d e p e n d in g
n "
peciı
ic o n th e a
w ith d r a w l ge n t b u t c a n b e life th r e a te n in
g

m TACCPHYEB
T he rep e a te d d m in is tr a tio
a n o f dr u gs t s h o r t in te r v a ls
p r o d u c e s le s s e ffe c t is c a lle d
a
ta c c p h la x is t
y o T h e E p h e d r in e 5 0 m illig r a m sh o w s cu rv e re d u c in g c u r v e a n d th e s a ın
ca n n o t b e a c h ie v d e e ffe c t
e b y a d m in is tr a tio n f th e
o sam e do se
The cu r v e fo th e
r a c tio n o f 5o m d 3o
sho w s
g an m g o f e p h e d r in e d m in is te r e d to
lik e th is T h a
a p a tie n t
e sa m e e ffe c t b y a d m in is te r in
g sam e d o se o f5o m g o r 3o m g o f e p h e d r iï ıe

ą £Ê

Scanned by CamScanner
i

=
P

rm lA Te x t B . o k o f P h' " . ' "


W íy d
d 羹

22

o b ta in
ffe c t M g h e r d o s e o f e h e d r i
æ be o b b in e
d To sam e e
p n e is re
q u ir e d to
a im o t o f e p h e d ń n e b y m o u th is 15 ' h
u s u a la d u lt d o s e
a dm in is te re d . T h e
g to 6 0
K h ild r .
. UP 秘
b e g iv e n thR e tim es d a ily
国 鑿
纛 -

园 。

ts t m d
dos e do s e

M e o d s o fa d m n is h a tim
i ıd r u g s a n d fa c to r s w h ic h m o d w th e ir d o s e o u r a tte
n tio n
w o u ld b e d im t e d b e c h a n is m f d r u g s a c tio n b y k e e in
n ı o
p g in m in d th e c o n tr a in d ic a tiċ
m s
an d s id e e fte c ls o f d \

□ Į D IO S Y N C
D h ıg idio s yn a a sy i m t r n w a r d r e a c tio n s to d r u g s th a t o c c u r in a s m a ll f
r a c tio n
o f J» tie n b a n d ha T e n o o b v io u s r e la
p to d o s e
tio n s M or d u r a tio n o f th e r a
p y T h e liv e r is a

qumtgetfmbńđ
y T ħe iä o s JT ıe r e s in d u c e ĵ
y 国
n m an y w a
y su c h a s 至
Æ

b ES O F ı
DıO SY N ER ES Y
th e t y p e o f a ll e r g y 践

ı
sh o w

ł
F ig 1 1 2 A d ia g r a m s

ı ł ıin
ı es (itr tic a r ia ) a r e
f th e b o d y It c a n b
s k in re a c

d by
tio n s th a t a pp e ar a s

lle r g ic r e a c ū
itc h y sw

su ch a s
e u in g s a n d
to a fo o d o
can

r m e
o ccu r o n

d ic a tio n
an y p ar t
b u t th e y

罗 蒙 蕪 纏 \
o e cau se an a o n

a ls o m ay o ccu r in n on a lle r g ic p e o p le T y p ic a l M v e sym p to m s are R a is e d re d w e lts an d

\
In te n se itc M n g

。 A tta g ic iĝ cz a n a It is an a lle r g ic r a sh th a t is u su a lly n o t c a u s e d b y s k ĵ n c o n ta c t w ith a n


a lle r g e n an d fe a h ır e s th e fo llo
in g sy m to Itc h in g r e d n e s s a n d o r dryiess o f th e s k in
fL1linduclion o f id io s J
w p m s
m m as
y t li r a s h o n th e fa c e e s e c ia ll c h ild r e n r a sh a ro u n d th e e y e s in th e e lb o w c r e a s e s a n d b e h in d
p y
th e k n e e s e s e c ia ll in a d lt
p y u s

A ı
ıe lg ic s ho c k (a n a p h y la x is o r an a p h y la c ū c sho ck ) T h is is a life th r e a te n in g r e a c tio n th a t
can a ffe c t a ber
n um of o r g a n s a t th e sam e tim e It ty p ic a lly o c cu rs w h e n th e a lle r g e n is e a te n
'"

X =
"
" da n d (fo r exam
p le fo o d s ) o r in je c te d (fo r
p le a b e e s tin g ) A lle r g ic s h o c k is c a u s e d b i d ĵ la te d
" ex am
m " " d a lle rg e n an d ıe a ky b lo o d v e s s e ls w h ic h re su lt in a d r o p in b lo o d p r e s s u r e s o m e o r a ll o f th e fo llo w in
g
T sym
p to m s m a y o c c u H iv d d is h d is c o lo ūon f th e
r s k in N a sal co n g e s tio n S w e 】
e s o r re ra o Ľn g
o f th e th r o a t t
s om a ch p a in n a u se a v o m itin g s h o r tn e s s o f b r e a th h e e z in g a n d lo w b lo o d
, w
p re s su r e o r sh o c k

Scanned by CamScanner
攤 明

聲 = 醒盛 翩 然弊 鱸 韉 。 酢 \ i蠲 "

Ė
IM IA Te x tB o o k o fP ha r
回国团团声 ņ a c o
M
le rg ic c ım jM c tip it is ) is in fla n ru n a tio n o f th e t is s u e la e r s
A ı te ıg ic e y es f;B ı
ll a n d th e u n d e r s u r fa c e o f th e
y 二二
(m e rr ıb r a r
o f th e e y e b a
ı" / th
c o v e r th e s u r fa c e y lid T h e in fla m at

n,ct'Ts
m a
i ti n a n d fe a tu r e s R e d d e r th e lid s
a lle r g c n e
e a c o s s u n
a r e s u lt o f a n
r
a n d ,
d w e llin g o f th e m e m b r a n e s Y e D v
erl
W a te ry itc h y e y e s a n s o

i f d r u g a lle ıg F D r u g h y p e r s e n s itiv ity r e s u lts fr o m i


M e c ha n s m o n te r a c tio

l ie a g e n t a n d th e h u m a n im m u n e s y s te m
p h a rm a c o o g
T hese t es o f r
yp
n s be t

e a c tio n s
w ee
n a
co n st
o fa 】 1 a d v u s e d r u g r e a c ū o n s A U e r g ic r e a c t io n s t
ih r t
b
ll
X
on yl a s m a s u s e t o m e d ic a tio e
n s re r
? g h w w w itiv ity r e a c b o n s m e d ia te d b y l e b r u n p es
a specific g u n

== = °ĥ ,

T h e n ıo s t im p a r la n t d r u g r e la te d r is k fa c to r s fo r d r u g h y p e r s e n s itiv i ty c o n c e r n
th e c h e
m jc a l
l l i h t o f th e d r u g
p r o p e r tie s a n d m o e c u a r w e g L a r g e r d r u s w ith
g g r e a te r s tr u c h ir
al
c o m p le x ity (e g n o n h u m a n p r o te in s ) a r e m o r e Ľ k e l t b i
y o e m m u n o g e n ic H e te r o lo
a n tis e r a s tre p to 】dn as e a n d a r e e x a m p le s o f c o m
go u s
p le x a n tig e n s c a p a b le o f e lic i
tin
h yp e r s e n s itiv ity r e a c tio n s M o s t d r u g s ħa v e a s m a lle r m o le c tıla r g
w e ig h t (le s s th
a n l0 00
d a lto n s ) b u t n a y s till b e c o m e im m u n o e n ic b
g y c o u p lin g w ith c a r r ie r p r o te in s s u
ch as
a lb u m in to fo r m s im
p le c h e m i c a 1 e r c o m p le x e s (h a p te n )
D iģ tr ib tio n
=Rex"ipb A b
' . " u ņ
« . ' " gra m o f'" r m ' " n '' "
F ig ' ' " y s t, "

O N
ı
L i4 1 A BS O R PT
th ite f
fi d
A b s o rp tio n is d e n e
as th e pro c e ss o f m o v em en t o f m c h an g e d 山 u g fr o m e s o

ic c ir c u la tio Th o f d Ju g fr o m its s it e o f
d m in is tr a tio n to th e s y s te m n e p a ssa ge
a
its tr y in to b lo o d s tr e a m is c a lle d d r u g a b s o r p tio n T h e ab so r pū on o f a
a d m in is tr a tio n to en

o f a d m in is tr a tio n s ite to a b s o r p tio n in b lo o d s tr e a m


d r u g r ėfe rs to its e n tr y fr o m th e ro u te

a n d p a s sa g e o f d r u g a c r o s s ce ll m em bran es T h is p a ssa g e is r e s tr ic te d b y th e lip id s b a r r ie r

)
t a t th e p e r m e a b le m em bran e
p re sen
T h e p r o c e s s o f a b s o r p tio n m a y b e s im p le d iffu s io n Th e d r u g s lik e u re a a lc o hol e a s ily

ab s o r b e d b y s im p le d iffu s io n

th e c e ll m e m b r a n e is a lip id b ila y e r s o th e lip id s o lu b le d r u g s d iffu s e q u ic k ly th a n w a te r


s o lu b le d r u g s T h e c e ll m e ın b r a n e is m o r e e r m e a b le to n o n io n is e d d r u s in c o m
p g p a r is o n t o
io n is e d w a te r s o lu b le d Ju s
g
th dru g
e m a y be a b s o rb e d b y a c tiv e tr a n s p o r t p ro c e ss th e io n s w h ic h a re tr a n s p o r te d by
th is a c tiv e tr a n + +
sp o rt p ro c e ss a re a am K o N r in a c id s
o r g a n ic a c id s a n d b a s e s w e a k
e le c tr o ly te s in io n is e d fo r m T h e d r u g s lik e p )x im id in e s g lu c o s e a r e tr a n s p o r te d b y th is


P r o c e s s T h is p r o c e s s is m o r e r a id th a n s im le d ifħr s io n
p p
P in o c to s is i
y s th e
p r o c e s s o f a b s o r p tio n in u n ic e llu la r o r g a n is m s lik e a m o e b a T h e c e ll in th is
P r o c e s s ta k e s u flu id fr o its s u r r o u n d in g s
p m
The m a o r
j r o u te s o f d r u g a d m in is tr a tio n in c lu d e a ) o r a l (e n te r a ı・ o r v ia th e in te s tin e
b ) P a r e n te )
r a ı(o th e r th
a n th e in te s tin e ) s u c h a s in tr a m u s c u la r (i m ) o r s u b c u ta n e o u s (s c )

Scanned by CamScanner





娟鞯

囊囊 弊

贓覊
-


廿
礬霾

M e m b ra n e T ra n s p o rt

を 参
p a s s iv e A c tiv e v la m a in ly b y
T P r i v e r n tr a n s p o r t er s

(P U m p s )
: > 4 7 =

S im p le Fa c ita te d

Ī
d iffu s io n v
ţ p r im a ry S e c o n d a ry

v ia v a r io u s v ia ı
o n
ĺ tra n s p o r te rs chnne\s

4 The a b
so
q tio n o f the d r
u g thr o u g h su b lin g u a l r o u te
w h ic h is H o fm o u th c a v
or o ity is
sm au in te s tiI ı
h
e ı an t n
s to ı
a ch n e b rg e r th e
/ 11 F ig 1 1 6 M o de o f tr a n s p o r te r
s u r fa c e a r e f a b s o r b in
a o
ill b e

5
A c id ic
g m o re w
dr u
gs a re P a s s iv e m e m b r a n e tr a n s o r t In h d le c u le u s u a lly p e n e tr a te s b y
ra p id l
p p a s s iv e tr a n s p o r t t e r u g m o
d iffu s io q a lo n l d b ila y e r S u c h
g a c o n c e n tr a tio n g r a d ie n t b y v ir tu e o f its s o lu b ility in th e ip i
' " n " " t, i
x - al a

in
d m in is tr a tio
s m a ll in t
e s tin e s
n w h e r e a s E h e d r in
th is c a u s e s th
p e
tr a n s fe r is d

m em bra n
ir e c tly r o o r tio n a l to th e m a n itu d e o f th e c o n c e n tr a tio n g r a d ie n t a c r o s s th e
p p g
e d e la e
y in

F!' 囌 辦 驪 瓏 。 覇 项 戳 部 鲻 襯 飘 驢

Scanned by CamScanner
'" " " ・

:
bl ro ce ss b y h ic h a ce ll d ir e c ts th e
y to s is is th e d u r a e p
w
F i 1 17 T n n m t n fd m p m n lp m lp ç h r v = r in u # n " p R
liz e d b y th e ce ll E x oc
an d in te m a
d v e s ic le s
ll b T h ese m bran e y b o 1Jn
f th e em
f s e c r e ta r y v e s ic le s o u t o e ce m e m r a n
c o n te n ts o
e ll a s m e ın b r a n e
b t d t th e e x tr a c e llu la r e n v ir o n ın en t as w
c o n ta in s o lu
b le p r o te in s to e s e c r e e o

f th e c e 】 1m bran e
d lip id s th a t a r e s e n t to b e c o m e c o m p o n e n ts o
em
p r o te in s a n


LA B ı
1 1 4 3 B IO A V A ı TY
i i t tio
f d r u g th a t is a b s o r b e d fr o m its s ite o f a d m n s r a
n
D e fin itio n : T h e F r a c tio n o f a do se o
il
th e s y s te m ic c ir c u la tio n is c a lle d b io a v a a
b ilit y
an d re a c h e s in an u n ch a n g e d fo r m
la tio n s ab ility to
Th e p e r c e n ta g e f th e d r u g a b s o r b e d is
o a m e a su re m en t o f th e d r u g fo rm u

d e liv e r th e d ru g to th e ta r g e t s ite
A d by f tw c r ite r ia e iM e r 1l e a r e a u n der
m ou n t a b s o r b e d is c o n v e n tio n a lly m e a su r e on e o o

th e tim e
p la s m a co n c e n tr a tio n c u rv e (A u c ) o r th e t o ta l (
cu m u la tiv e t am o u n t o f dru g
U iv e r s ity
e x c r e te d in th e u r in e fo llo w in g d r u g a d m in is tr a tio n a c c o r d in g to th e B o s to n n

Sc h o o l o f M d e r th e an d do se
e d ic in e A lin e a r r e la tio n s h ip e x is ts b e tw een a re a u n c u rv e

w h e n th e fr a c tio n f d
o ru g a b s o rb e d is in d e p e n den t o f do se an d e lim in a tio n r a te (h a lf-M e )
a n d v o lu
m e o f d is tr ib u tio n a re in d e p e n d e n t o fdo se a n d d o s a g e fo rm

Scanned by CamScanner
ı Ţ B o o k o f pharma lo g y a c o lo g w

Geneø
cihı
c o

T o c ı* v ıł
w
【 a
M TC Ż
ď d ie n A U c
» * u
ı a

r S u b ħ ııa p e u ū c ı
eve ı

! mr ı a ıl n
B ) '


E u m ïn tï o n p h a
ģ a s e

O « T
m T im e
1 1 8 B io m ū a b iliı
r

A lin Ĥ y af ū e n la tio n s h ip b e tw ee n a rea u n d e r th e cu rv e a n d do se


m m ay o c c u r il fa r
e x am p h Ĥ e a bw lia ı S is a s a tu r a b le on e o r & d r u g fa ils to h th e s y s te m i du h y d r o ly s is h y ? a tio n c o n ju g a tio n
re ac
liz e d b y id a tio tio
m e ta b o
c o x n re c n
be
1aıiımbecansea{ g b in d in g o f d r u g in th e in te s tin e o r b io tr a s fo tio n in th e liv d r u gs c a n
e g o a l is to m a k e th e d r u g e a s ie r to
e rm a
er is o m e r iz a tio n w h a te v er th e p ro ce ss th
a tio n or
du ? g ū e \ ]u o u g h th e p o r ta l s y s te m
fin s t b a ıßit ı co n den s

e x c r e te
U 4A D ISTR IB U TIO N M a n y d r u g s m e ta b o lis m o c c u r s in 2 p h a s e s 1t in v o lv e s c o n u j g a tio n w ith
JT M c tio n
p lm se
D is b ib u ū o n in r o ł b s ta n c e (e g 9 lu c u r o n ic a c id s u lfa te , 8 ly c in e ) th e s e re ac tio m a re \ th e tic
v es a re v e n ible tra n s fe r
o f a d r u g b e tw
e e n c o m p a r tm e n ts It is d e fin e d a s a n e n d o ge n
Du s su
e ibı
e transfer o f d r u lite s fo r m e d in s y n th e tic r e a c tio n s a r e m o r e p o la r a n d th u s m o re re a d ily e x c r e te d by
g b e tw e m o n e c o m p a r tm e n t to a n o th e r T h e b lo o d to ta l
te v m
M e ta b o
w a le e x b a c e llu 】 lym p h a ū c a n d c e r e b r o s in a l flu id
bciy u r in e ) a n d th e liv (in b ile ) th a n th o s e fo r m d in th e tic r e a c tio n s
th e k id n e y s (in
u er e n o n s yn
p s a r e in v o lv e d in th e m o v e m e n t ò f
dr u g ı a
h ro u g h d ıe b o d D e e n ä
y p n g u
p o n its c h m c a l a n d p h y s ic a l p r o p e r tie s th e d r u m a
h e b o u n d to g y
P p r o te in s o r d is s o lv e d in b o d fa t d e la in
a c tio n m e ta b o li
y y g its p r o g r e s s to its s ite o f
s m o r e x a e tio n

1t is a P o ces s w h
e n th e d ru
g js a b s o r b e d in th e b o d it is d 沁出 b t F u n c tio n g ro u p
d ĺ lu id s T he y u e d to v a r io u s b o d
y tis s u e s
ar
d\ w hic h a ss
p e a s ily th r o u h c e ll
a n d d ru g m e m b r a n e s a c h ie v e w id
g s w hid ı d o n o t a e d is tr ib u tio n
p s s e n o u g h c e ll m e m b du
r a n e h a s lim ite d d i
s tr ib u tio n T he d ru g
fr ee d r u
g r ro v ı
o e
g ro u p
E Je d m ja a Ic * cu h tin u
h a se of r
p gg n a n t w o m en d r u g e n tr in to f t
fe ◆ c ir n il o y blo o d p ta c e t y e a l b lo o d c ir c u la tio n is
a ti n alb an ie r T his b a rr i
e r e x is ts b e tw

簌認隹颀 二
e e n m a te r n a l a n d
.。
' " ,。 。 , ,囀 h p i, 。。。 。 '" i' " - 。 。
O u t

drug ırp jà s o lu bıe F IB 1 1 9 A s y s te m a tic d ia B r a m o fm e ta boı


is ï n f d ru g
n te r s th e o
er al nep
oug s
ys Ł
em th r o ugh 11 1 d l
ra in b a r r ie r

Scanned by CamScanner
ı
'

re @ j a te x tb o o k o fp h 靈
ıÆ .

ic d e dĵ d e n c y n dr u g H e i u T n "
i" d r u g m e ta b o°lis m d r u g m e ta b o lis in
g e i u l m te s c- a n b e
in h e

ŞŞ
ge n e t
m e w
th In r a b b it a tr o p in e is m e ta b o lis d ritn A
e ta b is m is d i e
o】
fĺ ıe n t h species e đu e to
Dm g m

H u n u n s a re a c ok f th is e r n m ıe s o a tr o p in e is to
x ic to
o f enzmealropinase 爨
n o n ro ×fc
协 la bb 让
Đ t rı
ľ 鑾
R UG S
£1 4 6 EX C R M O N O F D n o jjJ
n Į9
re m o v e d fr o m th e b o d y b y e x c r e tio n "
= c
a bo
o r lh e ir m e ı
i*e is

Dm g a

m e la b o 】
ite s a i e im v e rs ib le tr a n s fe r r e d fr o m iś 騵
w h e e by d r u gs
or

W d r u g is b k e n i e in g e s te d it is a bso rbe d a n d 韶
em ū o n m e n Ł n en
a

f th e b o d y It is th e n e x c r e te d fte r
e s E u id s a n d o rg a n s a a
tis s ı
ı

fa d r u g d e a s dm
iı tio n o f a c ū o n Th tio n o f
E x a e tio n o

o x id q M e dr u g m a y b e e «a e te
e a se s

d in a n a c tiv
a

e o r in
e ex a e

a c tiv e fo rm Th th e a p p a r e tV fo f th to t a l

ı e
io n in c re a s e s n m ax r a b io tr a n s fo rm a tio n re a c tio n b e c a u se o e
/m th o d s ittd u c t
cc re te d fro m b o dy h th e fo llo w in g w a ys e d in th e r e a c tio n in in th
a
e in v o lv e c re a se s T h is ca n ı
e a d to in c re a se s o r d ea e a se s e
en zy
m
Jß i o r f h e m ic a ls d e p e n d in g
E Ja J e tio m d u o ılg h 】
dd n e ys a ! biogical e ffe c ts o c u po n w h e th er th e p aren t ch e m ic a l o r th e

s Jjro d tiv e e n tity
T he di u gs e te d du g h kid n e y s b y c jn lite is th e a c
m e ta b
are e m o u o

i m o f en z ym e in d u c t io n A d 】u g s m e ta b o lic c le a r a n c e in & e ffic a c y


echa n s
Ał can cre a se

f 2 n d d r u g in d u c e s th e e m y m e r e s o o lis m
de cre a se s i ib le fo th e ic tim 山u g m ta b
a
p n s r v s e

th is m a y c o m p r o m is e th e e ffe c tiv e n e s s o r s a fe ty o f th e d Ju & o th e r s th e F D A


Sin c e g
d r u g in te r a c tio n T h e p h e n o m e n o n o f in c r e a s e d d r u
re c o g n iz e
s
g m e t a b o lis m a b ili ty o f th e
by se v e r a l d r u g s a n d c h e m ic a ıs is c a lle d a n e m
e n z ym e s y m e in d u c tio n A n u ï n b e r o f d r u g s
can cau se an in cre a se in liv e r e n z y m e a c tiv it o v e r tim T h is in in « e a s e th e
y e an

m e ta b o lic r a te o
f th e e o r o th e r 山u
sam
g s P h e n o b a r b ito n e in d u c e d th e m e ta b o lis m its e lf

- G e n e tr a n s c r ip tio n )

M e c ha n ı
s m o fE n z ym e ı
n d u c t io n

F ig 1 2 0 B a s ic m e ch a n is m o f e n z ym e in d u c tiIn n

En z y m e In h ib i« o n E n z y m e in h ib iū o n r e fe r s to a d e c r e a s e in e n z
en z m y m e r e la te d p r o c e s s e s
y e P r o d u c tio n o r e m y m e a c tiv it A n u m b e r o f c lin ic a ll i
be tw e e y y m p o r ta n t in te r a c tio n s
n dru s
g r e s u lt fr o m c Y p 4 5o in h ib itio n c Y p 4 5 o in h ib ito r s a r e ? f
se le c ti e r e n t in th e ir
v it to
y w a r d e n z y m e s a n d a r e c la s s ifie d b th e ir m e c h a n is
:ro J J n g lo q y m s o f a c tio n so m e dru s are
P O te n t c o m g
rr
ys n 9 n ï lJ p e titiv e in h ib ito r s a n d c o m e te fo r th e a c tiv e s ite b u t th e a r
the e p y e n o t a s u b s tr a t f
e o r
nz m
y e (e g , u in id in e a n d c Y p 2D 6
q ) w h ile o th e r d r u g s a r e n o n c o m p e titiv e in h ib it
o rs

Scanned by CamScanner
İ İ

rP

p re se n Ł :
İ rjjı【
n i sr I n h ib ito r
C b H p e titiï e In M b itio n ta tio n o fu n co m p e titiv e
se n
B
F ig 1 2 2 A re p re

th tß L ĵs 】
u ge r An d
tq ;G 9 To ł
s c c e T ıĦ h ı
S
R
VERY S HO RT A N SW E q u

d ph arm a co dyn a Jm ic s o f
ith p h a co k in e tic s an
lo g y is th e s c ie n ce w h ic h d e a ls w a rm
p h a rm a co
im ls
d ru gs on hu m an bo dy o r o n a n a

lie d fie ld s
ı o fPh a rm aco lo g y ?
Q 2 w n a t a re th e a
de fie ld s h as (1 ) P h a rm a c y (2 ) P h a r m a c o g n o s y (3 )
s c ie n c e a ls o in c lu s su c
p h a rm a c o lo gy
M g h ly s p e c ia liz e d ū e ld a n d m a k e s its
A n s
b d iv is io has a
g y E a c h o f th e s e
n s
l (4 ) p o s o lo su
»ıto x ic o o gy f
th e w o r ld e s p e c ia u y to th e p e r s o n s o
.
f d r u g s to
p o s ite k n o w le g e
d o
đi R i b i l t i o n to a co m
V
go ry T h e k n o w le d g e o f P h a r m a c o lo g ie p r in c ip le s
M e d ic a l p a r a m e d ic a l an d N u r s in g fie ld c a te

l h e a lth f th e h u ity d im a ls
is e s s e n tia l fo r th e m a in te n a n c e o f o p tim a o m a n an an

bs ı iĺ o ĺ s r lT
A T h e d r u g s m a y b e d e ń v e d fr o m P la n ts (v e g e ta b le ) k in g d o m a n im a ls m in era ls sw th e s is a n d
n e
m a rl fr o m m ic r o o r g a n is m s T h e d r u g s m o s tly w e r e d e r iv e d fr o m r o o ts le a v e s an d b ark o f p la n ts
N o n co m
p e titiv e In h ib itio n IT
ß 9ı T h e a lk a lo id s g ly c o s id e s o ils (F ix e d a n d v o la tile o ils ) r e s in s g u m s T a n n in s an d an tib io tic s m e

蔗 荔む立发 で三苡立よ丁九に竺 一
!
一 。


Í切 八 A n s A n tib io tic s a r e th e s u b t
s a n ce s
p ro d u ce d by or d e r iv e d fr o m liv in g
J rtjj j e ith e r to k ill b a c te ń a o r
o r g a n is m s T hey a re e d
p rev t m u lti lic a tio n
in '
T P e n ic iı
lin w h ic h is
en
p o f d is e a se c a u s in
g orgms The ex m p le is
s a co m
p le x o rga n ic a c id o b ta in d fr o p en
e m ic illiu m n o ta tu m o r p en id Jlim

Scanned by CamScanner
PHA

N G TH E C H A pTER
DUC ı
N TR O
ı

iia m ıa c \ ・

e c h a n is m s o
i l e s an d m fdru g a c ū o rt

e to tr s in te r a c tio n s
D r u g re c p
eories
R e c e pto
r

aūo n o f r e c e p to ıs
d as d ic

Slgnaı
uction ın e c h

a ū o n o f r e c ë p to r s
i eg u 】
l

iproteiïcoupled r e c e p to r s

lo n e l r e c e p to r

T ra ts m e m b ra n e em ym e lin k e d r e c e p to r s

m b r a n e JA K S T A T b in d w

R ec e p to r an d re c e p to r s th a t r e g u la te tr a n s a ip tio n fa c to r s
D o se r e s p o n s e r e la tio n s h ip

t h e ra p e u tic in d e x

C o m b is e d e ffe c ts o fd r u gs

F a c to r s in o d ifyin g d Ħ ıg a c tio n

A d v e r se d r u g r e a c tio n s

D r u g in te ra c tio n s (p h m a co k in e tic an d pham aco


ı d y n a m ic )

Dugdiscovery
Pı1ed in ic a l e v a lu a đo n p h a s e

C Un ica l e v a lm d o n o f n e w d ru g s
D m g d ls c o v e r y p lıa s e
a in lc a l tr la l h a s e
p
%P a ï m a ç o v l lla n c e
g

西日

Scanned by CamScanner
;h A į ąv ・
p e r a tu
cha n g
iıı
lebody
e
te m re

ĺj eJ
O

吕n ßd ) ŕ
w h a t th e b o d y d o
to d r u g
e s W
G
n a
e n e raıP h a r m
t th e d r u g d
a c o
«»e s
lo g y 4 ı
to b o d y 攤
ĥ I / m i1

kn l yeiı (ı)P h y s ı o ıo g ıc a l fa c to r s la e a n d
g re n a ı fu n c o n )

(ıı) P a th o ıo gı c a ıfa c to r s «e
g K ıdney ı ıv ・ a n d m e ta b o ı
ıc d ı
s o r d ・r *
P o s s ib ı ( ) e n e tı
lıı G c v a rı a n ts
)
e d ru r e Ja Jn þ
g te d m z z Ða a
(ıv ) D r u g r u g In te r a c tı
o n s
r s łfd o ıq (v ) D e v e ıo p m e n t o f re s ı ıta n c e o r t o ı
e ra n c e

F ig 2 1 A s y s te m tic c o
a r r e la tio f ph am
n o a co k in e tic s an d ph dyn
a rm a co am ic s

L ł
u r,iĦęsi
g liz e d b o d y c e lls I
n j D o a m in hen
p e w d m in is te r e d
!b ów !Ēte r a b le r is e in b l a to a p a tie n t it b ń
o o d


p r e ssu re
n gs



Scanned by CamScanner

B i88F r z o n e ) o f the an d o f g a s tr ic m u co sa

X
E 4 =tpł
* ct m en Ł1 ħe d r u g s n ıa y b e ııç p d
a s a ıe
p la c e m e n t w h e n ^ '

W
su bs ta ııo e is fo u nd d e ó c ie n t ū ıth e b o d
y T h e ııs e o f s u b c u ta n e o
in s ı】
in fo r ä a b e ? Ħ tie n ls sm u s is a n a
a r ty w e a ls o
g iv e h o r n ıo n e s to a ti lo n
or
p m ts

? 2 1 M E C H A N Is M
OF D RUG
į X
AcnoN

e qpıd n n g b o ū f a d ia m d
d t u p is d
o an
dresponse r e la tio n s h ip T ħe h a n is m
a s s ió e d o n th e b a s is m ec
f
o f p r o p e r tie s
(a ) an d c h e m ic a l r o
p w r tie s o fd ru g s
(b) bi o l o g i c a l
The ofdm
g m ay b e p r in
d
m y a c tio n a n d s e c o n d a ı a c t i? T h e p r im a r a c tio n
m g s is th e p ffp r t o f y y f th e
tmdged d r u g in th e b o d
y a n d th e s e c o n d a ıy a c tio n o f th e d r u
o

g w he n
ađ o n h ū e b o dy

fn
w ĥ ic h (z ıı
s e s c e ll d
讌囊 C u b id o p a ıe v o d o p a
th d 】
$M e t h a
ea an
y s is 7 ħe exa m p Je js o f s ilv itr a te , d ds,
no l
er n sh o n g a ti m in e

R e v e r s ib le an tic h o lin e s tr a s e s e g ,
N eo s tig nn in e, p h yso s g
声 o d lrc e lo c a l
jn o a m ıï ı
a tio n a re ca JJe d n z y ın e

3)
as co u n te r ir r ita n ts Jb r exa m p le ib le u n til th e n e w e
m is ir r e v e rs
titiv e r e s p o n s e
k iu N o n C o m \ titio e ı
n h ib itio n m p p le
e n o n co m e
m it r o o r In d Fo ŕ exam
E x am g a n is m . . n p e

e B o r ic s
titiv in h ib itio n a re
li 画画画画画
ac tio n a re ca lle d as d is in fe c ta n ts bı
genJimted M e e ffe c ts o fn o n co m p e e

Scanned by CamScanner
sı =
= so j r81b . R Bg , k o f P
h

In erm db le a n ti c h o lin e s h a s e s e g , O i g a n 叩 h o s p h a te co m
p o u n ds
q c lo m q ge n a s e In hib to rs
i e g A s p ir ir Ļ In d o m e th a d n

M A O i b ıs e g,】
p r o n ja z id P h e n e lz in e

F to to n P In h ib ito rs e g O m e p r a z o le Eso m e p r a z o le

» F a ' " C O ıy
In d u ce d F it T h e o r y h e n it is
r o n ly w
fr o m a re c e p to
a n a te s
a re sp o n se e m
i id e a th a t
T h e o ıy It s
an
fdru g
o cc u p a tio n l to th e am o t ın t o
tio n a
o n se th a t is p ro p o r
ltin g in a b io lo g ic a l r e s p
th e m re s u
a c tiv a te
b,r o f'' " p m ' ' " p ie d
" n u m

X-caef '" a l '"


f' ' " . D ir - tly p r . p o ,

R D R - E
D +

liz e h o w tw o dr u gs can o ccu p y th e


th e y do t r a tio n a
p ie d
n o
ll th e r e c e p to rs a re o c c u
w hen a

d a n cy th e o ry
th a t is b a o n o ccu p
o p e r a tio n a l M o d e ıA m o d ifie d , Semimpirical a p p r o a c h se

d re sp o n s e
te fa c to r r e la tin g a g o n is t re c e p to r co m p le x an
m o d ilie d to in c o r p o r a
a
b a s is o f th e k in e tic s o f
d e l It w a s d e v e lo p e d o n th e
Th e kusl«te (m u ltis ta te ) r e c e p to r m o lts o f d ir e c t
r e ta tio n o f th e r e s u
l t ń c in h ib itio n a s w e ll a s th r o u g h n e r p
i t
c o m p e titiv e a n d a l o s e fa
ce o r ab se n c e o
a r d le s s o f th e p r e s e n
b in d in g e x p e r in n e n ts It p o s tu la te s th a t a r e c e p to r r e g
i r o n ) a n d T (T e n s e
n a c tiv e o r o ff)
i
li吕a n d , e x is ts in tw o d is tin c t s ta te s th e R (r e la x e d a c t v e o
l l l l c e p tu a l m o d e l
s ta te s w h ic h a r e in e q u ilib r iu m w
ith e a c h o th e r T h e r e is a m o e c u a r e v e c o n

th e fa c t th a t m a n y r e c e p to r s a r e n o t ju s t s im p le
o f R e c e p to r T h e s e m o d e ls e m p a s z e
h i

Scanned by CamScanner
ı
E GÏ IA Te "
H o fPh
52 1

p le x m u Jti u n it S c h ır e s b e in g
p to rs h a e p o sed
v co m co m
o f
O tħer ıe « m o re
i t ti e x is t b e tw
pro ditalory a n d in h ib ito ry n e r a c o n s
ı th e s e s u b u n i
ee n
ts a n d
in te ra tio n F e w r e c e p to r s a r e n o t o n l d
y y a m ic in te r m s o f
tħe d tu 吕apfur c n
th
m o b iı
jn th e m e m b r a n e lik e a n ic e b e r8 in th e o c e a n
b u t a ls o e

R an d R a r e ï n e q u iı
・ ib tiu m (e gu ilib r iu m c o n s ta n t L ), w h ic h defines th e b a s l
a a c tiv i
ly o f
9 n is ts b in d o n Jy to R a n d P a r tia ıa g o n is ts b jn d p r e ı

r e c ep to r Th e F u u a o ėr e r ıtia lj
y t o
ń ıu in v e ıs e b in d o n ly to R a n d P a r tia l in v e ıs e a g o n is ts b in d r e fe
p r e n tia ll t
y o R
q J a u in itie s fo r b o th R a n d R (iıo e M e c t o n b a s a l a c tiv ity )

a n tıg o n si ts l m v e e u a
D D

L

:- -x
ın d

_ ı
n

du e ch a n is m
F ig 1 2 T ra n s ce r m

th e la r g e s t fa m ily o
f m e m b r a n e p r o te in s
td to r s (G p c R ß) G pC R s a re
G p r o te in c o łtp ı re c e p
itte r s , a s w e ll a s b e n g
i
P ır u" h o rm n d n e m o tr a n s m
a l c ha n
ge r a r tia lr e sp o n s e
a n d m e d ia te m o s
t ce llu la r re sp o n se s to o n es a

t b a s ic Ie v e l, a ll G P C R s are
is io n lfa c tio an d ta s te A t th e m o s
m r e s p °n s ib le fo r v o n
one
ts s e p a r a te d b y
,
or t h e lic a l s e g m en
b y th e presence o f s e v e n membranpanning
w a
herat c h a r a c te riz e d
o f m a cr o
n is t o r a n ta g o
is t b in d s to th e
ntracellular a n d e x tr a c e llu la ŕ lo o p r e g io n s If a g o
m o le a ıla r n
p e r tu r b a tio n js p o s s jb Je a sped Jic alternating
chan co n fo r ın a tio n
it th e r e c e p to r a n d G p r o te in to ge
G p r o te in co u p le d r e c e p to r ca u se s

Scanned by CamScanner
'






:

Scanned by CamScanner
,

p o lm ıtia ı n e a r tħe ha
c n n e l T ħe m e m b ra n e te n t ia l a Jt
p o
e rs th e co n f' " ' "" o f th e
tH po n s e Io c h a n in th e
g æ m em ı
m n e o te n tia 】 b u t th e
p
y can a ls o ń u tc

ty f o s ln e In p r o t e in s

Fi 2 7 F . . I k d T lin tn

匡 T a n s ın e m b r a n e ]_ S T A T b in d in
g T h e ty T o s in e k in a s e a c tiv ity o f JA K is a c tiv a te d w h e n

歹 th e r e g u la to r y m o le c u le b in d s

R e c e p to r d im e r iz a tio n b r in
a n d b r in
g s tw o r e c e p to r m o le c u le s to g e th e r to fo r m a d im e r
g s t h e tw o JA R s in t o c lo s e
p r o x im ity w h e re th e y c a n
P h o s p h o r y lq te e a c h o th e r P h o s p h o r la tio n
y fu r th e r a c tiv a te s JA K
a u o w in
p h o s p h o r y la te th e r e c e p to r g it t o
T h e p h o s p h o t r o s in e r e id
y s u e s o n th e r e c e
p to r p r o te in s a r e b in d in
S T A T s ta n d s fo r S i g s ite s fo r s T A T
g n a l T r a n s d u c e r a n d A c tiv a to r f
o T r a n s c ń tio n T h e S T
c o n s id e r e d la te n t t
r a n s c r i tio n
p A T p r o te in s a r e
p fa c to r s L a te n t
m e a n s th a t th e
c y to p la s m a n d w a itin y a r e a lw a y ś p r e s e n t in th e
g to b e a c tiv a te d b y JA K w h
e n s T A T b in d
it in to a o s itjo n s to th e r e c e
P w h e r e it c a n b p to r th a t b r in
e
phosphoat d by A K o n ce h
p o s p h o r y la te d tw o £
H & z 6A n u c le u s
sn te r n a ū c d ia w h e r e it b in d s
g ra m o fn ı
o v em m t o f io n To s p e c ific s e
s an d th e ir e ffe c t
P h o s p h a ta s e s qu e n ce s in th e D N A In
e ac tiv a tio
p h o s p h a te g r o u s fr o
re m o v e
p m v a r io u s
n o ccu rs w h en
p r o te in s in th e s ig n a lin g p a th w a y

Scanned by CamScanner
■匡
rm lA Te x t B o o k o F P h a r m a c o lo
gy Iv o li Pharmacoıo f 59
ı
G e n e ra

c y to M n ı ・

" - ı国

5 S T A T D RM E R
STAT d r fo tm i

S T A T D IM E R

F ig 2 9 N u c le a r r e c e p to r

n u c le a r r e c e p to r L ip o p h ilic b s ta n h a s s te r o id h o rm o n es
V ańo u s dru g a c ts th r o u gh su ces su c

d iffu s e th r o u g h th e c e ll m e m b r a n e a n r s in
d in te r a c t w ith rec ep to
an d th y r o id h o r m o n e s c a n
l T h h t l e x t h e n a l te r s g e n e tr a n s c r ip tio n
th e c y to p la s m
o r n u c eu s e o r m o n e r e c e p o r c o m p
/ i f ff t t i R N A T h h to r c o m p le x in te r a c ts
c a u s in g th e s y
n t h e s s o e e c o r s p r o e n s m e o r m o n e r e c e p
d im e r ic )
d c d ia p fT m b ıa w ith D N A
in p a ir s th e s e m a y b e id e n tic a l (h o m o d im e r ic ) o r n o n id e n tic a l (h e te r o
Ħņ U S J« e m a am o m m drm ıłe ıe « e p to r ņ ıo a ln e k in a ae a c tiv lly o F JA K

p a ir s

O th e r m em ber r e c e p tı
m h tęg ritu is o bı
ig a te h e te r o d im e rs m e a n s th e y ha v e tw o su bu n its @ o s E ? S P O N S E R E L A T IO N S 匢 ı
a (a lp h a ) and P (b e la ) Ih te g rin s Jn m am m a ls hav e tw e n ty to u r a an d n in e P su bu n its
d d r u g c o n c e n tr a tio n a r e th e e ffe c t o f a d r u g is
7 ħe R e la tio n s h ip b e tw e e n d r u g r e sp o n s e a n
In tq g liru ar e b a n sm e m bï a n e r e c e p to r s th a t Ta c iJlta te ceJlxtraceJIular m a tr ix (E C M )
d e p e n d e n t o n th e c o n c e n tr a tio n o f th e d r u g a t th e ta r g e t s ite (r e c e p to r ) w h e r e d r u g r e c e p to r
U P o n lig a n d b in d in & in te g r iru a c tiv a te a fg rıa l tr a n s d u c tio n p a th w a y s th a t m e d ia te
b in d in g is jn e q u ilib r iu m 7 e d r u g c o n ce n tr a tio n s in tu m d e p e n d o n p h a r m a c o k in e tic a n d
æ u u la r a ĺ a b s u c lr a s ï eg u la tio n o f th e c e u c y c le a n o qg a n iz a tio n o f th e in tr a c e Jlu la r
,
d o s in g fa c to r s G e n e r a lly th e in te n s iv o f re sp o n se in cre a se s w ith d r u g c o n c e n tr a tio n s T h e
c ypo a ıe le to n d f th e lt bra n
an m o v em e n t o n ew r e c e p to r s to ce m em e H p re se n ce o f
e
ı
y ie ld in g a h yp e r b o lic c u r v e th a t
,
res p o n se can b e p lo tte d a g a in s t d r u g c o n c e n tr a tio n ,
in te g riru a lı
o w a r a p id a n d fı
e db ı e r e s p o n s e s to e v m ts a t th e c e ı
ıs u r fa c e (e g s ig n a l p ıa te le ts
illu s tr a te s a s h a rpin c r e m en t in e ffe c t th a t d im in is h e s to w a rd a p la te a u (m a x im a l e ffe c t)
to in itia te an in te r a c tio n w i c o a gu 】a tim fa c to r s )
w h ile d r u g co n c e n tr a tio n in c re a s e s

T he ra n ge o fd o ses o v er a lin e a r r e la tio n s h ip b e tw een do se a n d re sp o n se is g e n e r a te d W n en


N u d t a r r ¢c tp to r T h e Ii id m ı u bı
e d r u g s d i f th r o u g h c e ı ım e m b r a n e s a n d b in d e ith e r in
p d o s e s (x a x is ) a r e c o n v e r te d fr o m tic to ]o g a r ith m ic s c a le , th e p lo tte d ı
a r ith m e o g d o se
th e c e lıuı a r c y to s o J o r in th e n u c Ja ıs G m e e x r e s s io n i
p s a lte r e d a n d p r o te in s y n th e s is ĵ s re s p o n s e c u r v e w ill c h a n g e to a ßig m o id äl c u r v e T h e im p o r ta n t lin ear s o pe (
l 2 5 7 5 % o f th e
e ithe r im r e a a e d o r d e cr e a
a e d , w H c h c a u s e s th e c e u u Ja r r e s o n s e T h is m e c h a n is m Js th e m a x im u m )b e c o m r th e r c h a r a c te r iz a tio
e s v is ib le fo r ń ı
p n
a b w e s Ļ a n d e ffe c ts c a
n u s u a JJy b e m e a s u r e d in te r m s o f h o u r e r a th e r th a n m in u te s o r
s e c

Scanned by CamScanner
貫鯊 夕 髦籲轟

B
a c 0 lg æa

h a rm
r ıa tB o o k o f m . ' "
M ūņı e n e


Te x 0 gy G

. ı i hı
c h ıb e
ïı
ED Ľ d o s e w w
th e n n e a r p o r tio m o f th e c u r v d o s e s lo w e

ı i
m e a lo n g r
concentrations l\e r a p e u tic w h ile to x ic e ffe c ts a r e lik e ly to
T he a p e u t"
rear l d d o se )c a n b e s

l
u b
f
4
f c t) T h e d a la p lo tte d in a r itł m i e tic s
th e m a x im a e e c a le
d o s e s fn e a r
o c cu r ń th h ig h r

c u r v e in s te a
&
p m d u ce s
ı ħıi c n in d ic a to r o f p o te n c y e s p e c ia lly
h a l f r e sp o n s e a s a u se ħd
£c j io e c t i v e
w h e n compatg
d o se a t
d iH e r e n t a fo r th e s a m e r e c e p to r
T h e s iın ila r r e la t io n s h ip can be ĝ
d tħe ń m c t io n o f ? e d o se o f d r u g a
d m in is te r e d a n d r e fi
n r e d to a s
doserespom
p lo tte a s d m in is ūe r e d a n d p a s
l m a d r u g c o n c e n tr a tio n s r e m a in in
ū rg tħa t ? e d o s e s a
c u rv e a ss u m

equ ib r iu
iı n _

,
M ED M TD (m o r e th a n th ı s w \\ıp r o d u c e

g n s o f to x ı
s ı c lly )
A ls o c a \ı e d h ig h e s t n o n t o x lc
d o s e (H N T D )
三 t
贸 f a d i u g a s d e te m n in e d b y q u a n ta l d o s e r e s p o n s e c u r v e s \h e
然 r e s e n ts th e s a fe ty o
m e g ıa p h r p
e
自 F i吕ユ 1 1 r o v id e s a t h e r a p e u tic e ffe c t (e g v a s o d il a tin n ) in 5 0 % o f p a ū e n ts th e T D s o
h e d o s e th a t p
富 & » w
h ic h is t
ic e ffe t* in 5 0 % n f p a tie n ts (e g a r th y tlu i a ) a n d th e L D s n W h ic h is 1h e
d s e p r o d u c in g a to x
穿 w h ic h 沁
出 e o

in 5 0 % n f p a tie n ts
le th a ıd o s e

P E UT ı C IN D E X
2 5 1 TH ER A
i f L D to E D 5 0 T h e ra tio o f L D 1 a n d E D 9 9 w ill g iv e b e tt e r in d e x sa fe ty o f th e
It is th e r a t o o 5 0
f h f d u ir e d to a tta in
d r u g 1ħe th e r a p e u tic in d e x s a m e a n s o c o m p a r n g t e a m o u n t o a r u g e q
\ i i r

Ħ& 2 1o A w te x o a ä c e lq g coa ıce nba tio nit ect c u r v e illu s tr a tin g its fo u r c h a r a c te ń s tic i h f
th e th e r a p e u tic le v e l in 5 0 % o p a t e n ts to t e a m o u n t th a t is le th a l to 5 0 % o p a e n ts
f ū I t is
ia M æ
r aı M e ¢f& d iı m n u n n d as a fm d io n o f in c r e a s in g d r u g concentration s ru r o u n d in g th e ta ıg e t e x r e s s e d a s th e r a tio
L D 5 o / E D 5o A h ig h th e r a p e u tic in d e x is p r e fe r a b le a s th e m a r g in o f
p
n c e p to r in fa r e d Ĥ P d ra g rn n rm h a tin m
s a fe ty b e tw th e d o s e th a t w o u ld b e su tftc ie n t to a c h ie v e th e tic le v e ls a n ıa t w h ic h
d tł
een ra p eu

w ou ld p r o d u ce to x ic e ffe c ts is h ig h
W p o lt m r a n d e ffic a c p R e s p o n se s to d r u g s m a y b e g r a d e d (r e s p o n s e m a g n itu d e is M dı
a n le th a l d o
@ w
p r p p o « tio n a ıto d o s e ) o r q u a n ta l (T W is ll o r
e s e
n se a n on e) C o m p a r is o n s b e tw een d r u gs a re T h e ra p e u c ı
tı n de x

u su a lly m a ? b a s e d o n ille m e d ia n M dı v e do
ffe c tı
e fk c tiv e d o s e th a t
e a n e s e
p ro d u ces a re sp o n s e in 5 0 % o f
p a tie n ts ? e ED bn L D so
P o te n c y r eı to ? e
o r
e rs am o u n to fdru s r e q u ir e d to p r o d u c e a n e ffe c t o f a g iv e n in te n s ity It is E D so
con V e n im t to ae t in ten s ity l
rra u e a t the E C Į o w h ic h is th e m e d ia n e ffe c tiv e c o n c e n tr a tio h
Cilat onesponds to 50 % f
To w e r tħ e concentration
o th e m a x in ı a l r e sp o ı
n e e d e d to r e a c h E c
rs e T h e h i h e r th e
g p o te n ¢ o f a d r u g th e @ C O M B IN E D E F F E C T S O F D R U
į o o fte n p o te n c y a n d to x ic it a r e lin k e d b e c a u s e Syn
th e fo x ic n e o ıu e j
w
y u g le m It c o m es fr o m th e G k o rd s y n e r g o s m e a n in g w o r k in
s a n e x te ıu ï
o n o f th e th e r a e u tic
p e ffe c t th e r e fo r e a m o r e th e in te r a c tio
re e w
g to g e th e r It r e fe r s to
n o t n e c e ss a r il
y a b e tte r d r u & p o te n t d r u g is n b e tw een tw o o r m o re d r u g s S y n e r g is m r e fe r s to th e e ffe c t c a u s e d w h e n
e x p o s u r e to
tw o o r m o re d ru gs a t a s tim e r e s u lts in h e a lth e ffe c ts th a t a r e r e a te r th a n th e g
su m o f th e e ff
e c ts o f th e in d iv id u a l d r u
g
T he r e a re e x a
m p le s in c lu d s

Scanned by CamScanner
习 四国
m a c o
lm 」 =
rm l x t lm a o T ľ h a r rń a ç o ı w
e d
A Te o p
W I)

s y n e r g is m It is th e sition w h ere th e

th l a lc o h o l) a l e in
d iv id u a lly to x ic to th e liv
d a n d e th a n o l (E y
te b a c N o r i e
gr bu t le s s to x ic th a n th e in d iv id u a l e ffe c ts fo r
)C m bo n
w y th a n th e s u n ıo
f th e ir in d iv id u a l e ffe c ts
m u ch m o r e l iv e r in i on th e
to N er ?q p u c e

m an y an tid o te s fo r p o is o n in g s Fo r ex am p le
can a n ta go n iz e th e to x ic e ffe c ts o f m e th y l a lc o h o l (m e th a n o l) b y

anagesic fp a in re lie v er】an d o iv e h y p


th e r s e d a ı n o tic d r u gs
:
: ;
d ts P ,
, fr o -

taı
ronism
' " ? ym
It is b
' '

a se
"

d
'

o n
' " S th ' ' " h.
th e p h y s ic a l p r o p e r ty o f d r u g s
o l

Fo r ex am p le ch ar co a l
be a d d itiv e an d su p r a a d itiv e
m e g g is m
m eı c an
lo id s an d c än p r e v eń t th e ir a b s o rp tio n It is u se d fo r ch a rco a lp o is in g
ila r e c h a n is m g iv to g e th e r Th e y t ıa

d r u g s w ith s im m s a re en
y p ic a ll rbs a
M diM pc w ħe n M o adso
ffe c t o f d r u g B F o y
J
fdru g A
d itir e e ffe c ts o f d r u g A + đ p le
o + e r ex am
p ıo d u æ a d is m It o c c u r s w h e n a d r u g r e d u c e s th e tr a tio n f n is t b y
A lg e s ic e M x t l m t« g o n
co n cm o an a go
ı A sp ń ı+ p a m c E ta m o 】
n a ic *
m ¢
o ı
A tih yp e r te n s iv a che
m ic a l c o m p le x a n d b e c o m e in a c tiv e p r o d u c t Fo r e x am p le
o d jp - e + A te n o lo ı
n e
Z m fo M g
A th e tic id ie e lk a lo id s It is u se d fo g a s tr ic la v g e in p o is o n in g
3 M il ic o x id ¢+ ï ła ï o lh p n e
v n es a r a
0 + o x
1 10 1N
A 1k a lo id s It is in so ı
u b le a lk a lo id is fo rm e d
+
2 T a Jm in s
{ M ta l C
A d d iti a M b c t (1 ◆1 2)
g e n ts + e o m p le x
c h e la th ıg
a
3
Ąıp k in ◆ pa « * ba m a t

t a g o n ia m hen dru g
A B A ◆ B acokinetic an o ccu rs w o n e a c c e le r a te s th e m e ta boı
ite

n n 1 \
/ U l ta o n is m in v o lv e s d r u g a c tiv a tio n f tw
? fe r m t r e c e p to r s o r b y d iffe r e n t
r h y a io lo g ic a a n 8 o o

a t e x is t to m a in ta in h o m e o s ta s is F o r
, \ , h
m ec h a n is m s t p le (1 ) th e e ffe c t o f n o r e p in e p h r in e
e x am

to in c r e a se b lo o d p r e s s u r e (v ia s tim u la tio n o f a a d r e n e r g ic r e c e to r s ) c a n b e a n ta
S tłlM U ïo
p g o n iz e d b y
r xazo ı
e ◆ M m e th o p r ï m
in is tr a tio n f a c e ty lc h o lin e w h ic h c a u s e s v a s o d ila ū o n b
a dm o
y th e r e le a s e o f n itr ic o x id e fr o m
th e v a s c u la r (a r te r io la r ) d o th e liu (2 ) G 1u d in lin b lo g a r le v e l (3 )
en m ca d
!= = iw go n an su o n o su

1 H is ta m ĵ n e an d a d r e n a lin e on b ro n c h ia l a s th m a
'
一 R e c e p to r A n is m
ta 8 o A n ta g o n is ts in te r fe r e th e ir e ffe c ts b b in d in
n
y g to th e r e c e p to r s th e y

/ L
S u p ra « d d ı
,
L ta r g e t a t v a r io u s p o s s ib le lo c a tio n s S o m e a n ta g o n is ts ta r g e t th e s a m e b in d in g s ite a s th e
r e c e p to r a o n is t w h ile s o m e b in d t
g
in te r a c t a t u n i u e b in d in
q
o a llo s te r ic s ite s o n r e c e to r s
p A n ta g o n is ts m a y a ls o
g s ite s n o t n o r m a lly in v o lv e d in th e r e g u la tio n o f a r e c e to r s
tM e e fFe c t (1 ◆l 4 ) p
a c tiv ity T h e b in d in
g o f a r e c e p to r a n ta g o n is t to th e r e c e p to r it t a r g e ts m a b e e r m a n e n t O r
y p
te m p o r a r y d e e n d in
p g o n th e n a h ır e o f th e b o n d fo r m e d T h e a n ta g o n is m is s e c ific e
a n tic h o lin e r ic is d
p g an
Į n o tb
g e c r e a s e d th e s a s m
p o f in te s tin e in d u c e d b
y M s ta m in e o r 5 H T w h ic h a c t th r o u h th ? f
g e
y c h o lin e r ic a o n is ts b u t m a
g g
e r e n t s e ts o f r e c e to r s S u c h a n ta o n is t
p g
y
m ay be co m
p e titiv e a n d n o n c o m e titiv e p

Scanned by CamScanner
咪珲皿 ヤ 6S 四国回国园ı国国
田。 o ı
G ď回
回P 쌘
m o re
i b a r r ie r ) t
hm a re
b a r r ie r s a r e n o t ħr lly d p e d (B B B b lo o d b r a n
e v e lo
T h e ir
B) 1 p a r ts o f th e b o d y a r e a ffe c te d b y th e d r g
u
itiv e to c N
s s tim u la n ts A 】
sen s

is in c re a se d
k id n e y s u se
h e n ic o l m a y c a
H p e a tic m e ta b o liz in g cap a c ity is a ls o u n d er dev p e d c h lo r a m p
e lo
h b d y s u r fa c e a re a
b yn ? o m e Th e do se m ay be m d ifie d u s in g e ith e r t e o
y ba y
s o
e
P gï
V :, w e ig h t

to b e p r e s c r ib e d f a c e a re a (m 2 )x a d u lt d o se
D o se
1 7

D o se to b e p r e s c r ib e d W t in k g × A D

TO
B o dy s u r fa c e a r e a in m 2 o f c h ild
' ' " N f' " " ° ' " m C h ild d o se x A D
rw - W
1 7 (a v e ra ge b o dy s u r fa c e a r e a in A D )


t th e b in d in g s ite th e
I t is reversbly b in d to rece p to r s a sa m e a s
\ tifm e
t a c tiv a tin g th e to r C o 呷 e titiv e a
q ta g o n is ķ in d iv id ls q u ir e la r g e d o d r u g in c o m p a ń t o fe m a le s w h ic h re q u ir e
o r a g o n is t w ith o u re c ep M a le u a re se o r so n
d o ge n o u s lig a n d 2 Sex d
en
n is ts fo r th e s a m e
b in d in g s ite o n th e r e c e p to r n ile b o W
\ ġ i to e Į , Ļ T e s to s te r o n e in c r e a s e s th e r a te o f b io tr a n s fo r m a tio n o f drug D e c re a s e
c o m p e te w ith a g o le s s d o s e
i t i b lo c k e d a g o n is t b in d in g iĮodß lstrf£ lis m o f so m e d r u g s in fe m a le (D ia z e p a m ) o c c u r s F e m a le s a r e m o re su sce p tib le to
t m e ta b o
i t i o n s s
re c e p to r a o o m p e
t v e a n a g
ie d r u g s (e s tr o g e n in h ib its c h o lin e e s te r a s e ) D r u g s u s e d fo r u lc e r m a y ca u se 一
a llo s te r ic s ite o r a iş ite İ g ţ b e r
ıd s to th e r e c e p to r it ta r g e ts a a n
l b ħ t a u to n o
m


N o n o e a n İ ag o n is k t
i b i d s to T h is typ e o f b in d in g is n o n c o m p e tit v e b e u ş ę h e
i in cre a s e d p r o la c tin
th a n th e a c tiv e s ite a n a g o n s t n
th e
o t h a v e to c o m p e te w ith a g o n is ts o r
f b in d in g A n n c qp ?ę
g W enstruation lic y la te s ld b id e d y 一
d sh o u y m a
r e c e p to r a n ta g o n is t d o e s ı ı ,
e
D u r in g sa an s tr o n g p u r g a tiv e s e av o as

i
a n ta g o n s t p r o d u c e s i rs b y in d u c in g a c o n fo r m a tio n c h a n g e in th e receRtg£中 in a easeb le e d in g S o m e d r u g s w h e n a d m in is te r e d to p r e an t w o m en m a y ca u s e h arm
ħJ1

c h a n g e s th e s h a p e o f lĵhe a c tiv e b in d in g s i r e v e n tin g a g o n is ts fr o m b in d in g fte r c r o s s in g p la c e n ta l b a r r ie r m a y c a u s e fo e ta l a b n o r m a lit y ln p r e g n a n c y


Ĵ o l 3ĵ 9 119 e ffe c t to fo e h ıs a

g n İ v ło į Į o ì fo llo w in g a r e to b e c o n s id e r e d (a ) C a r d ia c o u tp u t (2 ) G F R a n d r e n a l e lim in a ū o n o f d r u g s (3 )
CTORS M O D IF Y IN G D R U G A C T
H u Į o s r [T 71 e v o lu m e o f d is tr ib u tio n (4 ) M e ta b o lic r a te o f s o m e d Ju g s L ip o p h ilic d r u g s c r o s s p la c e n ta ı
V a ria tio n in re s p o n s e to th e s a m e d o s e o f a d r u
g b e tw e e n d iffe r e n t p a tie n ts a n d e ý e n ù d ĵ e b a r r ie r & a r e s lo w ly e x c r e te d D u r in g p r e g n a n c y u te r in e s tim u la n ts s tr o n g p u r g a tiv e s a n d
sa m e p a tie n t o n d iM er e n t o c c a s io n s w ill o c c tır T h e r a n g e o f v a r ia b ility m a y b e llm k gd io r d r u g s lik e ly to h a v e te r a to g e n ic e ffe c ts s h o u ld b e a v o id e d e s p e c ia lly d u r in g th e fir s t
lim ite d d e p e n d in o n th e h a m a c o k in e ti & p h tr im e s te r n o d r u g s h o u ld b e g iv e n le s s a b s o lu
g p c a r m a c o d n a m ic c h a r a c te r is tic s o ń jEh e d r u
y b g u n te ly n e ce ssa r y
n e fo llo w
ı in g a r e the fa c to r s H ch d ify th e d o s a g e
w m o o f dr u gs M e d e ta ils a re a s u n d er 3 B o dy w e iB h t T he do f th e d r u g is u s u a lly r e la te d to b o d y w e ig h t A p e r s o n o f o v e r
se o
1 A æ In fa n ķ d d \ild r m
an r e q u ir e le s s d o s e i e D iffe r e n t d o s e fr o m a d u lts In iņ fa đ a n d w e ig h t (O b e s e in d iv id u a l) r e q u ir e s a la r g e d o s e th a n th e n o r m a l in d iv id u a l If th e d r u g is fa t
c h ild r e n th e m e ta b o lis in g
W es an d th e e x c r e to r y p ro ce ss is n o t ń d ly devlQp ę d s o lu b le th e n s o m e p o r tio n o f a d o s e is a c c u m u la te d in b o d y fa t s o th e la r g e d o s e is r e q u ir e d
W o ld a ge
p a ăe n ķ ) r e q u ir e r e d u c e d d o s e b e c a u s e ö (n a ţ g a ħs b r fa tty in d iv id u a ls T h e d o s e o f th e d r u g is u s u a lly e x p r e s s e d a s m g p e r k g o f b o d y w e ig h t
h )ip o fu n c tio n d u e to o ld
a g e e f[e c t T h e a d l
u t d o s e is fo r A perso n
o f a g e T ħe tis s u e s f
p e o p le b e tw e e n 1 8 a n d 6 0 W a r s w ith u n der w e ig h t r e q u ir e s a sm a lle r d o se
o a n in fa n t &
c h ild a r e M h ly s e n s itiv e to a la r e n u m b e r o f d r u s
C h ild r e n lın d e r 12 ı g g g 4 R o u te f a d m in is tr a tio
y s r e qu ir e a fr a c tio n o f a d u ı
o n T h e d r u g s w h e n a d m in is te r e d b y in tr a v e n o u s o r in tr a m u s c u l a r
t d o se b e c a u s e
r o u te r e

A ) D r u g m e ta b o h z in E p ÐT 'h】(.ť í q u ir e le s s d o in c o m p a r is o n to o r a l r o u te T h e d r u g s g iv e n b y IM /IV r o u te h a v e
g m ne
\ te m is h e ffid m t in th e m (G lu c u r o n id ti
se

m o n th s to d e v l a o n ) tä k e ș 3 q u ic k o n s e t a c tio (o r a l r o u te ) is d e la y e d d
e op) n The a c tio n by m ou th an s lo w T h e d r u g s g iv e n b y 团
re c ta l r o u t
リロ了 Į お」 ) り了 e a re a b s o rb e d s lo w ly an d on ly a p a r t o f th e d r u g is ab s o r b e d S o a la r g e d o s e is 目

Scanned by CamScanner
W

日 6 力召团团团团国国
lo U
ı王国e r a ï P h a r m a c o

t T h e
d itio f liv er an d k id n e y is v e r y im p o i t a n
g ic a l
o
p a th o lo co n n
g n į s ta tė A
p a b id la i y n
f liv e r th e a c tio n o f
f d r u g s so in case o f a n y d is e a se o


d e to ific a tio
Hi i ã& n ai n s ite fo r x n o
f k id n e y w h ic h is m a in o r gan o f
is a n y d y s ń in c tio n o
Ĵ b a d e cre a se d w n en th e re
tio n f 山 u g s In c a s e o f
s lo w
o
f e x cr e
th e tio n f th e d r u g is d e la y e d b e ca u se o
b s o r p tio n o f d r u g s
tio n a c o
e x cre d

眉 so m e c a u se th a t re su lt in d e cr e a s e a

b e c a u se o f in cr e a se d h a lf life
f th e tio o cc u rs


n
a tio n a c
lhwer d i s p r o lo g d r
o
(A ]í se a e s n u
d le a d in g to a d v e r s e
to lb u t a id is d e c re a s e
a r fa r in ın e
jßr]așpa p o t i b in d i g f r e n n o r w
be
is du d c le a r a n c e o f morp hine p r o p a n o lo l m a y
Jfflits If h e p tic b lo o d H o w
re ce
a
e ls f D ia


i le v z e p am
y le a d to to x c
o
l p n es m a
zobacted Im p a ir e d liv e r m ic r o so m a e n z

a n d th e o p h y u in e
9 ,P i c i n
d p la lb u in m a y b e a ffe c te d le a d in g to

0
T ħe p a tie n t tio a a ï n
' ' " ä ū." w ith d is tr e s s in (B ) In l D is e a s e G F R ta b u la r ń r n c n an sm
g sym p to m s n ee ds ' '"
re n a
ic illin
"
. l e ffe c ts f d ig o in lith iu m ge n ta m y c in an d p e n
. a bn o rm a o x

n hn (ĉ Ĺu ptriti o n p la s m a p ro te in b in d in g of d r u l
g s is r e d u c e d a o n g
w ith th e n u m b er o f
z A d d ic tio n g d ep e n d e n ce
D ru or a d d itio n is d p o r tio n o f fr e e b d d Jn g
a s ta te fp i d ic al le a d in g to in c re a se u n o u n e g
intôiation
o er o hro ic r o es an
or c n ic m so m e m ym
一 w H c h is detrimental th e p e r s o n an d s o c ie ty It b e c o m e s a lm o s t im p o s s ib le to İ Jß\ jfarin
X
c a rt rıo
fu n c ū ' ' " ' " y ou t
. . '
' ' " ".'"'' ' 10rroEı
wnı
nental d tim f d m in is tr a tio M ta b o lis m is lo w in h o t an d h u m id
" "
henoniëniodif an e o a n e

O id a t io f
c lim a tm H u rga tiv es a c t b e tte r in su n u n e r w h ile d iu re tic s a c t b e tt e r in w in t e r s x n o
rf 西 e짐과 了b
A ) E u p h o r ia s e n se o f h a p p in ıe is a n d fo rg e tń ıln d r u g s is lo w a t h ig h e r a ltitu des Th e tim e o f a d m in is tr a tio n is a ls o h ig h ly im p o r ta n t 】
n an
ess
J le
Y jq ın s
em p ty s to m ac h 山u g s a re m o re q u ic k ly a b so rbe d F o o d in th e s t o m a c h m a y a ffe c t
B ) T o le r a n ce d u e to in c re a se d
rro il q r o a d ß
pro d u c tio n f en zym
o es
\
【 91 Ji a s
a b s o r p tio n f th e d r u g T h e d iu r e tic s a r e a d m in is te r e d in th e
o moing an d n o t in th e ev en in g
C ) P sy cM c d e e n d e n c e H it r e q u ir e s th e u s e o f th e to ile t s e v e r a l tim e s fo r m ic h u itio So d u r in g ig h t th s le e p o f
as n n
( a b ih ia tio n ) e

h
p
p en . " " .. s b" " b. . " f dru g in d iv id u a l m a y b e d is tu r b e d H
" . . an
y p n o tic s (p r o d u c in s le e g p ) a c t b e tt e r w h e n a d m in is te r e d
D ) P h ys ia l d t mind lle r d o
qpe n d e n æ It is q u ir e d A m in
a
g ly c o s id e 1ĵ k e s tr e p to m y c in w h e n g iv e n
sm a se s a re re
a b e h a v io u ra l pattern o
f
ë9 v ī1ł
JSL
o co m
p u ls iv dru g b äř
e a ' '" a' '" ew ' ' " c u 1. . B l. c k .
Ge . ' " s n o t o b s e r v e d a ft e r in tr a m u s c u la r

(A bs tin e iu e
e itle s m ess
qm ū om e ) s
ym p to m s a pp e a r ı
ik e p s c h ic 1ļ ..iqıt F a c to r s P h a r m a c o g e n e tic s is th e s t d
u y o f th e r e la tio n s h ip b e t w
ı
e tc y cra v in g bo dy a ch e iH io iř a 1iä )ì fąg ţ q ţ fo ëm d d r u
een g e n e tic
g r e s p o n s e T h e g e n e tic a b n o r m a litie s in flu e n c e th
r e s p o n s e to d r u
e d o se o f a d ru g an d
g s It a ffe c ts th e d r u g r e s p o n s e in in d iv id u a ls a t 2 l

į ĮF
& s p ec ie
s an d R e v e ls
a ce c as t
i】A
or o
p tır g a tiv e is in e ffe c tiv e in c h in ese . . d il, tin
i s til Ĵ A P
( A t Įl- le v e l o f r e c e to r
ţ p s

l l i le v e l o f d r u g s m
'
(
e ta b o liz in g en z w e
ゴ a ß! l 汀 (ĥ a ) It h a s b e e n re p o r te d th a t d u e to g e n tic ń a tio
e v a n s th e d e fic ie
d e h y d ro ge n n c y o f g lu c o se 6 p h o s p h a te
g o 7 b y ıfÐb
) a se in c e r ta in ra ce s r e su lts in in cre a se d to x ic it
d ru g) y o f p r im a q u in e (a n tim a la r ia l
(g u l b
b)D u e to g e n tic
o J u Ja (cl e v a r ia tio n s in fe w in d iv id u a ls is o n ia z id (a n
ace ty la te d a n d in s a n ti tu b e rc u la r d r u g ) is fa s tl
b s Jó ly jÐĵ ï o m e
p e rso n s it is s lo w ly y
a ce ty la te d le a d in
l{þ g to m o re ch a n c e s o f d e fic ie n c
y

Scanned by CamScanner
rm a lA Te x t B o òk o fP ha rm a c o ı
ggy w ) 1

,
J ? e
t r jie r in g
fa c to rs in e
tv ith th e fu n c t io n s su c h as r a te o f p la s m a d ru
g
e n z ym e
Thu s 3u r

ill la te in th e bo dy if th e ÐFa te
cu m u f
y drug
w o
st an
ı
n so m e ge f d r u g s is
tie n
Æ m ai
n
th a n ra te o f e lim in a tio n ī ħe s lo w e x e ? a tio n o Prtiņaar
a b a is M g he r d se o f c h lo r o q u in e c a u
u d a tiv e M Jd d q Fo f exam p oe p ro lo n g e u wetinal
ia b Je fu c a u se c u m tie n t h a s r e c e iv e d ,į t Wthin
ı ho ld n o t b e g iv e n if th e p a
lıo a d in g d o se o f d ig o x in s u
d Fu ı
' b n ıc
æ
p a st n T

hm en a d r u g js a d m in is te r e d reg u la r ly to a p a tie n t to
g p e iio d it r a lo n
ı3 t o je r u ıc e
o s e P a tie n t d e v e lo p s to le r a n c e (a c o n
d d itio n o f ta ld n
b e c o m e s n « e s a ry to in c r e a s e th e g th e
itħo u t p m d u c in g s }m p tu m s o
f to x ic ity o f d r u g ) T o p r o d u c e th e s a m ë e ł ie ċ t In
e x c e ss d o ó e w
i d ī ħe to ı e r a n c e o f d r u g u s u a lly d is a p p e a r s o n w ith d Į ą J?(a l
tħe b o d y a ı a r g e d o se is r e q u r e o f

: th e W
R to tħe n o r m a J th a a p e u tic d o s e o f th e d r u g p r o d u c in g a le s s e r r e s p o n s e p n o m
e s is ta n ◆
t le r a n c e T h is is a c q u ir e d c h a r a c te r E x ' 呷 ł
th m p e u tk d m e js f o w n a s o
n
i ç l】?d e 中相
m o tp ħ
i itia u y r e s p o n s iv e if c o n tin u e d c h a n g e s o c c u r a t th e c e liu ia r a
in e th e p e rs o n is n n d

PırarmacoJcineticlev r e d u c in g th e a c tio n T h u s o n e h a s to jn c r e a s e th e d o s e o f Bm ş t u

o v er co m e
n iıa Ð# ņ
ic s d o
A lc o h o 】 n o t r e s p o n d to h yp n o tic s a n d analgesic th e d o se o f w h ic h h a s to b e in c re d
m an y fo ld s 】
n fa ¢ ı h e y n ıa y e v e n to le r a te to x ic le v e ls

C r ū s s T o ıĦa A p e s o n to la a n t to d r u g s re s e m b lin g ĵ n c h e m ic a l s tr u c tu r e is k n o w n as
c r o s s to le r a n c e M o s e d r u g s ıe s e m b lin che m
g in ic a l s tr u c tu r e s s h o w c ro s s to le r a n ce If a
p a l o n js t o m w h in e ħe a ls o s h o w s to le r a n c e to p a th e d in (s y n th e tic 茹\ i
e ・ıv e ) M M ġ Ffa ll, D o se r e la te d C o m m o n R es ph a to r y B le e d in g w ith S e r o to n ĵn
andcod l
R e la ie ri to th e p h a rm a c o lo
g ie a c tio n o f dep r e s s io n w ith w a r ff in s p ? o m e w ith
◆ Ľd u K e a ıa z e an d İ lu th e dru g e x a g g e r a te d p h a r m a c o lo g ie o p io id s S S R Js
pam re z ep a m H ţ ç ņ m p le te
a Ds s E o c cu Is w ith th e dru g s s h a ī in
rb ? e P ıe d ic ta b le L o w m o r ta lity D r
g th e sa m e p h a rm a c o lo g ic a l
p r o p e r tie s
y
X Į Jo m p k s include ba r b iM d ge n e ra l a iı
r a le s a n
e s th e tic s OUt!OWith P ic w lic a n tid e pressa n ts
le n nc e
s ite o f a c tio n is C N S
w iįķ tė
Wfdiciabt
c oss be
m ay o b se r v e d a lth o u h th
g ey a r e e Nonose reı
a te d n c omm o o I mm og i e
samephaı
macogitalproperties N i thh o d a
n t u n o l
m. . r + W l nd
l\ ' " a m l re】
a te d to th e re a c tio i ı
s a v o id in fııh u e


p h a rm lo g ie
aco an a p h yı a x is to
Ib íq s T 6 a c tio n o f th e d r u
8 p e n ic iĽ ĵ n
£o U ó T j a īn U n p r e d ic ta b le 1d io s w c ra tic

ï peated
!qmó xa H i gh mo r t al ity
r e a c t ion s
adminintitmĻ ū e s e s to re s a re ex h a u s te d jJłA. 9T m a ] i8n a n t
an d p h a rm a c o lo
g ic a l ac tio n is n dt :Þ
ń ej n ? h y p e r th e r ın ia w ith
ge n e r a l a n e s th e tic s
3r' c D a se r e la te d an d tim e re a l te d p ih ıita r
'""
Xh
ijß m Jn
(C h r o n ic ) U i\c o n
cu m u ı
a tiv e dase H
un on R e la te d to th e
y a d re n a1 a x is D o & r e la te d
yp o th a la 】n ic By an d Tiin e
-

o s te o n e c r o sis
o f ; (O u n n ic j
th e ja w w ith U n c o ın m on

Scanned by CamScanner
s ◆玎n a s e A

sgw dau opu au ı


o ïB
p e\
汹脳 曾 卜!

ヨ a Ju ? u adx a u o 怀)e a ı 阿 四 四 lo o a ıw m un u e 可 信(M 璃 羽W お 髫呷 a s 》邸 e 吖



【邬p
(s q eE po se a
W W e tu a p a o
Äd e ıa q ł jo u g u o jw aw a j u ? a ? ao u x e w p u e a lw w w ď Ħp tu e q
a u o qen
s?ndw Ãn e n m J a tm o J a ql q £ noı p le a a v \ ÃR e a S ıre q w q
ss?ï sl łe w J A JJ? u e
ł
tīa »o sĮ łJ?uaapĮ s u u a ła w p\ q ei ıo u ł ı= u ie p g a u a q »q p ı ł«a J g n a d e ıa q
p?m
Äıæ Ę » W a Ħs V rp ū »i ap s m
q ł ıa q ło ßr u p e Âq p a s n e ? p ?w a
papwł
şĮ rđ
ql u e

oq p a m Ätu o ın m m sta E # lu a a a s a n a ıa q L
ĺ ĄĘd æw ヨ呷 尹 日\ a a s īa A p e a q ła q o sa p

M ı
su o Į łJ e a H ı{łpWsuaaMH J ° a
01 aausĮ sa=

ol uĮ Bu m e J sa Ŋs J a n e s u ó ıg ! sa m ] np ų a u u a
ł a łeJ
Ĺ oå sw ł

nw re q
u ï au
P a łe Į p a

二二 二 裘 。 ぶし二 三了 コニ茗1一
q ıa A a M o H
aļe w a u i « u n u ıu pa w & Ħ H
p 他 叫

su o gJ e al
' 。 . ' 図 。
d o t o 1 s ıo J łu n o J ? e - "

二二
u a JJa d 一 Ãq p æ

j
沪 a 。 严
。。 Ã 。。 ・

i Ĥ 9 ! q a ru p ıE ıa w B n ıp ıu a q

. x
9w pu e Jaw e au q » ıa o s
u o p aeaJ
aae ıa Ja ı s P a JJa
łıs a m d d =
.
. s lĮ c c p ıı au p m ın o l
Ála s J a A u o J
p ie s s! łu a g=d e
c ou Ącı et ıo Jn n
= m cx q
e J a io ł ? q o 1 [ ų Łw
a\

J !x o 】£lıła (Z)
a
9
J sa p 61 n aa
sł JJa 01
1 !a e sa qp
u o g u a au ţu T ı Æ q e Jo s IJ
a u a a s ıa A p
Jo Ãn e
łıat lł
a ru p
& m J )o e ja u a
d ı u rw ı
aso p a ql a m eaa q
o l o Ðg t u ıe q i= o Ą ) A ó o lo a e u u
ı e q d Jo w o g łx a ı v

Tt Į O \

' "
罐 く


?

