10.

MARKS
Explain in detail about factors affecting the absorption

Ans: ABSORPTION TOE DRUGS:

• Absorption is a process by which drug enters the systemic circulation or

blood. -
• Absorption ofa druginvolves the transport of drog across the biological
· '
mem ~
bio ,
The transport ofdrug fiom one side of the biological membrane to other side is called !.,,,-
transport.

FACTORS AFFECTING DRUG ABSORPTION AND BIOAVAJLABILITY.

~UGR ELAT EDFA CTOR S -t!_,'7""·~ ,
~TIEN TREL ATED FACT ORS. ()t>7 ~
DRU<, RELATED FACTORS: L.,. r 7 ~ '~
O · .
► PBSICAL FA
I. Physical stat · are more absorbed than the solids. ~
fystal · are more absorbed than colloids. / '
d
2. Lipid solubili or wmr solubility: Drugs in aqueous solution are more absorbe
thiiiibc drugs in oily solutions.
• Lipid solubla ttfup ?Ji ~ t e more in cell rapidly than that of water
soluble drugs. '
_..>-D OSAG E FORMS•
I. Particle size: The particle size ofsparingly soluble drugs can affect their
/ ~sorp tion. ' 0
~~, /
• A tablet contains the large aggegates ofactive co~pound may not
disintegrate even on prolonged contact with gastric and tntestinal juices and O;
are J>OC?rly absorbed. -- --
• Small particle sil.e is important fos:_absorption ofcorticosteroid ' antjbiot ice:
like griseo · chloramphcnicol, anti-coagulants. -
• Anti clmenthi ve the more particle size, these are less absor}ed.
• e drugs that are given in emulsified form are absorbed ~ g : Vita~
A&O. _.
2. Disinte
-- gration time ud dissolution- time:
I

;: :::w::th~,ch~m:::eas-m-1$.:.lbe rate of ?.~!_.o~_t,~e tab!~-~-~~ _

/ /';--;;:,::-s:;~::~:-n:tegrabon=;:.::-;:tim=e
~ dissolutioo rate is defined as rate at which the drug goes into the
solution. - - -- - - - - ,· · · -
~ Disintegration time s a
• Dissolutio,Jl.lime·is a better
measure of BA.

£We C2
 =-----____. ____ -- c· i ·' u ~,,., • .. ,: ~\ j
,
c~I ~ ) 1,r.
~ a;·o rnudatia n _..,..,..,.,. ,,,""° AtO .
c: I ...
c::.. I .....~' IIISt',,\ljt', lfrA1"r.s, ·- - ~
• Substa.n\"C" IA~ l:t<"'h..~~.. ~'""'":"' •lah,•)'I --~·••.!.'!rn ~~~, 1lyor c. I .) • Ahtorpliun <or lhc dn1p 11 olrcdrA m rhe dn,.,.. g,ndj11,:,m like )
lbe inc:rt dolurnis °';i;-,clt alk\:I 1tw •""111"1'"' Id ,o'('il ~ SI
- · . . mnM...,rpll1,1n, 1hy,ulruucc""• echl~:,ilna. d n ~ )
nu,.:lic,,mm1, . ~~ C: . --~ E "RMACOCV.NY.TIC ••;:CTOIUI: - - I•.
Cnleium and RIQ(!n~mm "'"' .. ~ 111.C aNO!llll""-'
,n .. I'/ -
\ ~'
Ir
-t;<"
•
•
C'-41 ~- - --•-' calci11111 llllCI"-' •
~,um ('h<,.<f'h,11<'-.. a d,luml ,fi,r <"alaft:rol _ . . - - --
C: . ~ • lArgc diffcn:nccs ; ill~
ac:cn in BA among !be ~c,ri,,us hum.ms. JI ) h ,. J..!"
-;"lt)--\_ I(. -- '
'
n,,•fa.:!\.'$<" "''"'-'ff·~
when '!r~ ....... . .i,s.,,rii.ml C: . --~ • Slow acctylntorsor~'!~"" the~ BA. 'S>'" t (' ·, " /.- I- l ll
h • Put aa:tylatora or1,omu,d shows lhc law BA.
-•~
C --., ~
# ~11\"S fOLOCIC\L FACTOR.'-· -- -
1 _..J. ~~TION: Thc ~~~I ~inge>rGITb~~ ~ o f
~ ~ a~°)hd,..T.U: hascs.-., ~
~ l a i n In detaU about lbe Pbase-l and Pbu.-ll ,actions of -.bolhm of drug,.
7"
,1; ~,1 • AloodypAmoste>fthcdrugSC'!_i!ltli!!..lmltonns
':•~ Explnln the factors affc<:ting tbc drug :lldio11.
'I
: 1__,_ Ans:FACTORSMODlFYTNG DRUG ACTION
1, t
,> ~ A. An uruoaiscd fonn ~ , o l ~-
13. An i<Mli:_<-ed form- t'~ solublcj .._ I .; Facton modlry the drug acdon either
dru is If the_plasma ~nrion is ~
unigaj,al ptotanJ,inding capacity of the cl~ a. Q ·ma o:,n~tion ii)_ld ac:!ion of dmgmay increase / deer~
b. Q ----::=----- (ypcofresponse is ,altered. Eg: allergy, u1iosync-,asy
& reduced so 11 reduces_n,r,: ofab50CJ>tioa..of.lbc: dna.&
cl~ ~.
2. P~ of g ~ i d lllld~~loocl:
~~c drv
~ ;#
more absorbed in the sto111ach due to the drug
e- ,-, V11rious racton arc:
~ i n unionised form in the acidic medium ~ -, V 'ody sk.5;.
~eakly basic drugs-~ ~ abmrt,cd Jbe smoll rotes.tine lhis due~ the
~ Cltistsirnmit1nisc:cTiurm in ihc albline medium.
.,,
c--1 -~ / • lt inllucnccs th£om:<.-nuution) of the drug-altered at the site o~ action.
• The average a ult dose_ rd'e:rs Jo. the ind!Yid11.ill.dos.e. For, obese or lean
__;/'In the intestine suongly acidic w basic drugs are in highly ionised form SO ~ 1..~ individuals and-!br ehlldh.-n dose W&itcuiai&i on th" t>Qdy weight basis. "\
rbey aw ,-dy absorbed.
~ I_~ ~dividual dose - BW (KR}QO><nvernge adult.dose. \) vJ ,
L ~ ~ v o l u m e , vist"Osity._~astric..contcotuU~rs_ihL_
ab~rpti~n byalttri~~~c;~ptyiog tim~.J .
~ 1.; /
•
•

Individual dose=BSA{m1)/I .7x avern e adult dose.

BSA am be calculated fro~fonnul
BSA (Body Surface Area) {m ) =8W(Kg)0425 x Uc\ght (cm)0 rux 0.00\1&4

~
~ -0
\1
J
• ,!'-D- increased ~51.111iic movcm,911mluces the drug abso~
_/L Age: .
• {.I\DTJ cholindi!cs will prolong the gastric chiptving time whicli im~irs the C ·~ • • The dose of the drug for chi\drcn.is often call:ulalcd from the adult~dosc J.
...::.=--✓--------,
cl~ ' ~ dose: Age/age+ \'2xadult dose fY oungs formula) . '.A.<,~ . P.
il>sorpfionoflhedru&
~ I d dose: Age/20x adult dose eoui, formula) ~
• [a~~• will reduce the ahso tionofthe cl~ 1
Children's may not rea<;~ to all drugs in the same manner as young u c l ~ ~ Y
Area or ■ - 1■rfxe ud Jocal clrcul1tion: . •
~ • Drugs are nions ab9orbc:d from smaJi intestine than from the stomach because CJ~ ~l'hc phannacokinet\cs of the drug may. change with the age. ~ • ~
ofl~_surlilcc: atta. _ __ -
• ~~ will maease llie-abso-rp~,io_,-'_
. C I._:;) • The gastric emptying time is prolonged :md giistric p" nuctuatcs in neonates d
inrants.
S. PrdeDCC ef otlJer ~- , ·•
C"J __';,) • The liver capacity to metabolise drugs is \ow, mial function is less in new boms.
:etabolic clearance of drugs su.ch as chloramphenico\, barbiturates, pefuillinc,
-
V i ~ I I increase c absorptio
PJi~n mluce I ral ir
CJ.. ~ /
salicylates, sulphonamides is less in infants than in adults.
11ic phannacodynamics of drugs in chi1dren may differ from that in adu\\s.
resenccofcalcimn in theJ11ilk wc.lrn:ducc thfF~on·or-
rani~ - - - ··· - ·· .
~ --~ ' • ·Some drugs.disturb the paitems of growth and dcve\opmcnt, er,: tcttacyc\ine..,;,
- --· · glucocorticoids in children.
c~ • Metoclopnunide and other dopamine antagonists 11roduce acute dyslonic effects
~
more in children lhan in adults.
/<c;
(/'~-'>
~-
'70 ')
 -~
C I .)
. .)
Ono~ .
~•""'m o"' -.:1wc nnd """" 1oxlc In nc-w ""'"'"
• Old l"<'Oplc nl,o prc,in, t f"'>t-lcr11J ,n

...
ct.~ ..i;u..imc-•"

1hon in"'"'" '

,..,.1..i,kff..
111ii Jiff« whlc Y
1 i
n c•~
C"
,. I .., /4,. ,. ur action 11 qulclt In 1/V ro uta
7. Ge•ell e facton :
,, • Vari•lion■ liitt, e p,e1ie constilutl<>n

•
Ille
dic:tatc _ gcn~ ~y _ medi11cd
<l•ITcn-nt pc,;,r tc.
. • i11 ct<lcrl)' 11nd - I -> d iffer - In drug mc:lllbofism and 1c:,ponsc:.
lnis ,esuhs in drug accwn ulat\on
. -• The hepati c blood flow and .,.... 11,oli""1
.:,( dnlp 1114)' dhnmiilh
mny prudU<lC
CI ~ and 1nxid1y.
-- -..
n:nnl functi, ,n dccli - " ith ~
. Toe rate or acc:ty\ation of fNH,
- -· Cent" '! dq,.-- ants such u h_,-pn<
\lia and lr1lft'llllhsert CI ~ Eg; L A~1 loa aad liy.!ff!lllJ'latloe o~~P .:
dllpM)oe and sulpho namid a la c;ontrollcd by auloSo
mal rcces,sive gene and dMe
-
CI ~ uals.
.
confo.,onnl s1:11c and rau in o ld l"'""l'lc .
•
of drug depend s on acctyla&or lllatua of individ
• l'll1SJ113 httlfli re of dNp such 115 di&Z,q\11111,
pdhidino is lllf8C' '" el<Jet$. 11. Metab o& dhl1n banca :
3 . S~:
: . FemaJ cs h o,-e smalle r body size and rcquin
ll doles ofloWCI' llidc ~da1 lon.
I '...~
I;..
,,-
~ haogci Tnwat cr, el-.ily tc: and acid bal~
the cffcc:u of drugs.
~ y trmpen rturc tna)'._!l'lodiry
~
In women considmtion will be giwsi lk> meo,11Qllllion.
picgnancY p11ysiological
fOCIUI, lb~ are marl<~ch allet drug
• I ~ f Eg; ~ body tempe rature only.in
lhep rese n~~
c is_rcduccd in the ~<: 1ab o\ic
..-. Drugs during pttpw ,cy can alTcct lhe C ··i '..) -;::: • V ~ effc:c:t o f ooradt enalin -
~g~ during Pffll'& l1c,' esp«i ally in dlird triJDcS
Rf "' ~/ acid ~
dispos ition.
Gastro intesti nal motili ty is redoa d_ duo '°-~~~~~~L
. f oral! ·
c- I'..) / - Presm cc of disuse :
• 0rull,'I like morph ine and chlorpromll7.ine
may produce prolonged effect in
• .
administr i:'O'L - -
lhis voluinc of dnlg dis11t'but100
C I "':) c:iahot ic patienl s.
mainly by kidneys may
Plasm a and ~ u l a r volum e expand due to Antibiotics like streptomycin and kanam ycin exctetcd
•
r: I""':) •
prove lollic when kidney function is impaiR ,d.
•
may inct'C4Scs. •
Plasma album in levds fails lhal of cu gJycoproleins
n of ocidic drug increa ses and the basic drug

inctel$CS the unbound

decreast:S-
C--., 10. Other drugs and chemi cals:
.,.- Previou.s or concu m:nl lher.rpy with ecrtain
chugs may result in stimul ation or
tractio
• Reml blood now ina-cAses due to Ibis ])Ola-c
hug are climioaled faster. _ c-1-., / inb.t'bition of metabolism of other drul!,'J.
induct ion many drllgs arc mctabohsed Cyt P-uo enzym es. 'They accele ralc
• Hepat ic microsomal enzymes UDdergo-
fast= . c-L~ / Tobacco and alcohol consu mptio n induce
themetaboll!lltl of many drugs and alters lhe etfcc:t.
4 . Speci es aad race: CL_,;, 11. Cumulation:
- .....-ff tlic?d Ng is Olltcet ed slowly , its repeal
ed admin i.stnlio n may bui\d a
~
s and race.
• Re:5p0nse to the cfnlgs may vary &om specie
y Rabbits are more resistant to eb"opine, r.ats and roice
are resistant to digitalis. e- I sufficieo1.\y higher conce ntratio n in lhe body to produc
• Eg: ~ c t inc, heavy metals.
e toxicil)I.
c•~·"~;)
__:,-- R.ets are more sensitive to curare than cats. drugs:
/ Among huma n beings some racial differenoesiequir are observed . C • --~ U . Comb ind e ~
effect o[ the drugmay varies
Eg: Black s · · and magnolians e lower co11CCJ1trallons of • When two or more drugs will be used concUtTently
· c the pupil depending upon the drug used.
..,....a1ro !11 ~I
1
-----' Tndi ic)aee1UOne er than whites. • There mny be~: Synergis~
u.A nto go~
S. Diet ud mvir ii
• ~ood iolen era with absorption of m1111y drugs. present in food and arc properly
C I '";l ~ • Synergism: facilitated or increased effect of
one drug will be produ ced by \he .
/ - Eg: Tetnic:yBiries lonn complexes w1Di ciilaum C I .J V
7
other drug js called as syner gism,
► ln synergistic pair both the dnir,<l can have the same action in
and enhances
a b ~. smoke may induce microsomal CI _:) same direction or given alone, one wil\ be inac6vc
• ~ly cyclic h)'dn>c:atbons presmt in ci~t e
lhe action ofll,c olhcr when gjven together.
enzymes result in enhanced metabolism of drugs,
c• J Synergism can be of two ways: \. Additive
effccl2. Su~
~ p t ion iacn::ascd by fpod- spironoladonc,
· ~ t i b n dec:rased by food- Ampicillin. rifamp
1/The dose~ypn otics requir
chl~ qui!J~..Oboflavin.
icin, tetracycline.
ed to produce sleep during daytime is higher than
ce sleep al night. ..-. ' ··.
dJe dose required to produ
·- · :,· ·- ' ·
•
c. ~
-
c-.:.• --:)

►
a ~ t.
► Addit ive effect Summ ation
· in same direction.
The efrccl of \he \WO drugs a:
► 7:ffc ci ofdrug A+B= Effoc l of drug A+ Effect
of ilnig B.
6. Router ~ I ad,!!!!! than oral doses partic ularly in ► Eg: Aspir in+ paracetamol- Analgc.c;ic I antipy,C\ic.
~:::>lb¾vi:nuus d09CS of the drug are usually smaller c- ~ Nitrous oxide+ ether- General anaesthetics.
ca,e ofdrugs which are incompletely absorb
ed orally.
Bg: Morphine and ~goxio c: ~
c-".'.i:
~~
 ~
:-a •... :,
~ ~
" - I ...,
/
y\ v"''V ~/" )
~ 1 ~ ,.:"' ""'""'""' ,,, -=· . ' '
r-:~ . ,/
l9 ~-- <""'
1. 11'e ~n,.--t •• , ""
► S\trn, .,J,loc"~ (~ " . " ' • .,1,"1111'-
drup i, !tl'l'lllt'f lhl\ll 1hr ,aJ,,.,JI l'r
• Ulfl'' l 1h11fl fl,. : 1 ~'
... I >l' \
b f , , _ «-r■11u If ■n lnd,.....i uut i•lly develops wlcnncc to
• '1mg bctunipnl( lo puticular pwp, he abo •ho--"' 10\cr.mcc lo
t . ,1
.
(?)
► Fffi-n n(dn1gA ♦ II--F~ ,,(Jn•• ~rtrir"'ct•I 111t'l•h1)IIJIII,
► u-w,t.•r• • l~........... ltlht"4II•'"" lh<' ...,tK'l\<'f~lhe!~ 8 C"_• • v
J
'<" ,,,'/
,.,he, drulP' ut a11mc 117oup. ,,_ ,, ullcd d aou u,\eiance.
c:,,_
I' 1- 1Ulcr11nCC between w,hul and general onaesthcl:lcs
r1 \l}
"rt~~ r,-Jni& lokcdhd.
> ,, t ,s 1naC1!.VC.
► App■rcDI
-. "
• Anr•)lon l,m : \\"hcn<'fK'dni& -,II .tc--._.,.C'C'1nb1MS.
/
, a.••~ r- c-- ~=
.., pMtwlo lblwnoc:r.11- ii confiDcd IQ oral adminislDtion
~ •-~
\.., then ~y an, u,d 1., l'C'~~..:. of drug,. Uuc IQ loc■I ch1111gca dcvdoi,c,d by GIT which drug
., ,·,
)f but d~45cs lbc c:ffi:d of <'their. is of various Lypcs: .
gctllng absorbed inlO •Y11lcrmc arculation.
► °"'1md•ns"" m"•han,_ inw,1\.-d anbll,('!!~
'..:, ~'\
J ;' ~.
► T■~byphyl■xls: II any oflbe drog admioistcred rc,peatcdly Ill shon
-
,. \ ,
V
A ,-.,)-
r'

l\_ ?~Yiatl: 8-.l <'I\ ph)_.a pn,po1Y Or dl\laS-kaloids and prcvenl their
·g; cha™1 m,d alhhfdtr Jll,coal adlllwbs al
absoq,tioa.
► O.c:mlal: \\,_
eom,,.,uod.
111-v drugs~ rcactcd dlall
ic:all and fol1II active
Es; Poim.uiurn pamangana1e cwcliRI alkoloi~- u.'l!Cd as e~-

t ---
-••nc 1&1vyo
·
-- I --.;.,))
...~•-
... I .......:>
\ I
::-1
/\ er
I '·
d ~-pcndcnc:e.

intc:rvab the pharmacological rapome dicitcd dtt:Tcucs. lhls IS c:al\cd

as tacbypbylaxis.
14. Drug dc:pcaclenu: Repeated administration of drup may ioduce a habit and
• WHO defines It as A stale, psychic and somdDnlCS a1so physical, resulting
• I........,
\
in J!('ll!IOI\UIP- • •__ _. from interaction between a living org;,num 111d • drug dmaclcri2A:d by
T ~ and ......,._.-•L..•-,...._ imoluble altaloidal lalU)8le ,s fom-• . behavioural and other responses lhat also indudcs a compulsion to \be drug on
•> Pliy11lok,pca&f fiaaccioaal: WIim two clrvgl an: ~
• 00 di{fa-all
{fed 011 c- I":) a continUQ!.IS or periodic basis.
I. Psychic dcpendeou; A feeling o f salis&dion and a psychic drive that
__:,..,,,,- recq,co,s or by ditTCl'CIII ~ haw opposice e C"' .......:)
ph~~~c ial~lo,i cal effecL---.._ require periodic: or continuous administnlion oflhe drug lha1 produce
Eg: Hislmninc.. adreoaline- bnmc:hial muscles 1.11d BP.
1 c--1"', pleasure or to avoid discomfort is called psyebic dependence.
Gl.>-copa. insulii>- Blood..,,.- kYd. - - - - 2. Physical depe,idmce: ln case of pbysical dcpcndo:nce the body achieves
> Noa "fllilibrium: Jftbe 111tapst biads 10 receptor by SlrODg ~val~I c-~ an adaptive state that manifests itscl fby in1mse physical clisnubmccs
bonds, it will irrevcnibly Woct Ille reccpeor. If the antagooist w,11
combine wilh same sire o f..,..- then it is non cquilibrilllll type or non
-<:Ompctitive type.
C'h
c~"""I S~1

when \he drug is withdrawn.