Scanned by CamScanner
靉 骥類 多 数鳥芦 荟 衾雩券" ".:寡
多 ,

戛 乙く ぢ
こ 帛

(v o wı lp h a rm a c o m
B k o f P ıa r m
a c o lo g y ĽG c n e ra
l A
l l ıa T f el
o o n o rm a
e ilt
o n ・ d ru g to e
f ch em ic a l r e lia n ce


l s ta te o
r e fe r s to a p h p ic a
■ .
& ・ a lw a ys

I o th e r
ic a lly a d d ic te d to it n
d ru g w ith o u t b e in g phys
be depen den t o n a
h im A p e rso n can
b t th is is
t a v a 山山 le
u
h e n h is d r u g is
n o
d e p re s s io n w
f lo ss o r ev en
a se n se o
m e n tá lid is tr e
ss

litie s o r o th e r
tio n s a b n o r ın a
c a u s in g m a lfo rm a
f d ru g s
T e iàtd ËĖn lc ity p a b ility
o
It is th e c a

ca u se o
f h a l t th e p re gn an c y
ht D a y be ą fe tu T ë r a to g e n s

:X
m s
to a r tu ic ia l h g
ru gs f th e e m bry° o r
lig h t o r e lo en t o
. k in re a c tio n e ith e r to s
u n
a gė h ť ih ä t c a n
d is tu r b th e d e v pm
th e
s te r o id a l a n ti 삐 \ 岭r y Th fo llo w in g d ru g ca u se
R e ce n tly n o n
ic a ls d dru gs e
ty p e s o f r e a c tio n sys!WėNd
s he a n
e d in th e s e A s b o th raaiť i? maternal in fe c tio n s c m
th a t c a n b e im p lic a ı s itiv ity
f p h o to se n
in ta b le
c o m m o n ca u se
o
d r u gs
b
h v e b e e n s h o w n to e a
a abńtirł
ility in fe tu s T hese a re g iv en

ch ro n ic a lly n o r rl
l in e 叩 le íi i
su ch rea c tio n s e s p e c ia l y p
i k f o c c u Jr e n c e
p o te n tia 】r s
ħ o
c o n s id e r a tio n ı e A b n o m a lity
d ia tio n D ru g
u u ltr a v io le t r a
e x p o se d ı
Iph oco m e lia m u ltip le d e te c ts
t t xi
P Thadomide
M e dï io n

G u p d d ru g
园四国园 la s tic d r u g s
en 上 :
1加国国目日目回 国回 国
1
蔭三 上
Fu m m id e
ca di as cu ır a d s
lıı
m

I
卜一 . ? 。。 。 紐 "

Thbzid ı
l ı m a ı
a n tib io t ic @ e w ę
s u tio n am *ı
e t + I ţ

c þro ñ o = c in e ı + 1 3 Į]
AÆ? gal G r is e o ! ı Į
ノ D M A RD ı I J + = = = a

T b p td e n
'
@ m ı L + I
I K e to p rd e 1 1
T a b Je Sh o w s th e P h o to to x ic d p h to a lle lg ic
an r e a c tio n
Rn s J u bn i
D ıu g D ep e n den d D
ce an ru g w iM dr a w a l r e a c tio n D ru g dep en den ce is c åh æ t%
ì
th e le a d in g c a u se o fhu o r ta lity a ll o v e r th o r ld
an M e s sh o w
m m e w o s t c a n c e r tis s u
i ñ u ìh k o fco m p le x ch ro m o so m a l ab e r r a tio n s Th in d u tio
e c n an d a ccu m u la tio n o f gen e ūc
a bo u t u s in
g ille g a l idr u ¢d &Ëà(ċ a n ca u se ge n o m ic in s ta b ility d it is k n
gs ï a s a c r u c ia l s te
p in th e g e n e r a tio n o f
an
or exam

e a d ia b e tic
ca n be c o m depen de n t
o w n
ı
n su ı
in W ith o u t tħis
dug tM
e
o n N ęJ w g ċaiJeeŕncogenicity
: s tu d ie s o f c a r c in o g e n ic p o te n tia l u s in g g e n o to x ic ity a s s a y s a r e o n th e
p e r so n
s w ou Jd d ie D r u
a b o n g de p e n d e n c e is differņt A n ïłiį ĺ Àlær e d g e n e e x p r e s s io n a b n o r m a l c e ll r o w
or \ a bu se a lth o u h
g p e o p le th , a n d d is r u tio n o f n
co m m o n ly u se a ll th r e e te rm g p o rm al c e ll c t i o n
s in te r c h n e a
q g þ jr l äy b ë l fel at ed wi th the g n o t ox i c ef fec t o dr
e f u g s.

Scanned by CamScanner

四 日团团 ■ ■際 四国 国

\ . ','
"
'

" lPharmacoıg
M a ı G e E

I: -
a .
P h a rm

H
a Te x t B
EiO lı
r= :
e @d r u g in t e r a c t io

d e cr e a s in g its e ffe c t c a u s in g a s id e
ļ n =

c tiv ity b y in c r e a s in g o r
d a ffe c ts its a
D d n ıg a n

t
J
d ic a l cond'""
d in'"actions d ru g m e
' " ' " ' " d r u g fo o

d in to ph a rm a co dp am ic o r 囊
ħJ r th b d iv id e
y b er su
In v iv o in te r a c tio n s m a e
is m s
m e ch a
n

d s y s te m ic d ru g :
b e tw a to p ic a l a n a
Co' - 0 n ı ― ―
I G a s b ith u p P
e
; ay oc cu r
b e tw e e n tw o d ru gs a i ll
p p lie d to p c a y
o r e en

..
a ls o o ccu r Th e
tic o s te r o id a n d a lo e
v e ra ) m a y
(fo p le to p ic a l co r
in te r a c tio n s r ex am
d is e a s e
tio n ca n o cc u rs a t a n y le v e l
d r u g in te r a c

į ° - p in ,

H y p o le s io n
ı

A n x ie y
cN s
efupnyumer'"ľ 1 2 0 a + a r b id o p a
Ł p s y c h o s is
¢ MeaylpıemOIOne

i
d n is o lo n e C o g n itiv e d ys fu n c tio n
¢ Ħ,mobaıbine p re

白 Ĥ
手 C y s titis
F ig 2 1 3 A d i u g in te r a c tio n a tv u io u s le v e l

e JJ S lls e ffe c ts
M y a lg ia

do lts in la r g e

襄薤蓑蓑
iiìt r e a §Ë in p h a r m a c o d y n a m ic e ffe c t (w h e r e a a ll in in

識 國
sm cre a se se resu a
A'"mja
s a6 s n ní in c r e a s e in p la s m a le v e l)
Bo n e m an ow su p p r e s s io n ;n o ìz a g T q u e
q
雞。 i ıig h İ ir s t a ss m e ta bo ı
p is m It is d u e to th e d r u g s a r e e x te n s iv e ly m e ta b o lis e d in th e liv er o r
H ie m o b ri i
I g a s tr o in te s tin a l tr a c t a n d a r e th e r e fo r e s e n s itiv e to th e e ffe c ts o f m e ta b o lic in h ib iū o n o r

o ilĵ u bn İ in d u c tio n

S i}ıg ı e c Jı It is iln te r a c tin g f d ru g


e m a n is m o f e lim in a tio n o can c a u se a s ig n ific a n t in cre a se in
) ßm a ó lq p la s m a co n cen tr a ū o n (e g Re n a l c le a r a n ce c y to c h r o m e m e ta b o lis m )

a b b a

Scanned by CamScanner
■ [M į lA T e x t B o o k o f P h a rm
a c o o g y (v
ı o ? G e n e ra
lP h a rm a c o a@
ı r II
?7 ı

bo iın d b y
be d d is tr ib u te d
a re a b s o r
h ic h d r u g s tic
ffe đ th e p ï c s b y k n o w n a s P ha
w m l
In l= a c ı
tio n s ııa t can a
d a ne æ d a re
b bo 】i z an e ¢

a s m a p r o u in
p】
an d sequestra m e

d r u g i r a e a đi
i
t o f a b s o rp t o
n ż h te o f
t n
e o r ex e
ra ı
ith e r th e
n
i v o lt e cha n g e s in e
A b s « p tio n

b e in fl. m ced by seco n d d r u g s th a t b 1ë It h °


rm

f a b s o r p tio n ca n
c id s b in d i
d r u g T h e e d e n to
a ]u m ir ū u m co n ta in in g a n ta
f th e
d ıd a te s (w ( h p ro d u c
t o
ħB uı
ł Ae com p le x e s o r th e p d y c o p r o te
in t e
n o ta b ly
o
s y s te m s
d ru g w w w

k l th a t _ t * in
. o fd rugg - e ra ' " lth "
X -

Jr li e y
j iJĵ ĥ v /
u n r h a ra đe r iw d

d ie n d r u g s a æ
s iv e ly
e x te ıı p r o te in
bo u n d .D ĝ
incrié
h
Th e
in na ia ni o cc u r
d a c tiv e fo r m T h is
n o n bo u n
-
ofa sm id c a n d is p b c e it to th e
a d m in is tr a tir m

d p la s m a im r ease
concentratio*i lee '

ltin g in an
p la s m a W
re s u
phenym l e n t a r e y u a lly fīc rıp rJ 9
h M t o f p r o te in d is p a m
d ń s k o f to x ic ity T e
e c s
e
T h e Ëe In te r a c tio n s in c lu d e th e fo llo in g
p r a lle l w ith th e
w
p h m y ıa n d a n in w e a e d r u g u s u a lly in c r e a s e s i n a
o f th e a ffe c te d
4 i v e d b p m w Ĥ e n te ta b o lls m h w e v e r b e s ig n ific a n t fo r Naitiínteractions a n d com bin e d to x ic iiy If tw o d r u g s th a t h a v e th e s a m e p h a r m a c o lo g ic a l
D is b ūbu « o n jn te r a c tio n s c
a n o
b a äm b o th th e
二二
in a æ « d É e e d u g c o n c e n

二 k 。 。 一

F竺 ėff&ť ŕ é g iv m to g e th e r , th e e ffe c tsc a n b e a d d itiv e A d d itiv e e ffe c ts c a n o c c u r w ith


A P e u ? .
。. ˜
鲫 e 加 n e ly ī a 口は f th e d r u g s ll h i id ff S ti th d d ic ti e e ffe c ts a r e
m a in e ffe c ts o as w e as t e r s e e ec st o m e m e s e a v

s o le ly to x ic
M e ta b o lis m
D m gi n
in te r a c tio th e r e a r e s o m e p a ir s
h m e P 4 5 0 (C Y Ħ in th e A n ta gó ilis tic g in te r a c tio n s : ln c o n tr a s t to
o r o p p o s in a d d itiv e n s,

W ? u m b o l i s m b y d i r e n t is o e n z y m e s o f c y to c r o
g s re ly o n ? lw ith e r ofdrugs w ith a c tiv itie s th a t a r e o p p o s e d to o n e a n o th e r
2 C 9 2 C t% d JA 2 In te a c tin g d r u g s h a v e th e p o tm .E

\ d a n y 3A 2 D 6
a n r
liv e r
n
i e ta
c r ea se a le o f m e ta b o lis m b
y in d u c in g th e fo r m a tio n o f m o r e C Y P i s o e o r

dea b o łi s m b y in M b itin g is o e n z y m e a c tiv ity 自 闭 "m e in d u c e r s (t g P Ļ ę n y n ,


e a se
v e $i n 【,
łifampcin) gm e n lly reduce p la s m a c o n c e n h a tio n s a Jlh o u g h m a y e n h a n c e c o n s p Ąq
E n z y m e in h ib ito r s (¢ l h
* c a t ro m y n , d d tid i , g
a p e fr u it
g Io ils a c tiv e fo m
ń n ıe n e r
pr-

ta te c o
: n cm tr a tio n

Scanned by CamScanner
c o l o J ı
m a
w
G W p

B o o k o r P l, a r m a c o ıo g ¥
l iM lA \
N O F N EW D ©
V A L U A T IO
O V E R Y A N D C U N IC A L E
D R U G D IS Ç
is th e p ro ce ss tlu u u gh
v e r)
D ru g d is c o d
v e red e
ith e r b y i
d ru gs h a v e b e e n d is c o
n th e p a s i
ı m có t
p o g y lle d " " m ・
a ıe c o n tr o
an d in Ř c tio n . .
u n d d ho w d is e a s e

f can d id a te s s y n th e s is
i n o
lv es th e id e n tffic a t o
d i s c o in v o
th e c e ss o f dru g tic e fó c a c y
p ro fo he a
r ı peu
jn
sn ee ı s a n d a s s a ys
o n
m
li ìo ri)

4 1) a a 9 ] o

VERY
D R U G D IS C O

p m d in z ・ P »

i A * » i l

l th o f
d r e d (1o 0 5 00 ) p a ū e n ts a l e s e le c te d w ith e ta r g e te d d is e a s e / c o n d itio n T h e e n g
bs Tb n u rï hu n

d d m a y b e s e v e r a l m o n th s to 2 y e a r s T h e m a in p w o s e o f th is d e s ig is to
n
J eí v b u Z s tu d y is c o n s i e r e
f d i r fo r m e d in th is
ıııı t s ty ¢ ) İ t e ffic a c y a n
d id ff t
ec s o f th e d r u g V a r io u s typ e o s t u y s p e
wh e d i ¥i + Ľi ł
s e e
ind ou t
i &i ・
e s t i n g a dr u g i np e o p l e, e s e a r c h e r s mu s t f l b lin d e d s tu d y s in g le o r
to ln n n a n i T ħe p r e d i n ic a ıs tu d ie s a r e c o n d ti&i a e t r p g e R a n d o m iz e d p la c e b o o r a c tiv e c o n tr o l p a r a Ľ e l d o u b e
tb e p o m ia ı c a u s e s a io o s h n m
" Iq u iu ın m u ltip le d o s e s a n d m u ltic e n te r
a r ń n a Jm o d e xs m d er c o n d i T ire tw o ņ p e s o f p ï e d in ic a l te s tin g
n d
n pa Te s in led ö*ii¢ - p j% n % $J h e p u r p o s e o f clinical tr ia l p h a s e n is t o fin d in g th e d o s e r a n g e (M in im u ın a
ex pe t me a t s ar e om d ua e d ou t si de tlre a n i ma l c o n t ro l
1 m E ffe c tiv e n e s s fo r th e tr e a tm e n o
t f th d i o d itio n fo r
e ffe c tiv e d o s e )
N U ın i x ĥ m e s e a s e o r c n
rm d ŕFin n $ Zr T he se e cp a n
i × M s a re con ń ıd e d ni s id e th e an im a ķ

ıaany p r o d in ic a ls in d ip a re n D t v a y W H o w ø e r th e s e s tu d es m u st p r o v id e
? o n n a tio n on dm * a n d to w je v e ls A fte r te s tin & r e se a r c h e r s r e v s
}o l 9 l o r r£
p a n d d e c id e w in ? æ the g c a n b e te s te d in p eo p le

M e m io u s e q e im e nße b e e n c o n d n Ħłd u r in g th e s tu d ie s su ch as
Cı in ic a t tr ia ıp h a s e m (T h e r a p e u ū c C o n ßr m a to r y ) ln th e clinical tr ia l d e s ig n P h a s e m
J) ¥īrJ
ı L a rg e n u m b e r o f p a tie n ts is s e le c te d 1 0 0 0 to 5 月刃 p a tim ts w ith th e ta r g e te d

edosea»cicitrsinđ
æ n

Scanned by CamScanner
u /P r o
d u c t q u a lity
(A ) D r g
v e rs e d r u g r e a c
tio n
(B ) A d
i a tio
(e r M e d c
n e rr o r

ìo n ou n g

Ďił
di}¢
iooı d i ue n pha n n a co u ig iı
an ce ik e
ı

iw ts w ho a re th e u se rs o fm e d id n e s an d m e d ic a l p r o d u c ts

o rm

ī?ï
a c is t. n u rs e s d ic s d a ll o th e r h e a lth c a r e p r o fe s s io n a ls w g
p a r ai m e an

re m o v ed

5 Ť . H
J tr ia ls p r o cæ s l d r u g s ħa v e b e e n M A ) d th in th M ber
c tin ia se v a a
d L
EOpe
th e M e d i c i n e s A g e n c y (】 an o se e e ın

R e g u la tm y Auoaities including U S FD A U J( s M H R A an s
N a tio n a l u g
EM EA h a d d itio n Io th e n m m o v a l o f p o tm tia lly to x ic d r u g s fr o m th e m a rke t OJĺ tļ o f
. . s a fe ty o fm e d ic in e s

r e la te d s id e 7 r e ffe c ts ı
ąbFharmaceutical c o m p a n ie s an d co m p a n ie s im p o r tin g or d is tr ib u tin g m e d ic in e s
ir e d a dd a d d itio n a l warnings to
夢i声ヂ e v e ry

c on
iv
ı e d r u g s a re
b a in d ic a rio n s e tc
requ

G lo b a ll» on
to
Jy a b o u t 5 0 0 0 to 7 00 000 a d v e rs e e v e n t o c w a re (5} P 】
iá í m acolo g is ts w h o d e a l w ith a d v e r s e d r u g r e a c tio n s f p a tie n ts
o en ro lle d in c in ic a 1
ı
c ap h zr e d e a c h y o w e w m Jo w ? to m id d Je ? In c o m e c o u n tr ie s w h ic h r e p r e s g n ţ ìi n o re
TOrtHM§fr o m ń m d a m e n ta l p h a r m a c o d y n a m ic s tu d ie s to s tu d ie s o f P h a rm aco k in e tic s an d
tħa n tw o ? th ir d s o f w o r ıd p o p u la tio n c o u n t fo r a
e n y fr a c tio n f a ll h e ADdąJil In n l Filjř b
g m e ta b o lis m to p h a r m a c o g e n e tic s
th is s tu d y fo llo w in g s te p s areiı ıvved in A D R r e p o r tin g
m )C o ı
le c tio n tħe d a ta of p lt a r Jm a æa n d its s 山山s in In d ia
($ )ř ha r m a co v ígila n c e s ta tu s jn A y u r v e d ic /h e r b a l m
re
s p e c t to e d ic in e
(C )S u r v e y o n A D R qe p o r Łin g a w a r en e ss o f p h y s ic ia n s a t s u rr o u n d in h o s ita ls
g p

Scanned by CamScanner
一 团团
a c o o gw
ı
e ra lP h a rm

to w a r d m e d ic a l
u n
im p lie s th e s e a r e a n y

Ï Y I ĮË
n am es

d is a b i】
it y o r

- su its h ' '" ' ' " d . _ t


t
ly b ir th d e fe c t
re s u lts in a congenJ an o m a o r

ı
= lĄ a c a se s ex p e a it e a ľ o
d in g o n th e ir n a tu r e 】
n so m e
・p e n titu t e s '
・ ls o c o n s
in ie c tio gen t a

ĝ ĝ "" p r o ' " t, " " " s u s p e c te đ tr a n sm is s io n . ' "n u s a


- ū o m sM p w iń the cm u se o fı
r e a tm m Ł

t
o f th is c ı
a s s ió c a tim i is to rea so n a bly is h th a t a r e la
e s ta b 】
.
źXH
tio n s M p b e tw e e n th e r o d u c t a n d
ş¥xt'X,.X.X
bn Jĵ bo
° th e in v es tig a to r

p ß u
th e r e a c tio n m be
ot r u le d o u v O th e
n ce
p r o d u c t h a s b e e n p la c e d o n th e m a r k e t J a T ßm ÐI
d v e r s e R e a c tio n s en c o m
pa ss r e sp o n s e s w h ic h a r e a a in
g n o x io u s a n d u n in te n d e d Ju d b Ŕb í 【
bu t
ır a t
o c cı the e s ta blis h e d r o u tin e d o s a e s
g w h ic h h a v e b e e n d e ı in e d fo r u s e in h u m a n s to o J a n ßm u ı
p r e v en Ļ d a gn o se o r tr e a t d is e a s e o r m od w hysiological ń m ctoni HOWeve 9 1 0 Sm o
T ece n t d e lin itio n s in c lu d so m e m o re
e r es o n s e s t d
p o o s es a n d u se s
o u ts id e th o s e
re c o m m e n ded


Scanned by CamScanner
阿 C H A PT ER J
Á

严 ıf
.
'
lHĄRMAcoLoGY PharmacolE o fD ru g s A c tin g o n p e r ip h e r a l N e rv o u s s y s te m ıo ı
=

O N P E R IP H E R A L C a tc h la m ln e a
o C a te c h o l a m in e s a r e th e co m po u n ds w h ic h co n ta in c a te c h o ın u c le u s
二 (o r th o d e hy d ro x y b e n z e n e )
N o n c a te c h o ] a m ln e a T h e s y m p a th o m e m e tlc a m in e s w h ic h a re dev o id o f ca te c h o l

ı n u cı
e u s
N T R O D U C IN G TH E C H A p TE R
A n ti A d r e n e r g lc s T h e s e a r e d r u g s b lo c k th e a c tio m o f c ir c u la tin g c a te c h o la m in e «E P &

CbzanħationofANS N E ) o n a d r e n e rg ic r e c e p to r s a n d a ls o in h ib it th e e ffe c ts o f a d r e n e r g ic n e r v e s tlm u ıa tio n

N e u r o m u s c u la r b lo c k ln s a B e n ts D r u g s th a t a r e in te r r u p t tr a n s m is s io n o f n e r v e
M u io ı
n ım on l tıa n s m is s io n
im p ls e s a t th e s k e le ta l n e u r o m u s c u la r ju n c tio n
u
m b s i o n Lo l a n a e s th e tic s
ca L o c a l a n a e s th e tic s a r e d r u g s w h ic h o n k x a l in je c tio n o r to p ic a l

řa as M im tfo fn a p p lic a tio n c a u s e r e v e r s ib le ı o s s o f s e n s o r y p e r c e p tio n o f p a in in a p a r tic u la r a r e a o f th e
n o e u ło b a n s m itle ï s
bo d y
dtotmimetics G ı a u co m a T h is is a d is e a s e th a t d a m a g e s th e e y e s o p tic n e r v e It u s u a lly h a p p m s w h e n
ţ d m ıy d c = flu id b u ild s u p in th e fr o n t p a r t o f th e e y e
S y】ıp a u io m ñ n e ti¢s

fgmipı
tħoie
:N b m t m ıa c u ı a r b lo c lón a


g g e n ts
ï d e tıl muscle n la x a n ts q n i h
IN T R O D U C T M
p p e aD
ıo ta l a w s ı T he n e r v o u s s y s te m i5 a co m p le x n e tw o rk o f n e rv e s a n d ce lls th a t ca n y m e ss a ge s k o m th e
h e tic a e n ı
g s
D *u g i u se d i
b r a in a n d sp b a l c o rd to v a r io u s p a r ts o f th e b o d y T h e n e rv o u s s y s te m in c l ud e s b o th th e
n m y a s d ıe n i
a g ıa ï is a n d r ll
g la u c o m a ìo C en tr a ıin e
r v o tis s y s te m an d P ę r ip h e r a l n e r v o u s s y s te m Th e ce n tr a l n e r v o u s s y s te m is m a de
q ĵ

f S r l} b u p o f th e b r a in á n d S p in a lco rd d th e p ip h e ra ln e r v o u s s y s te m is m de f th tic
r ır an er a u p o e so m a
a n d th e to ie n e r v o u s s y s te m
K EY TER M S a u n o m s

區 O R G A N IZ A T IO N A N D F U N C T IO N O F P E R IP H E R A L N E R V O U S S Y S T
M
■ P e r ip h e ra l n e r v o u s s y s te m Th e p o r tio n o f th e n e r v o u s s y s te m th a t is o u ts id e th e b r a in a n d
グ iËiHZbrd is ca l led PN s . h e ne r v e s in the pN s co n n e c t the ce n t ra l ne rvo u s sy s t em (cN s ) to

:
d h e a u
£to n
"
o m
"

ie
p h e ra l
n e rv e s
n erv es

M e a u
in c lu

to
d
n o m
e th
ie
e 12
n e rv e s a r e
c ra n ia l n e rv e s

co n cern e
th e s p in
d w ith a u
a l n e rv e s

to m a tic
fu p ç tiņ ņ s o f th e b o d ific a lly ith th e
y sp e c w re g u la tio n o f th e h e a r t m u s c le th e tin u s c le s
th a t lił
ie th e w
, y m
a lls o f b lo o d v e ss e ls a n d g la n d s

T Iw JP N 5 is o n e o f th r e e d iv is io f th e
n s o au to n o m ie n e rv o u s s y s te m d e fin e d a s So m a tic
sym p a th e tic a n d pa ra sy m p a th e tic
u ru ĵ o l d

* A d łe n a
g la Jh e s e a re th e d r u
ga n gı io n ic n e g s th a t p r o d
rv es u ce a n
e ffe c t s im
ua r to tim
s u la tio n o f
p t
o s Jz o q ìo n n

罵 哼螺 声翟無ニ
ム 廢野套圈 昭 多 3男四e a 8 目

Scanned by CamScanner
Scanned by CamScanner
◆ Ł

10 5 =
E h a rm a o g y o f D r u g s A c tin Ē
◆ ı {m p e n p h e ra ıN e rv o u s m s te m

a z İ S T E P S IN V O L V E D ı O N
N N E U R O H U M O R A L T R A N S M IS S ı

田 Tim iin rr \ 出 es is F or w p tic s i o n to ta lce p】


a ce ın o le cu ı
es o f n m i t t m

亩 n iııs i ó é p r e s e n
ī
t h th e n erv e H ce
e rı th e E l e r s y n th e s is a s fir s t s te p in

F o r e ca ın p ]e N A fro in l y r
f il s
Tį tt¢rMorage A f【
e r ı
ra n sm itte r is \ lh e 5 iz e d it m ııs t b e s to r e d łm ta d le o

t in th
p d m
e a x o n
T n m sm ifte r s to ra ge ta k e s place w ith in V a s presm

】 be f tnnn nit ter Æ e d v e s id æ i


F a r h n e r v e te r m in a ic m ıt a in s a a rg e ıı
u m r o

□ N EOBO H U M O RA-
ı ť Į Į Ï, T he 出 唱 łr a n nł n e p o te n t ia l is 0 0 m v n e g a tiv e in s id e l
Im w co n d u c tio n r es sï n e = )r a

n a tio
i
e s ta b lis h e d b y M g h K e a b i】
ity o fa lm
x o n iı e m b r an e an d M gh a x o p la s m ic co n cen n
3 ı8 æm 3 8 Ħ C a i c a ł p e rm

c t r a c t i o n s W W W la ti« m s o r
d íts t iv
呵겋 ア尸こコア 臼 뇨 登 台
o f th is io
m c o u u n s 1
p le d y iť 】
o w n a a n a c e
a i
i Ħ £ * a
į f a n e 】e d r ic a l p u l s e c a ııs e s a s u d d e n in c r e a s e in N a c tn ıd ı« l a n c e d e p o la r iz a t o ıı
s W 5 c c h e x a i r a ł (z p # p Ę =
ı = m M M f h e ir
\
t0 i th d i t i o t
m 05 S a h ıx ) t (T e v m e p o la r iz a tim ı) W im ı th a n ın o v e o u t n e r E rc r m

S Ê æd b Þe r e A e u w ¢= Tæ li d d i the
a D s s
? t i o n g r a d ie n t a n d re p o la r iz a tio n o c c u ıs lim ic s r d i t m tio n in n o r m a z e u r n g
国团四围 弓と宝 ど 缸 d ia t e d by
二7 掣
x i m e d ııi c a J s u b s ta n 14 e r io d b y th e a c io
tiv a ł n o fN a+ K p u m p
c es p
t«ı r el ea se T h e t ra n s m i tter e
( ) cci tat o« y or i nM b i loi y ) is s t or e d in pT W c t ion a l

im p ls e p te s ń ıs io n o f v ascu la r an d
W v e s s e ls N ro m o
d in g t h i n p tic er v e u
n e rv es en




三二
資 卫四 国 ゼ 亟鹰 買 加国 王 园 区 血 妇 +
ııid iz e d
h ic h fı bra n e s T he r e le a s e p r o c e ss c a n
gh C
th ro u a w e n tıy w ın e t n

ï = q = 5 bp==qmicneuro in e r ip h e r a ıg
:
iz% & ïu l a te d by th e tr an sm itte r its e lf b y o th e r a gm ts th ro u gh a c tiv a tio n o f s p e c ific
p \ 螂?ņd.
oc ed on t he ior ıal me mb r an e . he v e ssels a r e ıni gi at ed t ow a r d t he
a t p r e J un c t

tic ost

I
itte r p to
s ite d y tic explosi R e le a s e th e n e iır o tr a n s ın re syn a p p
Æk a cæ =i ai t p
äaıymoda*ginp&e b n is s i a t e itı
ıer a a e a th e
m em b ra n e a n ex o c

g b £b e j ? a i o ıi ¢ , s tn d r o ŕ a ıd o n o m ic p h a m a c o Jo

y idĤ iiăL
r
g y r e q u ir e s
æ cee*aeide«aâg , .
ii*ittr r io ac t n on p o 5 t jun c t ion a l me mb r an e 1 he t ra n s m i tter r e l ea s e an d c o ınb i ne s

i \ r e to ec p r s on the p os tíun c t ion a l me ın b r an e an d de p e n d i ng on its rıat ur e ind uc es

]łe i = ci r e d Ė a n e x c i ta to ıy p o s ts y r ı
a p tic p o te n tia l (E P S P ) o r a n in h ib ito t y p o s ts y n a p tic p o te n tia l 0 P S P )
ıx a a Tm m im is s io
a m M æ¢ Ëe d i id e r i «
a aa ¢
n a ï s yn a p ses a n d n e u rw ffe c t o r g '
9 1 f ex c ita to r y n e u r o tr a n s ın itte r a c t in c r e a se in p e rm ea b ility to a ll c a tio n N a + o r
a m
CO n& i di o a n d r e le a s e o í
E c Ęp lw e a se d s
a a d a í e įe » e a r o b a n ¢m
į\ P i łx c a u se s d ep o la r iz a tio n fo u o w e d by K ・
e fflu x
ia er s J ħe p r ii?
pa J n e u r o tr a n s m í tte yił
jirr ır


rs
t in in p b ility to lle r io n s T h a t ın e an s
If in h ib ito ıy n o t r a n s n ıi t t e r ac cre a s e e rm e a sm a

Ï r 汇 Pa ¢ a e ta = a d « a etea ıe d
Cl m o v es in r es u ltin g in h y p e rp o la ń z a tio n

lly A ty l
h g ı
n ¢ia fr o m f N tr a n s m itte r N e u r o tr a n s m itte r is d e g r a d e d lo ca e g ce
th e p r
w g lim ic $ppyal a c tio n o e u ro

ı
ıı
er v e e n d in g o f b o th T he
tio l tiv e d ifħl s e m ec han is m
is r e s to r e d in p j
r e tın c n a n o n e a c o r

į
n e u r o tr a n s m itte d d e g r a d e d b y e n jy m a tic a c tio n
lf Ŋlci ıı
p J JF

Scanned by CamScanner
a đp
f P h a rm 7
a Të i t B ' "
rÆ ı
o " " o g y !v °
U a c û g y f D ,u g s A ċ t in g o n p e r ip h e c a l
N e rv o u s B e r p
lw "
o



習 C

V W
P
= ı

F ig 3 4 A p ro c e s s o f re le a se C a h a n s ın i s s i o n

It is e s ta b lis h e d th a t s u b s ta n c e sho w n to b e lo c a lis e d in n e rv e s a re a c tu a lly c o tr a n s ın itt e r s

7 ħe su b s ta n ce is syn th e s is e d a n d s to r e d in th e n e rv e u la tio nd r e le a s e d n erv e tim


an u po n s
Th e s p e c ific r e c e
p to r s fo r th e s u b s ta n c e n e e d to b e id e n tifie d o n p o s tju n c tio n a l s ite s th a t
w h e n o c c u p ie d le a d to c h a n
g e s in p o s tju n c tio n a l a c tiv ity T h e tr a n s p o r t s y s te m n e e d s t o b e
p r e s e n ıjfo r th e s u b s ta n c e its e lf o r its b r e a k d o w n r o d u c ts u ta k e o f w h ic h le a d s to r e n e w a l
p p
m e sse n ge r s to r a g e in n erv e te r m in a ls It h a s been p a r tic u la r ly d iffic u lt t o e s ta b lis h
c o tr a n s m itte r r o le s fo r th e m an y p e p tid e s fo u n d in n erv e s p a r tly b e c a u s e
specific re ce p to r s
an d p h y s io lo g ic a l r o le s h a v e n o t b e e n e s ta b lis h e d fo r so m e o f th e s e an d p ar tly b e c a u se o f th e
9 iUiyćkMblective a n ta g o n is ts It is b e c o m in g c le a r th a t A T p is a p r im itiv e s tg n a h n g m o le c u le
(

tħl1Hgíbeen r e ta in e d a s a itte r in e v e r n e r v e t
c o tr a n s m
r y y p e in b o th th e p e r ip h e r a l a n d
ñ*ä?ervous s y s te m s lth o
g h th e r e la tiv e r o le o f A T P v a r ie s c o n s id e r a b l in d iff
a u
s p e c ie s an d p a th o p h s io lo ic a l c o n d iti y ere n t
y g o n s A T P a p p e a r s to b e c o m e
a m o re
p r o m in e n t
r
łtj¢i ćtrammither to e th e r w ith c la s s ic a
g l fa s t tr a n sm itte r s su ch a s A cH
e r ë á ń d o n e o r m o r e p e p tid e s N A g lu ta m a te

3 2 3 C LA S S IF ı cA Tı o N O F N E U R O T R A N S M IT T E
R
:X X
'
N e u r o tr a n s m itte r s
a ls o k n o w n . s c h e
m ic a l m e s s e n e r
e n a b le n e u r t g s a re en d o ge n o u s chem ic a ls th a t
o r a n s m is s io n T h e y tr a n s m it s i n a l
g s a cro ss a che m ic a l ìq
sw ap se su ch as a

eË "
》歹 て
d シ習ロミ

Scanned by CamScanner
l rTa°
ıOgy o f D ru g s A c m E o n p e r ip h e ra lN e rv o u s
s t e m j ıı团团=

I
fr o n e u ro n m erve ce ll) to an o th e r ta r g e t i
n e t ro n
u s c tłJa r jım c tio n b m o n e m u scl
n e tu o m e
le ased fr o s yn a p tic v es ic le s in s yn p s e s in to th e B y h
cE L
ı o r g la n d
T ħe s e a r e re m a
a þtj
a n e r e o e i\ by n e u ro b a n s m iH e r n e c e p to rs o n th e ta r g e t c e lls
c iw w h e r e th e y
d a ls o c o n tr ib u te s to
N e u ro tra n s m itt e r ca n ı
pe d a s s ffie d a s e ith e r e x c ita to ıy o r in h ib ito r y è ĵ k ita t
o r
y
cat#aņttiety a n m o to r c o n tr o la n d v is io n

itt u s ńm c t io n s fu a c tiv a te ıe c e p tų r s o n th e p o s t s yn a p tic m e m b ra n e te M o s t co m m o n b r a in n eu ro tr a n s m itte f


n eu ıo b a n s n
an G lu ta m
a
e v e lo p mr R
g u la te s d e e n t a n d c r e a tio n o
M f th e a c t io n p o te tia l
h ile In h ib ito ıy tr a n s m itte r s ħın c tio d h e n c e is in v o lv e
p a th w a y s a n
th e e r o n w
en ı
ıa n o e e n s tQ m
h e rv e d in learning a n d m e m
n ew
1 ib it o ry
t m a p t ic m e m b r a n e a n d d e a e a s e th e e « ė c t o f th e a c t io
th e c v to ıs o n p o s g n p o te n tia l R e le a s e is a s s o c ia te d w ith fe e lin s o f
g e u p h o r ia a n d a r e d u tio n in p a in (b o d y s
ı u
y ä a ı t \ \ a )s m c a s s y n e u r o tr a n s m itte r s D iv id in g th e m
W
c
m e t e a r e m a ıı tg k ille r s ) R e le a s e d d u r in g e x e r c is e e x i
a n d c te m e n t a n d s e x
a c id s p e p t id e s A n d m o n o a m in e s a c e ty lc h o lin e is s u ffic ie n t fo r so m e c la s s iĥ c
a tio
n
p 1 ħe m a jo r n e u r o tr a n s m itt e r s a ıe g iv e n in F ig
3 3 P A R A S Y M P A T H O M IM E T IC S S Y S T E
M A N D D RU G S

They
f a c e ty lc h o lin e ac tiv a te th e p a r a sym
p a th o h tic th J1e d h lin g ic
o m n e s y s te m u s ca c o e r

fib e r s
Introduction P a ra sym p a th e tic a c tio n b e p r o d u c e d e ith e r b
u la tio n o f c h o ìin e r g ic
can
s tim
y
fib r e s w ith a r e le a s e f ty lc h lin
n e rv e o a ce o (A C H ) a s tr a n s m itte r
b y th e e ffe c t o f c e r ta in
e o r
dmgs c a lle d P a r a s y m p u th o m im e tic s ıin e s e s u b s ta n c e s a c t p e ń h e r a ll o n th e s a m e e ffe c to r
p y
th e n e u r o h o r m o n e its e lf O n e d i
Orgarg s tin g u is h e s b e tw e e n th e ir m u s c a r iï ı
k a cū o n o n
v m u sc ı
s m o o t】 e s a n d g la n d s a n d th e ir
n ic o tin ic a c tio n o n s k e le ta l m u s c le a n d a u t n m i o o e

Ħg 3 3 A s y s te m a tic cı
a s s ilic a tio fn ł
r"
(e ß7 ßq
n o e u ro tr a n s m ittu s ľ J w J u m u Łic u ia r an d g a n g lio n b lo c k in g a ge n ts r e
T he ı o w
o lı j
m a or n em o b a n s ın itte r an d ńu ıc tio n s

A c e tr lc h o lin e m v o lv e d jn th o u h t Je a m in
g g a n d m e m o r y w itM n th e b r a in a n d a c tiv
a te s
muscle o n b a c t i o n in th e b o d a n d is a ls
y o a s s o c ia te d w ith a tte n tio n
a n d a w a k e n in
g
A d i e n a lin « A d r e n a lin e is r in ıa r il
p y a h o r m o n e r e le a s e d b y th e a d r e n a l la n d b u t
n eı g so m e
ır o n s m a
y s e c r e te it a s a n e u r o tr a n s m itte r

ı
t is p r o d u c e d d w in
g s tr e s s ń d o r e x c itin
g s ih ıa tio r ıs
N on dn n a lin e ı
n c o n tr a s t lD a d r e n a lin e n o ra ? en a lin is p r e d o
th a t ĵ s
e m in an tly a n eu To tr a n s m itte r
o c c a s io n a tı r e le a s e ìsu im
y d as a h o rm Jt e n ßr Dı * tr ı
b u tı
on o ¢
on e c o n tr a c ts b lo o d v e s s e ls a n
no w im p r o v in d in cre a s e s b lo o d b o o Įd p a r ııy m p a th o tı
g a tte n tio n a n d th e s p e e d 29 2 5
c
a tc h r e s p o n s iv e a c tio n ・r v o u s ıy ıto m
n s occu r
D o p a m in ı
t js p r im
e
y
a r i】 r e s o n s ib l
p e fo r fe e lin s f p te a s u r e
g o b u t js a ls o in v o lv e d in Í bĵ v lo v ı
le a d in
g to a d d ic tio n s A b n o r l9 1
m al do am i JP 6 9
d is o r d e r s lik e P p n e s e c r e tio n is co m m o n in
9 11
a r k in s o n s d i s p e c ific m o v em en t jr rÐ【n Ðv
se a s e I 1吕 3 6 C h o ı
ln e r s lc n e u r o
o rr m ın is s i[o n p a th w ays

Scanned by CamScanner
iC hoM o - M a.

ı X S ta n g e

.
o f a c e lT ı
c h o lin e in v e s ic le s T ħe a ce ty ic h o ı
in e is s to r e d in to p r e s n
y a p t ic v e s ic ]e s
by

P 竺 °C'"・ ・一 ・ ・一
c o tra n s m itte r a c tin g a
・・・ ・

t p r e ju n c tio n a l
・・ ・ ・・・・ ・・ ・ (A 一 )

p u r in er g ic
. 。. . .. . . .・. . 。。 T h e A T p is a
re ce
p to r s to in h ib it th e r e le a s e

a c e ty ı o lin e o r n o n f
p jn e p fu jn e o

R e le a s e o f ßd ı
a ce l o li
n e W ħe n an ac tio n Ħg 3 7 A
ge n e ra lp ro c e s a o fa ty ı
ce e ch o ı
in e

olo g ic r e s o n s e
p w ith in th e c e ll s
u ch as th e in itia tio n o f a
ĥ b e r o r a c tiv a ti
o n o f s e c ific e
p n zym es in e ffe c to r ce u

ï x x =
m s as
e sse n
ge r m o le c u le s
' " h " " . °" " p . . . T h is r e le a s e " " e ty b h
p ļł
ņt,
ßåĝ łį o . o f ace ty lc h o lin e The s ig n a l t th e
tèï m a ţëd b e c a u
a
p o s tjtın c ū o n a l e ffe c to s ite is
B jn d h
g to tħe r e c e p to r ) il
s e a c e t lc h o
y lin e s te r a s e cı
r ra p id ly
A c e ty lc h o lin
)
q ó ır z
y eav es ace ty lc h o lin e to c h o lin e
e r e le a s e d fr o m syn a
p tic c le ft B u t r l h an d a ce ta te in th e
th e s jjn a 1jc s th e sy n a tic v e s ic ie s y y c o lin e s te r a s e
P pa an d it b jn d s b p diffuss r ĉ i ś so m e tim e s c a lle d
p s e u d o c h o lin e s te r a s e is fo u n d in th
e h he r o f tw o p o s ts w uc
P . b u t it d o e s n o t la a s ig n e
ap rm
q th e ta p y ific a n t le in te r m in a tio
rg e t c äjr b iu tb
on on ro
n o f a c e t lc h o li
P o s tsjm
ą S J y n e s e ffe c t in th
e
a p tic c h o ı
in e r ĺ c
g rec e
p to r s on th e s u r ia c e o
◆ f th e e ife c to r
asstıscarinic a n d n ic o tin i o
rg a n s a re d iv id e d infofvQđ
c ş)m n ţ hat tr a n s o r ts th e
イコı p m o le c u le b a c k i
てゴ9 3 月 ty lc h o lin e th n to th e n e tı h e r e it is
ace
a t is s to r e d u
n til r e le a s e d b
a s b
ro n w a ce ¢1a te d in to
y u se qu e n t a c tio n
tia l
1 o te n

jjıibmīJ s tim u la t d
e by ace ty lc h o lin e r e le a s e d b y th e n erv e te r m in a l A fte
r A c H h as b
een r e le a s e d in to

Scanned by CamScanner
r屋国jA Te x t B o o k o f P h
四国团团日■
i
a '" a c "
w (v o ˜
Y
it b in d s to on e o f tw o c la s s e s o f rece p to rs u su a lly a
th e s y n a p tic e le r o n

s u r Ta c e o f th e p o s ts jm p tic c e ll
a I
ylchollne r e ce p ı
om (m A C H R ) a re se v e n tr a n sm e m b ra n » h e lix G
A ? m ıl c p r a te in

三野三二二邛
m u 日c a ' " c r'"p'"'" ^ d i
n ic o 匣 n ' "

T a b le n o 1
d 9 8 u ßJ 9 8

M 2
W e* sm th se v e n
-
oo tr a n
M sm e ın bran e 】
n h ib itio n
u s c le
s e g m e n ts G i/o p r o te ir ı cA M p
In ke d
p ro d u c tio n

a c tiv a tio n àlq ë« qJo q


9 ru
i]W . m mı s ・ e v en b a n sm
M u em bra n e

Iİ b Ç q / ,:
p r o te in


― ―

Scanned by CamScanner
liGBI A Te u B o o k o f P ha rm æ °
[ j .
W
' "
A
'
"1ı
DnÐ
fj
ti Z Đv J
n
u iJq iJ ï
u rr

ir r ó r b
s .. .
V IJ I ı9
y j ,


sícloq
3 3 1 C H o IJ N E R G Ic
D RU Gs 119 コ タ山

c h o lin e r g ic d r n g s a r e a ls o lo n o w n as C h o lin o m im a t Įc P a ra sy m p a th o m im a tic d ru gĵ , tine


tio f c e ty lc h o lin e Tin ese a g e n ts ac t o n th e
h ic h p ro d u c e th e s im ila r a c n o a
ale th e d tru g s w

m u x u r o n ic a n d n ic o tin ic r e c e p to rs Jĵ jT ib n i

a th e tic n e r v o u s s y s te m
m im ic a n ta g o n iz e o r pM [s
th e
D ru gs g th e p a r a s y m p
a fie c tin
ilFÁiı
i'at
D h t i i lo n g th e a c tio n s
in ic r e c e p to r s r u g s t a m m c o r p r o
a c tio n s o f A c H a t m u s a u lĐ r l]o b n
m u s c u in ic receprs a r e te r m e
d p a r a s y m p a th o m im e tic s o r c h o lin o ir 出m e tic a
名n ix ßlD T
C la s s lĦc a tı
o n o f C h o lin e r g lc D ru g b9Ju bn i
m
ir n ĵ e c lß Y cl
Anüchw::g .. ı
s
)o m a s í【
l th e s m o o th m u s c le s
f
By tim la tio n
p t v a s c u la r )
o
矿 砂
Sm o o th M u s c le E ffe c ts o n sm o o th m u s c le s (e x ce s u
Choe N a b r a lA Ha lo ld s
s c le
e s te n
ty lc h lin lic its In c r e a s e th e c o n tr a tio n in s m o o th m u
ru fq a o r lq p h o s p h o lip a s e C a ce o e e

8 3 In te s tin e A n in cre a se in to n e w ith so m e tim e s a n in cre a se in th e p e r is ta ltic co n tr a c tio n s

寺 中 T N a u sea an d v o m itin g te s tify to th is s tim u la tiv e a c tio n


In iv e ra ib le Re v e rs ib le Į ĥ 9a "
J
a n tlc h o u n e s te ra s e a n tic h o lln e s te ra s e
: U r e te r s In c re a se in to n e o f u te r u s
W a g e n ts
attad f a s th m
B ta n M r o n c h o c o n s tr ic tio A lo f a ty lc h o lin e c a n a

R Æ B o
w ın o p h oıp ı x . .. . .. (E s e rin e )
n n a ero so ce ca u se a n

Secretı
os (i e c e p to r s M ) A ty lc h ı
in in tio by tiv tio o f C
R s ce o e cre a ses se crec n a c a n

ŝ ĵ i*i
" ."
la c r im al
p h o s p h o lip a s e d ig e s tiv e (a b u n d a n t s a liv a ) b r o n c h ia l c u ta n e o iıs (s w e a t) a n
d
, r lq z o r lr4
h bu n s e c r e tio n s In th e g a s tr o in te s tin a l tr a c t a c e ty lc h o lin e in c r e a s e s s a liv a r y s e c r e t io n a n d
in rrnİ jÐ
TjÐ
s tim u la te s in te s tin a l s e c r e tio n s a n d m o tility It a ls o e n h a n c e d th e b r o n c h io la r s e c r e tio
«
n s In
ı n ïu rn î Je

Scanned by CamScanner
r Jl

r th e g e n ito u łin a r y
tract Th e to n e o f th e d e tr u so r u r in a e m u s c le is in cre ase d P ıa r m a c o r o o y o f D ru g s A c t in g o n P e r ip h e ra ıN e rv o u s S w te m
łmı
i $p u s jt ı
e x p u ls io n o f u r in e 8
r i!o

(R e ce p to r s M j ) A c e ty lc h o lin e a c t iv a tin g th e p u p illa ıy s p h in c te r m u s c le o f th e


rı) iı
Uiit llisenerauy n o t u se d a s an a d m in is te r e d d r u g b e c a u s e it is b r o k m d o w n v e ry r a p id ly
io s is w h ic h facilitates th e n o in ia e o p h th a lm o lo g ic a l a p p lic a t o n s
i
fp p iıd ia m te fu l ĵ n
ł
jn d u ces a d em e e o u e r o r m
w o f by c h o lin e s te r a s e s b u t it is u se so m
a qu e o u s L
N U la
th e in tr a m m 2 0 Jm g / v ia 】 In tr a
a n d te n d s to ı
o w er a r p n es s u re o r
Ddar& B ran d n a m e 】
w o c h o ] E 1o m g o p h th a lm ic 】
w o ga n p w s o c u r

: n u r ıZ L

is t to s tim u la te th e
M E T H A c o I IN E It a c ts a s a n o n s e le c tiv e m u s c a r in ic rece p to r a go n

N ic o t in ic e l 1 A c e ty r c h o ı in e a c ts o n n ic o t in ic r e c e p to rs Re ce p to r c ha n n e ls w h ic h in c h a lle n g e te s t

a c t iv a e t s o d itım a n d c a lc iu m
te d s ø te ı e n te r in to lls Th u tin g dep
an
M th a c h o ıin e c h lo r id e 3 2 o g M e th a c h o lin e O m e g a 100m g
ce s crea a o la r iz a t io n B 】? p qiŅ a m e e m

N ic o tin ic to t It is m e m b e r s o f th e ligandated io n « h a n n e ı fa m il
m ep
y a ls o c a J1e d [f
b s tr u ū u ıin e
t iv e /p tp h ım n o n o c v e
p to r s N ï c o tin ic ī e c e p to r s h a v e a p ıe n ta m e r ic s tr u c h u e fo r m in g â Jr jĉ ë iĺ b íä l
to p e o s ar
d in ra
p ic It h b p o s
io n o tr o r ece B EM N IC O L a s een u se
lo d g a s tr o eso ph a ge a l re fle 1J x
o r c lo s e d a n d a r e a c tiv a te d b y a c e ita l e g a co n an
g e n ic b la d d e r a to n y
m
c h a n n e l w h ic h c a n b e o p e n v l c h o ıin e T w o m o lëć u le Ėia f ge
co n n
Jr ę ņ tg ıtą tio n n e u ro

hi lic in iu n a to ry u r in a tio n / d e lic a tio n flushin


p r o m in e n t B le a c n g
v o
l h li d d f r a c t v a tio n o f o n e r e c e p to r a n d o
i in g th e c h a n n e l T h :Sı.e Hects a re co
a ce yt c o n e a r e n e e e o p e n
łfävėa
s ţ v ę ą li g fa ll in B P B ro n c ho sp a sm
fa s t r e s p o n se 1r p
b le t U to ta in in g
D 1 0 m g to 5 0 o ra l 2 5 to 5 m g s c U ro to n in 2 5 m g ta b T a ro n e co n

A u to n o m ie g a n g lia e lle c t r A c e ly ı c h o lin e is r e s p o n s ib le o f tr a n s m is s ıo n in th e a\itioilŕill


o se m g
.
Jthąņechol h y d r o c h lo r id e 2 5 m g ta b le t
n e r v o tıs s y s ie u _ D ı e p re s p a p tic n e r v e r e le a s e s a c e ly J c h o ıin e w h ic h B y a c tiv a t in
g n ic o t in jc
ıł
n il o E n
r e c e p to rs in d u c e s a d e p o ła ń z a tio n a t th e o r ig in o f a n e w im p u ls e ín th e p o s ts y n a t ic n e r v e l l in I n o b e
p M u s G A R IN E I t is a n a h lr a l p r o d u c t fo u n d in c e r ta in m u s h r o o m s p a r tic u a r y
TM s g an g ıio n ic s tim u la ū o n e ı ic its in its ttım a r e le a s e o f a c e l rc y ho ı
ín e iı b ¢h e C d lb ł M h i th e g e n e r d
a E n to to m a a i ı
ito c y b e s p e c ie s h th e d e a d ly a u s r o o m s n
ū a * ld p su c a s e « a

n ip a Æe tk te rn ıin a tio n s a n d n o r a d r e n a ı
in e b y th e dren g ic te n ! d a n g e r o u s if
r ıin a tio \r \ d to c o n ta in le v e ls o f m u s c a r in e w h ic h c a n b e
n n uJ
paw a er n s
W c e tı
a ha v e a ls o be e n fo u n

nejiiiß
j H y g " ac y b e t a r i u s

ıţ H
s k e l e t a l m u s c ıe T ħe s 向 ia tio n f n ic o ä n ic to r s by h o lin is been fo d in h le s s tr a ce a m o u n ts in B o le tu s
u o r ec 中 a o e c e . u n arm
A ita m lłs c a r ia th e
o fn e u r o m u s a ıı
ar transmission T ħe s tim u la t io n o f th e m o to r n e r v e jin d u ces a c e & Qjiie is o n ly a tr a ce co m po u n d in th e fly a g a r ic m a n

ds fr o th is M u shro o m a re ib o te n ic
r e le a s ein th e \ tic d e ñ o f th e d rr & if
h a ił r e le v a n t po m
ap n e u ro m u s c t ıla r jtın c t io n O n th e o th e r t y m o re co m u n

s tim u Ta tio n o f tħe m u s c le ev en if jt cau ses co n h a c t io n s d o es n o t in d u ce a ce lýjzini«i . , ą ¢P ş m u s c im o l


ıe le a s e A c e ty l c h o lin e It tio f th e tr a itte r ty lc h o 】
in e b y b in d in g
a c ts s e le c tiv e ly o n th e n e u ro m u s c tıJa r ju n c tio n A t ı
o w d o se u ħæ c h a n is m o f a c tio n m im ic s a c n o n e u ro n sm a ce

a c e q ic h o ı b ty p d ia te u s c a r in ic
ir ih ib i
in e e lic ıts a m T he M d M re sp o n se s
u s c u la r c o n tr a c tio ín 】 ty r c h o lin e c a n he in ic a c e ty lc h o lin e re ce p to rs z a n 3 su es m e m
n a ıg e q u a n t ity a ce tı[ Jm ų șd M

Ĵm u s c u ı
a r c o n tr a c tio n s r e s u ie tis s u M d M b ty p o re b tın d a n t in b r a in an d
ltin g fr o m th e s tim la t io o f th e n e r v ie d v e ör M sa t p e r ip h e ra l a u to n o m es a n su es are m a
I t is ppı
1 4
u n e a n er e
m u s c le a a r t fr o m d M in te ith G q p r o te in to s tim u la te p h o sp h o in o ș itid e
p th e ju n c tio n jt d o e s n o t c a u l Fe c t T ħe tio te tiã ırë ĦiM s a u tg i Į g m ic g a n g lia M , M a an 5 ra c t w s
se a n y e n erv e a c n p o n z
G i
a lo c a liz e d p o s tiu n c tio n a l d e p o la r iz a t io n h y d r Q ly s is d th e r e le a s e o f in tr a c e llu la r ca lc iu m M 2 a n d M 4 rec e p to r s in te r a c t w ith
c a lı
e d en d T la te p o te n lia ı w iìën īb t tū s a n
d e p o la r iz a tio n r e a c h e s a s u ń ic ie n t th r Te iĮ ts to in h ib it a d e n y ly l c y c la s e w h ic h r e s u lts in a d e cre a se o f in tr a c e llu la r c o n c e n tr a tio n
it A p p e a r s b y o p e n in g o f thezı
e s h o ld ioJtägF p(
d q p e n d a n t c a tio n a n n e l s
g ïh rd ic a d e n o s in e m o n o p h o s p h a te (c A M P )
r o p a g a te s in il*bgētllar
a p o s ts n a ti t i a l a p p e a r s w h ic h
y p c p o e n t p
lib e r s Tħe io n s C 2 ◆
a a n d W 2 + a r e jn v o Jv e d i
th is tT a n s m is s io n íđb n t tM iıd ic a tio n It is tr a in d ic a te d in p a tie n ts w ith d is e a s e s th a t m a k e th e m su sce p tib le
n C a 2+ ı a c iJita te s th is e co n
tr a n s m js s io n w h C O PD tie n ts w ho
ere a s M ho hav a s th m
g + h a s a n in h ib itin g e ıfe c t
2 p
to p a r a s y m p a th e u c s tim u la tio n p a tie n ts w e a o r o r a
i T /s c t ? l
ı n d ic a tim ı t is u s e d to o b t i h ą M e Jp ę p tic u lc e r d is e a s e A ls o p a tie n ts w ith an o b s tr u c tio nin th e g a s tr o in te s tin a l o r u r in a r y
a n m io s is o f th e ir i í
e r Jlė f fg ıln
rr
s n s e c o n d s a ize r d e liv e r f th
c a ta r a c t y o te th e o b s tn ıc tio n i c a u s in g p r e s s u r e to
W a J/ in p e n e tr a tin g k e r a to la s n o t p r e s c r ib e d m u s c a r in e b e c a u se its a g gr a v a
u iń d e c to m y a n d o th e r a n te r io r ! tw ţ¢
w ħ
p segmenfı iŕ geı y
e re ı
apidmiosismaybe p ıb ı iu ıı
b u ild u p th a t m a y le a d to p e r fo r a tio n

Scanned by CamScanner
二二 . 塗佷女攀 韓 纜 舞 撚
: .

rm !ı
a Te x t B o o k o fP ha rm a c o lo g y
n j f Druce A c p e r ip h ıN e rv o u s t e m
lll I pharmacolo o o n e ra

e x p e r im e n ta l p 呷 o se su c h as g la u co m a p o s to p e r a tiv e ite n
u b ¢i n js u se d o n y fo
ı r s
r e te n tio n a n d x e r o s to m ia
u r in a ry
co n ge n ita l m e ga o o ı
on

i tic a n d a p o s itiv e ly c h a r g e d q u a e m a r y
p tL o c A p ı N E ı t js a c h o lin e e s te r m o a l n M
i i te d o s a g e c a n in a e a s e s e c r e tio n b y th e e x a c r in e g ia n &
co m p o u n d
p iJo c a rp in e n a pp p
r o r a

J i Ļ gas ic p a n c r e a a n d n te s n a l la n d s a d th e m u c
M w e a c sa
e s ıiw w a c r m a

be tim u la te d
ą
p ır a to ıy tract
m ay s
o f th e ıe s

ı la tin g ń ic to
M p ic a u y to th e e y e s ) b y m a in y s tim u m u sc a n r e c ep rs
i
à tm en t a n d d ia g n o s is o f n y a s th e n ia g r a v s
A dv e c t It m ay p ro d u ce h yp e r te n s jo n a fte r a b r ie f e p is o d e o f h \àR gio r ı ţ ą2iqbe t re

in g
p o is o
e rs e d
b9eu d in th e tr e a tm en t o fC u ra re a n a tr o p in e n

B r a d y c a r d ia an d ta c h y c a r d ja h a v e b o th b e e n re p o r te d w ith u sE o f p jlo c a r p in e U se

th e tr e a tm e n t o f p o s t o p e r a tiv e ile u s (p a r a ly tic )


U It p r o d u c e s a s u s ta in e d m u sc a ń n ic ac tio n o n e ye a n d p r o d u ced m io s is It Ĵ s ln §ėa in (c )ip s p d in to f
ses
la r te n s io in g la u a an d in th e tr e a tın e n
e d u c in g in tr a
co m
u do Ja il in b lo o d p r e s s u r e th e M g h e r d o t æ t þu s e o cu n
th e tr e a tm e n t o f g la u co m a Sm a se s c a u se
(d )fu s e d in r
in b lo o d p r e s s u re a n d ta c h y c a r d ia ı qu s o lu b le
o d o m le s s
a
r is e
1IG M IN E B R O M ID E It is a w h ite c r y s ta
u in e p o w d e r c o lo u r le s s
itr a te P ilo d r o p s P ilo m ax eye d r o p s Ħ l叩 C a ıp in e E O S 7 l S 1P h a 【e
p ilo c u p in
re s s N
B ra n d N am es : e n ca r
d n d N e o s tig m
in e M e th y u

d ro p s 2 % 4% N e o s tig m in e is a v a ila b le a s N b r o m i e a e th y l
1
P ila g a n C a r p in e ıo c a ıp e y sj ĥv ı n ì in w a te r d fo r n e o s gti m in e m
u la fo r N e o s tig m in e b r o m
id e is c 12 H 1 g B r N 2 0 2 a n
riı
uJSlo1 M o le c u la r fo r m
H N 0 S
id b ta in e d ı
io m th e b e te t n t (A te c h ) fr u jts C i¢ıñ l át
p m su lp h a te is C 1 3 2 2 2 6
a n a Jk a io
u re c a ca u
A R E C O L IN E n is o

d n ic o tin ic ty lc h ıin p to r s I t is d in th e rĮ J n ib J
tre e It is a n a g o n is t a t b o th m u s c a r in ic a n a ce o e re ce u se .

ic s tim u la th o im tic d ifu g e i t ıl Ðg u lir r


g a n g līo n n Ļ a ra sy呷 a m e an v erm
fo r m o fv a r io u s s a jts a s a p a

ha n f c o g n itiv fu n c tio n s, bu t n o t fo u n d u s e ń rl ha s įı
t - ul u ・
h a s be e n M ed in d e m en tia as a n en cer o e

n o th e r a p e u tic u se

(s tru c tu ra lfa rm u la N e o s llg m ln e B ıo m ld e )


l w h ic h in c r e a s e s
3 3 2 A N T I C H O LIN E S T E R A S E D R U G S o f a c tio n N eo s tig m in e in h ib its d e s tr u c tio n o f a c e ty lc h o in e
M sm
Ęș i io n o f im p u ls e s
i heı p in t
A n ti c h o lin m s s
c h o lin e is r e le a s e d T h s
s
A c e ty J c h o lin e is in a c tiv a te d b y th e e \ e a c e ty l c h o lin e e s te r a s e e s te r a s e
:JZß
ation a t s ite s w h e re a c e ty ı
r a n

d r u g s a r e a lso c a 皿e d a s c h o lin e s te r a s e in h ib ito r s T h e s e d r u g s a c t b y ĵ n h ib itin g


ę å : . U n c tio .
i e a t c h o lin e rg ic s it
a c e ty i c o lin e s le r a s e T h is p r o d u c e s a c c u m u la tio n o f a c e ly l c h o l r ı
In d ic a ti . M y a s th e n ia g r a v is p o sto p e r a tiv e ile u s b la d d e r d is te n tio n

D o sag e M y a s th e n ia g r a v is
u r ly
lly I V 1 5 ith a tr o p in e 0 4 m g to l 2 5 m g 1 to 3 h o
g d a ily g
A d u lts 15 to 3 0 m o ra m w
R E V E R S IB L E A N T I C H O L IN E S T E R A S E S ! ,

3 to 4 h o u r ly P O St
C h ild r e n lly : 2 m g p e r k g b o d y w e ig h t p e r d a y in d iv id e d d o s e s
P h a ın a c o lo
ı g ic a l A c tio ıu o fR e v e rs ib le A n tic h o lin e s te r a s e s o ra

b o F » ra tiv ile u s a b d o m in a l d is te n tio n


th e tic d r u g s P h y s o s tig m in e js a n Jh a t\ a i
e
A Ľ th e r e v e r s ib le a n tic h o lin e s te r a s e d r u g s a r e s yn
4 to 6 h o u r ly fo r 2 to 3 d a y s
a lk a lo id o b ta in e d fr o m c a la ba r be a n It is a se e ds o f p h y s o tig m in e v e n e n o m T ħe ÐM U l l l M / S C 0 2 5 m g to 1 m g e v e ry

M y o s tig m in P r o s tig m in 0 5m g p e r
p h a rm a c o lo g ı
ca l a c tio n o f r e v e r s ib le a n tic h o lin e s te r a se s, a r e th a t th e y p r o d u c e m u s c a r in ic :ilł
iuii?Ĥ mes N e o s tig m in e b r o ń id e : In je c tio n M u v er e

tip e o fe H e c t o n o r ga n s
ı
m ın l
A c tio n ti l o b s tr u c tio n
e õ? ł H y p e r s e n s itiv ity to b r o m id e s , in te s n a
ŕ
on eyes A ti c h o ı
n in e s te r a s e d r u g s p r o d u c e m jo s is , s p a s m o f a ccom m o d a tio n an d łń d ic a tio n s
d e c r e a s e s in tr a o c c tıla r te n s io n

Scanned by CamScanner
s fd e e ıfe c ls Vomjtin d ia n h o ea n a u se a c ra m p s Jn c r e a sed
p e r is ta ls is sa ı
iv a r
y a q d
lp n n rm a C 0

i
ı
0 g
d °f D r m Ac w O n P e r ip h e ra ıN e rv o u s
t e m 匡
in c re a s e d g a s ni ic s e c r e tio n s A trO S iS bı
u m d v is io n la c r im tio bn ū y ıßv ï
a n v is u a l ch a r
ı
ŤH a
ÝH '

W io m Ļ E C G ges
ie n s c ha n ges s y ııc o pe c a r d ia c a m s L dysp n ea re s p ir a to ıy a rr e s t Sk i
nfad3
n Ra s h
u r t ic a r ia h e a d a c he mratin w e a lm d ro w s in e s s Jo s s n j
e ss o fcon s c io u s n e s s :N l C Hr N H C O
心H a
U i th p ıt io n s F b eg
se w łe c a ı n a n c y H }p o m io n as th m a ı
a c ta t io d
n a n c h ild r e n Sbu m aı
ı n m
i b p ıy ūg i e
H ha ım k in tic s «h ny T
In d ic a tio
a ◆ e a t t io n 4 5 ı
o n se a c u 60 n in u
ı te d tio n f
n = o r e v e rs e C N S e ffe c t
u ra o a c t io n to 4 h o f d ia z e tic h o lin d itu y ia
o u p am an e r g ic h e re a ta x
Į s łW
X
a c tio n JO iu 3 0 in le Du tio n 2 to d ħo u r s A lz h e im
p re s s a n t
m u
a n tid e d is e a s e
i ıa e r s
W o n se t 4 to 8 m in
u te s Ex c r e te d ir ı
DSiį Ëoverdose o f a n tic h o lin e i i
g cs

A d u lt lM or rv in je c tio n 2 m
g A d m in is te r lm g p jn
e r ın u te m a y r e p e t a ħe r 5 to 1 0 m in u te s
Treatmentofoperdoseanabwjnesı
ılphate 1 t
a
'
u 4 m g īV ċ Ĥ iia ą ijw / r v in je c t io n 0 02 m g p er kg bo d
l ıs J c 9 y w e ig h t n o t m o re th a n oB in te

V E 0 S n G Ħm E Aa n n n S U L P H A TE
m g p er ın u m a y
n js p fte r 5 to 1 0 in te
u se d as a d ia g n rep e a t a m u s in te r v a l to a d m in is te r
o s t ic m e a s u u p 2m g ın a x im d
tr e a b n en t o f m y a s th e n ia ra
re A n d in th u m o se
g v is ï d ia g n e
o s is P b s f【M ä e s th e s ia
u r 1 to 1 5 m g is a d m in is te r e d JM A d u lt IM / r v 0 5
to l m
" g in je c tio n
c?yf o f
o ' t m th a n
s ig n a n d n o o re o 5 to l m g p e r ın in u te
sym p tu m s o c c u 【s w ith in 15 ,

n ıjn u te s in ca se o f re a l/ e cas e f
iñ拶\ a t a fte r 1 5 to 3 0 m in u te s i
n te r v a le s
ı
rea bn en t I 2 5
o m y a s th e n ia Fo u p to m a x im u m d ose o f 2m g
m g S E L IM / rv r
a re a a 而 由 te r e d se v era l tim es a day a cco r d in g to
äńiJtaications H y po t en s i on , ard io
co n d itio n C h a i a d m in is tıa tio n th e va s c u l ar di se a s e , mt
ł
f st a,
anw e i ab e t e s .
į į .ts
o n e o s ti m ne ,
g in e b r o m id e is a ls o u s e a U tic a r ia
P a ra ly tic ile u s p o s t c e r a tiv
r '" h head a ch e
p sw ea tin g d r o s in e s s
e u ńn a ry r e te n tio n n eo s tig m in e m e th y l
w
'"nitring d ia r r h o e a c ra m p s
in b a ın ı1a r o r jn
ux ı ba n
i
v m ous je c tio n in d o s e o f 0 S to 1 m
r n iit ĵ L ı
g la c r iin a tio n
P JĪ Y S O S n G A Æ v E
n js an a k a lo id
ı o b ta in e d ıo m
caı
a ba r b e a n th e
v en see d f p h s o s ti P h a ım a c o k in e tic s Peak
ħjs an o d o u rı
o
y gm a
co n cen tr a tio n 5 ın in u
e ss c o Jo u r ı te s d tio n
ta ls b ' " 召ij己0 2 u r a 4 5 to 6 o in
ligk
ess c 6m te
\ m u s Ex cre te d in
It s h o u ld b e " p in k '" x p. .. .. To u r in e cro sse s b lo o d b r a in b a r r ie r
s to r e d in a ir ti
g h t c o n ta in e r s o te c te d fr o m J jß b n ß Jí
in İ ig h t s o Ju tio
P n p a r e d if if is to b e n s sh o u ld b e fr e s ħı
k e p t s h o u ld b y
e s to r e d in h Ylíiei 9 ; b J r ' " ıu e s a n a e s th e tic s
q u in id in
u
M
e rm e tı d e cr
ı
o ım u ı a is C
ca y seaı
e d co n ta in e r s J ts e e a se a c tio n f
臨\
H o
J5 2 JN 3 C 2 in
£ m '

i J l :a ĵ e tl
M e c ha n is m U
o f a c tio n ı
ses It is u se d In A lz h e im
t in (x e a s er d is e a A ta
e s a ce ty Jc h o ı se x ia D ia
in e a t ze p am p o is o n in g

Į ċ i=Ţ im °TIGMINE I
+ " P n e ra ' "
ticho'"ergjce'"ct T' " t .' '" b 1, s ith tig m in , It h a s a l
c ho ı
in e r g ic n e rug w . '"
o n ge r d u ra tio n o f a c tio Ľ
rv e
ending ĵ t r e v e r s e s c e n t n e ss
r al a r ı
d p e r ip h e r a l a n tic h J
o in
ı r JŔ Jd ĥ j
ÃWiredin y " ・ a' ,n i' g . . v is d . .. T . ta l d a il d '
y '" oo ' g to ļ 2 gm o r a 1ı 6o
e rg ic e ffe ta b le t 1 to 3 t b y m g
c ts a le t th r e e tim
es a d a y In c a se o f p o st
T E O ðe u 9 fi o p e r a tiv e u r in a r y r e te n ū o n ly tic
ile u 60 p ara
s m g th r e e tim es a day
B ra n d n am es p y r id o s ti m in b r o m id e
g e T a b le t M
nj g n o ð
ı y e s tin D is tin o n c rav ito r M \ıs to n e
6 0m 3om g
g ta b le ts

Scanned by CamScanner
国 二
画回
'。 国民国团国




Age n t To r yasthenia g r a v is
tIT 亡js u se d a s


.,
:r '" j. i

A M B E IV O M ID W ıb t io
a c n s a g a in s t m y a s th e n ia g r a v is b y co m titiv
p e e r e v e r s ib l
e in h ib i
o f a c e q łc h o ıi n e s Jt ti o n
s im ila r to
Pjidostfgmine a n d t ig m in
łY A T E S
n eo s e is d
tr e a tm en t o fm u sc ı
e w ea kn e ss a n d Ta t ig u e in p eo p le ith
u se fo r th e ţ
w m y a s th e n ia g r a v is I It is h o lin
cA R BA R Y L a c e s te r a s e jn ħib ito r an d is to x ic to h
m an s I t is in sėc tic id e s al e
IR R E V E R S IB L E A N H C H O L IN E S T
ERA SES
Ī
ćJwoi s lo w ly r e v e r s ib le in h ib ito rs o f th e en z
ym e ace ty lc h o lin e s te r a s e They re se n ? 1e a c ė t y lc h o lin e
O R G ıU V O PH O SPH O R U S C O M P O U M b u t th e c a rb a m o y la te d en z ym e u n d e rgo
)S T ħe s e e s th e fin a l h y d r o l s is
co m p o u n ds a re e s te r s f p ħö y s te p v e ry s lo w ly (m in u te s )
d il T h e s e
.
.. w ith th e a ce ty la te d
a o rg a n o
p ho pho ru s co m po un ds a re
w eJ en z
ym e ge n e r a te d by
o w e r ń ııin ty lc h
a r e v e iy h ig h ly to x ic d Jo n g a c tin
p h ib ito rs o f c h o lin e s te r a s é §・ i?iśe i? ļ w R = w ith th e c h o lin er g ic n e rv o u s s y s te m
a ce o lin e (m ic r o se co n d s) T h e y
an
g T ħe s e are n o t u se d th e r a tic a lly fo
an d ca u se d e a th b e cau se th ffe c ts f th
p eu
hu m an b e in g s
r Th e
treåţ ìfťóf T!F}Hgļ ţ smitter a c e ty lc h o lin e can n o t b e te m
e e o e

ļ o y la te d a c e t lc h
a te d by car bam o lin e s te r a s e
y
Th e P O IS O N IN G W IT tI O R G A N O P H O
o rg a n o
p h o sp h o r o u s com po u n d ca n be b s o r b e d th r o Sp H O R U S C O
a M pO U N D S
u gh a ll r o u te s in c lu d i
n g įijd ħ a il
lu n g s as th e y a īe M g h ly li id a T h ę p p b q n in g w ith o r g a n o p h o s h o r u s
p s c 出山le T ħe s e p
a re m a in ly u se d co m
p o u n d o c c u r s b e c a u s e o f th e r e a
w o r k e rs h a n d lin la r e
an a g r ia ıı
h ır a l
insectijde T h e s o n s
g g q u a n titie s n 】
ay su fı
e r Tr o m to x iLc łirty b
Ni
tà O rga n o p h o sp h o ru s C o m
po u n d s lik e
o e ca u se th e s e d r u m a la th io
m a y e n te r ]n th e b oo d b i g s (s u b s Ja n ce s)
n P ara th io n are d in tic ĵld
y y nn g ( :g J u a ġ r iċ ltu
u se a s se c e s in
g e s tio n s :k in c o n u re ith
ta m in a tio n an d in h a ı P e rs o n w o ccu
p tio n in
a tio n s sp ra
y in g in s e c tic id e s m
M a la th io n ĺ ßıfn ì ay b e h av e is o in g b y
】t js a a r a s
p in h a lin g s k in
p o n
y m p a th o m im e tic o r co n a m in a tio n
jn s e c fic id e ı g a n o p h o s p h a te c o m o u n d th a t j
o r th e tr e a h p s u 5edYa s

ı h tım a n to x i i
n en t o fh e a d
lic e It js a n i
r T e v e r s jb le
c h o lin e s te r a
an
Ť r oĵ )e ĥ A te e id e n ta l P o is o n in g b y e a tin
g a g r ic u ltu ral
ow
c t
y īt is a n o n s s te
s e in h ib ito n
a d has
q p r o d u c ts Ľ k e v e g e t a b le s fn ıits d
in h ib its a t
y m ic w id e s e c t
p n ım o rg a n o h o
f
e ßı
fp í c íd u c ts sp ra ye d w ith th e in s e c tic id e s
an

c e y ıc h o lin p s p h a te in s e
e s te r a s e a fi d e Į t
c tiv it
y n c a ta ly z e a n d hy? o ly s is f th e
&ř g e s tio n o f th e s e co m ds
o po u n ith a ll in

fo r e h ım
^ '" °
ä \ #T 1
"g
w te n tio n h a v in g su ic id a l te n d e n cy
tD i台 北 s t[ ch' n in
"n "
Bm d n a】
n g s ta te
a fte r a c äv a lio n g
ııe M aı
a th io n o o o5 / 1
9 m L 1o t ir m
u u v 1o e 0 00 5
9 / tm L to tio n S i8 n s an d sw
p to m s o f p o is o n in
g a re
!; D (j)
(i) G a s tr o in te s tin a l s m to m
y p lik e itin g
s v om n a u se a abdoal cra m
p s d ia r r h o e a


胃 ı」 密雲覆愛 變
轟 莓墓靉
Scanned by CamScanner
)s u o n e go x e ( d e tc e jn i o t s e s n o p s e r h tiw
sre se
t e n ilo C
h
n a h t y li a e r s s e s r u c c o b ıolir r ):
d l s ih t tu b en ip o r ta y b d e tib i n
e b yam o s la n o ita lu m its e v ren c ig r e n h i

ohc c in o ilg n a x ts o p o t se sn o p s e R )e c s u m ifr 【
r id iJs
b
dn a h to o m s s d n a lg e n l c a id ra c sa d e ifis s a lc e b n
ir c o x e e i( e n ir a c s u y b detiŁ ac gu rd
m
ini ro d e ta lu m its e r a ta h t s e r ih c u r s
:ßī b ió Ĵ I
ciŁ
yıoMapmy
la r e h p ir e p h t e r a e n ip o r ta y b d e z in o g a tn a
e t
s r o tp e c e r e 己目广エコリ天了9
ro hT tp e c e r e h t fo e ta ts e v c q g
o t m u ir
b iliu q e e h t tfih s ta h t )e n ip o r ta g n it de h te s tśin itg a tiia s c ily o n
id u lc n i( s ts in o g a e s r e v n e r a e
i n ilo h c ly te c a
sTo tp ec e r c in jr a c s u J iJo h,c r o s c ity o
m ıh ta p in ys a r 3
lb ta h t s g u r d ts o m d n a e v c a y e
X X Ï ŢH
e h tk co sa
fś nó iE aja v

į ľ xiĹ
.