E11plaln the differ ent sounes of d r u ~
Eg: Adrcnalinc and phcnoX}'balzlllninc. /
J J. Drug tolc:raJt«: Whal an 111NSU81Jy large dose of drug is required lo d ic:il an effect C .. . ;
Ans: refer nota.
ordinarily produced by normal ~ dose of a dru& the phenomenon is called
as drug tolerance. CI ·:> #:plai.a different r outes of drug admlnbtration .
► Drug IOlcranc:e is of two types:!. True tolc:rnnc:e, 2. Pseudo or acquired
C • -~ Ans: rdu notes.
tolerance.
► Tne loleruce: This is SCICII in bod! oral and p11m1tttal administralion cl";) JrE,cpb.ia In dctllil about tbt dlstTi b u t i o ~
ofd,e drva- It is subdivided as
1. Natural: This is seen in vmousmim.al species and among Vanous human races. / Ans: DISTRIBUTION OF DRUGS
C • -~
A. Specla tolenna: Certain animal speciCll can tolerate certain /Drug distnl>uHon means paltem of scatter of ~ified amounl of drug amon~ the
drugs in quantities lethal to man. cl";) ~various ~ wi!llin..the.hody .
Eg: Some rabbits can IOlcnre large quantities of beJJadoMa.
8. .Radal lillnuce: A solution of ephedrine instil.led in conjunctiva
C: I.. J .• After ~ n t o the blood stream a drug distnl>utcd to al\ the organs mclud\!lg those
that ate non-relevant to phannacologic a\ or ther.q,c:uticcffcct.
· of the eye CID produce dilation of pupil in Caucasians but in negros
if may nor produce any .dilation at all.
C IJ / The part o f ~-- kin · which deals with distn"bution, metabolism and exaction
- o f ~ called disposition.
2. Acquired faleraace: It develops on ,q,catcd administration of drug and may takes CI.'";>
wceb or months IO develop.. _ • __ _
PHYSlOLOG lc:AL BARRIERS OF DRUG DlSTIUBOTlO N:
·~ - -- . . a. Tlalle tolerance: The development oftolenmce confirmed is C'--;> ~ o o d Brain ~arrier:
lo certain effects or ccr1aln systems:
Eg: Morphine produces tolerance for its euphoretic effect c:1'"":l • Endothelial cells o.f..ru::~n- ~api\\aries wil~_fu)m...m _Q£L_capi\ltu ie':I of t\i
~y, they_¥e very tightly joined and lack 5~tace\lulaT l)!lres. ·
c. ,■ J
~i:
~·~~
c·A~.
 C ,.
c.· I . . ,
~no•"" ,., i;hn\J -,... I~ ""-,
,.-
8 "!1.n c uriltarics .,.. •'"" ..,,.,..i..,.,..i lo)· k"9 re"'""" "'"""'"·"', -· I
,- ~
• CU'· hr••n li■mn 11 nln:m<:ly pnmablc IO drut m•>lccula frnm CSF lO br:un
cell ■• - •. - -
~ UL'"' - •.---,,,,tr I
• r •
Morpholo6'cally ii .-,.nlUIC'.11 1~ bl<,l,al In"' i,..m I t,I ,._...i._.('SI' blll11ar
~l••m!cnlly. IJmL~ ,tual twnl( I~ ll_ll!' ~n• - ~ ·
=-•I .) V
• l!G: r cnleil\in i~ Ina llpiJ .,,\ub le, poo,ly ~ rated in10 Ul39. Bui when 11 u
adminiatctcd by inllatlicc,il rtJ\lte""" c t ~b n l ~-
1
::.--~
, 1111 I...,
(loauoo 'i.n clJllllUlil plu.~ , h bl(1(111 IO the t,ra1n '~
CSr,:-----=-:....:.;,_ .
I
BBB pla~ C\'!IISlrmlS Clft !he JIIISSl&"'ofdl'II&' from Cl
. easily to bruin !"'
~ ,-- ~
;:.~-a:~
-~
• Onl_y. lipid Mlllllt UllioniSC'd fonn of cJrugS f!C'11'~~ore ·
compaii;;Tlo.--,.,iuble.ionind ronnofdrllP· I, rt acting bllfbituralCS
Vcalati_l~ &DIICS1hdics Hlce_dhcr lllil~• ulua·:;inc t a l l ~ ~
like thic,pc,,ral. nan:olic analgesics liloe 1,c101n ..,cl "'!~
c---.~
·o. d-lut,oc:UJ1IO"O,
•
_BBB.
Poi&!....C O ~ like, d o p a m ~ strCP'Olllyca ..., I ~
•
hex11111dhonnmr~1eBB
~ like pmicillin. chlo t m n . J ! ! ! ; ~
. , -..,_ ·c1rarion tht9. ,._ I :>
~!~-
.C"". :,
~-,
~t . . , ~ bc,tntsal burfor:
~-• ~ ~ 0 lnc~.!aj_,!Jl_~ rane j~\j_pill in na~ ll=8dilµll.owa-tlit>-IJU!lfer of non- polar
~·. ~
~-.a ~
lipid molecules nuunly by a process <:ailed eassive diffusion. --
• _Lipid solubh: n6 n ionisable d,ru~ like hypnotics, oarconc:s, cardiac g\ycosidcs
-
r~ lycrosslhepl~ arri~. -
~ -; • ~ ~ _s' :( ?lce quaternary ammonium sallls,_~ving..hi~o\ccu.\ar
l~ and !!!:!lllm cannoc aoss lheylaeenul ~
e~-
w~ -~
~~
• Some drugs_ a..1\minis~ red d ~ first uimestet of pregnan~ may eausc
.lcratogenic effccls. Eg: thalidomide and phtnytoin.
, -- ~ .~
.... '

~~
~
~ Blood-CSFbarrier: . .· . •-;) ·
• ~ is seaded by lhe epilhelial·cdlnftbl!'t'horojd plgns:arul are liocd b~ .,_ ,_
oc:duding zonale. ·• -- .
• lllcasr:~BBBonl no · nlsa eli idsolubledru scanpassfromblood toJ!ic
CSF. . . -
• ~ i ! !_baajR.i,s__composc!_l_or 91i1helial cells lining lhc ventricles.
 c- -
c-1 . "
c- II "~,
£.<> MPARTMENJ:S ot· flRUG JllU
B 1n(T l011 ;
-c-, .., ~
/y "-•pl ah1 the ._...11,lal tlru11
f"':
'"""-pl i. ddal l. [
~ f.:: .- L-)
I , Crll u1., "U
• __!!"ofr._
'1t"il . l\,r J)l•sma nmlf tns t,,s1 ~-.i 1y ,ii•m1'11lrd in llto-
ns,ue
• s, . _ I .) E••tnll~I dn1" 9:
n<:cd, or rnajority of
OCcu rug h
rs ha,c •111 ru~• __ c::•:: =.: E!!knt1~ drug s ue drup that ufuf y boh h e&rc
u.....,.
h !i"·. :-- appto priolt do,,i& c
w Clllh eri
df · . l'-•ur as h,p effinily fi,f the
dnlC C . --~ pl)flUlot,on avail able al •11 lim"!
t_!n adeq uate unoun11, and in
_ _.
~
~ ""~
f;g:
l d a ~ ~c.!!_ - -- -- -
Pmtcin8;~!..."-•net__ , _ . a . c _forms. - bccu
- - - - - - -bas
- tlal drug- list in 197'1 , wbich
.
• . _. (l,nund 1111-tmuc pn,1e111s) •~ ~n - ..._..ub,·'Is h ~ t _ ! ! ' ~ f ew:n ~
" ' - -
~C I ~
Iodine in li\u• chlDmqU&n • e mu upda ted cva:, - _
DDT, end ~ p\ace of
a new I.am calle d :.sa,t1_al- mcdi
- enton
_o --lhiop . c.
---• WHO bu rccenUy conn otal
• !!!!:Oo - -
2 lipid ,olub le _drui' _ lik C8!1e nliald Ng11 ,-
· F'•t IU n,sc, rvoi r: High ly essential medicines: _,,,..-
' I I iD fet m:L adi paN - ~ ~ Q ( the selec tion of
,,,,.._ '
ph~~-~ulldl of the peop le, prior ity should 'be given
to
.., I ":>
3. Tra u1 ttlh &J ..-~ 1. To..._mcc.-t the neecb of majority 1
~. - ~
"-
y. U11nCCC5SUy duplication of drug.<
• Aqu eous hum our- ChJo rmnp
haiic ol, prednia>1onc me~~ncs or proven efficiency and aafes ~eas ed suni lv dru~ should only
New ly
and dosage fonn.s sboold be avoided.
• ~f: ._~ ! ! I ~ sucrose ucts currently in use.
C " ---~ be included if they have simil ar prod
Endo l)'ln ph. syno vial Ouid - ~
•
=
i l l.
. lille, cisplalin,..!._cad, ......1 . . . " 3,,--Eotb·selccled medicine must
mce \ lhe prcscnl>cd standard of qual
\oc:ally prevailing climatic and
ity, inc.luding
storage
• Pleu ral lluid ~ e , metb
adoM.
cu .resel"\'Oin: Dnigs hl:o ~
io ~n cs anu ~ 'X bioavailability and shelf life in
4. Bon e ud con nec d~ tisn ' .....__ /Eonclitions.
arsenic; Ouorides form complex es wid !~- alls..are deposit ~ s appe at to have simihr dfu:acy
and 5ifCI)',
l_!:"-'th. - · - - -·
• .Ant ilung aJ dru p lilcc sdsc
ofillvin have inoie affinity ror keratin
precursor cells, ~•..:, 73-~ Wl,cn two or more mc:dlcinc
pttfc rcnc c shou ld be given to the
iovcstlgiitcd. b) have JDOSt favourab
medicine which a) has been moS\ th01W be
le pharmacolciactic data, c) that can
ghly
ub\e
ua.ails-
gee 8CC\lln11Jatcd U!..slcin IDCLJiDgadin
• Bon e acts as a n:sa imir for
s]Qw g toitic drug s like lead, arsenic etc. e- ·•- , ___ _.,/
reliably manufactured wilh indigenou
s rcsoma:s i.e., whic h could be avail
- - - with good quality and low cost. crite ria
e---•---~ ld be cons \dcm l as selection
5. Plu ma pro tda u dnls rese
~ -•...,
rvoi r.-
to plasma components like albmnin.
globul in, / The a>sl of lhe Iota! treat ment shou is
• Mo a of lhe dnig may bind d dose combination of two medicines
inclusion of e;ny medicine in EML. Fixe c data
acccp1ablc only these two medicatio
ns meet the requisite pham ueok incli
•
lransfarin,_g._,S ~c im .. ~
Free dnlg whc a combioes with protc
io molecule and roans the complex .
~ I; lfinc lude d in EML , these should
medicine as :regard~ their therapeut
have JITT)Yell the advantage ovet lhe indiv cosL
ic effect. safety, patie nt compliance
md
idual
c•~
blncUftg: al non-
Jmp orr, a, pgt dps coptriburc ro
dnrg
C I~ EM!. should bear the in1cmalion
/ 1'hc medicines included in the ishing
prop rieta ry nam es. WHO owns
the responS11li\ity of assigning and publ
J. Plu ma alblllllfm: ributor co dtugJ1.il11lin&-- .'ian and Spanish.
• Alhumin is lhe mo:u impo rtant cont TNNs in English, French, Latin, Rus: ly means
:s outside eM L arc not lllleruL It simp
• Acim c drugs like warfarin, pcn!
cillin.~l lll !idcs may bind lo a
l ~~
C I. ,J 6. EML docs no\ mean that mc:dlcinc
that the medicines included in EML
arc most ,1sefu\ £or maiority of the
people
• Two bin di~ areTdenlified alence of disease! and cost benefit ratio
i. Silo-I: leis ·sp«ific i;-binding e.g.:
warfarin, di~ I, phen_ytoin. C.I .J for most of the lime loolcing to the prev
~~
of the medicine.
vaJproic acid. -
Ibuprofen, naproxen, pro b~i d.
ii. Site -ii- more specific in binding e.g.: Upd ating of El\l L:
. E.g.: Salicylic acid, tolbutamidc,
iii Som e drug s may bind to both site 1&11 inued PfOCC!S and~ s\ s~ l_d be~
~lin ued
<: .I J ~ t ion of EMl . should be_a cont medicines on
'<"' indomethacin. idlne, imip,amine. ble lo acc om ~~~ or_dc\ et~
s: Lipophilic basic drugs like quin process and -lhe list should be flexi
2 . ~. . J add &J1copntcio
a] glycoprolcins.
c- :·J the basis of any new and relia
b\e infom1ation about the old as
we\\ as new
g1:s in
lidocaine.pn,pranolol bind , to alph becomes necessary because of chan
os: Drugs having high ~pparcnt
. volume or
~ --· ;) medicines. "Revision of EMl. also _ t ~ view
J . Tla ne prol eiaa and nucl eopr otei . E.g.: digoxin, emetine, chloroquine. lodge gained in drug
invaleru:c..ofcliscase, advances. in. lcnow - -
diafribalion wm bind IO tissue prot
eins - - ..
:
of clinical experience.
◄. Mfl cie llae ou llNadbl1 prot eins ~ --~
ing globulin_ caned transcortin.
13g: ~"2.uncf to_ ~co ster oid s bind /
~
~
 .:_ I ~
~• ··~
- I ~,
n•I •n d Sf■ I<' 1..,-d F.ML:
Niuio:--
C
-
I' 'V
J,t') .N.r.Y l\-l~ IN11111rr10N
:-,....
,;-- drugs wilh result incrc:ase in c l ~
_lndiit. nntio
M111s try o fh .!'111 EOL wu rdt-.-
~
- - - ..1 t,y 11,c llirffllwale (lcrJQ'U Q ( J l ~ ~
ti!?'-ri~
.
in 19116t Whilo
- l- \ \
r-- ..) ~
,-Al • One drug may 1nh1b11 lhc mctaboham or other
levels of aluwly mc:tabolixd diug ancrproton
~ll6ri orp6{mlianng~ \ o g i e & I
Pl"q>aring lheeah h and_ ~ily welflf tt, New
was pn.-p anxt! OL£ Ui<l ehnc o~b) 'Mf0 _.ji,1
l)llhl die
lc,wc d- Firsts lolc Jcvcl EOL -l ,. e ffect. -
y lhe MinislT)' of lleallh . -- -
C;' "I'\ ~
- 1 "......., ,
• l!nzyme inhi bil~ rhcr be~ bq,a• ic E1ixc
d f~
spec_,n~functions, ~g: )§iihl!ie ox.icta.c.
ion o~ o ~ c s havin g
Adv• nlagc s of F.DL: -
-.., -, • Rop1d~~
~!ab ility of mc,dicinCS II n,oSl ,aat.a of lhc
popul111ion,
.:J " • ftrr~crsafu; ~U cco bad ,i~ ~ dosa .
i/ ~
I. POrti
11 make s fur wad«
culart . Jifm
lllfflC .ncl timited ....,..ces uvo 10 bo ulillsc
d efficiently. ~ , ..... . • Classical inhibi toa of cytp4SO enzym e isproai
~
- 11 helps llse without
• substanrial saviag
2 effec ting ...~lsiclle S ill ICl1DS of (orcigll exc:ba :;-' Chem ical eltuif ::oun zyme inlpibtdon: -
- . -- c__.;. --- - - - -
~
J ....,IJl aJ.._-
substanti.n7~'
• rt help s· .,.~a dnla .dispellSina aod patient compliance by
a,ds ,: ;-1, Advcncconsequcoces:
18
ugs ,wila ble in hospitals. _ ( ~ ► Theopbyllinc+ chlorampbenicol- Nausea, vomit ing.
4
· II helps p l ~ the mnl,c rofdr
i ~ C S IO allocalO
..-anea1 ~ funds and rcsou n:es C" , ► Dicoumarol+ cimctilf~ bleed ing tcnda icy.
► Morphine+ MAOI-Sevcre respiratory dcprusion.
. for supp ly of ~ J
be m a d e ~ EVIIII and cfislribu!ion<>f rocdicinea can
md unifiJrm II all Jcyc)s of health c:arc system.
• ..)
- 1'._:, ~ apeutic effects
►
._ y oflevodopa.
I Levodopa+ carbidopa- Increased accessibilit
► to inhibition of ald<:h'Yde
C: 1' .:, Alaihol+disulfunm- increase in ala>hol due •
lloa IIJld aazyme lnhfbltiOD, ~~ I'""-,, ,-.... dchydmgcnasc enzyme.
al muscle paralystS.
~ t o ahor t notes oa mzym e ladac · I...., ► oc:urarinc+ ncostigmin~ rcvcm ole of skelet
D·tllb
S,;S> -ri:, \~~
Aaa: ENZ YME INDU CJlO N ~ - '-,
~- '~~
late or ioducc the growth of s~
~ • Several drugs oa rcpearcd admiaistration smnu o_!Dal ~YI D.u ctin ~ 6. Writ e short aotcs on drug depu dHc c
and tolcr utt.
v':f • This stimulatioo rmbibitioois rcvas,1,lc and leads to micros ally large dose of drug is_rcquircd lo elicit
an
and is .2_~~ pi:i_armacolo~ca!_ ~I_ :-, Ana: Drug tolera nce: -wl1en an unusu
:"-t' Yr • This indDCtioa l'l5UIII in lll:Cden1cd_211eta~lism
effect ordinarily produced by nonnal therap
eutic dose of a drug. the phenomenon is called
as
/ ~· ~ oftbudmioistrrwlclnig.
and some extent in lungs and kidn e~ f""'J ...... ~cc.
<f • ,,}P~ • Enzyme iadll dioo is prom iaent in Uva- of proteins gradually occurs over a peno d of
1-2
: I; :\. True tolerance, 2. P~-udo OT acquired
,' o"< c•~
\ / • Enzy me induction nllUires synthesis ► Drug tolerance is of lwo types
tolerance.
~ wcc b lo a muim am c:xtm l.
► Tru e tolen ncc: This is seen in both
onil and pm:nt1..-ml administration
Cbem fcaJ elfeca ofpzyme lpductjon:
of the drug. II is subdivided as
A. Drug inlcn ctiom IIIIY..OCCW..,
> _!lffl!~-JAlllllllcy___- even in the users of oral contracept
ives if potent
- JI ""'' 3. Natu ral: This is seen in various animal speci
es and among various human races .
--'-
1- - - l species c:an toh:n.le certain
~ lite phenytoin, rifa~ tcin ~ ~m ~ Spec ies lolera nce: Certain anima
itan dy. -,
► en zym e~ lilc ~ytoin accelcrarcslll• Plda bolia of vita mi~ ~ drugs in quantities lethal lo man.
ilies o[be\\ndonna.
> Enzy me inducers like barbifiirall!J" enhan
cleYdopmai1 ofiolcrance.- -
ce their metabolism and leads to
- - ~J .~ J Eg: Some rabbits can tolerate l;uie quant
led in conjunclivt
t,l· Racial lolcrnncc: A solution of q>bcdrlne instil asians but in neg
B. Enzy me illducePi.;ijjS;cte,rieity.
cJ ~--:. of the eye can pro,luce di\ation of pup\\ in
Cauc
► .Elbanol drinkers may have mo~ probabilitie
s ofbq,aloxicity from paracetamol
:.t. it may not produce ony dilation al all.
ops on repeated administration of drug and t
:--•~
ovd" 'cto& 4. Acquired tolerance: It develops\\ devel
C. Knowl* on enzyme induction leads to th~ ic eff«ts.
YTo treat lhe neonatal jaundice in pregnan!.._~m..ffl. phenobarbitone is
used 7-14
takes weeks or months lo develop ..
c. Tissu e toler ance: The developmenl of
tolerance is confirn
~
· .-
lransferase enzy ;e to certain effects or certain systems.
~ ~~r to_ ind ~ ~ ~ c glucoronytacid.
_ _ __ ;_dllJs_prj_ot yses orciiccffcci.
the conJugahon ofbilirubia to gluc:uronac ·- - Eg: Morphine produces toll-ranee Tot its cuph
-- which cacal
~
~
 -I"
r-
-l V
,-
.tt,,ch'I-S 1111Cf11l1CCI 10 - I \..'
d. Crou ........ - ·· """ ti•'"""'' ,n,bally1 0
1,.. t, 1 ,howJ I " 1-1-10
-- - ► t"""-""-'P" • Corblt1t.,.., W.ilritlc1n of pcnphcnal me\ab<,h,m .
a drug l,c,!,,n,:in,t ...,,,.,,101 II"'"" • : I '-)"' ,.ntaaunl ,m: W1- one dntll wm d,a,-o , \nhrlnta the ac:1,an of anolhcr
I(> • •ICf'ftUCC. dntg
NII« drop.. ,_ ll""'f'• Th" i, ralll'CI M cn1S!I1t<~CJlhcli
CS
- l then they arc Mid tobc Mlaav>nlll tc. In., anugon»ai<: ~• one c!Ng is inac:twc..
Ft1; Cro,.s " " - ~ atrahol end 11'""°" • C I 'V buc dccrcues the cited of other.
· I f ► Depending 011 mechan\am tn'IOlvcd antagonism la of Vllrioui types.
► Ap,..._ , or .,.:..... ...,......: 'This is confined to ornl oJuun stnt ion
likoeih..-
► Plt.y11c.at: ~ o n ~
of dnap. Due lo k>c:al chlngcS clcYdopc.d by OrT which prcvL'tllJ drug : 1v l!g; chaNX>al uiir.ikiioiw.- dlatcoal amoibs aluloids and pn:vcn\ \bar
.,.,.....ic circularion- .. I v
►
scnlng ab:,Qmcd into
Tw•n,1a ,-tua: If any ofllle druJ a.tministc:icd rcpcutcJly ~t ~hurt
inlorvals ttw p1wauw ok,p response elicited c1ea'U5CS. thiS "called CI ~
r' DbSOIJlllon.
...¥"'Clu(mlw :
compouod .
Wba, two drup - RKled chemicall y ~ - fonn ictive
D..,.
IS. .t-..!1cp • ladtyphyla.,,.is.
e_ndaac e: Repealed adminlslnlion of drugS naay induce• h•bil and
WHO ddina ii as A Slllle, ~ and ,ome1imeS also physical, re.,ultillg
-l""""cn ce.
•
::.~
- I~ (