H ' X
it l v itu tits n o c e r a s r o tp e c e r c n ... .
ht n o
i ir a c s u m ta itc a e ht " ' lb
p
e n i o r ta y h t s e ta c id n i tI .
b d e k c o lb o s la e r a s n o r u e n a r u m a '
l ilg n a g d n a h to o m s s n a g e n
s r o tp e c e r c n r a c s u
r tn i n a a
d
d l aW JO H T A P M Y S A R A
i i M d e k c o lb e r a s r o tp e c e r c n r a c
lla n o e tis g n id n ib n o n u n o c a r o
i i s u m e lc s u m c a r a
ir c o x e n i
id C r o tp e c e r c in ir a c s u m
i【ı 9 X O ı P @
f s e p
te m o c e n ip o r 田 了1己っ危立 门ï
e n ilo h c y te c a tA s ts in o g a c n r
l fo s n o itc a e h t fo ts in o g a tn a e v i i a c su m r e h to dn a n rı
itite p m o c a s i e n ip o r h o Jlı
tA n o itc
)e v itc a n i 1o n a p o r t( e n ip o r t n a e A f o m s n
i h eM
a c
) M A D ( e m ix o n o m lv e c a
d ) v itc a ( d ic a c ip o r t o e s p iD 3
e n ip o r t y f d o
i ) i a yc so yh(
{X ¢
A e m o c s e
n ic s o s e h 1 i n īm a
lo p o cs
n m
i id e r g n i e v itc a e
n tn e )A m e n o te c a o
ts o n n a s i y tiv itc a
i c in h T r e m o s i 1 e h t o t e u d y llo h w a ib n
i o st o n oM ,
ir a c s u m ü in a e
h t tu b e n im a y c s o y
ip o r tA h 1 d n a d
fo s tr a p la u q e fo s ts is n o c
en a c ilo im a c a ilo p o c
s d ir a r e g in s u m a y c s o y ĵ o tt e e a
í J )M A 2 æ e d id o ih te m
id ir yĮ 1
am ix o d la 2 e n
H bu rh s e ht n i n u o s e n m a o p o c
m u in o m a r ts a r u t D
a dn a d f i i l S e J o q a Į ßtR
lıb a p a r tA m o r
a n n oda e sro ta v itc a e r s a s tc a s pm g n iw
f d e n ia tb o s i e n p o r dn

u o oc
i tA EN I R A R T A e ta v
it c a
o llo ıe ħT enllohcreca
n in a c se m yz n e e er f e ħT e sa re ts e n iı lí h p s o h p e h t g n ita ly ıo h p s o h p e y tc a
o h c d e ta r o

r l 回国国园国国
了ß0 9 T Į了っ yeh
T e sare ts e n i1o h c em yz n e e ht e ta v itc aer sdn u o pm o c e s e ħT
d b
s ıo ta v ilc a e R e s n e ts e n ilo h C

n o s io p e ht o t ia u d iv id n i f o e ru so p xe re h m ń fo n o it a n im re T 5

:
ê á
i
q īt ßjJ ī y r o ta r p eru lia f
Te a
i se r o t e u d y lla r e n e g s Iu c c o
h ta e D yaw r ia n ia ı
n ia M n o it a r ip s e r n ia ı
n ia n ı o T 4
a İ ßS 9
q ßn m a pe z a
iD h tiw n o is lu v n o c
f o lo r tn o c e r u sse r p do o M n ia ln ia m t n e ita p e h t e z i iW 3

1 ßn 9 ıv i : h tiw a w dn a p ao s


e n a re
bm e m s u o c u ın
d n a n d】
s e ht
hs aW eca p
ı n e po ıia h ie r f n i t n e it a p e ht p e e K 2
ru c co
h tu o m fo s se n y r d llit s e tu


, ! ü ąo n in ı5 1 u f0 1 y ıe v e V Jgm 2 n ev ig s i e n ip u b A ı
r

n id d ig n o is ı
ńnoc y te ix n a n o is s e r p e d e kĽ SN C n o n o itc A )v (

n o it a d o m o c ca fo m saps s is o im e k i ı y ra llip u p seye n O u i(

ssem la e w d n a e ru s s e rp
doo
lb n i uaF )ji(
sn o it e r c s la ih c n o rb ta e w s av ila s e k it sm e lb o r p t c a r t y u
ı fa r ip șe R

= 巫生
\ 卫 ll l。・・
厂 二
匹띱・鬲蛔w 加川" ' . . 。 ,
.ぷ
五竺
と出
ぷ五
竺と
出团
E国
回国
四E国
回国
囲囲
rr

Scanned by CamScanner
w a

iiá b e u se d ll in d iv id ı
' w a ith tio in u a s
. A rs o fage w ca u n a

to to x ic ity th e r e is ? fic u lt in
y sp e e ch
llo in g
sw a w an d d ry m o u th
th e s k in beco m es dry d th e r e is
ąu ĥ Į an
a n in c r e a se in th e b o d y te m p e ra in ır e
!ií g u
b T he re is m ydń a s is a n d p ara ly s is o fa cco m o d a tio n (c y c lo p le g ia )
n o q?ßT h e r e is u r in a r y u r
g en c y an d d iffic u lt
y in m ic h n itio n

i T
re s tle s s n e s s a
n d th e r e i
s m o to r in c d in
o r a tio n
, A d m in is te re d iv s c im It d is a

1i Ţ H
o r
pp e ars ra p id ly fr o m th e b lo o d

'" '
' " p ar tic u la r l h
'
T
y " " ' ' " 1 3 '" " . ' " . .
r a c e s a re fo u n d in v a r io u s s e c
re tio n s in c lu d in g ilk I t is d ily
p la ta l b a r r ie r a n d re a
th e ce n m
cr o s s e s e n te r ś th e f t
e a l c ir c u la ti
Iť ffe c t
fu n c tio n d e c lin e s r a p id ly in a ll o r
o n s e o n p ara s w p a th e ū c
gan s e x ce
p t th e e y e E ffe c ts o n th e ir is d iJia r y m u s c le
r p e r ś is
t do r s e v e r a l d a y s an c

s iđe E ffe c ts M o s t o f th e s id e ffe c ts


e f a tr o
p in e a r e d ir e c tly Ţ e la te d to its a n tim u s c a l in ic
o
b a c tio ń ıtD r y n ess o f th e m o u th b lu d
rre is io
p h o to p h o b ia a n d ta c h c a r d iav n
w ith c h r o n ic a d m in is tr a tio n o f th e r a y c o o n l y occu r
p e u tic d o s e s C o n s ti a tio
p n a n d d iffic u lt
e . % u
' in e ld e r ly ū
p a e n ts O c c a s io n a l h y in ın ic h i r itio n
y p e r s e n s itiv it r e a c tio n s h a v e b e e n o b s e r v d
ï ū # R N y s k in r a s h e s w h ic h in s o m e in s ta n c e s p r o r e s s e d ty e
g o e x fo lia tio n
ŁtT ö tâ c U f e c ts o f A tr o p in e

T(
) ū e M to x ic ity th e r e is d iffic u lt in
ı
sp e e ch
y s w a llo w in
g an d d ry m o
"
iq[iqsidn b eco m es d ry an d th e r e is in
u th
cre a se in th e b o d te m e r a t
y p u re
3) T h e r e is m y d r ia s is an d p a r a ly s is o fa cco m o d a tio n (c c lo le ia )
y p g

£ixci te m e n Ļ r e s tle s s n e s s a n d th e r e is m o to r in c o r d in a tio n


ĵ íjo i b ír ĺ n ĥ
A h p ii
? e is d fo r fo llo w in
u se
g p tır p o s e s

edSiñ I
b ilia r y a n tis a s m o d i
p c
2) A s p re a n th e tic m
aes e d ic a tio n
bn 8)
ı
organophosphorous p o is o n in g
rri b ÐJ j1 ĵ j;

Scanned by CamScanner
;
ıı

S C O P O ıt ĵ s a ls o 】
m o M m as H yo s c in e I t is a b e 끄a d o n n a a lk a lo id js an
an tic h o lin e zg ic a ge n t
M ech a n is m
r e c q p to r s ite s o
o f a c t io ıu

f th e parynı
a il .
n '

pathetic n
c ts
"mpetitive in h jb ito r a t p o s tg a n g lio n ic į £
erv o u s \ te m an d ii i'
: a c t o n sm o o th . J & ai

r e la te d p a in d ın in g abd o m in a l c r a m p in g n o 9 J ĉ a rlT

au b n ßr h

s o m e c as e s to tlińng d e g r e e s T h e v a g o ly tic a c tio n o f s c o o la m in e is


p
aopjne as js ils e c t ĵ n p r o d u c in g m y d r ia s is 】 h a d d itio n w h e r e a s a tr o in
p e d ¥d e p ro
s tim u ı
a tio n o f th e C N S s c o p o la m in e d e r e s s e s th e c e r e b r a l c o r te x S c o o la m ín
p p e p o sse sse s a
in le d tßn g ffe c t th a n
m o re n s e e a tr o p in e q m qu o ìä

S id e It h a s p o s s ib ı
e « e ct e s id e e ffe c ts a r e e x c ite m e n t r e s tle s s n e s s d is o r ie n ta tio n a n d
d e lir iu d u r in g th e p o s to e r a tiv e r e c o v e ı
#
m
p y p e r io d T h is d o e s n o t o c c u r w ith .
m c o p w o la te E h e r g e n æ d e lir iıım , a s jt ĵ s Jcn o w n is m o r e lik e ly to b e o b s e r v e d i
y o rın g o r o Jd e r a d u ıtp a tie n t
X % ¥ė žĮ u n re sp c lig h t u p o n
f th e ď ia r y b o d y to ch o lin e r g ic s tĵ m la tio F e r tı
g gu c o n ıa

Ilab后\g a u s c le o
tiv e u n
pham a c o k in e tic l ı
t is w e ll a b s o rb e d b y tr a n s d e rm a lp a tc h Th e o ra ıb i. . . . ŕ m

n w ith h y d r o c o d o
an d 0 25 % o p h th a lm ic s o Ju tio n is rap id ly a bs o r be d a tte r o cu la r a d m in is tr a tio n T ħe I ・°
#śĦ? It i s in d ic a te d a s an o v e r d o s e r e s c ııin g a g e n t in c o m b i
n a tio n e

d is u ib u tfo n is in d ic a te d fo th e in d u c tio n o f m y d ń a s is w ith ophalmic s o ı u tio n s

ı
n o t w e ll
characte bu tm a y be r e v e r s ib ly bo tınd to p la s m a Ħoteiw§P T \ It is a ls o r

cn o nm to c r o s s th e
p la c e n ta c a r in ic ty lc h o lin e
ir a n s d e m a ıa
ı
a n d bı o o d b r a in b a r r ie r T u n e
? 吐 出 tr a tio n is 2 4 h o u r s Jt i
to p e a k c o n cen tr a tio Ĥ a f te r Ų§R= ıo iș an linergic d ilig
antichı th a t a c ts as an an ta g o n is t a t ın m a ce

s e x te r u ív e ly m e ta b o liz e d an d con ĵu ġ a të d jc m ĒT ręępg și It is u se d as an tim siv e a ge n t


re n a ıe x c r e tio n is le s s th
a n 10 % a n d ıe s s th a n 5 % is tın c h a n e d
,
g B ra n d N am e : Is o
p to H o m a tr o p in e 2% ,
H o m a tr o p in e e ye d ro p s, H o m id e 1 % 2% e ye d r o p s

Scanned by CamScanner
ı3 0 E I 田园团团团团团团团国 国国■ A T = 四 国 团团团 团团团团团团国
― e x !B o o k Of P h a r

y a ' " 0 四国团团团团■
1 眉目团团团团团■ VOI
J 昌团团团团团团园田 L ı ■
N E S U Lp H A TE
A TR O P ı Ptarmacolo o f D r Æs A c tin g o n P e r ıp h e r a ıN e rv o u s t e m 回 亜再句团 团 国 国
It is i c o lo u r le s s o do u r le s s w h ite c r y s ta u in e Po w d It is 27"
er so lu b le in w te qa3sı
a r It is i h i ila b le d e x e r ts la c aı
avi it re m a in s av a a t th e s ite o f tio in th e in te s tin e an a
n g re ce p to rs a c n

lr n u c l e u s fin d in ı
k a lo id W n e p ąs m o
ly tic e ffe c t
o p än e a m m a n y a s e n tr o p a n o l (h y d r o x y tr o p a ) is h s c in e
p h a g e a l a n d g a s tr o in te s tin a ls p a s tic c o n d itio n s R e v e a le d th a t y o
n e
w ith tr o p ic a c id a tr o p in e is fo rm e d u à& 9 l iæ b se d fo r e s o

is tic h o lin e r g ic d r u g w ith M g h a ffin ity fo r m u s c a r in ic r e c e p to r s lo c a te d


r la
b u ty lb ro m id e an an
M e c ha n is m o f a c t io n rlj
u s c le
s c le c e lls o f th e G I tr a c t 1 ts a n tic h o lh iė r ic a c tio n e x e r ts a s m o o th m
ty l c h o lin e
"
\ariix, ! on th e sm o o th m u
g
Atnopine b lo c k s a c e a t p a ra sy m p a th o m jın e t ic ly tic ffe c t
ffe c to g /s p
N e u ro a sm o e
e r s ite s in r e la x in
M a c o u tp u t b y b lo c lc in g g a l s tiın la tio n in th e h e a r t c re a s
g /m l
can v a u es
B r a Ƣe It i5 av a ila b le in ta b a n d in i. tio n fo rm B u sC o p A N 1o m g ta b 20 m

In d ic a t io n s In s e c tic id e p o is o n in & b r a d c a r d ia b e f qıł


y o re s ıır g e r d e cre
y to a se se cre
am p
an tis p a s m o d ic b r o n c h o ď 1a to r A lle r g ic a n d in fla n u n a t tio m
o r y d is e a s e o f th

蕊蕊
e e ye
g e ' '" N ı
TR A T E '" ' '" f ' ' " d d ' ' " _ gs " '" lo w h e a r t r a te
o th e r c o n d itio n s A tr o p in e
Iıu e c tid d e p o is {m in 吕 A d u lt a n d c h ild IM o r rv 2 m g h ly an d d e c re a s e sa liv a p r o d u c tio n d u r in g su r ge ry an d
o u r u n till m i ic
u sca r n
L a r g e p u p ils U r in a r y

;L
. ha fo llo w in g s id w ffe c t s s p e c ia lly d r y m o u th
Mlm?t v e

T"
e s e
ral im is u s e d
reĮ aioKconstipation a n d fa s t h e ar t r a te A tr o p in e m e th o n itr a te 2 5 1 0 m g o
° . ° Iv o 4 to o 6 m g b e fo r e a n a e s th e s ia c h ild o ' " . lco ı d h yp id ity
. . fo r \ Ţ IW a ic s an e ra c

nllii e M Y D R IN D O N 1 m g (a d u lt) 0 1 m g (c h ild ) ta b in S P A S M O L Y S IN 0 32 m g

ta b
t 67 ĥ i d
iŕ Åť iŁöi>iuM B R O M ID E Ip r a tr o p iu m b r o m id e . syn th e tic a n u n o n i co m po u n

b h o d ila to in th e ın a n a ge m en t of
ì im ila r to a tr o p in e is u s e d a s a
s tr u c w a v s
ro n c r

tiv e p u lm y d is e a s e
i8? äł ĖiŁm e d ia te d b r o n c h o s p a s m a s s o c ia te d w bs m
ith chr o n ic o ıc o n ar

a
Mê ith th ld ith a】
1e rg ic o r
aı ta tr e a tm en t o f r h in o rrh e a a s s o c ia te d w e co n u n o n co o r w

n łĝ .e a so n a l r h in itis

f tio Ip r a tr o p iu m b r o m id e is a n a n tic h o lin e r g ic a g e n t It b lo c k s m u s c a r in ic


Meķism o ac n

d ó lił
iëł
ğlć p re ce to rs w ith o u t s p e c ific ity fo r s u b ty p e s r e s u ltin g In a d e c r e a s e in th e
n o il ßr m j f c y c lic g u i
a n o s in e m o n o p h o s p h a te (c G M P ) M o ßt lik e ly d u e to a c t o n s
o f cG M P
) j fo rm a tio n o
D r a s in ta a c lirm A n ta c id s d ffe c t f
e c re a s e e o a tr o p in e A tr o p in e d e c re a s e ięĮ ţ ęļ nof. O&Cł
nMèqlular c a lc iu m th is r e su lts in d e c r e a s e d co n tr a c tility o f s m o o th m u s c le
P ħe n o th ia z h e s
k in « It is ab so rb e d b y In h a la tio n (lo c a 1) m in im al N a sa l ra p id an d
ph a rm a co e cs
B ran d A lr o p in lp h a te In
n am eı e su je c tio n A tr o su li A tr o T ro p in e in j ec t io n 0 6mgrp, 9 r [丁 The r íö lū rh e o f d is tr ib u tio n is 4 6 L / k g ) o u n It b d to d a Ĺ1 a c id
p la sm a a lb u m in an
one m l A tr is o l A tıis o lo n e ye d ro p s i jjo rq o r o te in s It is a n d th b in d in g M in im a u y (0 to 9 % in v itr o ) It is p a r tia u y m e ta b o liz e d t o
T ([ g ly c o p e

ta b o lite fo e d p ń m a r ily v ia h y d r o ly s is a n d c o n ju g a tio n T h e m a n


i m e ta b o lite s
ļ! ī rn 8 Jz Ĥ JI j a t le a s t 8 m e s rm

m e th o b r o m id e T h e s e m e ta o b ıit t b in a c tiv e T h e
H Y O S C IN E B B R O M ID E It w as fir s t r e g is te r e d in G e rm a n y in 1 9 5 1 a n d maiı
】Ziii I? T Ĥ
aĮęiÈļ åqĺ ţ opyı
nortropium e s a pp e a r

h
o

lf
e

ı ife (t ı/ 2 ¢) w e re
19 5 2 a n d h a s s in ce be co m e av a ila b ı
e w o r ld w id e b o th a s a p r e s c r ip tio n d r u g a n d a Ķi ? ï i WFiŕ ?į bution p h a s e h a lf lite (tl z l a n d
l te r m i n a l e ı
iın ĵ n a ti o n p h a s e a

theounter medicine in 0 W jja b Ģh o u tiv e ly


ı1a n
ı y tr ie s H y o s c in e b u
co u n ty l b r o m id e 2 o - 4 o m g o ra l i* L : ÄU W o ia n rs re sp e c
e s
is le s s p o te n t a n d lo n e r
a c tin g th a n a tr o B d N IP R A V E N T 2 0 p g d 4 0 p g / p u ff m e te r e d d o s e in h a le r 2 p u ffs 3 - 4
g p in e ra n a m e an

Ph m 0 4 2 m ın e b u liz e d in c o n ju n c tio n w ith a p


2 a g o n is t 2 4
a c o k in a ıla A ft er o ra l a d m in is tr a tio n The p la s m a c o n c e n tr a tio n s o f ttçditlġ i ,
d
\ ipg / m l r e s p ir a to r s o ın
b2pı
gen e r a lly b e in g b e ı
ow th e lim it o f u
q an tita tio n Th e bioavaiability is es tim a te d frdı
i\êñnil t i m ¢M
e x c r e tio n
:: w as ge n er a lly < 1% H o w ev er be ca u se o f its M g h tis s u e a ffin ity fo r m u s c a r in ic Ŕ in iıĥ J a u l

Scanned by CamScanner
8 2 ı lĦ
iį l A Te x tB o o k o fP ha r m a c o lo g y (V ° E Ì

SYN T H M C A N T I C H O H N E R G IC D R U G

M Y D R IA T I C S A
tr 叩 ic a m id e a re u se
m y d l ia tic is '
d in m e d ic in e
"e nt th a t in d u c e s
to p e r m it ex am in a
a tio n
d i】
tio n o f
°f th e
x ŕ ,

m u sc ı
p a in ħıl c ilia r y
f th e e
S t r u o y e a n d a ls o to r e d u
e ce

3 0 -4 0 m cyd o p le g ia t a lr p « 1 3 h o u r s

la te p ro d u ces ą la ta tio n


- -
q rc lo p e n to ,

o f th e p u p il (r n y d r ia s is » a n d p r e v e n ts th e e y e f r o m

(c y d o p le g ia ) It is b lo c k s th e m u s c a r in ic r e c e p to r s c y d o p
ţ ă
o d a tin g
p u p il (m y ? ia s is ) a n d p r e v e n ts th e e y e fr o m a c c o m m
is 沁 出 c a m a į n ly to p ro d u c e myhm
a n d w c io p le g ia o
f r ia g n o s c p u Lp o es
u o j brJ
B r a n d N a m e C y d o ın id e y e O 5 % 1 % c y c lo g y l 1 % e y e d r o p s

h a r m a c o lo g ie a c tio n s im ila r
T R O p I C A ĦW E It is o n e o g o n is ts w ith p
f th e m u s c a r in ic a n ta
i ti It þ
l
łı
to a m in e a n d u s e d ın a in ly a s a n o p h th a lm ic p a r a s y n ıp
a th o ly c or m ydr a c
ti Įe qĶålĐe
t o rs ) T h e s e r e c e p
to r s a r e in v o lv e d
r e c e p to r s in th e m u s c l e s o f th e e y e (m u s c a r in ic r e c e p
d th e s ı
c o n tr o u in g th e p u p il s iz e a i ı ıa p e o f th e le n s B y
b lo c k in g th e s e r e c e p to r s iţ ・s
¥ ę¥
d t th e f ro m a c c o m m o d a tin g fo r ńëiiīśi n
d ila ta ū o n o f th e p u p il (m y ? ia s is ) a n p r e v e n s e e y ĵ [h t
th e p u p il a n d r e la x th e le n s s o a eye
(q rd o p le g ia ) It is g iv e n a s e y e d r o p s to d ila te e j}d iıĮ r fi

X ĵ th p h e n y le p h r in 5% e ye d r叩 s
. . . 5% ' o% eye d ro p s T r o p a c p Jtiêåţ
b n yŁ
,

p lu s 0 8% w e rn o T
:
eiJiTJnA
QU LN A R Y C O W
A TE R ¢ UN D

iċ i th a t r e d u c e s th e r e fft Ec tip f
p R o p A Iv ī H E L ? It ĵ srg ic d r u g , a m e d a t o n
an an tic h o lin e

th t ti l te m u s c le s b y b lo c k in g th e
r e le a s e d ħo m m u a
c h e i n ic a l n er s a s
a c e ty Jc h o lin e a v e

f ] h li o th m u s c le (a ty p e o f m u s c le )
ıe c e p to r s o r a e ty
o c o n e o n s m o

M e c h a n i s m o f a c tio m It a c ts o n (1 ) a s p e d lic a n tic h o lin e rg ic e ffe c t (a n tim u s c a r n c ) a


i i t th e

ı
n d ic a tio n Fo r th e tr e a tm e n t o f e n u r e s is t has
ı a ls o been u se d fo r h yp
\
e rh i tud
cra 呷 s or sp a s n 】s o s to m a í th e c h in te s tin e s o r b la d d e r
Jn iü 1 32 ß8

U s e s I E a ls o h a s a d ir e c t r e 】 a x in g e ffe c t o n s m o o th m u s c le It is u s e d to tr e a t o r p r e v e n
t

s p a s m in th e m u s c le s o f th e g a s tr o in te s tin a l tr a c t in th e in ita b le b o w e l s y n r o m d J ll Ė a
d ls o
in h ib ib g a s tr o in te s tin a ıp r o p u ls iv e m o tility a n d d e c r e a s e s g a s tr ic a c id s e c r e tio n a n d i¢p n ł r o ls

e x c e s s iv e p h a \ g e a Ļ tr a c h e a J a n d b r o n c h ia l s e c r e tio n s ; JI

D ose 15 4 30 m g o ra J u s e d ı
o r p e p tic u d g a s tr itis
lc e r a n Jia q Ðq e y b
B ra n d N am e p r o b a n tM n e 15 m g ta b , pr c b a nt h i n e T a b le ts 1 5 m g p r 叩 an th e l T a b 15 [ilg ßìr rî

: ţl

Scanned by CamScanner
gi
=
% ı rm o - . " " ' " m iĦm a a w
= Pfiarmacoıo o f D ru g s Ą c t in g o n p e r ip h e r a ıN e rv o u s t e m s \ 团团

o f a tr o p in e It is re d u ce s th e e ffe c t o f a ce ty lc h o ı
in e a c h e ın ic a l
t s tim u la te s m u s c le s b y b lo k in g th e fo ty lc h o lin e o n
c re c e p to rs r a ce
a ls o to r e d u c e u s c le :
p a in ń ıl c ilia r y m

h a n is m f a c tio
e c is s iın ila to p p e n th e lin
m o n r ro e
M
D o se 5 10 m g (c h il? en 3 5 m g)o ra l s im ila r to p ro pa n th e lin e re co n u n m d e d fo r p e p t ic
o í th e p u p Iı (m d r ia s i
y s) d p r e v e n ts th e Tr a m d a tin g h
\ i.
a n ey e a c co m m o °
W t

r
B ra n d N a m C yd
e om id o3 % t% cW tr o ls e x c e s s iv e p h
ey e o gy l I % ey e dro ps u se d to co n a ryn g e a l tr a c h e a l a n d b r o ĥ c h ia 1 s e e t i o n s

? a ce q ıc h o ı
in e o n sm o o th m u s c le (a w e
łH
(ğ te by
:h B ra n d

g n iÄJ r
n a m e sp a sr il q ir e x 2 5 m g ta b w ith

ı
MjDit$gaslTointesı
inaı
propmwmovand d e c re a s e s
g a s tr ic a c id s e c r tio n
(J iit äidition it s h o u ld

andgasus andp11¢
rpls
D e
o 8e 15 ı 3o m n o t be u se d if y o u h a v
~
g o r a ıtı
sed ı
orp ep Hc u Jc E r
e th e
fo110wg c o n d itio n s H yp e r s e n s itiv ity
" " " " ' "n " "

£Į
. Ta P b " " , T a b l" " d y s P e s ia a d
' ' p r o p . . Th e l T a b p n o th e r c o n d itio
n s 5 1o m
in fa ◆e c o li g (c h ild r e n 2 3 m į o r a 1
s: cs a n d o th e r g u s e d fo r
flalent d y s p e p s ia
g a s tr o in te s tin a l s p a s m
B ra n d n am e P ip ta l p i e n 4
p m g + d im e th ı
y p o ly s ilo x a n e 4 o m
g / ın l d r o p s

Ę = 团 团 国 国回国
e 姒

Scanned by CamScanner
眉 国
月 目


巴 团团国

回 X X , X X T E R h A IŁ
Y AM ı
N E
.
th e e ffe c t o f
.
VilDicĹOMiNE It is an an tic h o lin e r g ic dru g a m e d ic a ū o n th a t re d u ce s

CetylŁ
holine a c he m ic a ı r e le a se d fr o m n e rv es th a t s tim u la te s m u scı
e s b y b lo c k in g th e

lin e r g ic ffe c t (a n tim u s c a r in ic ) d (D d ir e c t


a n t ic h o t th e ty lc h o lin s ite s a
e
p to a n

!
a a ce e « e ce r

b ilia r y d y s 】
c in e s ia a n d c h r o n ic d o le lith ia s js
ı D u o d e n itis ' ' " ° ,
iM į ë.. '" " . . ' " . . ' " ' " ' " b . . ' " l r i t a b ıe b o w e l sy n d r o m e in c lu d in g
U ses it is u sed in th e tr e a tm t o f p e p tic u lc e r a n d th e r g a s tr o in te s tin a l a is o r a, C o lic k y a bdo m in a l p a in d iv e r tic u litis
en o
Ťs m a rke d
hotility
£X
y
X
y u Jp e r a a a ıt an đ t
a
"

ith trillu
Ļ .
w o p e r a z in e 1 m g zs b e u rn
m u s c le s o f th e g a s tr o in te s tin a l tr a c t in th e ir r ita b le b o w e l s n d r o m e I t a ls o inhibi
: ırÍ o T ıaß g y
l p r o p u ls iv e m o tilit
G LY C O P yR R O ĽA Æ n Ė is in e r gic a g e n t w ith a g a s tr o in te s tin a y a n d d b e a s e s g a s tr ic a c id s e c r e tio n an d tr o ı
co n s
a șy ııth e tic a n tic h o ı qu a te m a ry
iĵ åmôńīum
s m c tu r e yęsęP$Ș¥ę p h a r y n g e a l tr a c h e a l a n d b r o n c h ia l s e c r e tio n s
) ĉr
M e c h a ııis m f a n m Iis b h d
o com p e titiv e ly to th e m u s c a r in ic a ce ty , c h o Ľ n e " e6Fıaike jWpq B e n ty lo l D o sp a n 3 o m g ta b D ic y c lo in c D ic y c lo h lo ń d
m e a p 1 g m in e H y? o c e

u2 Jr
m g l m ıa ın p ım
'

gh 5 m ıiaJ
p yr o ı
a te o2 m g I m la m
p 1【
rm l v i
a i G i co p
y '
Į
ik=đ
°
liame G a s tr '
"pin T a b 5om
g

V A L ET H A M A m
: 67 J H9 ) It is a n a n tic h o lin e r i d
la n d e ri h e ra l
c e n tr a
g c r u g iıs e d a s s m o o th m u s c le r e ta x a n t
p p a c tio n It is u s e d It h a s b o th
a s o )cy to c ic a n d
a n tis a s m d ic
p o

Scanned by CamScanner
1 96

】 e V a le th a m a te b lo c k s th e
y lc h o in
o r o f A ce ı
M e ch a n is m o f a c tio n It is a co m p e titiv e in h ib iı
an d in h ib its th e a c tio n o f A c e ty lc h o 】 in e a n d p r o d u c e s i m u s c le
m u s c a r in ic r e c e p to r s
Tmu p
r e la x a tio n s

p h a m a c o k in a tic s It is w e ll a b s o r b e d p
d m in is u a tio n
a ħe r
It is Y
a r e n te r a l a ide]y
d i b r e a s t i r出血 M e ta b ä u Ëë đ
d is tf ib u ıe d in th e b o d y It m o s s e s th e p 】 a c e n ta a n d e x c r e te n

s m e b b o lite s a r e e x n e te d m a in ly in
th e u r in e I t is in d ic a te d to s y m p to
th e 】 iv e r T h e d r u g a n d iı In d ic a tio n m a tic r e 】
ie f o f d y s u r ia u r gen c y n o c t u r ia su p r a p u b ic
In d ic a tio n s c e n i c a l d ila ı a tio n jn th e 丘 rs t s ta g e o f la b o u r an d o f Symptomaticjlief; p a ip iĮ fĮ e q u e " a n d in c o n tin e n c e as m a y o ccu r in c y s titis p r o s ta ū tis u re th r iū s
(J 0 T T s tit is / u r e th r o tıig o n itis
u r e th r o c y
◆ s tr o in te s tin a l c o lic B ilia l y c o lic U r e te l ic c o lic
c h ia l sc* e tio n s b d in
s id e e ffe c ts e s s o f m o u th iī s \ vomitin m y ? ia s is r e d u c e d b r o n ìh h a s v a r io u s u r in a r
ee n u se
U s ęș y s yn dro m es an d a s an an tis p o d ic I t m a y h a v e
a sm
a n d b ltiH iin It is
q r d o l
p ge i a p p
a 】 ila ıio n s d r jm e s s o f S c o n s tip a tio n u r in u y r e te n t o n
i g of lq c a ņ# p ș th e t ic ac tiv ity u se d to r e le x th e sm o o th m u s c ı
e in th e u r in a r y tr a c t I t is u s e d t o
9 ılj tiv e b la d d e r
tr e a il th e
G ov era c ith
» is io n w sy m p to m s o f u r ge u r in a r y in co n tin e n c e u rge n cy an d

c o n t r a in d ic a tio n s H }p e ıs e n s itiv y Io v a le th a m
iı a te Fostatic en l\ m en Ļ P y Jo r iĒ ł& ģ Uę,£
ir e qu e n c y

P a ıa ly tic ile u
g ra M s
s tJlc a a tiv e c a litis T o x ic m e g a c o Jo n C lo s e d an g le g la u co m a an d M y a s th e r ıia
J Ðļ d t T :į į m e ' " a 5 1'''".' H a v o x a te h c l 1 o o m
g ta b le t an d A p o F 1a v o x a te 2 o o m g

U s es it is d a s a n tic h o 】
n
i e ıg ic (a n tim u s c a ıin ic J a sm oo th m 1】s c le r e ta x an t O x y to c ic a n d
u se b n J iJ o J v
an tis p a s m o ä c T O L T E R O D IN E It is a c o m p e titiv e m u s c a l in ic re c e p to r an ta g o n is t B o th u r in a r y b la d d er
D o se 1 o 2o m g 8 12 h o u ıs h a d a y p a re n te r a l o M or W 4 8 m g C h u i¢ t '
ęe9, î ,ņ
łr
a n d s a liv a tio n a r e m e d ia t d
e v ia ch o lin e r g ic u s c a r in ic
m re ce p to rs
reco m m m drd M e ch a n is m o f a c tio It a c ts
n
an d M 3 su b t
o n M 2
n e ji ¡r y p e s o f m u s c a r in ic r e c e p to r s T o lte r o d in e
B ran d N am e V a la m a b gm gh I mlinjlidosin 8 ĵ 10 g ta b an d its a c tiv e m e ta b o lite 5 hyd
m g n ı
n
w w w e th y lta lte r o d in e a c t a s c o m
ro

m u s c a r in ic r e c e p to r s A fte r o r a l a d m in is t t p e titiv e a n t a g o n is ts a t
r a io n to lte r o d in e is m e ta b o liz e d in
i g n illu th e liv e r
V A S IC O S E 【E C n v E D R U G S
eb r e s u lt n g
i in t e fo r m a tio n o f th e 5 h
h
y d r o x y m e th y l d e r iv a tiv e ' " j o r
9 rf r Đ l ij- :
a c tiv e m e ta b o lite T h is a n ta o n is m p h a r m a c o lo g ic a lly
O X y B U Ė a n a n tic h o lin e e d ic a
g r e s u lt s in in h ib iti
o n o f b la d d e r c o n tr a c tio n
g ic m tio n u s e d to r e lie v e u r in a r
y andblddder th e d e c r e a s e
di f ó c u l jn id ė b h is ò r p r e s s u r e a n d a n in c o m
indg Ėe qu en t m a l l o n an d jn a b iliy to c o n tr o l u r in a tio r ı b p le te e m p ty in g o f th e b la d d e r
m u sc ı
y d e c r e a s in g Ińtł iEätiì R e c o m m e n d e d fo r th e t
e șp a sm s o f tire b la d d e r
r e a tm e n t o f o v
] Y J ßır ir u e r a c tiv e b la d d e r (w ith
M ec ħa n iSm 0 f a c tio m c n js d ir e c t a n tis a s am
ı
u r in a r y fr e q u e n c
y u r g e n c y o r u r g e in c o n tin e n c e )
sW p to m s o f
a
p o d ic e fle c t o n sm o o th m u scı
e an d in h iY ts th e
U ėb g iV į ś rá n a n tim u s c a r in ic d
r u g th a t is u s e d to t
r e a t u r in a r
la r u n c tio n s o r a u
n e iu a m u s c ıı
j to n o a n ic y in c o n tin e n c e
g a n g lia fa n tin ic o tin ic e c t s ) p a r tin ıta r il i
th e M I a n d ?
In d ic a tio n R e
c om
r e c e p to r s o

m en d e d fo r
fa e b 】a d d d
th e tr e a tm e n t o f o
aa H
ų reas d skeayd
y n h ib itin g

v e r a c tiv e b la d d e r
w ith s m
y p to m s o f u rg e

h c lu

fa
d in g
bı ńequentuńnationandįı
Hbuvtoconi tu 山1a
a d,凶 Jt e x tio n
bydecreasingmuscldtiaám。
o e
e r ts a
D o se 5 m g B D /T D
an w asm ? jc e o n sm m M m u e
b a r r ie r an d is
S o ral cha dr
e n a bo v e 5 25
T m g BD
: ? ıĻ L y sır a n C b¢y s p a 5 2 5 J ıI J u ıì u
m g an d 5 m g ta b s D ilr o p a n s r '
y up
ıA v o x A TE
R ı
s a s p a s m o J ti
y c n a v o n e da i
w tiv e th a t
a c ts b
y r e la x in
g th e
Smotþ
,qw§
Ęł£

Scanned by CamScanner
u 闸阳 ņ ぴ迈 四 回 画回 国
l i m B O 0 k o fP ha rm ac o ı
0 gy
w l)
,

, - 团团团团国。 ı
l31 ı
brjpT c r İm in a te b e tw e e n
th e M

; r ıb ıe . d g la n d u ]

fo
th e s y m
r
a r ) Ita

p to m
, (c o r tic a l

a r tia 】
o f p a r ld ı
ly
o r n e u ro n a

ï
D a n d th e p e r ip h e r a
tch
. Jjn " g i. a c tiv it
y in th e
l
c N s
m u s c a r in

w h ic h
ic

d r in E l× 2 5 Xem a d r in T a b 5 m 8 P ıo q æ
lid E lx P t o c y c lid 11#119 8 iiiility o f d o p a m in e a b r a in
c h e m ic a l
u o n s
th a t is c r itic l i
It is a ls o th o u g h t to in c r e a s e d i e
B ıa n d N ıiııe K a
e ıtı l
n ta r y m u s c e m o v e m e n t
a n th e in itia tio n a n d s m o o th c o n tr o l
o f v o lu

裟竺鹭式
t It h a s th e r e fo r e so m . . 。 。 。。 一 。
tic h o lin e B ic a ge n e 。
B I p E R D It is a w e a出 p e ip h e r a l a n d İ Jı J.
。 吣 ― ― 。 ' " o v ra m i一 。 a 一 。˜

a n tis e a e tm y a n lis p a s m o d ic a n d m y r a
d i tic e ffe c ı s
i h lin ęł
a c tiv e a n t c o g ic d r u g a o n e o f th e tr a lly
f e n tr a 1】y ce n
ün g
ac
tio n c
M r c h a n is m o f a c t io n T h e m e c h a n is m o f a c
o
o f a c e w $ho lin e d is o r d e r s
m u sc n in ic an ta g o is ts d fo tr e a tm t o f
a n b g o n is m d d ru
n an n u se r m
l te lt r c o m p e titiv e g in d u c e d
a t
s u c h a s b ip e r id e n is c o n s id e r e d to r e a e x tr a
p y r a m id a l
h li i b i t h s h r a h ım w M c h th e n r e s
to r e s th e b a la n c e rrzcqİ j h "
m o v em e n t d is o r ders an d as an
c o n e tg c ıe æ p ıs n e c o t p u s
t alan d p e ń ph e ra ln e r v o u s . P a r ka n e T a b 2m
d į n b o th th e c e n r g A
u s e M It is a m u s c a r in ir a n ta g o n is t ū a t iıa s e ße s r ta n e E ix 2 m
8 /5 m 1 A
l t i j d ia p a th ic a n d postÆ eļ ?litic dylT a b 5m r ia n e T a b 2 ın g T t M ex yp h m T ab
t r io s c c
s y s It is u s e d in ıħe lr e a in « m t o f a r e
e r o
g
id a l s y n ıp to m s jn d u c e
d b y p h e n o tfü äz in e
w ia Ee e x b a p y ıa m d
p a r I t tıs e d to a lle
i e n ts A k a th is ia a k in e s ia d y B k in e tic M W o n a v e rs e e ff e c t o f m u sca ń n ic rece
p to r if B lo c k a g e A
d e r iv a tiv e s a n d ıe s e p e It is u s e d a s n e u r o le p t c a g
.
n tic h o ı
in e rg ic druce
llis a n d p r o fu s e s w e a
tin g a r e m a r k e d l Ĵ 1nm 91 M łs c a r in ic R
tr E m o r s r ig o r o a ılo gJ r ic o r s s Qi i a s m o d ic ro r tic o y ı ece
p to r T y p e s a n d E ffe c t f
s ro m T h e ir B ı
o d «a ge
redu ced o r e ł im iï ıa tĦ l O r g a n S y s te m R « e p to rs

B 口 n d N am e A l n p h m 刀山2 m 竺

B E N Z T R O Ė Ė a n tic ho lin d r u g is a b o u t e q u a l to th a t o f a tr o p in e It in h lb ib ą
s It is a sdéėtie M 1
d a p a m in ıe m p ta ıe a tħe d o p a m in e transporter a t n e r v e te i m in a 】
m u s c u in ic a o d J? o ı a g t m is Ł l 【is a b le to d is c r im in a te b e t w e e n t h e M 1
in e r e c e p to r a n ı ! JÄa¢
Ĥ iagti§
SUe M 2
T ą ch
y c a r d ia p d p iı
a tia
gdiı
làrļ
(c o r tic a l o r n e n n n a D a n d Æe p e m m u s c a r in ic s u b q p e s (c a r ď a c a n d
E È
n s
It
43
in e ¥ ic a d ir ity h tħe C N S w h ic h is r e sp o n s ib le fo r th e s y m p tq p ry
p a r tia D y bb d s c h o ı \ of e ye s M u m d v js io n m y 卤山Is is
f a ım s o n ķ k ĵ s a ķ o tħo u g h t to im r e a s e th e a v a ila b ility o f d o p a m in e r a b r a in
c h p m ir a l tħ a t Ė a ū ita ı h tħe in itia tio n a n d s m o o th c o n ı r o l o f v o lu n ta r y m u s c le nij*ëĖiėlit M 1 M 2 M 3
S】 o w in
8 o f tr a r s it tim e
8 「富 国d N a m e 妇 够 娅 刀山 2
\ 妇 劬 呷 妇 施 吵 地 h je c lio n U S P B e m tro in e し p 泣 吕a R i 【ī n r a n d g a s tr ic a c id
s e c r e tio
co n s tip a tio n e ffe ċ ts o n sphincte to ń e
n
ĺ n j ır J M 1 M 2 M 3 M 4
M 5
Tt is a d m g u s e d to re d u c e lĦ re Js o f a c e rJ h li
d o p a m in e in tlie b e a ım t a n d m a
q c o n
n a g e m e n t o f p a r k in s o n ķ d i se ase
e to r e tu m
\ ï ţ ith
' b v ńłt ó r j
r{c o r te x
b r a in
an d
c o n ħt s d e lir iu rr ı se daüo n hallucinations i
d is r u p tio n , e e d
A k c h a n is m
M t łá ,
į t l
o f ad io « t b in d s m
】 e m u s c a r in ic a c e ty lc h o lin e r e c e p to r
in h ibitin g acetyklıo M is d e c r w in a cet d ro lin e

ace Đd c h o ı
in e ba 1a n c e a n d r e lie v es he
ı
r e s to r e s th e n o rm al ?ijiśiiin ° $¢
e tr u s o r M 2 M 3
Decaed c o n tn
s ym
p to n ıs o f
ı " U H
ii ic tio n u r if iá tio n i e te n tio n

d is e a s e ı
L¥ M u śc a r jn i"
eæpt . . Įįį


t is a d r u u se d
g to re d u c e ie v e b f
o acetylđ a noenirß'
l 1
oe A c e ty lc h o Ľ n e is u s u a ll i
,w M o
y n
f ' "amine are
p re se n t
H
b 'a la n ce
$ S Ĵ n ó fßd

sU n
n

í In s e s
ìYĮT
F
□ G A N G L IO N IC B L O C K IN G A G
ENE
T he
p e ń p h e ra l n e rv o u s s y s te m is (e g p a r a s y ın a th e tic
p p a th e tic
\ Ě
sw d
th ' "t ' "
, an m o to r n ervo u s
' " ^ o f g a n g lio n i. B lo c k . .
r 19 ıt īıig ĥ ï
va al
g n e rv e s th a t e x it th e b r ä t e m , th e ir lo n g p r e g a n g lio n ic fib e r s
en te r th e ta r e t
g o r gan

Scanned by CamScanner

ł 国
ı 厦园區 园 区 回 國 區
ı
囫 踊 哅 ı y . ^ 。 翩 陬 보- v ã 四国国国团团团团团国 邮

ith in ll g a g liits L iķe d h ë l liä fo r b o th th e p a r a s y m p a th e tic


m Ė L g $iı g
sm a n
n e u ro n s w an d s m
) w h e r e th e y s y n a p s e w ith p o s tg a n g lio n ic o f n ic o tin ic c h o lin e r ic r
y p a th e tic n e r v o u s s y s te m u tiliz e th e s a m e
(e g h m
N c su b w p
e
d it b i g ece
p to r s fo r s y n a p tic c o m m u n ic a tio n T h e N
th e tr a n s m itte r is A C H an
c ga n gı io n ic
sp p a th e tic g a n g lia n e u ro
t ih i? r eceptors h a v e a d iffe r e
n t s u b u n it
n ic o

re c e p
to r s e x p r e s s e

bl oc k e r s -
d b y s k l
e e ta l m
u s c le X °
P
NG noİ ł
!nfį a l
n g ioŤ
° h i ch se l ec t iv
e bl oc k NG
re c e p t or s .

Pa ra s

S y m p a th e tic
y m p a th e tic

ııa c a m y la m ı
ne
ıŝ i o o d

jtu ı

v e s s e ls
ßn ĵT ł
°

HŁ īïĮ ï
ïīïīŁ
a la a

, . '"' p en to lir ıiu m in h ib ib re le ase . '

N e Tn me p ha n N o rE p i «g

ı J
'

f th e le a d s to m e ın b ra n e
四国团团团团国 国画 0 罨 「
j .. B lo c k a g e o re ce p to r sm o o th m u s c l
G a n 目ı
ıo n ïc r e la x a tio n an d v aso d ila to n
A CH
JOJĐ U se B lo c k a g e o f th e r e c e p to r le a d s to sm o o th m u s c le la x a tio
re n an d v aso d ila to n 1 t is d
a n tih y p e r te n s iv e
u se
as an an d can be a d m in is te r e d lly in tr a m
u s ly
o ra u sc u la r ly an d
s u b c u ta n e o

G an gHo n k
an g " o n ic

G ıU V C U O M C B L O Q CE R S P E R S IS T E N T D E P O L R IZ IN G
þ
1 Quamm yimm mńtm c m p m m cb inİTı
ĵĵeïim
P m ın lin iï n n (e a J o T Ľ Ĵn
N ic o tin e (la rg e d o s e )

2 , le n ia ıy )
An tic ho ı

Timethaphan
in e s te r a s e s (ia T g e d o s e ) \brĮiTqrfly.
rĵ in oTlĉ ĥ
p e r p id in e
j Ðq ß t9 ıĮ j £
i
M e c a m y la m in e
3
W ¢ń n n c o n p ou n d ń ırÐ J d
Tnm e Ĥ a p jr n u j t [ı rß jĉ ĵ 1
C am fo m u lfo n a 勿

O g39 A P EM P ID IN E It is
q sm a tic w e s e n ta tio n o fd m g a n
co i ti
n ic a n ta o n is t m o t
a cto n
吕a n g lia an d d r u g c la s s ific a tio r n s s d e n r! ha s b e e n
g s co m m o n l u s d
y e a s a n e x e r im e n t l
n
u se d p a to o l 1t
a s a g a n g lio n ic b lo c k e r in th e tr e a tm e n t f h
W a th e t ic a u to n o m ie g a n lia su pp la n te d fo r th a t p u J o s e b ın o r
o y p e r te n s io n b u t h a s l
a r l
g y b een
e
g a re co m p r is e d o f th e a r a v e r t b p y e \ m c d ru gs
p e r a l a n lia
g g (s y m p a th e tic Ĵ ù Ŕ!Į jJi ı
q nv
dLE A AMiNE It is a p o te n t o H l a n tih
y p e r te n s iv e a g e n t a n d g a n g lio n b lo c k e r
:T n d a ry u r ıin e
It is in d ic a te d fo r th e m a n
a g e m e n t o f m o d ėr a t l
e y s e v e r e to s e v
a n d is a

yp e iw
i1 ı
o n a n d in u e r e e s s e n tia l

sM
n co m
p lic a te d c a s e s o f m a lig n a n t h y p e r te n s io n
e ąh h H § in o f a c tio
! Zï oJq§
»ī n It is a g a n lio n ic b lo c k e r w h c h
re c e g p r e v e n ts s tim u la tio n o f o s ts n a ti
p to r s b y a c e t l h p y p c
y c o lin e r e le a s e d fr o m p r e s y n a p tic n e r v e e n d in s T h
g e h
y p o te n s iv e e ffe c t

Scanned by CamScanner
て盛着鎏
蝨壁姜
老 ,

.
'




ごラ巷議墾郵
n1 Ę ° lo ga o f D ru \ ACti o n P
rm jA Te x t B o o k o f p h a rm a c
o lo g y (v o y ]
' "
E h N e rv o u s
st e m j 14
1
v a so a u iítim u a A arr tÐ
ib u te d tu th e re d u c tio n o f s y m p a th e tic to n e
o f ee camy la m in e ĵ s a th Đn ßr d m r r 【
d is p r im a r ily po sh u a ]
r e d u c e d c a r d ia c o u p u t an
dera ı e ly s e v e
re to se v e re äi
In d ic a tio n It is in d ic a te d fo r th e r e a tm e n t o f m o
ı
t ß Ðn il ?
a li n a n t h y p e r
te n s io n
h } p e r te n s io n a n d in u n com p lic a te d ca s e s o fm g

o fte n u s e d a s a Æ s e a r c h lu し
u
ininï [qr į
B ıu ıd N am = M e cam yı
a m h e h y d r o c h lo r id e d 6 9a69 T

It is in d ic a te d fo
n i¢
łq!ţ ie ņ r th e re 】
ie f o f n ic o tin e ith d
w ra w al sy m p to m s an d a s a n a id to
t io n
b
n ta in a 4 P2 s u u n
its Jt m u s t æ\ - s n ¥ ssa
b o th parynı pathetic a n d s y m Ħ th e tic B a n g lia th a t c o
b y Ĺ v In ń rs io n s m i e o n s k e le ta l m u s c le th e
s o f d tu b o c u r a r n
a r fu th e e ñ Ėc ı
e ffe c ts o f line N
Brmdlrı ic o re tte In v is ip a tc h 2 5 m
g N ic o tr o l 4 m /1
g
◆ v a tin g s y ım p tic le v e ls o f a c e ty lc h o ı
in e
g a n g lio n ic b lo c k e rs c a n b e s u m ıo m ır d b y e
3 6 S Y M P A T H O M IM A T
e n t p r e v e n ts s tim u la tio n o f p o s ts y n a p tic
IC S Y S T E M
M ec ha n is m o f a c t i H is a ıi
g a n g llo n ic b lo c c n \g a g Ju 平H YzJ A D E G I C D RU ĒB
r e c e p tu ıs by
p e tin g w
co m ith a c d w c h o lin e fo r th e s e r e c e p to r s ite s A d d itio n a l e ffë ť « u iä y
( ı
SyŢptnimetics (a ls o c a lle d a d r e n o m im e tic s ) m a y d ir e c tl tiv a te th e ir
jn Tn th a p h a n h y p ö æ ń s iv e y a c a dren o ce p to rs o r
include d ir e c t p e r ip ħe a l Ţ a s o d ila tio n an d r e le a s e o fM s ta m e m e s

e ffe c t is d u e th e Æ d n c tio n ū ıs y m p a th e tic to n e an d v aso d ila tio n an d is p ń m a r ily p o s tu ìā 1

I n d i c a t i l t i s h d ic a te d fo r th e c o n tr o lle d ıe d u c tio n o f b lo o d p r e s s u re d u r in g s u r g e ry an d
in th e b e a b n e n t o f ħ}p e r te n s iv e e m e r ge n c ie s (c í n o Tu n

B e ll an d a ls o fu r ra pM r e d u c tio n of b lo o d p r e s s u r e in th e tr e a tm e n t o f hy 'lli Ųê k .
emergende e s pe d a ūy

lr e a b n e n t o f p u lm o n a ı e d e m a h
h th e
g acu te d is s e c tin a n e u ry s m It is u s e d in th e egigéhËýk
y p a tie n ts rtpith p u lm o n a ry h yp e r te n s io n a s s o c ia te d w ith
s y s le m ic h
w e n e n s io n A t M g h d o s e ils s h o w s th e a c tio n ĵ s tic h o Ľ n e s tr :w
an es ,e s b íe g v
B Ja n d n am e Tn m e tħa p ha n c a m s ı
y a te ĵ an ı
yx o ï by í
ir a i JJ u b
P ERSı
S JE N T D E P O U ı
IZ ï N G B LO C K E R
mì r
i
sns 9 ıll Y ci
N ı
COn NE ı
t js h ig h l to x ic
y a】
k a lo id ıt js th e r o to l í l
y " " ra m a tic a u y
p }p c a g o n is t a t n jc o tin ic dĮ Įil 9
s tim u la te s
..
n eu ron s an d u ltim a te ly b lo c k s f ì.

M e chm sm t a c tio n
o n js a s tim u la n td ru
g th a t a c ts
ıe c e to r s
p M ese ar e Jo n o tr o jc
p r ecE
p to rs co m p o se d
as an a o n j t
g s a t n ic o tin ic
acèiı
crı
i.lMQni
u f liv e h o m
p o
o m e ıic o r h ėt ä¢a n
co n d u c ta n c e of m uı
b pı
e ca tio n s in c lu d i
n g so d i
d e p o la ıiz a tí um c a lc iu m

Ļ w ħ
Jc h a c !iw an d p o ta s s iu m
te s v o lta
ge at d Tħis le a d s to
g e c a Jc iu m ch a rı o J ab s l
n e ls an d a llo w s m 9 協
Ł
o r e c a lc iu m to
01m u i

t

Scanned by CamScanner
し 強司国目园園园

l

= = ĦĦil
a c o !o g y o f D g A
匈 rm
ru s c t o n p e ri
phe ra lN e rv o u s s y s te m I t s

Ť a iiĮ n ¢ iÈ

o n o f adrenec re c e
p to r

iĴ Ê;1
3 6 łA D R E N E R G ıC D R UGS
P m R æc M ŕg T ÐU ij ic in d
)T
A dr a m e s a re ru g s th a t s tim la te th e
u
rg ic
sym
p a th e tic n e rv o u s s
y s te m (a ls o c a Ľ e d th e
adren e n e r v o u s s y s te m ) T he s e
3 ıo A p m c e as o fn o ra dren u g ic co m
p o u n ds a r e a ls o
A c tio n
ı
thĥ qmu { ca lle d sym p a th o m im e tic d Jn g s T h e
on p ost sĦ a p tic W N o r e p in e p h r in e r e le a s e d ıa m th e s y n a p tiç
? I i es
T H ęș c ı
d iffu th e syn d b in d s to e ith e r p o s ts y n a p u c r e c e p to r s o n
p tic șp a c e
s e i a m as s a an
thÐ! fię ç ĺ o r M + ö iĤ ħť à iy re a c tio to
o r g a n o r to w w
n s s tr e s s It
w c n e c tp ? ıs o n th e n e r v e e n d in g r e c e p to r s o f th e s y n ıp a th e Ęç jş yË te n s tim u la te s th e h e tb
m a y b e d in i? d h b a ıħ
ı öth=rśtisrelated b o d y ar e a t sw ea tin g b re a th in g te d
p a (a ] B e la (P a n d d o p a 】ıt in e (D ) r e c e p to r s D r u g s th a t b in d t
ra
p ro ce sse s an

th e s e r e a p a n d m o d u ı
o o J b n İ d Jĥ
a te o r m im ic M e fu n c tio n o f th e s
y m p a th e tic n e r v o u s s y s te m m a
b e d iT M e d in b th o s e w h ic h a u y C LA S S ı
g m e n t th e s y s te m (s y m p a th o m i? tic s ) a n d th o s e w h i h F IC A T ı
o N O F A D R EN E
a n lz g o n iz e tħ
c rb b iv í 9 2( RGı
c D R UGS
e s y s tEm ) A d r e n e r g ic r e c e p to r s u s e b o th th e c c ı
m a n o pħ a ș pı
y ic a d e n o s in e g n įeo n s bĥ A d re n e rg ı d ru g
ra te s e c o n d m e s se n e r
c
g \ 纽m 2 a n d th e p h o s p h a tid ı in o s ito l c c le 3 t *
lr a n s d u c e th e y y o 9b t +
saJinto a n e « e d ol yJ D ir e c t +
a c tin g
R e m o v a l o i n o r e in
a n d e n te r th e
p q fu in e T ħe n
w - E p ħıin e n u y (1 ) d ifftıs e o u t o f th e
s y n a p tic s a c e
p
e g ' .'
!!!A
'" t a c tın g
p h e ta m in
g e n æ a ıc ir cu la tio n (2) b e m e ta b li n
Ð) ßq a J î jc r
E== =
e
o z e d Io o m e th l ı . .
(ii) r y ra m
c e ll m e m b r a n r y a te d d e r iv a tiv e s b y ın e
a s s o c ia te d c a
te c h o l o m e th ı Yd ĉ 9 v ijĥ

Xxx)be
y tr a n s fe r a s e (c o M T ) in th e
'" a
p tu ıe d b y - U P ta k '
" ' "m th . ' " tım
P' " . ^ '" ." pineph P a g ? n ls ts
qanİ ・
d
V


i\i
transporter \

!Ťę-ì
ıfre ĥ lq o J J iv .
te m an d be se u e s te r e d f
y . . .
e ts is t ł or r e le a s e by (iï ) E p ı
n e p h r in e
P h a p r o te c te d an o th e r a c tio n
§n ĵ ın Ji s lĵ
ı
p o o l A Jte m a liv e ı p o te n tia l it
:
o r

n
y n o r e p in e h i m a y
p r n e ca n be o x id iz e d Yßıa ji īo r
by m o 1a g ..
on o am in e . . ļ
sni【
nßonor A a g o n ls ts

i
!!!p h e n y ıe p h rln e o) c ı
o n ı
d ln e

bı liĮ,
rrs
\ Đn ī ì
ŝ!ł
į ŝ£
(v ) R o m ı fid ıne
ģ{m
!!i

ll) M ta p r o te r e
,

. .o \
n .
(v il) M e d e to m ïldd in e v »R ı
to d r ï n e

Scanned by CamScanner
I厦团四国国匪 赵国四 国 重
・ ・・ ・
・ ・y 四国回
U L6 ı o n P e r i p l l e ・a l a 明

ıÞ
Ą) n ic r b
N O N S ELE C H V E a A N D PA G O M ST c h a in
(M L C ) S tim q a tio n o f p re sy n a p tic o 2 r e c e p to r s re n d e rs in h ib itio n o f re le ase o f
s y s te m s c a u s e s s )= tëın j
d be ı d re n e rg ic c n e u ro tr a n s m itte r A c h fr o m in tr a b in d
E p u 4 E p H R I? It s tim u la te s b o th th e lp h a
a an a a
bro h chi a Ė x d ta tę r y m u ra l n erv e Th e se th re e re s p o n se c o ın e
th e h e a r t an d d ila te s
nd
v a s o c o n s tr ic tio n an e s tir u
d g a s lm in ı l r e la x a tio n sulats
b s o ıp tio n o f lo c a l
fa ilu d to d e la y th e a
c e r e b ra lv e s s e ls It is u s e d in a s th n ı a an d c a r d ia c re a n
tio n a n d th e Đrpęqnd
d th e c o n c e n tr a
s p h a r m a c o lo g ic a l e ffe c ts d e p e n
o n
a n es th e tic s Iı w

o re a Ĥ in il
n u m be r o f a v a ila b le r e c e p to r s G e n e r a lly it h a s m

J ť Ðleur (a rs) o f th e b la d d e
m u s c le s re ce p to r

o t d ir e c tl e x c ite
y s k e le ta l m u s c le b u t fa c ilita te s n e u ro m 1á r
u sc u
tr a n s m is s io n th r o u g h th e a c tiv a tio f
n o a a n d pz r e c e p to r s o f so m a tic M o to n e u ro n s re le a s in g
Ti
n e tw itc h te n s io n f
o w h ite m u s c le (fa s t co n tr a c tin g ħb r e s ) is in a e a se d

o ]a r

į
co m p o u n d e p in e h r in
p e ca n n o t en te r in to th e cN s b u t re s tle ss n e ss
hea da che an d tr e m o r m a
y o ccu r du e to its d
s k e le ta lm
se co n ar y to so m e p e r ip h e r a l
u s c le s a n d in te r
e d ia r
y m e ta b o lis m
m

m ñ\ ti n e « ce T h o
g h e p in e p h r in e is a b s o r b e d fr o m th
u
e G IT b u t its b io a v a ila b ilit is
Pĥ ł
. ŊÞqhse it is r a id l d e
p y w a d e d in th e in te s tin a l w a ll a n d li
v e r (b
y
m B Ťļ °r p tio n f im y M A o an d c o M T )
, Ē r o m In j s ite is m o r
e r a p id th a n in j s ite (d u e to lo c a l
/ 矓珊 \ c tio n )
s c

rHņ##ıiQn A ? en a lin e in j (B A IF 18 0 p g /o 1 1) D g s o 1 to 0 3
ņaļ *Éļ u 25 M u lti d o se v ia ls (3 o m L )
m o m 1 iv in i S in g le d o se
1 1o
U SE

C tiv a tio n o f m o i l
y s n ig h t
i
浜三 女 丁

Scanned by CamScanner
:
l h e ra lN e rv o u s s y s te m à 9

_ . " " m

A d r e n a lin e
(a ) A cu te a ım p h y la c tic (o r ty p e I h y p e r s e n s itiv ity ) r e a c tio n R I N E I t is a s w p a th o i r 山n e tic in th d in tly


am e t ts re o m an o n o【
a a c p

む发二二
; ・・・・・ ・・ ・・
筋。.

鯔二
。,
, 。. . . . . . . . .
. . . . . . . ... .

!ğ (b ) B r o n c h ia l a s d m
(c ) A d eco \
ia

也 n t (a lle r g ic
e p jn e p h r in e is o p r o te r e n o 】s a lb u ta m o l
roiqJ
re c e p to r s u
b ty p e s
. . . . . . .. . . . . a r s . . . . .

p p e a r to b e in v o lv e d in
a
. a r ly

maing
o n . . . .. . .
la r to
. . .
T h
. . 、

aiAreceptor
th r e e

h in itis ) p in e p h r in
s r e e iu v asc u n e e
n n İf lv
rr
i s ba sa a s c u la r to n e w h ile th
m a in ta n e
aifeceptor m e d ia te s th e v a s o c o n s tıl c t o r e ffe c ts o f
C p h th a 】
m ic u sE (tu d i】
a te p u p il) ep h e ? in e p h e n y le p h r in e
'"980ZU o u s a ľ a go n is ts It b in d to
ex o gen s
p to r tiv p r o te in s w h ic h r e s u lts in
a ľ re ce a c te s G
i ı119 J ß U
a
q
n l llu la r s tim u la tio n o f p h o s p h o li a
h tr a ce
p se s C A 2 an d D 1 h is r e s u lts in m o b iliz a tio n o f

m u s c le in th e p er ip h e r y It d e cre a se s n a sa lco n g e s tio by tin g o dren


n a c n a p a e r g ic r e c e p to r s in
thę,§
rĺ i0les o f th e n a sa lm u co sa to p ro du c e c o n s tr ic tio n th is le a d s to d e cr e a se d e d e m a an d

DO Se a i2 5 m g im O l 0 5 m g s lo w iv in j 3 o - 6 o p g / m in i v in ħ】s io n 5 1o m g o ra l o 25

b
lı . ļ
īı h yp o te n s io n a n d sho ck h yp o te n s io n d u r in g s p in a l a n a e s th e s ia
v a sc u e
a n a e s th e s ia l p r o lo n g a tio n o f s p in a l
P aro xysm a su p ra v en tı ic u la ta c h y c a r d ia
i r
syn ı
p to m a tic r e lie f o f ex t e rn a l
internal h e m o r r h o id s o r

.
°r i E W 1% .o l. Ti' " M / Iv NesynephrineLiq1% ph en y le p h r in e

e rİ j 1 0 l b sĵ
. M E T Į ĘX A M I N E It is an a lp h a a dren e r g ic
M e cħa n is m
; n n J o
zß a g o n is t th a t c a e s p r o lo
o f a c tio n M e s tim u ı
a Eio n th r o u h b e ta d
n ge d p e r ip h e r a l
g a r e n e r ic
g

二二 攝贏 瓦
_ _ yz es 。 ~ ' " i 。 o f

' "
竺 n o s in e tr ip h o s h
p
, a se o fm e d ia to r s f im
o m e d ia te
htypersensitij\ tiin

.
B ra n d N

īin
am e fs o p ń 4
n m g /2 m J in È
\ in in e 2 o m
g su b '"gual ta b J
U ses It is a ls o in d ic a te d
e anoiJŔJiÐ
-t
as a d jtın c tiv e tr e a tm t of
r e a c tio n s
en h y p o te n s io du
to m d ic a tio n e to hem o rrh a
e n s s u r g ic a l ge
co m p lic a tio n s an d sh o ck a s s o c ia te d ith b r a in
w dam .A
ge
Or
D o se 10 2 0 m g im 3- 5 g s lo w i v in
B ra n d N
m
j
am e v a s o x in e 2o m g / m l in j

į 殘 项
拿募
Scanned by CamScanner
国团团 团四国国 =
四国ı = ■
ı四国国 耻 日 o f D '" °、 生 t m ı
园喀目置a . 忑 团团国
.°: 匪醒 园 s y s te m 团团团国ı 、

b f tio n lts
m ą hÆ m o a c an tm y p e r te n s iv e
e ffe c t is th o u g h t to b e d u e
s t im la tio to ce n tr a l a ı
pha
a d r e ū e r g ic u n w h ic h r es u lts in a d ecre ase d
d p e r ip h e r a l v a s c u la tu s y ın p a th e tic o u tflo w to th e h e a r t
k id n e ys a n
r e in a d d iti
o n to a deeased s y s to lic a n d d ia s to lic b lo d
p ęș e y a n d a s ig h t s lo w in g o f p u ls e r a te c h r o n ic
l o
a d m in is tr a tio n o fgu an a b a ls o
i i h
p r p e r a l v a s a ıla r r e s i t
e n z ca u ses
a qłf
ease n e
s an ce

pı \a r m a c o k in a tic It is a p p r o x im a te ly 7 5 % a b s o r b e d fr o
b in d in g is 9 0 % a n d h a lf life 6 h o
m g a s tr o in te s tin a l tr a c t T h e p ro te m
u rs

D o áe rG u a n a b e ? ace ta te 8 m g T a b le t
U i*á Ţ ï t is u se d in th e tr e a tın en to f h yp e r te n s io n

ijiËjiwiDiNE D e to m id in e a n d r o m iñ d i
n e a r e th e m o t
s co m m o ly u s e d a 2 a d r e n e r ic
a g o n is t d r u g s fo r an a lg e s ia in h o r
n
g
s e s In a d d iti
o n to th e ir an a lg e s ic e ffe c ts th e s e
h a v e p o te n t s e d a tiv e
a n d m 1ıs c ı e r e ta x a n t ff
e e c ts th a t can lt in p r o fo u n d s t u o r
a ta x ia d r e lu c ta n c e to m
a rı o v e
Re su
p
R o m ifid in e (N (2 b r o m m flu o ro p h e n y l) 4 5 d ih d r o 1 H i i
ir o c lo n id in d has y m d a z o l 2 a m in e ) w a s d
m e a n a ll th e e v e lo ped
m u al
p r o p e r tie s o f a n a 2 a o n is t It
g is u s e d p r im a r ily fo r

"1j Į U J
*4 Ęņ ĘT O M I D IN E It is a p o te n t n o n n a rc o tic lp h a 2
v e s se &
a a d re n
M is J ips u Jts jn a dea ı
o re ce
p to r a go n is t w h ic h
n p er i h er a】
ea s e
p v a s c u la r iT ħe

K X
r e s is ta n c e a d jjn itia l v a so
o f p er i h e ra l
p a lp h a (D a d
n a reductiohjn hea t p re sso r re s o n se
p is
r e n e r ic
g r e c e to r s h e a r t ,r a te d ia te d b
a cco m
p a n ie d b y a co m
pen s a to r y m a r k e d d
p m ay a ls o
m e
co n tl ib u te l to y a v a
g a l b a r o r e c e p to r m echan is m
e c r e a s e in
n l lm ıb Th e b r a d y c a r d ia m
eo tlc ı Jt js
e ay b e
dn g
a pp r ox im
a te l To % b o u n d to p a r tia lly
y a n tic h o lin e r g ic a A d m in is tr a tio
ta 】
c e n b a tio n
a n d m e ta b
oıiz e d i p Ja s m a p r o te in s jn d gen t n f o A n
n liv gr ıia m t e p e tĺd e n t o f
e a b o lite s Ųq #
w h ic h a r e * J Ï t is fo r
e x c r e te d
B r ın d N łm
e ln tu n iv
pririJy
in
c lin ic a l, e x a m in a tio
u se as a se d a tiv e an d an a lg e s ic in d o
gs o v er 12
ım g /1 o r a l ? E Jı c】
in ic a l p ro w ee ks f
tfł a ıex 2 m > H r ly n s
ce du o a g e to fa c ilita te
e« ı i i« tıae d a l g ta b le t so s ln tu n i re s a n d m in o r
s u r g ic a l p ro
o n e o r jf v 1m
g ta b le t x )S )n Ĵ Jııb 1 ce du re s t
ıc o r n bâ
n a tio n M
tħo th e r d r o u te o f a d m in is tr a i
n o re q u ir in g
Jbr 1h e m
a ira e m
g en t o í a tte ti
g
m d e lic it h
H
r u s fo r t
h e h e a lm e
n to fh
y p e r te n s io n
t o n is m o re e ffic a c io u s fo r d e n ta l c a re
ıy p e r a c tiv iy d iao ırrj iz n lï
rd e r (A D H D ı J
)
c ü TA A 4 ß tq#kFWvE Pr A G o N Is T
EN z ı
łh a n al h D O BU TA M
p a 2 s e je c ti IN E
v e a d ie n
e r g ic a
g o n is t u ee d a s
an tihı
p & te ń Ėld e
an
y
bpł
il a d re n o c e
p to r s o f th e he a r t h ile
w
p r o d u c in g co m
p a r a tiv e ı
y m iı
d c h r o n o tr o
p ic
ri'
[Jbíyj
Jt
ł
rrlu j j lı
: ^'"inephrine,
d o n d u e to d
e p re s s e d
" does
c o n tr a c lllit
d o p a m in e It is in d ic a te d w he n p a r e n te r a l
y r e s u ltin
g e ith e r fro m o r g a n ic
p
h e a r t d is e a s
e or

Scanned by CamScanner
= d uuu
+o m
ı c a r d ia c s u r g ic a l p ro c e d u re s It d ir e c tly s tim u ı p to r s o f th e b e a r t *
a te s b e ta 1 re ce
ö i t i
in m a s e m o c a rd ia l c o n tr a c tiĮ i
y q a n d s tr o k e v o lu m e r e s u ıtin g Į n in c r e a s e d c a r d ia c o ti tp tıt ıt b r c in c h ó c o ı s r c t in g a g e n ts f r o m t ns
r rn a s ee in h ib its ic r o
m la ı
e a k d h
in u c q c ü a r y c le a r a n c e
v a sc u r
is p r p o s e d a s a c a rd io to n ic ft h t
a ge a n e n a n c e s
o a e r m y o c a rd ia l in ı b r c tio n o r o p e n e a r s u r g y
e ı ı

U s e s I t is c a r d ia c s tim u la t d A

:;i
a c tio n w ith b u t e v o k in g v a s o c o n s tr ic tio n o r ta c h y c a r d in B ra n n am e sm a v e n t R e s ir a to
n I t js p r S o lu tio n In h 5
m g /m l L e v a lb u te r o l H
P r o p o s e d a s a c a r d io to n ic a fte r m y o c a r d ia J in in r c tio n o r o p e n h e a r t s u r g e r y A ir b m * 1 o 0 m c g X o p en e x 0 63 y d r o c h lo ń d e
m g / 3 ın 1 s o ıu tio n x o p e n e x H F A 45 m c
B ra n d n a m e D o bu t Jn h a le r g /a c t A e r o s o l 15 g m
a m jn e 12 5 m o r id e Cdjject 5 0 m g / 4 m J
g / m J D o b u la m in e H y d r o c h ı an d
2 50 m g p e r 2 0 m l a m Irr t Į
p D o b u lr e x D o b u s t 250 m g v ia l r f

O R C IP R E N A L IN E It is a b e ta a d re n e r ic
:?rHlrfr g a go n is t u se d in th e tr e f
S E Ľ E C T ıv E a tm e n t th d
Pz A G O N ÏsT bro n c h o sp a sm s It a ls o kn o w n a s m e ta
o a s m a a n
p r o te r e n o l a s y n th e tic in
Jt is a s e le c a m e is s tr u c tu r a lly d
tiv e b e ta 2 d r e n e rg ic a g o n is t u s e d a s a b r o n c h o d iı
a a to r a n d to c o ly tic th a t h a p h a rm a c o lo g ic a lly s im ila r to is o
te r e n
an
s Jiu p ro o l
o r n o e iı e

a d re n e
e c t o n a l h a a d re n ı i
p e g c r e c e p to r s T ħe d r u g is e x e r ts a p r e k r e n tia l e ffe c t ħ
iį ihiń\ı
h of a c tio n Its s tim u la tio
rg jc r e c e p to r s b u t s tim u ı th r o u
a te s b e ta « d r e n e r g ic r e c e p to Æ ıe s s s e le c tiv e Jy th a n
n
g h b e ta a d re n e r g ic f in tr a
s e le c tiv e b e ta 2
re ce
p to rs o c e lı
u la r
a g o n is ı
a

to c y c lic 3 li a den o s in e
p h o s p h a te (C A M P ) I
m o n o
n cre a se d C A M P
T ER B U T A U N E w ith r e la x a tio n o f b r o n c h ia l ıe v e ls a r e a s s o c ia te d
Jt js
M b c h a n is m
se ı
e c tiw b e la 2 a d r e n e r g ic a g o n js t u se d as a b r o n c h o d jı
a to ran d þ6 h lw ć i im m e d ia te h y p e r s e n s itiv it f
s m o o th
m u s c le a n d
in h ib itio n o f r e l
e a se o f m e d ia to r s o f
o f a c tio n Jt act b e ta a d r e n e r ic r e c e y r o m c e u s e s e c i ll
g p to r s o i jn lr a c e Jlu Ja r den yl ¢
en z y m e th a t ca ta ı y z e s th e c o n w r s io n o f a d e n o s in e tr i ħo s h a te
a
i H ś " trie o f o q ip Fe n a lin e a r e m e d i
p a y fr o m ın a s t c e lls In t
r a c e llu la r l
p (A T T ) to c y c ı a te d b y th e a c tio n s
d e n o s in e m o n o h p lö ır ß 5 y c A M p th e
a
p o sp ha ¢ e k A M N ıilc r e a s e d c A M p ı s tim u la tio n a n d r e la x
p r o d u c tio n o f w h ic h is
e v e ]s a r e a s s o c ia te d a u g m e n te d b
o f b r o n c h ia l s m w ith r e Ja x a ti
a tio n in s
m o o th m u
s c le
y b e ta
o o th m u s c le a n d ı n h ib itio n
o n
o ï r e le a s e o f m e d ia to r s
o f iq n Jęd ia te
, iĥ þ
ii. . N e rv o u s n e ss
Hea da che Tr e m o r
ı
t js a ı
so us d a c u te N d
b ų th e r a
an su H
p y I s e le c te d w o m e n to jn h ib i
fa
Ţw p a la is e a n
ı d in so m n ia
D ry m o u th
p a lp ita tio n N a u se a D iz z in
h p re te m ila b o r
(to c o ly s js ) a n d ro lo
p n g g e s ta tio n
t u te r in e cońtt】
Ctions e ss

B ra n d n a m a B
r ic a n l T a b 2 U r rr l t
y 5 m 8 B r ic a n J T # Tu
y u r b u h a le r p o w d e r a d re n e r g ic a n is t th a t s ti
go m u la te
n u Jbl up r s re c e
/
v a sc u la tu p to rs o f th e sm o o th m
s A LB u TA M o u s c le in th e lu
L ı t js a pr a d
re su p p ly in g s k e le ta l n gs u te r u s
ren e
rg ic a g o n is t a n d th u s i e ro ı
q tı Y r m u s c le w ith an d
M e c h a n io m o f s m ila r ı re c e to rs m in im l
a c t¢
o n It jn n sı
r u c tu re to te r b u ta lin
p a o r n o e ffe c t o n lp h a
a a d
a ea se s cA M
p p r o d u c lio
n b y a c tiv
e re n e r
g ic
a tin ad
Bran d M
g en y la te w c】
a se an d th e
m e M e ta
p r o te r e n o l 1 o m g ta b le t A p m ip r e n
rc a lin 2
m y o s in an d ı
ow eı
s in b a c e ]ıJ
e m g /m l syru p
u ar c a Jc iu m
c o n cen h
a lio n s A Jo w e re d jn lr a c e ll l '
u ar ileiuń ņf m a n o r
y ga n s in c lu d in
g u te r u s

l'tŤţib . Th . ' " " ' " b ,a n ' "th. ' Yo ' " rial '" 1
a s u im a Ac tiv a te s a d e n ylc cl
an d c o pD
0 a d d itio n
J y a s e to d e c r e a se
Io b r o
n ch o d u a ti
on sa ı
bu tiu n o ] i
n h ib jt
s th e r e le a s e
f
ę!řīĮļ¢
iş d a ren e
rg ic b e ta
o
Ëi a l\ilrN
a g o n is t u s e d to c o n tr o lp r e m
am e a tu r e la b o
Y u to a r I r
p n ĵ 5 om
g /5 m l Iv Y u to p a r T a b 1o
m g p o

Scanned by CamScanner
■ 154 ı rÆ lA Te x tB o o k o F Phar'"ology
rm a c o
lo g y o f Dru A

m
ı
c ti

昌团团团团团团团■
o n
lia iaäh e ra lN e rv o u s s y s te m
B IN D IR E C T A C H N G

A M P H E T A M IN E S T h e se a r e n o n < a le c h o la m jn e sym p a th o m im e tic a m in e s w ith


C Ns
tim u la n t h a v in g im ic ı
c in g th est【UChu' i i
p h a rm
s a c o lo gy p ro lile ephe d r in e By m
.
'
c a te c h o la m in p h e ta m in e s :i
:X
e n eu ro m i tte rs d r e n a lin d - ' "
n o ra e an
j
m on oam in e r e le a s e itħin th e b r a in
re u p ta k e a n d s ig n a llin g w

M ed u n iım f a c tio m It s tim io


o u la te s th e r e le a s e o fn o r e p in e p h r in e ı m

r e c e p tu r s A t M g h e r d o s a e s th e c a u s e z e le a s e o f d o p a m in e fr o m th e
g y
s y s te m an d th e ig m
n s h ia ta l d cp am in e s y s tem s It n a y a ls o a c t a s a
】 d ir e c t
į g 5 H T re ce
p? ts a n d m a y in ħib it m n n n am n
i e ox id a s e o d A o )

M a
J ¥ s u se d in th e tr e a tm

Ĺ
d e n t o f se v
er I d is o d
e in c lu
'
"ghtīedmionËased . caı
o r i. N s u ic tiu .
s d in g s th m a h e a r t fa ilu
patients . r h in itis
i , c t.
Tiiåşbý
ı re
Ry to a ı
te . Ti. . ° j

I
.
n a rco le p s y an d d e re s i
p s o n It h a s b e
" D a m m a co m e 1e ss e x te

m
5 Jo n s iv e d ?
m g fc fu ao h e n 5 y u se th e dv
m g) o ra ı A dz ť a e n t
Deæ
dine5agtab en y s J(R o D T .
I\elamine5-JOmgoralMethedrne5mg ņ rr iT b 9
J ,\
ı
W A ko v az ln j, c tio n 5o m g / m L iv c o r
p he? In
a j. . tio n so lu t io 5o
* P h c d l jn n
g / 'm L inv
Ujja\ehjccti. ' " p 5 0 8
m
"
' g im j v

Scanned by CamScanner
ti ı r屋 國 IA T e x t B o o k o f P h a rm a
W !I r tm 1
a ç o lo g o f D r L ıA c t in g o n p
e E æh e rà l Ne r vo r s s y s te m
L
ıt is th o 云山m t ic a m in e th a t in c n e a s e s b o th \ to lic
M E T A R A ĦH N O L a p o te n t sym p a e an d

tlia s to lic b lo o d p r es s u re S rß 9 1 J J ïT

M e a n i a m o f . c ti" " t . c ts o n b o th . I' "energi ' " c e p to . b . t app ea rs to h °


f" ?ftė c '

It ts b th l d r e n e r g ic r e c e p to rs b u t a pp e a rs i '
Ĥ Ļ\
o n d ıe n e l g ic r e c e p to r s a c o n o a a iį o

Its ts tfu gh p e r ip h l v a s o co n s
e ffe c t o n P a dre n e r g tc re c e p to rs a c o u e ra
t ・
tly In c r e a s in g y s te m ic p r e s
a s o n a lp h a 1 a d r e n e t g lc re c e p to r c o n s e q u e n s
w
[b o th s jn s to lic & d ia s t o lic ) iis e ffe c t is th o u g h t to b e a s s o c ia te d w ith th e in h ib itio n
h Ł\ yi
cy c ı
a se w h ic h le a d s to a n in h ib itio n o f th e p ro d u c tio n o f cA M P It r e le ase s n o re p in e p h r in e

if ic a t io n o f s J rm p a th ly t ic d r
Tr o m its s to r a g e s ite s in d ir e c tly a a s s o a ga

n s iv e s ta te o c c u r r in in Ľ
U Se s I t js d fo t io n d tr e a tm en t o f th e ac u te h y p o te g w i th iv / g n A n u a d re w ıle D
u se r p re v en a n g*

d fo in in g th e fo f th e hearť s p u m p in g a c tio n a s w e ll 5ĺ 9w e J 3' f U


s p in a la n es th e s ia I t is u se r c re a s rce o as
+
d 】
s I t is a ls o d d ju tiv tr e a tm e n t o f h y p o te n s io n
c o n s tr ic t in g p er ip h e ra l b lo o v e s se u s e as a n c e N E W lh e a
ı l

d h k a s s o c ia
d u e to hem o rr ha ge Re a c t io n s to m e d ic a tio n s su rg ic a l co m p lic a tio n s a n s o c te d

w ith b r a in d a ın a ge d u e to u m a o r tu m o r

+ U *
c e p to r B o th a a n d P p tm
m c e " n o n ıM m pı
C L I N T C A L U S E S O F A D R E N E R G IC D R U G S a ? q o n * t* ・a @ la b ıta ı
o l g o nl s t ı
m M e d ro x a ıo l
? lin Th ese dru gs a re u s e d in ıj h ĵ ĉ u 9 T5
1 C lzr d io n as cu la r s ) s le m n js u se d jn C a r d ia c a ır e s t e g A en a e (U l) B u c ı
n d o lo l

d in H t b lo k (A V b lo c k ) ゴコ団 イ

d o b u ta in Dop
T U ea r c 专
se -
C a r d io g e n ic s ho c k - m e e
, N o n s e ı
ec th re S e ı
em e
is o p r o te r e n o l : íi) g 9
i
fn p h e n to ı a m in e Ç \
2 Áwp¢ychir
A d re n a ı
in e
n s A cu te a n a p hy a c tic (o r ty p e I h yp e rs e n s itiv ity )
ŢĴŤ " " .
( )
ı

o i
D
i
n o il ] r o il T o la z o lı
ı
b
n e
e n a m ln e

1_
e g
o 1 a n la

ţ =
) p ra z o s ı
(ı n
go n la b

e * m

"
a z a n

h lm M
Y o

吵 A t ıF 旧 m
"
la 8 o n

n e

e xóo
1?

ı
e

3 H is u se d w ith lo ca l a n a es th e t ic to p ro lo n g th e a c tio n - a ? en a lin e (


v a so èo n s tr ic to r " " ì. . n
a m

a 吕e n t)
N o ru ◆n c h ra
ı S e ı lv
e c ı e
įo n ī Ê Ju d Įr
d H ıs u se d as a to ıs B r o n c h ia l a s tı
B r o n c h o d iı I l m p ro pn n o d
ı
1!0 ı
§ d o lo l *
gıı!T ım o lo ı #1 m lo n Æ P z a n tıg o n \s t e
W P ln d o ıo ı N e g m B u to x a m ln e
(q b u t ū ıq _ m ı
ııopmı

ó U s ed n C
ı p h th a lm ic ü o d ila te p u p il) 4 ep h e d r in e p h e n y le p h r in e M ņ C ır tıo ıo ı m
ı U se d as C N S s tim u la n ts Ħ
8 U se d a s a n o r e c tic s

Z
9 U te r in e reı
a x a n tan d V a t o r s a R Em H O R A N T A G O N I S T (N O N S E L E C H V E )

Scanned by CamScanner
g ¥
'
l t m B . o k o f p r" "
t j j ! . y . Te rn I jıs 9
ţ\

id e n in o f th e b lo o d v e s s e ls r e s u lı
s in lo w e r in f b lo o d p r e s s u r e v e s s e ls w
id en
w g a g o

ta c h y c a r d ia p a r tic tıla r ly p o s h u a l v o ın jtin & le th a ıg y an d sh o c k N J ßn r c r


»
uaesï tincreasesblood◆owtothesmucosa a bdo m in a i v is c e r a andl0wersbb?giļ pine
d t b lo o d p d ila to r it
an e rec n ess u re s it is u se d to ir e a t h yp e r te n s io n an d as a p e r ip h e r l v aso

has ffe đ th e p T ıı
p a th e tic s y s te m
n o e o n a ra s y m ï u

le a d s to
t % m ps e s v a so co n s tr ic tio n w h ic h c o r r e la te s ith
2) th e lie f f ig r a in
headacę a n d tiv a tio n w re o e
a c o f5 HTD re ce
ın
p to rs o n sen s o r d in g s f th
e su lts in th e in h ib itio n o f p r o in fla y n e rv e en o e tr ig e m in a l
ir u n a to r
y n eu ro p e p tid e re le a se
rha m la c o lo g ic a l ac tio n T in e dru g h as
p a r tia l a g o n is t a n d / o r a t

* ţ
n a g o n is t a c tiv it
' i
b y p ta m in e r s c
dopa m in e r g ic a n d a lp h a a ? y a g a in s t
e n e r ic r e c
g e p to r s d e
p e n d in g u p o n th e ir s it I t is

eigëİidproducesdepressionofcentra o o r c e n te r s ħ v a so m t
dig r a in e a tta c k is b e lie v e d t o
be d u e to g r e a tly in c r e a s e d
p litu d e o f p u ls a t io n s i
am
n th e c r a n ia l a r te r ie s e s
heningal b r a n c h e s o f th e e x te r n a l c a r o tid a r te r p e c ia Jly th e
y th e p a in in d e u c e d I t r e d u c e s e x tr a
b iò o d rr iñ o w c a u s e s a d e c lin e i
n th e a m
c r a n ia 1
p litu d e o f p u ls r tio n in th e c r i l
d e im Įe a s e Ė h y P e r p e r fu s io n o f th e te i an a a r te r ie s an d
r r to r f th b
y o e a "s i
B r a n d N a m e E r g o m a r 5 1t 2 m
i łr
W
a r a r te r
y
U ses Jt is d jn th e g M e d ih a le r E r g o ta m in e
u se tr e a tm en t o f h )p e r te n s io n an d h yp e r te n s iv e em e rg e n c ie s
a g tJ n g g r Ðr t
P h e o c h r o m o c y to n u

回二
v a so s a s m
p o f rap ı d d is e a s e d fr o s tb ite c lo n
au an id in e w ith d r a l
s jm d r o m e Im
p o te n c e an d p a ip h e r a l v la r
a s c tı d is e a s e
w a
lil%VE a l A N D a z A N T A G O N IS T S
D o5« 5 m V /ı
gı M M ı
? p reo
p e r a tiv w e p e a t if n e c e s s a r
y q2 4 h r P R A Z O S IN It i E l. .
B ra n d n am e m en to ı
a m in e A fe s ı n
i
i JĮ ľ o o 6ı1 : ° Tiv . a l a ? e n e r ic r e c e
g p to r a n ta g o n is t h in g
y a te je c tio n s a n d o z s ta n d a r d 5 m
g iv im phen
av o 1 o 2 s e le c tiv e ra tio

、 qgı
ţpł llę :
5
ĥ aß
iFfostate P r a z o s in an ta g o n iz e s p h e n le h i
b ts v §v ï o ]1 y p r n e (a lp h a l
H ow ev er d ila te s a r te r io le s m
a g o n is t) in d u d
o r e th a n v a in t
ce co n tr a c tio n s
T D ıA Z O U V E Jt s
js a c o m o d b e lo n s to th e M
p un
c la s s
ech a n is m of
be? e n e an d g of o a c tio n It b y in h ib itin
s u bs tih z te d d rg a n jc com ds kn d w a c ts
e r iv a tiv e s Tħe se a r
p o u n n ra s g th e p o s ts y n a p tic a lp h a (1 ) a d r e n
e arom a tiċ o ce p to
m 0n 0
q _ c ńng \ te m c o n s is tin fbe n
co m po u n ds con ta in ï n
g? o n e
rs o n
g o zm ] e le a e d n i c a te c h o la
e g in
m es (e p in e p h r in e an d n o r e in e
v as o d ila tio p p h T in e ) ltin g
n re su in p e r ip h e r a l

ı
n d ic a te d
use d to d e c r e a s ¢? id ħd s to
e p uı
m on aı
sm o o th m u s c le r e la x a tio n in th e e r i h
y v a s c u la r
r e s is ta n t e
(p Y R ) i n e r s is te n
p p e ra l v a sc u la h ır e an d p r o s ta te la d
p t
ū g w g n it
) ÇO 】ıg e s tiiv
ę h e a r t fa n u It is
re u se d a lo n e o r in b in
co m tio ith
a n w P b lo c k e r s in th e
B ra q d
N a 】ıte M in ipP r e s s 5 m g Cc a p s u le Pp r a z o s in 1 T a b l m
g

じ 了
: 惶

Scanned by CamScanner
i

į j
ı
屬回

Oiśé if a \ w o u ld b e to lo
w er it
A r e n e r ic
g re ce
p to rs Its e ffe c t o n b lo o d
öļ į W ţ u se d a s "
ympatholytic a n d
ibédc o r ig in s a n d p sycho
m y d r ia tic It is U se d in a le Im p
g e n ic o ń g in s
m o te n ce w ith v a sc u la r
" " o co n T a b le t 5 4
h yp m g o ra l Y
e r te n s io n d p m s t e e n la r e m e n t ı o h im b in
an
g t w o rk s b y b ı o c k in g th e a c tio n o f adie} į ń
e H y d r o c h lo id
r e T ab 2m g Y h im b in
sm o o th m e o f th e b la d d e r a n d th e blo o d v e s
s e l w a lls
o ķ

B r an d H ym ı
n am e o y s te c lmghb ı
usu aıym a jn ta in e d d o s e 2 to 1 o m g
in d a n es T ħe s e a re co m
p o t ın ds con ta in in

Ħ " ta n e ń r æ d to "
g an in d a n e m ie ty
' " '" r in o w h ic h c o n s is ts f
g o a

n e rv o u s
g.-'ţ esŁ
inıtr a c t k id n e y u te r u s ) T he y
sy s t m
SCUlare an d t is s u e (e g
e x is t p re s n a
y p tic a u y p o s ts y n a
B ra n d N p tic a lly d

.
am ◆ C a ld ıır a B m an
g ta b c a r d u r a x L 4 m
g ta b D o x a z o s in m e s y Ja te ĵ n o » bs ĵ q
Id '"
: ı
iíoclß
jYm cro sse s th e b lo o d b r
a in b a r r ie r T
m e ta b o lite s te n s iv e
he
a re
p r im a r il e x c
y r e te d in
ex
h e p a tic b '"
a n " " m .
Y o Jı u r in e
M f B JN E A pı U se s It is
an t a R a ı o id w ith a sy n th e tic
d ıu a u o n o f aı p ħa 2 a d r e n e jc b t
RJS ÐV iıßb s ć a 2 a d re n e r g ic r e c e
a c tio n ıt a ls o b lo k
th e 5 H T r rg o c k in tiv it p to r a n ta g o iıis

X
c
e e to r g ac
y w ith sh o r Ļ in d ic a te d fo
M e c h a n is m p t r th e
o f a c tio n
Tĥ e e x a c t
r e v eS r s a l o f- th e
m e c h a n is
m ı o r jts u
s e jn im n ł

/į tbl0
b th lp h a
andchoJinerícræ
epto. o th e r ^ '
" ' ' " S in itte
a an d b. ° ' '" " g ic re ce
p to r s th a t is
Ţ X . .
' U Se d a s a n

s in
a
g le su b s ta n c It b lo c k s

◆ i

Scanned by CamScanner
Scanned by CamScanner
4 4
1 T
r m B ' ' " ' '"
m m a c o ı
o g y o f D ru g s A c t
1
a C tiv a tio n o f P1 a d ren u g ic r e c e p to r
o n p e r
w e ra lN e rv g u s s y s te m \ i. =
/ 't iäģės o f a te n o lo l a ls o co m
p e titiv e ly b lo c k
br o n c h ia l a n d v a sc u la r sm o o th muse b e ta (2 ) a ? e n e r g ic res p o n se s in th e


Uë?ï iġ u se d a lo n e o r w it h c h lo r th a lid o
n e in th e
Eraiái(iameAct A te n o lo l ta b 1 o o
m a n a
ge m en to fhy
p e r te n s io n a n d e d e m a
m g A te n o lo l 1 o o m
g
in com b in a tio n w ith o th e r a n tih
}p e m iv e a ge n b e s p e c ia lly th ia z id r ty p e diuretic
D r E%Ħ\L I ts is ' '' r d io s e le c tiv e p1 rece
p to r b lo c k e r ith
w ra p id o n se t ' ' " y sh o rt
:f
Y Jj v ijJ ,
activityatth sy m
p th im
r
era pe u tic d o s a a o m e tic o r m e b s ta b iliz in g
C A R T E O Ľ O L It i ges m ra n e
: s a b e la ıa n d b e l 2
a (H o n « e le c tiv e )
d o es n o t 】
H p e s i n ffi
/ g c a n t in u in s ic s r n
} p a th o m im e b c

ļ ll n ıe
m o f ac tio The pw ėc h a n is m
þłè a ' "" " " " °° l re ce
p to in . "
n m o f th e o a ıla r
rs car d ia c u ssu e '"
It d o es N o t h a v e in tr in " id . . .
s ic .
hu I!Ol
Processjsinitiatedbyaenonectvebea an d b e ta 2 a
Ru e o u s
d r e n e rg ic
m or p r o d ...
r e c e p tu r bıo c ka d e
a n ti a n
an d a n a n ti ı g in a ag en Ļ an ' "hwertens i Fia g e n
g a n c o m a a ge n Ł t
fi¥þ ・o te in w h ile th e Ac id m e ta b o lite is 1 0
P 1 S E L E C TT V E a bo u t 2 m in u te d % b o u n d It is
p id d is tr ib u tio n h a lf life
A N TA G O M S T s a n 】
im in

ć'"ß rnilu an e a tio n h a lf li
fe o fabo
ra
o f
M m o p R o L o し lt j u t 9 m in u te s
ł
İ 1 ħe a c id ın e ta b li
s a com
pe litilre b e ta l
S e le c tiv e
o te h a s an
(c a r d io R p l

re ce
p to r

ora
" ' " g . B$ęi# Æ ł
" '
"
re u e x
ą e
t a tic ħy p

\ $ Ħ« í i í

Scanned by CamScanner
o W
ı o f D ru g s A w a a Jı6 7
"l a c o c o n b łm h e rá lN s y te m
[ e rv o u s s

f 5 h y d r o x y tr y p to p h a n (5 H T P e p r e '
prec u rso r o f norepinephrinand o o f
s e ro to n in in th e C N S an d in m o s t p e r ip h e r a l tis s u e s
irn
U ses Its p r im a r y c lin ic a l u sE is an an tM y p e r te n s iv e a ge n t rc T ı

B ra n d N a m e A 1d o m e t E s te r H C I In j 250 m g A ld o m e t T a b 2 50m &


M e d '"
f .'",
'

M e th y ı
d o p a 12 5 m g l
ri, ł
u Y M !

i n in h ib ito r
b x la s e in h ib ito r Rt s a
C A R B ID O p A It is p e titiv e d e c a r o y
a n o n co m
i e It s i m ix e d w ith
d e c a r b o x y la s e p r e v e n « n g c o n v e r s io n o f le v o d o p a to d 叩 a m n
f le v o d t o d o p a m in e
c a r b id o p a in h ib its th e p e r ip h e r a l c o n v e r s io n o
o p a

d e c a r b o x y la tio n o f o x itr ip ta n to s e r o to n in b y a r o m a tic L m in o a d d decarboxyla '


T h is
o st
tih y p e r te n s iv e a ly tr a is s io in p
g e n t th a t s e le c
b y in h ib itin g tiv n sm n
i il b le fo r tr a n s p o r t to t ie C N S It
t U ıe ı ï t is a n a n a c ts e
r e s u lts in in c r e a s e d a m o u n t o f ]e v o d o p a a n d o x ilr p ta n a v a a
r e n e r g ic n e r v e s
a ls o in h ib iķ th e m e ta b o lis m o f le v o d o p a h th e G
I tr a c t th u s In c r e a s in g th e b io a v a ilfib iı iıy of glic a d
guı e lin
trealment f P k i d i d N ım c A po G u a n e th id in e S u lfa te T á b 10 m g G u a n e th id in e 1 o T a b 1 0 m g , Is m
le v o d o p a It is u s e d in c o m b in a tio n w ith le v o d o p a fo r e h
t o a r n s o n s s e a se Bn n

i o f ]e v o d o p á Io
U s e s It is a n in h ib ito r o f D O p A d e c a r b o x y ı ase p r e v e n tin g c o n v e r s o n
h l d f f t o f lc v o d o p a ï t
d o p a m in e It is u s e d in p a r k in s o n d is e a s e Io r e d u c e p e r ip e ra a v e r s e e e c s
N EU ı
Į O M U S C U L A tĮ B ıO C K IN G A G E N
h a s n o a n tip a r 】 d n s o n a c tio n s b y its e lf
a r e in te m is s io f im p u ls e s a t th e s k e le ta l n e m o ın a r
gs t
J e Ħln r J 】p t tr a m m n o n e rv e
B ra n d N am e to d o s y n 2 5 m g o ra l D ru
la r N o n
s ta b iliz in g b lo c k e r s (N e u r o
đ io n T h e y c a n b e f
o ty p e s c o m p e titiv e ,
tw o m u s c tı
: o iJ» r r u iu n
(N l r D ep o ı a r iz in g
;ì n Į ry ¡
b ! dep oı i
a r iz n 吕 8a e n ls ) o r n o n c o m p e ti tiv e d e p o la r iz i n 吕 g
a e n ts e u r o m u w a
D R U G IN H IB IT N A S T O R A G E ı t a c tio n a n d th e y a r e
A ¢e n s ) B th p r e v e n t a c e t y ıc h o li n e fr o m t i gg e r in g t h e m u s c e c o n r
(l n ? ! l o r

R E S E R P IN E ı
t is lk a lo id Jb u d in th e ts o f R au m o lM s e ıp m lin a a n d R t10P11 Rt d l d u r in g e le c tr o s h o c k , in c o n m ıls iv e s ta te s
u s e d a s a n e s th e s ia a ju v a n s a s r e a x a n ts
an a n ro o t
in h ib its th e p ta k e o f n o r e p in e p h r in e in to s to r a g e v e s ic le s r e s u ltin g
u in d ep ı
e tio n o f
a m in e s a n d s e ro to n in fr o m c e n tr a l a n d p e r ip h e r a l a x o n te r m in a ls
c a te c h o ı
s ke ı e ta ıM u s c ı c o tı
e N ı n ı
c
M e c lia n ia m fa cdon I【a c ts th r o g h in h ib itio n o f th e A T P / M s p u m p r e s p o n s ib re fo r th e li i
o z'
u M t 1 :
R e c e p to r s (N ıı)
s e q u e s te r in g o f n e u ro ı s m itte r s in to s to r a g e v e s id e s lo c a te d in th e p \
r a rı a p tlð n e u r o n x l l r9 n
ı
M o to r N ・u ro n
The n e u ro b an sm itte rs th a t a r e n o t s e q u e s te r e d in th e s to r a g e v e s ic le a r e r e a d iı m e ta b o liz c d ī ir ıd
y
by m o n o am in e ox id a s e (M A O ) c a u s in g a r e d u c tio n in c a te c h o la m in es

U It is d n& ı 1 1 N m ıłım ıa r b lo c k in g a 吕e n ı
a
ses u se a s a n a n tih y p e r te n s iv e a n d an an tip s y c h o tic

h l t th e u sc u ı
a r
g e n ts w h ic h a c t o n p r e p a r a
le x a n t n e u ro m
u s c le
a
D R U G IN H IB M N G N A R EL EA S E f & ł9 l s ë S k e le ta l m re a re a

r a lly in th e c e r e b r o s p in a l a x is to re d u iıs c le to n e
lu n c tio n /m u sc le fib r e it s e lf o r ce n ı ce m
B R E TYU N E rt is b ro
b e ltz y l q u a te m a
a m o
w a m m o n iu ın co m poun d w h ic h şęlssţiyely i
h e m u w
a c c u m u la te s in s , a c tin g m u s c le r e le (a n ts
w p a th e tic g a n g ıia a n d th e ir p a s t a n lio n ic d re n
g 吕 a e r g ic n e u r o n s It in h ib its
th e r e le a s e o f n o ıe in e h r in e
p p
M e ch a n is m o f a d io n ï t in h ib its n o re p in e h r in r e le a s e b y d e p r e s s in
p e
g a d rm e r g ic n e rv e 9 n 9n J ig i
te r m in a i e x c ita b ilily
U sea ıt d e p r e s s a d r e n e ı ic n e r v e
g ta m jn a l a b i】
e x c iı i It
ó b ıilla tio n a n d v e n i c u l a r a ır h th m ia s
v a】
so su pp re s se s v en tr ic u la r īd u )h įn 9 /
y

Scanned by CamScanner
o 66 ı ıÊI A Te x t B k fP ha lo g y aan 67
o o o rn ia c o
(v ° acolo o f D ru g s A Ea o
W p
c n e r ip h e ra l N e rv o u s s y s te m
IW rT 1

P r e c u tT s o r o f n o r e p i n e p h r i n d o f 5 h y d r o x tr
y y p to p h a n (5 H T p ) th e p re c u rs o r
S e r o t o n i n th e C N S a n d in m o s t o f
p e r ip h e r a l tis s u e s
U Ses its p ń a r y c lin ic a l w
m is an a n tih y p e r te n s iv e a gen t 4 irn z n ß lj
B ra n d N a m A 1d
e e t E s te r H C I In
M th y ld o p 125 m g
o m
j 2 5o m g A 1d o m e t T áb 250 n tß Medimbpsotab
e a / ß z i J:
ai qs J on

C A R B ID O P A It is a n o n co m p e titiv e d e c a r b o x y la s e in h ib ito r It is an in h ib ito r o f D o p


A
d eca rbo x y la tin g c o n v e r s io n o f le
p
§Įia p ら
se re v e n v o d o p a to d o p a m in e It is ix e d ith
m w
c a rb id
m " b .: ł
in h ib iķ th e
pa p e r ip h e r a l
o
c o n v e r s io n o f le v o d o p a to do pa ・

d e c a rb o x
y la t io n o f o x itr ip ta n to s e r o to n in by a ro m a tic L o a c id d e c a r b o x yfä
T h is
re s u lts in in c r e a s e d am o m t o f le v o d o p a a n d o x itr ip t a n a v a ila b le fo r tr a n s p o r t tû tiie C N s I
t
a ls o in h ib its th e ın e b b o lis m f le v d o p a in th e G I tr a c t Th u s in c r e a s in g th e
o o b io a v ā iï iiþu it o f
y lin
le v o d o p a It is d in c o m b t i o n th id in e S u lfa te T a b th id in 1o T a b 10 m g Is m e
w ith le v o d o p a fo r th e tr e a tm e n t o f P a r k in A p G 1om g G
d is e B t a n đJ N
so n s am e o u a n e u a n e e
a se
U Ses 1 t is an iııh ib ito f D O PA d e c a r b o x y la s e p r e v e n tin g c o n v e r s io n o f le v o d û isá
r o
to o 3 25Ħ
gJv
d o p am in e It is u se d ir ıp a r k in s o n d is e a s e re d u c e p e r ip h e r a l a d v e r s e e ffe c ts o f le v o d o
has n o a n tip a r ı
c in s o n a c tio n s b y iķ ?
p a It :! ĥ qo bo
國 N E U R O M U S C U L A R B L O C K IN G A G M
B d N Lo d
ra n am e o s y n 2 5m & o ra l n ag u T a
n o íJ J n u į
D R U G ひ 好 书 B IT N A S T O R A G E iTß
foqbİ 。

R E S E R P It is D ca 】
o id fo tm d in th e r o o ts o f R a u u Jo ljia s e ı m tin a a n d JŁ

::
an a
p It
in h ib iķ th e u p ta k e o f n o 呷 in e p h r in e in to s to r a g e v e s id e s r e s u ltin g in d e p ie tio n o f
c a te c h o la m in e s « n r l s e r o to n in i
n o m m tr a l a n d p e r ip h e ra l a x o n te ? in a ]s
M ħa ııis m f a c tio S k e le ta l M u s c ı
e N lc o t ln ı
c
e c o m It a d s th r o u g h in h ib itio n
f th e A T ? / M g 2 p u m p r e s p o n s ib le fo r th e o Ðrll 1 o ì u ld İ
s e q u e s te r in g o f n e tır o tra n s n ı
itte rs in to s to r a g e v e s ic le s lo c a te d in th e N
presyna? n e u r o n nm u 9 rr M o to r e u ro n
T h e n e u r o tr a n s m ittp r s tħa t a r e n o t s e u e s te r e d ĵ n th イ■国虹
q e s to r a g e v e s ic le a r e r e a d il m e ta b o liz e d b Ðs i Į o d ĥ j r j r
y
b y m o n o a ın in e o ocid a s e 0 ) c a u s in g a r e d u c tio n in c a te c h o la m in e s L J
U lt js d F ig 3 1 1 N la r b lo c k in g a ge n ı
s
sea u se a s a n a n tih } p e r te n s iv e a n d a n a n tip s y c h o tic
e u ro m u scu

h a ra l t th ı
g e n ts w h ic h a c t o n p r e p
a e n e lu o m u scu a r
D R U G IN H IB M N G N A R EĽ W b i łs l s ê S k e le ta l m u s c le re le x an t a re a
E
b i l a x is to du u s c le to
c e n tr a lly in th e c e r e r o s p n a
re ce m n e
B R E T Y I IN E It js
ju n c« o n /m u s c le fib re its e lf o r
b e n z y l q u a te m a r
a b ro m o
y a n m lo n iu m co m po u n d w h ic 】 龠 sti Ýe ly

a c c u m u la te s in s n ı a th e tic .
fl p e n e r a i ry a c tin g m u s c le r e le x a n ts
y p g a n g lia a n d th e ir p o s tg a n g lio n ic a d re n e rg ic n e u ro n s It hibits ı
z lid İ ıñ Jl
r
th e r e le a s e o f n o r e in e h r in e
p p
M e ch a n is m o f ac tio n It in h ib its n o r e p in e h r in r e le a s e by dep
p e r e s s in g a d re n e r g ic n e rv e a v19n Ĵ I8 T O
te r n ıin a l e x d ta b ility J ;q

u se l It d e p r e s s d re n e r g ic
a n e rv e a l e x c ita b ilit
te l m ir ı It a ls o
y su p pr e s se s v en tr ic u la r Tńı
u]ijı
rcjv
ibriJJation a n d v en tr ic tıla r a ır h y th m la s

Scanned by CamScanner
■ .
" . 68
Rg g m m m B
r . . . . .. .. ..

d ū lt
°' D
"

1 v 0 4 to o 5
ru g s A c t '" ' o" n p e r i' " '"

g p e r k g b o d y w e ig h t th e n o o 8 to o 1 o ın g p
m
e r kg b
I 8 ı6 9

o dy
q
C L A S S IF I C A H O N O F N E U R O M U S B L O C K IN G A G E 闪了S


:2 o t' ) 4 5 m n
i iu te a fte r fir s t d o s e if r e q u ir e d fo r lo n er )
g p r o c e d u r e s (s u r g y

u ıd
d e p o la ń z in g N ĦO b lo c k e r s (e g R o c u r
"
iu & o th e r
每 o N Iu Jw p a n c N
u ro n m o n
F n th e tic a n
a lo g s
d in g in l f
ıı m & o th e r d r u g s en n iu m o r i
r u m ) a r e e x a m p e s o s y
e r s id e
N dep la r iz in g N M J b lo c k e r s
D e p o la r iz ln g N M J h ic h h a fa b le p h a r m a c o k in e t ic p r o p e r t ie s a n d fe w
c u r a r in
o n o e w v e m o re v o ra
L c t in g E 8
b lo c k e p E g of
d tu b o
s h is ta m in e r e e a s e )
o n g a l
Su c in
cı y lc h o lin e įt ( e g Ie s
co n tr ib u te
T bo b h ic h la r b lo c k e rs ca n
3 m e c h a n is m s y w d e p o la r iz in g
u c tır a r in e D ec a m e th o n itım n o n n eu ro m u scu
a re
P a n c u n »n itım tı
ıe re
u s c le r e la x a tio n
D o x a c tır it ım : m
to
(A C H ) fo b in d in g
c o n c en tr a tio n s th e y co 呷 e te w ith a ce ty lc h o lin e r
G a lla m in e tr ie th io d id e +o ıJA A t lo w
1 la jıın c tio n
In t e ıt e d ia t e a c t in ic o tin ic p to r s ite s in th e k e le ta l m u s c le n e u r o m u sc u r
p tic
n n re c e s
g n a
loq p °s ts y to
R o c tır c»n iu n Ļ A tr a c tır o n i\u r Ļ la x a n ts ls o in te r fe r e ith p r e s y n t ic r e le a s e o f A C H * om ın o r
d e p o la ń zin g re a w a p
C is A tr c bn o >{ 2 N on
e ls a n d
t ır o n it ıır Ļ V a c u ro n itım
d is m (s ) B o th b lo c k s o f N a ch a n n
d in till p o o r ly d e r s to e ch a n
sı t t in g n e rv e e
n gs by s u n o m
T h e p r e s y n a p t ic
to r a c
ic o tin ic h b e e n im p lic a te d
M iv a c tır it ım b lo c k o f p re syn a p tic n a u to r e c e p to rs av e
th e m u s c l t y p e
p to rs h a v e a d iffe r e n t su bu n it co m p o s itio n co m p a re d to
n ic o tin ic re c e

t iIn Ŕ Ìn n ic o tin ic rece p to rs

N D la r iz in g la r B ı to b lo c k a d e
o n e p o n em o m m cu o cke rs tr a tio n s th e y c a n ls ro d u c e a m o re In te n s e m o r
A t M gh e r c o n c e n
a o p
W B O C U R A R IN E It is th e p r o to ty p e " epolarizing s k e l, ta l . u s c l. .E l_ . Àĥ i . Th e jı
3
u e i tıy ĵ
ı lo c k in g t h e p o r e o
f th e n ic o t in ic re c e p to r c h a n n e l c o m pı
e x

a c tiv e in g r e d ie n t in c u ra re th e S o u th A m e r ic a a r r o w p o is o n

M h is m f a c t i It is s e le c t iv e c o m s k e le ta l u sc ı îJo J in b
e c a n o a p e titiv e an ta go n is t fo r m e n ic o tin ic Ĵ in ĵ 8 【ヨ
eJo[cĺ 3í
re c e p to r s (N M t i s s u e c o m p o s itio n o f 2 a P Y a n d ö s u b u n its It b lo c k s th e
) th a t h a v e a j fl
l
N a ◆ i
o n s B e c a u s e th e b in d in g o f d tu b o c tır a r in e is c o \ 硅tiv e its e ife c ts c a n b e r a p id ly
r e v e rs e d b y a d m in is te r in g a c h o lim x te r a s e in h ib ito r (e g n e o s ti m in e ) w h ic h in c r e a s e
g
sy n a p « c le v e ls o fo ıi n e .
P
A s a r e s t ıll o th e r s y n th e tic nonepolańzing an a lo g s w ith fe w er s id e e ffe c ts a n d m o re - b
fa b le p h a k in tic p r o p e r tie s h a
v o ra a co
rn ı e v e re p la c e d iı
s c lin ic a l u se

I n d ic a tio n s E d o tr a c h e a l 血 红 山a tio s k e le ta l m u s c le r e im tio d l


n n a n u r in g su rg e r y o r ge n e ra
a rı
aes th e s ia

C on lıa in d ic a tio n s H yp e r s e n s iM rity P re g n h e a r t d is e a


a n cy se

匡 S id e e fk c ts H yp o te n s io n s k in ıa s h flu s h in & u r tic a r ia in c T e a s e tio n s e y e s N o se SZ O l a s ys F ig 3 ı2 M ech a n is m (s ) o f a c « o n o fn o n d e p o la r iz in g B k e le ta l m m c le r e la x a n ı


s

J ."d 9 "
s e c re r

th r o Ļ b r o n c h a óp
陟 c y a n o s is r e s p ir a to q d e p r e s s io n ta c h y c a r d ia
a asm
' r e lm a n ts d u r in g s u r g e ry gen era l
" ' . " " " " a " e
. " a "

30 in te to l l / 2 h o iīiilĮflĝ ónc
m u u r p la s m a h a lf Jife l to 3 h o u r c ro s se s p la c e n ta e x c r e te d
d ig h t fte r 3 0 in te s to
g per kg bo y
m u o n e

:x%
w e a
0 0 4 to 0 1 m

ith p r e c a u tio n s d u r in g p r e g n a n c y la c ta tio n


tiv ity U se w
d is e a s e "
e ie c tr o iy te d is e a s e d e h y d r a tio n r e n a l a n d c a r d ia c
im b a la n ce r e s p ir a to ry

ds pea k c o n c e n tr a tio n 3 to 5 m in u te s c ro sse s


rh u k in O tio 3 0 to 4 5 se co n
m a co e tic s n se t a c n

ĥ JrJ w Ľ !q P la c e n ta e x c r e te d in u r in e

Scanned by CamScanner
回国 团 团{ j 7 o 【 ĺ 0 姻 lA Te x t B k fP ha
o o o rm a c o
些y (V 이

D n ı吕 in te ra c «o In d gı
y c o s id e s
n s n e 1ır o m u s c u la r b lo c k a d e ith in
c ıE a s e w am o c lin dam
lin y c in
com y c in q u in id in e lo c a l a n a e s th e tic s n m o tic a n a lg e s ic s "
W n m
D o l a ge A đu lt 】
n tr a o 0 4 to o I
v e n o tı
s m g p e r k g th e n ın a jn te n a n c e d o s e o 0 1 to o 1 "
k g th e n
88
m a in te n a n c e d o s e 0 o 1 m 1 h !U r T
g p e r k g b o d y w e ig h t a R e r 3 0 m in u te s to l h o u r s
D rniı sr!q

I I I mauı
r, ・
ith tħe h o lin e r g ic r e c e p r s ite s in u s c le d 呷 titiv e ly b lo c k in g
b y ċ o m b in g
, in w c to m an co e
"
(d a )
c tiv a tio n o f
r
itte r a c tio n o fa ce ty lc h o lin e It b lo c k s th e ac tio n o fA C H an d p re v e n ts a
sm
r rjı1 Ð u th e tr a n
ty lc h o lin e
m u s c le
co n p r o c e s s It c a n
tr a c tio n a ls o a c t on n ic o tin ic p re sy n a p tic ace
th e
C w h ic h in h ib its th e r e le a s e o f A c h
W P ın c u r e n n h ım «e w ın ın
o i q Ðĵ T t p to r s
re c e
i= T ' C « n p ıd lh ı* \ TO F = 10 d d ju n c ts to a n th e s ia to in d ske ı l u s c le ı
ax a tio n an d to
It is e ta re
m d ic a tio n
u se as a es u ce m
7o F R 13 TO F R 0 5 (F ıd ı)
h an a ge m e n to f p a tie n ts u n d e r g o in g m ec h a n ic a l v e n tila tio n
Ja c ilita te t e
4s u p n m
m ' " « a H 4 *ı
s)
lclìı
bsī
Sh ııb ı
k th e d ia c d ta c h y c a r d ia d o c c a s io n a lly
e ffe c t It b lo c s c a u s e s in u s an
ĦR m in « I m io
S id e
car v a g u s a n m a y
R R U o
d in d c a r d ia c o u tp t
h yp e r te n s io n an cre a s e u
iì Ðq
C m en ı
ı» m o fN ıu ro m u ıc u ı
a r b lo c k !O
y f
B d d e p o ia r iz in g la r b lo c k in g d r u g (N D M R D ) u s e d a s a n a d ju n c t to
P a n e Įs a n o n n e u ro m u scu

lÀĺ
ra n n am p iu 】
es anc w n m n je c tio n F a n cum n pav u lo n N eo cu ro n
tio n It h a s a lo n g e r d u r a tio n o f a c tio a lc in
per m L , Jriiı ,to in d u c e s k e le ta l m u s c le r e la x a n m g
" . ita b le fo r a in ta in in la r r e la x a tio n d u r in j
a o T s u T g ic a l

ÈĢŁ ıĝ Ë
D O X A C U R IU M . ë su m g n e u ro m u sc u g m
It a c ls a s m d e re 】 t h a v in
a x an g th e le a s t m p id o n se t an d
a c tio n It is su a b le fo
iı 】o n g d tm
r tio n s u ıg e r ie s It in h ib its tr a n s ın is s io n o fn er v e
b in d in g w ith c h o lin e r g ic r e c e to r s i ta g o n iz e a c tio n a fa ce w
p an h o lin e
M e c h a n ia m o f a d io n It b in d s c o m p e titiv e ı to c h o lin e r ic r e c e t n eu ro m u scu la r b lo c k in g a g e n t w ith a ra p id to
y g p o r s o n th e m o to r e n d
l t t in te r m d ia te d u r a tio n It in h ib its tr a n s ın is s io n o f
p a e o a n la g o n iz e th e a c tio n o f a c e ty lc h o lin e r e s u ltin g in a b lo c k o f n e ä=iķibar e

tr a n s m is s ia m iz tio fa ty lc h o ı
in e
e p o l a ńz i n g ) T h is a c tio n is a n ta g o n iz e d b y a c e ty lc h o ih i s e r e c e p to r s ite s an ta g o n e a c n o ce

in h ib ito ıs s u c h a s n e o s ó m in e
g M « h a n ia m a c It ts b y
co m pe g fo r c h o lin e r g ic r e c e p to r s a t th e m o to r e n d p la te
tin
In d lc a d o n Eıdobacheal in h ib ito r s s u c h a s n e o s tig m in e a n d
a n ta g o n L z e d b y a c e ty lc h o lin e s te r a s e ir ı
"i Ș¢
ł
h lb a tio . k e le ta is
anaesth
n l m u s c le r e ta x a n t du r in g s° īrn ã Ģ °n
, dpĥ um It a c ts b y c o m p e titiv e ly b in d in g to n ic o tin ic c h o lin e r g ic r e c e p to r s ıi n e
b in d in g o f v e cu ro n iu m de c re a s e s th e o p p o r tu n ity fo r a ce ty lc h o lin e to b in d to th e ń ic o tin ic
S id e e ff« tı S 】
dn ıe c e p to r a t th e p o s tju n c tio n a l m e m b ra n e o f th e m yo n e u ra l ju n c tio n A s a re s u lĻ
ra s h m ic a f ia h
ı
yp o te in s io n m y o c a r d ia l in fa r c tio n b r o n c h o s p ąșĦ
\ h e e z in s r e s ir a
p w d e p r e s s io d ip ]o p ia
.W ņea ßs ð
\ a t i o n is p r e v en te d c a lc iu m io n s a re n o t relesed a n d m u s c le c o n tr a c tio n doe s n o t
n e ak n e ss
w
p r o lo n g e d s k e le ı
a l m u s c le reltion
nonBMlsT
Ph m a c o k in e tic l E ica
e te d in u r in e u n c h a n
g e d n o t m e ta b o liz e d
D In d ic a tio n u s c le
tu吕 in te r a c tio ıu In c r e a s e d n e u r o m u s c 】 b F a c ilita te en d o tr a c h e a l in tu b a tio n s k e le ta l m r e la x a tio n d u r in g s u rg e r y
u ar lo c k a d e b d r u 】
lo c a l a n a e s th Æ c s lin c y g jk e h a lo th a n e te tr a c y c ljn e sn gq em lpa n a e s th e s ia
o m y c in c lin d a m
y c in lith im
"】 ce p h e n ß C O n lr a in d ic a tio H y p e r s e n s itiv ity u s E w ith p r e c a u tio n s in p r e g n la c ta tio
y o in c a r b a m a z e p in e d e c r e a s e d u r a ti n s a n c y n
o n o f a c tio n a n d
c a u se p r ù lc h g fo ins e t JĴ ad w b tio n e e c tr o ly te im b a la n c e r e s p ir a to rr d is e a s e c a r d ia c d is e a s e
l
D o ııg ¢ A d u Jt lv r h a m ia c o k ln e ı
0 0 5 m g to 0 o 8 m ic s D tio n o f a c tio 30 in u te s
8 p er kg y n
u ra m
w e ig h t fo r
bıo c k a d e M a in te n a n c e 0
o 25 m g p e r k b o d w i p r o lo n g e d n e u r c Þm u s a ıla r 1 ó hn e u
m o !
g y e 吕h t
C M JD 2 b 12
y e a rs by ln u a v e n o tß t o u te o o 3 lo o o 5
m g p e r k bo d w
g y e lg h t
P4

Scanned by CamScanner
P
蜀 国 ■■ E拐
r r
1 目园IA
「 Te t B o o k fP ha nĮ
x o ł
a c o 匽园
ı

D ru 吕 in te r a c tio lu R o cu ro n iu m a c tio n is b lo c k e d b y phenylepe in c re a s a c tip n


a n a e s th e äcs :1 1 Ißr ıĵ
S id e e ffe c te : V o ın itin g n a u sea s k in ra sh u r tic a r ia c ha n ge in b lo o d
bro n c h o sp a s m a pn e a c y a n o s is r e s p ir a tio n d is tr e s s
: 1U re

U Se s
It is n e u rD m u 5cu la r b lo c k in g a g e n ts D ru g s th a t c a u s e
in id
a n am o s te r o
nonepolarizing n e u ro m u sc u J? b lo c k e r
m o dem a n a es th e s ia to ı
a c ilila te e n d o tr a c h e a l in tu b a tio n a n d to p r o v id e s k e le ta l m us l
c e
Fq i Đ ĉ Ł
D o sa ge In tu b a tio d u lı
s Iv o 6
n a m g p er kg bo d y w e ig h t
B ran d N am q Roa iru B ro id e In n cr l o
ır o n n m je c tio n 1o m g Iv z em u ro n 1o m g Iv q 9 :


M £
北 ぷ u sm a n d d is tr ib u tio n
. '" . " .^ . . . . . . ... . ,。 Ėį 女d u e

Y : ÏĪŤĮ Ś a .
S
ū s A jT M c U R IU M It is
r e le a s e a n
n eu ro

d its
m

s id e e
u sc u

ffe c ts
la r b lo c k e r (n
fe w
o n d e p o la r iz in g ) d 】u g It D o e s n o t

k e h is ta m in e a re er
pro v o
M in iį in c tio n
It b in d s to th e ic o tin ic ty c h o lin e (Cho1ĵ nerc) r e c e p to r s in th e
Ä& £
ł o f A n a ce

d p la te an d b lo c k s a cc e ss to th e re c e p to rs In th e p r o c e s s o f b in d in g th e r e c e p to r is
p °to r en

a c tiv a te d c a u s in kn d e p o la r iz a tio S in it is n o t d e g r a d e d in
Ĥ m l g a p ro ce ss ow n a s n ce

th e n eu ro m u scu la r ju n c tio n th e d e p o la r iz e d m e m b ran e re m a in s d e p o la r iz e d an d

u n r e s p o n s iv e tD an y o th er im p u ls e c a u s in g m u s c le p ara ly s is

F a c ilita te f d o tr a c h e a l in tu b a tio n s k e le ta l u s c le r e la x tio d u r in


,b*ięiDn o en m a n g su r ge ry
r ŞÎ raesthesia
.

C o n b a in d ic a « o n s H y p e r s e n s itiv ity u s E w ith p r e c a u tio n in p re gn an c y la c ta tio n car d ia c

fļ ehydration r e s p ir a to r y d is e a s e

Ph a m aco k in e « c s O n se t a c ū o n 1 to 3 m in u te p e ak c o n c e n tr a ū o n 2 to 5 m in u te

M ugu iń te r a c tio n s In cre a se d n eu ro m u sc u la r b ı


o cka d e w ith d ru gs am in o g ly c o s id es

jT
;
lin c o m
Ï yd n , c lin d a m y c in q u in id in lo cal a n a e s th e tic s tic lg e s ic s

X
e n arco a n a lith iu ın

X,Ī
.
'" le tr a c c lin e
" _ o m u s c u la y
.
r b ]o c k h (n on d ep o D 】
a r is i ) 0 1 5 to 0 2 m g pe r kg b o dy w e ig h t C h ild a g e 2 to 1 2 y e a r IV 0 1 m g p er

e= a s

Scanned by CamScanner
团团■ ı7 # 1 ı rËğl A Te x t B o o k o fP ha rm a c o '"
gy
1
N YV A C U R IU M I t is s h o r t a c tin b lo c k e r d o e s d
g c o m p e titiv e n o t n ee r e v e rs a l It is
n oń
d epo la r iz in g n e ı
ır o m u s a ıla r b lo c k e r v ib J tij
b re ,
M echan is m f a c tio It b in d s
o n
p e titiv e ly to c h o lin e r g ic ıe c e p to r s o n th e m o to r
co m
lo a n (a g o
n iz e th e a c tio n o f a c e t l h li
endplate
n e n Es u ltin g in a b lo c k o f n e tır o m u s c u la r
I t b in d s c o m p e titiv e l to c h li
y c o
transi§ in
śił
n e r g ic r e c e
y o
p to r s o n th e m o to r e n d p la te to a n ta g o n iz e th
a c tio n o f a c e e
w lc h o lin e r e s u ltin g in a b lo c k o f n e u r o m u s a ıla r tr a n s m is s io n T h is à ti
ç o ıu is
a n ta g o n jz e d b
y a c e ty lc h o lin e s te r a s e in h ib iı u r s s u c h a s n e o s tig

S id e e ffe c ta H
y p o te rıs io n b r o n c h o s p a s m p r o lo n g e d ap n e a w h e e z in g r e s p ir a to r y d is tr e s

i X
s
d ip lo p ia s k in r a s h ıM ic a r ia w e a 】
m m Đ Jc d lıl r : d
C tr a in d ic a tio , ... . Ra l. . . . E s i. To fa c ilita te tr a c h e a l in tu b a tio n a n
o n H y p e r s e n s itiv ity u s E ith p r e c a u
d e h y d r a tio
n s w tio n s in p re gn a n cy ı
a c ta tio n
Siv, u s c le la tio n d u ń n g eu rg u y o e cha n ic a l v e n tila tio n It is e d in
n elderl re s p ir a q d is e a s e J iJ jv o T ◆ ro v id , s k e l, I m re x a r m
[t d th e r p d f d fm u scı ta tio n
Ca l in w h i h a b e r io x a
U It is d to fa c ilita te an es th tic a o ro ce u re s e e r
ae u se e n d o lr a c h e a l in tu b a tio n s u ıg e l y gen e r a l a n a e s th e s ia

ıni1_ le b y
d la x s k e le ta l m u sc
/ b §z d in th e em rg e n c y
e ro o m an s u r g ic a l se ttin g s to ra p id ly re
i u ei JJ lt is u s e
u s c u la r tr a n sm is s io n
e u ro m
J JI gı
riŔol ・ blo c k in g n
i D E P O L A R IZ ı
ı N G N E U R O M U S C U LA R B L O C K E R S
d kn o w n as
p o u n d b e lo n g s to th e c la s s o f o r g a n ic c o
-
S U C C IN Y L C H O U N E It is a u a tm ıa ı s lc e le ta l m H O N IU M T h is co m m po m s
q y u s c le r e ta x a n t u s u a ll
y u se d in th e fo rm D E G B ĹM E T
o f its b r o n ıid e D tlo r id e o r io d id e I t i h l t d d e r iv a tiv e s o f c h o lin e It is a s h o r t a c tin g d e p o la r iz in g
s t e o n ly d e o la r iz in
p g sk e ı e ta l muscleriıdĖahtlL ıc lf c h ū
in e s T h e s e
ı a re a c y a e
li
y
c n ic a lly a v a ū a b le It is a d ep o la r iz in g r e la x a n Ļ a c tin la r b lo c k in g
g in a b o u t 3 o s e c o nd s andhï arrr musdle?ant o i n e u ro m u sc u a gen t
d u r a tio n o f e fte c t a v e ıa in d ır e e t ó d ts
g g v e m in u te s ila ty 1C h o 】
in e a n a c
o
M e ch a n is m o fa c tio n lt B in d to th e n ic o tin ic re ce p to r s It is s im r to a ce
# th e
M e cha n is m c h o lin e r e c e p to r In th e p r o c e s s o f b in d in g

be
o f a c tio m T ħe m ec h a n is a n o f a c tio n o fSu c c in y lc h o lin e in v o lv e s w h a t a p d ie a ts ıto z h a s ì a ip a r t a i
l a g o n is t o f th e n ic o t in ic a c e ty ı
a p
ı e rs
s i te n ľ d e p o la r iz a tio n f th e la r ll tiv a te d c a u s in g a p r o c e s s k n o w n a s d e p o la r iz a tio n S in c e it is n o t
o n e u ro m u scu j u n c t io n T h is d e p o la r iz a tio n iś c a ıt e d i
q r e e e p lo b is a c tu a y a c
by Su c d n y lc h o lin e m im id d n d b r a n e r e m a in d e p o la ń z e d
d e g iá te d in th e n e u r o m u s c u la r ju n c t io n th e d e p o la r iz e m e m
g th e
e fle c t o f a c e t lc h o lin e b u t w i th o u t b e in s
h y d r o ly s e d b
y g ba þ id lp ).
y ac e t yJ c h o li n e s
U ıis d e p o la r iz a tio n le a d s to d
e s e n s itiz a tio n ĵ Đ \ rv h è n tc n d lln t e s o n s iv e to a n y o
h i l
t e r m p u se c a u s in g m i ıs c le p a r a ly s is
a u p
a d ın in is te r e d it r o d u c e
p s a n in itia l d e o la r iz a tio
p n o f th e m u s c ı e e n d p la te r e io n la b lo c k in g a g e n t It a c ts a s a n
in m u s c le fa s c ia ıla tio n s ) fo ll g hJJşting n ia i!tťęiits a s a d e p o la r iz in g m u s c le r e ta x a n t o r n e u ro m u sc u r
o w e d b y a Ða c d d m u s c l
,
e p a r a l s is (w ith in le s s th a
ßin ö ffn ic o tin ic r e c e p to r s in th e m d p la te d d e p o la r iz a tio n It is u s e d in
f
a te r JV a d r 而 出 tr a tio
n ) d u e to d e o la ń z a ti
y
o n in d u c e d N a c h a n n l i
q l1łłtĘn a g i*【 o to r en an ca u ses

p n a c tiv a tio n r a
b lo c k ) W ith c o n tin u o tıs a d e ĥ i
a J e śd ĺ ë to in d u ce p a r a ly s is
m in is tr a tio n a t M
g h c o n c e n tr a tio n s Th is c a n e v e n h ia 1J b e
fo llo w e d b th e d e v e lo ı
y y sd y Į tßu )
p n e n t o f r e c e p to r d e s e n s itiz a ä o n (p h a s e 2 b ı k
oc )
In d ic a tio ru T o Ta d lita te e n d t
o r a c h e a l in tu b a tio n d
u r in g s u r e
o p e r a tio łu o r th g \ g e n e r a l a n a e s th e s ia S h o r t nIRECLY A C H N G A G EN T S
叩 a e ? c M a n ip u la tio n E le c t r o co n
a c tin s k e le ta l u s c le ta x t It is
D A N M B LEN E S O D IU M It is c la s s ifie d as a d ir e c t g m re an

h ib it a n tie p ile p tic actińty lik e


ľ= X ' d ıem ic a u y d a n tr o le n is h y d a n to in d e ń v a tiv e bu tdoes n o t ex
In h l b a tio n 50 e a
m g ĺ ım J) to B O m g (i 6 m 1)
, ib
y rıT g rtJo o th e r h y d a n to in d e r iv a te s p h e n y to in
:
su ch a s
ır
a e c tr o c o n w Jıiv e th e r a 40
py m g 10 8 J) to T 5
g (1 5 by
M ec h a n is m o f a c a o n It d e r e s s e s excitationontraction c o u p lin g in s k e le ta l u s c le
m m 1) m
m
C h ild rv / 1M 1 to 2 p
m g p er k g bo d y w e ig h t n o t to e x c e e d 1 5 0 j w rib ııid bin d in d e c r e a s in g in tr a c e llu la r c a lc iu m c o n cen tr a tio n
g to th e r y a n o d in e r e c e p to r 1 , a n d
n
m g

Scanned by CamScanner
雞 。
躐 蔑袋辦
ESi

ıv tr i b ıc 山
k åH a c fk ö į íėr o m d n a e v itc e ffe e n iu qo r o ı
ħc
s se l s i ti g u r d la d ic itn o z c s
ih a sA e m e ħ e ta r s
śtİ rifarijtaiti1umucca g n iw o lla y b e r e h t e s a r e n jy o p ty c t bu s c ix o to
l e m e
h g n itib iħn i y b tc a o t t g u o
ł
İ t?ñiclaf p æ
] u c a v d o f e h t n i d a r t n e c ııo c s
i ti w b k a e w a s iti e s u a c e e a
h ht s i

p r d ñ a i i V p ts n ia g a y tiv itc a la d d o ty c o te m a g s a o s a B ń a la m
h l tj h g u o h tla e d d itn o z i c s o o
a s a s tc a e n in iıtQ e e rt a n o c n c e h d lb
h i h t fo k r a b e h t m o r f d e v r e
i d d io la k la n a s i t r E N lv jIU Q

lm / 0 5 2 m u id o S e n e lo r tn a D x e o n a y
d ßm 0 0 1 p a C
)e iA h « R m u ir tn a D « m aN d n arB

)■ 動
noitartnecnoc
m u ic la c r a lu lle c a r tn i g n is a e r c e d d n a 1 r o tp e c e r e n
id o n a y ı e h t o t g n id n ib y b elcsum
hteiki g n ilp u oc n o itc a r tn o« n o ita tic x e se s s e r p e d t】_ r o itc n u j la m e n oym e h t d n o y e b e tis
°
,
ta
,
g m e h t fo esn o p se r e litc a r tn oc e h t g n itc e ffa y
b n o ita x a le r e c u d o r p o t n w o hs n e e b s a h
ti
:
?i?Æ
ę)tepyh tn g ila m
an ro f tn em ta e r t e v itc e ffe d n a cificeps y ln o ū y d m r ju c s j ti s e s U
e

lim a p a r e v h tiw s a im h ty h r s y d s e n im a ls M itn a e ta h p lıı


s m ıï is e n g a 】
n s e v it a d e s

i« sc ito c r a n s e ta r u tib r a b L o h o c la h tiw n o is s e r p e d SN C d esa E a n I sn n id m tn i g u r D

c ite h ts e a n A e c a fr u s \ I c ite h ts e a n A j】
e lb u c e n
° is J ū d ls
e n
i m n i d e te r c x e Ļe v il

t ia 9 b ĹN
j 【
ro
h d e s ilo b a te m sr u o h 8 e fil fla h n s a lp
a ı s ıu o h 5 m a ita ıtn ecm a k ab r sc ite n ik n r a m ra hP
s a is e h ts e r a p n o n e ir o s id
ita ı s ıa m erl ssen is w o rd s se n iz z id

ar iłe h ı
*en a la c o l fo n n ita c ilis s a lc ae su a n g n itim o v a ń u la ts y a e c n e to pm i yı
ivitisneohP s itir i m p h sa ın icls Ļ i o ita lip la p

g p gm t 4 y lla ıO
i th g ie w y d o b fo k 8
re o
2 o t 3 n d liıd d n a tlu d A
? E 4 ĦH
1 ro
ro f se so d d e d iv id 4
em )n o itn e v e rp f ıi m t e h t n a n g ila M
gm oo3 in iu Q gm 423 e lu s p a c n iu q a la u Q
s e n į n iu Q n a do en
am mį fİ ß
ıiß
gm oo2 p a c ta u u
e a ir a l

ıJ

Scanned by CamScanner
r l n Te x t B o o k o fp ha rm a c o ı
w a q lo g r
o fD ru g s Actiııo n P e r ip he ra ıN e rv o u s s y s t e rņ

p I1 Ņ e

三 拳芠 ,,。 。 , 。
二 。 。,。 。 m 一
. 一 Th e r e is

X X - Lo cal

lik e a ? e n a lin e p r o lo
a n aes th e tic s a re n o t a b s o r b e d fr o

n g th e ir
du
ın

ra
u n

tio
b "k

n o f
'

ac tio n

e o u s in
iu te r a tio n v a s o c o n s tr ic to r s
b c u ta n l b h ? o ly s is
su
i d in th e liv e r a n d in p a s a y y
e ta b o l s e
m

11ıe y a re m
m m 5p h m a tic d iw m o fm e ch a n is m s lo ca lan es h e it s
ı

th e tic s c a u s e c a r d io v a s c u la r s ym pt
la n a es
It is an in tıa ce llu la r h a n 8 e f ro m \
c tiv e to p o s itiv e T h is o c cu rs b eca u se N a + Fs p e c iti
c jliJ ii L p r z
a

c h a n n e ls a r e o e d (o r a c tiv a te d ) A llo w in g N a ◆ to e n te f th e c e ll A N a + en te r iś :th e c e ll


pen s

d d itio l N ha ıltin o s itiv e fe e d b a c k lo o p P ö tä s s iu


a n a a + c n n e ls a re pen o ed r es ı p g in a m
sp ed lic c h a n n e ls a r e 0 a llo w in g K + to m o v e o u t o f th e c e ll a n d in to th e

: X
ex tr a ce llu la r

s io n s tr e m o r s
W b ra n te m m e s r e v e rs e d to a p p r o x im a te ly 35 illiy p lts i'" " " " " "u''"s' co n w
p o łe n tia l ı
sp a m n en + .
m em e m th e ''" e e xc

m o v em en t o f N a + i n th e o e il a n d K + o u t o f th e c e ll s to p s (N a + c han n e ls b e c o df 1 】a n ae s th e tic s
m e
W a
C t i v a t e d ) a n d th e N tia l b a c k to ffe c t
y th m ic
(N a + c h a n n e ķ a r e a t a
a+

r e s tin
/K + p u m p r e s to r e s th e m em bra n e p o n a '
Ęg s ta te
Sjólīfwäy a re in d ic a te d fo r s y s te m ic u e fo r an t ir r h e

to b u u lc e r s Ĥ is lu r e s
c in g p a in d u
g s la te m s
th e s ia fo r re du e
) a re u s e d a s s u r fa c e a n a e s
l to p r e v e n t a c tio n p o te ĘÆls fr o m y
Lo l d in g s by
ca a n e s th e tic s a rk t th e 】
e lr e l f d ıe N a+ chan n e al th e tis e n erv e en
w a o rr o
e s th e s ia a s lo ca l i
ar a es th e tic to an a es
b e in g p o te n tia te d a n d t by lte r in g r e s tin g o r th r e s h o ld p o te n tia l Its m o le éu ı ULAş in iilte r a tio n an a
o
ıı a e s a re g l fi
m in is tr in g a s su b c u ta n e o u s in je c tio n
s tm o s p e c ißc a n d b in d w id ıi
n tı
ıe N a + c ha n n e l or its 叩 e n in g L o c a 1 ıäń e s th e tic
n ear J ils 山zJ R ¢ ific
d to th e s p ec n erv e
le le s h a v ffin ity fo r r e c e p to r s d u ń ı吕出 e ir o p e n o r in a c tiv e s ta te W ıie n lo c a l į )ıЫ ä u s e s n erv e b lo c k an a e s th e s ia w h e n it is in je c te d o se
m o cu e a grea a ïm o
b a ra chn o id sp a ce
an es th e tic m o le a ıle s b ni d w ith ū e N a + c h a n n e l it p r e v en ts a con fo rm a äo n a l chnge d
a rı b í rĥ ◆g
m u se d fo r s p in a lan a e s th e s ia w h e n in je c te d in to su

th e in Ħu f N d d e p o la r iz a tio n s lo w s
x o a + An E v e n tu a lly th e m in im u m b lo c k in g gniĵ ofd r r
tio n o f d ıe lo d lo la th e s ia
co n c en ? ca l a n e s th e tic p r e v e n ts a n a c tia m p o te n tia l fr o m b e in g a c h ie v e d a n d bn G b s v s ïr :
c o n łp a r a t ių e fe a h ir e s o f gme*l a n nes th e tic s a n ca n a es


ec b it a l c o n d u d itm is b lo c lce d

s ite l= ß e n e ra la n a e s th e d cs I Lo ca l an

P e r ip heraln erv es
Pha zın a t» lo # c ıï a d io n o fLA s ite o f a c tio n
CN S
CN S l y ıte m ıo c a 】a n a e s d Produce s tim u 】 w n o le bo dy
a tio n o f c e n tr a l n e r v o u s s s te m
y T h is c a u s e 92u 63 eb p A rea o f b o d y in v o lv e
c tb e u se d
p h o f ia r e s tle s s n e s s a n d tr e m o r s C o c a in e c a ııs e a d d ic tio n w h ic h is d u e to į ts e u h o r ic
eu P r e ffe r e d an n o
p J iT o ńqu s zątajors u r g e r y
e ffe a n e fe r r e d
M in N o t p r e fe r r e d
o r su rger y
C a r d id v a l c u la L o c a l a ııa e s th e t ic s S a fe
r
em W Ħ o d u c e v a s o d ila ta tio n a n d h y p o te n s io n js ei n o an i }c p o or h e a lth p a tie n ts R is k y
o c c u ır e tL i n e Ħ o d u c e s v a s o c o n s tr ic tio n d u e to w h ic h h yp e r te n s iv e e ffe c o c c u r s A U IIA N o e ffe c t
Ļ alu ĵ Po ċ o n s c io u s n e s s
m t
lo c a l a n a e s th e tic s
p r o d u c e a d e p 'r e s s e n t e ffe c t o n th e m y o c a r d iu m N tp o ss ib ı
e
P o s s ib le o
N o n co o p e r a tiv e
T ÐIÌ A '
ST
atlentś u s e
X '" d' ' " em "
' '" ' '" g a n . n

Scanned by CamScanner
P R O C A IN E It is a n a n a lo o f c o c a in


e It is

ī¥
g
o n se ta n d a s h o r t d u r a tio n o f a c tio n ï t i
s an m
o r r e g io tıa l a n e s th e s ia
p a r t ia ıla r ly fo r
a d v a n ta e o f c o n s tr ic tin
g g b lo o d v e s s e ls
a n e s th e tic s

M e cha n is m o f a c tio m It a c ts m a in ly b y in h ib itin g s o d iu m in flu x th r o u g h v o lta E ¥


so d iıım c h a n n e ls in th e n e u ro n a l c e ll m e m b r a n e o f p e r ip h e r a l n e r v e s T ħe jn H u x
is in te r r u te d - A c tio n
p p o te n tia l c a n n o t a r is e an d s im a lco n d u c d o n is th u s in h ib
ş+d ,
r e ce
p to r s ite is th o u g h t Io b e lo c a te d t th e c y to p la s m ic (in ) p o r tio n f th e
a n er o
ģdiarı
cham e i P r o c a in e h a s a ls o b h een s o w n to b in d or an ta g o n iz e th e fu n c tio n o f N ın ėth
y ıU
a s p a r la te m Æ A ) r e ce p to rs a s vell a s n ic o tin ic a c e ly ı
c h o lin e r e c e p to r s a n d th e ś ġ ŕ o tö ń i
n
re c e p to p jo n c ha n n e l c o m p le x ıiıJ J u lj J

P h a i m a c o k in a ti{ = J t is a n e s te r a n e s th e tic I t is m e b o l i z e d in th e la s m a b th e
p y en z m
y e
p se u d o c h o ı in e s te r a s e th r o u g h h d r o l s is in to
y y p a r a a m in o b e m o ic a c id (P A B A ) ŕ hiċ his
th e n e x c r e te d b th e k itln e s in r th
y y o e u r in e

S id e ffe c ts It co n s ı t ttin f th e s k in j th th e lu tio f p


iił
niEoı
ATEP O T E N C Y A N D
e c au ses a n w e g o w so n o r o c a in
" ON
D UR A Tı
h y d ro c h lo ń d e d e r m a titis d r y 】e s s a n d c ra c 】
d in f th e s lc in t u se d a s a n
g o
d d ia d e p r e s sa n



c

\ 姦
th e tic a ca r


' c A IN E ) It is a lo ca l a n es n
U s e s I t is in ly d fo in m b n a n e s th e s ia
m a u se r a tio p e r ip h e r a l n erv e b lo c k an d s p in a l b lo c k Rt
is u se d as a lo ca l anestheticprimaryh o l s u tg a y Iy r h T ıï il rr n
一 一 ・
p i.
ra 。 ,
。 。。 。 。 。 。 u c
°, , 。 。
B ra n d N a m e ' O C a i n 2o m g / m 】N o v o c ıin u q 2% íIı
iJOTq irJ b y in h ib itin g th e io n ic n u x e s
b iliz e s th e n e u ra n a l m em bra n e
ha n is m o f ac tio n It is s ta
th e tic
M ec lo c a l an es
d du tio n o f impulsis th e r e b y e ffe c tin g
d fo th e in itia tio n a n co n c
bĐTiuljr q u ir e lta g e g a te d s o d iııın
r
re
P reca u tio n s a n d in te ıa c t in m
l d tio in n e u ro n s b y b lo c k in g th e fa s t v o
It lte r s s ig n a co n u c n
J
ı iJ J n tio n a a ū o n
n o ac f s ig n a l p r o p a g
th a t a r e r e s p o n s ib le o
r
h l ll m em b ra n e
(N a + ) c h a n n e ls in t e n
e tır o n a ce
ill n o t d e p o la r iz e a n
d
2 In j t th e L A sı dy a n d tale k th e m e m b r a n e f th e p o s ts y n
o a p tic n e u ro n w
į th s u ffic ie n t b lo c a g
ec o ïı e
c a re n o t Io ex ceed th e m a x im u m s a fe do w
se e s p e c ia lly iin ,,
c h i 】 fa il to tr a n sm it a n ac tio n p o te n tia l
z H l iıİ ıi/ w ill th u s
l a e s th e s ia in se c t b ite s,
l s p in a l s u r g ic a a n
3 /w w w o lo l (p m b a b ly o th e r p b ıo c lce is a ls o ) a y re d u ce m
ııı e ta b o lis m f hdo F In d jæ E o n s p e r ip h e ra l n erv e b lo c k e p id u ra
o c a in e a n d
o th e r id e L A by n ed u titis
d 吕あe p a tic b 上ıロイ 月o p y p a in fu l c y s
am s n w ı户ゴ了o n irr n
ı in or bu m s c y s to s c o
f ld e r ly hep a tic
4 W so co n s in ic to r (a d r e n a lin e ) itiv ty ch ild b e lo w 12 ye a rs o a ge e
c o n ta in in
g LA sho u ld be a v o id e d fo rp a tie n ts n iith r!nnt?niņdjcatione H yp e rs e n s
is c h a ic ħe a r t d ise a s e
匿 em

d th o s e
c a rd ia c a ï r h
Ħh m ia th y r o to x ic o s is u n c o n tr o u e d h y p e r tè n s io n in ip a ir ın en t p re gn a n cy
f eyes
an r e c e iv in
g b J o c l s (Tis e in B p d u e to u n o f th e p p ils
回 an tid t p e ss a n ts (u p ta lce b lo c k a d e o f A d
p p o s e d D ū a c tio n ) or tr ic y cı
jc Ĵ i§
idTėffects V o m itin g n au sea b lu rre d v is io n tin n itu s , c o n s tr ic tio n o u

c a r d ia c
o

a lr e s t
r) ede b ssu n e c r o s is
げ U ır is a in ly
ıyń q c n nf an a p h y la x is s ta tu s a s th a m tic u s u r tic a r ia ra s h m a e

s in e s s lo
æ m u se d fo r in H » a tio n a n e s th e s ia
p e r ip h e r a J n b lo c k h yp ö te ħs io fe ta l b r a d y c a r d ia m y °c a r d ia l d e p r e s s io n tr e m o rs s h iv e r in & dro w ss
e rv e an d s p in a J b lo M r4 y r ! n

Ŕ iŔ a n o J Ì {J o fco n s c io u s n
i ta tio
e s s c o n v u ls io n s d is o r e n
n

C H L O R O P R O C A IN E It i
s a n a n e s th e tic a du tio f a c tio n 3 to 6 h o m s p ı a s m a h a lf
o n s e t a c tio n 4 to 17 m in u te s ra n o
a n e s th e s ia
p a r tic u ı
a r fy fo r o īa 】s
g m t in d ic a te d fo r
p r o d u c tio n o f lo c a l o r r e R io n a ı [biymqţ pkinects 90 in u te s h a lf life is in c r e a s e d in
u r g a y It (lik e c o c a i
n e ) h a s th e a d v a t
n a g e o f c ö如因o tA n]jĮ iyAy I je c tio n is a bo u t 13 m in u te s b y 1 M in je c tio n m

:E Z
n
M c h r e d u c es b Je e d i g
n & u n lik e o th e r ı
o c a J a n e s th e tĵ c s lik e d o c a ir iý ıt7 j§h i n]iv£
'j¢
ase It is m e ta b o lis e d b y liv er c ro sse s p la c e n ta e x cre te d in u r in e

Scanned by CamScanner
U I t is u s ed a s a lo 】a n d
tianhwa
s eı th e tic I t js
ca es an d c a r d ia c d e p re ssa n t u se as an a n

a gen t
B la d 2 % tj d o c a in e H d m c h 】 o r id e In je c tio n U S F A g o n E a z e A m n io c e n te ș i
n n am e
y şl T r a
l% y
A
g ra m r th r o
T r a y 1 % li u id 1 % A te io c o i】 Im p la n t 3 % jn tr a d rm a ı Fn je c t i
:ĵ:"į "
q a ge n
o n
G e s ic a in e (L ig n o c a in e h d r o c h lo r id e ) 3 o m l v ia 】 G e s ic a in e w ith a d r e n a lin e 2 %
y 3 om l
ı
D U R A T IO N
"
X y lo c a in e x y lo c a in e w ith a d r e n a lin e x ï lo c a in e h e a v 5 % fc o n ta in s ı
) y ig o c a in e h y d r o c h Jo r id T EN C Y , LO N G . .
Ta tio n a t

Xı X y
e
5 3 5 m g + D e x tr o s e 75 m
& u s e d fo r s p in a l a ııa e s th e s ia fo r s u r g e ıy ) IN . p ń lo ca in e h ' ' " m '
\ ¢
: fo r

' s JŁ
a s đi
P R IL O C A IN E It is lo la n a c o lo
a ca e s th e tic th a t is s im ila r p h a rm g ]c a lly to lid o c a in e ijß r s Jı
jĵ n i
M « h a n is m o f a c tio æ lu la r s ıııfa æ o f s o d iu m c h a n n e ls w h id ir u e d
It b in d s m th e in m c e ı
çs
th e bsequ
su en t in Ðu x o f s o d iu m in to th e c e ll A c tio n p o te n tia l p r o p a g a tio n ñı ħepér
fu n c tio n is th e r e fo h l t ħis b ? is r e v e r s ible a n d w h e n th e d r u g d ilń iś a ś ų w a
w w w ı re
y
fr o m th e ll d ħm
c h a n n e l ń ın c tio n js r e s to r e d a n d n e r v e
ce so
p r o p a g a tio n r e h ıiĺ ń g z m e
a n tia r r h y th m ic a c t io n s u e m e d ia te d th r o u h e ffe c ts o n
g s o d u m c h a n n e ls in P u r k in je rfib tį r s t

U s « It is u s e d a s a lo c a l a iu e s th e tic a n d is o ñ e n u s e d ĵ n J !t b o ï h
dentistry yl l
B ra n d n am e 4 % c ila n e st Ħ a in D en ta i 4 o ' & D en ı
sp Jy 4 % p r ilo c a jn e H yd'' " ı
O'dg=Èal Fu=Ue=*
In je c t io n L iv ix ū P a k

了E T R A C A JN E T ħis is w h i in a n a e ın ic
a a y s ta iı
in e o do u r Te s s po w d e r Ft is v e ıy lu b ı
e in ia a v o id its t ıs e
g lo b in
so w te so
c a u s e ın e th a e m
a r o e m
T e tr a c a in f p r ilo c a in e a y
e h y d r o c h lo ıid e does n o t p ro d u ce th e v as o co n s n ic to
i r a c tio n o f iio d áh e Fn [ p s n w d o se o m

CO n c e n t r a t i o n s f 05 【
o 2 % te b a c a in e js p ą tie n ts
o
p o w e r ń ııth a n c o c a in e
m ore or p r o c a in e Iq tq s b o th rflo d ë
su ń ace an d d tio n b lo c k a n a e s th e tic H is a ls o c a lle d a m e th o c a i
th e s ia in d ig its it ın a y
o on u c
n e cm Jï
tbe d fo in d u c in g an aes
d r e ria lin ld r
ith e sho u n o u se
p r ilo c a in e w a

a hh nn c w c FB N {c H a ・ ľ le a d to g a n g r e n e be ca u se o f p r o fo u n d is c h a e ın ia

fr ıo a c a in e ħW B Ń U U ) b lo c k fo r re lie f o f
It be u se d fo r n e rv e
Its u se is r e s tr ic te d to tc p ic a l a R o p IV Ą c A IN E It is an lo c a l a n a e s th e tic d r u g ca n
Fp ı
ic a tio m to th e tr a c h e o b r o n c h ia l tr e e a c a in e It is e qu a lly lo n g
:& &
ey e N o se f b u p iv

P ×
an d th r o a t ıt ' '
ge n er o
. Tiv e m d la b o u r p a in It is a n e w e r co .