l!g: l'owaium pcnnanga natc oitidilea llbloi&- used as g;,stcic lavage

in polsoninp..
Tannins and albloids- insoluble albloidal ~ is fotmcd.
► l'hya~ I/ fonc:tion •l: Wbca two dnig, an, IC\mg
on d1ffm:nl
&om ~ belwcaa a liwig arpnism and• drug ghoractcrizcd by
::0 receptors or by different ina:btnisrns have opposit.. effcc\ on
behavioural and Oilier responses dial :also includes a compulsion IO the drug on
; continDOUS or periodic basis. • _ .
· ~ dependence; A feeling of satis&dion od a psychic dove lhat
~ periodic or ~ adaninimation of the chug that produce
;~
physiological fl.au:tiona or pbarmac,olopcal efic:ct..
Eg: Histamine. adrenaline,- bwachill muscles and BP.
Glycogen. i11SU\in- Blood sugar level.
► _,Non equilibrium: lf the antagonist binds lo teeq>tor
---
by !5.trOl\g covalcn~
~~
t will
. / bonc!J, i1 ..wjll--tneversi'oly blodt the ta=qJtOr. If \he antagonis
plemurc or ID avoid discomfort is called psychic clcpellden<:e. comhine with same sile of agonist lhcn it is non eqwul:lrium type or non
✓Y
physical dependence lhe body achieves
4 · Playsfcal depeudirncc: In cue of ~ -, ...:ompetitivc type. •
an adaptive state lh111 manifests irsclfby iolensc physical disturbances
~~•-.:~.
e-c-•~ 2~: Adrenaline a.od-pbe11oxybenzamine.
""'1m die drug is withdrawn. '1~
~t~
7. Exp,.._ fa delail about the combine d cffcd of drugs.
Alls: Whm two or more drugs wt.II be used concum:ntly effi,ct of the drug may varies
;J~
,....a:I _~ r2: pl•la. In detail about tile transpor t mccll.ais ms of drug mnlecnlcs. /
J- ~ \
J. The major tBnsport mcd,anism s arc:
r '\, ✓
\)I
dependi ng upon Ibo ctrvg usaL
• There may be i. Synergism - I~ I. Panivc ditlilsion or non-ionic or dmp\c diffusion.
2. Cmietmedialcd tn.nspon
0/
'- ., ~ ,Y" ~
~
./' ii. Antagon ism. : I ..;) a. Facilitated diffusion t,?
,.o./\ )<- ~
~!_ "~~ Facilitated or incn:ased effccl ofone drog will be produced by the
other drugis called as synergism.
► fn synergistic pair both the drugs CID have lhe s.me action in
same direction or given alone, one will be inactive and enhances
~
C I
•-~
I ·,wl

b. Ac:tivc trunsport
3. Pinocylosis or phagocytosis.
4. Fihralion

-"'
/'
./
~
~:
, '1(:-
the action oflfie other when given together.
> Synergis m an be of two ways: I. A ~ 1 2 . SUJ'..ra ._ I ;> PASSIVE DtFF\ISlON:
addirive efTed.
►~ l i v e efffd (SIUllJJUliOII): The effect of lhe rwo drugs are
c-· --~ ► 11 is lhc lmlSfcr_process by which \hefflgruolcculcs_pass lhrougl}_a b\ologi~
phase ofliigh conc:_entra!M)Q.lo the phase of lower cooc.ffllralion witho
barn~
ut~ any a ~
-
~a
....-- ·--·-- ;-;
in same direction. .
► £1Tec1 of drug A+Be Em:cr of drug A+ Effccl of drug B.
c-1 ":> ---= ---
~energy.
-~Non dcdrol~cs _lnon- ionised dru~) may diffuse passively which
is~iana l to 1!£!d:
>· Eg: Aspirin + pa,acetamol- Analgesic/ antipyretic. '°'-l J ---· - coefficient i.e~ drugs that arc h1g\1\y lipid soluble may diffuse rapidly ,lw lipid ~o\ub\e
- - Nitrous oicidc+ elh'-T•-General anaeslhcrics.
> Supra additive: (Polenliation): The effect of combinalioo of c-L-=, A will dilTusc slowly.
F weak electrolytes ( partly ionised drugs) diffusion dq,emb on the d c ~
\ i o u QL.
►
drugs is greater than lhe individual drugs.
EITcct of drug A+B>E!Tect of ilrug A+ Effect of drug B.
~ -
1 ~ a n d lipid; water 1XJC£ficicn\ of tl1e d111&
~·
~
 --
c:-- I . •
I ~"
- I "
>
w cu clC<ltr\'1)1cs""' cilJI« ~-al. .,,.i. ( ri,m,1,,.,., ....,.,1,o,t,,,,....., ..,Ji\l1n ,..1rcylote
> morph,.,.,_
~ u, iut,rh«ami...,.-11<\ln I
'JJus1<'111 of .,..t'l'ff\'ffl'!\1"' ..,...,_i.
-
'
-
ur<"' 111.'11"! ,,( ;.,.,.p,1,01\

) or (
-
:- I.--~ ~I
I'A(' ll,rl',,,rv,o 'I kANlll'Ok'f :
► ~
d"f'(:n<h which in 111m
~,.., d1 ·• · ""
- I j hip
Thc.rda1.:~~Hand T'b,,.h,.. .,flhciln~ - ,•.,•; co-.Clon
$hor .....,, c,iprcs...J ,n - N 11...ien,.•o ha!UfClt,orJ cqo>0ti<V1 C ..- v
""'....,._ rnnnn nm·nnnn
1
~ ....
-- I V
.... lUUUUUlJ UUUU
I,,. l~ / ··•:• .....,
:tl.~
channol pr,,toln
C" 'V --,,inllon
► Carrier moves a drug sub~-u-atc along lhc coaccntralion gradient ( higll cone. To low
cone.) ·' - - - -- - ·-
Upid-.oluble
dN9 ':. I_,) ► ll is also called down bill transport~
> No extracellular energy is rcquir~ .
,_,..~ ':. 1',) ► Capacity limited process i.e., depe:ods upon .i,\lity of the drug binds wilh camennd
soJut,ledN9
- I ,:-, availability of the carrier.
.
~•-~
/
c:-- ·~ ACTIVE TRANSPORT:
► It is a carriennediated transpott takes place against electro i;hcmical gradien~
► ltTCquin:s cm.-rgy fortr.mspott of the drugs which. is generated by membrane A,:Pase.
c:---1.,:,~
► Stnmger lbe acid 1-cr lhc plcnalue. stro11&cr the base higher the ~lea ~aluc ,
► Weakly acidic drvgs .Im Aspirill, pbmyloin. barbinntes me u_nioru;~~tc.m<,dia~
. ~-•~
~·~
• •.
--ben.... ~ - a,· _-. - - - - --~ . ' . · -
► Weakly basic drugs like mo,phiJle, dian:pam are '!¢onisodEl aikalillc P!!,a r • ~ ~-
abswt,eil mlhe ·Ul1£5tiae. , -·
~1; ~-.Y..1
- I _,:,
► Pb of the drug= ph oftheclrug-50% ionised.or unioni~cd.
► Strongly acidie OI' .saroiigly t,mc drugs n:maio~ ~ at all.ph,ud •~tb.S
> Th_! ~form o(acidic drugs-~s the mrmbiane Cl.f!aslricmucosa)
CAR.RJ.ER MEDIATED l"RANSPORT:
e ·• -~
CI ;)
-.---.
.:=. G
,Ji __. /rr7\ \<';,
~,,"\
"X'"
--- - - - ----- 'PTNOCYfOSIS OR PIIAGOCYIOSlS:
► Polar compounds Sidi ass sugars and amino acids C3llll01 penelilltc ll1rougb the passive
C ~· ;)
diffusion and moved lluougb ,he carri~,ml~ pr~~iJ;il;c celliiiifacC:
> Carner molecules an: usually proteins which combine with the drug substrate and forms a
complc:x. Ilic dnig-COITfllex g~ penetraie iiitu thcce11 oimbraru: and rhe earner diSSOCJales
with the drug. Caintr rct~IO the ongiiialsite o( lheccli membr.ine of reuse.

-- I~
: ..lJ
► P.HAGOCVTOSIB;llt
' --
► 1:JNOt-Y-r-OSIS: ll is a process in which cell engulfs the fluid or drug in ~!ution
locariiivagination of the cell membrane.
.:. _______ - ---
is a pxoccss in which the pankulate maucr is transferred by
~
► S~ - - -
► Cmicrmcdj•1cdtnmponisoft1u-ee!ypcs: -. - - · - · ---
1. Faciliratcd diffiaian~- - - ~ _:~ I. Mai.-romolccular solutes are firsl trapped in the microscopic c11vilies formed in lhc
2. Aerlve tnmpOd membrane surfaces. ·
c·...J : 2. Membrane then fuses completely encloses tbe fluid to form a vesicle.
~L'j ~ 3. Vesicle i&·scpar11ted from the membranc·inlo the interior of lhc ce\\.
~
~
~
 f
'
Pinocy~os

FILTRATION:
► Passage of drugs through the aqueous pores in the membrane or througll Para cellular
spaces.
► Upid insoluble drugs cross biological membranes by filtration.
► Molecular weight more than 100 or 2QQ. cannot penetrate through the memM3!1e /
 r
L)N \T - JJ_

10 marks•

ro ::~SDI
~ l n in deblll abo11t the types of ~eceptors. ~Or) Explain the principles of

rccepton.
of action of drugs. Explain in ilct:iil nbout G-l'rotcin coupled

A. REFERNOT
~~a n in detail about the drug drug !!>:_teractions.
DRUG-DRUG RACTIONS
• Definition: Drug intcractio ·s the alteration in the uratioo or ma · ud of the
pliaii;acologi effects oft!ie one drug l;Y, another drug.
yDrug interactions may lead to cohaoccd or diminished effects that may be useful or
hannful.
,..----The useful effects are due to synergistic or combination of drugs.
Eg: antibiotics and anttnypertcnsives.
.,,,,.- Harmful interactions are numerous.
~ Drug interactions may be categorised into two types:

? 1. lnvitro, in the syringe before administration. Mixing of drug in syringe can cause
J
@ie_mical or pbysical mtc:raciions.
2. In vivo, in the body after administrati n
a. Phannacolcinetic interactions
b. Phaonacodynamic interac:ti
·--1.-........
~arma cokinetic lnterasti.ons·
• One drug may affecL the:lbmiiiuoon. distribution, transport. metabolism and excretion
of another drug.
~en:
~rug s gjven orally, can interact with in the gut to form complexes which are not
absorbed.
Eg: Ca+, Mg•, Ai♦ 2 , Fe+3 salts interfere with absorption oftetrac;ydine and p~.$0lon e.
Such drugs can be avoided by ad(!l~nistering !'_v~ dru~ ~eparately by at least t~ ho~.
/Drug s altering gastric p11 c.m alter the solubility of another drug which-alters absorption.
Eg: Sodium bicnrbonate retluccs the absorption of tetracyclines.
• /t>rugs may alter the absorption by altering the gut motility and gastric emptying.
, / Eg: Opioid analgesics alters the absorption of anticholinergics by delaying gastric
emptying.