... . Eþjd e ı】ıa l a n d e r i h e r l a c tin an d is m ild c a r d io to x ic d r u g


p p bı
ock
ı rß g n Đĵ ß g
n a e s th e s ia
a n er v e S P in a la n aes th e s ia l b lo c k p in la
l b lo c k g in a s a
D ıV In d ic a tio b lo c k cen tr a l n e u ra v a
o a lg e
O n s p ra y Ttp ic aJ a p p lic a tio n d o s e
n p e r ip h e r a l n e rv e
v a r ie s w ith te m ila b le in je c tio n 2m g 5 7 5m g
ș th e s ia
ro u
Co tr a in d ic a tio n
an ae
į
'
te o f an aes th e s į ı It is av a a s
n a
tivíly, h e a r t d is e a s e ıiv er d is e a s e in p r e g n
V a r ie s a c c o r d in g to ro u
a n cy
i【
ąĮţ?・

Scanned by CamScanner
国 国国 ı8 4 \ 弓
rm lı
aTe x t B o o k o fpha rm a ' " D A t P he lN §t e m
y . C0 l ru g s c o n e r ıp ra e rv o u s

I P ll a r
C o n tıa in d ic a tio s
łı
itiv ity Iiv '
, d is e a s e c h ild r e n b e lo \
P a tie n ts / p e rs o n s W ith p rec a u tio n s u s e in
a lıe r gy p regn a n cy A n d in p a tie n ts

S id e e f fe c ts V o ı
n itin & n a u s e a
is io
an a p h yla x is R e s p ir a to r
y a rre s t s ta tu s a s
V n tin n itu s C O n s tr ic tio n d r o
w s in e s s tr e m o rs s h iv e r in c o n v lıls io n s T h is re v e rs ib ly
dem g l in h ib itio
e a s k in d is c o lo ra tio n a t in e c ti
j o n s ite Tis s u e n e c r o s is c a r d ia c a r r e s t
F
'nĖ s n e rm eab i】
ity to so d iu m io n s th r o u gh so d iu m c han n e n

.X=X
h y p r te n s io n e ta ilu r e
g in th
c a r d ia c a m in h jb '" ' " . '" z a . . re su m n
o [ " o
s Ļ m y o c a r d ia l d e p r e s s io n b r a d y c a r d ia
Phu b se qu du
m a co 】
dn e tic s o tia l a n d su en t co n c tio n b lo c k a d e
p °te
n se t a c tio n 2 to 8 n
acdo
in n
m u te du ra tio n o f a c tio n 3 to 6 h o u r m e ta b o liz
D ru 吕 in te r a c tio n s H ) p e m e n s io n is
ed
Sü[Ł
iĖA N A E S T H E T IC
ca u se d b y d r u g s lik e tr ic c lic i
P hen th ia z in e s y a n tid e p r e s s a n ts M A o ľ fir s t r e c o g n iz e d L A e r tie s d to x ic ity e
a s th e
o I ts a d d ic tiv e p an
c h】 E
c o c A JN It p
w ro
o ro
p r o c a in e d e c r e a s e a c tio n o f r o p iv a c a in e
s
d
c N s d d ia e x c it a ū o n an
n d p h y s ic a l d e p e n d e ' " . m o o d a lte r a tio n an car c

p śýc
iliigic
ł ,

a so co n s tr ic tio n p r e c lu d e its c lin ic a l u s e in d e n tis tr y


h te n s e v
w a te r B u p iv b y
a c a in e is to c a i f ac tio n It p r o d u c e s a n e s th e s ia b y in h ib itin g ita tio n o f n e r v e e n d in g s o r
n a e hħa h is
a m o e x c
a iu e s th e tic h a v e s ii
n ila r tio n
ac to lim o c a in e bu t d
dą#qn is
b 1ö ćliİ ń g o n
JĒ du c tio n in p e ń p h e r a l n e r v e s T h is is a c h ie v d b y r e v e r s ib ly b in d in g t o a n
e

n iıßv ilĵ d iu m c h a n n e ls S o d iu in flu x th r o u g h th e s e c h a n n e s l is n e c e s s a r y f o r th e


ßrï i in ac tiv a tin g so m
it is ed l th e
a n d s u b s e q u e n t p r o p a g a tio n o f im p u ls e s a o n g
m as a s o lu tio n f ll m b ra n
co n a in in
ı
g o 5 % b u p iv a c a in h y d r o c h lo r id e d e p °la r iz a tio n o n e rv e c e em e s
2 00 0 oo o r o 25%
e
w ith d re ńa ı
ith in It is th e ly lo la n e s th e tic w ith v a s o c o n s tr ic tiv e p r o p e r tie s

enateredı
ocauy.naesthesaastfor7
dren a nn a
w a e m o oo e j b c 【iu i s c ib
f th e n erv e o n ca

io
X= . ' " s s e 1. It in s tille d in to th e e
y e it b la n c h e s th e c o n ju n c t iv a a n d d ila te s th e p u p
il
s e
YJSTci s o lu tio n f 5% to 10 % d fo
r a n a e s th e s in g th e n o se qn d th r o a t S o lu tio n o f

岱 /̃
Sp r a y o u se
t ßT in s ĵ rıo
! "
J co n ce n tr a tio n s u p to 2 0 % m a y be u s e d fo r th e la r n x It is u s e d a s c o c a in e h
y y d r o c h lo r id e

n ßb ř Jf It is d a n g e r o u s fo r a d m in is tr a tio s p in a l a n a e s th e s ia T h e r e f
n s a s a
p e a te d u s e o c o ca in e m a y
W T b oĵ Ī ĥ r le a d to d 】u g d e p e n d e n c e It c a u se d ila ta tio n o f th e p u p il r is e in b o d is e in
y te m p e ra tu r e r
_ a cn m ft b in d s to th a b lo o d su g a r le v e l a n d r a is e s b lo o d p re ssu re
e inacelluı
ar p o r tio n

H
o f so d iıım fı l (to p ic a l) a n
pīoËrigī
th

Ï
' re v e n ts d e p o la r iz a ti
a es e s ia o f a c c e s s ib le m u co u s m e m b ran e s o f th e o r a l
o n In g e . A l th e

(3) to u c ħ ' " yn cr ''. H e a d a c h e fa in tn lo in g f co r ne a l


) P e ss o sen o
p ith e liu d co r n e a l
W o c e p tio n
an d (5 ) s k e le ta l m u sc e i
e m an

to n e T ħe a n a lg e s ic ffe c ts
r ece
p to r s su b tJ
p e E P I (P G E 2E Ħ )
e o f #iĮ ņiņg In te c o c a in e
w hiA in h ib its th
a cu
p o is o n in g c o n v u ls io n s m a y b e tr e a te d w ith d ia z e p am
e p r o d u c ti
on o f p r o s ta la d e p r e s s io n w ith th e ar tific ia l r e s p ir a tio n
In đ« tio n g n d in s
Jereby
a n a e s th e s i
s p in a
Urlt i '
a lo c a l a n e s th e tic in d ic a te d fo th
a l a ıı
a e s th r e in tr o d u c tio n f lo l (to p ic a l)
e s ja o ca an es th e s ia o f

Ĺ,,-
a c c e s s ib le m u co u s m em b ra n es o f th e l la r y n g e a l a n d
o ra n a sal c a v itie s

B ra n d
X °' ' " H '' " cM ' "" T o p S' ' " . 9 /m 1 C o c a in e H yd ro cł
ū o r id e T o p ic a 1 S o l
n am es
B u p iv a c a in e īu o d ßt >
In je c ljo n B
u p jv an M a r c a in
se n s o r c a in
e A n aw in 5 m
gp er m l
Ir rt t a
qr ;

Scanned by CamScanner
2 1 In H lt m u o n « t h n i ı D

【n
ilu te s o lu tio n s o f lo c a l a n a e s th e tic js infiltrated (£
in th e a re a o f s u ıg ic a l o p e r a tio n It b lo c k s e n s o r n e r v e e n d in g s L id o c a in e 3
y ,
b u p iv a c a in e 12 0 180 m in u te s h a v e d u r a tio n o f n e r v e b lo c k
rr ir
3)C o n d u cd o n b lo c k
i
T h e lo c a l u ıa e s th e tic is in je c te d a r o u n d n e r v e s o th a t th e a re a d is ta l
to
in je c tio n is a iı
a es th e tis e d d
aiı p ly s e d L id o c a in e 1 2 %
a ra w ith in te r m e d ia te d t [
a c tio n is ly be
co n u n o n u se ¢ fo r ı
o n g la s tin g u ıa e s lh e s ia b u p iv a c a in e m ay u se d

4 ) s p in a l l h ¢S i a
T h e lo l a rıa e s th e tic js n je c te d in th e s u b a r a c h n o id s p a c
L2 4 L 3 - 4 lu
ca
ę beeen
o r m bar v e r te b r a Ĺ e B e lo w th e lo w e r e n d o f s p in a l c o rd It c a u s e a n a e s th
e s ia to

ıo r s u r g e ı
y o f lo w lim b s
p e lv is Io w e r a b d o m e n ı
er ia c tu r e s e ttĵ n g o b s te tr ic ł;
tmen
ca e sa rea n o p e r a tio n 1 1ıe 山 m
l lio n o f s p in a l a n a e s th e s ia d e e n d s o n th e d r u
p g u s ș a n d its
co n ce n h a tio n W om ,
e n d u r in g la te
p r e g n a n c y n e e d le s s d o s e fo r s p in a l a n a e s th e s ia It i
s
b e c a u s e in « n io r v e n a c e p a c o
w h ic h th e r e is d e c re a s e h
呷 r e s s io n I E s u LB e n g o r g e m e n t o f v e r te b r a l e to colu\du
? e c a p a c iy o f s u b a r a c h n o id s a c e T h e s i l
p p n a anaestĥ sia h a s
fo lo w in g a d v a n ta e s o v e r
g g e n a a l a n a e s t h e s (1) It is s a fe (2 ) It p r o d u c e s a n a l e s í
m u s c l e elaxaıus w ith o u t lo s s o f c o n i g a a n d
sc o u m e ss (3 ) D ia b e te s c a r d ia c r e n a l D is e a
se
Pu 】 n ıo n a ıy d is e a s e d o n o t h t a æ
m u c h a n d p o s e s le s s
C o m p lj« tio m o f ı in a l a n
p a e s th ¢ıia
p r o b le m in tr e a tm m t
7 ħe c o m p lic a tio n s o f s
1
J I ıu

b d
:
S A are lIjl n g r ı w h e n th e p a tie n t is to b g iv th e s ia T h e fo 11o in g p o in ts m u s tb e re m e m e re
(l1) H er a d a c h e u/+ e en an a es w
d u e to s e e a e o f c e r e b r o
p g s p in a l flu id u s e s m a ll b lo g y p h y s ic l c o n th fe r e n iv k id y
o r e ń ē e d le to o J 4 b s l ar e ) ľ sych o i io n w r ce o re p ir to r y s y s te m e r n e

(2 ) V O m IW d zib d is e a s e a n d o f c a r d io v a s c u Ja r s y s te m C N S s y s te m fu n c tio n s d is e ase if an y b e ch e c ke d


an lıa lls e a

b į o Ė o ? ie p a tie n t s u ffe r in g fr o m d is e a s e lik e H y p e r te n s io n D ia b e te s m e llit u s D ia b e te s W


Tht :iz n i in s ip id u s a n d th e tr e a tm ė n t ta k e n b y th e in ? v id u a l b e re co r ded b e fo re a n a es th e s ia is

(5 ) g r IT Th
c a u da e q u jıı 9 e a n x ie ty s ta te o f in d iv id u alb y n o te d an d o b se rv e d T h e r e is d iffic u lty o f an e s th e s ia
a s jm ? om
@ ' " ' '" " y
' : X
s ta te m o re do se i' ' " d . ° T h e r e i' ' " . '" h'' " h '' " a n a e h . "
. _ on in tr D d u c e d / e n t
e r e d d u r in
g l. . . " ' "

a n a e s th e tic d r u g TH e

an d a c ts a s a n tie m e tic

Scanned by CamScanner
二 に 二二
° 。 " ' " v Is
ty lc h o lin e
。 。。 。

8 In c r e a s e th e p a tie n t is o n t ic o s te r o id g iv e th e p a
co r tr e a tm e n t
H y d r o c o r t is o n e 1 0 0 m g to a v o id s e s s o f a n a e s th e s ia an d a ls o a v o id
c o lla
p se

i5
K ,m o v al °
' " m ' ' " lh y n t e c to m y ) T h is ' ' " p tio n i' '" e ca æ . . M ym ec to m y

回回 D R U G U S IN M Y A S T H E N IA
G R A "
q r rr i n
can
im p r o v e sym p to m s fo r so m e p eo p le w ith m y a s th e n ia g r a v is
d in th e
s te id d ic a t io h d is lo t a b le ts is o fte n u se
M y a s th e n ia gra\s is d itio e d ic a tio n ro m e n su c a s p re n o n e
a co n n w h ėr e m u s c le s beco m e e a s ily t ir e d d
k I t i¢ a n w
i,g ņ ę to a
e a
P r o b le ınw i th h o w th e n e r v e s s tim u la te th e m u s c le s to ti
g h te n fc o n tr a c t) T h e
a r o u n d th e e e s , Ħy § ic le s
y a r e c o n ım o n l a ffe c te d fir s t T ħi
y s ca u s es dro o i H ig h e r d o s e s m a y
p n g o f th e e y e ı
v is io n T r e a tm e n t is u s u a ll e ffe c tiv e E h
y a c m u s c le is s u
pp ı ie d b y a n e r v e w h ic h
id a
g 4 , ? tţ Þ 1e t Įik ģh tTb r p e o p le
w h e re s y m p to m s o n ıy a ffe c t m u s c le s aro u n d th e e ye
a ffe c te d
It m a y
s m a u e r n e r v e s th a t
s p r e a d a lo n
g th e m u s c le İ ib r e s T h e r e is a t in y g a p b e tw e e
,t o
p?i to p re v en t sym p to m s if m u s c le s o th e r th a n a ro u n d th e e y e s ar e

gë1 m o n th s b r in g s y m p to m s u n d e r c o n tr o l w ith
to s te r o id s o n ce proved th e

to m s
' ó ly r e d u c e d g r a d u a lly to fin d th e lo w e s t d o s e n e e d e d to p r e v e n t s y m p
d o s e ig ĉ m
m o n
h a n d le d
a y b e q u it e M g
a
l th e d o s e o f s te r o id n e e d e tt to c o n tr o l th e d is e a se m
】n so m e peo p e
to s id r e ffe c ts

su ch th ia p r in e
d ic in e s A n im m u n o s u p p r e s s a n t m e d ic in e a s a z o
Im m u n o su p p re s s a n t m e
be a d v is e d in a
d d itio n t o s te r o id m e d ic a tio n T h e s e m e d ic in e s w o rk by su pp r e s s in g th e
m ay

加国隽 u n e s y s te m

r k b e tte r
COmbjrions o f m e d ic in ės A s te r o id p lu s a n in u n u n o su p p r e s s a n t te n d s t o w o
e ith e r a lo n e A ls o th e do se o f s te r o id n e e d e d is o fte n le s s if a n im m u n o s u p p r e s s a n t is
th a n

ad de d w h ic h re du ce s th e r is k o f s id m ffe c ts w ith s te r o id s

d ru gs in te r fe r e ith la tr a is s io a n d e x a ce rb a te th e
O th e r So m e ca n w n eu ro m u sc u r n sm n

s ym p to m s o f m y a s th e n ia g r a v is Tho se m o s t o fte n im p lic a te d in c lu d e a m in o g ly c o s id e


d p e n ic illa m in e T h e r e is
an ū b io tic P a d re n o ce p to r a n ta go n is ts p h e n y to in c h lo r o q u in e a n

a ls o lte r e d s e n s itiv ity to scu ıa r ju n c tio n b lo c k e r s ith in c r e a s e d r e s p o n se to


a n e t ır o m u w

la r b lo c k e r s b r e s is ta n c e to
H = 3 I tL M y a s th e n ia r a T is
g İ jİ ı
gq【
no co m pe titiv e (n o n d e p o la ń s in g ) n e u r o ın m cu ju n c tio n u t

厗 n erv e en d in g s r e le a s e a c h e n ıfc a
leFt\ g neuromusar ju n c tio n b lo c k e r s

lca ı
Je d a n e t ır o tr a n sm ittre r in to th e u s c ııla r j tio n ilm i1 1 N
n e u ro m
T ħis u n c n o u
n e u r o tr a n s m

th e
itte r is ca lle d ace ty lc h o lin e Th e a ce ty lc h o lin e q u ic k ly a tta c h e s to re ce p to r s 2 10 l119 ] 9 7 0
B 1 1 D R U G U S E D IN G L A U C O
on m u s c le s TM s in h u n H g g e r s th e u s c le flu id
m to tig h te n T he re a re m a n y a c é ty lċ H b ]ı
-ė ◆醐 W ą is a d is e a se th a t d a m a g e s th e e ye s o p tic n e r v e It ually happen s w h en
r ec e
p to r s o n e a c h m u s c le lib r e M y a s th e n ia G r a v is is th e p r e s s m in th e e y e
a bo u t ı in ı0 0 0 o p o u la to î n Jt is d u
an a u to im 】n u n e d is o rd e đrá f¢ U iiñ ģ §ippLin th e Fr o n t p a r t o f th e e ye That e x tr a ū u id in c re a se s e
p e to d e v e lo p m t o f a n tib o d je s d ir e c te d
e n töimtińic B ;th e o pūc n erv e

Scanned by CamScanner

ノ : 。

ふ实耄葵叁多燕 苛 ぷ

y ? ia s ls o y
tic (s u c h as p h e n y le p h r in e ) w h ic h a ls o p ro d u c e m
th o m im e

e 132 1
29
R e fe r P a g
d in ir ıi
n le d
a ċ ¢rn
a
tIt is te a n a lo f a tr o p in e th a t is u s e an
m br o m i d e .
a qu a m ar y g o
Ēu
fe r P ge 131
dĥśģėŁ f th m R
d e a
m o r p re v en tin g b ro n ch o sp a sm a s s o c ia te d w ith c o R D an a s a

u ĥ i
e f ßrrĺ o J

Ļ LA T E
A qu a te m a ry a n a lo g o f A tr o p in e u se d m o st coonly a s a p re

GL XçR EY R R o b in ū ith
re du ce sa liv a ry & r e s p ir a to ry se cre tio n s an d in co m a o n w

"
k ġĥ . ' ' " v e , th eı e ffe c ts o f n o n d e p o la r iz in g s k e le ta l m u s c le Re la x an ts (e g
:(
ÈX v a 9 a iı T
_ ) a t th , en d o f ." g e r y R e fe r p a g e 1 3 4
ť

N u m e ro u s p r e s c r ip ū o n & o v e r th e co m te r m e d ic a tio n s h a v e
M Is c E L L A N E O U S
D R U G S U SED
JN T H E T R E A T ilo ıb iJn
Ħt E N T S O F G ly
tic h o lin e r g ic p r o p e r tie s o r s id e e ffe c ts W ile th im p fa s in g le d Ju g y b la tiv
J rŔ
LA U C O M A ĥ an n e act o m a e re e
A T R o P IN E
A tr o p jn e is a sm a J1 th e c u m u la tiv e e ffe c t o fm u ltip le d r u g s ta k e n con com ita n tly (e g Fo r d iffe r e n t c lin ic a l
n a tu r a lJ
y o c c u ıt in g z e tla d o n
ıio m na aı Ł n lo id th a t
pı a n ts s u c h
a s dea dl can b e J ie x iŕ äc tė d b iń d ida ū o n )c a n b e ific a n t ld e r ly p a tie n ts
y n íg h ts h a d e (A tr o a b tı s s ig n e s p e c ia lly in e
p e a do n n a ) i
coı n p e titiv e J m so n w eed & d r a k e It is
a n ta o n is t m an
g o f a Jı liv e a Ji e İ JI 9 l l/ !
kn o w n
a d m in is t
e re d s
ystemicatıjt a n ta g o n iz e s th e n g r【
vï hn ĥ
re st a n d d
ig e s t e fk t
c s
p ro du ce d b y th e

m u s hr o o m
s c o n tain in
g m u s c a r in e R ek r p a g e 12 5 Yd B n in ü a io
I

IL 。 国画區 国屬
Scanned by CamScanner
h .
r 1
D r u A t in g 207 国
ı国国
l '
c o n C e n tr a l N e r v o u s s m e m 1
C H A P T E R 4 "
a
ų
p rq

á P H A R M A C O LO G Y O F D R U G S
A
O N C EN T RA L N ERV O U S
S Y S Į
iN T R O D U C iN G T H E C H
A PTER

N eu m hu m n ra lı is tio
ıa n sm n in th e C N S ?
m A n e u r o H u
G lu la m a b p n e u ıo b an m itte r
«ıy d n e n eı
u o lr a n s m iı
t r
DOp m in e n e irıo b am iH e r
m

S e m lo n in n e tu o ı
ıa n s m itlp r
G e n e ıa ıa n es th e ó c d
aan e i
S ed a tiv e s h yp n o tic s

C bn b a l m t łs d e a x a n t
A n ti e p ile p tic s

K EY T ER M S
h ic a l tio n s a r e c a lle d n e u r o tr a n s m itte r s n e u ro m o d u la to rs
itte r s I t is c em se cre
N e 1ır o tr a n s m
d ia to r s a n d n e u ro tr o p ic fa c t o r s re sp e c tiv e ly It is syn th e s iz e d in p res yn a p tic
# n e u ro m e
Ganunaminobutpzic a d tL It is th e c h ie f in le a d in to p tic c le ft to p id ly s tim u la te o r in h ib it p o s ts y n a p tic
h ib ito ıy n e u ro tr a n s m itte r in th e m am m a lia n c e n tr a l IrJæ
lļ cqnslnd a re re se sy n a ra

r e tic t ıla r fo r m a tio n )


n erv o u s
lin e d o p a m in e n o
ty lc h r e p in e p h r in e (e p in e p h r in e in
* Geneanaesthetics n e u ro n s E g A ce o

o on s d o IE m e Ħ i a n d la ss o
J h , g e n e r a l a ıH . th , ti'
f a u s e n s a tio n s to e n a b le
" e d . G s . H ic h
p ro d ' '" . . s ib i. . į . . hydrdxirtryptamine g a m m a a ın in o b u tjn ic a c id g ly c in e g lu ta m a te a s p a r ta te e n d o gen o u s

su n gic a l o p e r a tio n to b e c
c tio le c y s to k in in a n d ta c h y in n s e
a r r ie d o u t id s k i tc
o p io
v an o u s
ga ses Ha s be en u s e d jn jn d u c tio n o f a n
a e s th ' Ē d
æ s e o u s a n a e sd ie tit s e a
m p le n jh g o rcid e
o tı
ga s c y c lo p ro p a n e e tc
e s ia
% ¢į h ı t a o rs Th e se are r e le a s e d by n eu ro n s an d a s tr o c y te s to p ro d u ce s lo w e r p re o r

N eu ro m o d u la ū p tic p la s tic ity th a t ın e a n s


ge n e ra lly re la te s to syn a

二二 二二二 二 二荔 骂
o n
° . ' " p o s ts y n a p tic r e s p o n s e s
-
。 h l ic a l
a n d e ffic a c y fo llo w in g p a t o o g
◆ T ia

. - . 。 , 。 。 。 。 i
lo n F t aa ç h a n g e s n s y n a p ti c tr a n s m i s s io n COnnectity
la q m il e n A th e d r u s u
。 。。 。
。。 q learning a n d
tio n s in n e u r o n a l a c tiv ty (
re sed i
g to ca】 th e lt i a s n
s c itn ıs ıı
c o rı es s
m a g ita te d p a tie n t w ith o u t e ffe c ti
n \ä r tı
te ir laa n # ] o r fo llo w in g p h y s io lo g ic a l a e r a


m e m o ry ) C a rb o n d io x id e d
lo c a lly r e le a s e d a e n o s n e i s o m e p u r in e s p e p tid e s
Eg
b r a in ttı
a t c a u s e s s e iz u r e s lillh ita la h d in s a r a c h id o n ic a c id m e ta b o p te s a n d N it i
r c o x id e
+ A ]c o h o ı
a c M pjj
y su ch as in ep ile p s y ġ ,

T ħe fo « m o ŕ a 】 co h l o th a t is v o lu n ta r iJy c o n su m e d by h u m a n s js th y l
e ą ço h o l o r

iBuJfua"UXtederivative£
saxx$i
' U '
b s ta n
su ce w ħe n a d m in is ter e d a lo n e Bu t in a r k e d Jy :te r s th e
聰 嘩 ic r o g lia
a lc o ho t a in te r m d ia r y b o lis m d by C N S n e u ron s a s tr o c y te s an d m
f r e le a s e
e e ta
m o
Ì ï e m dtn bÞic fa c to r s T h e se are m a in ly
d h o lo g y o n e u r o n f
a te th e g r o w th a n
]J t o rp s
t , nr ,
d d u la to to r e g u l m
an lo n g e r th a n n e u
act ro m o rs
łr tn J bn i l tic ity rem o d e lin g p h e n o ty p e
a n d c o n tr l l h a n ge s in i
bra n (s y p
n a t c p a s
o o n g te r m c

Scanned by CamScanner
团团团■島 ,

202 08 ı l i A Te x t B o o k o fP ha rm a c o lo c o ıo °f D r w A c tÆ o n C e n tr a ıN e r v o u s s te ı 1= o ż o 9
gy y s m

c h a r a c te r is tic s ) m a in
ly b y a ffe c tin f G A B A in th e B ra in
g g e n e tr a n s c r ip tio n b y tin g th r o gh w o s in e ń o
"*d
a c u
lin k e d k in qs
o
re c e p to rs E g C y tu lc in e s c h e m o k in e s g r o w th fa c to r s J ćJ
»
It h a s in h ib ito r y e ffe c t in th e b r a in

G A B A m e d ia te d in h ib itio n d o e s n o t a c t s o le ı a s s im p p r e s s io o f
(田 y p le su n
b ility (T o n ic in h ib ito r y in u t c a n tr a n s f
4 1 G A M M A A M I N O B T H R R Į C A C ĮD (G e x c ita p o rm fir in g pattern)
G a ın m a a m jn
b u tjï r ic a c id is th e c h ie f in h ib ito r n e u r o tr a n s m itte r in Th e m a m m l
o It in h ib ito r y c o n n e c tio n s m a y be o rgan iz e d to p ro v id e n e g a tiv e fe e d b a c k
y a ia n c
(r e c u r r e n t in h ib itio n ) v ia
e n tr
n e rv o u s al n e tw o rks o fn
\ te m Iı s principal r o le is r e d u c in
c
eu ro n s
g n e u r o n a l e x c ita b iliy th r o u g h o u t th e n e p p c
s y s te m T h e b r a in ħın c tio n in By co n tr o u in g p r e c is e tim in g f ff in g l】 in M b ito r y
n e u r o tr a n s m is s io r
g r e q u ir e s a fin e t i
u n n g b t
e w e e n e x c ıta to r y an d inhibito Jili
li ñ
' i
h r o n iz
o in m u ltip le tr a g e ts ce s

Ļ a b a la n c e m a in ta in e d th r o u g h th e r e g u la tio n a n d r e le a s e o f l I in te m eu r o n s m a y syn c e a c tiv ity a n d e v e n h th ita to r y e ffe c t


n ó jıJ g
e n an ce e ex c
g u ta m a te í
a n d G A B A

G a ın n ıa a m in b ty r ic a c id
o u
p a th w a y in c N s G 1u ta m a te a n d G A B A (g a m m a
a c id ) a re th e b in
-arþ,yri c
p le n tiń ıl n e w S in c e G A B A is in h
t
i Ël ,h
ra s m o s t r a n s m itte r s
d
g lu ta m a te is e x c ita to r y B o th n e u r o tr a i u n n n itte r s w o r k t o g e th e r to c o n tr o l m a n y
# ss se s
in c lu d in
s th
b a la n c e o f ı
e b r a in s o v e ra ll le v e l o f e x c it a t io n M a n y o f th e d r u g s o f a b u s e
g u t a m a te o r G A B A e x e r tin g tr a n q u iliz in g o r s t iın u la tin g e ffe c ts o n th e b a i
u
fj ņ
H ĐD i T
F r r ıß3 rJ lÞ

Stonlı
ge û r e l£ s e y n th e s iz e d G A B A is ta k e
n u p in to v e s ic le s w h e r e it is s to r e d a n d t s

in to th e ft b tic c le
t i A f i l G A B A i t k i to
r e le a s e d y p s n a y e x o c y o s s te r ts r e e a s e s a e n u p n

ti t e a l v ia G A B A t a n s p o t r s a d k d i t i le s f u b s e q u e n t
p re s y r p
a
ı c r r e n r e p a c a g e n o v e s c o r s

l
u s e It is a s o
ta k e n u p in to th e g lia v ia G A B A tr a n s p o r te r s In g lia G A B A is c o n v e r te d to

by a m ito c h o n d ń a ı e n z y m e G A BA tr a n s a m in a s e (G A B A 1 ) A n o th e r
glu ta m a te
e n z ym e g lu ta m in e s y n t h e t a s e c o n v e r ts g lu t a m a t e i n to g l u t a m i n e w h i c h is th e n tr a n s p o r te d
in to th e n e ig h b o ń n g n e r v e te r m in a ls w h e r e it is p r o c e s s e d to s y n th e s iz e g lu ta m a t e

E in tr y o f C az io n s in s id e th e n e u ro n s ıi
n e a c tio n p o te n tia l g o e s to w ar d u pw ar ds The

\ a yn a p tio v e s ic le m o v e to w a r d m e m bra n e s id e a n d e x o c itic e x p lo s io n o ccu rs T hen re le a s e th e

G A BA n e u r o tr o s m itic a ct o n p o s t s y m p a tic m e m bran e

D is tıib u tio n G A B A is fo d h ig h c o n c e n tr a tio n s in th e b r a in a n d s p in a l c o r d b u t is a b s e n t

ļįįľ
u n
G A BA is th e in h ib ito r y n
n u jo r e u r o tr a n s ın itte r f th e b r a in h e r a l tis s u e s U n lik e g lu ta m a te G A B A is n o t a n e s s e n tia l
g in 3 M łö % fl n Iilhcpipheral e r ip
o o c c u r r in
sy n a
p s e s (s e c o n d o n ly to g lu ta m
pc b n e rv e s o r p
a te a s a m a o r b r a i
j į į t!lłiî ghly d in to p r o te in
d in th e s u b s ta n tia n i
c o n c e n tr a te
n n e u r o tr a n s m itte r ) It is
I}Ę$ţpþ
gņţę a n d it is n o t in c o r p o r a te a
g r a & g lo b u s p a l]id u s n u c le i o f th e b a s a l

į H i
b y th e h y p o 如 也 lm u s th e
i
g a n g lia fo llo w e d b9 tro tlctl ßi:
d u c ta l r e
p e r a q u e
g y m a tte r ( c m tr a l B e y ) a n d th e h i o c a m
pp
i
pus :aīï q - m o q q i:
a9 田田 ßロバロバ !

Scanned by CamScanner
爿 出 国团团团团团■
셰翻 b イ


= m 0 j r IA Te x t B o o k o fP h a rm a c o lî g


y

e A A A hm ı
n o b o t e rz u u r )


Glutamate
+i l ln b rb II(

:Ĺ X F IB ' ' "stematic p a th w a y o f G lu ta m a te

n g n in ißjr v

區 p a th w a y p r o je c ts fr o m
th e p r e fr o n ta l c o r te x to th e

国 p a th w a y ) a n d to th e n u c le u s ben s
a c c u r ıı (c o r tic o
o r tio n f tic o
歹 d c o n s titu te s th e c o r tic o s tr ia ta ľ o co r
"
p
P r o te in m e d ia te d
p a th w a y o T a ın e ın br an deı
im ite d th e th a la m u s a n d
e
h y s th a t a sce n d fr o m
Jó r LT
l g lu ta m a te p a th w a y s a r e p a t w
m an n er c (ċ ) T h a ia m o c o r tic a
a

n gn n î in n erv i
a te p y r a m id a l n e u r o n s n th e c o r te x

ta l th e
(d ) C o r tic o th a ıa m ic g lu d e sce n d fr o m th e p r e fr o n c o r te x to
ta m a te p a th w a ys
th a la m u s

Scanned by CamScanner
ģï
rece
p to rs An d k a in a te re ce
p to rs T ħe s e g lu ta m a te r e c e
a c tiv a te th e m p to r s a r e n am e d a fte r th e
N M D A W th y l
a g o ń is
ts th
m e
aspartate) A M p A (a a m in o 3 hyd at
ro x
y l 5 meţ hyl-

T h e s c a ffo ı d in g
t
4 ) b u t o n ly o n e P s u b u n it e n c o d e d b y s e p a r a e g
e n e s
bu its (o 1 to a ts o f
o r w ith fila m e n
su n
b d h l i e p t
h ]n in b in d s to th e P s u u n s a it n c o n n e c t s t e g y c n e r e c
r o te in g p r In
e
p ĺ t h c e p t o
c lu s te r in g e r e
a m o n g o th e r s
o
u s c y to s k e le to n m e d ia tin g
e m b ra n e o
th e s u b m i ı i e fa c ū ita te s
its ħ1 n c tio n as an in h ib ito r y n e u r o t r a n s m tt e r g y c n
i n to
a d d it o m it te r in th e
th e m a jo r e x c ita to r y n e u r o tr a s
n
m is s io n m e d ia te d b y g lu ta m a te
n e t ır o tr a n s
i t e fo r
D A (g lu ta m a te ) r e c e p to r d o e s n o t o n ly h a v e a s p
e c i fi c r e c o N t i o n s

c N s T in e N M itio n s ite s
b t ls o a s e c o n d o n e fo r g ly c in e
T o a c tiv a te th e r e c e p to r B o th r e c o g n
t e u a
g lu ta m
a
it f r l c in e w ith in th e N M D A re c e p or can n o t
t
n e e d to
b e o c c u p ie d T h e specific b in d in g s e o g y
A t h b n p ro p o se d
h in e a n d a n im p a ir e d ħın c tio n o f N M D
o r s a s e e
r e c e p
b e b lo c k e d b y s tr y c n
h ia tń c d is o r d e r s
to c o n tr ib u te to p s y c
tic c y to s k e le t o n b y th e
B o th g y c l i n e a n d G A B A a r e c e p to r s a r e a n c h o r e d to th e p o s t s y n a p
i s io n in
h in D o w n r e g u la tio n o t s p f h i r o t e in c a n a f fe c t i n h i b i t o r y n e m o tr a n s m s
p r o te in g e p y r l d t d is e a s e
r e s u ltin g in n e u r o n s th a t a r e
h y p e r e x c ita b le w h ic h c a n e a o
th e n e r v o u s s y s te m
b ll l le v e ls o f
ep s y h a v e
w
l lo b e e p iı n o r m a y o
p a tie n ts w ith te ?n p o r a
a
' " . p le
.r
ī.5・ "
l l d i t h i n al co rd an d
gfiiii i t p
c a e n e s
in th e ir te m p o r a l lo b e s G 1y c in e r e c e p to r s a r
e m a n y o

A U o f th e io n o tr o
p ic g lu ta m a te re c e to r s
p a re s e le c
n o rı tiv tio
e ca n c ha n ls llo in g th e lj
n e a w grrì'nJj
k a in a te d JMDA

ĝğ
an A CÌ M A
r ec e
p to r ac tiv a tio n a lw a s
jJ l
A n d Ľke o th e r
y p r o d u c e s e x c ita to r y o s ts ıı ti
ligandated c h a n n e l r ec e
p to r s A M p A / k a in a te a n d
p y a p c r e sp o n ses

N A D A r e c e p to r s a re ï ïN a T o Jq jì
P ro d u ce a 1a r g e n u m be r fr ece n l
o
p to r h m Y ßN Y łl

b o th A A I P A an d N M D A r e c e to r s
p A j t rir l J己o rn
ta g o n is t o f N M
n a n
P ħo s p h o n o v aı
e r a te ) is fte n
D A rece
p to A p V (2 5
o u s e d to d i£
rs a m in o ë rın irn £) a r iz a tı
H y p e rp o ı o n
fe r e ıı? te b e tw ĥ
e e n th e tw o r e c e to r
p ty p e s
tic d ia 吕r a m o f G \y c in e re c e p to r
F ig 4 6 A s y s te m a

Scanned by CamScanner


島 ◆ 艮 仍
: 旨 才 召 可
氢을 g コ 过 目 個
: 。
了 管
召 : 巳 . ツ
霭 ぐ

ーーー名
: 島 伯 局 뉩 仍

昏 コ #
; g 中 9 ツ




目 d コ



ロ 招 a 野 多
q 邕 » 。 や ツ 角




=
n V 目 。 #

二 」
.
° 良

。 급


習 瞥
暨旨 R 牙 自 . 守

臼 략
y s 巴 言

ロ = 主
日 分 벽
& 卧医 며 也

ー咛
0 伯
子 。 区 ソ
的 島 : 。 于巴 吋
旨 自
饷 내 甘
習 g 歹
晌 习 才. 。
寸甘 コ


ぞ 區 掣 塗
唱蔑
目 写
a . æ . ,
S の

Ĥ 才 Sn 圧
ー当

ツ 申
净횹
n げ
甘 只

!
n
户 9 日 。
。 子

ツ マ 馈
» 島 。 닉 晌
卫 Ė ヨ 目 劬 日
0


복 角


寸 , 自 角 習 君 日

俨 邕 三仁
으主
ヨ R 罗 目 。
9 昏 & オ
習 日

售#
伯 の ロ 。
. 歹 ヨ 、

尸 ロ ロ 。 日



g 。
ğ S
声 目 包
#

ー。 卧

田 .



匡巳 鸣 含 ユ す 口

吕 蓉 裙


マ . 如 コ 0 确 言

、 . 莳 닉 ヱ V 锄 如 の
P ą 0

0 莹 巴 。 门


寸 勺 暨 巴 。 巴


切 切 . 0 卅 n
쩝 国 쩝 、 ロ 国
ロ 0 ツ .
仍 a ゆ コ
歹コ 子 경
. 、



.
n




3


H

口 ー目 オ 孑
曾净
V n
国 苣 . 日 角
コ 自 の
e 多
百医
此 也 コ
、 即 言K 旨 P 国

占 . の 臼 自

9 己
,日
區 龟 匈 刁
づ 。 刁
刁也
。 ワ


認 饬


也 句
巳 。 巳 自



圣 匈 コ


召 キ
n . 、 臼 ツ
丽 ヨ
ロ の 角


. ロ 닉 ロ 快
닉 ヨ ツ



コ 겁 旨 国 コ 分 臼


.
.

m
目 莨

ロ げ 君 艮
伯 ー
自 .

响 国
コ 島 個 了 コ 、 コ の 聲
. 。 ロ 已
長 苫 匕牙
「 巴 飞


g 月
巴 석 キ

子넉

币 一 角 。





イ き 切

如 眝





.

축監


.

n 一 ユ 邕


冒 吶 自

め 丁 の



ロ g ド

歹 因
る ・ " " 。
一 :
:
褪¥
計 獾
ď " h 一
詈 :
罅 ◆ "
コ 一 e y h ツ e e e
c e ( 一 ( ;


引 r
e
P
. 西 5


r
e
.

a

:

黔 料

U e e

華 雛
. 瓦
h b d d :

詳議
っ 卣 u m 了
.

電 ; .

邑m¢
n
a
e
n

Ţ
a 。 目PFc n n

:
:
:
e

f 3 。 n
, U U a :
甘 》
荟 n 专
= u 9
낵 n
P
r
u
s U
. 冬0 .
n




.
h
e
. h
ヘ n n

:
:

V一
n d

n
a a
e
U


0
H 萑 口 a v 첩
.
e
リ .
P
コ :
:
; 。


n c
e . 中 n a 々 . T e

.

¢ u y
. ツ

나日
e 。

n P . 。 0 。
a A .
n 9 T s
》 a . . 0 u 。
。 .
田 C
鲁@
. . r . .
目 -
o f m h

m 。
。 口
h h 넋 a
爿 口
n
e
m 5 n 4
u 0 . a .

m
H
n e 겁 P m
一 冒 P 牙h s
4
ご 9
e
e
y
h 自

a
C リ 口
落 p
P
T
.

P
a
I
. げ
a 伯 a
)

コ )

召 h .
P .
。 . 0
甘 h ロ
m 9 。
=
4
e
e
e . 甚 。 ロ y
s
e
C
匕 U 。

w 一

》 a
P 日 P
口 》 a 벽 g 。 넉 t 口 a .


巴 no
n
a
s
h
.
目a 。
þ y
s 볍
e k
e 穹
A
づ e
e
P
。 良 p a
.
h


u n 。 M
d

a 。 .

r
m . 。 m v .
e
.
낵 n 日p e 诂 N
e 甲


g f
a
t U
S
.
e
e

X


u
a
:

.
r , 角 h
e

角 h . 쿄 E
》 p C
、 口 ン 。 日 e R
m
# h . a a
t b づ
d
.
.
G
巨e
。 I
n 口 . . .

芽 d
げ n .

く u
a
ヨ U

m
.
. 日p e a

8 9 c 一
C

,口日
。 n
a h 「 U e n n 0 s 。
껍 .
ば Ę r h 口 。
オ d
只 巴 P
》 y b e h , u V 。
w一 /
门 ラ C

. g
e
I
n e
。 住 m.
.
.

。 S
,볍0 h
e
巴e
h
T

# a
u .
U
d e 。
,# ) r h イ W
弘 . 口 d b 。 . 多g
n

n n

艮 弘
歹 ş d f

m
5
.
s
a


日a e
U

h
e . 0
e
s
u

ミp
c .
.

.


ー m
M
U 已 1
。 n 낵 b 。 1 c c
ロ d P

S


0 g 、 a . 법 . 印 a

ロ e t
n . 낵 . AYS
,日


s b r 。
多 cu 、 S の c

t g e u
1
e

a
h


g
e
a 日 U
1
a 。 。
c
e
客w
a p ヨ 0
. m
m
a h 田 S
多y
m
。 t f
口 T e 。 田 、 e づ e

ゴ 9 多 一 i
. f 。 며 n 伯 . ヨ 百
m
p m ゼ 。 昏v . 、 a
、 一 b
言 a
e


1

ヨ 昏

1
c a e T 。 如 U 、 c
r 川

の 。 ys h d h 日 d 日 a
、 ゆ 。 目
i
n .
ヨ ン st w
i
s 、 中 쩝
区 昏
.
n .

佴 n 。 。
、气 T
e




. e a
y 氏 g 、
、す
一 。

w m y e
m
s
t 。

の h 么 .
.





目9
t
m
n
.
e n m 沽
e 印

e


、 多 e

召 口冒
v g e . 一
m n
弘 u
e 、
色 l 。 匕

u
l l n s 只 日
e 、

4
. 砧
日 v a
t
c
e
m 。
、 m
.
. 日 。

づ h 写
ta.1&thefah\

n e 弘
っ e s u a 、
n 。
、 官 i
c ct.lisc.n\p.sed 。

。 丘 t
1
g f
n
。 目 t
a 诂 ygdala&.he 、匕 h
。 5 h h h y
t
可 弘 e\cti6Hs(suchas l

e e e
m

Scanned by CamScanner
l j A Te x tB o o k o fP ha rm
9

M as o « o t « c t> 4 im bı
c Ħ M w a y

n& 4 7 Schp m a ic d æ w
ı in g o f d o p a m in e rg ic p a th w aya

FU N C n o N O F D O PA
M IN E
a ) ıt ħa s impot r o le s h c a r d io v a s c u la r r e
g u la tio n th r o u g h its e ffe c ts
d ils on b lo o d v e ss el
an a l a c tio n s
ru ı lth o u g h its s
A c e n t ra 】 r o le in b ı o o d p re s s u r e
Jv co n tr o l re m a ir ı j
u ru e s o e tL s łn i6 0 19
1
F ig 4 8 S te p s in v o lv e d in th e syn th es iş an d re le a s e o fdo p am iııe

CO M T ca te c h o l0 m e th y ltr a n s fe r a se M o n o a ın in e o x id ase

Ðnim[ou
o l b ĵ ız ßt l
D 1 D z D 3 D 4 an d D 5
JıD o p a m in e re ce p to r T h e r e a r e fiv e s u b ty p e s o f d o p a m in e r e c e p to r s
w h ic h a re m em b e r s o f th e la r g e G p r o te in c o u p le d r e c e p to r s u p e r fa m ily T h e d o p a m in e
īO ĵ q S x JT r e c e p to r su b ty p e s a r e d iv id e d in to tw o m a jo r s u b c la s s e s ty p e s 1 a n d 5 a r e s im ila r in
d dru g s e n s itiv ity d th e s e tw fe r r e d to th e D 11Ĵ k e gro u p
s tr u c tu r e a n an o re ce
p to rs m e re a s

o r c la s s o f to r s D in e r e c e p to ty p 2 3 d 4 ls o s im ila in s tr u c tu r e an d
re c e p o p am r es an a re a r

p e d to g e th e r a s th e D 2 lik e ty p ic a lly
SmMrfore g ro u gro u p D o p a m in e re ce p to rs a re

aicswł
į Ę9 G a n .
d G im e d ia te d tr a n s d u c tio n s y s te m s

zi iR ie su ltim a te e ffe c t o f D 1 lik e a c tiv a tio n (D 1 a n d D 5) can be ex c ita tio n (v ia o p e n in g o f


to d o a m in e i
p n th e c to ı
b sa d iņ m ) c h a n n e ls ) in h ib itio (v ia f p o ta s s iu e ls ) th a tiın a te e ffe c t f
y p a sm b y th e E n zyr n e a r o n
lic b a m in o a i
o r n o p e n in g o m ch a n n e u o
d e c a rb o x )d a s e ) ı
a
c d d e ca rbo x J
y ase (D IÐp Ą /Dikeactivation (D 2 D 3 an d D 4 ) is u su a u y in h ib itio n o f th e ta r g e t n eu ro n Th e e ffe c t o f
S to r ıg e D o p a m in e is th
e n a c tiv e l d o p a m in e o n a ta r g e t n e u ro n depen ds o n w h ic h ty p es o f re cep to rs a re p re se n t o n th e
tr a n s o r t m y tr a n s p o r te d in to th e
s to r a e v
p e c h a n is m In th e d o a
p m in
g e s ic le s by t h ť ¢ś , 7 S a n e o f th a t n e u ron an d o n th e internal re sp o n se s o f th a t n e t ır o n to th e se co n d
s tm a e v e s i l d e p a m ín e r e
g c e s a n d Js
r e a d fo r a in s u n cha n
gM fth e M P [2 1 D 1
m t n u m e ro u s d o in th
y
'
a rB i F W \
' cA r e c e p to r s m e th e m o s p am in e re c e p to rs e ħu m an
R e le a s e

U
D o p a m in e r l
e eased i
n to th e s
yīı a p Hc c ı
n e r v o u s s s te m
y a n d D 2 p to r s a r e th e s e c o n d
rec e m o s t a bu n dan t re c e p to rs D 3 D 4, an d D 5
e ft '' " l
by
' '"'"" ac , 9 r 1 1 ?a r e p r e s e n t a t s ig n ific a n tly lo w e r le v e ls
w h ic h d o a m i
p n e an d
th e r c a te c h J
o
ır ĥ M 9 5 r e c e p to r s m
X
o a m in e s a
re
d in p a s t s y n a p tic in h ib itio n D 2 D 3 a n d D 4 r e c e p to r s
o s tly in v o lv e
n o v ed
re ı Tr o m ,
・ th . ' " n o s a l tn n ii
n a l fa b
th e s n a ti
y p c clėft i '
o f tdgfiïtievFlyed in b o th p tic in h ib itio n D 2 r e c e p to r s r e g u la te s in g o d
d o s ts y n a
o u t 5o % ) is p p re a n
tr a n s
p o r te d in to theéķfikglibr 1・Ħq a tie eąl s ta b ility in th e liın b ic s y s te m a n d m o v e m e n t c o n tr o l in th e b a s a l g a n g lia

Scanned by CamScanner
团团团■■
W

n ce re b e llu m A ip p o c a ırı n s
j
h yp o th a la m us i BU ß) 9 ?
k id n e y
+9 T S m n i
D E itp r e s s e d in M h le v e ls in a s
g G i k A Ao 】
M v o lv e d
s u b s ta n c ia n i oı fa c tm y d
m r ew a r m L
b u lb CUada p u la m e n n g iu a le
v en b a lı
a gem en t a l a r e a (V T A J fu n c tio n s
g a s tr o in te s tin a l
nucleus a ct u m b e n sF o ı
m d in m o tili
q d ila ta tio n s
v aso
r e g u la t
e
ı
o w le v e l jn h jp o th a la m u s ]o c o m o tio n p r e s y n a tic
se p tu m k id \ c o r te x h e a rt r e c e p to r s in h íb it
loomotion a n d
b lo o d v e s s e ls dru l g la n d s
A ı
a
p o s t s y n a p tic r e c e p to ī s a c tiv a te

0 3 6

B n o fi
n m d o u b id e

D 4

u
Gi E R e g u la tio n s o f r e n a ı fu n c tio m
ppo ca m p\ 【1 g d a la
am
g a s tr o in te s tin a ı m o tility
th a la m t» ħ} p o th a ıam u s v a s o d ila ta tio n s b lo o d p r e s s u r e
k id n e y ńon la l c o r t e ħe a r l
M o d u ı a tio n s o f c o g n itiv e
例 宏 淄輒 a d r e n a l g la n d s fu n c tia n s n ucı
el C au daı
gastrotestinal b a¢ ra ph e
s y a p a th e t ic n ucı ・ı
g an gı
ia
g lo b u s p a lid u m L o w e s t F ig 4 9 A e y s te m a tic p a th w ay o f s e r o to m ıg ic p a th w a ys
r e c e p to r fo u n d in a s th a n a ll
Se ro lo n e rg ic p a th w a y s a r e im p lic a te d in m a n y ftın c tio n s a s ıis te d
d o p a m in e r e a to * s ł ıo T s ĉ in n e r v a te th e s e
p grs n o n e u ro n s

岛 Ħ h e dal n e r g ic n u c le i h e a v ily in n e r v a te th e s p in a l c o r d m e d u lia a n d


S u b s ta n d an ig ra G r In v o lv e d = ca u s e ro to
あ刀一 tha la m u s M Fp o c m nlĦ 号 目同層同目隴= l iF ん gen e ra l m an ip u la tio n o f th e c a u d a l n u c le i (e g p h a r m a c o lo g ic a l le s io n
b lo o d v e s s e ls a d r e n a l g la n d s
D o p a m in e ı
国■M鲥 陵墓驯■
J ĦM N Æ
国 æiu re a
p to r
m a n i u la tio n s
la o c k o u t)
ı th a t re s u lts in d e cr e a s e d
in
a c tiv ity

in
d e cre a se s
ın o to r tiv ity
m o v em

S e r o to
en

in
t

is
w h ile

a ls o
g a s tr o in te s tiin a ı lr a c l p to in cre a se ac tiv ity ca u s e an cre a se ac n

W a th e d c
吕a n g lia ri b s js ĵ jı
qm j im p lic z te d in in in
se n s o ry p r o c e s s in g a s s e n s o r y s tim u la tio n ca u ses a n cre a se e x tr a c e llu la r

r r im lt , t m l a er
o lo n in in th e n e o c o r te x s e r o to n in p a th w a y s a r e th o u 吕h t to m o d u la te e a tin g b o th th e
ln u o rft f m oun t as w 끄
e a s th e m o to r p r o c e s s e i associated w ith e a tin 吕 T he s e r o to n e rg ic p r o je c tio r ıs

Scanned by CamScanner
c 0
p ı
o fD ru g s A c t o n c e n tr a ıN e rv o u s s y s te m 1

困 p ll
"

ū ıö iÆa w
IM ł I
r h ji ı
in to th e h yp o th a la m r e le v a n d ı= li
n ı
p a r tic u la r ly h
th o be l* ıı r ・ı e ıı
u s a n e u g h t lu t a n a n : n ・ıu
,
s e r o to n e ï g ic s ig n a lin g is th r o u fo o d
弘 ii :
İi
gh to gen e r a lly d e c rea se co n s u m p tio n (e v id e n Ľ N S R a ph e ñ ijilėi m e r g ic a u
to rec e p to r
by ı
Ėn o
ced M bn a d e n y la te ł
cA M p 1 S e r e to
u ra m in e ho » æv er p to r s u b ly p e s ig h t ke th is m ore n u a n ce d Se ro e s H ip p o c a m p u s
r ece m m a
i. wir c y c la s
e an d a c tiv a te
PN S C h o lin e r g ic
2 N e u ron
i
a l in h ib iıo n

P a th w a y s p r o je c tin g in to th e lim b ic fo r e b r a in a re a ls o in v o lv e d in e m o tio n a l r o


p re c e p to f o p e r a te d K +
F a c i】
ib te A h a n d n o r
ce ss i l !a 4
J
l In h ib it het《Orecepr In 3 c

w ith d e o e a s e d s e r o to n e r ic a c t i i han n e

to w a r d s
g v y re s u itin g in d e m ea s e d c o gn

d Js
itio n a n d an em o t io n a l
bi ï id Ió r
c

v o lta g e g a te d C a 2+
m ym te r ic pı
ex u a 山e a 】
rı jn e æ le a s e

e r g ic n e r v e
te r m in a l
n e g a tiv e s tim u li T h e ń ın c tio n o f s e r o to n in in m oo m o re n u a n c e d w ith a iĮ
jt a an n e l
4 M o lin
Some a tu
in te r ic pı
ex u s
ev id e n c e p o in tin g to 1ų a r d s in d le v e ls le a d in g to d e p r e s s io n fa t ig u e d ĺ
m y em
a e ase an s ic kn e ss rtTí Oed to
s H y p e r p h a g ia
b e h a v io f a n d o th e r e v id e n c e o in t fu th e o s ite
p 叩p o b e s ity »
S Y N T H E S IS S T O R A G Ę R E L E A S E A N D T E R M IN A T IO N O F S E R O T O N IN den yı to p to r
,
In ı ıib it a a te
ł
cA 】
W J CN S c ra n o o d
ja l b ı v e s se ı S e r e to n e r g ic a u rec e

5 HT Æ d
s y ıt th e s is
s e m tu n in æh y d r o x y t r y p e ) s yn th e s is is a 2tep p ro c ess Th e Jir s t į Ī,
,
o f 1 c l
e Je :.
c y c la s e
PN S
M u s c le
V a sc u la r sm h
o o ı 2
C h o lin
G A BA
e r g ic
e

h e te
rg ic
ro re ce p
an

to r
h ic h q u ir e th e ith
p h a n h y d ro x y ir o 8 1
w re e tr J p to d TH B
s e n zym a se w o x y ge n n a n
as co aß
3 v a s a c o n s tr ic tio n o f
fa c to r s N e ith e r th e en z th e co fa đ o rs a re ra te lim itin g fo r ith e r s te f th e s e い ia 1 M d v e sse l
yin e n o r e
p o 9 !杉 加加 c ra n o o

t io H uy ll b ī a in is d i o o lh m d
phan Se
in e
re a c n s r tu a a m to c o n v e r te to s e r o to n r o to n in is n : sn ı u r
a ls o z íf z
th e s iz e d in th e p in l g la n d Jo th e bs e q u
syn ea as a p recu rs o r su en t en z y m ą tic fo t"
j?ç th
r rm a
e
p in ea lh o rm o n e m e la to n in cetyl 5 m e th o x y b J p ta m in e )
S to ra g e a n d re le a s e S e r o to n in js p r in c ip a lly fo u n d s to r e d in th T e e m a in ce ll ty p es i)
se ro to n e r g ic n e u r o J ls h th e a v s a n d jn th e 组 曲 tin l m y e n te r íc p ı
e x u s ii) e n te r o c h r o m
a a ï tin
1】
s jn th e m u c o s a f th e
ce o g a s tr o in te s tin a l tr a c t a n d iin in b lo o d p ia te le ts S e r o to
n e u ron s a n d e n c e lls c a n \ 出 e s iz e s e r o to n in ıo m its p r e c u r s o r a m in o
gi c

a d d
L tr y p to p h a n w ire re a s p Ja te ıe ls r e ly u p o n u p ta k e o f sero to n in fo th e ir s to r e s L ik e
r w is e
g ic n e ıir a n s
s e r o to n e ı Ħ f# n h a v e th e c a p a c iy fo r a m in e u p ta k e v ia s e r o to n in tr a n s p o r te r ș r:
T e ım in a tio æ
M e ta bo ı
is m f s e r o to n in is c a r r ie d
o o u t p ń n ıa l iıy b y th e o u te r m ito c h n ij r ia l
m em bra n e m o n o am in p o x id a s e M AAT h ic h o c c u r s a s tw o le la r
w m o cu su b ty p es
ca lle d M A O A an d M A O B B o th s tłb ty p ha v id e s p r e a d in th e b r a in
es e a w o c c u rr e n c e a n d in
p e r ip h e r a l tis s u es A lth o u g h th e y do sho w so m e r e n c e s In c lu d in g s p e c ie s j, ģj ł
ed
v a r ia tio n s w ith re s p e c t to th e e x te , i t o f th e ir p r e s e n ce in c e r ta in t is s u e s an d ce ll ty p es
S t z o to n in re ctp to n

ecı
assilirfi{M s c h e m p p e
r e c e p to r s T he
ro o se s 7 su b fa m iı
ie s o f5 H T
a in
n ı receptors a n d th e ir b ty p e s
g . 5 H T r ß H T u Ļ 5 H T IB , 5 H T m 5 H T IE a n d 5 = tm r ) 5
su e
H 1 2 HliiA, 5 H T zB d 5 - 0 , 5 H T a 5 10 4 5 H T (5 H
a ıı
, 5 T5A 5 H T 5 B ) 5 H T 6 a n d s H T ?
hav e b e e n id e n tifie d

:T IJ
了 JtJ ンシ '

ı:

Scanned by CamScanner


潲回
国国 冒2 2 ı ど工


ー忒 鬣 麗

B Jo c k in p m
y o f th e
p r a c e d u r e {a n u re s ta )
:
J hi
・c in
g u n c o n sc i
o ı
ıs n e s s S TA G E O F A N A L G ES IA
n b itin
g n o rn n J bo d
y
R e la x in
g th e m u s c le s f
o th e b
o dy
G e n e t ıı trß ĵ u o ıu í

a n e r th e i
t c a a re
C O ru c io agen t
ıu n e ı¢t rhlch in d u c e
ı r
J e v e z ai
b le lo s s o f ıll a ėń Ėa Ĥ M ]y
äh d
C
ë n jıb j ÐT
l) j

r!Zı
ı
Z n o e ßņ 1

ClrsJzär
t
ı ť u o rg
gn s b
ı
ıßı
qyıa i
! » ilÐr ll a j rln
\

!



śi ı
a
f

t 国

Scanned by CamScanner
u
s
e
h
e
M 4
d n 6
u
o n m Ī N C
W d r
c
o
m
g
s
a

a
N
H
o
L
A
h
e
p
p
e
s ◆V J
n p
a
u G S r u e
p h v A s a S o r S r n
a s e
a e L
O s u s
a e
a
c
o A o
r
e p x Ħ o g s 4
r
a T
d C h n
o D e
e r d n a
n
h
v c
O e A e
a o
e o c p
e o N T c e
f
p n n A c T E
f h a h
o c L
y c
h
D s E E
v n
h
O r
c
a
s m r
a s
e c h e o N u h e n e
e o y o n
5 n G p h o s
Ħ h a e s d y p
n Ħ a a a
c 0 r E o c o u u e O y u s
a
o u r r s
e % a N p o
h Ħ a a e o F o e u s
s E o a n s a r a n
o o
a
a o n n n G y p g e
o f n R n
e c m e e e q E a e s y a
f d u
p A e
e N n a
u
v L d I d
a
a
M A
y
e
E
R
d
o V
p
e r
e
e A G e
o n N n e A y s
f
r
u C e
n L p e
s s A e c p h s
ı
s
E A r e r e a
n r S E a a n o
P M h N s r
h o T A o e e p n e
h o o e ı A
a m e
H m p h p n E y
r n a
E o o
a r c d
o o e e S s n e r s
e T h n s T n
o a o u T o
o s e t h H
p n C p h v
n e x e E p h d
a o
c
e
S i
e s c e
n o S o a r
n a c r s n d a
g
e
d
r
n
e
s
A m a n o e
n
e
n
g
a
N
c
o
e
d
g
e
o s
e d r
r
a
o
n
a m u
o b
s
p
u
ü
o a f e
a p 3
a s o
u
a
n
a r m
n u f a n e a A
e s d n v r
q a e s
s g d s k T

%
n F O D s d v h
h c e p
K B e h e
e a e
a e s e o d x
e n n o a ĥ e d
h a s n w e s
b o
a d o h
c
s n a n m c
z
o
e
r
r
a q y w B
a v u o
c a y n n d a a o h
a a a o
s a e a c p s b c y b
o v z o v k p d
k
o g n d
n
n e
e
L
e
p g y
m o y o o o
a s a
n
'
n d
o u e m
e n P
T c o
s
W
"
a s e e n s n h
h n s u s r y n a
g o a
s e
h s u c e
s P e n n n
e e r
v
a
u
h
e
9
9
T
q c
s
W b
o p
u o Z
n
e
c
u
d
p
s
o
r
p
e
s

o
, r C T i o c
r
e c d o 9 j
a Ĵ a a n r a
q u
s n
g
p j o d 9 z 9
b
s
a
ĵ n q u q u s o
/
q
Į e n n
J
u o
z
Ð
1
z
ū w v e a
e e o o a
u n
e y d

=
4
A c
c
n s r
p e y o e
s
ņ e x s
J
p c
u p
s i
r
b u

y
r o b e
e
ß Ð e o p c
r e e s
v ń p
e r n r
Z
T
c
a ĥ
e e o
g w a u
b
p
q h
a
名 e e n u h s

L
目 h s
团 p e r
e
e
r
m
团 h r a e
e s
n m
O
象 e c r
a a d a s
s c
p u r
a n
u
p e b y s
I e
a o s e
r n u m s h
a a s o o e
r
o
u y c e u r
b e F
s n e o c
u
m e
a
c o
e
a g
4
s e h u ń v
a a r s
e 1
e
m s
u
k
a
s
o
e o s 1

o s d
r
e
g
e m s d
a
n r M
e r u e
c s e d g c
o n u h
u b r o f g p
H c a
e f
2 a a t a o n
s
r o r n
y
C
f
a u h m c
s
m
d d r
c
o
o
r o d
e
m a
o
e
n o
p
m p e m a
b
s
e n t
r
f
o
u e n a a
I
p e c n
a
a
d b e h o h V
n
ń g e e o a
e u f
n
į
a a c
H s o r a p f
e
2 s s i b
C a c m
m
t o
r e
3 n r w t
i
e t n
H n g o i
a n w a
6 m h
t
s e n
m o p e e
s
f
a r n
s t
h e T h
e e t
u c s h e
b h s e w
t
h e w a u
r a
o c
a r
s a e n i
f u c e s
e s t w s s
f g e i u
f
a o r h e
e s
f h e s
c s
r t
t n i

b
i
s
u
b
c
a
c
s
w
e h
ı b o g t
e
c
a n e d h n
r v
ı d o a
e u e t
s o h
e r r r n a e
t r
t p s
I e r
h r y t s
i e n s h p
s s t
s
u i a
s h e g r
m t ł t

e
e
r t a l a
a y
e s l
y c

Scanned by CamScanner
M ł

%

团团国

。 山h ,

l . '

« ih l\ ū ] i n rr 2
" " " " am h " " e p to '" 【

iŁX J (N M D A ) h b im p lic a t e d
v J ben zo d ia z e p in e re ce p to r s an d m e th y l a sp a r ta te re ce p to rs av e e e n

r e la tio n sh ip fon ith th e th e r is t kn o w n


g h th e e w o n o
a lth o u o

l h i th e r a p y / A d ju t to g e n e ra l an e s th e s ia 1t
ī I Ť ř ?" a a lg e s ic th e r a p y G e n e r a a n e s t e s a
n c
n
,
d lg e s ic ffe c ts
m e ta llic cy ı
in d e r s It i
s n on to
" tĮ s u r g e r y a n d d e tis t y fo r its a n e s th e tic
Į ? »iĦ n r an an a e

x ic to live k id n ey s a n br a : D IE T H Y L E T H E R (A n a es th e tic e th e r)
n I l j: ch / t is -d o
I an
m n io ń l
y !llb is ] a , c
ie a r c o lo u r le s s m o b ile liq u id w ith a c h a r a c te r is tic o do u r sw ee t burning ta s te I t is a

rr v 0 1ä tile an d h ig h ly in fla m m a b le Its fo r m u la is C 4 H r o O

bzu tn ıo x C zH 0 C 2H
5 5

a n a e s th
s ia
eı A ı
o rı
e n itr o u s o
x id e
iíy p e rc e n t
ï\W'ii£
t
Ĥ
ril ii¢rċ h ëh p a n d c a n
scre

į utiMnt o f th e a n e s t h e i c s
tio

b e g iv
n s a n

en
d
requ

by dro p
r is k o

ir d
f in

m e
\ \la tio \

th o d a s it is c h e a p
n eu m o n ia is d e c r e a s e d

It is h ig h ly
m

s o lu
o r p h in e r e

b le in b lo
du

d its
ce

w ith o x
yg e n ĥ ae be e n l d u ėa ü İ iis r o l
tť ' i l o
u se d fo r d e n ta l an d in ír Fk jn ĵ b
p on ge d an d u n p le a s a n t
ı

m S» V
Ëi a ļ
4Į ĝ

Scanned by CamScanner
ie

. q p

r趙 례 A Te . TB ' " O f p h' "


g
w
°

: Z X X X ī
" " a U 8eS e
a o n en e ss yes co n
ge s .

華鯊

b lo o d q u ic k l
y J t s h o u ld la x ū an d
b e s to r e d in ffe c t It ĵ n du ce s m u s c le r e a o n
p ro te c t fr
lig h t I ls \ t ta in e r tio n o n c N s a n d little a n a lg e s c e
i
illts p r in c ip le
o m co n
m oı e n ııa r io r m u ı is C 2 H B
a t
te m p e ıa tu
a
r e b e lo
w
tj᧠a c

l i ti e x c ita b ility It m a y p ro v id e a m ild s t im u lu s to


a
C I F 3 Į t is iti ity 】 b y a te r n g s s u e
r
n o t in ı la IT u
ra n d ŕ eduäi
ŕ eduëÈ p a imn s s e n ss ı
v 】 ĉ

M e c ]u n iıın

a bı
e ia n h i
e o b r o n c h ia l s e c r e t o n s
o f a a d śa liv a ū iĵ n o r tr a c
om ıt c a u se s E th r a n L iq ln h 1 00 %
gen e ra i an ae th e s ja E th r a n e E n flu ran e liq 9 9 9 % e
du e to ĵ ts B ra n d N am es
a c tio n s in d d
ím m o b iı o n m u ltip ı h r iĦ 1 a n o r iz e r 5 to 3% u ce

d is h n o s t ab se n t It d o e s n o t
l a n d h e p a tic to x ic ity P o st o p e r a tiv e v o m itin g an n au se a a
re n a
r e s tr ic te d
s o it is ħr l in n e u r o su r ge ry I t is co s tly s o its u s e m a y b e
p r o v o k e s e iz u r e s
l u se

à th e n n >is e it h a s b e e n u s e d a s ro u tin e a n a e s th e tic

MËMinłs o f a c tio n The m e ch an is m o f a c tio n is s im ila r to en flu ran e

b,it įė . Ge n e ra l in h a la tio n an es th e tic u se d fo r in d u c tio n a n d m a in o f ge n eral


te n an ce

s e n s itiv ity b ylte r in g tis s u e


a n e s th e s ia It in d u ce s m u s c le r e la x a tio n an d re du ces p ina s a

eiB It d o e s so b y d e cre a s in g th e e x te n t o f
g a p ju n c tio n m e d ia te d c e u c e u c o u p lin g
M d tM t Èg th e a c tiv ity o f th e c h a n n e ls th a d e r lie th e a c tio n p
t u n o te n tia l

rĖiäiłr ť aim es F o ra n e liq 1 o o % F o ran e Ľ iq In h 1 o o %


w rtßn Ðln iı
ņ F§
R MR A N E It is a d c o n g e n e r o f is o flu r a n e It is le s s p o te n t th a n
n ew flu o r in a te

i#Wą»f Ť° h ig h e r
,
co n cen q u ir e d fo r in d u c in g a n a e s th e s ia It is h ig h ly v o la tile
ta tio n m e re

a th e r m o s ta tic a ll h e a te d v a
y p o r is e r is u s e d to p r o v id e c o r r e c t e x a c t d o s e / c o n c e n tr a tio n s o f
d e s llu r a n e v a p o tu s in th e c a r r ie r a s (N itr o u s o x id e lu s o x
g p y g e n ) m ix h ır e
It h a s a n a e s th e tic in d tio d fa s t D
u c n an re c o v e ry v e ry e p th o f an a es th e s ia ch an ge s ra p id ly
$Päș . in '" ' " . . .. . ... .. A ti. . p o s t a n a e s th e tic co gn itiv e an d m o to r im p a ir m en t is

Scanned by CamScanner
i o t v o la tile a n
d is
N E C H C I C C 12 It is a n a n a e s th e tic liq u id it s n
(ii) ï ts in d T R IC H L O R O E T H Y L E b a n e s a n d is n o n
u c tio s m e m r
n as a n a es ttı
e tic is h lo r o fo r m It is n o n ir r ita n t to m u c o u

(iii) C M o t o l
īa p id an d p Je a s a n t ı1 9 1o
l ĉ 9 ! le s s p o te n t th a n e th y l e th e r o r c th ly a n d q u ic k ly
in a ir It in d u c e s a n a
e s th e s ia s m o o
rn does iJĥ mrrifį Driì i d ith x y \ n o r
n o tp r o du in fla m m a b le w h e n m x e w o
ce cap iu a ry b Je e d i
(iv ) ıt is n n g h ı e n e is it d o n o t p r o
d u c e d e e p a n a e s th e s ia
o n irr ita n t t
o m u c o ıls m bra n
i. N ißm 9 r T T h e m a in d r a w b a c k o f tr ic h lo r o e t y
k in s p ir a tio n s a n d m a y in c r e m
em e
D iıI d v m t es
rg e* o f Æ ti n s It c a u s e s s h o r t Je r y
o r o fo r m lo n e i ii s o it is n o t s u ita b le fo r lo n g o p e r a o
(i) c u
iï bı
iq q

o r o fo n ııc a
p ir a tio n te
rr ra
u se ıaı
ï h b lo o d re s
(ü)C M j» w sï» g a n d d e c r e a s e ĵn in g in d u s tr ie s fo r d e g r e a s in g o f ın e ta ls a n d fo r
o r o fo r m ls o d in d r y c le a n
du T ń c h lo r o e th y le n e is a u se
in o c e s c ar d ia c li h o u ld n o t
罗 iii) 1 t d
an ń y wh m ia s d u
e to its s e rı
sa tiz a tio n o i m
ı
i
y o '" H W
b n c

n Rí
Iir : o il a n d f? t
bJ á i t e r e d
e x tr a c tio n

a t th e
D u r in

sam
g
e
ex po
tim e
re
s tı

as
to tr ic h lo r o e th y le n e

th e r e is a d an ger
v a p o u rs a d r e n a n e s
o f v e n tr ic tıla r fib r iJ1a
tio n b y
e p r e ss e s
re sp ir a to :y c lo s e c ir c u it a p p a r a h ıs cra n ia ıp a ls ie s m a y
c en » e s c a u s in
tr ic h lo r o e th y le n e It s h o ld a ls o t b u s e d in
v ) H Js to x ic to ı g re s p ir a to ° d r e s s i

ıiu o trj l【b iıj u n o e
iv o n

L二
er
. T J io ıRJ J H ) 。 '" " ' " v e "

Scanned by CamScanner
y 8 0 to
,
75 m g a t Ĵ n te r v a ls o f 2 o to 4 o se co n ds


Scanned by CamScanner
N a rco a n a ly s is A d u lt In tr a v e n o u s】
y 1o o m g p er m in u te In j Pentothae n o t to e x cee d 5o
ın lp e r m in u te TO
SH i n
C tr a in d jc a tio

o n n s H yp e ıs e n s itiv ity to B a r b ih lr a te s s ta tu s astaticus liv er d is e a s
e
。 c a r d io v a s c u la r d is e a s e r e n a l d is e a s e h yp o te n s io n

. P h a rm a c o k in e tic s
I V o n s e t a c tio n 3 0 fu 40 s e c o n d s Ħ a s m a h a lf life 4 to 8 h o u r s C
r ss
. p la c e n ta e x c r e te d th r o u g h u ıin e u n c h a n g e d
es
"
fb r i
。 tı r u g i n te r a c tio n s
lm r e a s e a c tio n w ith C N S d e p r e s s a n ts
U s e s it j
s a b a r b jtu r a te is u s e d ı


b r th e in d u c tio n o f a n e s th e s ia P r io r to th e U S e
oiŢß
iĖŕ
g e n e r a l a n e s th e tic a g e n rs a n d fo r in d u c tio n o f a n e s th e s ia io r s h o r t s u r ic a l D i,
一 th e ra p e u tic r o c e d u r e s a s s o c ia te d w ith
g gn . ģiiŁ
p m in im a l p a in fu l s t im u li T h ío
一 p e n ta ıis a n u ltr à Ėtio r t
a c tin g d e r E s s a n t o f th e c e n t l
p ra n e r v o u s s y s te m w h ic h in d u c e s h y p n o s js a n d a n e s th
e s iá į bt
notana1 :(n in r íł
ı jî
B r a ııd n am es T ħio p e n lo n e in je c tio n p e n to th a l s o ä A th a l p e n to
u m n es n e T h jp e n '
M ih a i
50 0 m & l g m I Jr iJ a s s n r

f an aes th e s ia p e a d ia tr ic
s t ır ge ry
d a in te n a n c e o
ń田田扇a iis
¡ In d u c tio n an m

tim la c ta tio n
d d u r in g d e liv e r y
e
N t re c o m m e n d e
C&Ĥ tił
idica«Ons H y p e r s e n s itiv ity o
d
d
E ld e r ly r e u c e o s e
h yp n o t recoended
e ip o la r iz a

p r o lo n g e lL
tio n The p a ó w
p tic in h ib î to r y e ffe c t o f G A B A in th e th a la m
u s is Éi t äk : g WŤĖ s th e s ia b e lo w 3 ye a rs a ge
d is t r ib tio q u ic k p la s m a f life 5 to 1 0
haı
X U E i n e «C S ds u n
o n se t a c tio n 4o se co n
U sel ï t j

:
- s , b a r b itu tE js U S e d io in liv er
ıa
th e in d u c tio n
g en e r a l a n e s th e
r
o f a n es th e s ia P r io to th e e p ö l ,Į
ith a lc o hol d a tiv es a n tip s y c h o tic s


tic r d se
a g m ts an d fo r in d u c tio n s y s te m in crea se w
o f a n es th e s ia

IV 1 to 1 5 m g p er kg
b d w e ig h t E ld e r s
A d u lts 2 to 2 5 m g per kg o y
Ť appwiTņately 2 o m
In tr a v en o u s

g p e r 1o se c o n d s u n till in d u c tio n is s e t

M ain te łl ą n c e in te r m itte n t A d u lt 25 50 m g is re q u ir e d
In
g /k g p e r h o u
r
ca ti
G 5 u te s fo llo w d b y 0 3 to 0 6
e ın
g p e r k g fo r
:
e n e r a l a n a e s th d a tio In itia tio o3 m ĵn
e s ia r e d u c tio n Ic u se n n m
o f fr a c h lr e s d ju n c t w ith kg per hou r
a 0 3 to 3 g p e r
In tr a v e n o u s] 5o to 12 o
otheranaestheti¢
JDJfi in c re m e iit o v e r 5 to 1 0 m in u te s M a in te n a n c e m

c on tıa in d ic a ◆o ł y m g 1 m l in 5 to 1 o D ip ń C e lo fo ı1 0 m per
o fo 1 P ro p o v v an
p ifo l R
R a n
u
e i s e n s iliv it
se co n ds B ra n d N am e s :p ro
p o fo l : In je c tio n o
h } p o te n s io n r y s ta tu s a s th m a tjc u s
en a l h e p a tic d is e a s e D re p n a n r J {
P h a ım a c o k in e ti
cs N o n se t a ď
o n 3 0 to 4 0
a tta in e d e x óeco n ds
c r e te d u n c h cro sse s
a nrg e d
d in ue r in e p la c e n ta pea k iJR !jn T 1
co n cen tr a tio n m

Scanned by CamScanner
■國召 四 ■

赜郦 ◆

i an d fo r se d a tio n in d u c tio n a n d a n te r o gra d e a m n e s ia
is ė p ile p t c u
s
s ta tı
kg bo dy ig h t) I V in j
s i į 3 m g (0 0 4
Do ¢ i o
m g p er w e ec tio n
U w U se d in th e in d u c tio n o fge n e ra la n e s th e s ia Lo T a b le t 】
n je c tio L L T Z to L o r im L
d ıte s
n a】 ra z e pam : n o re n o rv a n ra p e x e r o pe z
Bm B ra n
ıd n a m e A id a le in
- m
j 2m ghn lĹv Vjri lm g 2 m g
C a lm ese

S LO W A C n N G D R U
GS P A Z Q ıW . Į It is p re fe r r e d ov er d ia z e p a m fo r an a es th e s ia u se I t is an u ltr a sho r t

+
be n zo d ia z e p in e ha v in g rap id o n s e t a c tio n It d o n o t c a u s e v e n ö u s ir r ita tio n an d h a s n o n

Ï °Į
' in d u c tio n o fan a e s th e s ia d o s e N 1 to 2 5 m g o f m id a z o la m
p
・ Ęa n d ņw e s M id a z o la m In je c tio n 】
W d az M ez o la m S h o r ta l B e n z o se d lm g p er lm 1

ĺ cTM«INE It is a n N M D A re c e p to r an ta go n is t w ith p o te n t a n
a e s th e tic e ffe c t I t is a n o n

d r u g u s e a s g e n e r a l a n a e s th e tic
b a r b ih u a te It p r o d u c e s d is s o c ia tiv e an a e s th e s ia

c h a r a c te ń z e d
b y s u p e r fic ia l s le e p a n d c o m p le te a n a lg e s ia It p r o d u c e m ild m u s c le r e la x a tio n

It d ą f ņ o t c a u s e r e s p ir a to r y d e p r e s s io n a ir w a y re fle x e s are m a in ta in e d m u s c le to n e

in\qęąșş L im b m ov em en t o ccu r E ye s m a y rem a in o pen The a n e s th e tic s ta te p ro du ce d by


K e ta m in e h as been te r m e d as d is s o c ia tiv e a n e s th e s ia in th a t it le c t iv
a pp ears to se e ly
in t n p a th w a
a s s o c ia tio
w pt y s o f th e b r a in b e fo r e p r o d u c in g s o m e s th e tic s e n s o r y b lo c k a d e
ţFĦfin s Įe c tiv e ly d e p r e s s th e th a la m o n e o c o r tic a l s s te m b e fo r e s i n ific
y g a n tly o b tu n d in g th e

WĮ F \ e n t c e r e b r a l c e n te r s a n d
p a th w a y s (r e tic u la r a c ū v a tin g a n d lim b ic s y s te m s )
\ Sþ f ļ Įșm o f a c tio n K e ta m in e in te r a c ts w ith N m e th y l D a s a r ta te A
p ) r e c e p to r s
9Pį ųi E ę c e p to r s m o n o a m in e r ög ic r e c e "p to r s m u s c a r" inU iLc r e c e p to r s a n ad v o lrta itlv
ta g e s e n s ı iv e ĽC a zz +
W

X H 3 ï w
i9 g Çw e l s U n lik e o th e r e n e r l
Gg a a n a e s th e tic a e n ts K k e ta m in e d o e s n o t in t e r a c t w ith G A B A
g

_
'
=
"e c e,p t"o r s
r
m an a e
' " ' '" o tj' '"
g m en t o f a lc o h . .h o rt
o l w ith ? 1 7 9 3 Jì o ! fz
aw a l s yn ? om e
K e la m ln e
ÐrĮĵ n i bn t

k
2m

F
& 5 m & 10 m b ri D iz e C l
g ta b ı
e Ķ Jn '
je c b o p a m p o se

t
n 5m v a liu
g p er m m Ħ a c id o x p a x tı
m
u x Js' Į t
。 :ın xo

, H: h r e e tim

THth
es

:1
' ' " .' '" " ° "
pa m p '" It is Je s
s ĺir r ita
n t s lo w a c tin K

一 M w a ke n i B n iJJ ß w o h 70 M V
e c h łn bm o f ıc tlo
n g is d e Ja y e d an a rı
H y p e rp o ı z a tı
b n t b j ĥ iÐţ o n
n o tr o y
p ic
ıu
r e ce
p to r s ĵ n th
e c N s Bi
n d in
g p o te n tja te s th
e e ife c ts 97t r b ir ł
w
o f th e in h ib i
to r y
T ín ĵ itjirlrr i J

一 F ig 4 1 3 M
echa n is m o f a c « o n k e ta m in e

Scanned by CamScanner
P a tie n tķ to l t m a p e tıli ĉ ! C rb r o
e ra n c
e c v a Ju n c h ia la n d sa liv e ry se cre tio
Jf th e a ín e n s
p a in its e ıf m a
y s tiı
ıb P e n ce p ı c o m p le tio n s o fG en e ra l A n aes th e s ia
e re co io n o f s u ıfe
g n iz e d Fn

İ Ï HX,0n
r jn
a d đ tio g A lth o u h t
n to g h e r t ir e s e ħc e -
an a Jg e s ia
jt c a u s
se
d'"ing a n d a fte r a n a es th e s ia
e a Jte r a ti T h e re i

o n s jn a re m a rke d

L
回国团团团团■上

Scanned by CamScanner
î m 9 ı
!¢ ræEy 3lA Te x tB o o k o f P ha rm A t in g C t r a ıN s y te m \
a c o
ı m a
'
D ru g s c o n e n e rv o u s s

p nľ
1) R eș p ir a tio m d e p r e s s io n an d h yp e r c a r b ia t rıs e d The days b e ca u se o f th e ir
'
1o y c lo p r o p a n e m e th o x y H u ran e are n o se
th y ı
h c
T oı r en e
2 ) J a ll in b lo o d p r e s s ıır e fĵ i
rT ı o e
u "o r tiv
ri R V h T r ic l d u r in g p o s to p e r a
e re c o v e ry
ni b ta ・ es
3 ) A s p h y Jd a d is a d
v a ・ o
an d ]a r y n g o s p a s m

4) a s y s to le c a r d ia c w w w as

5
) th ere a re ı
o w r e s p ir a to r
y an d sa liv a tio n s e c r e tio n s I t is b e c a u se m o s tly n o
a n a es th e tic s n jn it
a re u se d an t

6 ) T h e p a tie n t h a v e d r e a iìfu l p e r c e tio n a n d r e c a ll o f th e e v


p e n ts o f b e fo re a n d D
su rge r
y J t Js d u e to u s e o f lig h t a n a e s th e s ia a n a l e s ia a n d m u s c l u
rin g
g e r e la x a n ts
Iıh iT
7 ) A s p ir a tio n o f g a s tr ic c o n te n ts c a u s e a c id n e u m o iti jb v
p n s

8)
X X J X " s i. ' ' " _ Th e se d ru s d u e
g . . } ,

A fte r
9)
.
a n a e s th e s h
'" u m o th e r e x d ta to r
y e ffe c ts a re n o rm a lly se e n w ith .
Ł
,į・
t ib r 【o ĵ
fi8=ĥ
d itio
ı

o f
o
"

f la c k
" ht '.
o f
A

s le e
fte r
p is
m id n

c a lle d in
ig h t T h e d r e a m
so n m ia H ypn
o c c u rs

o tic s
du
ar e
r in

th
i l s le e p
g lig h t o r p a r t a
e 山 u g s to tr e a t
th is
fc o m p lic a tio n s ) 9 Į T he co n n
(in ia )
th e r w is e c a lle d a d iś e a s e
s o rr m
1) Vomitinzı
auseaareconunon r ro īj íb r ro ) co n d itio n o r o
s y s te m th e iŕ
h e n tr a l n e r v o m
d a tiv e s b o th c a u s e d e p r e s s io n to t e c
2 ) O rg a n s to x id tie s liv er an d k id n y dam
eĵ il o
q { }:
lt H y p n o tic s a n d s e b id e re d
e a ge d to C N S T h e s e d a tiv e ın a y e c o n s

H
i d e p th o f d e p r e s s io n p r o d u c e
3 ) T h e r e is em e rg e n c e d e lir iu
łJ r r g tsì1į d iffe r e n c e is b e in g n
h y p n o tic s a s m ild s e d a tiv e s
m
ţ t 【f k Į ir n Ł a s m ild h y p
n o tic s a n d th e
4) D u e to o v er d o se f a n a e s th e t m th e
o tic d ru gs s io n o f c e n tr a l n e r v o u s s y s e
an d du e to th e h lty p o s itio i a n d s e d a tiv e p r o d u c e d e p r e s
o ccu ń n
g n e r v e p a ls ie s
u n in g tlï è iķ ījśi Q u ą liţ a b v e ly h y p n o t c s
n tita tiv e ly
) r [9 19 1ì ËiJ d iffe r e n c e b e tw e e n th e m is q u a
5 ) T h e r e is im p a ir e d W - o to r fu
om n c tio du to p i o c la s s e s
tic s a r e c la s s ifie d in to tw
n s e e r s s ta n tsed a tio n by an a e s th e tic s r The sei a d tiv e s h yp n o
6 ) T h e r e is a t e le c ta s is ia
pn eu m on
lĵ J ř d T ß8 (ï j (I) B a r b itu ra te s
n T h e re tio n l d is o rd e r s

)
as em o a an d c ha n ge f tr itu d e in
e ld e r Jy d u e to u n dergo n l a i ıa e s th e s ia
o a so m e p a tie n ts e śp ét iá u y m )ļÞĮ g ņ ıB a r b itu ra te s
e g en era
o f lo n g d u ra tio n B id
D O rg a n ic h y p n o tic s ro m e
ru g in te r a c t io ru
iıım h b d d a tiv e s B ro m id e s are

X
d e en tıs e as se
ta s s iu
īI
d iu av e

'
1) Bo rm id e s o f so m p o m a n a m m o n
^ _ o le p tic s ,
M o n o am in e o x id a se in h ib ito tio n r e q u ir e d fo r s le e p c a n n o t b e a tta in e
d b y a s in g le
, rs
po te n tia te ï io t u s e d Ŕfa r h y p n o s is d u e to c o n c e n tr a

d o s e tr e a tm e n t T h e la r g e d o s e o f b r o m id e s c a u s e b r o m is m c h a r a c te ń s e d b y h e a d a ch e
2) H a lo th a n e s e n s iti z e ħe a r t to
' Jßs tl Y u í
d r e n a lin d / d is tu r b a n c e
d e r m a titis c o n ju n c tiv itis g a s tr ic d is tr e s s a n d n e u r o lo g ic a l i
a e se a se s
a n o r e x ia
3) H '

P re s su re
" "

m ay
t is o n
fa ll m
a n ti

a rke
h yp
d ly
e r te n s iv e d ru gs an d '" iven g e n e r a l a n a es th e ģ ĺ£ h o o Įd ßlż J !
d
N o w ą d a y s b r o m id e s a r e n o t u s e d n o w b e c a u s e b e tte r a n d s a fe r u g s a r e a v a iı a b le

d ) If a p a tie n t is o n c o r lic o s te r
o id s th e r a
o p e r a tiv e l p y a n d Į s to b e iv e n
y lo oN g gen e ra la n th e s ia ĥ tj n i N IŁÐJ I
,
g yd a e s in tr a
y ' " iso. . B e g iv e n s i
n c e a n a e s th
e si a is , s tr e s s w h ic h r ır J rl ìıīv ï
ca n
5 ) ıf a p a tie n t is d a b e tic
a n d is on o ra i hty p o l c a e
n e e d o f in s l g y m ic s d r u s d
u in is in c r g u r in
e ase d g a n a e s th e s ia T he
h y p o g l c a e ın i
so g iv e p Ja in in
s u lin e v e n i
y f th e z i
cs
p a tie n t is o n o ra l In ï o n o

Scanned by CamScanner
邦寸


c
h
a
n
n
e
U
C
h 式
n


巳 A

B

R
ー げ

パF 言
角 d B 戊
e 罚
n
角 h ん
.
e h
、 y a
n

;
、 宁 e n 鸣
。 녘
a

多 d E 囪
日E
n



u h 阮 霉S
: 、 了
P
a 。
a
孚 u
e
h
a
S m


T
h
e
n
多e S

g
F m
劬 녀

a
V
垫g °

ぎn
4 S e e e
l 。 S - 0
4
。 の p U 歹 r
、 国 r
b 褚 g
h e 田 m
e
C
劈合 o
n
U
n 田 勺

C
h 阵 气
。 ロ g
a
= 。 e
S

§ 名 yh
S


オ d a
Ė 目P
n
a 「 「 e 》 国 n
p e

.
a 。 角 S 氏 巳
t
。 国 e コ 丁
B 。 n # g 相 낵
.