l Drug d~rion •

I---·- _-7's0·_·_·_ ·-
1---- ·ve.
ll}'C ~~gly_~u_nd to the plasma protein~.and re~ain pharmacologically

Some drugs seem to share the limited number of protein binding sites and displaced
from another drug.
 ·\.~l •
~
l J .. _
I ...
td F:Wi • fft coe ■ t ' t tr 12 d 11 ts'. rs , e 1 rb
,,
...1 •
,
.J '-'.
. ......
,.. ~
.... • -1,.- Jru ·, ·IP lhc UICR!<l,,.C
theresull
ufnl!I . in the 11nl>1ll1tlll onJ rhArnln,'QIOJW!Jlr adi•• r.,1111 ur ong .J~ 1· l'HARMACOKINl!TIC l!urnples
Es: c,;6b& l'flJs 10 to~ieity. ;J'v INTEll/\CTIONS
Dru11 ah!!Omlloo
Sll!ky;::" an diJPI•"" wor/anJI fit,11111,c binding $lie lc:acls 10 bleccling.
hyro ,..,.••_ '."' can cfi~rlac-o rolbut.uni« from lho bindillll silo leading 10 ,J ----., A.
I. f'onnlng wmploxca with 01ha-dN,i:t • ea• Mg' Al'2 Fe•> salts interfere with
■b..:....wifar,Acw!ffic tmd orcdoir.clone
8 J -......11ccoma. :.(._) 2. Allers l'h • ~ mh>CeS the absorption
... '
-l.
o u:tr clines.
. . .,;) 3. Out molllily and gaslric, emptying • Oplolaiiilgesics alien the absorption of
llllic:trolliictg1cs by delaying gastric
--
~
I ...)
.
coinnnno
---
':) 8. Drue: dislribuiion
Dru_r tn.nspors;- Clofibolc can d i s p l ~ liom the
• Ooe drug di.!plac:,s the another fiotn
_.Y'<;uw,~dine UK! related admiergjc mugs -wen, aclivoly innspoited inl9 ad!!!!~ic
I ' ·,:,
protein site.
. 6liiding site luds to bl
S~lleSCllld~fromthc
g.
~~ns. by lrunsport systems. llu~ system
ii inhibiled by_a n l i ~ ! , ~
amipl"llmwc interli:n,s antih)l'ert,,mivo lffl1/iiy ofguancthidllle.
:L'J
-1 '
b' "'ngsilc Jtadiog to
. coma
hypog)ycaentlc
-1. .) Drug transport • Ouanedli~ne _and n:lated ~encrgic dtu~
,:.i -~ . . were aclively lrmlSpOrted mto adn:nergic
-·- ' )
Drug moubolism: neurons by tran.qpon systems. Ibis system is
inhibited by ~~ants like imipraminc
~
~llmqJadoa: The .l)'Dlhcsis ofdrug metaboliziD&_miaOsomal cm:>m~JLeol!!!!!ccd by
theme-ordrup lilce iwcticicles and polycyclic h)'l,!10(.«rf>ODS- This {WµC~ efficacy-
:,-, - .
interferes an ypettcnsive adivi'!y ·of
anm1clhidine .
--
and iaCtta$es die lhc:npcolic dose of~ ~L-
£11: Phenytoin induces the IIICblboliJIII ofglucocorricoids, ,iraminD, lheopbylline. :1 -~
~ .)

Drue. metabolism
a. Stimulation,
.
Pbc:n~in induces I.hr: metabolism
g111c6c:griic-J11~;_ villllnlJI D, iheopby\liue.
of
Griseofulvin ioduces 1h1t mdaboli.m uf wmfnrin. _J • Gnscofulvin induces the ruelabolirni of
../ e: :.i~~ . warfarin
Tllhlbition: lnhibilionofmo1abolism ofono d,vgby.anothm:drog leads lo 1oxfci~.
Bg:-Allopurinol inluoils Ibo metabolism oftolburamidl:, mell101ra,u 10•
KetoaJllllZl>le inhibits the mctaholis,n of cydosporine
Dr"II ~nndon:
:..1 ~
:J '.,)
---
b. Inhibition
•
.Alloporinol 111hibits the metabolism
tolbutamule, mctholrcxate.
Kctocooazolc inlul>its the metabolism
cyclosporine

or
of
• The cxcrmoa of111mly addle drugs like sulpbonamiiles, Slilicyfatcs and l>arl>ilurali;s
can be iam:ased by making urine alkaline.
Eg; Probenadd iPhibils I.he lubularsccn:tion ofpenicillin, indorneihac/11 and riboflavin .

:.J)
:J ~ ---
Drua excn:tfon
a. lncn:ascs lhe excretion • WC11k!Y _ac.idic.-acid&--like.. sulphooamid~,
salicylalei, ~j:ri;Jion..is..ingeesccl by mnkill&
--
urine alkaline,
Ph..--eodynami., drug larm111tions: :..t;, b. 1)ecreases thuxcrdioll • Prqbc:nccid.inhibits the. tubular .secretion of
penicillin, 1ndotnc~iocinMd n'boilav~: ··
i.,_ I :,
A. Receptor site: Dnlss_ acting on same~eplor Jilc or O!!_~ilTen,nt active si~ may
~
mhaace II!!~Ibo @cti\'.ily.
.Eg: Tuboc:urmne and aminoglycosidcs blocks ll1e neuromuscular junctio11 and PHAR.MACODYNAMJC INTER.ACTIONS
~
A.. Recptor site Tubocurajn~ a!_lCI ~inogb•c~ic!.~- J>lock.s
causes mar:1:ed CNS depression.
tJic neuromuscular junction and cu~cs
8. Clluga In lbe Dold aod dcctrctlylc b1l■nL'(; maetod CNS.denrcssion
~
.
E'g: Drop Iha! c:ausc:s porassium depletio!I mwu,oten_tiarcs .!be .!!ffec:15 or digitalis . _ ! _. _p~gs_that CQUSCS p0111ssium dcplelion muy
___ B. . C~~.!!L!luid__an( 1:h:ctrolyte
111d anca,onises lhuPlillJl'hylhmic actions ofli&1ocain -- · -
,,..-.-- - - -
~
- . balance potenliatcs the eITects or digitnlis ond
antagonises the anliurrhythmic actions or
~
lignncainc.
~
 • I
-.. I ,,
_ _[ -- -- --] :1 "

,.,
.:..1,.,
: 1v
• 1111111111 r,,., u po, 11rc, d rv,i ,nay""' u ■n ~
(lflJ h!1111 l·10.:.m,1c, on1 1s,,..:-nte.

. wluch ■11<1' wmbmc:s w11h hosl

• ~poc:illc 0111ibodic a aro cttculatmg o n re C1.p<11U'" lhc an11br>dic
■nllbody complac.• which in 1um rdea-.c. thc ch<-rn1cal rned1a1DCS

s w,11 f,,rrn antigm

flf allergy.
...,..t:" Typo-1 ( ln,mctlla lc)!
: 1 ..) ► Allergy tlcvcl11pt within minute, and I...U f<1r 2-l
hrs. The dni& cuu'ICS
3. E.1<pl.., 1k drws t1t.c.-,, pn,cu, In detail. :..1. .) formation oftwuc1C ml11,ing lg£ .-,tibodlc s lhat an: rixed lo mast
► 'The subseque nt capo,un: to the drug acuntcs mast c;d\s IO
cells.
rc:leasc chemical
~
A. REFER NOTES.
:..1-) mediator , or ollcrgy.
► The p:,llc:nl i1 unlralcd ii 1-SS lo acaphylae11c lhock.
I . £splaia • ddall .._, !k " " - drua ttadioat
: 1 ,.) l. Type • II (Aul o o r acuknl.cd al.ler gy)r- -
~ ► lt occun 72bnof dNgadml nisttation . Tbc.drug combincs wilhhos\ p«>tcins
A•r. AD\"ERSF. DRUG REACIJ ONS
: I ::, and convert them lo antigen. 1bc body lhus tn:ats them as fo-reigJI
proteins
rcspmsc_!o_!be~ • -
- l -~
,.... '
and form antt"bodies.
• Dcfiuilioa; A-.nliag lo \\1 10, advme Jnig IQdioll is an any ► On.re c:Aposure with the same drug. an -,itigcn anu"body
reaction lakes place
that is aoltious and unlntcndcd and lhai occurs 1n doses u5cd in mnn for pro_ehyla,
us, ._ l ~ which activates mast cells and damage the cells.
OUS, baanolys is.
~ I-~
diagnosis md thcnpy. ► Clini~ J manifesla tions include fever, lupus c:rythc:mal
-
• Adva-,,e chg reacliam are c:a1cgoriscd as follows lhromboc ytopllCDia. - - -
~ ic effects: I. Desirable or bcncfici11I effects
2. Undesirable or unw111\led or adVCISC arug responses
c:- ---~
i-L ~ ./Type·lll _(Delayed alloergy)!
► It occurs after 72.bn bat wilhi.n 1·2 w eeks of drug administr
ation..
a. Type · A (expc,clcd) - I ,l ► Antig<:o antibody comple1<cs are formed wbicb
are dcposi1cd in vQCU\ar
l'ype-A: i. Side clTccis.
ii. Secooclary effects

b. TYJ>o-8 (un<:X-J)ttted)
Type-8: i. Allergy
ii. Oenelically determine d
Iii. Idiosyncra sy.

~ •.
, I .;)
". ;)
endolhcll um and ildivates complem ents.
► ll is chwactcr ised by all ergy inflamma tory n:ac1ions
nephritis and =
sick ness_
in tissues, glomc:Nl ar
iii. Tcwc:ity. 4. T ypc-tV (Cell meolitUoed aU•rgy)!
• Type-.\ adve,w elfffb:
with the
~ I ..) / ► Anligen specific rece-plors arc develope d on T - \ympbocyl.c:s. which
when
tt11elions.
~
_... I. Side dl'eas: Tbesc arc the: undesirab le clTccts which are observed even
dmapcut icdoscs oflbc drugmdo reu.ruaU ymild.
Ee: Dic)-clomine which n:licvcs lhc pain of in1csti1111l colic but in therapeutic doses
itc:aasa a side effect of dryness of mouth.
~-•..)
- I ..) ~
activated afl<.'T e1tposurc 10 drug, leads to local or tissue allctgi.c
ldlos¥_1_!t r!-5y:
1bcse ate hann fu\ and sometime s fatal reac11ons \hat occur in small
minority of
~ 2. s-dar y effftb; These are the cuggerai ed fonn use
predictably eilba- due to o,-erdoses or after prolonged
of side effects wh ich occur
of the drug. c:1 ~ individuals for which cnusc is no l known.
Tlim lolucity could be C .) £gs: i. A condition o f m:ilignant hyp.."fl)~TCXin caused due to
drugs hlu :
azinc and
L Phannaco dynamic Eg: bleeding due ro h igh doses
of h alothane, succinyl ch oline and newoleptic drue,s \iltc chlo(l)fom
c·· • -
, ..1 ~
heparin. halopcrid ol.
b. Phamm:olcinetic: Eg: Ncplwotoxici1y due lo gmtamycln
ii. Occurren ce of ap\astic a naemia with single d ose oT w ilh low doses
of
io cases having renal insufficiency.
cl .., ch\ornmp henicol. This effect is d11c to presence of P-N 01 group
in
~.-:··•-·:~
~
Twe-B llchawd l'eas: chlonmp bcn'icol.
ms
)
di11re1ics
• lbca:ai sa unexpeckd)y even when drug is used in lbcrapcutic dosC3 by mechanis ill, A spirin induced late asthma or ch ro nic renal failure a nd thia:Lide
1Defa1at to lhe main phannacoJogieal effect of die drua. induced en.-c:tilc impotcnc c.
lly
• Thms illaludc either immmological med"iatcd action of lhe drug ~ c a -- - - ·- - --
•-- --.... . 811w:zsc rapanseo r icliosyncratic cfTCICls.
A. .or.a. ..., or •ypersns11.M1y reat'lions: ~-=• -:) PRARI\IACOVIGILENC E- -
• AJleqic 1-.aions ta chp occur when there is • f)fflliaus exposwe
lhe .-ftiwe individual is re exposed lo the lllffle dzug. ·
to drug 1111d when ~-'• -";) • Pharmacovigilancc is the scien ce and activities rclatine lo 1\e\cction ,
11ssessm ent and understa nding and preventio n of adve rsecffecl
s or any other
~~-: > drug rela lc<l problems.
 •-c:c • •• • , • I• I, i •
, •.
_,"-, '
-,._, .:J- . . '-' -'\11
'
l)_>J IT
(
~,·i
{ , t::7
I I
11>- •
111111 f" •
nJ ml ion alu soo fdm
gs.
. -ll c:c lcd Md

_J
~
-
........
I

~
- V
~ e c.lucumen
Alf[ONQMous NtR
QUS SYSTtM

t tlt lel
'J /
I ,·igi la11cc_.ill dn ta1 1-
The •im ofpb.,rmaca . .._ .m id •":la1edfod vcno droll n;.-porling ' v
::. k •
;:11,..-. ,~...,. - ~ D t:U NchoNs 91 ANS
.""' • Tl
1c oJVl:l'Se Jfn ,•
rc-a NIS IIR II O A. OftC,:\N t/lA.Tt ON AN
\
~ by f'han1M
IC(\\it1ilance SyslCD (O . •
-1 0 uola lhc autonomi c
• w· nervoua system con
igilanc c aoftwani vig,Oo invohm lary par t of um.
~....,. l - •
c:en1rcs.
The d11 111 COllccrc:d Is
up loDdod in pharmecOY ;.i 0 ► Th o aulooomlc ur y I.e., inhla1ed In the bra in and below tho cerebr smooth musc:.lc,
I\Jn ~io n, or lhc bod lhc effCCIOr organs
an,
mic l)'lllem is rapid and
-l
'-- .
j ► Th e cfTce1 or aulunothe glands.
cardia c mu scl e and
~
int o two division,;
... .)
lnl lnl ls
2
• Ex plllUl i. dd
ajJ •b o•r UM .,. ._ or dla -1 . ► Autonomic nCTVou
s sy,ccm is sep ara ted
a co• ple cl ~
a. Sympathetic
:, I€ I 3A. .IU:F£1aR faNOdeTE S
tau •• .,_ , G- pro tel c:- 1 .) b. Pata 1ymp11thc6
c
L
3 - • £.Yp1a
A. RE FE R NO TE
S. cuo nal ly In opposi
ng m& MQ '. Sy mp ath
eti c
• W nr . • ■ore on
JK AK STAT nc ep
ro n.
=- ' structurally and l\m
ns and pllnlS)'fflpo.tbdic
activity during
n=r
:) .l 4 To e divisions arc
J inate the stress situatio
actlvlty tends to predom
A. JK AK STAT
RJ :C EP TORS:
> Th e JKAJC ST AT ing (Janus lw wc s si p!
1n1115ductioa and act
lhc infonnallon &om
ivator_ of
chmnc■l ·-.... 1 ..) . res t
hways bdWC:en the
CN S
lnn scr ipl ion ) slp wl
padlw■y ~ I J
DNA transcripllon ond
activity in .the :- 1 ~ has two efferent.. neu
ron s in its peripheral pat
_,, I/ _I
~ ~,
sig mJs ollbicfe the
ccJJ wh ich -
. c- 1 :,
► l!ach division
and cfTcctor orgnn.
•
--·
..- - , b) JAX-Janu., kinasc
s, c)
1S1 mp onent, : 1) RCCJ)for ► Preganglionic
nairoo
► Jt ~ nsi srs of h main co b'anScription. I~ c neurons in or spinal cord. Alt
ooal
r ► Po st gani;lioni
I-!: >
STAT- 1.ignal lr■n
lducer and activatar of cptor. nC\ll'On is in \he bra
and dirncrises tho n:c ► Tho cd l bod
y of the prcganglionic post ganglionic neu
rons. Post ganglionic
xf binds to recqMor h the cell body or the
► In the tin t atep li,-tion of JA K. terminals synapse wit organ.
~ ► Th is ca .- activa _. - I .).) ulses lo the effector
otion)
ibclf. (•utophosphoryl neuron conducts the imp
s lyr osl nc res idu coa 111laches to
► .I.AK J)hOISJ)horyla«e
g ST AT molecules In
► Th e freely movin tyr vm 1c r""idue.
d
die cytop lasm goes and
- .)
e I S)'MPATRETIC NE
RVOUS sy sT EM
the pfl osp ho ryf ale !ein and dimeriscs it al11mu.•, ret icular
j~ ,ylare s the STAT pro oricin in the hypoth
► TA K also phospho
enters the nucleus and
11t11ches to 1he S])c:ci
fic region of
pro tei n
e -1 .) Ncuroot convey lhe
Impulses from \heir
or orgiins 11nd tissues
.
► Th e STAT dim er tes transcription ota particu lar scq u.ence and the
t;:c
"'
tho DN A end pro mo e ffect.
lhu s formed sh ow ,
tho c--• .)
C --1 -c_".>
formation and medul
► PU GA NG

la oblongata lo erfoct
UO NIC NEURONS:
ganglionic neuron.~
is in the IMo..-ral colU
111n of gycy mu lle r In
vertebrae.
~ Cell body of the pre
levels of I" thoracic
and 2_. 11nd Jnl lumbar
t and lcmiinales in the
--• •cs_.-~)
1. -
spi nal l:Old between the
'The nerve fibre of
the cell leaves ll1e cor
d by the Mtcrior roo
ganglia and passes thr
ough the pre vertebral
ganglia .
-I ~
synapse in one of the
N EU RON S:
~
--•
IC
. . . !! . . . . . . .
► l'OST GANGLION organ or tissue
n Md tcrminu\cs in the
Cell body in the ganglio
·. ,
_,, .
--~ " ! - ~
:,
.
RV OUS sy sn :M
-rJ - - PARASYMPATHETICNE
ission of impulses fto
m their source to the
olved in the transm
Two nc:urons arc inv
-----
- ·-- - ,
.......
-
~
,~J

.. I~
-~
..: • -
r ·::;..a ·~
-- J

elTector orp A.
► PR EG AN CL IO Nt C
The c:cU bod ies ■re
NEU RO NS :
either in the brain or
brain arc cranial nerves
stern and their nerve
ter

in the spinal cord. Th

111,Vll,r x, X, .,;sin&

ose originates from th

from nuclei in the mi
tside rhe brain. Th e
minates ou

d brain and br11l

cell bodies or 1\1c aao
rnl out On
~
ra1
TES
PHARMACOLOG'I' NO
~
-
· c or

(
(
(. fll ,\
~-
~ --,
.,.)
" I'll ,_\
,\
orutc,,1,.
Th= rttq,tt,r, .,., sclC'<'tl,'Cly _,-.icJ by nk<-1,ne an.I t-i...1:nl by .i-111ht1C\1ran n Cont raca~ 1roo<Jlh
..
•
hQamclhonium. D. GLANDS: Chu\incrg1c ,11mul1111on - J b c p$ltic inlcstin•J and pancu,alic
C. scarctlon, do,., 10 1hla th~ hwl saliv>CX, barn 111I, n ~ I sccretion_:i_
These l"C<'Cplllr, IK"I t-y h$And p t<d i"n chonnds. ncti\'olio11 of 1hc nicotlnlc r"';•1>h•rs
shews the orcn"'8 of ioruc channels,. hich inm-ucs the cct1 rm11c1billly causmg Ilia
C. I'll j ere uui,ncntcd. - -
<krobrisatio n. -
". - ; - gahv.ary scctctions arc p<olu.'IC and watery.
-,-••
-)
C. EYE: Installation or Ach in the c:yee it is DOl abso,t,cd.
On lbc buis ofl001tion of sdn.'tivc agonist and antog,mist thcn1e nrc o_f two trrS': C. I -> ' Conslrictian o f pupil is seen cao.aing mio,is which is due w the contraction
N.., These -
Mediates ,k-cld:IJ m~
--
- , in skdccol mll5dc end pl3ll'S -
Stimulu,,d by phen>1 trimeth)'I ..,,.._jun, and blocked hy d-tubocurarinc.
l--.
.;.;;ction. ;- II,.)
,)
.)

of circular fibres cf sphincter papillae by reducing the in1noc:ulw tension.

• Conttaction o f ci\i:uy m uscle and the ~ taxation or suspensory ligaments of
the lens will reduces the ocular lemion •
It causes inc:n:115e in the thickness and dcctcasc In the focal length of the
•
Ni<: Preseuc in the gang]ioaic cdls and adtezul mcdullacy..cclls..12inal00rd and ~erUiJL
;__11 _) lens - spasm o r occommodutioo
~--.)
areas oflnin. - -
NICOTINJC ACTIONS:
Stimulated by dimethyl phenyl pipcn.zium and blockl'<l by hexruncthoniurn. ~.JII ., A. AUTONOM lC GANGLIA : Ach induces pngliooic stimulation due to the
increased
output of Acb aod NA &om parasympat hetic IIDd sympatbctie nerve endings.
.• .,)
~--•-,
I. CHOLINE FSTt:RS: Eg: As:rM ~olinc
• It increases lhe blood pn:ssurc due lo peripheral vasoc:oostriction.
~
PHARMACOLOGICAL ACTIQNS: B. Sl<.ELETAL MUSCLES : Stimulation or somatic nerves iocluces the cootraction of
Oq,a,ding upoo the type of n:ccptor l.brough which ii iJ mediated the actions or Ach sk.cletal muscle.
are cm:goriscd as mu,carioic or mcotinic. • A very hif>i concentration of Ach at m)'OtlCUr.il jUDCl.ion causes the paralysis of
, .) skeletnl muse\.,,,.
r-- -
-
MlfSCARl ,cJC ACTIONS :
A. DE.ART: A~ shows the hypcpolarisaliun of 1he SA node and dccrcu a in the
d~ti_o n. decrcues the impulse gcnentiou.
Effec:t ofAc:b-on the bean is due to vagu.~ slimulanon.
•
c- •
c -• ~.)
.>
• Intra arterial injection of Ach to the bronchial artery produCl:OI fasciculatio ns of
THERAPEUTIC USES:

skcle1al muscle followed by prolonged weakness.

c-• -;)
•
•
-
It causes bndycardia and cardiuc m-est
Decreases the· co111ta dici~usclc ( • ionouopic effect) nntl causes
AV blocbdc. --
~-•,)
c.----,)
• Ach choline is not used for aoy therapeutic pw,,ose.
• Ach substitutes like Mc:1hacbolinc, carl>hachol, bclhaoac:hol arc 11.~cd.
~--••·
• Bcthanacol is used for post- open11ivc paraly\ic ilcus, abdominal distensi on, relief of
• 'Veiiiriaiar contractility is NJuced. gastric atony, urin11ry retention. congenital mega colon.
• In;;;;;;; the conduction ofvcl~ity ofutria.
~ ADVERSE EFFECTS:
,-,--•--~
,)
~
B. BLOOD VESSELS: Ach dilaus the blood vessds of i kin and 11ucou1 membrane. Flushing
•
.- W1iciiiMJ rcc:cptors a"!_stimnlatcd the ~
dotbelial cc].s releuse nitric oxide
~
it • Salivation
which caiuses~ ar rdaxatiun. If the mdotbclium is tlumngcd tl\en
• Sweating
caases VIISQl!ar contraction.
• Bradycria
J=e
• II also dilates coronary arteries.
• Hypotcnsioo
~ -~
• When ii ;.. adminisl«o d Uttough IN route ft SOMc or warmth in skin,
• Syncope
lbn,bbing headache is seen.
C. SMOOTH MUSCLES : tone and rhythmic activi1y of smooth • Bm11chill spasm
. ~ e a ororr and cau.~~7 is1s. - c~ . !-,-Ocaasion ally cardiac nnhythmiu s.
• Cc,nlrac:15 smoolh mwcclc of gall bladder.
CO~IC ATION S:
• Contracts dctrusor muscle of urinary bladder.
•
- -- - -
~bronchial smooth muscle andciiu5C8lironchospasm
··- - - •
-
!fyperlhyroidism
 ..
p• · , - .
,~ ,\
; •)
; ,)
• 8nindual asthma
~ -~
l'IIAMMACOl.(K;! CAI, AC-I Ull'l!I:
~-v
• Pq,ric ulcc,-
.C..~,)
• The phann.1cnlui;kol 1(1iuru, o f 111t<,pinc and ac:opolmlinc: arc simillt except that
• 1'l)'t'CU'dJJ\l mft11e1i"n.
Alloplnc la CNS stim111ant whcreu Scopol1mine iA CNS depressant .
• si1e af choline, c.<tcra.•c •11J h1'\lmh"" 11 1<1 a~c-lic nuid
• Allopinc h.u longer dura1fon of acti,m than tlw of scopol.mine.
• II ~'<!UCC\ tern~• ,nhiNbon llf the C"IIZ\'nlC. ,. u I . SECRETIONS: The bc11"'1onna albloids reduce the ,cac:lio,u of the exocrine glands
• •
l=1o·c:rs,1,tc llh<lline CS!\'n.<cs \\ill «-mt-inc •only with the cs1c1i~ site of 1I,c cho inc
cstcnuc and the C$lcric site ,nil~ r'bospboryla1t\l.Thr hydroly"s . Of ..,_"'111101}'
•"-
1RIC\1 c•j c~tcpt lhe production of mllk.
/ Salivary secretion•: Atropioc blocks the wala)' salivary secrdions and _c a~
site is slow a n d ~ im,,'Cffil,lc inhibition of the cnz)'mc.
Q • l art anti-<hallner,:ic. Cbssify them. '£l<plaln th• pllannacology of atropine
; ,) dryness or mulllh and difficulty in swallowing.
., • Cutrlc ncnllons: It red~~- voiume of pstric juic:e "1d total acidity of
g11.'ltric socn:tlons.
._.)
~ .
Anll-dloli~c arc ihe drugs • ·hich block the ~•lions of Ach on nutonomic efferents It also reduces the secretions ofmucin and gastric enzymes.
~. J
and in lhe CNS c.,cned lhrough muscarinic rccq,1ors. ,- • Other ucreriaas: lt reduces the secretions of nose, mouth, pharynx and
■.
-- ~
C
~-•.
Atropine is lhc prototype of ibis group and is highly sclcclivc form~nic rea:plnrs. bronchi 11 also reduces lhe sweat secretions in low doses.
,,.._ '..) 1. SMOOTH MUSCLES:
CLASSITICATIO:O.: • Ctr: Atropine reduces lhe tone and moulity of all !he plll'.lS of the gut showing
I
~~ anlispusmodie effect. 1t blocks tbevagus nerve stimulation.
•.
A. Nalur.ll albloids: AlrOpine, hyosciuc (scopol~c)
•-.)
, B. Semi synlbdic derivlllivcs: Homacropine, Atropine mclhonitrntc, Hyo14cine butyl ) • Biliary tnid:Atropinc bas weak spasmodic action on biliary tract and gall
'- bromide. bladder. - - -- • '
~ C. Synthetic compounds: • Urinary tract Atropine reduces normal as well as drug induced un:ter.il
I. M)'llrialics: Cyclopen1alonc. Tropic amide
2. Anli-sec:mory- Antispasmodics:
L Qoalf:mlU:y amines: Propanthclcne, Oxyph~'tlooium

~
. _.)
~

.)
peristalsis. In thmp...-utic: doses it reduces lhc tone of fundus of the bladder and
enhances the tone ohrigonal sphindcr ca1Lscs unnary n:1ention.
• Rronchil: Alropine relaxes the smooth muscles of bronchi w1d b1oucbioles. l\
( b. Tertiary ammcs: Dicycloamine. Oxybutynin
C ■ ..) relieves b1onchoc:onstriction produced by the cholincrgic drugs. Since, it dries
up lhe seaetions ii is not rccommcm\cd in bronchial asthma.
Anti-parl.illsonism drug:s: Trihcxypbcnidyl, Procyclidlne, Biperidin
■ ..)
.
• IJ1£ru1: No significant effect on tone and motility of uterus smooth musclc.
ATROP11''E:
C 3. EYE:
"■ .·\) • On low inslillution 11ll'01)ine produces mydriasis by blocking the c110\inergic:
L Two importa.nt alkaloids Anti-parkinsonism dru&S: Tnliexypbonidyl,
" -na\>~ -----
•- ,)
Procyclidine, Oipcridin.
_.) • II paralyses the ciliary smooth muscles which causes ti&)11cning of suspensory
• orBdladonna are Atropine and Sa>polamine
" ligament, results in flattening oflens with inc:r~~ its-focal lc;gfu
,.~. _:,
• Atropine is an ester or aromatic organic acidcalled tropic acid wilh an complex organic
• Because of sphincter -paralysis 11,e individual cannot constrict Ille pupil foT
base atropine
" • .3 viewing lhc objects clearly or .i n response to hril!,ht light. This is called as
l\lECRA."llS~I OF ACTION: ~ paralysis of accommodation or cycloplcgia..
• LoC!ll instillation of 1o/o all'opinc drops causes ma.xi.mum mydriatic effect
•
•
The .Belladonna all(aloiils blocks the mll.'icurinic cftects of Ach.
'The antag0aism between lhi: Ach and mtropinc is c1.1111pctiti11e type which is revmed by
C.. ,_!'!ithin 3 ~_min and_TCCovery ~ ~ ~1in 7•10 _?;-ys and lll&x_im~
,:~ ~ ; cy~lo~llhin 1-3 days. recovery within 7-11 days.
increase in Ille concentration of Acb at mu~carinic neuro effector site.
'.l. CAR.Dlo'VAs°CULAR SYSTEM: - -
• Atropine is more effective in blocking th.!, c!fi.'CIS ofi\ch than the effects of cbolioergic
• 111 therapeutic: dos1.-s atropine reduces heart rate , ll,is effect is fol\owe_d ~
nerve stimulation. = - - -
~ycudia particularly tn young individuals. - -
• ~ ~ d r u g that isrcqnin:d for nerve blockadevarL~J!'Q111.orM11 tooigan.
lncm!$C irt lll~}1Clll(fuLis_ 4~e
• Salivuy or bionclual ~ n s are sensitive to atropin~ blocbd~ wbile ~ SIIIJI..Otlt
muscle oflhe OIT, eye, anil the heart ere less eff~l~
~ . ·-·
- . . . .'11
•
_.
pacemaker.
to l>l_!)ck,ing_of M2 receptors ln the SI\ nodal
· -- - - - -
• Jn !argcd~5_'."5 atropine blocks tl,e nicotinic llCtions of A~~~Dl!l!!,!~_l~f~~a.
\J i"~-t r/) 1ii cf(; ...1 {Vcud,. l 1~
 .. -,
... "'
~ . ,t
• In 1h
n"l'<'ul•~ .i.,,.,. ~1n,.,00 "'mrl,'1.-1)' ,.,,u111
h, ..., m1I • &.'IOOlilol i<1fl lllkl
m 1 • l'IC'l'1• 1 · : I \)
J. M1ilr.ln1J1.ll!lll.ml29Juia;. _!! ~
J..'= dalat,c,,n .,, culall".'<lt
11,,.
hyr,,,.,.,,..., ea,~«-1 h,•rh.,liu,ri.,r •~"1'Mn.1<I , _ I , ~ lls in 1ln-'f'lno tlu.,ih nml
;I" • Due to m ydria11cpnw ,aty ( d1lm oo <tfpup
,l)a11 opme o u,c,d indJC lra1c mcfll
In 1,,\fc
.:_ I v irilia, lri<loc yclh b.kcn lilll.
inll.wncd nn& ICW -. o f ins and cil..r y body
.
h~l''la\.<>,m.
.:.1 \) Atropine nxluccs the paiD by rclu in1
plr.C,oncdioa c,( www ,,oda ti"" -,uo
pia.
5
0'1'T R.'\I l'-'TR\'01.IS SYSTEM :
• I n lhmif'C'\lbc ck'>C< ,1 cusc s
• n,iJJ $1imuli tion of ,-.gal nuclei ond highe
r
-
-l~
• UIOd in IRalmcn& ot q,:Jo plcgja . Eaaa
4. il.6.. t&EANAP.S'.UJfflel,1!!DlCADQN:
ml llled lOmia before pn,:n l macs
tbcsi L
.. \.)
:1
C"C'n'bn,J <Ulln::. _!..-PN: anaa lhdic dnip an adminislc
and ina-cssc in nJC and deplh of ilc pnea l ~ may pn,ducc unplm
sad.
~.- -Jl y i1 rioou a:s breJ)'CM\h• -•- lfae of uropi ne w!1h - inila lll YObl
TC:$piranon. ION: throat •
• ID itt'tic doses Atr0rine r roduc<:s cxcita
lion. :-I .\.) S. CARDJO v ASCl/1,,U CQND[IlONS:
rigidi ty i n ~ bloclc clue ID Yap! adivity.
In modcra1e doses 11 controls I l l e = and y Alropinc ii weful In aboli shing AV
~J~ ..,,.-, U111:ful in countering 1bc syneope and
lm,dy,:adiL
AO\ fE;
parentcnl site of administration ml 6'11111 IIUICIII ...l "' 6. IJRINARY INCONTINENCE:
..-·~Various synlhctlc:substiwtca llkodicyclo
minc , oxybu1ym, -ma l to rcdu ceun mble
• Atmpiru, obsa vcd &om GIT. from
mcmbr:inc.
;.i ~ d1.11U1or contnctioos.
• Pwy de 1oxi6 cd in li\'er and J)31'1ly cxcrt
tcd unchanged in kidneys J..:) CONTRA INDICATIONS:
• Plas m.tv.i 4 bows
• Cros s the plnocntal bAnitT" and is s«rcl
ed in milk anJ saliva. ~ ?.,)
;L
Atropmc should administered with caution
yPal icnts over the age of 40 as it prccip

in
il31c an anaclc of ac:utE a,ojc sti"" &laucoma.
_,_....lacliYiduab with ailu-ged prost ate
as rac:nlion of urine may dcwl op.
~~
ADV ERSE REA CH ONS: reduces secretions .
n, bluning or _,. OvoDic: lung condition - drying and
owing, 1achycudi1, fever, c:onsdpalio
•_. Dl)n css of mouth. difficult in swall ,,> Coagative heart failure •
,~sion, men tion of urine in ddcrs. r--- Pyloric obstnic:tioa, aodi o span .
• l'r<.-cipi101cs glaucoma in elders.
nctivitis and swellio, of eye Ilda.
:..i..~ 3. Wlia t are sym pthomlm elkL Class
ify them. F.llpllla Ille pbar m1t olo1Y
or
~
• ,,, AUer-gic reactions like dermabtis, conju adnu llne.
SYMPAmOMIMMETICS OR ADR ENl '.RGIC DRUGS
PREP,\RA TIONS ANO DOSAGE: AIII:
ut.~ ufb11l1sdonna hn mimic the respo nses obtai ned ~ a ,esut,
of
/' .Belladonna dry e:xtracl - I% of lhe alkalo /Syinpalhomimetic m the mu~ that
.,,,.• BcU3donna tincture - Dose: 0.6-2ml. c llimullllion or sympatbdic OI' ~ c
nc:m:s.
in an inlaa orpa rtially substilulcd l-NH
, ) llJ'OUP 111\d
s or in powder form.. I>- . 0.2S-2mg. ~ 3 ~ j orityortbcsosubslancesc:onta
• Alro pine Sulph~te - Orally 0.5mg tablet es.
bmce me also called a, symp athomimctic amin
~
{
• Atropine eye oin1mc:n1- I ¾
inc sulphate jq Sm!: Doe 0.2S-2mg SCIIM
• AITOpinc sulphate injcc1inn :0.Smg of allOp
cus smC AnoN:
~
THERAPRUTIC USES: A. Tbcn peat ic clam ficatio11:
blood pressure: Eg: noradrenaline,
1. Adrcnagic: drugs used for msma
I . Gastmintesrinal Colic : metaramlnol, phanylcp,ncpnne.
colic pain. lnotr opic actions on the bean : Eg:
dnpaminc, llt1bu1aminc,
~
~ Controls hype r motility and 2. · Those used ftw
:,- Consti1>3tion due to spastic slate
of bowd is relieved. e.
isopraalill
~
Conlrols spasticily induced by lead and
molphinc. · amphclamine, dcxtro amplietlll!line,
~ 3. Those used a , _ t N ~
2. 0 1her colic..~: mcth}4phcaidate. • - -
trca1mcniof bi!ilr y colic,
• Administered along with morphine in !ht =e
4. Thol · :
• Atropine along with ~ hine is u
sed~ L on«k divc jJ atimullll!S: Eg: ~ inc, isopmialinc
Atro pine sho\Ys lhc rcl_~ anr cffcctOAb
iadderWIIJ,
•
 c~ •
C. 11111 -.)
C. . . __,
C. . . --> OP ADR r.NA UN! t A."'10 NA:
truno l. 1CltNlallnc. PllA RMA COI. .OCt CAL Acn ONS
b. Sdc- cn, •e f\, bloc l.as: q : ..Sbu C. . -,~
Eg: ldrm ahno . ~ n e ltaznl;,..,, phcoyl and II •s,:,nisL
Adrcn•linc lets u ■ _.se lecl i,c a
r.
J
.j
~
(