S


a
a 氐 n
I
b g e S 多 h
コ m 角 e
h ロ e
W B

f 门
。 的
a


式 h
h .
N
吕U .
e e n b
。 く e n ツ 4
.
n 刁 の c
b 급m

の 。 门 h
a

a

ツ a
司 自

ヨ す 国

n
n
.
h


n e
S

.
の 쩝 m e h コ a 。

ヨ 已 の U r
ザ : . 国 e
日 ロ
响 e

: e d 。

刁 m
.
.

艮 玎 日 e

n の . コ

m .
. ツ g

コ 》 V

m 印 a u

ツ の
n 巨 コ
艮 V ヨ
Ŝ 。 敌 c

e
s
u

§ Ŝ
一 h m 门
ヤ H
. 。 u 巴 e
f 으
吾 望d
. i 一 ロ

넉 コ b 口

따 一
く a の
。 e 门 r く
。 旷 の ひ b

。 エ
u 唱 っ 门
除 丁
n


s atesbindt(,li1BA 了 己
c

Scanned by CamScanner

IV H u id s a re u se O r l fo r m a in te n an ce o f b lo o d v o lu m e an d o p tim u m
ii
n e se
erapy
ssu re
p re

Ñ
ŜĤ
b e in c re a s e d b y in c r e a s in g u r in e n o w Fo rce d d iu res
can
e tio n
excr
T h d ilJ? e tic s 1ĵ k e
beca " I d o th e r tr e a m en t d o es n o t se e m t o b e e ffe c ı
ĵv e e

及苾茖嚣二万二二d f
ra re an
a a re
" ' " 。
Į iua

ÖiG%BTING BA R B I Tu R A T E s
ri b a r b itu ra te s (a c tio n 8 h o u rs an d m o re ) e g P h e n o b a rb ito n e

二二 ' " ' " û e m 二二 ご ' "ym


・ .
・ a
' " ' " ,。
p to m de

te n d e n ı
cy e a d s to b ?
jtu te s
ra
pohog s ig n s (P h e n o b a rb ito n e S o d iu m )
d s ym
X
an
p to m s :b b b iu e r íj j

deae
Tħe fa la J
c tm
p bm
aĦiffsm of
a re
wiraqpars a c t ion G A B A re c ep t or - on cha n n e l co m p l ex i s m a d e u p o f five sub un i ts
co u ap se d
T R E A TM E N T
O F P O IS O N
IN G
an
p a tie n t ŕimhëlmajor for m of the co m p l ex co n t ai ni ng a, , nd Y su b u n i ts. h e i ne sbe n z o d i az e p
O F B A R B JT U b r Ef
R A TE S an d b a rb itu r a te s a r e b e lie v e d to ex ert th e ir e ffe c ts o n c o n s c io u s n e s s a n d s le e p b y fa c ilita tin g
: iv jJĵ ß b ı
h. ĵ
th e ac tiv ity o f Y a m in o b u ty r ic a c id (G A B A ) a t v a r io u s s ite s in th e n e u r a x is G A B A th e m o s t

z
U ıs
ofharbljh'"tesin,edb y
E n d o tr ıc th e
p a tie n t
u b iq u ito u s in h ib ito r y n e u r o tr a n s m itte r in th e C N S r e g u la te s th e e x c 出 山 迅 ty o f n e J r o n s in
ea in h łb a ı łg e í Į » e
io n ln b a r b jh
r a te s i
ı
altibśťrvery n e u r o n a l tr a c t G A B A A r e c e p to m h lo ī id e io n c h an n e lh b in d in g
as s ite s fo r
n to x ic a ti c íħo s n 9 ĺ
on h e a tm ben d ia z e p in
en t a d eu n a 【e◆ z o es an d b a r b itu r a te s as w e ll a s a lc o h o ls s te r o id s an d iï ıh a la tio n a l a n es th e tic s
v e n tila ti
sho u ı
d be on is
ı u se d to tr e a t h p a tie r ıts i (E ig ilr é iļ J1 5 )
a ir w a

f i
ı yp o ven tiı io y

H. x
a【 n Ĵ v ijie o (Į :
th ,
p Ja s m a c o n

ä x
c e n tr a ti
ı
ea ds to w ith d on . .' '"
° i' '
ra w l a o f b a r b ih " bn 6 b Ðs fn o i ï
°- ・ °n rr a te s » b r a in
°' " om
" . '" : n r N ijn d n
' u se d fo r th i
s p u rp o s e
: d v H u id s U ė o C Tru q a ii
, r e m t d e hı d
P )ı h lr a v e in g b a r b itu r a te s
y ra u on ì Tvs D e
n o us u i ds are a 9 lb ì [ I
h e ıp
x l ro s e
n o r ma ı H ń u for f or c e d d

X
i tıre s i s t o
' "
X
' "
js u se d " ia9 ujb Jy
fr o m , '
.
a b İ u lł e u o n
N r

Ęt
n s
i

Scanned by CamScanner

T ES
A C T IN G B A R B r r U R A
sH O R T
P to b a r b ito n e
bar b it r a te s (a c tio n 2 to 4 h o u rs) e g B u to b a r b ito n e en
S h Q r t a ç tin g
u

d
e s c a lle d th e b a rb itu te s m a y b e w
n IJT Q Ę A R B IT O N E Its b e lo n g to a gro u p o fm e d ic in ra

te n s io n d in s o ın n ia I t is th gh t
o u
a s m ild s e
d a tiv e & h y p n o tic to r e lie v e a n x ie ty n erv o u s a n

B A r e c e p to ) c a u s in g th e r e le a s e o f th e che m ic a l G A B A "
to a c t o n r e c e p to r s in th e b r a in (G A rs

f t h e b r a in ltin g in s le e p in
7 i s :c h e m ic a l in h ib its c e r ta in a r e a s o r e su ess

ċ ÀBĮ Áį . ļ h ic h th e c 1 io n o p o r e is o p e n T he
'
e p to r in c r e a s in g th e d u r a tio n o f tim e fo r w

: Șaþ p r o lo n g e d A J1 o f th e s e
in h ib ito r y e ff' " o f G A B A in th , th a la m is Th e r e fo
«C u s re

n e u r o n al c d c iu ın
èi & :r e a s s o c ia te d w ith m a rke d d e cre a se s in G A BA se n s itiv e

Yį nce (g c a ) T h e n e t re su lt o f b a r b itu ra te ac tio n is acu te p o te n tia tio n o f in h ib ito r y


G A BA e r g ic to n e It a ls o a c t th r o u gh p o te n t (if le s s w e u c h a r a c te r iz e d ) a n d d ir e c t in M b itio n O f

J um c
Ð
i
e i c itätŁ
iq A M P A ty p e g lu ta m a te re c e p to rs re su ltin g in a p r o fo u n d su p p r e s s io n o f
J ul
g lu ta m a te r g ic n e u r o tr a n s ın is s io n
S id e e ffe c ts D r o w s in e s s Im a ir e d tr a tio n M
p co n cen e n ta l a n d p h y s ic a l s lu g g is h n e ss M e n ta l
co ń ħ1s io n (& T ra tftc a cc id en ts )
Im p a ir e d p e r fo r m a n ce H a n go v e r N a a D iz z in e s s
Id io s y n cra sy e x c ite m t P o r p h y ń a H y p e r s e n s itiv ity
en r e a c tio n s e g R as hes sw e llin f
g o

allo 1o o h 2 ooi
eg#ġs{jĘpş e tc T o le r a n ce an d D epe n d en ce
n
a ıiı
d 8 dalyjn th r e e
C o n tr a in d ic a « o n s
īc b Į】y
a e
q u a ıd o s e s
A c u te in te r m itte n t p o r p h y r ia L iv e r a n d ıcid n e y d is e Sev
mgpTkgbod'
" a se e re
: fc n ü ıa bjq
ig h t j
o r to t J
a d o se
H s (a t b p u lm o n a r y in s u ffic ie n c y e g E m p h y s e m a O b s tr u c tiv e s le e a n o e a
"
tw o e d tim p p
h a s in n et
o pm äF g】
e dos P h a l n ta k in e tic s
!q p la s m a p r o te in b in d in
g is 2 o % A n d m e ttib o lis m is
e Ie d * tio n e
re p o r te d h e p a tic

o nW J 0 0
- - - - W I y , O r t O t âa " °C . . ' ' " f' "
a j ' " n d ' '" m . h a lf lif. . " ' " r s
. ' "oin
' '" 1 5 to 3 0 o s e fo r s e d a tio n m a in te n a n c e (r
m o tıth
6m _ be ı
o re Htīĥ ilĵ
m g D o u tin e d a tiın e s e d a tio n ) t
g P er kg s, ĵ v a ī y
W ï ve
fg h tp e r {; i
ĥ jı
JTnoni
r e lie v e a rw ie ty te n s io n
p p r e h e n s io n 5 o to 1 o o m g d o s e fo r th e s h o r t te r m t r e a e n t f
o r a
, o

? y in t in
h r e e d iv i so m n ia an d is g iv e n a t b e d tim e a n d r e c o m
o
de d d o s- r r n
o iŔĵ Ji b n í m e n d e d fo r D o s e fo r
in d u c tio n an d reıie f o f p r e o e r a tiv e a n x ie t a n d i i
p r e p r o c e d s e d a tio n
p y s g v e n 6 o 9 m in u te s b f
e o r e s ıır e r
g y

自国画も 飞

Scanned by CamScanner

Ptwptic in h ib ito r
y e ffe c t o f G A B A in
e Ħe d s are a s s o c ia te d w ith m a r k e d d
e c re a s e s

characterizedj
o ıJ u ım r a t e s a ls o a c t th r o u
in h ib itio g h p o te n t o f le s s w e ll
n o f e x c ita to i A M p A ly e d a ń d ife ft
y p g lu ta m a te r e c e p to r s ltin g
su pp n e s s io n
re su in a
o f 8 lu t a m a te r g ic n e u r o tra n s m is i p ro fo un
s on d
U se It is u se d fo r th e tr e a tm t o f s h o r t te r m
en in s o n u tia It b e lo h e p a tic d is e a se
g s to a sm
H y p e r s e n s itiv ity a
n
c a lle d c e n a gro u p f
tr a l d ic in
COnàindica tio n s gN
o m
n e rv o u s
\ te m (a ų s ) d p r e s s a n ls th a t in
e
es s n e e z in » co u n g
du ce ? o w s in e s s a n d


lie
二二ぷ二兰主严 ご。二二 袞
re
P r o lo

v e te n n g
陣 y c a r d ia
' s
" ˜ . , '" 一 。 。。 e s ia ta c h
。 ' " s s io n r e tr o w a de a ın n

ł
ŕī n c
ł
i sp' '" r e s p ir a t o r y
d e p re

io n
l d is e a se liv er d is e a s e h y p o te n s
o th e r se d a tiv h y p n o tic M y a s th ia g r a v is a s th m a re n a

a d d itiv ffe c ı
e s An d o th e r c e n tr a l n e r v o u s s s te
y m d e p re ssa n b w ill ca u s
tī*i'wńprecautions en

e e s e Į p ¥ le to 1 2 h o u r s c ro sse s
ds s e n u ıt h a lf life n
m g / k g g iv s lo w ly tic s Iv o n s e t a c tio n 3 o to 4 o se c o n
en o v er 1 to 2 hou ph m aco k in e
rs m on ito b lo d P
re s p ir a to r y r a te
r o r
e s s w , ?d
U LT R A S H O R T A C n N d iu A n es th a l
G B A R B IT U R A T E S p to n e In tr a v a t so m
p to th a l T h ip m en
tn ı
r a s h o rt a d i B ra n d n a n ı(s T h io p e n to n e : In ie c tio n en
n 吕b a r b itu r a t
e s fa c tio n 15 to 3 o ın in u te s ) T h io e n t
T H Io W o p o n e M e th o h
e x ito A ġ 'rnix 50 0 m g ļ p0 0 m g v ia ls
N E $Q D m Jt js a h y g ro sc o
p ic w h ite p o w d e r w jth h
th a t
c a r a c te r is tic
o d d t d tio o f a c tio n
tic w ith a s h
o u r a n o r u r a n
in tr a v e n o u s a n e s th e
M ET Į Į Q Ņ E X ıT Q Ņ E 1t is A n

C þ io o re a t th e
d e p r e ss e s d in g ite a s s o c ia te d w ith a n o p
ıe s p ir a ü fo r s ho rt is m f tio It b in d s a t a d is tin c t b in s
n
tim b lo o d M e ch an o ac n
The
e
h th e C 1 io n o p o r e is o p en
p r e s s tır e fa 1】
s iı
ıu n e a a te ly d u r a tio n o f tim e fo r w h ic
a fte r jn je c tiä ıť / jË G A B A A r e c e p to r in c r e a s in g th e l n e d
c a r d io v a x tıl
lla p s e h b it r e ffe c t o f G A B A in t e
h th a la m u s is th e r e fo r e p r o o g
p o s tļ śy n a p tic in i o y
a r co
ııı
a y o cc w if th e r e is h
r g e n e r a l a n e s th e
du tio n IE is a v i】 v o le ın ia f th ūc
ra
a a b ]e yp o It is u sed fo th e s ia p ń o r to th e u s E o o e
as
500m v ia L
r a n a e s th e s iä
sho rt u e e d 1 t is u s e d fo r th e in d u c tio n o f a n e s
gm i th e r a p e tic
u
fo r s h o r t s u r g ic a l d ia g n o s t c
o r
C r e Jn a g e n ts a n d fo r in d u c tio n o f a n e s th e s ia d by
i L ittle a n a lg e s ia is c o n fe r r e
J Ľ

i t d w ith m in im a l p a in fu
l s tim u ı
pro ce d u re s a sso c a e I i d s m ild
f a in m a y r e s u lt in e x c ita tio n
t s a
ï ĥ r u J iď rí b a r b it u r a te s th e ir u s E in th e p r e s e n c e o p
n n ia
ie ty n e r v o u s te n s io n a n d n s o ı
i
ı rJViJct, s e d a tiv e & h y p n o tic to r e lie v e a n x

D o s e 6 6 to 1 0 m g p e r k g Im a n d iv d o s e l to 2 m gp e r k g o f b o d y w e ig h t
n , ) )

(n d o p e n ı
on e ıo dlu m )

r
Scanned by CamScanner
2 51$
s te m ı
y

2 5o ı rgĦ
rıaTextBookofpharmacolo[W

A Z E P \N E S
B ENZO D ı

'"
d ru g
,

s o
˜ w M . c tu r a lh r

f tħis g m u p a l e e lle c tiv e ı


ls T ħe d r u g s n itr a z ep m
二二二 ' "
r e a b n e n t o f u w ie ty
br ı
Ħ u r a z e p a m a n d d ia z e p a m
二 じ凭む二 :二暂芝芝
a l e u s e d a s n y p n o t ic ij
' " ' " U s c le
!

r e la J m n n ié
d r u g s d ia z e p a m d o n a zep a m a le u sed as an tic o n w ls a n
ı ts C h lo r d ia z e p o x id e is u s e d
as
s e d a d v e ln th e y e a r 19 6 0 D ia z ep a m an d C h lo r d ia ze p o x id e w e re Į n tr o d u ce d a s a n ti a n ĉİ e ı
i
y
d r u gs Tu o ıf O ĉ O

,
į " n o 1"
-

Q Ţ ĄZ E P A M ï r is lin e p o w d e r w ith s lig h t b itte r ta s te It is s lig h tly ś a a B ı


h ite a y sta 】
a w
ë i*
w a te r It is u y p id ly a n d c o m p le te ly a b s o r b e d w h e n a d m in is te r e d o r a lly It h a s
ıa

h a n q u illis e r p r o p e r tie s It js u s e d jn th e a t m e n t o f s c h o n e u r o tic d is o r d e . "


p y rs
nxiety
s ta tu s epilepti I ls m o le c u la r fo rm u 】 a is C 16 H 13 C IN 2 0

per day
M echa n is m
o f a c tio n I t b in d to a n a llo s te r ic s ite ı
su bu ib
o r m e d b y th e c le ft b e tw e e ıu à ï a

d th is fa c ilih tp s G A B A b in d in a n d in c r e a s e s th e ħe u e n c o f c iu o ń d
n d
Y tqeed g
n an
g q y ę cha n n el t d a ın n e s ic
u s c le re ta x an an
o p e n in g B a r b itu r a te s b in d a d a c e n t to a a n d
j p s u b u n i1s a n d in c r e a e th e d u r a tio n io ly tic s e d a tiv e m

c h a n n e l o e n in
c lo de 0 h ú Į I u se d as an tic o n w ls a n t an x
en t o f a lc o h o l w ith d r a w a l
p & r a tio n f a c tio n It is u s e d in th e m a n a ge m
r tie s a n d a lo n g du o
p ro p e
P 1a c id o x C a lm p o se
P
B ra n d n a ın e s D ia z e p a m T a b le t C a p s u le In je c tio n V a liu m
1
2 m g 5m g 10m g In je c tio n
10m g p er 2m
D ia z R e p a m
D ia z e p C a lm ta c k

ly lil n in te d d 】U in
d ia z ip in h ic h it is s lo w e a
ņ p A M i t is a dru g o f c la s s B en z o es w

w h ic h a c tiv e m e ta b o lite o ccu rs

d e p r e s s io n a t th e lim b ic th a la m ic
M echa n is m o f a c« o n It p r o d u c e s ce n tr a l n e r v o u s s y s te m
) in
d ia te d b y th e n e u r o tr a n s m itte r (g a m m a am o
d h y p o th a la m ic le v e l o f b r a in It is m e
an
tio n a n d h y p n o s is
s c le s r e la x a tio n a n x io ly t c a c
i
b u ty r ic w h ic h r e s u lt in th e s e d a tio n m u
In d ic a tio n s a n x ie ty s h o r t te r m a n d tr a n s ie n t in so m ia

D o sa ge O ra u y 15 to 3 0 m g a t b e d tim e

T Om V C on tr a in d ic a tio n s M y a s th e n ia g r a v is H y p e r s e n s itiv ity g la u co m a h y p o te n s io n


O m v
(H y p e rp o ı
a r lz e d ) tin
Ħ& 4 1 6 M
S id e e ffe c ts : D ro w s in e s s dru g depen den ce b lu rre d v is io n u r in a r y in co n en ce
e c h a n ia m f a cd o n
o o fben z o d ia z e p in e /B a r b ih ir a te s a n d G A NA
T ħe B r an d n am es C a p s u le N in d r a 1 c o n ta in in g 1 5 m g F 1u ra ze pam h y d r o c h lo ń d e
res tin g m em b e r p o te n tia l is TO? V b
e n z o d ia z e in e i
8 0in v ıJia z p n c r e a s e d th e m e
m b r a n e P o te n tia l IßiJn Ŕ Jo q f
ep a m p o te n tia te s th e a c tio n o f a m
m e d ia te d b g m a a m in o b u t i
y r c a c id Its a c tio n s a r e
y e n h a n c e m e n t o f g a ın m a a m i N ırr R A A EPA M 】
n o b u t T ic a d d
} a c tiv it
t is u se ħ】1 fo r p a tie n ts h a v in g fr e q u en t n o c tu m al aw a k en in g s w h en day
fn d ic a lio n y
S e d a tiv e ı b r s u r g ic a 】 r o c e d 山 山 9 e jın iJ tim e se d a tio n is a cce p ta b le
p u r e s a n x ie
u te n s io n m u s c le
a n d b e h a v io u r d spa sm s y c h o s o m a tic M ėt h a n ie ih f
is o r d e r d s m e n o ır h p o ac «o n It d e p r e s s s u b c o r tic a l le v e l o f c e n tr a l n e r v o u
y e a c e r e br a l a l s s y s te m in c lu d in g
p y la b o u r te ta n u s e c la m s ia d
p Je t a J ic lm u l ı
u m bic e y s te m an re tic u la r fo r m a tio n U s e fu l in s o c ia l h o b ia d e
p p r e s s io n

Scanned by CamScanner
l = . '

' d ic a tio
? n s tn so m n ia tr a n s ie n t s le e
p d is tu r ba n ce
r E
c o lo q o f A c t in g o n C e n tr a l N e rv o u s S y s te m 1

D o sa se 5 to 1 0 m lı
g o ra y a t b e d t im (b e io r e g o in t to s le e p)
e

C o n tr a in d ic a H M w
?ãì o m s th e n ia g r a v is , n a rr o w an g le g la u co m a

å c t= sw e a tin » w e a lc n e s s ? y m o u th b lu rr e d v is io n n ig h tm ares b ĮX Ĺ
B d N itr a
ran n a m e s z ep a m c ap su le s ta b le ls D in
o rn ı N in d r a l N ib a v e t N itw a n
ľ
A LPR A Z Q W 1 t is a u ia z o le a n a lo u e o f b
g e n z o d ia z e ín e
p I t js e ife ċ tiv e jn
h ?J l ıb ・
- M y a l' '" n i, g r a v is Respiratoryinsuf{iciency,premani'
actation

d is o r d e r s a n x ie t a s s o c i
a te d w i th d e r e s s io n
a n x ie t
y Z Z o liu n ı Z o p itr a n
y p , Z id o n e o n a
p Z tic , L y z o
Z o p ic lo n e T ab Z o p iv an e o
,
M e c h a n is m o f a c tio n It d e r B ra n d n am es
p e s s s u b c o r t ic a l le v e l o f c e n tr a l n e r v o u s s y s te m in c lu d i
n g
\ te m a n d r e tic u la r To z m a tio tL 1 t is u s e ń ıl in s o c ia l h o b i d b ic
7 śffiġ e ib le ts
p a e p r e s s io n
D o sage a ra d y 0
l
tu O 5 m
g th r ic e a d \ m a x im u m 3 to 4 m g p e r d a in d iv id d
ħo u r ly y e do ses 8
d fo r 1 to 2 e e k
ia c s It is to b e t ıs e
g e d in im so m n
is p r o lo
Ci th e s le e p du ra t io n n

b ic th a la m ic
C o n tr a in d ic a tio n H }p itiv ity r v o u s s y s te m
d e p r e s s io n a t lim
g le g la u I t p r o d u c e s c e n tr a l n e
s e rs e n s n a lr o w a n
a c i d an d
co m
E ld ly D ho ld b e
a
M e ch a nis ın o f a c « o n
o t ra n s m i tter c
À A am i no b u w c B
d s. t is m e d i at ed by ne u r
er o se s u d
t c o m ru ls a n t
re u ce
l ev e l
. :r J
q y ı[ b n hy po t ha l mc i c tio n a n d a n
i
S id e f fe c ts U
nd
s c le r e la x a tio n
h y p n o s is a r u đo ly t c a
e r o w s in e s s a n o r e x ia im p a ir m da t oi k e le ta l m tı
h e a la ie s s
m em o ry en t lo s s o f coordinatiiéd q u ş is q
n s
ia
W e ec w
p ru r itis i ıİ It i ń r l in tr e a tin g in so m n
a c tio n
N o ilĮ s u s e
c
B ra n d n a ıı
ıe s A lp ıa z o la m T a b le t A ]p r a z o Ja m A ı
z jp A ı
z o Ja m Q t ıíe Ļ R ty l A ilu tie n t 5 m g H S
E ld e r ly a n d w e a k p a
es ? m
Ą iz o Ļ A lz a n 2Ptra Z b ld a c 0 2 5 m
& 0 5m g l m g ta b le ts By th (o ra lly ) 1 o m g b e fo r e b e d tim e
/ ĺ D o sa ge m o u d ep r e s s io n
r e s p ir a to r y
I
he ot he r dr u g thi s gr o u p liv e r d is e a s e
s of ar e T e m a z e p a m , n a z o ıam , wd a z o ıam . Wd a z o J am ĵ s t hr e e ,cońträindiations H y p e r s e n s itiv ity apn ea

' " t " \ a m a n d js ııs e d ín a n a e s th e s ia o o 2 "


Im g p e r k g p e r h o u jy
h e s t p a in ? o w s in e s s am n e s ia e m b o lis m co n ń 1 s io n Dry m o u th

S id e e ffe c ts H ea d a ch e c
Ţ h e r a p e u tic u ses o fB en z o d ia z e p im
iiq o lc ib L y p in So v e So za
m e se d r u g s a r e u s e ń ıl th e r a e u ti Jt Z 1e e p , A m b iz D a c tiv e , ,

p c a y a s a n ti a r w ie t
y a n d s e d a tiv e s a n ti c o n v u ıs a n ts B r a n d Įm am es lp id e m
Z o C a p s u le s ı T a b le ts
m u s c le r e ı a x a n ts a n d
p r e a n a e s th e ä c m e d ic a tio n in a n a e s th e s ia Z o ld e m Z lp id 5 m g 1 0 m g ta b le ts
:(ıS r n g b lo x o
A d w n e e ffe c ts B e n z o d ia z i ín e s c a u s e li h
p g t h e a d e d n e s s, ı o s s o f c o o r d in a t io n a ta x ia
c o n fu s io n ffe c tiv d is
d r y m o u th W e a k n e s v t i i id in dru g
ł
t i e an
,
s e
p yr a z o lo p y r m
e
er go b ltır r e d v is jo n d ia z e p in
jo in t p a in o m it i p g a s tr ic
i : It is a n o n ben zo e

Stress
v n g e
B e r ız o d j z i in e s a r e r ,
p a r e y h ta ıjn a rg r d o s « a d are a t v e Jy s a k d r Ľ M
trazepam s o m e p a tie n ts e \ r ie n c e n ig h t m a r e s a n d b e h a i » d ın in is te r e d fo o n e to tw o w \
sho u ld b e r
ıýiaėį nd It a
ır c h a n g e s w ith muscle r e ta x a n t a c t io n
s w e a t in
g w o c c ıır T n a z o la m ta k i
v o ı
, \ H ļ # d d iffic u lty in fa llin g a s le e p
n g p a t ie n t e ts u
g p e a r ly morning a n d t ee ts u n ęș g ¢ irıb duiiHó£
f[iŕ p a tie n t o f jn s o ın n ia o r p ĉ tie n t fın
In d ic a tio n s S h o r t te r m tr e a tm e n t o f in s o m n ia

k p a tie n d tim e)
d a y ) E ld e r ly an d w ea ts 5 m g H S (a t b e

Scanned by CamScanner
Çņ l @ w Į ły
d r a t f s a h j n o tic a n d s e d ti
p a v e
s a fe ty m a ıg in
is to o n a m o w fo r h l
c o r a l h y d r a te to b e
b u t it is c o ııu n o l
n y u se d ı b r th a t p u ı o s e Jn a n im a l
p la tiv lo se
p to 3 m g cu m u e
lo f1 m in u te u
u s e ń ıl a s a n d s i a t in te r v a
a n t i e t y m e d ic a tio n :s e c m
b la to r y p a tie n ts
y la c ta t io n a m u
H yp e rs e n s itiv ity p re gn a n c
tr a in d ic a tio n s
M ELA T o N ı
co n
fa t ig u r ig o r s d iz z in ess a g ita t io n ,
N R EC E Ħ o R A G O N ı H da che in cre a se d sw ea t in g e
sT ffe c ts ea
is io t in n itu s
s id e e b lu d
. v n
h . " pai ^ h yp e r te n s io n pa lp ita tio n rr e
It is th e fir s t itin g
XS j
c
s e le c tiv e m e la to n in a o n is t I t ・ ・m
. . M n o l. . .
. . . ..
g w o rks by m im ic k in
g . n in oj c [9 r n
be r e s p o n s ib le
fo r th e r e g u la tio n o f d r c d i n 3 J r fg u o r
tJ ,
a n r h th m ıın d e r l in
LA X A N T S
a
y y g th e n o r m a ıs le e p w a k C LE ?
c y c le It h a sM g h a ffin it fo r th e M T
a
y ï a n d M fz to r s T h e M T a n d JW
e ıri H q ÐÐlf 4 8 C E N T R A L L Y A C T IN G M U S
lo c a te d in th e b r a in ķ w z r e c e p to r s a r e
e
s u p r a c h ia s ın a d c n u c l i s
Cï ock" b e c a u s e it r e u ta te s th 2
e ( a v w h ic h Js la ıo w ıı a s th e b d
y ! M i ch ac ce n t ra l ne rvo t i s sy s t em ( cN s ) an d de c r ea s e sk e l et al ı
nu s cl

g e 4 h o tır s ı e e p w a ke c . e n h a s
o te r lh ë &' r ė' he dr u g s wh t on
t f a c u te
y a n a c tiv e m e ta b o l T hese d ru gs a re u s e d fo r th e tr e a tm en o
le s s p o te n t b u t c ir c u la t i
es n M h
jrę tï ıą ţ Js ióĥëJiítii iinv o lu n ta r y m u s c le m o v e ın e n ts
g e r c o n c e n b a d o n s th a n th e p a r e n t c o m o u n d T h hi
d te ta n u s T h e d r u g s b e lq n g s to t s g
ro u p are
a ls o h a s w e a k
anryıor tħe 5 H T ž B r e c e p to r
p e
pgtaolite itġ ĉ lë§Èra s m o r th o p e d ic co n d itio n s a n


' s

M e c h a n is m o f a c t io n Jt is a m e la to n in
r e c e to r a
ıD T , a n d M T ir e c e to r s
p g o n is t w ith b o th h ig h a i [in ily ıb r m e Ja to n jn
A n d ı

HjĮ
p o w e r s e le c t iv it fo r th
y e a r e c e p to r M e la to n in
c o n c u r r e n t w ith n o c h
ım a J s le e
p r o d u c tio n is
p m e a n in g th a t a n in c r e a s e in m e la to n in J
th e o n s e t o f e v e ls is r e la te d to
a tiv e
sereported s le e p in e s s a n d a n in c r e a s e in s le e in (D B e n zo d ia z e p in es (3 ) G am a a m in o b u tp ic a c id d e r iv
be ı ie v e d to b e r e s o n ib l
e fo r r e u la tio n o f J
p p r o p e n s ity M T ] lle r ĉ ä o $l M $ co n gen er

p s
g s e e p in e s s a n d fa c iJit ti g B a c lo fe n
e g D ia z e p am
M T z r e o e to r s a r e b e ı a o n o f sı e e p öh s ť ä ī td bę g M w Ęe n e s in e
p ie v e d to m e d ia te h a
h iftin g e l fe c ts o f m e la to n i 4) Ce ra l o2 ag on i st
p w n o n thecailiàn c】ilorz)«azone (
nt
r h y th m Vħıle A n ï a n d A dT z ıe c e t
com pı
p o rs a r e a s s o c ia te d w ith th e s Je e w a k e
p cycleMTĵ ,h a s t a E h 1ó r ilib ż a n
e g T iz a n id in e
e te ı d
y ille r e n t p r o liı
o n e
e , a n d th e r e fo r e i
s n o t lik e l
cy c ıe y to b e in v o lv e d in th e . slęprwdce ņ lhėthabamol
ıt h a s n o a
p p r e c ia b le f lin ity fo
C a r is o p ro d o l
a th e
r
gammaaminobutyric a c id (G A B A ) r e c e p to r co m p le x o r
neı
ır o p e p tid e a ,

X Į e X e =
c y to k in e s s e r o to n in d o p a m in
Ê 5 1 t ¥
o r e p ín e p h r in e ,
acety"hotine, ' " p j ' "
, e, n

. ,
U se s Jt is u sed fo in s o m n ia
& À
r
p a r tic u ı
a rı
y deı
a ye d sı u b le in
ı It is th e ld
e e p o n se t R a m

rıihëř lig h tly a te r d e x te n s iv e ly d d g It
,
sho w io p r o d e lte o n B d o u r le s s s so w o an u se ru w a s
n u ce d epe n den ce an d has sho w n n o
,

p o te n « a l fo r a b u se
th e lir s t d r u g fo t ın
d to c a u s e m u s c le r e la x a tio n w ith o u t p r o d u c in g u n c o n s c io u s n e s s It h a s a
\ıT h le r il ıu
ı
f t s im ila r to p r o c a in e m q p h e n e s in a t v e r y la r g e d o s e s p r o d u c e d e a th
lo c a l a n a e s th e tic e f e c
l !ıť ) r r [fi ĺr n i

Scanned by CamScanner
ı

256 1 r題田园 T e x tB o o k o fp ha rm a
ı 7
ac o
lo g l o fD ru g s A c t in g o o c e n tra l N e rv o u s S y s te m 1
S ı

ha em o ly s is a n d h J p o tm s io n c c
n
ti g s k e k ta l m s e le r e ta x a n t its s tn ıc tu r a l fo rm u la is as m er

U st a It is u se d in c re a m s fo lo l W o
T ca a p p lic a tio n s M e ä c re m e o in tm t M
NH 2 co o c H 2
en e phen e s in has ıT ī ,
! rl

su h w m a y p ıe v en tin g

£X i ï H Ī įiL .
H Y
° x d X H

le r g ic r M n i ıt is u se d a s a n
o p h th a Jın ic
s o Ju tio n to tr e a t c o
j
n u n c tiv itis d ís
an
\ e

jn eu q a ıd iv id e d d o s e s M D ru g in te r a c tio n
H ï
th r e e H m e s
o ra lly 2 o s
g p e r kg
bo.Tşgķt
o or m
" ' " " tri'"】
ic
MEiileþ
iģijśhs
a day '" "
.. ..c . . .. ..
B ran d n am ea c a ń s o p r o d o l T a b le t s
o m a fla m c a r is o m c a r is o m
a a co m p o u n d
ł
h
1 £a « a s a

Scanned by CamScanner
\

S ld e e ffe c ta f c h lo d a tiv b a rb itu ra te s


o rm c N s d e p r e s s io ith a lc o h o l n arco tic s se e
e za n o n e D r o w s in e s s r a c tio n In crea se n w
n a u se a kn d Ĺ z z in 吕in te

X m
w ea ess e ss ħe a d a c h e D ru
ly IM
ï .. _ s io n w ith A lc o h o l a n d o th e r c N s
depșts,
D B e p a in :
o sa

5 0 0 Ėiġ 9 1U te a
l m
A d u lt 1 5 g m o r a lly 4 to 6 h o u r ly fo r 2 to
u s c le s 6 h o u r ly
3 d a y s T h e n 1 g r a ın 6 h o u r

X
B ran d n a ın e l
W . _ e r e ta x a n t B u t ba n th r o u gh o u t th e w o r ld
uęi tq :
' " ." M '' "
i "
T a b le t R o b in a x R o b in a ın F 1e x in o l Ib u g e s c
F 1e x in o l

m lo r m ezan o n e T a b le t M ez o n a c D ilo fe n M R o n ta c fo r te p a m a g jn M R ñ lv i n
Q l I t is a w h ite a y Ta lı
in e P
D (G A B A
G A M A A M IN O B U T Y R IC A C ı )D E R ı V ES
VATı
o w der s o lu b le in w a te r It is le s s se d a tiv e

u l īu s e x
p e r ie n c e ń is d r u
g w a s s a fe a n d fle c tiv
e th e r o f l c e r o L
e e It is a m o n o ca r ba m
g y a te e s te r o f tĥ e gu a ic o l

(M E u Io c A R B M no L) iĵ
M e c h ın ll m
? a Ðn ßÐN kn It is le s s
o f ıc tł
on
w ea e ss se d a tiv e th an d ia z e p a m It is e ffe c tiv e in n eu ro lo g ic a l d is o r d e r s lik e
J t d e r e s s lb ı
p ocL p
9[ilı
ır .
m u ltip le s c le r o s is s p in a l in j u r ie s It is n o t e ffe c tiv e in s tr o ke c e re b r a l p a ls y r h e u m a tic
m u s c le r e la x a tr a u m a tic M u s c le s in ffe c tiv
tio n jĖ U n k n p a sm s e e in th e tr e a tm en t o fp a r k in s o n is m
o w n It h a s d ir e c t
n
s ia te d u s c Ie
n o
tio n M * dh iħl!n
m th e m o to r
ac On th e C o n tr a c til i o f a c tio n B a c lo fe n is d ir e c t
endpıa o r th e e
mec hņi §m f
a a go n is t a t G A B A B rece p to r s T h e p r e c is e
em e ĥ be r o
eċ liäiü§o f ac tio n o f B a c lo fe n is n o t 6 0 1y kn It is
r eı
ie fo fs § ĥ ır e o n r ım
y
o w n ca p a b le o f in h ib itin
g b o th
p a s ın
an d
p a in in ın u s c u lo l D is e a s e
s ce le ta l c te ta n u s
T e tın uı A duı o n d itio n s
t r v jn iu s jo

to3gmperurofDnottoexceed3gmperday
n :ıu 119 lß» İ u iJ J
c lin ic a l e ffe c t It in h ib it
s y n a p tic re sp o n se s in th e cen tr a l n e r v o u s s s te m
w jn c ıo 【rif r¢s in b u ty r ic a c id y by de cre a s in
am o
w hi h d c
g g a ın a
e c re a s e s n e u ro tr a n s m itte r ftın c tio It d
ĥ rJa b e u ııt m u s c le s a n s e c re a se s s e n e r it f
p sm s y o

l l
˜ 彆盞覊舞 籤鼗籲縈 妞議 豔 。
Z Ĥ

Scanned by CamScanner
rr u ilA Te x t B o o k o f P h a rm ĝ C o ı
o
Y °a
ı
= m ' " ' " ' " ' " . ' " b ra t o r ig in s p in a ' " r d
it ıjlı
ty

D o sa g e

rí?
A d lt m lly 5 S ?
u a m g 8 h o u r ly fo 3 d y s th 10
!i }
g th r ic e d a ily × 3 d a y
r a en m s th e n 15 m
d a iı
y To r th r e e d th e 20 g th r ic
a y s n m g th r e e t im es a d a y fo r th r e e d a y s d q s e n o t to
e
e x ce e d 80
pe r d a y m g

C h ild o 7 5 to 2 m k g in
g p e r e qu a l d iv id e d d o ses th ree tim e s a day :J

C o n tr a in d ic a tio m H yp erse n s it iv i ty
S id e e f fe c t s S ed a tio n n a u se a
VOmittin res p ir a to r y d e p r e s s io n d r o w s in e s s H e a d a che
tr e m o rs D is o r ie n ta t io ï co
n n » ç n n g e s tio n B lu rr e d v is io n tin n itu s h y p o te n s io n c h e s t
d p a in
o e em a c o n s t ip a t io n In A 石丁 (S G O T ) llm
c re a se a e p h o s p h a te d r y m o u th a bd o m in a l p a in
s 】
c in ra s h p r u r itis
r !ri llb w p f
Ph a rm a c n k ïn e t ic s O lr a u y p k tr a t io n 2 to 3 h d
ea se ru m c o n ce n o u rs u r a tio n ofaction8 h ó 'u r s
Seru m h a lf life 4 h o ıu s n ıe la b o liz e d ín ı
iv e r e x c re te d in u r in e :n 1 İ
/
r :r !

b a r b itu ra te s te n s io n
an c y h yp o
! u rĵ [o j o tĦ tio n s in p re gn
ity w ith p re c a u
n s itiv u se

' X y u =
,e

ife
h a lf 】
p la s ın
・ a
, tr a tio n h o u r
d '" ,' " p e ak c o n cen
e p re ssa n ts
H ' .' '" o m p l' '" .

= =
," . . "
d in u r in e fe c e s
e x c r e te
T a b Je Ļ ın je c t io n R ic lo fe n c h in o fe n L io k n L io r e sa l 1 1H q 5 l o liz e d in liv er
l c o n tr a c e p tiv e s d ecre ase
. L !ı
ith A lc o h o l o ra
d c N s d e p re s s io n w
10g. 2 5 m 5 o m g ta b le ts In c re a se
D r u 吕 in te r a c tio n
di
tio n o f tiz a n i n
e
ac

by in c r e a s in g p re s y n a p tic
d re s m ab l e du ces s p a s tic ity
b e ta p d fF lo 7 to 1 5 d a y s s ite s a n p
e re o r
» ig rg n y rb £
a d re n er g ic rece p to r

A v o id d r iv i n g a n d w or k w ith m a c M n ely, a s ? o w s in e s s o c c ıır s in h ib itio n o fm o to r n e u ro n s


u f rn İ d ir
jı l lj
h' " V
T o av o i d us E of c ou g h sJ T u p s . n t ihi st am m e dr u g s wi th t re a t me n t un l es s a d v
(
:
by d
D o s a 吕e È. inf ul m u s c les p a s' .
11
d o c to r
z lu fo r te , N e ls id
T a b le t N ic ip T T i z a m
u
To ta k e m o re H u id d ie t u p to 2 h ir e s p day (a d d itio J) ith fo o d Io a v o id z a m ı
er n a w
T iz id in e T a b le t T iz p a
B ra n d n am e s a n
tip ati on
M R ta b le ts
T tm tof do Jn p ı1íd ıij Ï P/
r.ee a en o v er ae c o n s c io u s p a tie n t in d u ce em e s ís la v a g e

Scanned by CamScanner
#lì n* . ° °・
ı IEB ZIı
=T e x tB o o k o fP
harmacoı
医回A N 丁Į E P琵EP T ı
C 回国回国目 나 ır " 1l i
。 an
A n tic o n v u la a n ts (a ls o ly kn
co m m o n o w n a s a n tie p ile p Ł
ic d ru gs o r a s antjse
a)
b r a in th a t c a u s e s s e iz u r e a c tiv ity s u c h a s in e ile s
p p y J

is n o t k n o w n
tic a c tio n lu is h n e s s , - _ - ' " - _
q ĵ uii iCqsîUJn a n tie p ile p ic a lly in ċ 1u d e s g g sh a llo
o v e rd o se o f p r h n id o n e ty p in e s s o r c o m a
w
ffe c t dr o w s
A dv en e e ch fa u lty ju d g m e n t
s lo w n e ss o f sp e e
th in k in g
.
M 7 A s y s te m a tic d ia g ıa m Im b a la n ce b e tw e en e x c ita tn ıy a n d in h ib ito r tr a n
y s m
f
ittÈ u ĵ ìtìil,
/ d iffic u lty In

1
)
in h ib its g ı
u ta m a te in d u ce d d e p o la r iz a tio n s 1 te ta n ic po te n tia tł
o n pre v e n ts
M e c ħa n h jm o f ac tio n ı
t acı
s on G A BA A r e c e to r s in inrl irİ T it :
p c r e a s in
g s y n a p tic in h ib itio n T h is h a s
n o

s e iz u r e ı Jt
o cu s m a y a ls o in M b it c a lc iu m c h a n n e ls r e s u ltin g in d e c r e a s e ĵn e x c ita to r
, a y

Scanned by CamScanner

Ę



七 宇 团 ◆
盘 反 。 甘
富 芎 段巳
叼 ゼ

ぼ ' 口


h 角




h


.

w

-

佇 : 日

田 吕


: 氏



ロ 宁
龆 :
コ 口 营
b
:
了 如
: 屋 日
:

b
:





牛 \
ロ コ
ヨ ı
e

自 加
U ロ


e
e 多

h d X

"
ヨ 国
U 中 。
コ 。
e
h
导 万


b 歹
回 コ
:

ひ ヨ





;;:;;;; 리



F

臣 dA
h
万 b m n n F n


» l h U
o u

怀
m u a u e U Þ e e
n 障 n m u


Ĥ 一 v a
= S
:
遐m 凹
e e e h P e u
0
m m a :
n u
P a u
> L n a


Z
一 e n u e
a 口
虞 벼 n N
苜 u e m
S
Z
習 皆 e
U
a
n m d
P
U
þ 5 e 会 ;
o h
田 n e d 目 e 一


d h N 勺
w e e S コ V
썹 P 口
c
n
U
h
e
n þ m 腎 ロ 旧
e

。 d
e
U e m a
e
k y g
/ N

ロ n


m
a
售 ロ
召 T h u

c
T
m zm ヨ
U

P プ
h e z
u 4
C
h
m h く Ð
叫 n
4 P e
b
m
S n a u じ / 叫 d ロ
e e U U a h
罝 껍

m
P
n
e
u
n n e
e d n
n
n
U W
U

.
.
F
n ロ n
d
C e
n e 5 근

@
e Y C
邑 . n
a
印 u 々 낵 . e b e 口 0 c
ロ y e 寧
・ d
u a ロ U P
. 0 k r
c d
n
e s
n 3
h
邑 s
U s a e
e
a 2 o
日 且 叫ヨ
.
섭 C
U H
U
a a
C
k b a 多 . 口 Y U n v

. h m I n e U n W x 中 e n 6
S r r
e n n
C
y U d プ U
r U e d = h g » d a y .

腎u
a 门 P
u C q m b
h U
r
e
n 闭 口 U

c C
s
水 コ
e U U


m h
N e
F
w
u
n
n =
n
h
e
q 0
접 껍 e
v

9 Y
P
a
n m S 。
b .
e 歹 n g
c
a h S o
U
e
W 區 口
.
.
n e d


e h S
e e
n n
U
0 e m A n コ
コ y
c
C 田y 4 n
U s r
n u C U

. 口
n u A
e g 艮 & 日 门
弘 . 1
. e S
m
U y b っ R 良 n m g
u e u 6 e a m
e
d
d e 歹 g d
e
弘 u
C
u
c e a


p n 》 b d n S U ツ
n ? n h U
»
e ロ
m c a 日 Y e n
e S 川 s u m P W P /
m P U

口 n ロ

e
r
c o e
d
H
y e n h
口 ロ 4 e
p

づ h 2 u u

A e c a
q
子 a
P 困
v
e .
r e U m I
e
n
d
m
e
n 3 ヨ 邑 e c
の u
s
C
9 y
C


n
了 & n
» e
s
n
n
p e y 》 叫 d n
歹 h 0 口

ヨ e a P s » n P 口 s a
2
印 u
k
S 田 a u
n
e
m
C
h
&
e
e
昏n
U
m

邑 e n e
v
n
d
e S
售 e
田 d o
e o く ダ v d h 낵
0 u
C
v
m
S
n v
U e
3 . e 田 e
C e
C
C
W
p
e
a
n § e
r
p
u
m
e
V
a
r
C
e
U
o e
5
e
S P
I 由 以 C e 角
a
Y
r
p
a A ン


n e 困 s
e . a d q & n U 々 召
日 n
a 》 d 2
P
甚 く

W a m の
n
p
o
I
e d s
e m C
c
a m
ゆ I n P r 鹵 角 s 丁 石

y
a 弘 e e n
I

n
r
e
b
U g e
h
e U

/ 昆 d く g 1
9 y
c


a n n g 已 s C ヨ
n
m
e
u a c
a
n q
g S
e
S
..
u d b m
m 邕 ロコ e
u
c 녘

k g 田 b m e l h
佇 v h a 困
u
I

u
n
c
g y b
U
m »
a
c n
a S .
1
e H S n 冒
a n e
日 旧 8 口 y u e

c
Ë y n s p
5
e 9 d
m m
注 U 口
口 u g b a
n U F n
o a
n h 田
日 F 旨h n e e
n u
s U 口 p e 5 U C
p d a 0 H o a
a

路 u
e 口
艮 C m C r 信 叫 p
n » b b
s y o
k ! e V C 口 へ a 日 u 4 国
W
U

c a n b S
» e e a h 才 。 い e 낵 5 H
e e a n u 巳 u s
S u g e
す 岂
c
目n ¥ t S
C a s じ r e
W

s s u m g e u & n a 自
口 弘 n u e
a
e h H p n 体
彥 n
u p 9 s
e e
U
n ņ s -
S
e e 胃 叮 p 可 &
p c
r
&
内 p a く u m n s
e z
a
t
。 u
.
u s 召
n 口 & o
m 巴 1 e c m s
h c
巨 e l
9 P u
i 8 첩
m
m 角 e a u 8
召 e e e a
y . m p h
e
s e n e
n 饷 e
W

l m n


e s 。 n
a e m m e
& 日 9 內 h a &

.
n o y
》 p a & t
m H e l
e
図 m コ s 弘 c
の a 叫 b n
e p w
ーu c e e s
n n e H
H B u
a ydingthe c
已 e 口

Scanned by CamScanner

黄 弦罐
難霧 贓

秘 繃
バ 嘩 。 葚
Ę

. g

(s o d iu lp r o a te ) I t h a s tic o ls a n t p e r tie s d in th e
A c ID u se

pROIC m v a an n v u ro p
tregnent o f e p ile p s y

ac H o n t di ss o c i at es to the pr o a t e ion in the ga s t ro i nt es t ina l tra c t an d the n


ċ h ın l lm I va l
t of

d in h ib its G A B A tr an sam in It in d th e b r a in c o n c e n tr a t io n s o f g a m in a
b ń d ś to an a se cre a se

a īn in o b u tjn ic a c id (G A B A ) an in h ib ito r y n e u r o tr a n s ın itte r in th e C N S d u e t D


,
in h ib itin g

e n z y ın e s
b lo c k th e reu p ta k e o f G A BA in to g lia a n d n e r v e e n d in g s It m a y a ls o w o rk b y
in g p e titiv a l fir in g th r o u h ls
:
re e n eu ro n
g h in h ib itio n o f v o lta g e r s e n s it iv e N a c an n e

: rh a m ıc o k in e tlc l It is w e ll a b s o r b e d in to th e b lo o d s tr e a m w ith b io av a ila b ility o f 8 1 89 %


th ep e a k p la s m a c o n c e n tr a tio n is 2 h o u r s It is h ig ld y b o u n d T o p r o te in in th e b lo o d T h e
yolue o f d is tr ib u tio n is 9 2 L A p p r o x im a te ly 3 0 5 0 % o f th e o r ig in a l a c tiv e in g r e d ie n t is
ecqętęq in th e u r in e a n d th e r e m a in in g m a jo r ity is fir s t m e ta b o liz e d T h e o v e r a u th e
c le a r a n c e o f th e d r u g r a n
g e s fr o m 7 1 6 h o u r s
A dye n ¢j e ffe c ts The to x ic ity o f v a lp r o a te is lo w A n o rex ia v o m itin g h e a r t b u m ? e
1 Ç0 l m q ņ . D r o w s in e s s a ta x ia an d tr e m o r are do s e r e la te d s id e e ffe c ts H ow ev er c
g n itiv e o
m ◆ıþ ę h a v io r a l e ffe c ts are n o t p r o m in e n t A lo p e c ia c u r lin
g o f h a ir a n d in c r e a s e d b le e d in g
eq d ę ņ ç y. a v e be e n serve . a s h e s an d
ob d thr o m b o c y t op n i a ar e inf re q
lp h ę ņ p m e n a
e u e n t hy p e r s e n s i ti vi ty

D Ose Aduitstart w ith 2 0 0 m


g T D S m a x im m 8 0 0 m g T D S c h ild r e n 1 5 3 0 m g /k / d a
s e iz u r u It is d r u g y
es u n a
cc o m n u jıij i!
ıe a
g o f c h o ic e fo r a b s e n c e s e iz u r e s M a n ia a n d b i
p a n je d l rr ru
lith iu m p o la r illn e s s a s alternative t
M e c h * n iı It h a s s o m e o
m o f P r o p h y la tic e ffic a c y in m ig r a in e It is u s e d
s e its iliv
*cHon
Į t is b i in m y o c lo n ic a n d a
e ca ı n d s lo
c iı
ıtn c ha n n ı T w e
e s 1 v o lta
are aı
so
jnvoJv z n e d ia ge
s e n s iti
v e ca ı
so m e
p r o p h y la c tic e ffic a c y in ig r a in
ĵn a v a te th e c iu m m e
r ie t en hy o fc cha n n e t


ı
nentwilhoutaffe"cgotherweca2ependent o f caı a lc i v o lta e
s
c iu m u m io n g
s in to
e x c ita b J e E ŃZò o ı
Az Ep ı
NE
' " p ro c esses ï t e c e 1ı
s an d
ľ c on ce js s e ı
d
n tr a uo or N a c u rr e
n t It l
e c tiv e ı
y s u p p r Ęş ș e ș T L o Ėp A M Tt is

:g b
işį Ţ
taı 1n ar tic o ls a n t u e d ¢

JinH.i
so d o r n v u a r
es n o t sev era ty p
p o te n u a t s J f s e iz u r e s
in c lu d in
e ä a
,

M e c h a n is m o j ac l n It
. x se iz u re s A lth o u h
g
g
ai..
a l s o n ben z o d ia zepj ,
p '" h u r..

i
Scanned by CamScanner
/
'

Y
\
Scanned by CamScanner
/
l
į i
沾 ミ丁

H
晌 写
n 了
乜 台
巳 ミ 。

一 セ 。
、 日 巴 肾 。

: 场


.


n


. 肆
ひ 宁
マ 刊


.
歹 》
コ の 四
.
亏 艮


昏由 &
国 口 可
孚子 コ 1
m
.

肙 子g の


:コ 七
n

(コ
-コ
a 。
叼 コ




コ 了 。

ヨ ロ



ー 勺







吕죠

飞 四 巴 目
肾 匣

.

巴 の
. 、

'



の ◆ 巴 の
内 。
门 口 千 于 山 自 。
ロ 印
甘 守
の 。




e

.
倉す 。




h ロ 口 ツ 。
氮 军n a
团 了 团

。 田

m

m e
\
匂 赵 닝 自 m
ツ ゴ 。


闵 の 、

) 人

i
.
e コ

手n 。 了 コ
巴 ロ ゐ
卫 吐


u 區 曹 。


m n ヨ 由 。



良 ロ e n
芽 으
.

一 眉

0 . a . . a
式 U
m
引 절
b h . h P
. & n 。 U
\ h U
0 吾


g y U e U P d g
n .
b 。 W U
P G U e a

V A
n
h . .

U 。 a n 口
e u g B W .
.
U
S n g 百
b . A U
C
。 d
U
n
p
y . A h a
.
。 d
P
a

.
e m a
U h e
d ブ . n 。
. h X 国 e h
S
U
n
u
e a .
P
G

P W 。
g . . a
g b S U
U
U
U A ロ
门 P y
n

n S
u . B 口 e
C
a . q e
A 困 C P
U . の
d m e
S U e 弘 . d
n
C

a n n h e

U e G h h ロ U
e e . S
g a A . ロ S d コ
h
e
.
e e
e
B
.
C m 巴
P
h e n

c
a
e . n A e
S
a n e n g っ
m p . U
3
n ロ
プ P
Z
n

a e ロ 门
n e . h a の
g r
s . e
3 e C
国 e e コ
S e e
a .
T e a a の
n h C 》
d h . m C
S
C
U n
. a
e . e U n U n ヱ
m N n e e n
y . (
h
5

e e a

m
n M n e n ロ .
U e

e
U a h d ロ C a
. e
r S e S
A n n コ r
y S
9 a S G m e
. 国
A h
r
e
C C
々 B b 日 S
N T
e


B c a
9 っ d a C
3 m
a p
e
e n m A U 叮 e
/
+
P
e
e

C
k u
d S
n
.
:
r
y 巴 I K e
m ヨ
e 丽 . b
U r W y n
. I
r


S
U e
n A a
s e e S
5 h u P T n
h T e
m h e
m . P
- p h
.
n e ロ . a
S
p
r
P h e U a
づ e
r
e u
r
e c
a
N C げ e
. U 낵 a n n
d
U e
d
m h
e
叫 n
a
d e
s
s
S
e
. e & e
h n エ n h
C n e y a a
f y U ロ U
m C
ヨ n y m
m a S p
e . W n a
n h U .
u r
y a n h C .


S . y
b
目n
a c
a P 1 . C a
.
p U s
C
U 弘 a
r
c p
e s d a
e h
a
:::;.:: ベ
c h s e s e
C
mrylu5s s e e

Scanned by CamScanner
Scanned by CamScanner
'
t

o th e r c e n tr a lly tin g d
N AD a c ru g s s u c h a s b a r b itu ra te s b en z o d ia z e p in e s g e n e r a l a n e s th e tic s a n d
d ĵ l ru 7 ı

H
C u

)eF
s o lv e n ts d ti ls a n ts A lc o h o l a ls o
an an co n v u en han c e s th e s e d a tiv e e ffe c ts o f a n tih is ta m in e s
u ) T ĥ In ï Iı
th a t a r e co m ly d in th e tr e a tm fn l
!u
m o n u se en t o asa con g e s tio n C o m b in in g th e se m e d ic a tio n s
) Ìc d]łı
ı/ ı birr Iņ ıi
. n o rm al fu n c tio n s su ch as au to m b ile d r iv in g A 1c o h o ıc a n a ls o e n h a n c e th e h e
o
p a to to x ic
e ffe c ts f in
ning
o a c e ta m o phen (T y le n o l) an d th e g a s tr ic ir r ita tin
g e ffe c ts o f N s A ID s th u s
n r ıi
f ・
u] rr in ĥ ・i
nc re i g t he s kf or dv l p me nt f a si tisa n d p p e r l C
; eding. h r o n i ca l co h o l u s e ・
can in te r fe r e ith th e b o lis m
w m e ta o f c e r ta in d r u g s d u e to e n h a n c e d l
e v e ls o f liv e r e n z m e s
y
C = > CO, ◆ Hao
F J& * ıa
M eh b ◆fım It is
o ıa jc o h J a c a rb a m a te d e r iv a tiv
o e u se d a s a n a lc o h o l d e te r r e n t It is a r e la tiv l
w hen d m in is te r e d e y n o n to x ic s u b s t
a an ce
a lo n bu t a rk e d ly
e m a lte r s th e in te r m e d i
w hen a lc o a r y m e táb o lis m o f a lc o h o l
h o l is in g e s te d a fte r a dm in is tr a tio n o f d is u lfir a m b lo o d a c e ta ld e h d e
y

. ď
姗 隸 萬
凝鱷 癮

盛 一

Scanned by CamScanner
co n cen tr a t io n s a re in c r e a d Fo llo

?
se
w e d by H u s h in
g s y s tè m ić v as

H
ï
in h ib i t in
g a Jd e h d e d T
y ehyd ro g en a se
L

3 Éd lıċ b {k

, 二二 二刃ヨ 吼 ・
; .
歹 ?
礖回 国 国 国 国 阳
h◆
'
ĺ 四回 M ET H A N @r
f l p r o d u c ts
c o n u n e r c ia
t is fo d in v a r ie ty o
!r m b Þń M g h ly to x ic a lc o h o l th a u n a
th a n o l is
,3 【 u
M a
a in t th in n e r an d
e
r a c in car fu e pls
Ų yd e 0 x id a s in d s h ie ld w ip e r flu id s o m e g
e '
» u b r ti in c lu Ń a n tifr e e z e w

k e e p in g fo o d w a r m T h e re w e re 1 0 r e p o r te d d e a t h s fr o m 1 958
e 占飞 白lid fu e l fo r
ca n n l th l d fo r a d u lts is
1 ) ın
i e s tim a te d m in im t ım e a o s e
C HsCo o H -
l in 2 0 0 9 (F ig r e
/
e
Y ru e o m e th a n o ı
ı
qx D ex p o s u r e s to iv in g in g e s tio n s gr e a te r th a n
M A IN L Y E X 了 30 m 1 T h e r e a r e a ls o r e p o r ts o f p a tie n ts su rv
RA iċ ŕï o t l 15
H E pA T p p r o x ir a e y
īq
qn a

4 0 0 m l ńt h o u t s e q e la e
u
L a c t a te

Ħ 4 2o A s y s te m a tic d ia n t
g m o f D is u Jf iıa
m in h ib it tħe ld
a e hyd e d e h y dro ge n a a e
ln P y ru v a te
a d d itio ft F o rm a d e hyd
ı e
p e titiv e Jy b in d s
n co m
a n d in h ib its th
e p er ip h era l ben z o d ia z e p in e recepto
JPh am ı
a co o g fc a l tio m
a c It p ro du ces a s e n s jt iv
u n
p le a s a n t r e a c tio n w h e r ı th e
ily to a lc o ho l
p a tie n t u n d e r tr e a tm
en t in e s ts
g e v en sm a lı a ts f LT , Fo r m a te
m o u n o e Jn u o r r tr

[r łrlo ] ļ b a l t i ] ¢r
Fo ı
ın ı
c A c d
ı

co ho l aı [i n i ņ r r iT tt
o n e A ccu m u ı
a &o n o f a ce ta ı
d e h y d e in :
i , In u u fn ĥ P
th e b Jo o d pro d u ces
r ea c tio n
a co m p le x o f M g h Jy
w h ic h is r o o F ig 4 2 0 M b o lis m fM e th an o ı
p p r t io n a ıto M e d jrjT íjolJJ.
e ta o
ı
o n
g a ı
o s a g e o f b th
d is u Jiir a m
:
a s c oh o ıis b e in o
g m e ta b o ıiz e d Jt d a n d a Jc o ho l
o es n o t a
w jjıp e r s is t as
p p e a r to ĵ n fï u e n ce th e r a te o f a Jc o hol In r ir Ï f ło Ðł
i

Scanned by CamScanner
: f g lu ta m a te a n d
a tio n
ı d r e le a s e o
< Re v ie w Qu e s t io n s is s io n a b a la n c e m a in ta in e d w w g h th e regu an
> rj j ıi . ro tr a n s m
i G A BA
V ER Y S H O RT A NS tio n o f G A B A in U te B r a jn
W ER Q UEM O NS QB E x p la in th e fu n c

Q L W iu t a r e e ie ıa l il (i)
g a n a e s th e tic ı (G A s )ı ity (i o ic
fe tc ita b i】 n
C m d ia te d in h ib itio n d o e s n o t a c t s o le ly a s s lın p le su p p r e s s io n o
en a ıu e s th e tits a re d ru gs w h ic h p r o d u c e r e v e r s ib l (ū ) G A B A m e
e lo s s f fir in g pattern)
a 】
lse n sa tio n s s o th a t to e
n a b ]e ? n
g ic a o w r a d o to b e c a r r ie d o u t
o
consciousnes[nđ
oss of ll Oinhibitory in p u t c a n tr a n s fo rm

8 a tiv fe e d b a ck (r e c u ıT e n t
p r o v id e
e
i s m a y be o rga n ic e d to n e
(iĵ n (iii) It in h ib ito r y c o n n e c t o n
f
in h ib itio n ) v ia n e tw o r k s o n e u r
o n s

ceus in h ib ito r y in te m e u ro p m a y
i i f fm n g in m u ltip le ta r g e ts
(iv ) B y c o n tr o u ĵ n g precise t m n g o
n c e th e e x c ita to r y e ffe c
h t
i
syn c hr o n z e a c tiv ity a n d e v e n e n a

tic m e m b r a n e ?
Q 9 H o w th e G A B A r e le a s e fr o m p r e a y n a p
w h e r e it is s to r e d a n
d it is ī e le a s e d in to th e
v e s id e s
A n « s y n th e s iz e d G A B A is ta k e n u p in to i l v ia
r e le a s e G A B A is ta k e n u p in t o p r e s w a p tic te ī m n a
sw p tic c le ft b e x o c y ta s is A fte r its
y
i v e s id e s fo r s u b s e q u e n t u s e
l
It is a s o t a k e n u p in to th e
G A B A tr a n s p o r te r s a n d r e p a d ca g e d n to
i t d t lu ta m a t e b y a m i t o ndrial
A tr a n s p o r te r s In g lia G A B A s c o g
n er
v e o
g lia v ia G A B C O n v e r ts
G B A T ) A th z y m e g lu ta m in e s p th e ta s e
G A B A tr a n s a m in a s e ( A n o e r e n
en zym e
i h b i t r m in a ls
in e w h ic h is th e n r t e d
In to th e n e g o r n 吕 n e r v e e
g lu ta m a te in to g lu ta m
th e s i
n e g l t m a t e
w h e r e it is p m c e s s e d to s y n
u a

10
is n
ns da t ion a l co h o l a t t he a c e t al de h y d e s t ag e d u r i ng a l co h o l m e t ab o l i
. t b l oc k s t he o x i of

causg a n iu la tio n of a c e ta ld e h y d e in th e b ı o o d p r o đu c in g
fo u o iv in g d is u lfir a m in ta k e a cc u n

i 1ßr a m b lo c k s th e o x id a tio n o f a lc o h o l W W 8 h ite


h ig h ly u n p le a s a n t sym p to m s D s u
h d d h d h ic h a c ts in th e sec o n d s te p o feı
han o l
1・ nfjilersible jn a c tiv a tio n of a ld e y e e y r o 吕e n a s e w

W c ï 1. {ū 往山 a ū o n

Ļ rıĥ U j lJ Ľ i

Scanned by CamScanner
ĉ g

am iı
ı ıa iw
A R M A C O LO G Y O F D R U G S A C T I N G
C E N T R A L N E R V O U S S Y ST E M II
Æ -

N G T H E C H A PT E R
NT R O D U C ı
ı

t i m a n ie s a n d h a llu c in o gen s

u sed in P a r k in so n
'
s d is e a s e an d A lz h e im e ť s d is e a s e
D ru gs

C N S s tim u la n ts an d n o o tr o p ic s
io id a n a lg e s ic s a n d an ta g o n is ts j

K EY T E R M S

* A ti p s y c h tic d A n tip y s c h o tic s a re th e d ru g s u s e d fo r th e tr e a tm e n o


t f m j
a o r
n o ru 8s
d c a lm th e d is h ır b e d b e h a v io u r o f p a tie n t
p s y c h o s is T h e s e d r u g s re du ce a g ita tio n a n

d in th e tr e a tm e n t o f d e p r e s s io n is k n o w n a s
* A n tid e p r e s s a n t d r u g s D ru gs a re u se

an tid e p r e s s a n t d ru g s
h ic h liv th e sym p to m s o fa n x ie ty a r e c a lle d a n ti a n x ie ty
gs D
e
* A n ti an x ie ty D ru ru gs w re

d ru gs D r u g s
d r u 吕s th a t a lte r th e u s e r s th in k in g p r o c e s s e s a n d
'

< ・
H a llu c in o g e n s T h e h a llu c in o ge n s a re
f l
h t le a d s to s ig n ific a n t d is to r tio n s o r e a ity
p e r c e p tio n in a m a n n e r t a
i s d r u g s a r e a g e n t w h ic h r e lie f th e s y m p to m s
* A n tip a r k in s io n , s d r u g s : T h e a n tip a r k in s o n ,

i P a r k in s o n s d u g s
'

o f p a r k in s o n s is c a lle d a n t
'

ru g s im p r o v e th e
fu n c tio n o f d e m e n tia a n d lo s s o f
* A n t A lz h e im e r s D r u g s a r e th e d 】

t A L z h e im e r s a g e n ts
'

c o g n itiv e a b ilitie s is c a lle d a n


r s u p p r e s s th e p a in s e n s a tio n b y th e ir a c tio n
* A n a lg e s ic s T h e d r u g s th a t r e lie v e o
k
c io u s n e s s m a e s
th e in d iv id u a l u n a w a r e o f p a in
w ith o u t c a iıs in g lo s s o f u n c o n s ,

Ėe h i h li e p a in a n d c a u s e d e p r e s s io n to c e n tr a l
N a r c o tic a n a lg e s ic s A r e th e 山u g s w c r e e v
*

ttit u d e
a nd b e h a v io u r o f a p a tie n t to w a rd s p o s itiv e a
l
T h e d 】u g s a c t o n c e n tr a n e r v o l ıs s y s te m d e cre a se ın u s c le
# C e n tr a l M u s c le re ia x a n ts ,

h been u d in th e tr e a tm t o f a c u te
e m e n i in e s e d Ju g s a s
se e n
to n e an d in v o lu n ta r y mov
d i d it io n s
o r th o o
c c n
p a in ń tl m u s c le sp a sm s, so m e ae p

Scanned by CamScanner
J
rm rı
a Te x t B o o k o f P h ' " l a ' "
ogy fD ru g s A c o n c tr a l N s lł I 299 =
W
o e n e rv o u s te m

U . .

caı
l.
X e

,
D

X . . ' " u m b ic p a th w ä y

f p o s ts y n a p tic in th e im b ic p a th w
ı a y
ı
コ A ty p ic a l
# D 2 re ce p to r b lo c k a d e o m eso

d 5 H T p to r b lo ck a ū e ın
◆ Enha n ce d d o p a m in e r e le a s e a n 2A re c e

t m s
th e m e s o c o r tic a l p a th w a y to r e d u ce n e g tiv e s y m p o
a
t e ffic a c y in
◆ O th e r rece p tob in d in g p r o p e r tie s
r m a y c o n tr ib u te o
an d
tr e a tin g c o g n itiv e s y m p to m s a g g r e s s iv e sw p to m s

d e p r e s s io n in s c h iz o p h r e n ia
In c rııs e O a
ı h v ・I

\ S H T In ßn ln j
\
C D R UG S
P SYC H O Tı
CA L A C N O N S O F A NTı
OG ı
PHA R M A CO L . A ir e s

t
;

図 國 \i龉 亀 豔
鑼 ,
th e h y p o th a la m u s a n d p itu ita r y
pro d u ce d b y b lo c k in g th e a c tio n o f d o p a m in e o n

d r u g s a r e (1 ) s k e le ta l
M is c e lla n Th is c e lla n eo u s ac tio n s o f p s y c h o tic
a n ti
eo u s a c tio n s e m
ff in h ib itio n o f h ic c o u g h
ia lo ca la n a e s th e tic e ec t
' m u s c le s r e ta x a n t e ffe c t, h y p ° th e r m
"

Scanned by CamScanner
ł&

:O O ı rm ilA Te x t B o o k o f p h a rM a c "
团团■ 30 1

A d v e rs e e ffe c ts o f a n tip s y c h o tic d r u g s


.