5. llios c, wrcd in allcr pc rc:ac:tion•:

6. l lll'llle U$«1 fnr local ''UOCOnstn
q,hn ne
B. Thes e dng s •~ also d.... n,,,s
I. Cat<'Chola m,nc s: Adn:nolin
2. Non -a.tc cboh unin cs: Eph<

u :

ctw err« t: Es: ad!UIIIUM,, """

e, NA, Oopa mina .
drinc ,

C..
c., . II ·u
c. lll'u
~
~ Noradrenaline Ids -
-1. CVS :
ac.lectlvely n a IOII ~
A. BLU lT: Adr 11imul■tcs 11
contraction end

aai,nuL
1'tCC p10n of ~ and iDa-e
lhe coaduetion vtloaty.
✓ I t alao increa:ics card !~ outpu
t by .-in & vm ~el ion

asa 1he n1e, fon:a of

Oms lncn:uill& the
3 "" • .,v - . s tt1\IDl and i.n creu ing the force
or aria! coolnil:UoD.
cardia in rcsporue to carotid simas.
C.
1'
CAT ECB OLA M11 ''ES:
d atccbo1311'
· --C · cl---'
• 1incs m uuc the symp athet
ic n1:urol111111onl bWIS mitia s like
0 PllllUnc, . the main hann one a( adn,n aJ

NA and
medu lla Ilka ac!Rnaline me! synlb
dic: c.·• -..l- . )
c -•
✓ Adr abolillbes lhc n:111:ll vagal bn,dy
✓ lt enhances conduetion ecruss \he
✓ NA does not increases Ille ~ 1111e
AV node and prod uce ventrlcwar
11fflhymias.
in• iacact lllimal but h:Nls 10 pn,clu
c,c bndy canli a
c-• -..l
c activlly.
~ due to compeosatory VIISCUlar reftc,,
~ mpound 1"'pr cn:tl ine. SSU RE:
_.8 - BLO OD VES SEL S AND BLO OD PREu, membnoc arc coasaictell 'by A.di and
~--=-•-~
Cl.
r . ► U ~ ~anun
l D F ACT IONadio :}
n by direc t jp(,m dion 1'Qlh rcccp
uns tc,ca1cd oa the • Bloo d vessels or skin and omco
~
.c:; ' es prod uce their
Cate cbol
- NA. of
-=-,.)~
\,)
~~-
111
cclJ membrane.. of skcletru muscles on aeco\11
i n ~ (mtcilatioP) or Adr dl\ntes the blood vessels
&ad drug com biaat ion is cilh« 1111
~
1" • by
► The ow com e of this rece ptor Iowa s the diulo lic blood pregsurc
.
.....
dccreru;c ( inhibition ) in the tiuuc
ity.
activ prq, ond ma~ of beta ttecp lOtS. il
pc:r iph~ actions.
V
► Th~ e arc two n:cp lors a and
II ,
;~ Increase in 'lhe systolic blood pressure
ucctl 'by the modctatc doses of
prod
~--•-=,.),.,).)
clfec ts of c:atccbolamincs. • RIC \s called
a recc:p10r stim uluti on-c xciw ory Dlpha receptors. This t<:SpO
.-h B rcccplOc stim ulati on- inhlbitocy effec
► a ■drencrgic rttp

ts of catccbolmdnca.
ton ,. re of rwo tn,a end s. a,
Adr often rollowed by stiroufating
as biphasic response.
a rise in bolh systo lic md dias.tolic
blood
I r ~
a-
,z adre gerg ic ~ G ; BR ac:icacx,,y in
natun: and act da.rougb G-prolien
( G,) • NA in an intact animal produces
► rea:p1o11
ci, pressuree.
~· , .... ,.
..
-- iated with rclle1t brtod)'canlia.
conccntralion of calcium by
-,.-)
~-.~ • NA induced bypc rta,s ion is. assoc
.
,... . ■
(
way , increases the lntlllaellulac now in man
~ ► Act through IP, DAG path significant red\K:tioo. in lbc bloo d
• Bolh Aclr and NA p«>duces a
'
-:. . ) ~
7 . the activ1nion of pbospbolip■se-Ccalciwl1 will eccou.ots for lhe ~timulating dfco ts of
CIIZ)lfflC. BP.
even in doses thal have no effect on
p
~ 1-, ► The inae3$C in the intn cdlu lar • ll reduces tow peripheral resistance
.
-i. ptor s.
agcr us !hat biod 10 01 rece coupled receptors by Adr also n~ the sy1tollc blood
PJCSSurc
J ] ~
through inhibitory 0- protein (01) C-:11·~· ) •
d vesstls ond
r-
;
..,
'. .t ~,.,
►
►

Alpb a2 adrc nerg ic receptors aet

inhibiting adco ylcy clase and redu
The se rece ptors activ ate G-p otim
ces the c:yclic AMP.
gared potasaium clwmels.
c - -,, • Both Adr and NA amsmct lhe hepatic and mesentcric bloo
raise lhel)ONl venous PR:U\ll'C.
pressure is raise d by bolh more by
Mr.
► TI1e activ ation of a, m:ep lors
ill the adreac::rgic nerves inhibits NA
rel1:11.Se wbere as
ing factor(
c ·' -.> • Pulmonary encr ial and venous
Adr on moderale doses increases the
caebra\ blood f\ow and 01tygcn
activ ation of vascular m:eplOrS
cause the release of endothelium relax •
~{
. ,;_-1
►
EDR F) which brin gs about vaso
a.
b.
Bd111 n:cep«ors -

diJalion.
Del a regp l9r1 an: sub divided illlo
dlree sub types:
se.
myocardial llimulalion 1111d rerun relea le vasodilation, uterine
BeU2 receptors- bronc:biaJ ~.:e iax
a1i on, skeletal musc

" .. . . 3
C. ..a _l
~
l, SMOOTH MUSCLES:

consumplion.
A. BRO NCP II: Adr by its beta tceq
smooth muscles.
)lor agonis1ic 11ctivi1y it rcla1tes the
. _
bronchial
_. __
~
rding 10 the
ls lo the catecholamines varies acco
{ <
t- rcla utio n.
c. Bc:1a3 rccc plon - Brown and whil
e adipose tissue, rcgalalcs NA indu
ced chilllges in B. lJTE1lUS: 11ic=poose of the ulel\
, -presence or abSl.-nce of gcs\3lion, perio
d of
species, the -pbu a of oestrous cycle
;} ~
..
· . •
-·-
ener gy meta boli sm.
aors by stimulating the adai yl cyclase gestation and the dose administaal. or all the fllctors.
, ► Reta. ad by srim ulat iaa Ille G-pulim ( (is) rccep u:d by these compounds irrc~pct\\vc
• The I'll ulau s is rel1u
Intracellular cyclic AMP levels. is stimulated 10 con1rac1 by
enzyme. llus results in dlerileofdle • 11ie human non-pregnant uterillG strip
by sLimul1lio1 protein 1ti nose.
,: ' s.,- nic cyclic AMP acta 10 die cell fimdions adrenaline.
►
J
..,,l
l1 u
 <'~ - ' -
~.- tlll'
r . I',\
c. Ill \
• In t~ 1.,,, mon1h llf t'ff'l!ll.tne)' ..ltfflahnc ,t\h,blts utcriuc
,'\!11tr..11MIS o1MI c.. • \,)
cau.!IIQ utmnfl' ttl1, .al•"'I\. C. . v
4, Clanlry 111111,nthlytlc. ~•pl■I■ tllt pll■rmacol"10'
of IMt,i blocken.
itJ "'"tlloty. ,
C. GI r : A.tr and NA ttl "' lhl- _,,h m11Jelcs o f the It'll
0 . OTltE k SMCXl TII l\l l 'sc:-Lt:s: Adr c,,ntm,1.1 the
1ml ~luce
rn.,,11.,t,,r n1u....:le .,r 1110 hnlf c.. lll v ), i\n,: /\drencrejc bluclccra ore the drug, wbidt 111tagc,ni,.,.
lh11 r,<eq)IM action ofadrenalioe
3

fulhcle.
• • t'c,n1ne1, the ,-c,,e,tl srh,n.'1"1' and tho lri11llno rclnxa tho
· £\ 1':: S),,•l'Olhc-ci.: l<limwlltic,n r...its in n,ydruuis due
dctnl"'r muscle.
toount111Ction <>fn,dial muscles
o f the ins. Adr on toric&J odminlstnlion do not rc&dily pcndnltC
rod
S into the C)'Cball. It
and glaucomolo\lS GY':'

c.. •
)
C.C.,.. ... \v
\.)
v

Md otha rdalod drugs.

► 'lllc,w, drug.t may either block a or I} n:ccpwn or both.
a. adrrHr pc ltloclwi& •SC-II
► 'fbcsc arc lhc drugs which inhibit ad,..,..gjc ~ medlllCd
n:ceptor1 wi1h affcc1ing those m«lialod tlwugb Pn:c,q,IOB.
lhlo11p, Cl lldn:nugj~
P uccs IIINcn tc n-ductio n in inlnlncl1l1r pressure in nonn•l CLASSIFICATION:
o(respin,tloo. (liven 111
◄. RESPI RATIO N: Adr as a brondio Glal(lf and wait stimubn t I. Non -selective a 4drcnergjc blacken :
IV both Adr and NA induce •I""""!, Adr in aerosol form
VCSS5~ llnd rcli~cs bronchial congestion.
S. METAROL IC [ F'FECTS: Adr inaascs bl-1 sup: 1cm.

constric!S lhc pull'!,onllI)'

bl()C)d luctntc,.!!!d p!Pl[lt•
C.-
.
c • v
v
,
a .phnlo alkyl wnlnes: DibcnamiDc, pbenollybcnzammc.
b. N,uural and hydrogenated ago1 albloicls: EtgOlmtine, Ergotox
ine.
-~ ,
2. Selective ci, adn:oagjc blocltas:
Im: f3lty Acid cona:nt ralioo and ICNIII p0tmi ~ levels.
;;dim, ,- ....
6. CNS: ~~ cross the BBR Adr prowccs 011, 1rcmor, stupor, vomiting. ltld
. --..,)
~
Quinaiolincs: Pn:wsin, ter1120sin, doumsi n, lndonm inc.
3. Selective n: blockers: Yohimbinc.
-
rcsllC!l.~ncs$.
by 11d on both sides of
7. SKELE TAL ~WSC LE: Skdcbl muscle contmclion 11-a drenerg lc blocke n
.
ncuromUKUlar junction. ~ II
.-\) These are I.be ~ which inhioits lhc a d ~ c
mediale d
►
:~ ■ "
re,poDSC S
rs ..Uercic bronchospn!im.
8. ANTI- ALLER GI C ACTIO N: Adr releases the malinto
ns from sa!Jv4,Y gland. receptors.
.- .-\)
9. M ISCEL LANEO US: Adr produces thiclc viscid secretio
> All I} bloclu:ni are competi tive blockers.
of their rnpid inactivulion in
ADM[ : C 31c:cl,olanincs arc not administcn:d onlly bcausc
the gut and in the l iver. Ct.ASS IFICATION:
On in lubtion of Adr or isoprcnaline oerosol~ snull qu40ti1i
es ore absorbed in
d '- ~~ l. Non•sclcctive(lh and lb )
"'- •-
: l'ropranolol, sotolol. timolol
systemic circulolion. ~ L Withou t intrinsic sympalhomimcl.ic activity
Adr and NA arc mclllboliscd by catc~J !lc!}ly l tronsf,
•
n ~es (COMT) an ,..
·- b. With intrinsic sympathomimcl\c activity: Pindolo l
•-,~.)
mono amino oxidase s (MAO). c. Additional fl blocking a1.1ivily: Labetalol, carvcdllol.
2. Cardio se!ec:tiv e (ll l ,: Metaprolol, Atcnolol, Accbutolol
ADVE RSE EFFEC TS: 3. Selective (~11: Butoxomine.
• Aw- sic causes p11lpi1111 ion, throbbing hcadnch e and 11cmors.
c.:~•-.)
~ .
P1t0 PRONOLOL:
•
•
NA i/v causes anxiety, pallor and head ache.
Both Adr and NA i/v causes increase in BP, sub-nrac
ventricular aaythmias, and pulmonary edema.
hnoid haemorrhage,
•-- .)
(;
~ I _J
PRARJIIACOLOGICAL ACTIONS:
I. CVS:
the card,ac outpuL
A. Hl!ART: lt tcduccs the heart rate, fOfllC of 1.-untrnctions and
TUERAPEUTIC US ES:
ADRE NALINE is used in the trcalmCOt of
~--~:, It prolon p lhe syst~ uciqg ,_the conduc ti~n.
Due lo 1cdoction in the oxygen consumption eart and the
aortic pressure is
• Aoaphy factic shock
• Bronchial aslhmo
<;·•-
■ J
reduced.
It increases lhc rcfraelo ry period of myocar dial fibres
automallcity due to this it CMISeS dea-casc in depolarisatlcm.
and reduces the
• "Cardiopulmonary tesuscillllinn
;- Conlrol ofhlemorrbage. • · •
~■ - J In ~ u s e s the di!,~c prcssi on and increas
sta!,ili,atimL.dJeef:. -
es membrane
• NA is used in the tre:llmt-'fll ofshoclc; control BP, 00rrcclion ofhypov
alcmio
c! ~ II blocks the stimul ~c:tjon _of llkcnggj_c d~l!f ~~~
calcium.
~f diRo:itin ~
-
 <~ .
c - - -,,
r•-
C 1111 ,,
C. . . \.) by reducing the: li1$1 pus
n. BLOO
N .
DVESSELS: tllockn L....lil:ab.!a and cmscs 611.loJll'..
111111
· • Pruprnnolol in1.-.cucs the blonvallalnhty of c.bkirpmmazine
r~•n.,ei elT~ on 1114'<'d Y<'SSclJ<. but"" 1'1'"°'1P 11<bni1tis1n1ti"" or. i;roJ Y C • u ll~holi am.
Rcduca t NA release &om lhc symrathc11o 1mninals co1~•c.,
ttc:cplo rs.
·
hRed~ . rcnm rdcasc from the kidney causes marted
)'peftCO st\'CS

Ille blocltaJe or II
p '
fall i.o B m
C.. \.)
C. . . \.)
c• v
AOVl!RSI! l!FFECTS:
•
•
•

Increases myocardial insufficiency by pm:ipitating Cl IP and

Bradycuclia.
Chronic obstructive: lung diseases.

edema.
2 · RES l'IRAT ORY TRAc n II ~ e s the brondilal rcsistanCC
S)'Inpathetic bmnchodJlntion is olinima l - c. ·• .) •
•
Prinzmetal angina.
Ttredness, dcacasc exercise capacity.
Asth miiis rn~- ~ ... .)
.,_, ~ C .
3. CNS: Longte rm 0 f rroi,ran olol, cailr.ll efrcc:IS like behavioural changes. forget,.,......., • Coli.I hands and feet
mares:--- --- -- c-• -.)
.
.-
increas ed drea ming •~,
• Periphc:ral vascular diseases.
tic as WI oftidocaino.~ • GI upsd
4· LOCA L ANAE STHET IC ACTION: Potent local an.csthe
~ecaus c ofirrirant prope:rty it is not used Lhmpeulically as
a local an_!!~sthctic. c · --'- .;,)") • Lacie of drive.
Jit inCTCase.s illfplimia lfcc
S. Meubo lism: By blockin g adrcoag ic ally inducat hpolysi • Nigblma n:S ·
futty acid levels.
A plasma triglyceride level, CDUHDL ntio is increased.
II inhibits the glycog aiolysi , in the heart, $1cde141 muscles and
in liver.

c- -
;.._ .-,)
,. • ---.:i
• Forgcllulness
• 'Rardyh allucina tions.
THERAPEUTIC USES:
-,.. _.=-.-~.>
;~
No etTect on ooanaJ blood sugar levels. arrythm iu
Prolonged therapy reduces the carbohy drate tolcnnc e. • Used in the trealmcn t of hypertension, angina pectori.s, cardiac
6. Ske.lct:il muscle: JI inhibitJ • ~ i i r c e s e d trern0rs~ • Myocardial infraction. l'heochromocytoma, thyrotollicosis
Oow.
Reduces the exetcis e capacity by /l mediated incrcoscd blood • Migranc, anxiety, glaucoma, c:anliom}vpathy.
7. EYE: Reduc a the sc:cretions of aquoous humour. .-r■
liiir.iocular tension is reduced .
~ f w : t ~ri.
8. UTERU S: R~~ .ofl,tm•s is bl~cd by pmpran
olol.

'
~-•=·j
C ■- j

j C:ONTRAINDJCATIONS:
• Bronchial asthma
• Partial and complete heart block
• C-orona.ty artery disease.
ADME :
• Well absorb ed through oral administration.
•
•
•

Low bioavailability due lo high first pass metabolism fn

Oral: parenteral ratio-40: I
the .liver.
They are Jipoph ilic and penetrate into lhe brain e~ily.
~ .-_,d. -~
r; • - ~j S. Classify aktlelal muacle relaxan ts. Explain the pharm: u:ology
Am: f\KP UAL MUSCLE RELAXANTS
Skeletal muscle relaxants are lhe drugs that acl peripherally nt

of d-tuboc urarioe .
neuromuscular junction/muscle
fibte itselfor centrally in cen:brospinal axis to reduce muscle lone
and cause p ~.
•
•
•

Metabolism depends on hepatic blood flow

Exaded through the urine as glucoranidcs.
More lhaD 90% bound 10 plasma prolcins.
DRUG INTERACTIONS:

c·•
(a; -
...
~ -• -,
~ .)
-J
CLASSIFICATION:
l. Peripherally acting drugs
A. Neuromuscular blockers :
& AV node conduction. • Non-depolarizing blockers:,
• When used along with digitalis, verapamil reduces 1he SA ~ -J ► Lonpcting-dlubocurmine,pancuranium,doxacurium,pipecuronium
cs.
Delays rea,va y from hypoglycaemia due to Insulin and oral.antidiabcti
~ .. I_
rium.
• ► Intermediate acticlg-Vecuronium,;atr,curium, cistr.lcur ium,,ocu
lhc blockade of
•PheJJylcphrinc, ephedrine: will increases the blood pressure due lo ► Short actinc• Miv;acunn1um:
•
sympalbdic vasodi lalion. ___
Jndomethacin and NSA IDS will incrca.~es 1he aotfhypertensive actions
_ ..- ...
ofpblockers. c.! ~ • Depolarizing blocker, : Succinyl choline:, dccamcthorium.
2. Directly acring dlUgs: Eg: Dantrolcne sodiam,quinine.
• Cimeudinc will inhibit ptopranolol metabolism.·
flow.
• PropnUIOlol retards lignocaine metabolism by reducing hepatic blood
 ,...- ,
. .·,"'
; , j 1
tl -tut>o..unirfnc-(J'n,rorn,.. dnu;l:
:1v Al)MI !;
This is the dc.,tro .
chond .
. ·11111 alhloid obfaint"d &otu plwll
rot.:IIOfY q11,1rcmary ammoru
~I V • l>•tubo curarin c being I qua,\CfflAt)' ■ll)UWIUllm.CO
IJlpound not -~ from !he GIT.
~i,J!d ro'!.! omcn to:rm , ,.......J \) • The drug !J wcll_ahs(ul!_ccl on 1M acfminlsfration and
widely dlS1nbutc:d in tlsrucs.
·-
· of action : - • On IV administration o.ftll~p eutic ;i;,; skd&
l -;;u,clcs_paraly,Sis wilh.niboc!!!3rinc
,.._
Mech musm
• D-tuboc:unuine combines wilh lhc nicotiniC ~or s
on tho motor end plote ... '-' Williino ne tcrone onilliill'm in and pea cffcc:t i.s obwnc
d wilhin five 10 ,cvco min and
action pmist within 60-100 min.
and blocks the action or Acb by compclilive blocb
de t' · \) _.l 1dmin~~tn1io_n parentally is eliminated IIIIChanged
in urine wii1:in 24hn.
crgic receptors at
Competitive blodcas hmvc the affinil)' towards NM cbolin • 33~
• u 'ibe dNg cannot cross ~.!!! p_l~ barrier.
•
muscle end pl3re
NM RCcp ton is ■ proldn with S sub units (o2,ll,s.1,6)
which are arraoged
~
,. ~, •
ADVERSE EFFECTS:
•
in n>5ette surrounding ,odiwn c:bamiel.
T• -u a subuniis amy two Ach binding sites, tJiese
hove neptiv cly charged
... ~) L!-- R)'Jl()xia and respiratory paraly,is.
,.. • Hypotcnsioa
subunits which combined with Ach-opc:niag of sodium
channel. ,._ ~)
• Most or lhe compctilivc block m have rwo or more quartc
nal}' W atoms
,. ,'I _
,. •
• Regurgitation of £11~lric juice.
OcsopbagQ! sphinc!a paralysis.
which provid e attractioo 10 !be same site .
e with rccq>lor
~
• Ada i.e relc:a,ed io the motor tnd plate is not able to combin
Ill gcncrate ac:tioo potential .
,. I~
! ~
·-
Preparalioo and dos-se:
• Tubocwurinc injection in 10 ml and 20 111! vials contain
ing 3mglml dose 6-10
...,_ g and action
.,J
.....
• D-tubocurarinc nxtuces lhe frequency or ·channel openin
potential rcduocs a1 aitical levels , it is unable
lo trigger the action poten tiol .
e· -
~ -- -.) •
mg Iv initially
Dimdbyl tuhocururinc iodide - rv initfol dose 3mg follow
ed by tmg aftci-15
muscle !ails to mntruct i=-o sc 10 nerve.impulse .
~ -- ~ -.) min.
,-. I. .
~
~---
...... PHARMACOI.OGICAL ACTIONS : ,- l~
'" __ Therapeutic uses:
:._J
.,;.,,----1. SKELETAL MUSCELS:
• d-tubcx."llririae on parcnlflll admirustratioo i11itial1
y produces molor -,"
C'. ~
• Adjuvants ann~slhllSIR
• Electro coavul~ive therapy
wcalcness ronowed by naccid paralysis I • Spastic disorders
rs and eyes are
• small ntpidly moving muse!~ of the lingers , toes.ca
tasks and
~I ..> •
effected first milking ii impossible ro perform dekcalc motor C . .> 5 INlrks
wing .
producingcf.iplopia , slurred spccch ind dlfticuhy in swallo
I:
• !he muscles of limbs , neck Md trunk ore
affo~led later followed by ,.. I .,;-«i plala in dcl•il about tbe tttholqutt or local
anaesthesia.
..f' intcrcosral mmclc:s
"' I ., Ans: TECHNIQUF..S OF LOCAL A.NAESffiESIA.
~· hypoxia
,:;;
,. • finally diaphragm rs paralysed and ut:lllb occurs from
recovers first and small
"! 3 I. SURFACE ANAESTill:S JA:
ctics 10 muco\lS membrane
J • recov ery occurs io reverse order the diaphragm • II is produced by topical application of surface anacslh
muscles recovering later. ~ :,
..J'"" ./·2. Autonomic ganglia: • J
and abraded slcin.
• Only the superficial layer is anaesthetised.
I • In the doses used clinica lly ,d-rubocumine can
produce partial
t-J ~ • Onset and duration or action depends on the site, lhe
Jrug 11nd its ~vnccnt1111ion .
J blockade of borll autonomic ganglia and odrcnol medul
in fa1J in BP.
la and results
-
:J
~
• EO: Lidocaioe spniye d in lbc ihroat acts in 2-S
~0-45 min.

min and produces anaesthesia in

J J. HiJtamine release:
• JI cen produce hisfam ioe rrJP.:litP from tissue by
acfing tlir~t ly on ~ • The absorptiOfl of soluble maeslhdics is rapid from
2. INFILTRAT ION ANAE STIIE.~lA:
mucous mc:mbranc.
• mast cells. _--~
sed salivary
~ • Dl1111c: solutios;s of LA is iofilh'atcd under the skin in \he
ation, blncks
area of opa
• This mny ocaisionolly cnuse bmac hosp ~, increa sensory nerve endings.
trachea bronchial and gastric acid sectt1ioll.i-(_)
..--i- -- 1··
 .-,
I
,\
l
,,
• On.tct of a,,to l'tn is ,m .-h~r,- 40
d Jurnm'" 1s sh-->rtcr.
. .
,,
I
l Spinal -i. a; a it u.ed b
~ oa Iba lowa-_JiJJ,
~pc!Yi• '-c c.
SO nun • aection.
• H-s; LidNUionc-.10-(,0 nun. ll11r•"n,·A111c- 1:!IH sions, oml hyllnx:elc. and -
t'flC!fllll<'IIS likc incision.', exci
'\) abdomai. prom tcct omy , hclurc ICtf lllJ. -
ln lillrlltion 1s usc,I t,,1 min11r s ergct;;;i ~ -
c.-mr,ircd 10 tho lll'C'4 4JIIICSthclise
d.
' • ri. aavaugcouov
larg er llltl<'unl of I.,\ ,, "'Jll in:d '\'
I. II is safer. lost of
►
P r ~ goo d ap :si a
aad ~ tdaulioD wilhoul
• It d,ies n-,i aOc,.,t mol\,r S)':'!C'ffl$. \,\ II. -
th ,rca distal 10 injection
is ~ ~~T oum ea s.
~ COl\"DUCTION BLOCK: ~ pot a fcwa- _problem
The I.A is IDJ «lrd around OCf\
ll.
an 3~ sa J 41id J'11'3l}ffmtr:
• Choice of l,\ :uid its ronc

~ mm J.s SO lhal e
llion depends on the W1I
d ti0 n of oction.
' ,._\
►-, .._,
iii.
CO MP LICATIONS OF SPI
-
C11dlac, renal and pulmoury
NA L AN EST HES IA:
lfllypolemion aod isdl aai a
• Lidocainc shows immaJQ
A. FIELD BLOCK: II is producxd
IC adion so it is commonly
used.
by injecting LA subcul&DeOWlly. ,t, ,,
\ ,._)
~ResplntoyY paraiy11
1: ill rare, maialains bR:albing.
of rcspintoiy centre is more it lead
10 aeapiaillllly .-aJysis
.
intacmlal mu d• • cou piD
g and
eltle ml'I lbdoarinal ud
particular field. I Due IO pml ysis of
• 11 blocks all the naves in edures, sca lp
/
• 11 is done in hcmiorrtiaph 1
y, ppmdicectomy, dental proc ' ..,)
\
,__
pulm ona y cmnplicatioos can
-B. Byp ouu loa: It is due lo
occur.
blockade of sympelbdic ~
oudlow of
l1lJlS and legs.
stitching. and opcnrions on fore d to inJi ltra ti~. blood vessels decreased venous
n:tu m to bea n.
slbetiscd with lesser drug compare J"
,,- • urg er area can be anae
8 . NE R\, Z BLOCK; It is prod
uced by injecting llie IA around
tl1e appropriate nerve .-.:,
a!.~.,
ct: Hea dac he: is due to seepage
D. Ca11da eqa
ofCSF.
me: Rue neurological
ina 1Y11dn>
complicatioo resa ltin g in
spbineta:n.
ll'Unk or Oexus. t' prolonged loss of con
~! ove r bladder and bow el
d. b•-pllllCtlft.
cted nerve p.lc:xus arc paralyse injection inlroduccd during luan
• Muscles supplied by the inje "E. Septf<- nwnillgjds: due to it is due to Dexv.s initialioa oo
• The la1cncy of macsthcsia
dcpcuds on llrc drug and the area
to be covered
et~ ~ Na• sca ud YOlllltb
ig: after abdominal operation
.J.
by diffusion.
nerves are anaesthetised with
in 3 min, bul ·~ ,r abdominal viJca-a.
SIA :
• Eg; Lidocaine- intereostal
bronchial plexus block may lake
• Flooding technique is used

IS min.
for blockage of the plexus and
larger volumes -·~
..L
~
S. EPI DU RA L AN AES TIIE
• The spinal cord dural spac
root s travd.

e is filled wilh sem i liquid

fat through whi ch nerve
ac prim aril y on nerve roots and
small amounts
are required. • LA is injected in Ibis spare
't \,
~
mina
~ , t. J .... e blockJ are lingual, intercolital,
ulDAr, sciatic, penetrated into intcrvertebral fora ing on the site of
• Frequently pcrfonncd nerv
..Y / '/ femoral, bronchial plexus, lrige
minal, facial, and phn:nic.
operation on eye; limbs, abdomi
nal wal~ :.-.; • F.pidural --,t hes ia can be
«tio n.
divided into 3 categories depend
thoracic region. Epidural spac
e in this
X -:rr • Used for tooth exrraclioo,
c,.:r . , • f'
'v"
frac1ur~. trauma on nos. ~ >"''Thoracic: Injection is made in theofmid
regioD is oanow lnw 1 volumes
dru g is required. Used gencrlll
ly fur pain
i -r 4. S PL"IAL AN
AE STH ESI A:
arachnoid space between L 2-3 and
L 3-4 bel ~ selirl fullowing thoracic/ upper
abdominal surgay.
vo\wncs of dru g arc necdl:d
because epidural
• The LA is injected in the sub
t
• ow
' { ~.I )l. Lumbar: Relatively large n, pelvis and hind
the end o ( spinal cord.
spM'AI is wide. It produce
s anaesthesia of lower abdome
1/ .,>, • The primary s.ile o( action is
nerve roor in the caudal u.
limbs. esia of pelvic ad
~ en~ hind limbs are an. 1es t~e
d an d~ ~e d. sacral canal. Produces anaesth
~ ' Caudal: Jniec:tion is ajvcn in
•Low u abd om . / al and
upon the \'Olume and s : . for vaginal delivay, anortct
•Level o( anacsthcs,a depends . peed ofin 1ccuon. specific pc::riaal region. Used mostly
grovi1y of drug solu f,o,u nd posture of the pabenl. ..-
gcnilourinary operations. t
hyper baric or isobaric lo CSF ANAESntESlA:
• The drug solution should be · 6. 1NTAVENOUSllF.GIONAL d limb such that th1
• TI1e level ofanaesthesia doe
s" ~ t h . ,,_ _ aft I 0m•m. • 11 co!lllsts of injection ofl.
A in a vein of toumiquel occlude
ange w1 in change of,r-• er 'iis m includi
. sthesia d ....,
vascular bed to non- vascular ·
• The durouon of spinal anae d and its drug diffuses tiom paiphcral - ·
- epe nds on the drvg use
· • nene ending.
conccn1ra2ion. 5-l Omin.
. .._
•. · d within 2-S min and lasts till
Addirion of 0.2· 0.4 mg . • Regional IOlllgesia is produce
, -::-.,:
• 0 uurena1me lo LA
prolongs spinal anaesthesia b and orthopaedic plOCtdures,
aboull/J rd. • II is mainly used for upper lim
 )
)
)
.rc ,,fhi&h ~ ~ c i1y,
'' i,.,•au
8ur1•n~.111ne ,h,,11 1,1 ,,.~ t,e n1111lo)" ) me 1o eilher_
a clcpcnde 11pot1 1ypica1 ~rmK
al r-s,a
• D I ~ o:r myw,sthcnia pavi -
~ nco sli~ lnc or cdrophooium, e stralg!la wbicb
gnu i,e IM- lmpro.cmclll orm mcl
of ,pht drln r, ~
I ts bf genus _Ep h~ ~ • Adminiatration or 1-1.5 mg of-U
· los11 for J-41n.
l . Exp laio tJ,,. pba rmuo l~ cainie drcc u
. ol,tsincd &om !hep mnaodLbell adrcocrgic rece ptor s and a whh DOOllipninc ~ 1hc maa
.,,d ~ •Atropine sulphale 0.6mg 1M Ilon
An.s: E1'11£DRl;\'E: Ir is ..n alk4J
· ubrcs both al~
- c $OIi! of Ach.
Pba rn,, .<-ologkal actions: Eph.
.,Jrin
nss-
J
relcuses Na'from the ncn-c.- eodi TR.EATM.!NT~.
. contn1ciion .-
. . and increase in lho clll'dloc
outpu1. ~ in die tn: atm mt of~ p-n
s.
.,,..1 . CVs: lncmose:s 1the furcc ofmyocanlW
lnaases BP duc to pcnpbcritl'
'aS(M.'!OOStnCUOR _,,,, nsc. f
th ~
• Neostigmine is formedyused
Bc:cause ofiu short duralloo of acdo
a, d.R ii a.......,._. oflD lcna cc, WWDg alld
side c&d s -
•
. 11. ~ ihe presser •-r - o muscles, wtn log of muscles, agen ts 1ri1h
mt duntian of adioa and low u
c,rcd adm inis tnno o _ smooth m11$clCS, uterine smo t) ambenonium.
• Rc:p utcs bro ~tal fbladdo-. pn,ferred. Eg: Pridostiginine and 30m in amd while on oral
I 2. Srnooth muscles: Rclr lleosbgimae appears with in
sphmcrer ~ ~
iety
. the restlessness, insomnia, anx • , • The effect of p,,m iten l
.., in= rs rhe tone of rrigonc and. tiCd0$CS ti C4USC:S •
poly S}'Dap(1c ~ o n proclucC$ a resp
onse wilb io l br.
h , cmiscs the monos)'llllpllc uid • pjri d -,f g · 1& )0-6 0mg ,
' .
J. CNS: Stunufar cs CNS at I mpt
IJ'on ors and inac ase in mcn
u. .
l:i.l ld!V lty. 11111 ~ • The lbc:npy is initiated
by Dmlligimae 7.5 -10.5mg.
y ~ 'IJlllil lhe
'1"' ~ a time and lbc dose gnd mll
__,, 1 ambaloni11m 2.5-Smg oral ly at
n:flc.~C$ of spu ul cord. ·...>
. . .--v-- n. mllXimllDI benefit is obtained. 3-4h n!y orally or
~
ctabolic rate and oxygen consum
ptio cstenscs are 11SUally administered
,s. . . h • The rcv111n1nle anticholinc
t. 4. Eye: prodUCC$ mydnll!,hed rin e~~ I em
ll' S. Met abo lic dftc ts: Ep
ADI\TE: Absorbed on om! udnuntsln
, • RC$istanr to MAO
lbon
-,.~ puen lall: , to ensure smooth and
• 80-90% of fflCOYelY occms in
S1lS1ained effect.
2S% of individuals.
is u.,ed in its mmagement in lhe
oosc o[25-100mg once
~• De aminared in hv~T.
15% is eliminated in urine io an
uncb11Dgcd form.
,.
!.l
•,-)
• J>ra!nisolooe a g)ucocorticoid
a day.
as ll.alhioprinc used as an adju11m
t thm py in tesis tant
__, • Other immWIOSllppR$Sml suc:h
: I S-60mg oral ly. j.,.
edrine hydrochloride tnblcl 30mg, dose casca.
Prc p»r alio ns and dosa,:c: eph
Eph edri ne hydrochloride eHx
ir- 15mglml, dose: 5- IOml.
...
' ,_)
' ;) 4.. Wri te ID detall lbol lt die dns
p ■ttl111 oa glaucoma.
3. Exp laill ;,. drta iJ abo ut lllt
drugs acting on myu rbcn ia gra
vis.
t:, Allr . DRUGS USED IN JBI
Df.ATMENT OF Gl,A\lCOMA.
unu eate d il lead s lo
TR£ATMF,NT OJ,' MYAESTHE
NJA GR AV IS, ch intraocular tens ion is raised, if
Ans : DRUGS USED IN TRF. • Olauc:om• Is • condition I.a whi
ress ive we akn ~ of
'~ optic neuropathy with loss of optic
nUflle.
ri1.td by easy fatigllbility and prog
~
n.
• Myasthmia gravis is charaac: • ThJS may be accompanied with
loss oflltripberal and later centnl visio
stria rcd muscle. a ~oss ofv isi~n is
seen.
• II is M autoimmune_disorder
: cau se< iJ.i x.l b~~ of postsynap
JiC.D.eptO!JlUSCUll!L ~ • Most forms of g l
b) clos ed angle c) cooge11ital d) drug indu
ced.
Ach receptor comple~.
• e n - is classified into a) opm angle da ~c om a is due lo
e are degraded and cleared mach
faster than ~ • Etiology of primary gl 1~
b not lcn o~ but ~n
Recepto rs in the my ~c niu_uscJ in t i ~ neuro vuculllrization
and ~gment dispcm;ion synd rom e.
•
normally.
Ach may be reduced lo 70-90%.
tat • Elfflted ialr l ocullll' pnlSUft'; an
be reduced by :
Number ofavailable rcccprors for 2w of~__,_
• o lna as ing th eo ut _!!
ger hypel))lasia or lhYmnrna eous humour by lhc ciliary bod y.
• Many palienrs with this diirordcr may atu o Dea-easing the prodaclion of
aqu
of Ill ·
rome (Lamhcn-Eaton-;}_..,romc) a ormmunc n re • :
• Ano ther myasrhcnic synd • sm..tll cell car~ino na oftheJun "" gs. • In, acutt ......,..;tt da n5 Thi s blockade by iris results in
occurs ,n. asso . . w11l1
c10t1on 1 • ·- · · - _ .•.,... _ o .l'he uis is
probably bloc:b_the lnlbecular specc.
• The 11utoa11tibo.dies nre dirc,,ted lo rhe
_tlll.ci11m .~.:::.j
·- '·
:-lhe
e tem
.
nnals with the
~ - - • tbc intrlnC:Ula pressure
producin& severe pain nausea and ol\c:
n loss
. the ~ch release from nerv-e tccm -=L . '~-m nerv
ioals.""" - - ··- - -
decrease m . . . . . . . lo opti cllm phy.
• Myaslbenia can also be induct-d•
by pcn~illamilll: dUri th e trcatmcn1 of rheumatoid
ng
arthritis and wilsons rlis~
 ~
..I -~
.l
o
.
h s • mC'\lrrAI cru~
.
and• rrk" "'l"' "' ,.-,Ill rhWlll
-. - - --- :-- . · - - -m