- a lly 1 0 '" " 9 4 ho ' " ? um . ・ ' " h c'" s. . per
1 T J】e y intra h e p a tic
ca u s e o b s tr u c tiv e ja u n d jc e
" ]i ede d
. nt ra m u s cu l ar 10 to 50 mg fou r ho u r l y.
2 T h e y c a u s e e ffe c t o n c en u a l n e r v o u s s y s te m as d ro w s in e s s
Y I i, a y if ne
co n fu s io M 0 5m g p e r k g
p s y c h o « c r e a c t io n s
n
p a rk i
n śo o r a lly
o 5 m g p e r k g b o d y w e ig h t in e q u a l d iv id e d d o s e s 6 h o u r ly I
c h il¢
u r ly
Tħe s e d r u g s cau se c o n s tip a d o n , b lu n e d v is jo n Ta c h y c a r d ja w e ig
h t 6 to 8 h o
th a t o ff c t th e n
A d u lt o r a lly 2 5 to 5 0 m g th r ic e d a ily if o r a l d o s e d o e s n o t e e
ccu rs d
c ho lin e r g ic e nect u e t. b le h ic c u p s
a
ĉ ır
u In tr a c ta 5 0 0 l t 1 0 0 0 m l n o rm a l
Th e y h o u r ly fo r s e v e r e M c c u p s IV 2 5 to 5 0 m g n i m o
c a u se hem p o ie tic e i s lik e to 5 0 m g 8
J/M 2 5
o a gr - lo c y to s is
u a p Ja s tic a n em ia th r o ın b
M e re a re e n d o c ra n ia ıe ffe c ts lilc e o c y to rp e n" đ n t e (in ń ıs o
i n )
a m in e n o r r h e a in h ib itio n f s a li
o o v u Ja tTio n d e p r e s s io n
H y p e r s e n s itiv ity liv e r im p a ir m e n t c o m a b o n e m a
gyn a s tia a n Ad rT o w
a e co m Ja c ta t
jo n c o n tr a iń d c a
i tio n s
i
ti s n p r e g n a n c y
, h ? a w a l C h ild b e lo w a g e 2 y e a r w ith p r e c a u o n

a lc o h o
l a n d b a r b itu r a te s w it
T Y P IC A L M M P S Y C H te n s io n s e c u r e d is o r d e r s liv e r
d is e a s e c a r d ia c d is e a s e e ld e r ly
O T \c s la c ta tio n h y p e r


i o n s tip a tio n w e ig h t g a
in o r th o s ta tic
C }n O R PR O M A
Zı v o m itin g n a u s e a d r y m o u th a n o r e x a c
N E ıt ħa s a c t io n s a t a ll ı s id e e ffe c ts
e v e js o f th e tr a l n d v is o n
i d u r in a r y r e te n t io n
cen er v o u s s
E C G c h a n g e s c a r d ia c a r r e s t b u r r e
l r y e y e s
y s te m
p r im á r iı h y p o ţęn s io n
y at i l k i s k in rash
W h e ra l a n tic h o lin b r e a s t e n g o qg e m e n t a n e m a e u o p e n a
P a m e n o rr h e a
e rip
e ıg ic a cü ï il» g a n ı lr ic
g e n u r e s is
im p o te n c e
g io n ic b ı an d

o c k in

ツ tio n i

so k
p o s s ts s e s s lig h t a n tih is ? g ac is r e la Łiv e ı t d iv e d y s n e s ai
. an d a n tis e r o to n jn y s jig h t it r e s p ir a to r y
d e p r e s s io n h e a d a c h e d y s to n ia a r
a c tiv it
y ti n 4 to 6 h o u r
o n s e t a c tio n 3 o in u te s a b s o r p t io n v a ń a b le d u r a o
p h a l m a c o k in e tic s o r a lly
。 m
。 r e c e to ıs
。 p on d c P a m in e i
g cw r t ion 1 5 t o 2 o m i nu t es I
v o n s e t a c t ion 5 m i nu t e, e a k
c
e p ltn s ubt}Pes D 1 D 2 D 3 d D 4 d iffe r e n t
. ' e l l ・b s o r b e d p e a k c o n c e n t a
x c r e t ed in
ho u r s , e t ab o l ise d by live r e
an
d 5 H 7Z
a n t ip s y c h o tic
ċ oi l 1 0 m i nu t es p l as m a h a l f life 1 0 t D 3 0
an
w r id ıa n x i ċ ė n t ra t ion
o Jy t ic A n tid e
p e s s iv e a n d ilk
tia g g r e s s jv e n te r s b r e a s t m
u r in ė j o s s e s p la c e n a
an i t
e p r o p e r tie s o n h is ta m i. B a r b itu r a te s A lc o h o l s e d a t v e s
i
sy n i a g ic
iĵ È1+
Mm E r
s s a n ts
p iı
," " ti" " o v e rse a d t io n b y c N s d epre
to (m ild ) b l d b r o m o c r u p tin e
.Ati h y p n o ń c s D e c r e a s e d a c tio n p
o o a
D o p a m in t y e v
d ą n ti a r k i e re u
p ta k e . In e s a n tid e p T e s s a n s
r '" e an
p n s o n ia n
e ftėc ts
w h ic h ńlþı ea d
ĺ f ıĺ l ! U£hi
D o sa ge b d
f g e o 5 to 1 m g per kg o y
p to 5 y e a r
a
t h r ic e d a ily c h ild u o
A d u lt o ra lly 1 o to 2 5 m g
rijlíiv
c 1o z in c a r b iz e n sR c a in
( B ra n d n am es c h lo r p ro m a z in e H c l T a b le ts In je c tio n e

ab l et s.
!ŕ iß& o l , pr a z i l 25 m g , o m g , 0 0 m g , 0 0 n ı g t
2 e g a t il su n
Its p r o p e r tie s an d 1 ıs e s a re
d in th e tr e a tm e n t o f p sych o se s
F L u p H E N A z IN E Its u se
M g h p o te n c y p ip e r a z in e s id e
f c h lo r p a z in e T h e s e d ru g s a re
ge n era lly s iın ila r to th o s e o ro m

% s ıD

Ĺ
n ıg ı B ł
od c th e a c tio t
In d i u o fD o p ann i

m ĥ m ° °n '"

hiccı
ı
,jnjtntpohyńa,hı
ypothermja :
.

, " " . .
d d o s e s 6 to 8 h o w ly n o t to e x cee d 2o m g per day
D o sa ge A d u lt 2 5 to 1 o m g in d iv id e

Scanned by CamScanner
J ■ E lt Ħ x t B o o k o fP h a rm
E o lo
g y (y

p吧
a co lo u o fd ru @ra c t im 】
o n c e n tr a l n e iy o u s s y s te m 11 53 四国匽
In tr a m y in itia lly 1 2 5 m g th e n 2 5 to 10 m g in d iv id e d d o ś e ś ' Ĝ to 8 ı
u s c u la r l
h ö ijŕ l '
F lu p h e ru z in e o a te 2 5 m g p e r ın l e v e ry 2 to 4 w e e k s
d ecan y n4 I1
i;
rr ;
' i'
1
;
: d i. Ti' ' " e v e n d e p r e s , i. . R e n a i o r h e a tic im a ir m e n t B
p p lo o d d s
y" Cr '. ". " :
" '
:
w ith p r e c a u tio n s in
p r e g n a n c y , la c ta tio n , b r a h i d a m a g e
.
iī Y}
s id e e M e c ls H y p o te n s io n d r o w s in e s s E c G c h a n e s D
ta c h y c a r d ia e x tr a
g r y m o u th c o n s t
iro a tjo n șu .
u yst
,
u já
ä ľ
p y r a m id a l r e a c tio n s
Bm d n am es T r ifı
u p e r a z in T a b le t T ra z in
e e N e o c a lm T r in ic a m S c h iz o n il 5 m
ta b le ķ g 10 1n
g

įeĺįį
T iiflu o p e ta z in e T h e se Th e dru gs
are " " ' ' "
p p e r a z in e

an d p r e c ip ita te s e iz u r e s in e
,
p ile p s y p a tie n ı
s

: - p h r m ia a g ita tio n o rg a n ic b r a in dro m


ł y
syn te n s io n \ıse . o mg
he
qąf h i ldr e n no t re c o m m e nd inj ,' " h ' ' " f'' " æ g en c y

e ar a.
g e P sy_ o tic d is o n d e r s A d u ltı 2 to 5 lly ffic ie n t
m g tw e lv e ho u rl d o se w ill n o rm a su
y (tw ic e d a u ) m
y a y in te m a n ia ly p o m a n ia
c re a se
ic s c h iz o p h r e n ia a cu
C h ild o lly 1
'aÈäiion A cu te a n d ch ro n
delional d is o r d e r s b a Jlis m
ra m g dany or tw ic e d a il t f s c h iz o a ffe c tiv e d is o r d e r
y sa l ßz i j d fo th e m a n a ge m en o
ta l
a ls o u s e
r
It is lly d ju n c tiv e th e r a p y in m e n
f c h o ic e ) a n d o c c a s io n a as a
e tte s y n d ro m e (a d r u g a
an d T o m lim in tio n t a v e ra ge s
ith H tin g to n s d is e a s e Its e a
d th e c ho r e a a s s o c ia te d w u n
r e ta r d a tio n an

2 4 h o iır s

B ra n d N
am e M e l】
a r il T ab
loom T M o r id a z i
n e T a b 1 om
g ( f ıı【r u x ßın o

ı
Scanned by CamScanner
rm m Te x tB o o k o pp h a r ı"
¥ "

PF m m r r n m
l


MOZlDEitjsaJecentlyinuceddrug J t js a d u o g e b tk b u ly l j CA L A N H P S Y C H O T IC S
p p er id jn e d e r iv
A T Yp ı
a tiv
e h r sys te m s a ffe c te d b y a ly p ic a ] a n ti s c h o « c s
R e c e p to p y

圆 e
? 5 H T zA 5 HTt 5 H T 2c 5 H T3 5 H T£ 5 H T ? D , D 3 D + M . H r

了 s e Ħ eï a l ? ys a do D in 5 H T 5 H r7
\ o ra Jd peń n e zA

ıiıt ĥ iic M ii
n r s ıA «a n ic e x c ite m e n
Ła c u te p in e D 2 5 H T w 5 H T zc 5 H T 3 5 H T 6 D r D D D M H
sch zo 3 4 5 1 5 t
p b re n ia

ti ïf
tia p "in e D 2 5 H T 2A 5 H T 6 5 H T n? a i A Ł H ,
" o J ıs i H w e rs e n s ftiv\ tíly d ia c
y D b 5 H T 5 H T 5 H T 5 H T 5 H T7 D 3
p r a s id o
c u l
a rr h y tlu n ia s p re m
n e zA IA ID zc
a r ıc y h aiJd below


c
12
. y e a rr s

三三 二三
h e m ic a l c la s s f ben z is o x a z o le
一 e s 占し C L O Z Ip ıN E It is a p s y c h o tr o p ic a ge n t b e lo n g in g to th e c o
。 h iz It is s e le c tiv e
- x tr a d e r iv a tiv e s a n d is in d ic a te d fo r th e tr e a tm e n t o f sc o p h r e n ia a

i T y p e 2 (5 H T 2) d o p a m in e
g o n is t w ith h ig h a ffin ity fo r th e s e r o o n n
in e r g ic a n ta t
, m o n o a m
It a c ts a s a n a n ta g o n is t a t
Ty p e 2 (D 2 ) 1 a n d 2 a d r e n e r g ic a n d H 1 M s ta m in e r g ic r e c e p o s
t r

i t o th e r th a n d o p a m in e a n
d
o th e ŕ r e c e p to r s b u t w ith lo w e r p o te n c y
A n ta g o n s m a t r e c e p o r s

l i f th t h e r th e r a p e u tic a n d s id e
5 H T z w ith s im ila r r e c e p to r a ffin itie s m a y e x p e
a n s o m e o o
an tþs y t h o ti
ċ a c tib n
to c h lo ıp e ffe c ts o f C io za p in e
ro m a z in e A s a n a n t ip s y c h o t fc
RISÞĖDONE It is a a n tip s y c h o tic d ru g It is ' be n z is o x a z o le d e r iv a tiv e

ffin ity fo to in 5 H T2
g b in d in g
r se ro n
f A It h a s e x tr e m e ly s tT o n a
M e 国 o c t io n an

a n d d M s ta m in e H 1 re c ep to r s
affinity fo r D o p a m in e D 2 re c e p to rs a n
ıe c e
p to ıs re c e p to rs a s tr o n g b in d in g
? n P a h a lo p e r id o l
ıńidi c a n s er o to n in 5
H 72 bı bo t 2 0 0 tiın es m o r e th a n
n ı
a n ife s t a s I o c ke r Its ä ffin iq fo r se ro to n in re c e p to rs is a u
ran T ħe r e is
q u iliz a t io n d
a m a r ke d c o r t ic a J
an su p p r e s s io n o fa gg r I n d ic a iio h p sy ch o s is s c h iz o p h r e n ia

p
o n d is o rd e r s b r e a s t can cer
M s e iz tır e
' "ally 1 0 ' C o n tr a in d ic a tio n H yp e rse n s itiv ity p re gn a n c y la c ta tio n
g W "
\ InitaJ d " " l im p a r im e n t he p a tic d is e a s
e
USU a I th e r a c h ild re n an d e ld e r ly re n a
p e u dc d ig h t g a in b lu 】T e d v is io n
o se 6 0 to ・ f a p p e tite tip a tio n w e
S id e uį ,ts v o ın itin g d ia rr h o e a lo s s o co n s
ie ty h e a d a ch e
? s in e s s in s o ın n ia an x
d y s to n ia o w
o r th o s ta tic hyp o te n s io n a k a th is ia

Ja u n d ic e
e r e x c r e te d in u r in e
lly it is m e ta b o liz e d b y liv
Ph a rm a co k in e tic s w n en g iv en o ra

Scanned by CamScanner
-

rm » øi x m m jıK
q

厂 a a ıd
* c « m i
a e e
n 1吨 n e \
挪 诵锄e = e e 《e 曳
ln

ww w A d & 螂? a E i
te i» n « « d ¢ lł

d e « # g
I # e b a ūt » ı» a m « o
ae
ï *

S ia o m R n a d ıL R b p id
W » # = ı ? p ı\

Į = g « »b
W m
« = « p i m k æ ¥ = & a w t So m e cen ł
r ıł
a n tif\m g a ls
a n t i n m æ
t * id e
s
卤 月沁园 阳 堅 o aa
ı
セ 雪マ 目 寧 胃邮 电目 身 自由

is d ec ū » e
H a
o u w z # * » g * M » d a a s ït b w
fo th e tr e a tm en t d ao pb n=
d is in d ic a te d r
Z 15 * f f z d o pÆ iæ
a n ıT yp e
d e r iv a tiv =
es
* ¢ ffin ity óo r th e *e u »
e
ta g o n is t w ith M g h a
m in e r g ic an
m ? i m on o a
= b i= m d B

a ・q p A * DL » ・* d 15»20 g o n c e d a ily a fte r đ iv ity b ı
ıld y d ı= »
g
ı r ı» ņ n a s se s s m en Ł
o f ı( t io n ı an tip s w a
S ł m A »
ha n il m a a d a£
to rs in th e m e s e ıi m łĤ c
M «
白 ? 咖 钮 轟 懸 鲫聞 阳 曲 唧 y i fu n c tio n a t D 2 l tx p
e
禁 姥 m 叫声

a n ta g o n is t c ı ł om s is d ııe 协 鳥 叫声園 阳
S iä w # * ķ P a s l ı» Ł d in « n »
D t y w e ig h t
i A lle v ia tio n o f p o s itiv e r y 呷
p o s tu ra l 心了 n 鬲 a i c o r t e x
t S H T 2A
m rM a i& Im p o lM o m s a rc d u e o
w h ii n lie f o f n e g a tiv e s y m p
1c e m t i a
db p
e i Đt b sw
p k
h y p o te re rio n w id Ë ı
ı
It i m iı d ıy s e d a tin » ı l a d ı
s id e t ffm
s
d k «= M o n p W o r = y
网岫 = 叫
二 由
吆 幽 明 自 心 钿 ta 岫 o ra 即 声 k t r a 姓m 6
le (iá iiá N a u se a a n d v o
m itin g a r e t e
h (o n u n o n &
h d l l im i a c
ï « ı« « d
◆ \ » R « a a d » = e u c * ņ
T in t« T v a \ o c c u rs ¡ l
E
l a tio n o f q M H Ď
r e la te d p r o o n g
笙螂 M 纫 分烯 侧 蛔 嗥 叫 * の曝 ¢ ıcto r a ld n ıp
se n ce o p n d
飘 缃春
向阳 a ic o ıo ııe d a d v e s a n rih is t a
f
y in th e p r e
図 自 ı in e s e c ia ıı
łıa M 》 ı
n = e
m a r rh y th m ia s e s p
p m m * i d a ily d o s in 吕
& m is 8 h o u r s n e e d s tw c e

锄时 傷目 甲自 tq « ł i e« n a a o k
ıı
索《 》挚
鳥聞 氐 阳怬曲 阻
td a» tb * ıııic ıł ¢ æ oł
硝南 邮 良硝 圳 和声 心 曲刨 比 鲫 m M 砭 0 1ın 0 U t is
ı a ps y c h o t ro p k a Bp n ! o n »
輸 名曲目 力蛔 头 島 R ï p I pR A z o L Ē
昏 昏 ?鳥 略 ï 锄 鳥 ď
峪 吆 划 躡 南 鲫江婚 聞 10 ın r th e m m i« n t
吕p 吖 踊 L d e r il ra th >e s an d is in d ic a te d fo d
D z * on
rı h d l ¢ m æo i n * f« h r a i* an
偶 爿璐 露內彰天 和 t1 8 o n b n ・l m
a c t io n lt is an
飘 \ 嚇 図曲 甲目 M ech a n ll m o f
aı o e Ħ & T **
ı p e x đd w
啕 聯 硝 渤 姗 姗 钠 國 国雄 耐 th e fm n ta \ A w m
心 acu 自
¢ m rn k 5HT2A1recptors ïn
s y m $ı# e m * a l
pm « »e w m
il s łm a m
p ro m s
w h iı
e a n ta ww w b m


w

l« ı n u y m ln ç a \ H E»ttaīamitĺ aıs id «
ı
ıı m \n ı
tıw ı
ly m w
s id ł d ı
n ı
q =
W
o ol ı Lı
ttı
e
h w p * « ın a e m łn hyï q*n m Q T a tç
¢f k u «ht
n N
ı W N łw m \ W t k ] n an d


u u M «h l
ı M ı
n l
*n ı
æp n * ĺ/ ıw ı
ph * ı* & »w * r » * fp \ lqe * dd a ı
w
W "
r Ą 14 fl 14
Ł5 »
lw4\ n ib
ı p Irï n * l
ł U ıt ł ird
tł a# a nu p # yt ı
\h d« w

Scanned by CamScanner



。 鳎 矚矚覊 纛 覊 譏巍
Scanned by CamScanner
ı . .

C la s s ific a tio n o fa n tid e p re s s a n tagen t

s e ro to n in
łıu p tık e īn h ïb ıtio n s

g . i m
Fı ri
u w u a m ħe
P a ıo x e «h e Mipine r n tıjŁ
S a n ra ūn a a
!ıin 0 10
1,
T ia n e p ı
in e )b ó
A m ln e p tin e q n :
M ı◆ S « T n ıp L §y e m ifo n ! h U 0 1 u n
ł j) 9 i
J
i0 7 ı
0 7ı
j ĵ {ı

R E v E R S IB L E tN H ı
B IT o R s o F M A O A R IM A
( S)
M O C ĽO B EAE D E n
is a s e le c tiv e r e v e ñbı
rs e in h ib ito r o f m o
n o a ın in e o x id a s
Ĵ n c r e a s e s th e B e id e (M A o ) w h i
s e s iEs r e s e n c e i
p ch
n sy m
p a th e tic n e r v e s th e r e is a n a b
u n d a n t e v id e n c
e th a t
a s s o c ia te d w ith
s e r o to n e r ic n
g e u r o n s o f th e r
a p h e n u c le u s
M « h a n is m o f
a c t i o T h e m ec h
a n is m o f a c tio n o f m
o c lo b e m id e in v l
o v e s th e s e l
e c tiv e
d e s tr u c tio n o f
m o n o a m in
e s in th e n e
u r o tr a n s ın ītt
m o n o a ın in e s r li e rs T h is r e s u J s in
e e v in
g d 中 r e s s iv e s w ! a n in c r e a s e in
th e SHT
p to m s R e fe r F i吕 5 4 p o s ts y n a p tlc
N E
R e c e p to r
D m g In [e n c tio n ı
tm be
ay c ha n c e s o f in te r a c tio T C A
b u t c a u tio n i ith e ch a n is m o f a c tio n s
s a d v is e d n w o th e r dru gs ng 5 4 M
w h ile c o r an d aı
co ho l
p ex r ib in a re sm a ll rn a :ı
d o s e 150 g p e th id in Tm
m g b d s td
s (m ,a x 6o o m g da
y į b ran d
e,

n am e 】
w w
an d s s R Is

w iv e , h y p o t e n s iv e
e f f e c (e g B lu r re d v is io n d ry m o u th
d fin
c o n s

e
tip a t io
tr e m
n

o rs,
15 o 3 o o A d v e r s e e fĺ e c t S e ? t W ea ţ i ng an
m g ta b s k n es s
l c o n fu s io n w ea
t e n t io n ), r e s p e c
fiv e ly M e n t a
'" " u r in a r y r e
°n ' " iv e
'

in . agen t an d ? o t e in W ith .
m o n oam in e ox id a s e It b d 9 5 % t o p la s m a p
o u n
. .
?h,į kneti ''" t has ite
. H a lE 】
o f 6 20 h o u
a x im u m
rs

o f 2 9 p g /1 o f m p
ra m in e a n d 3 5 p g /1 o f

f 2 o o m g iin w m n fn e a d a y , a m
n ņ ç Io b do se o
ilk
9 eo
e a s t ır e d in th e m
d e s ip n ım in e û n e t a b o lit e ) a re m

Scanned by CamScanner
翩 ra M IA Te x t B o o k o fPh a rm a c "
y
bd

l
lidl a lc o h o t b a r b ih lm te s c im e tid in e
In te iic iio n S ig n ific a n t in te r a c tio n s
d s w ith a n tic h o lin e r g ic e ffe c ts
(c e n m ı n e r v o u s s e d a tio n ) a n d o th e r r u g
in M bilo ī s s y m p a th o m im e tic s (h yp e r te n s iv e c r is is g e n e r a l r e a c tio n )
fc a r d o to x ic ilT ) Djı
C o n h a in d ic a tio n In d e r ly
eı peo p】
e a r e g u la r c a r d ia c fu n c tio n a l te s tin g (E C G ) J
8 pa
in 出国 le d u
i n r
m

c a r e is in
i, th , '

d ic a te d
"
w
二 ・ s u i¢id a l ' "
h e n th e r e is in fu td c a tio n
jects! B e c 。 m o f th ' "gh
' " 忑霉
\

ly lo b lo d re s tu por
r ig id ity tiv e fle x es se v e re w o p ressu
m u s c le
o v era c re
tu re
te m pe ra
vom itin g
a n a lge sic TCAs a le s c h tr a ū
y s im ila r to p h e n o th ia z in e s T ħe
?
R ose 50 1 5 0 m g
s ys ? n w ith a n a lk l a m i n e s u b s ū m e n t o n th e y c o n ta in a tr ic c lî
y y Ń a in til 1 0 2 5 m g ta b
B lin d
c e n tr a l r h c r in :
su rm o n
g jn n o n Ą e p re s s e d jn d i i g e
v d u aı
e£cct 囝
s it
m oa t m a r e p o te n t 加 加林
to r s o f s e r o t
o n in a n d n o re
M e c h a n is m o f p in e p h r in e
a c tio m It is m e ia b o liz d
e to n o r tr i
p y lin e w h ic h in h ib it
s th e r e
W n s ib le fu r " u o ıt s A i
up? e o f
norepinephrine a n d

c ha n n e

in v o
L M e
1v e d in a
e
二 二二
mcpain
s o d iu m
an d th e M u D
ろ・
A
馅 o *ıs o

eıFe c ts a r e
c h r o n ic
m
d iu m

te n s io n t
poı
a s 、iu m
e ch a n is m s
妨诋 苡
knoń to b e
yp
p i ¢M
" " h'
U

Jtĥasan''"b",ı
operties
se l "

!iih
Jt js tls e d '" " t dep. ..

o í tl« se n
i ue Um es h
p a in
闻 0 It h M
de ķ u sed In th e
D恥a n d m an a
y on a ge m e n t o f c h
ite 5 0 2 ooh
ı
ī4200g r o n ic n
c ıı
B輛 g o n
ī u mn a lı
iig n a n t
ra n d
n am e
A m nin
jJ c % į lıHu
Fr ííīí n ri
t A m ito n e T
i) p to
m an D O T H IE P IN
! V 【rT t o łz j !J tr ic y c lic a n tid e p r e s s a n t w ith an x io ly tic
It is fo rm e r ly kn o w n as D o su le p in (U S A N ) is a
玎 근j 」了り「 ı
to lo w th e r a p e tic in d e x a n d s ig n ific a n t to x ic ity in
y 닥 p r o p e r tie s It is n o t FD A a p p ro v ed du e u

Z r ) tj Y /
o v e rd o se

f b io g e n ic in in c r e a s in g av a iliıb le
M e ch a n is m o f ac tio n 1t in h ib its th e re u p ta k e o am es
ı rı
İiïrı ĥ T ır
p tic c le ft
? * ıı n e u ro tr a n s m itte r le v e ls a t th e s n
y a

Scanned by CamScanner
3 14 ı IBE EH Te x tB o o k o fP ha rm a c o ı
u
7 W A

%î X"--
U se s The u se o f d o s u k p s in is o n ly r e c o ırm ıe n d e d in p a tie n ts w ho '
u n r e s Ħ n s iť e ' ' " i\ T a n tid e p re s s a n t th e ra p ie s " . . X in '
' .
. ." ' " ' " . (u n la b e le d u se l a n d a tte n tio n deficit
f Aı
niı
ript}\inewi s im ila r eł
lic a c y th a t o f A
XX
o a to m itr ip ty lin

0
e a nrd a ls o ıu e
.
a n a n tih is ta ın in e a n d c e n tr a l s e d a tiv e p r o p e r tie s
D o se 5 0 15 0 m g
B 】a lıd N a n ıe P ï o Ehia d e n 2 5 15 ab
m gı

d e r iv a ti1 Ę b i rd ic a n tid e r
q p e s s a n t (t c a ) t c a s a i e s tr u c h u a u s im ila r t
do e s n o t a ffe c t ın o o d
y o p h e n o th i
a z iń ė
or b u t m a y c a u s e s e d a tio n i it
n n o rm a l
d e p r e s s e d c o n it e x p e rs o n H o w e v e r l
e tls a p o s itinr e e ffe c t o n
n m oo d
M « łw a is n ıo f t is a s h u n
om b
S u t n o t c o m p le te ly s e le c tiv e s e r o to i
(s R D iß m e ta b a đ n n re u
p a k e in h ib ito r
iıe
desmethyclompı
aınine
a c ts
p r e fe r a b ly a s a n in h ib ito r o f n o
The a r a d r e n a liń
ı w r bı oc ka ge an d
N o w n r e g u la tio n h a v e b e e n n o te d e
a n d m o s t ik I
l ty
.
h o th e r ı
ı r ic y c lic s a cco u n t fo r its ffe c t in
e c h ro ic
A d*m e e fft c Ł
n
p ä 'n ì In
lıy p o te r ıs lv e
a n d a n tlc h o ı
ln e c t s (e g B lu
Ýe t Șļ 50mg
e r g lc e
rr e d v ls lo n d ry ,
io 2 5 m g ta b
B ra n d N am e S e n s iv a l P a rm x

an d d is o r d e rs w iń h e m ic a u y
To d isa n d ls j
an o
vecompve
b s e ss i
co m
po n t (e g D e p r e s s io
rg b r o z ib !,
f th e d ib e n zo x a ze p in e c la s s c

tid e p r e s s a n t o
ttr e a e I en
s c h iz o tr ic y c ı
ic It h
n
p h re n ia ¢ıN E It is a
an
d d ib e n zo xe p in es a s a
D o*e 5 0 15 0 d ia z e p in es dib e n z o c y c ıo h e p te n e s an

JJ d is tin c t fr o th e d ib en z o
tn J t i ví ŕ m
B lu ıd N (5
am e a o lr ın il «】 d se ro to n in
a n il 10 2 5
50 Ë:l b 4 iJ Ï l l r
e u p ta k e o
f n o r e p in e p h r in e a n
P re d o m g ta b a s in g th e r u s c a r in ic
m in a n dy N A R t u l
p a k e In h ib ito r M e ch a n is m io n
o f ・c ı y d e c re
It a c ts b
l a r e n e r g ic r e c e p
d to r s a n d m

H 1 r e c e p to r s a
a ls o b lo c
k h is ta m in e
八 二)丁 (I H T) TC A s
tio n u r in a r y
to r s th c o n s tip a
re c e p d v is io n d ry m o u
b lu tr e
S e d a tiv h y p o te n s iv e

Ąqy ę Ħ§1 e ffe c t


e

d re a c tiv e d e p r e s s iv e
d to tr e a t n e u r o tic
an
t It m a y b e u se
f d e p r e s s io a n d
層 ų !ęĦA\ģ$ tų ș e d as a n a n t id e p re s sa n
d e p r e s s io n a n d m ix e d s y m p to m s o
n

d p s y c h o tic
격 4 ìș9 ıd ę r ęņ ęn d o g e n o u s an

tta tio n
- apis\¥R P F n g
ū e l 1 q o tó
300 m g
D o
ta b
N łm e \D em o o x 50 10 0 m g
ı
Ĥ łh ď



ı
th e fır s t
k in h ib ito r (N a R 1)
n o ra d r e n a lin e r e u p ta e
s e le c tiv e l e
i
E T IN E R c b o x c tin c is a iv a tiv e o f m o r p l\ o n
R EBo x ilo x y b e n z y l d e r

個 d ru g o f n c w n n tid e p r e s s
i
a n t c la s e It s
a n a m

Scanned by CamScanner
r m m ū e å h

:[
t
fp h
o
w =

1e u ] o tr ln sm is s i n
te d ith e rh a n c d se r n e ıg i

n ? k ħın c tio n a lch a n ge s a s s o c ia w

d is o r d e (O C D ) p a n ic d is o r d e r
d in d e p r e s s iv e d is o r d e r obsessivecompulsive r

u s e s It is u se
r d e r (P M D D ) a n
d s o c ia l
l dysp h o ń c d is o
tic s tr e s s d is o r d er (p T S D ) p r e m e n s tr u a
p o s t tr a u
m a

d (s o c ia l p h o b ia )
a n x ie ty d is o r e r

蕊お ,˜ 。 。 。 。 。 。 ' " 。 陀 。 . . . . . 。 .

little
to n in r e u p ta k e in
h ib ito r (S S R 1) w ith
is m f tio n It is M g h ly s e le c tiv e s e r o
a I b in d s w ith
M ec h an o ac l ta k e t
i (D A ) c e n tr a r p e u

ėifėc t' in ń ' p in e p h ń n e


n o re
(N E ) a n d d o p a ın n e
i e h r in e r e c e p to r s
a n d n o rep n p
th a n
t lc h o lin e
to h is a
t m in e a c e y
le s s a ffin ity


。, 。- Ħ 。 - 。、 二 e a tin g d is o
rd e rs a n d
obsessiveompulsive
r e s s io n a n x ie ty
u s e s It is u s e d to tr e a t d e p n tid e p r e s s a n Ļ a n ti a n x ie ty
d e r s It is u s e d a s a
;
a is bılër à m o n g o th e r m o o d d is o r
tid n t
ıa s s o f an e p re s sa
E S C IT A L O P R A M It is Snantiomer o f ita lo p r a m
c
b
wS R ig ) t ' "

.
ta k e in h ib it o rs (S s
_ o to n jn re u p d a n tib u lim ic
tio b s e s s i p u ls iv e an


sa n t an
f c« The a n tid e p r e s
M e ch a n is m o a o n

u p t ak e p m p of t he n e ur on a l
he s e r o t on i nr e
ėdäii.Ţtbocksthereuptakeofserotoninat
t
t
i o n n n
o 5 ř ľ r ıA a u to r e c e p to r s SSR 】 s b in d w ith
f
'
nėińij e n h a n c in g th e a c
tio n s o se ro

tr ic y c llė a n tid t d ru gs
e p re ss a n

Scanned by CamScanner
f D ru g s A c
t o n C e n tr a l N e rv o u s S y s te m ı
ı I 3 ı9
r ° l
o

d h in e r e u p ta k e in h ib ito r
a n t o f «h e s e r o to n in n o r e p in e p r
H x I N E It is a n a n ti e p r e s s
vM HA l in h ib it th e r e u p ta k e
a n d its m e ta
b o lite esmethylvenlafaxine (o D v ) p o te n t y
o f depssitz d is o r d e r s ıt ı
s g en ı
ı ń d in d e p r e s s iv e t k
e īa y m o re u se e d is o r d e r s ią ţ ę ą v i h i e a n d w e a k ly in h ib it d o p a m in e r e p
a n d n o r e p in e p r n
u a e
ft o n in
a sso c
in s o n ın ia a n d a n x ie t
y
! th o

r o to n in n o r e p in e p
h r in e r e u p ta k e
IN E It is a s e le c tiv e s N R I (s e le c tiv e s e
D tJL o x E T d i r d (M D D ) g e n e r a liz e d
i a r ily ta r g e ts m a jo r d e p r e s s ıv e s o e r
n ib ito r ) It is a d r u g w h ic h p r m
jn i l th I t has n o t ye t been
d to d ia b e t c pi ń h n e u r o p a y
d is o r d e r (G A D ) p a in r e la te p
e e r a
a n x ie ty h ib ito r o f
in c o n tin e n c e o r fo r ı ib r o m y a lg ia It is a p o te n t in
d fo r s tr e s s u r in a r y
FD A a p p r o v e
t i h ib it o r o f d o p a 】ıū n e
r e u p ta k e a n d a te s s p
o te n r ı
h i
l s e r o to n in a n d n o r e p in e p r n e in e r g ic
n e u ro n a
i i d r e n e r g ic cho ı
a ffin ity fo r d o p a m n e r g c a
It h a s n o s ig n ific a n t
re u p ta k e
l ta m a te a n d G A B A r e c e p to r s
M s ta m in e rg ic o p io id g u

d e p r e s s iv d is o r d e r an d
il in th e tr e a tm e n t o f m a jo r
e

T ıA N E p T IN E I t is a g u s e d p r im a r y
d ru
c la s s ifie d '
y it is
] S tr u c tu r a 1ı a s
d
b o w e l syn ro m e ( IB S
d in th e tr e a tm e n t o f ir r ita b le tie s
u se
n t (T c A ) h o w e v e r
it p o s s e s s e s d if fe re n t phcological p ro p e r

b ic y c lic a n tid e p re s sa
A Rv W sER ı
N s ıt is Tr ıi(
rp n f ,l
a a te b a ï c ı
q ic c o m
po d ith io id r e c e p to r (M O R ) T h e
M
u n w an t id e p r e s s a n t e ff
e c ts f fu 】】a g o n is t a t th e m u ty p e o p
tio It a c ts a s a
e cha n is m f a o n M ha is m o a c n
d ssa n t
a r g e ts fo r a n ti e p r e
o T ħe ec n
i
h a n is m b e in g s tu d ie d a s e ffe c t v e
m ec í t
o ac tio n js n o t u a r e c u r r e n tly
m u (p ) o p io id r e c e p to r s f
w e
d to its m o d u la tio n o
H is la
a Į g i
w d a r e n e J Jc " t o w e
g n ıin e H 1 ffe c ts o f tia n e p n e a r e
S id e H m
- d " " lp= o fse r , th e r a p ie s It is b e ı ie v e d th a t th e c lin ic a l e d i h d
e ıowsiness a n d ħe Jn a to Jo ic a J io id r e c e p to r p r e v io u s s tu e s a v e o w e
to its a c tio n s o n th e p
o
D
g p r o b le m s iĵ )97 9 Pi ! th e s e r e c e p to r s In a d d iū o n
O Se 3 0 l0 0 m
g e r o to n in r e c e p
toì r s
B nıa nn d N
r u ın oo ilJ] ñß p jīi its a c tio n to its e ffe c t o n th e s
a】
m e TT e. ttr a Ad
q p 1 0 2 Q 3 0 h g ta b
t Its s e le c tiv ely in h ib its th e r e u p ta k e
tr ic y c lic tid e p re ssan
w p ic a l
a n
A M I N E P T IN E I t is a n a d fa s t a c t in g
p h r in
th t ıs ex er tin 吕 a p o w e r ħr l a n
p in e e
le te n t n o re
n ım ßq o İj l Ł) fdopa m in e a n d to a sse r ex
AMRTAZA J t ħa s a te tr a
o

q cı
ic c h e m ic a ıs tr u
c tu re an d is s ifte d as a n o ra dren e r g ic

X X X
ngative ıs e d b a c k
. Th e to

X
pneswı
aptjc n
".X T u '
t t
er v e a n d c a u s in f d o p a m in e
g an in cr ea se in m o
r e le a s e B lo
Ţ c kad e

o rep
h e p h r in e a n d s e ro

itr ip ty lin
to n in
h
a c

e re a s
t io n s o o

th e b lo c k a
d o p a ın in e r g ic s y te m s a r e
d e o f n o r e p in e p h r in e a n
m

d
o re s ig n

s e r o to n
ific a n t th a n
in re u p ta k e

r a in in e o r a m e w
il n ip

Scanned by CamScanner
r蟹


V
3 2o ı r屬國IA Te ' " k fP h
g
. o o "
.
.
Egao fD r c e n t = "121
Y ı '" a c
o .. IN e ~ °' " ・- II

D ose 15 0 30 0 m g

C la ı
llc a tï o fA tı
a n x ı
e ty D r u g s
国 A N T Į A N X IE T Y D R 醒目
ss n o n

c le a r ly id e n tilia b le ā tı o c ke
p* ı rs
s tim u lu s It is a co m m on rea c tio n to s ig n ilic a n t lif #ljv l ı
ï J: B e nz o dı
az e pı
n e s A za p ir o n es s s e o v e
e s tr e s s is P ro p a no l
see n
in « ]w
c h lo ro d la z e p o x ld e G e p iro n e H y d ro x y z in e
m ıın e ro u s m e d ic a l
d is o rd e r s fe g h
} p e r th y r o fd is m hıy p o g ly c e m ia ls a p lro
p he o chro m o c t ne
c o m p le x
p a it ia l s e iz u r e s p u lm o n a ıy d is o r d e r s a c u te m o c d i y om a r=nJ f L o ra z e p a m
y a r a l in ia r c t io n Ir ıt
w ith c a ffe in e o r v a f io o x jc a ti A lp ra z o la
u s s u b s ta n c e s o f a b u s e ) A m
n x ie ly js a ı m o s t jn v a r ia b l
o n IN ï& \ M c
y a c c o m p a n ie d b
y
T a c h y c a r d ia a J ita lio
p p n s c h e s t ti h tn e s s d ia h
g p o r e s is d ia z t p ln es
7 B r e a th in d iH ic u Jlie s Ben z o
g n ř fJ
7 N a u se a d ia n ħe a in te s tin a l d c o g n itiv e fu n c tio r ıs T he
B z 2 is in lv e d in o ry m o to r s e n s o ry an
p jn g v o lv e d s le e p
a am lı
in v o m e m
" In
1 tiv tio f th e r e c e p to r r e s u ıts
W m ou M J . ? t c v t o r is a Ijgandated c 1× h a n n e l an d G A BA ac a n o

Tĥ n b in d ıin h ib itio n a n d c N s d e p r e s s io n B z 1 to
e s y im
p a th e tic a d n e n e ı ic n e r r in w a rd fı
o w ofcl w h ic h ca u ses c re a s e n e u ra n a
g v o u s s s te m
y re ı th e p to
y to b in d in g s ite s
sam e re ce r

- £X i t Į į į X H i M
e a s e s e in e
p h r in d p to r s u b ty p
d t s im pı o n
p e an
norepinephiin, ť v T B z 6 r e fı» s to d is tin c t re c e es a n n o

m o e c u le
ı
s tim ' ' ' ' " ,
u la tio n o f th e to r s i. ' h d .. " u æ s m . " '' "
p in
"
en d o c r in e s J/s te m '' " . . '" az e e re c ep
th a t w o rk w
m a y r e s u lt jn th e s im u lta n e ll it c a u s e s a ta x ia an d in th e lim b ic
ith e p in e h r in o u s r e Je a s e
o f h n d b r p h fn s it a c ts a s a n tic o n v u s a n t in th e c e r e b e u
ı m
p e an d n o r ep in e h r i b ra in s te m a n
th e
p n e to ffe c ts d is tin t h o m
p r o d u c e p h y s io Jo ic ffe c ts tio n a l b e h a v io r A n x io ly tic e a re c
g changrsuchas an d o o r tic a l a re a it a e ın o

:T m ase d bla d d e r b o
w el a n d g e n ita l fu
n c tio n in g an d in d b Jo iv d a tiv e h y p n o tic b y a c tin g o n th e
ı im b ic s y s te m a n d th e
cr e a s e
o d n o ・ to lh e Be n z o p in e s a đ a s a s e
d i? e
t t l l tim e
t n ? M s le e p a n d s ta g e
4 s le e p b u t in c r e a s e o a s e e p
) ¡»il Tf J ı
l s u b c o r tic a 】c N s T h e y s h o r e

t yjT
i d l il b l
tia l b e c a u s e th e y a r e s
a e
o w e y a v a
T h e s e m e d ic a tio n s h a v e M g h a b u s e p o te n

e u r a l d is c h a r g e s in th e p a
n
tie n t d u n n g
a n d d o ra z e p a te s u pp r e s s
? o n a z e p a m d ia z e p a m


r rłĥ ¢
Ţb \ h R r ı
tr a n s i i in th e m o to r c o r te x
i h ib ite d b y d e p r e s s in g n e r v e
m s s o n
s e iz u r e s s e iz u r e a c tiv ity is n

,= !: h a s h ig h
'
h ' Ė . C lo n a z ep a m
d w a v e d is c h a r g e , " e æ .
' ' " w p r _ in g th e s p ik æ a n

:XŢ: /
,

v a r ia b le T r ia zo la m an d m id a z o la m a re
d du tio n f ben d ia z e p in e s a re
ń丁 The o n se t an ra o zo
: rc ĵ9 en o J
an d te ır ıa z e p a ın a r e co n s id e r e d
'" d e re d sh o rt a c tin g a lp r a z o la m lo ra z e p a m _ a m
. ' ' " . ' " a ,
a n d c lo n a pam a re
p o x id e n
ze
c h lo r d ia z e
u ra z epam
N o ra d e rı
in in te r m e d ia te a c tin = an d d ia z e p a m
e
ĵ jĥ ih Đ í ı j m
5 H y d ro
x y tı ta m i
y n e n a l b97rjbir
co n s id e r e d lonacting d r u gs

Scanned by CamScanner
3 22 ı r j A Te x tB o o k o fPha rm a C 0
ı !V ° ï o Ðıo f D r u A c tin g o n C e n tr a ıN e rv o u s S E te m ll : 13 2 3
U I pha r r a C 0

a n O R D I A Z E p O X ID E It is an a n x io ly tic b e n z o d ia z e p in e d e r iv a tiv e w ith


d a tiv d It h a s a ls o b e e n u s e d in th e s y Jm p to m a
se e a n n e s ic
an ı p ro p e r tie s
a lc o h o l w ith d r a w

G A BA
h 】a r i z a t i o n
m e đa te d c h lo r id e in H u x
萋 th r o u g h G A BA r e ce p to r c h a n n e ls c a u s in
g m em bra n e

U It is a n x io ly tic b e n z o d ia z e p in e d e r iv a tiv e
X
ıæ an w ith an tic o n
Į
w
a m n e s ic

ith d r a w a
P
L
It lıa s a ls o b e e n u s e d in th e s ym p to m a tic ,
Ţ Į XX

thoughtheitstimu】
Sh
atetheGABAreceptorsjn th e a sce n d in g
'

.
, # 3 lài
\ ce G A B A is in h ib i
w p to tim la tio n in
ji
R e ce r s u crea ses in h ib itio n an d bl th
ん llo w in g Bm la li. . f th , b , a in
"īt) :jtjfe
. u o " " e tic u l' " ' ,

E d N tm A po
n n e«
Ompam T a b 1 o 3o m g N ov o xa T a b 1o 3 o
pam
1 5 m 吕石山 m g Oi'eqī 1o

t1ń is 2 5 hrs
LO R A ZEPm n is ly e x c ite m t
a
i n e d r u g u s e d a s a n a n ti D iz in n a u sea h ea d a c h e lig h t h e a d e d n e ss ra re en

e ffe c ts It a 】
s o ha s
hypno
a iw iė ty a ge n t w ith fe w s id e Jbs id¢fęç ţ s z ess ,
dv ta g e s o v e r o th e r
a n tic o n v tıls a n Ļ a n d c o liz e d a n x ie ty w h e r e it h a s a an
be e n Ħ op o sed a s n s id e r a b le d a tiv d in th e tr e a tm e n t o f gen era
se e p r o p e r tie d a n d h a s u Ëe a It J is u se d does t ca u se
s in e s s )
a p r e a n e s th e ti / n o
c a g e n t It b in d s to t ca u se s e d a tio n (? o w an
llo s te r ic it d o es n o
gs b e c a u se
w h ic h a r e an a s ite o n d
p e n ta m e rĵ c io n o tr o ic
p to
G A B A ・ A iŊe c ė to r s
p n annxiėty ru

in h ib ilo ı W rs h th e
c N s B in d in h i l d en den ce
y n eı
u o b a n sm itte r G A B A g p o te n tia te s th e e ffe c ts 6 f th e :İ O!rĮ ancę9 p y s c a e p
w h ic h
r w llo
u p o n b in d in g o p e n s th e c h lo r id T Ds A ip a r B u s p in
e c h a n īıe ıin th e rĮ DsĮ Ģť +al5 g O D
a w in g d ı】 n x
o irid e in Ðu m
x an d ca u s in g hı e
y p r o le r íz a tio n o f th e n e u r o
n R e fe r p a g e y\hĦlpÑainie B u s c a lm 5 1o m g ta b

U ıe a Į t is u se d to tr e a t a n x ie ty s ta tu s ile p tic u s
an te r q ep
g ra d e e s ia
an u ı An d fo r se d a tio n in d u c t io n a n d
, ix ib Ðtn b lĵ ĥ

b n r 1 B e r r b rt
ħ)P n o tic a c t io n s th a t js e flic a d
o u s jn th
e h ea bn
a g o r a p ħo b ia an d in g e n e ra liz m t o f
p a n ic d
e d a n x ie t
y d ia o rd e ıs It b in d
w h ic ħ m e d i n o n s e c ifi
p c a lı
a te s s le e
p an d BN z 2 w h y to b e m o d ia z e p in e
ic h a ffe c ts
m u s Èë
ı
i tėį ái£
O.

Scanned by CamScanner
J
}
【 r l A T e x t ßo o h o fp h a '" a '
"0@ (v o
l t
325 ■
PR O A T E It p p lie d th e s o d iu s a lt v a lp r o is o d iu d iv lp r D e
nw v A L
su a s m a te se m m o r a x
.
se d a t iv e p r cp e ñ ie s oŕ ħydnwili o cc u r a l th e su b c o r Łic a 】Je Ţe l o f th e C N S S e c o n d
a

in 뎌 l
9自
,

ż , ī İ k H 3 . In th e tr e a tm e n t o f e p ile p s y -

山 ity d o 繚 5 0-2 0 0 \ A m ax 琨 2 5 m 吕 怡 乜 10 呷 ノ山 村 s 厍 2 5 m 吕/ 2 m l in i

B E T A ßL O C Ł
(E R ¢ !J m

P R O PR M Jt b ı
IO L o L o c * s tħe beb«dimergic r E W P to l s

M bc h u ıis m f ıc t io « Jt
o l e s \ \ i th s y n lp a th o o m im e tic n e tu o t ra n sm i tte r s
c a te c ho 【
a m it te s
su c ti as
fo r b in d in g a t beta{ikergíc r e Ľe
p to rs ín th e J ıe a r t in h ĺ b íti
W pa
ı th e tic s tu l at i on U ıis lts in n g
du tio in
n es u a re c n
restg h e a rt ra te c ard ia b it t
p l it
c
Sj¢
Oıic a n d di asl ic b ı
o od
pï e is m e an d Je oex o r th o s ta tic h y p o m io n ! J rr
S id e e f ħ? The m o s t c o m m o n s id e e m are Jo he art ra
n a u se a an đw ea h e ss a r t im in
w er d ia īr h e d ty e e
a
y s į Łios
ı '

t e ss T ħe s e rio u s s id e e «ecr are A U e r g ic r e a c t io n s Bre a tM n g

s lm h e a r t r a '" s " ll i
n é

m W
j8 T a jn e
P 피 e nc
Ħ p au se a n d an x ie ty
x
D05Theņpmmñ
B ra n d da1oł
=ge40mggcipi
isio-aomgmen3-ļtmeswday
n am A
b e fo r e m ı
s a n d t b e d tīm
sTABLIZG
e e a a e
M m g tw ic e d a ily 國 A N T I M A N IC S o R M O O D
(c o n g n itiv e d is o r d ) It in c lu des
g a n ic b r a in s y n d r o m e
ers
It is an a cu te a n d ch ro n ic or

b b fte n d e fin e d It is ch a ra đe ń z e d by
d e lir iu m em en tia to x ic o r p a th o lo g ic a l i
a s s can e o

co n fu s io n d is o r ie n ta tio n d e fe c tiv e m e m o r y a n d d is o r g iz e d b e h a v io u r
a n

re a s o n i ng is ter e d .
ho u h t , e h a v i ou
mo t ion , g r an d al

'
Së*ii§
hrenia (s p lit m in d )

f p e r c e p tio d in te r p r e ta tio n fr o m r e a lity in a b ility to


In șM zo p h r e n ia th e r e is sp littin g o n an
'
\ 郵 ëŕ e n tly
lity a n a

tate s It is m en ta l d is o r d e r c h a r a c te r iz e d b y a n
im p a ir e d s e n s e o f
it
re a

e r s i st an t de l us i on s ( fal se be l ie ). h e r e is los s of ins i gh t int o ab n o r m a l y.


f

chan g e in d b e h a v io
"
Nfaidisorders In th is co n d itio n o f a n in d iv id u a l th e r e is m o o u r as

in
du d s le e tr o lliıb le th o u g h ts an d
in ita b le m o o d, re ce p u n co n

v ity v io le n t b e h a v io u r

Scanned by CamScanner
a 齒国团团
缶 쐬

ru ' u co w o f D ru g s A c B iE

L& ÆĒ U J Ðū N
o n C e n

e r
tr a ıN

IW
e rv o u s e m ı
l 1 32 1

(ii» D e p n e s s io n O n e (in d iv id u a l) m a y fe e d s a d n e s s , lo s s o f in te r e s Ļ p le a s l ır e
gu
p h y s ic a l a n d m en ta l s lo \ g m e la n c h o lia a n d h a s s e lf d e s tr u c tiv e id e a s

N eu ro ses T h is d itio is le s s
co n n s e r io u s p a tie n t h a s a b iliv to n
lı d e r s ta n d rea h ly
It is Į
an u n p le a s a n t e m o tio n a l s ta te a s s o c ia tle d w ith w on y te n s fo n l u l e a s in e s
s
th in k a bo u tń l
a n d

P k o b ic s la te

A n & n an
ı lc d r u &
p e r s o n fe a r s o f th e u n ]m o w n or\ificpersons s ih l a tio n s o r sp e c ilic o b je c ts f
w d r u g th a t s ta b iliz e s d by
a bn o rn u l p s y c h o lo ic a l s ta te o f
g ite m
m o o co n tr o llin g s y m p to m s o fm an ia th é
exc en t

A «m ic d r u g s d ı
p1
q iia t m
n a n a s s ilic a tio n
M ı
Lı u m ı

V PA
厂 u c o ・・W
G ı
ł e tio h y p o th e s is & B ip o la r s o rd e
D ı r D A ,G
In o s ito ıd e p ı n

/J rķ ğåi
s ig n a lin g


'
,ct o
lp r o ic a c id (V p A ) a n d c a r b a m a z e p in e (
f lith iu m

i
v a

h te 1 p h o s p h a ta s e a s e
Ip p In o s ito 1 4 b ip h o s p a
h e s M rr s o d iu m /m y o in o s o transporte
n o s ito ıs y n t a s
it l
in n s
C B U o n I n o s ito l p h o s p h a te (In s )
it o l 1 (n r ¢) m o n o p h o s p
p L C p h o s p h n lip a 5 e C D A G d ia c y g ly

h
h a ta s e l n 1

l c e ıo l
p

d
e n ic d ia b e te s in s ip i u s
e x c e s s iv e u r in e
S id e E ffe c ts T h e s id e e ffe c ts a re p o ly u r ia (n e p r o g
?r}nul t t M ild a ta x ia
L itjhinm th y r o id en ı a rge m e n r e m o r
ıw a s u se d d 【u in th e 1 9
g d ia r r h e a n a u se a w e ig h t g a in
litı th c e n ttu ,
ıit ıın tu b o n a b y to tr e a t g o u t L ith ilım i d h to x i ity
w e a k n e s s le u k o c y to s s a n
c
e COBI lith iu m c itr a t
e a n d lith iu
sa lķ ßh c h a ś d r o s i n e s s (c o m m o n ) m u sc u la r n e p r o
m o r o h te a r
e m o o
lith iu le v e ls an d ca n o ccu r a t
c lo s e ly r e la te d to s e r u m m
T D x id W Th e L ith iu m to x ic y is

th e r a p e u tic in d e x ) r e q u ir in g
fr e q u e n t te s ts t o
p e u tic le v e ls (v e r y n
t o th e a rr o w
do ses c lo s e ra
f lith iu m to x ic ity c a n u s u a lly b e
h ¢m iw rlith iu m tr o u g h p la s m a le v e ls E a r ly s y m p to m s o
d r e s u m p tio n o f t h e tr e a m
t en tata
h dru g a
tİ ëätë đ' b Jí r e d u c tio n o r c e s s a tio n o f d o s a g e o f t e
n

i i l t y c o lla p s e
p r ıo sphi
in o s ito l s y s te m
w he re ı
ith itıın
】 iŕ ilð äė f 2 4 t 4 8 h o u r s L ith iu m a t M g h to x ic d o s e s
a te r o
s e z u r e s c r c u a o r

o f gen in h ib its
e e cp r e s s i
on fo r ái(inetics
ŕĖı Th e V o ı
u m e o f d is tr ib u tio n o f lith iu m a p p r o x im a te s th a t o f to ta l b o d y
- ' d n Įs a u ct o n i
Cascades in c lu
X ding. į ;į 】is p r im a r ily e x c r e te d in u r in e w ith in s ig n ifi'
i
t a tio n Th e h a lt life o f e lim in a t o n o
f
' " x c ,e tio n h fe c es an d re n a l

maa
a c tip i1y fh is p r o p o r tio n a l to its p la s m a c o n c e n r
o
y p e ıa c tiv e c ir c u i
ķ h ı
ve d
mţ i?p p f lith iu m
h l tu b u le s
hprodug b
v o
b ti y t e e n a
24 h o u r s D e a e a s e s so d u m i r
Ę¢U m r e a s o r p o n
, japproximately
rĺu o J ıb ir h /
w h ic h co u ld le a d to so d iu m d e p le tio n

lo s s du lith iu m s re n a l c le a r a n ce
tic in d u c e d s o d iu
M ce
j
a or d r u 吕 In te r a c tio n s D iu re
m can re
í 11 Ða ßĵ
Tu i lith iu to x ic ry has re s u lte d fr o m in te r ä c tio n s
r
& in cre a se th e ń s k o f lith iu m to x ic ity T h e m
f rj ıi【
Đ Ðw l )d
b e tw p ir o x ic a m
e th a c in
h a v e b e e n r e p o r te d to
d
ee n an N S A ID a n d lith iu m (in d o m a n
h
a iB n ilic a n tl in t a tio n s ) D iu r e c
ti d r u g s A C E in h ib ito r s , s u c
y cre a s e lith iu m p la s m a c o n c e n r
ll in c r e a s e steadytate p a l s m a lit h iu m ıe v e ls u s e
a s e n a la
pń 1a n d c a p to p r il, ın a y s u b s ta n tia y

Scanned by CamScanner
f D r u A c t in g o n c e n tr a ıN e rv o u s s y s te ı
l 8 329
rm jA o m
Te x tB o o k o fPha rm a C 0 " c o lo g E
W rM a
°
Y l r
w ith ca ı
c iu m ha l b lo c k e rs : U
c n n e m y in m ea se th e r is k o f n e u ro to x ic ity p r o lo n g a tio 10 n o ij F W lt
n o f tħ
ffe c ts fn la r e 9 ï0
e o e u ro m u s c u
bloc】Cingagen
in d ic a tio n « It is lir s t lin
a e d r u g fo r m a in te n a n ce tr e ä b n tof b ip o la r d is o r d
en er It p
sv 9 :
re v e n l( j
du c e s th e in te n s ity ts a jn
o r re o fs u bsq u en t e p is o d e s o f m a n ia in b ip o la r a tie n ts
C o n tr a in d ic a « o n s
(1 ) s ig n ffic a n t re n a l o r can d io 】
a r d is e a s e (2 )
v asc u se v e re d e b ilita t io
d e h y d r a tio n
n «3 ) s o d iu m d e p le ã o n s in c e th e r is k o f lith iu m to x ic ity is h i h in th e s e
o r
g p a tie n ts
U se s lt is d in fo
u se r ın en ta 1«SS =i in d u d in g b ip o 1a r d is o r d e r d e r e s s io d
p n a n sc h iz o p h r e n
It is d fo i.
n k n t= e r h e a ? ıd a lc o h o lis n Ļ epileps d ia b e te s 】
iv er d is e a s e 】
c id n
a r ti
n itis s ı
e y d is o r d e r s
a co n d itio n ca ned sdxmhe d o v e r a c tinï e
an th y ıo id
O th e r tıs e s lt is u se d in d e
ı 加 e a tın t a t a s th n ı
en a H un tin g tu n s r Ł
I# p A sp G ra v e s d is e a s e h u
s im ph d is m d e r
voting
pes
a m o Ħ e n ıe n t
ca 1k d ta r a v e d y s l i n To u r et ū e s y n m Ę
M e n ie r p ķ d is e a s q cy ď ca
a = a a w s e n s a tio n in th e s Jc in (p a r e s th e s ia s ) d
b e h a v jm in p eo p ı
e w iħ a tte n tio
An a g g r e s s iv e
n d e ó c it h y p e ra c tiv ily d is o r d e r (A D H D )
L ith it m A lt m a tir e T h e s e d ru s h b ee n d e s c db e d
g » E
jnan?
/ J ŁĴ r r u r

th T o rs N tım b n ess,
Lo f a p p e tite D r y ın o u rem
g D iz z in
tin ess ss o
p re ssu re p r o fo u n d sw e a

Im p u ls iv M d in g s H a ı
lu c in a tio n s an d D is to r te d th in k in g
en e ss o o sw
e n ic
d im e th y ltr y p ta m in e ) is . H a llu c n o g
i
, rrittĦ2 F\ p s ilo c y b in (4 p h o s p h o r y lo x y N N
t t m e s fo r
u sh r o o m s ii n e co ı m o n s r e e n a
d in m o r e th a n 2 o 0 ty p e s o f m
n
su b s ta n c e th a t is fo u n
s , ın u s h r o o ın s an d sh ro o m s
i c lu d e a g ic m u sh ro o m
p s ilo c y b in n
m
;myHm th a t co n ta in
ly b re w e d a s a te a
h n r e a ls o c o m m o n
\ m e
q » )/§tŢ q o m s a re ty p ic a lly e a te n , a n d t e y
in c lu d R e la x a tio n S p ir itu a l e x p e r ie n ce s
u sh r o o m
e
A fe w e ffe c ts o f e a tin g m s

d V itin 吕
: :( , iJ ın j Ji lĮ J r H a llu c in a tio n s p a n ic p a r a n o ia p s y c h o s is N au se a a n o m

Scanned by CamScanner
1厔西园团团冤国 o f P h a r m a 圧生g y

d e s ig n d a n e s th e tic fo b th im l d hu u se
ė s ć ä iin a n m a n
m o T E pw e is
ı 】
】c a c h 】s co n ta in in g th e a c tiv e in g r e d ie n t m w as e as an r o an a
a sm a e M es ca lin e
s ih ıa tio N a d a ys k e ta m in e is a b d fo r its

t=î
o r em e rge n cy n s o w

:tīt
artiiciaw It be f th e ld e s t 】 h a llu c in g e n ic d r u g s T y p ic a
m a ly on e o o m ow n o
w
c a c h ıs b u tto n s a i e e a te n o r s o a k e d in w a te r Th ey can a ls o be g ro d d p
u n an u t in a ca iiśijle h ic h is p la c e d in
o r sm o ke d w i c o D j
o r m a ri u a n a M an y p e o p le te n d to e r ie n c e th e p s c h o liq u id h ite p o der th e la tte r o f w
ex p lly in a c le a r o r a w w
y i5 u su a
tiv
K e tam in
a c e
ffe c ß o r m e ix d
e esc a En e ? th in o n e to tw o ho u rs a fte r in g e s tio n an d its ffe c ts ia ls T h e d ru g be s n o r te d sm o ked n
i je c te d o r ın e
la s t g la
e can
p s u le s
ca n u o r ss v
p to 1 2 tic b a gs ca
h o ıu s 9 T ħe se e fóe c ts i
n d u d n c r e a s e d h e a r t r a te
】 an d b o d y te m p e r a h p la s tio ith in th a m p h e ta m in e am p h e ta m in e
ır e v o ııt itin
g H u shed d cs It is o fte n u se d in co n ju n c n w co ca e m e

S linM t:d r iı en t
e ct m n ie sw ea w ? o r d iıı
a tio n p r o b le m s Hallucinations A lte r e d ill ta k e k e ta ın in e r e p e a te d ly in a sh o rt peń o d o f tim e to p re v
p e rc e
p tio n l a ń d E c s ta s y ) U s e rs w
b o d y im d A x ie
dr M o M A ( de S p e c ia l K C a t
a ge an ïı ty ffe c ts K e ta m jn e in c lu
d m a in ta in th e p sych o ac tiv e e
J m
m e dow n a n
co
r a Se d a tio
D \n
y in c lu d e
n
D M T (N N m d
e th y lb ) p Ia m in e) o r D im itr i is h a llu c in o d K it k a t T h e ffe c ts o f k e ta m in e o cc u r ra p id ly an m a
a
ge n ic c h e n liė àl !th a t ıi z e r , a n
e
F lin g s o f
o c cı
n s n a tm u y ū ıs o m A p ia D is o r ie n ta tio n e e
a e m a z n n ia n
p la iıķ bu t ca n a ls o be ar tiñ c ia u
y s y n th e s iz H llu c in a tio n s D e lir iu m p s y c h o s is a ran o

is p r e p a r e d in
e d W ĥ ėr i it ĘfuĮ iess a
N a u se a M u s c le
g n itiv
la b m D M T lo o 】 im p a ir n ts
a a w cs li】
ce a w h ite c r y s ta llin A g ita tio A m n e s ia C o e te n
d p r e s s io
n
s ın o lc e cL T ħe id w id e f D A DT is
e p o w er an d is ń to st ftn tetment D e n
to k e ta m in e u şe de v e lo ps ra p id ly
w m il s e o
jncreasin it h D iz z in S e iz u re s T o le r a n ce
la r g e
cm
p
ıı a r e d b o th e r Sm n
as as a n u m ber o f i
r e n i・ iiśis ș tį f w s sl H ea rt p a lp ita tio n s ess

ic u s e r s
a am ou n ı fD M R d in hro n
s o ıiıa y o c c tı trir a lly in th e h u id e n f p h y s ic a l d e p e n en ce c
m ä ń dį iñ ,
r n a
The a ņd Tb e r ę is e v ce o
se trac» q t» u ıtitie s o f D h fr h j p o th e s iz e d to b e in
a re
v o lv e d in p e o le s r e o r t
ım īB u a l p p s o f c e r ta in
!tiM 7 9 J to
e r en ls s m as e a t h
The e ffe a
fD M T
en co u n te r s m y s tic a l ex p e r ie n ce s o r a lie n a bd u c tio n s p n o ilŔ ıŔ b ! 國 A N T Ip A R X İ N S O N S D
ın r indudeHallutions B o d a d
s o

a w a n e n e ss
y n s p a t ia l d is to r t io n s c h
a n g e s in
an d
perwption ]n cıe a s e d h e a r t r a te a n d b l
o o d p re ss u re A i
v o m iti
n g (d æ b a a lı g ta t io n S e v e re
y u asca ı e a ) T h e Lo n
g te r m D A ĄT u s e d o e s n t a
a n d th e r e Ė 】 it tk e v id e n c e s p p e a r to c a u s é ł ö ie ilM c C
u ıT m ın a n
g th e ]o n g te r m e ffe c ts o f a
d o e sn t
a Fp e a r ı o ¢z u s e
or any】astingp
h e a th r
p
y a h u a s c a u ś è l m ë te a
men
is a s s o c ia te d w iń s e r io u s s i?
th e d is s o c ia tiv
Iť s s till le a l fo
g r u se in a n im a ı
s b u t js ly
e d r u g is n o lo n ger w d éhiMy
m e u se d in
an d c ıy s ta llin e in a pp e a ıa a ı
ce ha
v e te r in a r
y se trin g s p u re g i ' '

a d d tiv es b
y g iv
c o iáz i p į
m a it
c o I n ın o n Iy 1a k e n e a ta n o r bro
o ra 】
ly h ta b ı
eto r
w n
ca p s u le sm o ked s n o r te d a s a
po w d er i ģëiä '

Withinlsminutesiftheħ
auuc\jsdorsmoked an d w ith in ab o u t 3o & łè è i j F
E u p h łn ia F e e lin g s o f in
v u ln e r a b i d u gs
lity an d ť § is ca lı
ed an ti P a r k in so n s
s tr e n P a r k ip
m D is o r d e r e d th g th D is o r ie n ta ti so ï
:
o u g h ts H u
a u d n a tio m
o n
Distortedrrsëtido
an d illu s io n s V io le n t o r b iz a r re beh a ııı
o rs

Scanned by CamScanner


1 3 2 ı Í I A Te x tB o o k o f P ha C tr a ıN s y s te ı
ı Ĵ 13 3 3 國
rm a c o lo g y
o gy o f Drug A c tin g o n e n e rv o u s m
(y °
■ ? a s s ilic a tio n o f a n d p a r k in s io
U j 1a r q

a c o ı

n s
d is e a s e D o p a d e c a r b o x y la s e is
f d o p a m in e r g ic d r u g s u s e d in th e P a r n s
o
i th i h l ti b t t in t h e b r a in b e c a iıs e c a r D io o p a u o e s
c a r b id o p a
s s u e s u n
e l n e p e r p e r a

默竺夢蕩 畜
d b y to lc a p o n e in

屬 蹦 王 th e b lo o d b r a n
i b a r r ie r C a te c h o l O m e th y ltr a n s fe r a s e is in h ab ite
蠶望
钿 。關 曲 口 \o ı
in 彆 ° c ro s s te d b y s e le g ilin e
。 not id B i i h ib i
l tis s u e s a n d th e b r a in M o n o a m in e o x a s e s n
e r ip h e r a
i
b o th th e p d d D 1 an D d d i t b ty p es
ļ ł DO pA C
d ih y d r o x y p h e n y la c e tic a
o p a m n e r e c e p o r s u

a la n in e d
i th e n a ttır a lly o c c u r r in g fo r ın o f
d ih y d r o x y p h m y ı an

p A (L D o p A ) It s
LE v o D o b t k o r a lly an d
U n Ľ k e d o p a m in e its e lf it c a n e a e n
o r o f d o p a m in e
e d ia te p r e c u r s
th e m b d i g i c n e u ro n s a n d
◆ 西 甲 国 画 ır 多图 自 臨 id ly ta k e n u p y o p a m n e r

耵 A m ın = m e
o s s e s th e
b lo o d b r a in b a r r ie r It is r a p
D m i n = i l q ı» i ıæ a
d to d o p a m in
ţĮ
e
c o n v e r te in th e b r a in a s

7 Ş M e ch a n is m o f a c tio n It
i
ly b y in c r e a s in g th e s to r e s o d o p e
a c ts m a in

b y d o p a d e c a r b o x y la s e w
f
h ic h is r e s p o n s ib le fo r th e
i r te d in to d o p a m n e
J
th e d r u g is c o n v e 2 D 3 D ł a n d D 5 M a in ly D 2
a r e fiv e ty p e s o
f d o p a m in e r e c e p to r s D 1 D
D m aa 0 n d0 e ffe c ts T h e r e w ith a d e n y l c y
d a se an d
m g i SF = = ıa n d o Ţe ? lĦ R l o f d o p a m in tD 1 actas w e ll D 1 a r e
in p e rip h e r a l ı
e is s u e an d b r a in Th l an ū r e c e p to r s a r e
in v o lv e d T o s o m e e x te n d th e cA M P
e c e n tr a
ıh e y e c r e a s e
h ib it a d e n y la te e n z y m e
th e r iï ı
a c t b y in c r e a s
in g c A M p le v e ls D 2 r a i d o p a m in e r g ic
d a re a s e n
d ir e c t p a th w a y s w h ic h m a y
c a iıs e e
!į Ī {: h c tiv a tio n o f in
4 In r a n d in M b it t e a d ir e c t p a th w a y s a r e
a th w a y s W n e n
cr ea s e l d t tiv a tio n o f d ir e c t p
e d cA M p e a s o a c
a c tiv ity In c r e a s B o th p a th im p r o v e th e b a la n c e e g
团团团团团团■ıA ce t姓c h o lln e i r ic a c tiv ity o c c u r s
s tim u la te d in c r e a s e in d o p a m n e g
a ııı» L
lin e
d o r p a m in e a n d a c e ty c h o

\ A C T IO N S O F L
EV O D O P A
IC A L
/
PH A R M A C O LO G

' " O r s r ig id ity Im p r o v e s


su ch " '" a se s

Tp :
~
D rag im p r . v e in ' " o f s y - " Im p r o v e fa c ia l ex p r e s s io n (m a sk lik e in
ia im r o v, e s p °s h ır e
h y p p k in e s ia / a k in e s
d s e lf
d r itin spee d Ļ facial e x p r e s s io ï Ļ ın o o
s o f p o s tu r e g a it h a n w g
Th e se co n d ary sy m p to m
T he s a ı tM w ls In cre a se s bu t n o
lı n o e d a c

& in te r e s t in U fe are B ra d u a y
ca re
a th w a y s h a v in g
do pa T h ey re8u ı a te th e a c tiv ity o f tw o p
o f th e le v o
in v o lv e d in th e a c ū o n s d ti n u la tin g D r & in h ib ito r y
th e th a la m ic
in p u t to m o to r c o r te x a n s ı

ite e ffe c ts
n
o ppo s th ļ v e m e n ts & r e d u c in g m u s c le to n e
tr ia m a c h ie v e s s m o o e n n 吕 m o
s in th e s
D z r e c e p to r th e y a r e s tim u la te d v o m itin g o c c u r s
r e a ls o p r e a e n t in L T D w h e n
e r ece p
to r s a
i e
D o
d in p e r p w i h b e fo r e e n tr y in to b r a in T h e d o p a ın n
h e D O p
A le d e c a r b o x y la te
c v s T ti u la te d e a l d in g to ın c r e a se
t h a lp lıa a n d b e ta r e c e p to r s a ıe s m
nn * p o r ıir e d in p e r ip e r y ,
e in c r e a s n s io n o c c u r s
le v e ls a r S t i p s t a l h y p o te
h c a r d ia In c t e a s e d b lo o d p r e s s
u re o m e m e s o u r
Do p ı r a te , T a c y
in h e M t c b lo o d v e s s e ls 1t a ls o c
a u ses '
s o c a u s e s v a s o d a ta o
il ti n In s p la n c h n ı
- In e a ı
Fı & 5 7 A sw ie ı
ııa tlc r e p n e* e n ta tı
on o r
n s w . !łH e
ı
d ıs c a te c lıo ıo b
m e y ı D o I l[ \ v n » ııiu ıľ rl
t

s u b ty p e s

Scanned by CamScanner
954 ı l l
ĺw
A Te x t B o o k o fP h
月■团团团团■
a rm a
C O ı (v U
d e c ıe a s e in cw t ra l sm p ıh e tic o u tH o w d tu lp h a 2
u e a re ce p to rs n e g a t iv e fe e db
d 《 ıe a s in g n o re p in e p h r iııe zl
. ł

富国殂丽园ı

E » d o « r i n D ūp m in e c B d n in e a s e fp la c tin
e a se o ro a ls o u s e d in h y p e r o r o 1 À į Į ij =

T
H
Ţ Į
,
n # h m d D y ıı
c in e s ia s V
a d v e r s e e ffe c t r e la te d t
e ry im p o r ta n t
o d o se f l9
n rt
Pha c o * i n e t i æ It is
p id ly a b s o r b e d fr o m
r = a ◆
ra
th e s m a u in te s tin e s 1
p ty in g ı
egradijz£
― ― o r L a s u ıc e m f it is s lo w T h e le v o d o a i
p s e x p o s e d '"
p r « ia ıt h g u t w a Ľ & fo r a lo n g e r tim e It is l
e s s a v a ila b le to
b a r r * r Æ e a m in ıo a c id s p e n e tr a t e b lo o d b r a in
p r e s e n t in fo o d c o m p e te fo r th e s a m e c a r r ie f
b io ï r a iı ty T lıe ıĦ / o d o a u n d e r
r o r a b so r
p tio n le s s respo n se s d e c lin e (P r d b a b ly d u e to
p g o e s M g h fir s t p a s s in g i M u c o s a & ith L D O P A w hen Ļ D O PA
l i v e r It is au y co m b in e d w
d in
s a d ab łi it \is u s u r iın a n ta e
h e a n y & c e n tr a lly It is e x cr e te d th r o u g h u r in e d e r iv a te o fa d am a n ta n e Ľk e a s iın ila r d r u g
A d Ħ e n e E f f e It c a u to le r a n ce ) I t is a
se s N a u se a V o ın itin &
p o s h u a l h y p o te n s io n c a r d ia c a r r h th lls to g e th e r
e t m b e łio ıı o f y m ia s
th en d in g s o f th e b r a in ce
an d a lte r a tio n fr o n erv e
o f ta s te s e n s a tio n L o n g th e r a a r s to b re le a s in g d o p e m e
t an ta go n is tic
h a s N M D A re c ep o
A bn o rm al ' e r
ın ñ d a n x ie t p y lħb u tl it ä p pe 1t a ls o
y N ig h tm a r e s s e v e r e d e p r e s s io n m a n i p h r in e resp o n se
a h a llu c in a t io r is m
l .M th s t im l a tio n o f n o re p in e
f a a t i o n in m o to r p e d o c e d i e n ta l u
o s s k in e s is A th e to s is s u n co a te ď
y s to n ia ī r z ıJ 引 飞J ir a l p ar ūd e to b e c o ın e
=«an d X d e d fo r th e v
Apcłevocarb T a b 1 o m g / 1 o o m h D w h ic h is n e e
g L a r o d o p a L e v o p a o 5 g ta b M 2 (a n io n c m e
N ìÐJ o r
p r o te in ll b y en d o c y to s is
in id e th e c e
: tj ł
İ W n rł o n ce it is t a k e n s
C A R B rD O P k It is an inhibi, f D O P A d e c a r b o x la
o tic tr e a tm e n t o f in
ftu en z a
y se p re v e n t in g c o n v e r s io n f le a c tic
ı o r s y ın p t o ın a
» It Ė u se đ in p a r lđn s o n d is e a s e to r e d u c e
o v o d o pa a t is u s e
d in th e p r o p h y ır e a c tio an d fo r
he a n tiv ir a l th t e x t r a p y r a m id a
n s
p e r ip ra l a d ï è ffe c ts \ ıu Į t is an t to tr e a
ı
t ha s n o a n a c tio n s b
y ise f
v e rse o f
A
ee s Ł

I t is a ls o u se d a s an an«parsonian a g e n

a đ io æ I t is d ıg į a
ith
ppWępetic
m ĥ ce le v d n e u ra
ĥ é+al
JAþ
w o o p a c a rb
o p a id
in h ib its th e J
C O m r f 】 do pa b !
o e r o
\ am in e an d th e d e ca rbo x ıe x Į R 2 5 8 / 1
a n om a l ie a r id d e
y la ä o n o f o x itr ip ta n to s é h to n in b ń 137 /1 0 sm o
ca r b o rty la Thķ y o o ııt g G o co v
«n ib lp t m a v a ila b le fo r
hmoro to ? e
se

C N s It
resu lts
ls o
in in c r e a s e d a m o u n t f l
o ev o d o
pa an d j,BrándNameEndmtadine 1
a in h ib its th e m e ta b li
o sm o f ıe v o d o p a in

P h m w i n a lt c an t c ro ss BBB The a d m in is tr a tio f


n o se p a ra te ta b le ts o f c a b id
l p
r o a

¢* d o p a n n in ıe w in n c o m a r e d to th
p e tw o d ru g s a d m in is te r e d a t s e a r a te tim
n /2 o f k r o d o a i
p l p ro ı
tm 8 e d & d o s e
o f le v o d o p a is r e d u c e d p
p e s Ťi
'
Pláa
k V t0 th e Į c co n c m tr a « o o fd o
Hpam
D is in h ib it th e c o n v e r s io n
e is r e d u c e d
=
R ł :J f ll iw
o f

.. h ib ito r is u s e d i
n c o m b in a tio n
V?Æ
3#êśģ pa

g x g Ħ ' " y n dopa Ħu s 2 5 m g + 1o o m g Tı


do m e t F o r te
, 6y n 4 9 p ą 2 75

Scanned by CamScanner
■ r l W B o o k o f P h a rm a C
ol0 W ・ a rm a c o ı
o g y o f D ru g s A c o n C e n tr a ıN e r v o u s s y s t e m ı
l ,,
3尹5 回国陰 :1
l£ ph

d in c e n tr a l \ th e tic tilo w d to lp h a 2 p to r ś
e c rea se
p a o u u e a re c e n e g a t iv e'
d e c re a s in g n o re p in e p h r in e
e
7 k
En d o « r in e D o pa m in e ca u s es d e m ea se in r e le a s e o fp ro la c tin a ls o u se d in h y p e rp r
It a ls o d e th e s e e t i o n o f G H in
a re a s e s a c ro m e g a ly G H in c re a s . s in n .

te ı hyc d ia p a lp ita tio c a rd ia c a rrh


ra a c ar n s
y th m ia s
! 1¡
f b l id ffe c t S o co m b in a ūo n
tin g to m in im iz e th e o cc u rre n ce o ex tr a c e re ra s e e
th e re by ac
id e fo th t o f
o r ld w a n a ge m en
Ph k in ti(s It is id d ı e m
p id ly
r
u ın a c o e ra a b so r b e d fr o m th e sm a ll in te s tin Its b io śıį L ts L ev o d o p a /b e n se ra z e a re u se co m m o n y w
es a v a ila \ J
p pc
i
a o y u as m c e m p w
a n e m
g U it is s lo w T h e le v o d o p a is e x p o s e d t o d e r a d in p a r k in s o n s d is e a se
g g .
p r e s e n t in g u t w a ll & liv e r fo r a lo n g e r tim e It is le s s a v a ila b le to
p e n e tr a te b lo o d b r a in
b a r r ie r T h e a m in o a c id s a g e n t fo r w h ic h
p n e s e n t in fo o d c o \ te fo r th e s a m e c a r r ie r fo r a b s a s a n a n tip a r k in s o n
ıt is a n a n tiv ir a l d r u g w h ic h a ls o a c ı
s o r p t io n l
A M A N T A D IN E d u e to
p r o b a b ly
b io a v a ila b iliv e ss
T h e L e v o d o p a m d e r o e s M h İ ir t A resp o n se d lin e (
b in e d w ith L D O p A w h e n L D O P
s e c
g g s p a s s in g i M u c o s a & liv e r ŕlt i i it !is u s u a u y c o m
m e la b o liz e d s
r im a n ta d in e
p e r ip h e r a lly & c e n ı r a lly It is e x c r e te d th r o u
g h u r in e d e r iv a te o f a d a m a n at n e l ik e a s i m i la r d r u g
to le r a n c e ) I t is a d
A d v e ıs e E ffe c ı It c a u s e s N a t ıs e a V o m itin ki n ic e ffe c t is n o t u
f lı y u n d e r s to o
s
g p o s h ır a l h y p o te n s io n c a r d ia c a r r h y 山 m ia s l f c« o n T h e m e c h a n is m o f its a n tip a r n s o
e x a c e r b a tio n
M ec ı h n s m o a
d i f th b r a in c e u s to g e th e r
o f a n o e
g in a a n d a lte r a tio n o f ta s te s e n s a t io n L o n g th e r a p ı s in g d o p a m in e fr o m th e n e r v e e n n g s
y A b n o rm a l b u t it a p p e a r s to b e r e e a h a s ÞÆ r【 D A r e c e p to r a n ta g o n is
tic
m o v e m e n ts m ild a n x ie t
y N ig h tm a r e s s e v e r e d e p r e s s io n m a n ia h a llu c in a tio n s m e n ta l l i h i e r e s p ° It a ls o
o f n o r e p in e p r n
w it h s t im u a t o n
h d Jtu g in te r fe r e s w
ith a v ir a l
b e la te d T e
s e e m s to e u n r
r
J ņ ıi e ffe c ts T h e a n tiv ir a l m e c h a n is m l to b e c o m e u n c o a te
d
w h ic h is n e e
d e d {o r th e v ir a l p a r tic e
B ıa n d N a m e A p o le v o ca r b T b 1 o m g l 1o om & L a d i M 2 ( io n c h a n n e l)
a ro o p a vopa o 5 g ta b n IÐJ o r
pr o te n a n

k e n in s id e th e c e ı 1 b y e n d o c y to s is
i ii ıH J o n c e it is ta

C A R B ID O P A I t is in h ib ito f D O P A deca rbo tm t E in flu e n z a


p to ın a tic tr e a
a n
y la
r o e n o
x se p re v t in c o n v e r s io n f le d tic o r s w
d in th e p r o p h y la c
en g o v o o p a
d fo
d tiv ir a l th a t is u s
to e
o p a m in e I t is u se d in lđn d is e ı
t is a n a n r a p y r a m id a
l re a c tio n s an r
p ar so n a se to re d u ce p e r ip h e ra l a d v e rse ė ffe c ts f u se« t t o tr e a t e x t
c in s o n ia n a g
o en
tip a r ı
]e vo do p It h a s n o a n t ip a r ld n so n a c t io n s b y i ts e lf A I t is a ls o u se d a s a n a n

ı
g ia
M l u n i s ın f h ę r p e tic n e u ra

c o n v e r s io n o f le v o d o
o a c « o n It is
pa
jx
' " b id o p a
m e d
in h ib its th e
w ith le v o d o '6*16hī&al po s

p a to d o p m in e a n d th e d e c a r b o x y la tio n o f o x itr i ta n to s é h to n in b o le x E R 25 8 / 1
p y G o c o v ri 137 / 1 0 Sm
a ro n ı a t ic L a m in o a ć id d e c a r b o x E d ta d in e 1 0 0 n tg
y la s e T h is r e s u lts in in c r e a s e d a m o tın t o f le v o d o p a a n d
a n
B ra ń d N am e n

o x itr ip ta n a v a ila b le fo r
transport to th e C N S It a ls o in h ib its th e ın e ta b o lis m o f le v o d o p a in
t h e G I tr a c t th u s in c r e a s in
g th e b io a v a ila b iı iy o f le v o d o p a
P h a r m a c o k in e t ic s It c a n t c r o s s B B B
T h e a d m in is tr a tio n o f s e a r a te ta b le ts o f c a r b id o a
p p
a n d le v o d o
p a p r o d u c e d g n n te r u r in a r y e x c r e t io n o f le v o d o a in
o f d o p a ın in e w h e n c o m
p p r o p o r t io n to C Ħ Ę o n
th 9
p a r e d to th e tw o d r u g s a d m in is te r e d a t s e p a r a te tim e s T iië iiis m a
p
t 1 / 2 o f le v o d o a is
p p r o lo n g e d & d o s e o f le v o d o p a is r e d u c e d P D is in h ib it th e c o n v e r s io n o f
le v o d o p a to d o a m in e th F ī D 【ĺ l ī {
p e \ tm c c o n c e n tr a tio n o f d o
p a m in e is r e d u c e d

B
10
ran

m g
d n am

+ 10 0
e an

m
d D
& T id
o
o ın e
T id o
tn u s
m e t ıs s y n d a p a 1 1 o 1 o m
S y n d o p a P lu s 2 5 m
g + 1 o o ın & s in e m e t Ë 10
g + 100 m T id o m e t F o r te
, \ 9 P Ą 2 T5
25 ın g + 2 50 m g
y J fT rc lıfq d o r ł
ų
ı
a

Scanned by CamScanner
团团团 ■自 如

336 fD A
A Te x t B k fP h lo gr o ru g s c ti o n c e n tr a ıN
o o o a c o e rv o u s s y s te ı
ı 3 37
' " a c "
y la rr m
U ]
in h ib itio n o f M A P K /E R K ı cin a s e D o p a m in e s tim u la te d g r o w th h o r m o n e b r e a k fa s t an d w ith ı
u n ch
r ë ie a ś ė e ith e r a lo n e (in earı y c a se s ) o r iı
h
p ih titu y g la n d is ın e d ia t e d b y a d e c r e a s e in in tr a c e llu la r a l i
c c u m in flt ıx th r o h fiomł
t a R e du ce b y 1 / 4 th le v o d o p a d o s e a fte r 2 3 ? s f a d d in g s e le g ilin
7A

gh y o e
g a te d c a lc iu m c h a n n e ķ r a th e r th a n v ia a d e n l l c c l
y y y a s e in h ib itio n S tim u la tio n o f
i
ô İ 场蒼
d o pam fif
'
e liı

tiv ry in th o s e w ith m IN H I B IT O R S
CO M T
a c M u scl
o v em en t d is o rd e rs e

U sæ
It is M fo r P a r lc in s o n ia n S y n d ro m e It is u se d to ACAPONE It is a s e le c tiv e r e v e r s ib le c a te c ho lo m e th y l tr a n s fe r a s e (C O ħm in h ib ito
f itr o c a te c h o ls T in e
r

hr o la c ti n em i a u e a tın e n t o f P a r k in s o n s d is e a s e It is a m e m b e r o f th e d a s s o n
It a 】
so ca u ses sm ta in e d s u p p r e s s io n l\iflaie liw t o In h ib it C 0 1vlT
s e c r e tio n in f a c ti o n o f e n t a c a p o n e is b e li e v e d t o b e th r o u g i it s a b i
in e e h a H s m
o
so m e p a tie n ts w ith a c ro m e g a ly It ls g iv e n in
h r a l ti s su e s a lte ï jn g th e p la s m a p h a r m a c o ld n e tlc s o f le v o d o p a
i e
B d N p t o c t in l S ic r ip tin ur per p u ch a s
ra n a ın e a P a r io d e l 1 F fi 2 5 d d t i u a c id d e c a r b o x y la s e 加 加 b ito r s
m g Ta b s E n cr ip t 2 5 5
g ta b s n c tio n w it h l e v o o p a a n a n a r o m a c a ı ı n o
c o n lu
m ) n fJ
n n ,ţ d s ta in e d th a n a fte r
f l d t m r e s u
p la s m a le v e ls o evo o p a a r e g e a e r a n o
ī ì b řc 【 c a rb l
dopa
d d e c a Jb o x y la s e 加 加 林 to r a lo n e I
ııs ı t
t t i o n o f ı e v o d o p a a n d a n a r o m a tic a m in o a c i
i t jï t l iJ l is r a
a d m in th e s e n ıo r e s u s ta in e d
t i f e n c y o f l e v o d o p a a d m in is tr a tio n
s e le c tiv e ie v e d th a t a a g v e n r e q u
D 2 /D 3 re ce p to r a g o is ķ ith ls rb ė ı ic s tim u la tio n In th e
n w n e g lig ib le
ffin ity fo r D 1 a n d n
a
o n d o l v e ls o f le v o d o p a r e s u ı t in m o r e c o n s ta n t d o p a 】n ln e r g
a m in e r i e
p pı
It h a s a
re c e p to r s re ıa tiv e ly te r a f{in iv fo r D 3 r e c e to r s g c a sm
gre a p T h e r a p e u tic
su l e ffe c t i\iŕ
pp e ın e n ta r
y d r u g s to le v o d o p a in a d v a n c e d c a s e s o f P D a s w ll
e c t e a s s id e ff
s iJm ū a r to b r o m o c r ip tin e b u t th e y a r e b e tb e r to l
e
p r o file is
e r a te d w ith fe w e r
C o n s e q u e n tl d o s e titr a ti g i s y m p to m s
y o n fo r m a x iın u ın im
p r o v e m e n t c a n b e a c h ie v e d in 1 2 w e k
th e s a m e ıi u e s i w h ile
y ta lc e s e v e r a ım o n th s w ith b r o m o c r i tin e R
p o p in ir o ı
e a n d
fr e q u e n ◆ u s e d a s m p r a m ip e x o le A f n o w
y o n o th e r a
p y fo r e a r ly P D a s w e lt T r ia ls h a v e fo u n d h
t em ĺq J a \ r d
s y m p to m r e lie f c o m
p a r a b le to ]e v o d o p a

ħt A 0 B IN H Ï B 】
T O R
bjzac!t) r
!
M in ľ bu v Ðı !)
o n o a m e o r c i d = P O W A O » is an h ic h
d o á i r ĥ It
em ym e w a c c e le r a te s th e b re a k d o w n f
is a se le c tiv e Irreveisble in h ib ito r
o
o f ty p e B m o n o a m jn ó x id a
e se Nilorjt Ju rr

fe c ııa ni s m o f a c tio n It is s e le c tiv e ir r e v e r s ib le in h ib itio n o f m o n o a m in


«m a o b » is u g h t to b e o f th o
p r im a r y im p o r ta n c e m a o b is in v o lv e d
d ea m ir ıa tio
n o f d o
p a ıııin e in th e b r a in It b in d s to M A O B w ith i
n th e n i r o s
in th e c e n tr a l n e r v o tıs g
s y s te m Th u s b lo c k in
g m ic r o s o m a l m e ta b o lis m o f d o p a m in e a n d
m ħ a n c in
g th e d o p a m in e r g ic a c tiv it
y in th e s u b s ta n t ia l n ig r a It m a y a lś ö C i H à s ë

' "

tr e a tm
It c
en
an . Is o

t o f d e p r e s s io n
in h ib i' " . . . z ı
n in . ' " d '" ty p e A (M A O A A U o w in it to b , a £
b ir ra H J J lıIH

A d v e r s e e ffe c ts P o s tu r a l h y o te n s io n n a
in v o ltın ta ıy m o v e m e n ts a d
p m e a c o n fu s io n a c c e n tu a tio n o f le v o d 0 rlläĮ ċg'j?
n p s y c h o s is I ts c o n tr a in d ic a te d in ón ųu
d is o r d e r s I t in te r a c ts w ith p a tie n ts w ith ċ ls iv e
p e th id in e c a u s in g e x c ite m e n t r i id it h
d e p r e s s io n I t m a y a ls o in te r a c t w ith
g y y p e r th e r m ia ŕ sŕ &láý j ţ o 19 2
t t in
n
tr ic y c lic a n tid e r e s s a n ts a n d
p s e le c tiv e se ro to n jn
r e u p ta k e in h ib ito r s
n
g
B ra n d n a m E ld e p r y l 5 m g Tab Em 12
e a m m g S e le g ilin e 5 m g Zeı
ap a r 1 25 m g

s
a

Scanned by CamScanner
I
8 13 3 9
A tı
n? n c e n tr a lN e rv o u s sm e m II
o f D r u c
a c o ı
' p l1I D
p ıw ı 1 b u te to th e d e g e n tiv e c a sc a d e in

X
e ra
to ry m e c h a n is m s c o n tń
SAG
N T M L Z H E IM E R , [ "ı '" ' il J ! ıl' "
"
[ d lo o f
d b y p ro g r e s s iv th e fu n c tio n f dem e n tia a n ss
e r c h n m a c tc r iz e dı
?meńtia o
iv c d ls o M o w h ic h im p r o v e
B e n e rn ı
;
ln n c u
i m (A D ) ¡
TA ı m e rĶ d
łh e ı ts
s a ge n

tio n o f A n H A lz h e im er s A g e n ta
C la a s ific a
th o lo 8 is t A ı
o is A lz h e m q n ıiy
l
i t nn d
ra n p s y c h ia tr s
n e u ro p n ţ er In ł 1
It is ïir s t d ¢s a ih ×J b y ıh c G e m fm lI
w o rıd w id e n s a m j
a o r c a u se o o rb ld iy y ]ib I
ť

1906 th e e p o n y m o u s s y n d ro m e s nxo8niz d
i an nï
b u n £e n h e a lth c a r e ıl
n tla lz h
r ib u « n g Io n m n jo r
o n s y s te m s łrn A
h i ı lio n c o n t
m o r ln lily in t e a s n g p p
o u n

K e x ・

M e m a n tı
n e
Ta c rı
n e
R lv a s tlg m ın e

G aı a n ta m ln e
D o n e pe z ı ı
th e tr e a tm e n t o
f
th o m im e tic o r c h o lin g e n t fo r
e r g ic a

R Iv A s T IG M IN E
It is a p a ra sym pa in h ib i to r th a t
lz h e ime r s ty p e
It is a c h o lin e s te r a s e
i f th a
a tiv e th a t
t a e
ld d e r a te d em en o
r b a m a te d e r iv
m i to m o
li t a s e It is a c a
l h s e r
l h o lin e s te r a s e a n d a c y
e t c o n e
in h ib its b o th b u ty r y c il n d t a c r i n e
b u t n o t to d o n e p e z a
d to p h y s o s tig m in e
is s tr u c tu r a lly r e la te (A C H E ) a n d
c ė ty lc h o lin e s te r a
se
e s a
i h ib its th e e n z y m
M e c h a n is m o f a c t io n 1 t n
s te m (C N S )
e s e n t b o th n
i th e c e n tr a l n e r v o u s s y
(B u c h E ) w h ic h a r e p r
b u ty r y lc h o lin e s te r a s e

t o im p r o v e d
C H E b lo c k a d e c o n tr ib u e s
t
n ıı
ı ıb o H ım ノ t o f a c e ty lc h o n
li e c a u s e d b y A HE
in th e c N s th e b o o s b h t s e le c tiv e fo r A C
) J ņ r fı
ti m in e a p p e a r s
to e s o m e w a
i I r tic u la r r iv a s g
c o g n itiv e fu n c
i
t o n n g n p a

F i* 5 8 T h e d l a sho w th e c a u s e o f / 山山 e im e ť s d ia 《a s e n tr ib u te to e n h an ce d
ı u rb in g lia m a y a ls o c o
de o f B u c hE
7o ) lï

tig m in e3 s b lo c k a
ł
x=
'

rofibrilla lėlogy
A

h
my lo id p ı

c o lin Ħ ic ı
g
a q u e d e o s itio n in th
n e u r o n a J lo s s a n d d
p e b r a in th e d e v e lo p m e n t o f . .
y s ń m c tio n o f n e u r o a n a to m ic s y s te m s in c lu d in
r a n s m is s io n a r e a m
g 出 品
'
"
a
į ii ;
ŝįğĮf\ Į
o n g th e c o ın m o n ly d e s c r ib e d ı
in d in g s in p e r s o n s w ith A D
h a d d itio n to th e s e c o r e
p a th o lo g i«a l ı
e a M res o f A D m u c h e v id e n c e h a s a c c u m u la te d th a t \ r l tl bl]rllĵ rrru r
v ť ıņn ) Tĥ ĺ u l l
t ! b ĥ ıp t J yviJ

In a d d itio n to th e s e c o re p a th o lo g ic a l fe a h u e s o f A D m u c h In r l) b ņ J ri l
u rn u ı ı
In e v id e n ce ha s accu m la te d th a t
c re a se d ox ld a tiv u
e s tr e s s d e fe c ts in m ito c h u ll j )
ı
o n d r ia l d s fu n c tio R lu rlo 1f
y n a n d ce llu la r e n e rg y

Scanned by CamScanner
tr a ı rv o u s y s te u ぴ
C e n
fD ru gž Acti o n 。

o
f
e r s ib le
bition o

v o lv e s
th e rev


f ac tio n in in c re a se
d
i m
m e ch a n s
o
e a d in g
ı to an
o se d f ty c h o lin e
3 40
1ts p ro p en ts th e h y d r o ly s is o ace

ï a se w h ic h p r e v
e s te r h
f a 8 o n is ta (B u c
lin
, as
ìd o
tio n o
l te th e ac
p o te n t a


l
an d ın a y p o s s ib y
choe re ce p to r s
e to r s
th e se re c p
a o lin e ) a t
ce t yı in h ib ito r Its m a in
ı
in e s te r a s e


l a c e ty l c
ho
ı
ı ac tin g r e v e r s ib e
1t is a ce n b a y
E p E z IL
DoN
lt f


a re s u o
f a c e ty lc h o ı
in e as

d e Ħc its is
deficiency o
d
a s a lis
a an
b
lo d co g n itiv e c o r te x n u c le u s
c e re b r a l
ss an
ith m e m o ry in th e
) ī r lj w i n e u ro n s
lo s s o f d \o lin e r g c
s e le c t
iv e
he y lc h o
aceı lin l
r e v e r s ib e


ħ o c e s s o f p r o le s ıı e ï v rJŔ
S 9 lly a c tiv e
th a t is a c e n tr a
d itin g d e cre a se d p p e tite a n d in d e r iv a tiv e
include p ip e r id
n a u se a an v o m a e
s id e 7 ħe s id e eæcı
s m ay It is
e« M s a c tio n
a
뇨h is ln o f
l k s lik e b lo o d o r M e ch
w t lo s s la c k b ı d» or n y s to o ls cou gM g u p b lo o d o r v o m it th a t o o
n
th
l
r e v e r s ib e
v o ı
w oo e
in v es
f a c tio n
m e c h a n is m
o
ķ feelin l ight fa in tin & c h e s t p a in c o n fu s io n a g ita tio n an d e x tr e m e d f
co « Ėe g m m
a g e n ts
It is p r o p °s e
th e h y d r o ly s is o
e s te r a s e h ic h p r e v e n ts
įl HJ I a n tic h o
lin ra se ) w
fe a r ty lc h o lin e s te


lin e s te r a s e s
(e g A ce
f ch o
n h ib itio n
o
pha rm am k b r tic It is w e u a b s o «b e d o ta lly w ith a b io a v a ila b iliv o f a b o u t 4 0 % in :tliė 3 m g
lln d le a d s to an
a c e ty c h o
e an
d Fh a rm a m\ i np t i is 】
ln e ar u o 3
p ı m g BÆ bu t n on 】
in ear a t h ig h e r d o se s Eliation
is ħr o u g h
ı th e u ri
n e F e a k p la m la c o m ce n ı
ıa tio n s a re abo u t on e ho u r w ith ì p ea k syn a p se s
ce t bw n
i a l ĦlJid mnrmlions a t l 4-33 h o u rs B ra n d N am e A r ic e p t 5 m g


n
i b y 15 g / daseaffï mr w
a e a se m
ee ks
f ch o ı
ty ı in e a t c h o lin e r g ic
to an a c c u rn u la tio n o a ce
th u s le a d in g
ch o lin e r g ic n eu ro n s
c h o lin
ffe c t o f n c e ty ı e
lt is a p r o lo n ge d e
sy n a pse s T he re su
tia f th e A 1z h e im er s ty p e
n ild to m o
i d e r a t뇬 d e m en o
to tr e a tn t e n t th e r
U s e ĺ lt is )ı§e d
to m o d e r a te a ffin ity fo r N
M D A
tiv e w ith l0 w
AM ta d in e d e r iv a
M EM N E It is an am an
i t t ah t b i d fe r e n t iñu y to
D A r e c e p to r a n ta g o n s
n s p r e
It is a n o n c o m p e ū tiv e N M
r e c e p to r s
k h ff f c e s s iv e le v e ls o f
It b lo c s t e e e c ķ o e x
d c a tio n c h a n n e ls
N M D A n r e c e p to p o p e r a te
i
a l d y s fu n c t o n
lu ta m á\ e th a t m a y le a d to n e u r o n
B


胃 \ イ 国虹

Scanned by CamScanner
/
.
l
3 42 = tEIA Te x t B o o k o fP ha rm a c o 1o g y
m
,T T
flin ily N m e th y l spa rhıte (N M D A
M e c h a n is n ı o f a c tio n It js a n o ncom p e titiv e lo w a )
t b in d s Io th e m
h n th e c h a n n e l is o p e n
q g n e s iu m s ih t w e
reapr an ta g o n is t th a

tic e øe c ts le a d to a s te a d y (to n ic ) le a k o f g lu ta m a te an d re s u lt in
o id
◆ If a m y ı ap
s s y ıı

exessive c a lc iu m in E u x jn p o s ls p ıa p tic n e u m n s th is c o u ld cau se m e m o ry p ro Ėle A J


e rn Ļ a c c u m u 】
th e ]o n g ı s a n d th u s d e s m
a tio n o f ń e e r a d ic a 】 c tio n o fn e u ro n s 5 n s Đ tri

(2 ) 身 ◆o d ts th e d o w s b e am
ıı e u n ic B lu la m
s o f¢
ffe c ı a be r e le a s e b y tugging th e m A io ł
į
JĴ b iv jb
c ha n n e l a n d th u s m ay im p r o v e m e m a ny a n d p r e v e n t n e u r o d e g e n e r a tio n n

Eii.XUase x infec'"n.c'"ica】'"paincanbeX
c a te g o
r ie s : (i) A r te p a in (ii) c h r o n ic p a in (
i The
iii) p s y c h o g e n ic p a n
acu ,e
t p a in h a s q
u ic k

T he a n a lg e s ic a d m in ris te r e d to an
l d itio n
It c o n c e r n s w ith p s y c h o lo g ic a co n
du res
p ro c e

e s tio n e d T he r e
de iĮ 2 1 5 in ju r e d m m 1» e r e qu
ïİn ď rec m tly w o u }ı
1 9 4 6 d u T in g w o T l
d w RT
the yr
The th e r ıuo u n d e d p a tim ts
r e p o r te d
ba d p a in o
ly 2 4 % pa tie n ts
A m a m -
in ju re d p e r s o n s on

sh o u ld h a v e th e
h ır e A n id e a l an a lg e s ic
id e a l d Jru g s a fe in n a
A n a lg e s ic d ru gs sh o u ld b e an

ħıl
i ll s ta b le a n d t a s te
1) Th lg e s ic d r u g sho u ld b e a ch e a p , ch e m ca y
e an a
li v e s e v e r e p a in o
f d iffe r e n t o r g a n s
2) A lg e s ic d r u g sh o u ld e ffe c tiv e ly re e
n a h (o r a lly ) o r
d m in is te r e d b y ın o u t
id a c tio n w h e n a
p ro d u
p
ld ra
3) nA a lg e s ic s sh o u ce
d u r a tio n o f a c tio n
b in e c tio n s ) w ith lo n g
p a r e n te m a lly ( y j
(4) It a 】
so h a s i o r to le r a n c e
h a b b it m a k in & n a r c o s is
o a n la
9 o n js t p r o p tie s a n d 4 ) A n a lg e s ic s s h o u ld n o t c a u s e a d d ic t o n al
r
w eak i d iv id u
5} 】
T3 a n ta o n s t
g te ın a n d s h o u ld a
h v e m a x im u m s a fe ty to n
f a c tio n in A l
properb butrit,i)gł
RIear 5 ) , f ltrs h o iJld n o t d e p r e s s r e s p ir a to r y s y s
o
z h e im er s
is so t fr o m cho lin e s te r a s e
rc rJiī r b
ł Ðrr
in h ib itio
ch
nol

hexpoitepontiiboh
ıaa 1iin e s te r a n m e m a n tin e is
h " ı
es se in h ib ito r ś 8 īĮI ŃA R C O T ıc A N A L G E S IC S
r

M a im a c o k i
n e t ic JF js w e u a bs o r b e d
o ra lly w ith
'
"oavailability o f
a p p ro x î m
. Te l t idö
"

ha s n o e ffe c t
P re d m ıth a n L /k o n a b s o r ti
Th
u y in th e tu in e u n
g an d p on e
d d e p r e s s io n to cen tr a l n e r v o u s
Bïan d , cha n
ge d N a rco tic a n a lg e s ic s a re th e d r u g s w h ic h r e lie v e p a in an c a u se
nam e
A x lı
ra 5 2o m g ta b le t ır ru e v a s y s te m

Scanned by CamScanner



a4 2 ı ■
IB l A Te x t B o o k o f p h a rm a c o I co ı D ru g s A c tin g o n c e n tr a l N e rv o u s s y s te m II
m {v o lu p 11arma
M h a n i s ın o f a c t io n I t is
recepr an ta g r m is t t
a

b in d s t o th e
n o n co m
p e t itiv e lo w a ffin ity N m e th y l spartabe
(N M D A ) (A ? M
vN ' \ \ H 15 8 0 P I0 1D A N A L G E S IC S A N D
ANTAGON
m a gn e s iu m s ite w h e n th e
(n c ha n n e l is o
If a m
y lo đ
ď p en
s s y ıu p tic e fn e đ s ]m d to A n a lg e s ic s a re th e d r u h ic h lie v
gs w
p p r e s s th e p a in
u re e o r su b y th e ir
S S i v e lc iu
a s te a d y (to n ic » le a k o f B lu ta m te d D lp e ıic s se n sa tio n
cz m in flu ) c in
p osıs y n a p tic n
a iın re s u lt in H r th e c e n tr a ln e rv o u s s y s te m w ith o u t c a u s in g lo ss o f c o n s c io u m e s s

X a ľ , " t ż =
em n s th is c o u ld on
c a u se m e m o ry
problemtáj
" " m e a ın f to
o n ic g lu t a m a te re le a s e
. ' p e rs o n o'
by p lu g g in g

Hīx,Za'X
' " M D
(3 ) B
Ť io
j
' " '' " m . . . T h e in tr a c ta b le p a in can c a u se
e cau se ın e m a n tin e ' fónity
??
" " " h e re h ' p h a s ic b u t
t
rs " " ・

a ū ln
, þ 9iotbe m e a su re ıy fe lt b y a n in d iv id u a L It c a n b e e x p la in e d a s a n u n p le a s a n t
d it is o n

q , į
o Ħr m o « z n a
e iır o lte d fr o d i s e a s e o r in fe c tio n ? in ic a lly p a in c a n b e d iv id e d ĵ n ı hree
u a n s m ķ sicM
& iĖón re s u m so m e

e p a in (ū ) C h r o n ic p a in (iii) P s y c h o g e n ic P
T h e a c u te p a ĵ n h a s q u ic k
c a te g o r ie s (i) A c u t
i h a s g r a d u a l o n s e t a c tio n It is
i n w h ic h is a t e m p o r a r y p a in C ır o n c p a n
ł i
o n se t a c t o
h i i i t con cer ned w ith p h y s io lo g ic a l o r a ıı a to m ic a l
t an d d ll P s y c o g e n c p a n s n o
p e r s is ta n
u
d i i t h l i d i i t d to a n
it c o n c e r n s w ith p s y c h o lo g ic a l c o n t c m n s a e
o n e a i ı
a g e s a
www w es
ld b id lan d fe
in d iv id u a l s h o u e e a sa

is n o t p T 叩 o r t io n a l to tlī e la r g e s iz e o f tu o u n a ıı
d d łe dł
o f tis s ı m i a In
T he in tm s ity o f p a in T he r e
ı ı W H d tl īu o u n d e d 2 1 5 i n ju r e d rn m īo n e
th e y ・ 1 9 4 6 d i
u r n g w o T t a r n r e c e n y
A ı ı l t a ti o n a l b a d in g e q u a l in ju r ies
ge w a s o f la r g e a
o s
ro o 1łn hsfr e s e n e r e t is s u e darrnı
r e a 1» e r e a m r

T te d b n d p a in T h e o th e T m o ım d e đ p a tie n ts
A m o n B in ju r e d p e r s o n s o n ly 2 4 % p a tim ts r e p o
a in
e r pr e s s id o n ly m o d e r a te m itä p a in o r n o p
a tu r e A n id e a l a n a g
l e s ic s h o u ld h a v e th e

ıalgesc d r u g s s h o u ld b e a n id e a l d r u g s a fe n n
i

fo llo w in g p r o p e r tie s
t b le a n d M s
1) T h e a n a l e s ic d r u
g sho u ı d b e a c h e a p c h e m ic a lly s a
g
i o f d i ffe r u ıt o r g m
tiv e ly r e lie v e s e p a n
2) A n a l e s ic d r u v e r e
g g s h o u ld e ffe c
a d m in is te r e
d b y m o u th (o r a n y ) o r
a c tio n w hen
3 ) A n a l e s ic s s h o u ld r d u ce r a p id
g p o
f a c tio n
Jn ith lo n g d tır a tio n o
p a r e n te m a u y (b y in je c tio n s ) w
u uT f q
£1 0 M d bm is m f
e o a c t io n fM n a r e
e h a b b it m a l c i n
o em a n « n e
« łı
ta M 】 ıp i
g iß n A 4 ) A n a l e s ic s s h o u ld n o t c a u s e a d d ic tio n o r to ıe m c
ıa s o
Ħ o p e r tie s
k 5 ıľ r a a n ta o n is t r an d g s a f e ty to in d iv
id u a l
g
w e a
h u ld h a v e m a x im u m
h a t t fm p o p e r tie s b u t it is j ıı
w p

b th e a đ io n s o
e n t in A lz h e im e ť s d i f th is a
g ţ ķ le a r 5
) İ ithoiı ld n o t d e p r e s s r e s p ir a to r y s y s te m a n d s o
o f a đ io n in A lz h e im s e a s e s in c e its m e c h a n is m
e ť s d is e a s e is s o d ilf rn a in n l b b ?
e r e n t fr m cho ı in e s te r a s e in h ib itio n m e m
a n tin e is

罨聲三二ご囂 二
u s u a Hy
g iv e n t a n d y w ith a c h o 】 ln e s te r a s e in h ib ito r t
o e x p lo it th e o te n tia l o f b o th o f 一 . 一 m '
ıl】eseappraadand ło g e t a d d itiv e r e s u 】ts in a ti t p
。。 。
一 。 ,一 ・・ ・ 一
p en s p f J IJ o T ï ) f 。 。 。 。 ,
P h a r m a c o k i i c It is w e ıl a o r a lly w ith a b i
Peak pı am a c t r a t i o n s a re
o a v a iıa b ilit
y o f a p p r o x im a te
'
lliöi
r e a c h e d in 3 7 h o u r s p
o o d h a s n o e ffe c t o n a b s o r tio T he ln e rv o u s
v o lu m e o f distrł p d e p r e s s io n to c e n m
tion iı 9 to 1 1 L / k a n d n
d c a u se
g p r o te in s b in d in g 4 5 % I t rl§ é âæië tM i h ı
ie v e p a in n n
th e d r u 吕s w h c
re
]N u
d y in th e
Hanged ır r ų J v z
co tį c a n a lB e s ic s a re
e y e te m
B ra n d n a m A 5 -2 0 g ta b le t
e x u ra m

Scanned by CamScanner
团 团 团■■ 3 44 ı fd ru @ra c t in g o n c e n tr a l n e rv o u s ? e m ii ,. ı
r i n Te x t B o o k o fph a rm a c o l w c w o
w ļv o
u r

M o rp h ı
n «


a s s iĦc a d o n o fN arco tic .


l . !{ ) ( pm
Ðru ¢l
r

D= c m ııı
n l
N A T U R A L O P IU M A L K
A LO ı
DS n ıl* ıım ı
ı

n ・u ro » ın s m ïı
tın

M O R ĦFH N E H Y D R
O Q I L O R ID E M e cha n is m f O p io id s
o ıp M n e is tu r a l F ig 5 1 ıM o
a n a o p iu m a lk a lo id I t is th e m ilk y rĮî【
【J J rt: l

b rm
ı la is C
: ľ X ĺį
u
17 H 20 a N 03 3 H 2 0 hl B r a d y c a r d ia . . ' " n a_ a
It is o d o u r le s s co lo u r le s s ' " ita tio n
' " '
c r y s ta llin e d ith ' ' '" m . .
i n
p a to r y d e p r e s s o
o w "
b itte r ta (M
er w a .
h i s p ir
s te o ıp h in is Flu s h in g d ia p o r e s s r e
fu l a n i r a s h u r tic a r ia
e a p o w er a lg e s ic a n d n a r c o ti I i
t s u s e d to r e lie v e eu pho ń a
s ı
eep n e ss d u e to P Jt ĵ s m o re effe c te d w h e n a d m in is t
c
Äàniciety
piħ 7 ¢ņN !tjp a tio n cra m p s a n o re x a
i i ti n i tis he a d ach e d r o w s in e s s s e ? tio n
e r e d th r o u
g h in je c tio io s is b lu r r e d v s o n n
ta k e n by m o u th » H is d in
n th a n
'
w hen . d ip lç p ia m
tıs e se v e r e p a in
R r rĵ je u ln J tr a tio n 1
p e a k p la s m
N Yh e a co n ce n
n m o ıp M n e is h e a te d in s e a le d t a đ io n 1 /2 h o u f
tu b e w ith co n cen tr te d hy d im / s c i
n je c tio n o n se
b r e a s t m ilk
ın o Je le is lo s t d e rg
a ro c h lo r ic a c id w a te r ı
Fhuı
naçokinetics p la c e n ta e x c r e te d ĵ n
liz e d b y liv e r cr o s se s
c u u n o es a c ha n g e a n d a o m o r M M e ta b o
tr a
p p n e is fo r m e d ıt d e p re sse s p ä ifi if ip u ls e ho p >i
dw a tio n 4 to 5 h o u rs
n s m is s io n a t th e s p in a l c o 'r d Je v e ıb in te r a c ti
y n g w ith o
p io id N e ßic h a lf life 2 h o u rs
re ce p to r s f J , þ¢r u r in e p la s m a

l a s th m a n cy
M h is m f r o n c h ia a P re gn
e c a n o a c t io 】Ľ
I E b in d s to a lr e e t d d ic tio h aem o rr h a ge b
yp e s o f o p io jd r e c e p to r s m u k a H y p e r s e n s itiv ity a n
r e c e p to ◆ T ħe y p r o d u c e a n a J e s ia p p a a n d d e lta r : C b n tŕ i in d ic a tio n s
g p r im a r ily b y a c t iv a tin g m u r e c e to r s H o w
p e v e u th e y A ls o
e n g a g e w ith a n d a c t iv a t
e ka
p p a a n d d e lta r e c e p to r s r o d u c in o th e r e ffe c ts
se d a t io n a n d v a s o m o to r
p g su ch a s
s tim u la t io n W h e n m o ı M n e o r a n o th
p
o p io id r e c e to r s A c tiv a ti
p o n o c c ıır s T ħe r e c
e r n a r c o tic to anaJgeMds
e p to r s s e n d s i n a ls to th e e
(A C ) to s Jo w a c t iv iy b w a o f G g m ym e a d e n
y l cy c ıa se
y y p r o te in s Gij D e c r e a s e d a d e n y I c c la s e a c tiv it
y le s s
c y c lic a d e n o s in e n ı o n o p h o s h a te (c A M p
p ) to b e p r o d u c e d A s a
y
cą}1
s u b s ta n c e c A M P is im secondä T ș 罴\ e r
p o r ta n t fo r r e g u la tin g c e ll m e m b r a n e c h a n
n e ls A r e d u c e d cixüvie+el

T ħis io n
imbaJancpeciauy th e reduced in tr a c e u u la r c a lc iu m ı
e v eı u ltin ta te ly d e c r e a s e s
f ne'"O'"JıSmjtteıs ı
io m th e c e lJ th e r e b
y b Jo c k in g o r re d u c in g p a in im p u ls e

ı} !« il i l r o iıJ J ŕt i

re sse s co u
in
gh b y d e p re ss g
co u gh ce n tr e s

tu s s iv e It a c ts n s a n titu s iv e d r u g It s u p p
A n tı

Scanned by CamScanner




34 6
四 四国国国团团园园
毽啕
州 到 劈 4d
口U '" . A 回 国 ・ ・ C Ê . tfä l N ' " 匡医理四国

lg g h /n gh d e d to
u s e fu l c u r in g d ry p r o d u c tiv co u N o t re sp o n

= X ,
ın co u o n e
'
in is
M o rp h
e
) v ith fo U o h g m ec h a n is m i
n It ]
.

fu l a s a h yp n o tic
e is u se


唏 ; m

a
o rp h in
d d i. Tio
e

"
is a u se fu l d r u g y e t its m j
a o r d r a w b a c k to th e u se o f d r u g is th a t th e r e

It is m ıly s a id m e d ic in e
b e in g u s e fu l d r u g ä n d is d e r iv e d fr o m o p iıım
籙 ; te (1 ) M o r p h in e

b
Ĥ i

ń u ı
c tio n in b lo o d
g ar c ir c tıla tio n T he M gher
h yp s im
o te ī ı d o se s o f m o rp h in e ca u se TYJFS S n ir i ļ
A c tio n o n b ilia 】y tr a


ct
h i n e in cr e a s e s b ilia r y in
b ilia r y s pa sm du e to ils p ressu re m a n M o rp h in e ev o kes d o p a ın in e D 2 a 8 o n is t
an a lg e s ic ac tio n f m o rp h in e th a t is a
a tiv o
It is a d e r iv
e
A tio n ff ts th e
c o n sm o o th m ııs

es rt iııc r e a s e s t¢m A p o M o R p H ıN E o rp h in e d e r iv a tiv e w h ic h p r im a ıily a e c
m
f u te r n a g o n is t
a
e o s an d d e c r e a s e s ts o f d o pa m in e r g ic
c o n s tr ic tio n o f b r o n peristals p ī o d e s It is Fa 1W
Th tr e a tın e n t fo r
p e u tic U o f a p o m o rp M n e a s
e ra a
se s o fM o rp h in h an is m o f a c tio n
e ec
Th r e c ıs e m la tio f p °s t
is m f tio e p b d u e to s tim u n o
p o s e d to e

!
h o a c m
1) ņ
M e c a n is p r o
Th e ın a in th e r a e
p u tic fm k n a lth o u g h it
l ıs e o o np h in e is to re ı
ie v e se v e r e p a r k in s
o n s d is e a se is u n n o w
2) M h in p a in r ır j N i Äì F !
h in tte n u a te s
o rp e is u se d In p a r tic u la r a pom o rp e a
as w operae ın e ä c in e (J b jIJi l r f p a r k in s o
n s d is e ase
3) ı im l m o del o
M o rp M n e is u se ń ıl in h e c k in g / tr e a tin d i fu n c tio n n a n an a
c
g a rr h o e a
4) M o rp h in is d in th y l ¢ p h e yl 1
2 3 betrahydropyridine(MPTP)in p r im a te s
e u se su rg ic a l h e m o r r h a g e T h e b lo o d ŕ r ł
f )rrr l
w itH M is \ké u h to x in 1 m e n

d e creaae d p re s s u re i8 lo w e re c1, b le e d in g ia

Scanned by CamScanner
j
181 A Te x t B o o k o f P h a rm a c "
o 1a

rĺ ï \a
c la = E » / Fi?
9 y !v o a
ı
u m It is . p o w e r f u l e
m e ti. M d h a s b e e n u s d f t h a t g I¢
ilįáigė
'
e o r
be łs e d in th e d ia n o s is
en
. M te
p o i.
g a n d tr e a tm e n t o f
p a r k i n s o b u t its a d v e r s e e ff
t ıs e It is m in th e b e a tın e n t o f e r til d
ec e
e c ts
y s ħın c tio n In M g h e r d o s e s it is a h i h l
】i i įi
e m e tic g y e ffe c tiv
e

H ER O 】
N ( D I A M O R P ım Đ it is a sem is y n 【
h e d c d e r iv tiv e o f m
P o te iıt a n a lg e s ic th a n
a o ip h in e I t is
m o r p It p ro du ce s e u p h o r ia an d p ro d u c e s s e v e re a
m o re
d d ic tio n It h a s

H
c o tm tr ie xs it is ls o b a n

į
a n e tL It o n se t o f h e r o in s e M e c ts is d e p e de t o n
n n th e m e th o d o f
UUing th e
bani so th e e ffe c ı
s a re th e sa m e a s ral 15 in es
o m o rp h in e T a ke b io du ces an e ffe c t in 1 0 o m u

h in
y
d e s ir a b le e ffe c ts In tr a m u sc u la . In jd n ro
W by
p r q ¢u
e n m ¢
n ra ıo f th e ce s u n
a « e ty l
g r o u p s th e r e fo r e It is 】 l
ın c «
P h in e l 】 P th a t ū m b in d s M th o io id r e
m o w n a s a p r o d r u g It is th e to r a g o n is t an d a】
5o h a s Io ca
p c e p to r s a n d
p ro d u ce s th e s u b j It is p r iın a r ily a ka ppa o p ia te r e c e p O P ia te
e c tiv e e ffe h in e
c ts
M ţ h a n is m o f a c tio n k a p p a r e c e p to r
m o rp
e
a ffin ity fo r th e
o f ffe c t s n h a s m o re

tm «m en d o ge n an es th e tic e
o u s m u
p io id
thespinaandguthostaumak
o rece
p to rs th a t a re sp re a d in d is c r e te
te in c m e» A
pı s
H e ro in a lo n G D P th e G p ro
g w ith f G ıľ fo r on
e e x ch an ge o
d s tim u la t e s th
o p ta ţ ę Ţ ec e p to r a n
c y c la s e
by n m c in

E\
g
h in
SOm e ti
m e s M u c t i o n o f th e e
nw n
d e o u s
w i id s h hëiin p io id s
de c re a s e
in tr a c e llu la r c A M p by ir ıh ib itin g
s u ch a s su
a d e n y la te
b sm ce P G A BA
s a re re u 】
g a r ly r e le a s e d in th e b r a in
w e ri is m e q ib r a n e o
n e u r o tr a n s
m itte r s
a n d n erv es tte th e le a s e o f n o c ic e p tiv e
a n u a tin g p a iń t li e ir s u b s ę q ņ e n tı
y re
b e s id e s a n a ı
g e s ia »
ı ť = Ja a e o x y o 》d o n e Hydro c o d o n e are n o IJ H Ł
t u se d in In d ia n

D IH Y i»R o M o R
pīn x E
T ħis o om d d t w ' " la b o u r p a in s

;
p «n 】n Ï ł - ĮF rr f i r r ex tiv e a
t " ū v . p re o w a

p a in
. s e v e re

la c ta ū o n r e s p ir a to r y
an cy
ity a d d ic tio ıĻ p re gn
e r s e n s it
iv
H yp
c o n t r a in d ic a tio n s
P H O L C O D E O IE
n b e lo dep r e s s io n
n p to th e o i i
p o d fa m ily o f c m o u r ly
ds 5o g to 1 5
o ın g 4 h
po tın an d it is w id e ly u se d It ĵ s D o sa ge s F o r p a in intrmar in je c tio n m

n eo w In İe c tlm o r
A d u lt O ra 1\y l s u b c u ta

1 to 3 h o u rı
y
repe a t
5 0 to 1 0 0 m &
p a in A d lt S C / I M
X

r n łn 】s ıił
e " L a b o u r u

P h o lc o d lııe h a v e b ee n r h } w ıın o t t
o m
kn o w n

ı« p
=

\ e i ıio n o f r e a p lr a tio
X
n cN s e »tc ita tio n o r o th e r

Scanned by CamScanner


'

A tin g C tr a l N
o f W c o n e n e rv o u s s y s te m ı
ı ã
ı
ţa°
l
,

ī ' xation.drowsess.
燕妻 雙
'

Ť j
..

Peak m om tr a tio n 1 / 2 to 1 h o
u r IĶ d u ra tio n o f á c tio
n 2 to 4 h o u rs Iv o n e F
k id n e y s ' i łc u o n 10
eXm te d h b n ea s t
ın ilk a n d
c r o sse s
ph ce n ta
'

f ın e th a d o n e its e lf m a y re s u lt in d e p e n d e n ce
ed u se o
u
p r o lo n g IV n u id s ,
ses It is a n ar c o tic a n a l N a lo x o n e (in je c tio n n a ]o x )02 to 0 8 m g IV ox yge n ,

g e s ic th a t f O v e rd o s e
se v e n ca n be u se d for th e T re a lın e n t o
pm in c l d in re lie f o f m o st t
g p o s to p e r a tiv yp e s o f
e p a in an d th e a in
p o f ]a b o moiiëHē i6 ,
yappresso r s
r Its p r o lo n e d
g u

k
se
m o rp h in m a y le a d It is
d w h ite p o w d e r
e an a re o f s h o r te r

ration It is a
lg e s ic It is a n o d o u r le s s c r e a m y
n a c ro tic m
n a 】ııe = . o c IN E in i i d r e c ta l
b d a fte r o r a lly i n t r a m
P e th id jn ect o n a n
H y d r o c h lo r id
te r I t is w e ll a b s o r e
e
ia L e In j p e th id in e H
v
c L p e th id i so lu b le in w a Its m o l l f o r m u 】 a is
o r id e e c u a r
In h y d ro c h ı
j 5om It is u s e d a s p e n tz o c in
n e e
g p e *ilij a d m in is tr a tio n d te r a lly (b y
h a d ın i is te r e p a r e n
ir a to r y c e n tr e a n d w e n
n
J¢ J Jr J
C 1 g H 2 8 c 1N o It d e p r e s s e s r e s p
:
::X ?ı
M ETH A D O f b lo o d
N E H YD R O w h i c h is fo llo w e d b y r is e o
W ie n t ta ll in b lo o d p r e s
s w
c r y s t a Jlin
O R JD E It
is
\ r i(l í j
J J i h j e c tio n ) c a u s e s a tr a n s
,
k w i t h d ra w a l
e po w der
w ith a b itte
a n a rco tic a n alg e s ic It is e th e e ffe c t o
f o p ia te s a n d m a y p r o v o e
r t a s It
is s o lu
o d o u r le s
s c òİ jėëė p e n ta z o c in e m a y a n ta g o n iz
b le in w a te r It is a ppșwe
M ec】 is ın
p o te n t a n a lg e ġ :Z ł
'
ll' h á .
ıa ıı
o f a c tio n M e th a do n e is a m u a g o n is t a syn th e tic o p io id a n a '
lls ic , w ĵth

壬蔻驪

N a rco tic M th d ıa w a l e î b ) ßíħ1 ĥ )
fu s io v o m ittin g
s in e s s eu p h o r ia ,
d r e g con n

H da che se d a tio n dro w


S id e e ffe c ts ea

o o d p re s s u
d bı re (w ith h ig h d o s e s )
tio n In cre ase
p a lp ita
j
H '
is , d ip lo p ia B lu rr e d v is io n ,
res
p ir a to n d e p r e s s jo
' '" ty
P re
gn la c ta tio n
h "
an c
n y '
'
i n jn u te s pe ak
d e p r e s s io t a c tio n 1 5 to 3 0
n
linia' į k i. e « c B 1M / su b c u ta n e o u s
in je c tio n o n se
e ta b o lis e d
H a lf life 2 to 3 h o
X £ ï H
. . u rs m
r e te n tio n 2 to 4 h o u r s
ra s h t tio n o f a c tio n

żTï
c o n c e n tr a tio n 1 to 2 h du ra

a īH
o u rs

0 la c e n t a
, b y li* ė r ė x c r e te d b y k id n e ys cro s s es p

Scanned by CamScanner
ı k & on
1 1 A Te x tB o o k o fP ha rm a c o o g y

d e p r e s s a n ts [ a lc o h o l
D m g in te r a c a o n s &ease e ffe c t w ith cen tr a l n e r v o u s syste

i t
ty is m o s t lik e ly d u e to its c o n v æ s o n o
m o rp h in e It is c lo s e N ty p e voltageopeated o ra l
th phen p in e
aze
fa m iw T h i
" " P・
=
Xs'.nx
a c tirń ic Fr o m e °-
du r o n a l e x c ita b ility id a n a lg e s -
N E 1t is a ııo F
T h is lts in h y p o p o lu iz a tio n d ce d n eu o . p -
c h a n n e ls res u an re
c a lc iu m A Zı 's ' " e n a to m
ET H O H E PT p o u n d itr o g
w ith o n
co m e n
a n ic
th e c la s s o f o rg
em b er
h e te r o c y c le
b e lo n g ș to te d se v e n
m
g u la r n a r co ū c th pye ra )i = n c iv a s a tu r a
ıe
co m po u n
ds co n ta g
B ran d n am e Aı
】s tra l 1o o 8oo u g su b ljn g u a l B n u o rľ
ł

D O L It is a n a n a lg e s ic d r u g w h ic h a c ı s o n o p ia te r e c e p to r s in th e c e n tr a l n e r v o u s

d p r o d u c e s a p ia te lik e a n a lg e s ic e ffe c t It h a s a n a n ū tu s s iv e e ffe c t a ls o It d o e s n o t


sy s te ııt a n
p ro d u ce
dru g d epen den ce ı h e r e is n o to le r a i ıc e a c c u r s d u e to th is d r u g Its b in d in g o f
d M 1 m e ta b o lite to p o p io id r e c e bo r s a n d w e a k in h ib itio n o f r e u p ta k e o f
p ar en t an p
n o r e p in e p h r in e a n d

M e c h a ıı
is m f
a c tio n T ra m a d o l a n d iı e s m e th y l m e la b o lite 0 1 ) a r e s e le c ti+ e ;W e a k
o
s ?

O P3 g o n is b O p ia te r e c e p to r s a r e c o u p le d w ith G p r o te in r e c e p to r s a n d itļ n ç ū o n
r e c e p to r a

a s b o th p o s itiv e a n d n e a tiv e r e u la to r s o f s n a ti ı
g g y p c r a n s ın is s io n 1 ń a G p r o te in s Th a ţ ą ç tį v a te
e ife c to r p r o te in s A s th e e « e c to r is a d e n y la te c y d a s e a n d c A M p lo c a te d a t ıç
s u « a c e o f th e
s y s te m
W er
p la a n ıa m e m b r a n e o p io id s d e c r e a s e in tr a c e u u la r c A M p
a d e n y la te
byjnhib\
q rd a s e S u b æ q u e n tly th e r e le a s e o f nocictive
n e u r o tr a n s m itte r s s u c h as
SUbsGABdopm a c e ty c h o ıin e and no ra is i t M

■画
, ł n
oTĮ ÐJĴ T u

ĺ y-
i » T " M
::? ş 0 i


毽 燐
ゾ° 嬲携

Scanned by CamScanner
C tr a l N e r v o u s S y s
te m ı
ı
355 ı
tin g o n e n
lc

3 5 4ı ı l l A Te x t B o o k o f P h a r m a c o lo g y (V ° ld

p a in «h r e s h o ld a n d a lte r s p a in p e r c e p t io n It is u se ń ıl in m o d e r a te to s e v e re p a in ıĮ a r ç q
a d d ic te d p e rs o n s ? :? īo ı? Ðr
J

I n d ic a tio ru Sev a s s o c ia te d ith tr a lic b u m s p re an aes th e tic d


e re p a in w u m a s u rg e ry c o ru g
C o n tr a in a ca tio ıu H y\ s e n s tiv ity a d d ic tio n ch ild r e n b e lo w 12 y e a rs H yp e r te n s io n
,

ca r d ia c d is e a se p r e 8 n a n c y ]a c ta tio n
S id e e ffe cu H ea da che s e d a tio n dro w s in e s s eu pho ń a d r e a m in g c o n ħıs io n v o ıııittin
g
ı ı a c ra m ps c o n s tip a tio n ra s h u r tic a r ia flu s h in g se v e re ir r ita tio n a t in je c tio q s
F
i
ın io s is d ip lo p ia Ļ b lu r r e d v is io n p a lp ita tio n in c r e a s e d b lo o d p re s s u re (w ith M g h d o s e ś)
ta c h y m d ia in c r e a s e d u r in e o u 中u L r e s p ir a to r y d e p r e s s io n
Ph a rm a co k fn e « cs IM / Su b cu ta n eo u s in je c tio n o n s e t a c tio n 15 to 3 0 m in u te s p ea k
c o n c e n tr a tio n 1 to 2 h o m du ra tio n o f a c tio n 2 to 4 h o u rs H a ? life 2 to 3 h o u rs m e ta b o lis e d
by ? ı: rJ u J r
e r e x c re te d b y k id n e ys cr o s se s p la c e n ta J

D ru 吕 in te m c t io n * 】
n c re ase e ffe c t w ith c e n tr a l n e rv o u s s y s te m d e p r e s s a n ts '
ilcŁ
ihbl,
se d a tiv e s A n t i æ D e cr e a s e e ffe c t o f n a rco tic s

D o sa g e A d u lt 5 0 m g to 1 0 0 m g 3 to 4 tim e s a d a y n o t e x c e e d in g 60 0 m g p e r d a y IM / S C
30 m g 4 h o u r ly n o t ex c e e d in g 3 6 0 m g p e r d a y IV 3 0 m 3 to 4 h o u r ly d o s e n o t to e x c e e d 3 6 0
m g p er d ay N u m ix r r

b m ıd n a m es p e n t a ? o c in e t a b le ts in je c tio n fo w w w z o c in W in ta l P e n ta w in d ċ u o w in
F o r s ta r in je c tio n 30m g per lm l In je c tio n S U S E V IN In je c tio n PEN TA W W co n ta in in g
P e n ? o c in ) N o Æ y j j

D E JE T R O P R O PO X YPH EN E H Y D R O CH LO ı
U D E I t Is a c e n tr a lly a c tin g a n a lg e s ic It

p ro v id e s e f fe c tiv e re lie f in p a in o f v g jn te n s iq It is a s lig h tly y e u o w o d o u r le §s p ó w d e r


a r y in

it h b i ta s te I t m o le n ı】a r fo r m 】
a is C 2 2 H 3 0 N C l 0
w a u
2 It is s o lu b le in w a te r J h d o e s m c it
lla v e a n t itu s s iv e o r a n ti in lla m m a to r y p p e r ty It is le s s c o n s tip a tin g a n d h a s à in
ro ''
MalËéiė
e £fe c t o fp o te n c y e q u a l to o r s im ila r to c o e n e T h e d r u g d e p e n d e n c e lik e m o r p h in ė d ó ės
d i ĥ ót
o c n ır

Ħ
niį lr J n 【ł i

Scanned by CamScanner
3 57
ı

\d e i c e in c o n u n c tio n
j
en t o f a lc ih o t e pl
m an a ge m
th e r o p io id s n
d I s u b je c ts
o rpM n e
h e r o in an o
n d e n c e to m
th e p h y s ic a l d e p e to a to lo g y
it te w ith d r a w a l s y p
m
u se s It b lo c k s m
w ill p r e c ip a
l depe n den to n o p o
i id s n a ltr e x o n e
ta b le t
p h y s ic a l y n e H C 1 5o ı g
n
5o m ta b le t N a ltr e x o
g
N a ltr e x o n e
ia 5 o g ta b le t
ne R e
Btņąi,aı v m

D e p a d e 50 m g ta b le t
ta g o is t
te n t a n d le s s to x ic a n n

th e s iz e d as a m o re po
n a lo x o n e w a s syn
N A L o x o N E In 1 9 6 o

th a n b y m o u th
it
te n t b y in je c tio n
id e it is 1 5
tim e s m o r e p ° h
a 1ėa d in g ć a u s e o f d e a th o r ld w b b l c k in g t e
a d d ic tio n
w o
y
o n is t a s a
tr e a tm e n t fo r
iś!iiÈed fo r a lo n g a c tin g o p io id a n ta g b i il b ili ty a lo n g
l o o d o ra l o a v a a
re a so n a b y g
e u p h o r ic e ffe c ts o f illic it T
h is a n ta g o n is t h a s

n e is n o t u
f 】 1y u n d e r s to o d Its
o f n a l0 x o
o f a c tio n
M ëch ä ił iàiin o f a c tio n T h e m e c h a n is m e to r s ite s e s p
e c ia lly th e m
u

tin fo r th e s a m e r e c p
antagoni?is th e o p io id e ffe c ts b y c o m p e g b in d a ll th r e e p o io id r e c e p to r s (m u
kappa

o p io id r e c e p to r R e c e n tly it h a s
b e e n s h o w n to

bu t e x te n s iv e fir s t p a s s
ab s o r p tio n
ila b ility is 2 % th ig h
pham {iŁo k in e tic s T he o ra l b io av a

B ilią ţ y t ì v l l

Scanned by CamScanner
S y s te m l
ı I ııııı
c e n tr a l N e rv o u s
s A c tin g o n
o fD ru g
le E 3 s ı r í ıa Te x t B o o k o f P h a rm a co ı
o
1 ) j

U It is p ia te d p r e v e n ts o r r e v e rs e s th e e ffe c ts o f o p io id s in c l
ıe « an o a n la g o B is t an
u d in
g
respiraq d se d a tio n an d h yp o te n s io n In th e a b s e n c e o f n a r c o tic s o r a
g o r ıis tic
d ı
e c ls o fo d m n arm a g o n is «s
tic a n ı it e x h ib its e s s e n tia lly n o p h a r m a c o lo g ie actiity
Bm d N N a lm co n e H J d r o c h lo « id e N a lo x o n e H a In
a m «
je c tio n 0 4 m g /m l

In com p a r is o n m d Ļ th e cN s s tim u la n t d r u s w h i h

佔able
d re g c a re
a p e u t ic ? u g s a re fe w an d in d e e d e H e c tiv e
as
T ħe c N S s tim u la n ts a r e ffe c ts fx th in e s a re
)u 41h e o th e r e o an

d iu r e tic e ffe c t o n k id n e y s
du
p o ijn ì, i(ip Xnthines p r o
c e n tr e e s e c ia n ce
p y w h e n d e p T= sed by n arco tic d r u
g s T ħe C N S l sm th m u s c le s
s tim u la n ts fb ro n c h ia o o
ar
fif]a s s ifie d as , e h T iii iý')Cinthines c a u
(r s e r e la x a tio n o

e ta l m
fske ı u s c le s
a a ı« ifıc a
:◆ f) (iii) c a u se d e c r e a s e in fa tig u e o
tio n
mstaanbare as
u ß in lu m e an d ac id ity o f g a s tr ic s e c re tio n s

(iv ) C a u se in cr e a s e v o
l a s th m
s e d in b r o n c h ia a
is
p h y llin e u
in th e fo f a m in o
ĮT
u ı (v ) T h e o p h y llin e rm o
dm in is tr a tio n They a re

d o ra l an đ p a r e n te r a l a
lı a b so rbe o n
X a n tM n e s a re w e

etxx.h.x' '"
c a ffe in
in
e
so m

is ı
n ia e x c ite m

h n th e o p h y u in
e s s to x ic t a
en t an d d e】
ir iu
e
ın ,
e p ig a s tr ic

i
p o is o n in g s
ffe in ra re
p a in u lc e r s c a e

d a ls o u s e d as a p h a rm a c o lo g ic a l
an
bev e ra 吕e s
CA F T EI E Į It is n a tu r a lly o ccu rń n g in so m e

th mu sc le s tim u la te s
It a ls o r e la x e s sm oo

in c r e a s in a le r tn e s s a n d p r o d u c in g a g ita tio n t o f so m e ty p e s
l in th e tr e a tm
"
g to b e u s e fu
e n

la te s d iu r e s is , a n d a p p e
,
' a r s
c dia c m u s c le , s tim u

XLX . ' " h ' ' " M ' '"


in c r e a s e d
M ' '" y , '"al ,
' '" o m ,, .

r e s p ir a to r y
' "

r a te
ir a to r y c e n te r s ,
It in c r e a s e d
o n s tr ic tio n a n d
v J :n ŕ lu ın g b r a d y c n rd in , v a s o c
m o tin lı w in g in h ib itio n o f
,
ł p ro c lic A M Ħ fo o
ťJ ï(

7 I Ju lı in tr a c e llu la r c y c lic 3 , 5 a d e n o s in e m o n p
' '
o h o s p te (c y
h a
th ln e a
i ĵ n T Jrıi
r n d e ı c y c lic A
M P It ls n o w p r o p a e d th a t x a n
h a p h o d le a te r a l e , th e e n z y m e th a t d e 吕

ıJrı
rl.rJı
ir p o

i
l .

Scanned by CamScanner
Scanned by CamScanner

8 2 j I国君 A Te x t B o o k o f P h a rm a c
oıogywi
Tn a lm E n t of o s e To a dm e r n u id s
in is ı a n ti h yp e r te n s iv e s fo r m å èa s E l, b lö 6a
p r e ssu r e 八国 m o n iu m c hlo r id e fo r in 口 e a s e o f s e 口 ìe 《io n s h e m o d ia ly s is
Bn n dN am a A d z e n ys X R O D T m ı£7 g Ta b D y a n a v el X R H
m m g su s Q v li]n c

łY :
t
r e d u c in g n o
ch a n n e lb y
11 ' " th r o g h th e
d h a lf a n h o
.g
: u
ur b e fa r e m e a ls du ces co n
d u c ta n ce
e x «z e d - a y in ' "s e It re
u p T. 4 o L . (in Hn e g ce 'o n th e ta r g e t n e u r o n

s io lo g ic a
l
ı w
ch an n e s
ith d is tin đ p h y
to c h l0 ń de
is a ls o lin k e d o n s e s e lic
f
ite d r o m
G A BA c r e c e p to s ie n t r e s p
r
Ħ°mt » e f st d tr a n
å i
an
o
In co n tr a s t to th e a
.co t. G ic a l p r o p e r tie s

in g b y CN S
d an m tid o te p o is o n
in
īi ĥ la n t an
C N S s tim
6
IJ '
as b een u se d a s a
u
in g r e p
s ir a to r y d is tr e s s
d fo r r e lie v
a r b itu r a te s
It is u se
uy b
ş a ľ e s p e c ia

Ph a m acn k īn r tin O zal do *


o h s e t a c ti Į iu b Ðn ī ü tl te r s
to 1 h o ga l
lm cen
u r d u r a tio o to r an d v a
n o f tio la te s th e v a so m

ihı
ypertensive
D ac n 4 td u G Į h b u ß ļ w a o 】s ş It a ls o s tim u
m s iM n H b ;
= w IĤ J b 9 ti v D l d ir e c t a c tio n on h e a rt
Br an d N a c ris . e le v a te d L e p ta z o l h a s n o
m e Aa
A p te r ııio x R a r
t Lw IE E R 27 m
p ø
ļ
a g o ra l A ct M
m g e th
P n r a y lp h e n id a te E R 5 4
fa r p = & m g o ra l Iriu a m Į >
nt

b
s io n
ı s s im ila r to th o s e c a u s e d y
du c e co n w
tio n ta r g e d o s e s p r o c o n v u ls a n t
d r u g s in
L o w d o s e s c a u s e e x c ita te s tin g a n ti
ls a n t fo r

' t in
co n w
\ çrqĮ i?ňţ p :ļ t.
' "o n l y u s e d f or .
z ol is as n re s p ra t'"
i s ul .
' ".
th e r a p e u tic u se o r pc y
"
a b o r a to r y a n im
ı aı
s The

N?t
şm%ęiĦ ・m e r8en c y

茉 二

Scanned by CamScanner
365

p ills f s tr y c n a u
o
n e U a
A se v e r
;y co n s tip a te d p e rso n m a y p o is o
n

U se s dJ hb e 11ia d . N n ,

Sï X
°n
ta n in g a lo in
i
p co n

te s o lu tio n a n
d be em p tie d
a
iu m p em le n gan
w a s h s to m a
c h w im p o ta s s
ibi jr G a s tr ic la v a ge is o la te d
i e a n d d a rk ro o m
f e e fr o m n o s
1ċ ėė p th tie n t w a rm q u ie t r
2 e p a
i
be g en
v
o f c h a rc o a l m a y

lon w ith m u s c le
rv in co n .i n c
so d iu m
lu tio n o f th ip e n to n e
6 Alternately to 1 o % so

c h lo r id e
r e ta x a n t a s tu b o c u r a r in e

eu bu n ı
ts

勇画■国虹
国 = 国 ■医■
a rgi

態 ビ
Ę
钮 釅

戸 鱸

Scanned by CamScanner
\ Į ŁĘHT tT
M e cha n b an o It b in d s to n ic o tin jc a c e ty lc h o lin e re c e p to rs o
f ıc tio n n e u ro n s dopanergic a ye
in th e lim b ic p a th w a y s T h is c a u s e s th e c h a n n e ıto o p e n a n d a llo w condtlctáńd ú r
c o r tic o

m u lū p le c a tio n s in c lu d in

w h ic h a c tiv a te s v o lta e
g s o d iu m , c a lc iu m a n d p o ta s s iu m T his le a d s to d e p o la r iz ä tįo
g g a te d c a lc iu m c h a n n e ls a n d a llo w s m o r e c a lc iu m to e n te r th e :X İ
te r m in a l c a lc iu m s tim u la te s v
e s ic le tr a ffic k in g to w a r d s th e w ol
p la s m a m e m b r a n e a n d th e w
e a s t 6 to 8 w e e k s
e A d u lt 2o 0 g th r e e tim e s d a ily fo r a tı
m
w
eu p h o r ic an d a d d ic tiv e p r o p e r tie s o f n ic o H n e It a l h
H eadac e ti re d n e s s s k in r a s h ıo G s o f a p p e tite , tir e d n e ss s le e p d is tu r b a n ces,
s o b in d s to n ic o tin ic a c e t lc h o li
sld e e ffe c b
, ,
y n e
r e c e p to r s o n th e c h ro m a tftn c e ı 】s in th e a ? e n a l m e d u lla B in d in
g o p e n s th e io n c h a n n e ı
bee n d in tń a ls d y in g th e tr e a tm e n t
s tu o f D em en tia , D e p r e s s io n ı

c a lc iu m c h a n n e ls ú ı¢fi It h ? u se

th e b lo o d s tr e a m
c a 1c iu m M g e r s th e r e le a s e f
g
w h ic h c a u s e s w so c o n t i
p 加印 h r in e fr o m n r a c e llu i r v e s id s to Ħ Sd riıo p h r e n ia A n x ie ty D is o r d e r s , a n d P s y c h o s o m a tic D is o r d e r s
s r c tio n in m a s e d b lo o d S u s p e n s io
En p h a b o l 1 00 m g , 2 0 0 ın g
n
p r es s u r e in c r e a s e d h e a r t l T a b le t S u s p e n s io
r a te a n d in c r e a s e d b l
o o d su a r
g ın ń ńım e s p y r itin o n ce

ti f th is d r u g if a n y is c e r ta in
loo m 吕p e r 5 m ıT h e th e r a p e u c
u se o u n

iľ y " " " " f' " " '"


. " " n d " " « d .. .
Ĺ " " ,
_ t. "
' . 1
. . . " " " " cN s " " " " «o " ar

B ra n d N am e N ic o r e tte ln v is i a t h
p c 25 m g p a tc h tr a n s d e r m a l N i. o ı
r o l ln h a l. . 6 10
. G X
C ER EBR A L A ?
V A TO RS

ıIM C ET A M It is l łıl Į u
a p V h o lr o p ic d r u g (n o o tr o i
p c agen t

J Pychodc p
:
ro b le m s in o ld age
p e rs o n s c e r e b r a l in s
: ):ï su p p o r t its su ch u ses) u tftc ie n c
y (L a te s t r e v ie w
: d o es n o t
D o lı l
g A d u lt 80 0 m g th r e e tim e ff-Jr l ,
s a da
y C h ild 5o m kg b o d
g pe r
】 y w e ig h t in th

: . :
r e e s e a r a te
p
H y p e rs e ' ' "
ty Tiv er d is e a s e K id n ey d is e a s e c a r d ia c
s id e e f¢
m S k in ra s h s le e
p d is h lr b a n c e s d
Ýî rq11
,
u r in e
e p r e s s io n
w ei ht ,
h i * u fe 1 0 to 30 h o u r s , m e ta b o lis e d b y liv e r e x c r e te d in
B ra n d g g a in ep ig a s tr ic d
ıı
am M P ir a c e ta iz z in e ss,
m : T a b le t P ıqe c a u tló fo
n s r P a tie n t
N
o t to co n s um e al co h ol.
at ion .
Wmgpermlsyrup500mgper5m
gp p r e s s 4 0o o m st imu l
" m l y Ło
er m
p 5oo g p 5 l s
g i;
8 p8 .D a to d inc rea s e
pY R m
IT IN o L・
I't "im n -
ru
m er m % grg e c r ea s e int ak e of co f fee , ea , ol av o i

Ĺ P ' " d is h ır b e d ni ・
h d r a w dr u g ter tap e r i ng of do s e .
sl ow ı y af
ņ t
m em o l
y , c e re b r a

"固
ures 裟こぷぷ
ムニ
'
。 ,。 旬
ご 。一 。。
. . .
co n c m

。 ,
tr a tio n an d
PRUGS
9 Z ftj
qi 1
' 'ı

e n t illat ion . ts si de ef fec t s ar e s e e n


T9 V 0 n į Y ín o
p
onse wi th 20 to 40 se c o n d s . t in c r e pu ımo n a r y v
d t p a in , n a 1ıs e a , v o m itin & M c c o u g h ,
m ta c h y c a r d ia \e s
noiztnoJ y in ov er do se lik e h y p e r te n s io n

Q ħfu s i
o n

Scanned by CamScanner
d ro sh ift w o rk s】
ee p

m
sı p in e ss) a pn o ea syn
e p s y (d a y tim p
e ee ee
N a rco ı
Ph ı tı
o \ıs
a rm a co o gy a c tio
Do xa p u la hn D u n d ic a
ı
gh
n c a tı
se re s p ir a to r y s tim tio n ı a c t iv a tio n o f
p e r ip h e ra l c a r o tid he
c m p to r s In h ig h e r
o re c e d o s e s it c a u se m e d u lı
a ry res r a tio
pı n ( c n t rw i J
le p ıy 1 0 0 to 2 0 0 8 o ra ı
ly m g
o n u n iııı

s tim u la tio n It a ls o ca u se C N S s tim u la tio n D o ıt A d u 1ı F o r n a rc o

In d ic a tio n s Po st th e tic r e s p ir a to r y s tim u la tio n d d ig h t d u ty s h ift w o r k


a n a es ru g in d u ce c e n tr a ln c r o tıs a y B le m ho b e fo r e s ta r tin g n
d n 吕 o
ı ra lly 2 00 m 8 o n e u r
s s io n h ro ic bs m ıc tiv e p u lm o n a r y d is e a s e ・k c n n e s ia
p re gh t a w
e c n o Nı fu s io n h y p e r te n s io n a m
n ia n a u se a d y s p e p s ia co n
D o sa Po t a th e s ia H e a d ache iıu o m
ge s n a es A d u lt IV in j ec tio n O 5 to l m g p e r k g b o d y w e ig h t n o t tu e x M S id e t ffm »

1 5 g p e r k g to ta l a s a s in g le d o s e m a x im u m
m 4 m g p e r k g b o d y w e ig h L ï V in fu s io n 2 5 0 m ıtr a c t o n se t a c tio n 1 to 2 h o tır s

in Z IO m l s o lu t io n Io r u n a t 1 to 3 m
g
ı
】 ıa b s
ı o r be d in g a s tr o in te s tin a
g p e r m in u te «s lo w 1 V » n e li c s
kı O ra y w e
pha rm * co
D ru g in d u ce d C N S d r e s s io n 200m g
e p da M d a p r o 10 0 m g
P ke M o d a le r t M o te c o

d a fın iı T ä b le t r o
A d v a
u lt In tr a v e n o u s do f 2 m g p e r k 吕 b o d y w e ig h t r e e a t in 5 M o
se o
p m in u te Ļ th e n ın T r v ] In 2 ır* n d n a m e s :
ho u rs u n till p tie ta ke n s N o t to e x c e e d 3 g r a m s
a n w a
per day ta b k ts

C h ro n ic O b s tr u tiv P lm D is e (C O P O ) Q u e s t io n s
R e v ie w
c e u o n a ry ase

A d u lt IV In f 1 to 2 in
m 吕p e r m u te n o t to e x ce e d 3 8 p er m in u he ı
v in ff io n ¢
o r n n t
m o re th a n 2 h o m

u M O NS
SH OR T A N Sw ER q
C o n lr a in d ic a tio n s H y p e r s e n s itiv ity p u lm o r ıa r e m b o lis m
y N c w se iz u re d& an le rņ
tio n o n cen tr a ı
s e v e re d ysp n e a U se w ith p r e c a u tio m in p r e g n a n c y la đ a tio n hyp th e p a in
a t i o n b y th e ir a c
e r le n s im c h iı
d rm lie v e o r su p p re s s
th e d r u gs w h ic h re
Ph arm a co k in e tic s IV in je c tio t a c tio n 20 to 4 0 n d s k A n s M ı * a rc
f e x is H n g p a in
n o n se c o n c e n tr a t io n 1 2
p ea ln
ıu n aw a re o
v id
k e s th e in d i
u a
m in u te s d u ra tio n 5 to ]O in te s p la s m h a lf life 3 to 4 h o
m u a u ts m e ta b o liz e d b y lh r r
A ge *
ı a d w T h e y m a

litie s / p r o p e r tie s
n a
e x c r e te d in u r in e
ı
ith fo ıo w in g q u a
ld e a ıd r u g
w
d be a n
D ru g in ıe r a c tio n s H a lo th a n e c y c ]o p ro pan e en flu r a n e c a ııs e « H r d ia c d y s r h y th m ia s a tu r e
\d b e s a fe in ī ı
a n

A lg e ık ı M
A n * m
B d D In f d ifte r e n t o r g
a m
ra n n a m e s o xa p ra m je f io n C a ro p ra m 20 m 8 p e r m l s e v e re p a in o
tt r ılly w ith
r e lie v e re n
ffe c tiv e ı tın e d o r a ıly pa
o r
o ıłld e
y d i i
T re a m e n t o fo v e r d o se M ito r e le c tr u d g sh hm a m n s
o n ly te s a c tiv a te d c h a r co a l A gd
n aı c ru
d
ı a cda m w

d g sho u
ld produce r ıp
3 ge k
A rw ı ru

M O D A F IN IL f a c tio n l
m g d u r in s i id
I t is o
tly in tr o d u c e d ty to th e in d v
ı u a
a re c e n
p s y c h o s tim u la n t d ru g It is t ıs c d by h ı s h ift
e m a x
im u m s a fe
ke rs d ho ld h a v
w o r n ig h t d ty p fe s s io n a ls w ho im p r o v e a le r b ie s s a n
a n s u
u ro w a n t to d W a w a ke P is d r u 8 d e p re s s re s p
ir a to r y s y s te m
to c e n lr a ı
d b 》 im p ld d e p r e s s io
is d iın
i t sh o n
a e ro v e a c y in c r e a s e a tte n tio n s p a n n e ss ) s ı u
co m p ro m iz e w 出あ s lw (s e e p ł i an d a ls o ca u se

d fa tig u ie v e s p a n
h a t reı
a n e
th e d ru gs ı
a re
dc a n a l e
M e c h a n is m o f a c tio n The m N a ıc o
ex act m ha is m f tio is unc le ar lth o W tu d ie s
ec n o a c n a u g h in s

c a n a
c ?
lg Ħ ı
h ho it to in h ib it th e tio n fn a rc o
p ta k e
a v e s w n o
re u f d o p a ın in e b y b in d in g to th e d o
o t e u p ta 】 ce p c \a ・・i
fic a
Q A E x p la ł
n
h in e co d e in e
p u m p a n d le a d to a n in in tr a c e llu Įla r d o p a m in e M o d a fï n il a c tiv a te s m o rp
cr e a se e x
g lu ta m a te r g ic It in d ııd e
d ru gs
D ih y d r o m o rp h in e
c ir c u h ile in h ib itin g g a b a m o
its lk a l0 id s h in e h e r o in
w d a fin iıis th o u g h t to h a v e le s s p o te n tia ıfo r z a h ıs e th a n (i» N a tu r a l o p iu m a A po m o rp
o id s
ı
iu m a lk a do ne
o th e r s tim u la n ts d u e to th e a b s e n c e o f a n i s y n th e tic p
o m e th a
y s ig n ific a n t e u p h o r ic o r p le a s u r a b le e I t is (in se m
k l id s pm d in e
a ı a o
p o s s ib le th a t m o d a lin il a c ts b y a s y n e r g is tic c o m b in a tio n o f m e c h a n is m s including d ir e c t (Ħi ) s y n th e tic o p iu m
lie v e se v e re p a in
in h ib itio n o f d 叩 a m in e r e u ta k e in d ir e c t in h ib itio n o f n o r a d r e n a li r b to re
e u p ta k e in th e V L P O h in e
p n e o fm o rp
in th p e u tic u s
a n d o r e x in a c tiv a tio n M o d a Ħn il h a s p a r tia ıa lp h a 1 » a d r e n e r ic a o n is t e ffe c ts b d ir e c tly (D T h e m a e ra
m e d ic in e
g g y /w
M o rp h in e is u se d a s t i v e
s ó m u la tin g th e r e c e on
p to r s JT

Scanned by CamScanner

You might also like