' -
,vJi(llill~ 11 • ~
-
lDl 'lil ~
:i~
:, "
,l
~ llllt'nl.
d ,n all crnaJC11CY
0 Ad1uvanrs such ;,.s 81.'ftaznlnmMe art"
c,n1•lll)'C'
.". l '"•
:,..
~
0
may be infu...~'CI IV 10 k,.,..,,. !Or.
Once the :ICUIC alt.Id ~ co,11 mlk-
hron fo( ,..Kl,...■ngll') si...,,lc- claJ
0

Ko!I• i
II uC'C\ls pam ancn r drvJ dlcrapy.

d swJC J)' i, advised,

.. -
,.. I
-\)
~ r~;
M JCplalrt die dtpo Invo lved Ill Ille .
N£URQ Ul/MQRAL TRANSMISSION
OF
.,.• •-- ' h.. ... ._ .,, ANS.
M!S
s die ,yna pte ia c:aicraJ and periphera
l _,, _
o Cau se of r.liscd IOP is no1 know
0

n.
B«:iusc c,f the dedrn<d in vision is pfu
ol di-,nosiS is dela)'Cli .. .
.......
,,._
\,) ► Tnw mw ion of nerve impulse ,cros
S)'Sfem o«u a • a n:sult ofnc:uro
bmnanl tn.nsmiacr MltllllC:II: ialo lbe
synaptic driL
mlssion coul d be ei1hcr chemical or ?'!1
dral ~
• J\bi or goals of dru c lb<'napy arr
;
0 To nwn1:sin illl IOP bdow •iuc h
further optic flCIW ctamaae
, 11111
II
lbly
lo
.. '
\,)
~
-¥
Dubois sugg.sled !hat jUMti"';;.;.r lrllls
Kunho- motor cud plate of the skele
tal muscle wa QjJa l a 1 "iuult
of cum :at IIG'lle
~- 0 impulse.
0

oca a.
o To reset rhc: IOP ro a Iowa- level
To minimise the local and sy,temic
.
side effeds oftbo clrUp.
.. \)'-'
'
J
►
~e y- J>resmce o f ~ o,
Low ci-V ~ intuoiled by hear
inhibitory subslaDaS in the effc:dOr
t by a chemical ~a cr A ~
cdJ
choline.
o
diJease.
To cdUC!te the palicnl o1bout the '"" . ,.,)
'- He perfused !he heart of frog. He allow
ed the perfusion 0uid from a &oghem
1 IO c:oin c
frog will produces
t Yago stimulation oflb e domr
• Tre: itme nr : icatioo. -.J in 00ftlac.1 with the second .livg hear
o The iruriru llim is 10 achieve
20-50% reduction ill IOP with med ient and the doDIJ' liop . He prop
otcd lbe llrClt of
o The Prostagladin analogues ~
_ilio drugs iniliaDy onc u day. c-1.'l ~e cardiac arrest in both lhe recip
recipient heart i$ due to subst4Dc:
e n:leased &om the pcrfusioa fluid
d as acety1 cholioc.
. The lutisimc:e
o Bcfa _ a<fmierpc-: bkdea, timo
lol are wed.
~ less d T ~ ~timofo!.
;£0flUt
.. .,)
,..... .
'
initially ca1lcd vagostuff. Tha i it is
Cllle
'lb:ase illbibilol' is used orally m• dose
o O;Z ~ c of0.2S- ~
NEUROTRANSMITTERS:
o Acetazolamide, a ?rl,ooic~ ,-I..
I gm daily in divided amoLmlS. ide and
.. . ~
/I.. Acetyl choline
o Topical c.irbonic anb)'drase
inhibitor prepanitioos hh Dunolam -l .,..8:- Adrenaline
and are prefemd. - : ,,,)
8rinzolamjde can cause Jess toxicity
o Reversible anti-choline esrcnis,,
o Miorics s.bould be avoided in
gives salisliicforilY n:.,ults in glaucom
patients wilh ca1arai:1 t,cc;ausc Ibey
a.
may impai..-
..
- l.
,.)
, C. Nor adraialne
.,.. D. Dopamine.
vision.
~->
_J
ACE TYJ , CHO LIN E (Ac h):
Y side..cffi:ds. en~
ca11se canl io~C l!f_ ~.re spil 'ltl!I
o Beta odrenergic blod cm may
-- - -
Dru gs used in glaucoma:-
- ----- It
~ .>
,) • It is recognised by the s c i
...- Jf'i san ester of cbolil1c.
~ I is S)'lllhesised in the naw
fibre by the combination of chol
ine &om the
• Those whicl1 im:reascs l11e oudl
/
ow ofaqueous humolr:
Cho/ine..-gic agents (M"t«ic:s) a: Piloc
:apme eye dlOps 0.25-4 %.
~
" , •
exb'xdlul• fluid with aOCIJI group of
Ach is ston d in the syna ptic vesic
acetyl co-A
les and is released .,; ;o c~
like 'acctylcholine esterase and buty
ryl choline
,milie 0.2S% ointment. ~3 • Ach is mdabolised by the enzymes
Cholincstc:rase inhibito,s ex: Physosti
/
0 ~ Prostogladin analogue
• TKosc which deacases productio
s ex: utaa opn )SI 0.00S" eye drop
s.
n of aqueous flumour by lhe ciliary body
olol 0.25-0.S¾ eye drops ~ - -
es&tcrascs,
ADR ENA LIN E, NO R ADRENA

I
LINE, DO PAM L'IE:
J
--o- Non scl« tive beta blocten mt: Tun
o Sdecti ve Beta adi aiergi<: block. .
,J' Non selective adraicrgic against
Q Carbonic anhydrase
' • Topical ex:
inhlmtorr;

eit: Beraxolol.
a: adnlnaline 1-2% eye drop!.
Briaralami._ -·
• Systemic CJ£' rorazollllJlldc.

t •
•
. _. •
•

These are called II catecholamines.

Prcsmt iD the high CODCCPlrationsi
~ ~~ ~se .J fi'om th e~ callC
I'benyJ■lanine undergoes Jiydrolty
. forms tyrosine which 011 fw1hcr~~r
forms di hydroxyphenylalanine ( ~ .

tbc {t~ I axons oflh e neurons.

!1'- enylaianfuc.
Jation· In the presence of hydroxylascs
l1ti 011 In the presence ofhy

and
drox.ylascs
DOPA un_dergoes the.~ ~bo x)'.l alio
n-
 ~
,v-
.> ~r~
C. -
C. -

-
c._. ,,_)
,.\
,)
---
'
1r .~ •
\9·
\.. .,.. .
rn the P""'"""" oroorA. J"""'bo1.lc~ anJ f,,..,,.. ,1<•1"'"'
i,,o. ,,..0 ~,u~no
h \roit)llnlll'°'
<:. _. ,\,) · of nerve im.,u\scs
► Loc11I •n•cothc1la. l,1n,;k the, 11£'M"alloo rwd e<.1nd..ct&00 r· at all part:!
orlhc 111:umn wllffl they come In contact without c:.ousing structunl damage: 1il50
" )~~ .,,..r
. ,. ~ ~, ,,,r· lhnl is formed is l lnr«I in 1hc C}1l'f'l"<nL Ol'11'11nin_cs ~.,:,,ll,..,.
:,nd fOnn$ Nor ~nlinc wln<'h on fu&thcr mclh)•~ion f.m - -- ':-• ·v ► They ore nol only net on 11e11:,«y nave■ but when epplied to mixed IICUfOD It -·
affects motor impul,n resulting in rnuaculwr para!~
'--.
NA nnJ Adr N"Cstrored in Ll~~ lm,~~ul~_) c;. • \\ ► CLASSIFICATION: -- - -
v"'' I. Injectable anacslbctic:s:
S-0:PS INVOLVED lN NEl!RO UUJ\IORAL TRANSMISSION: C . \ )
~i=
a. Low potency, s1,ort duration:
A, IMPULSE CONDUCTION: cg: Procaine, Chloroprocalne.
1 ,\
In the resting membrane -1ium is present oursidc lhc cell ond lhC Po C -. b. Intermediate potency and dUllllion: ,;:-
present inside the cc:U. Stimulation of electric impuls-• In lhc cell causes sudden 1nc:reasc
d' • h - .
,n
.0 nsD'loVC cl. . u Eg: Lidocainc, Priloc:aitle.
c. 1-ligb potency, loogduration:
,) \..
,--
so ,um ID I e axo~ mcn~l'lll'I" thi.• is due dq,olnrisation ofthe cell. 1bc potasstU'."° ' tential
o ul of the ceU cnusmg hypcrpolariSDtion. The potential genttalcd is +20IIW, Acl10R po
C • __v Eg; Tetracaine, Bupivacainc, Ropivacaine, and OU,ucaine.
■-~
·-
generates in the ceU which ncllwlcs ionic chaoncls at the next excitable p$IS oflhe inetnb~C. 2. Surface anaesthetics:
C -~ a. Soluble: t.- f,
B. TRANSMITTER RELEASE: Eg; Cocaine, Udocaine, Telracainc, BeooxiDate.
__, • .... _,., junctional
u . .
,.t:'W'Otnmsmtllcrs (excitatory and iohibitorY) me SID""' ID - .r•·. cd - . I ,.) b. Insoluble: ·
ncrYe endings in the ston1gc vesicles N=·eimpulse gcoCllllcdwill pt0motcs lhcv~cles7'us. -
with axonal membrane~e calcium ·=IIY lakes placAI. then all the contcnlS of the _vcs!cle w'.IL
~·· I -. ).
(" Eg: Renzocaine, Oxetha7.ine
► Local anaClllhctics arc high lipid and low wat~ublc will-not be useful for the
be exuded otil from the synaptic cleft. .Proteinsukesynaprot1gmin, synaptobn:~, n~rciun transportation lhrougb the aqueous pbllSCI surraundingthe na-ve fibre.
arc locarcd'in lhcvcsicul.v and the axonal membranes are participal~ in lhe :f\J..,;aoo. wilh lhe ~(~ ► Local anaesthetic,~ consists oflhn:e parts: ·
axonal membnlllCS by cxoc::ytos:is. c-1 \) i.)
ii.)
Hydrophilic amino group
lntcnnctliate chain -
C. TRANSMITTER ACTION ON POOOSTJUNCTIONAL MEMBRANE: c- -
The relea.scd transmitter combines with. the specific r,:ceptor.; on post !UJ)c~onal ,_I _..> ►~e
....) A iit.>fil,liilic ~gmup.
the -presence of amino nitrogen these are the bases and fo_rm salts with the acids,
membrane depends OD excitatory post junctional polenlial and inhlbilory postJUllCIIOnRI
-I ~ ►t Jf the tissue pH is alkaline the free bases is· liberated and vro<1.uce the phannacolog\C1ll
potential (EPSP and lPSP).
EPSP and IPSP arc due to depolarisation and hypcrpolarisa1ion of the memb18J1,C. Due
to the presence of EPSP and JPSP nerve impulse is gc11er.itcd in lhe cell.
~ ---
~.:.~
:.1_~
action oflhe tissues.
►, Majority oflhc clinically useful local anaesthetics are nitTOgcn nitrogen containing
compounds either in the form of esters or amides.
~ ... ~
D. TERMTNATION OFTRAJIIS~ll'J"I'.ER ACJ'ION: j.' Ester- linked local anaesthetics: Cocaine. procaine, chloroprocaine,let:racainc,
Combination with lhc receplor lhe NT either mll)I degrad~IJY or ll can either~ bcn1.oc:aine
taken up bythe_POSlj~onal neurons_by uef~e.mcc~ms, 'ii.) Amide linked loc:al anaesthetics: Lidoca\ne, bupivacaine.. Oibucaine.
~I..:, MF.CHANISM OF ACTION:
~
E. UPTAKE .MECHANISMS:
q_
'"J 3 ► Local anaesthetics block the generation and the conduction of the neTVc impulse.
UPTAKE J: Pick.ing 11p of ca1cdiolamine's liom cittraccllular spBCe by adrcoergic
c-1..~ ► The blockade results from lhe biochemical changes caused by U1e drug on the
o neurons and by the o1nl neuronal cells.
lJ1'TAKE 2: Picking up of NT by the effeclor cells in pcripher.il tissues like vasc..-ular
smooth muscle, hcut and exocrine glnnds. ~'-.
~-,,
~ t .
► Local anaesthetics like procaine prevent the increase in pc:nneabilily of the cell
mcmb- to sudiwn ion which is lhe fim event in dcpolansauon. Thus an action
is~ . - --- -·-- ··
► ~
l)Otcnlial
6. What are local IUlaadadlcl• C11ulfy them wilh cx:tmplcs. Wrile the. ml!chanism
or actio• or loc•I auestbedcs. :..L, a
The action :::the-process of depolarisation leading the failure of propngalion·ot .
C I-'
~
►. Ans: Local aoaeslhdics are the drugs which upon topical application or local impu!Se without affecting resting potcntilll is known as Mcmbrano 1tnbilising dfe'11.
injection cause irrevasible loss of sensation, especially of poin, in a restricted area of ► Smaller nerve fibres presents as a g,-eatet surface area-per unit volume of action 1\1an
large fibres. Small fibres are blocked first.
1he body.
► Vari~rcs are bloc~d in lhe follow~_g manner.
~
-
· c or

(
(
(. fll ,\
~-
~ --,
.,.)
" I'll ,_\
,\
orutc,,1,.
Th= rttq,tt,r, .,., sclC'<'tl,'Cly _,-.icJ by nk<-1,ne an.I t-i...1:nl by .i-111ht1C\1ran n Cont raca~ 1roo<Jlh
..
•
hQamclhonium. D. GLANDS: Chu\incrg1c ,11mul1111on - J b c p$ltic inlcstin•J and pancu,alic
C. scarctlon, do,., 10 1hla th~ hwl saliv>CX, barn 111I, n ~ I sccretion_:i_
These l"C<'Cplllr, IK"I t-y h$And p t<d i"n chonnds. ncti\'olio11 of 1hc nicotlnlc r"';•1>h•rs
shews the orcn"'8 of ioruc channels,. hich inm-ucs the cct1 rm11c1billly causmg Ilia
C. I'll j ere uui,ncntcd. - -
<krobrisatio n. -
". - ; - gahv.ary scctctions arc p<olu.'IC and watery.
-,-••
-)
C. EYE: Installation or Ach in the c:yee it is DOl abso,t,cd.
On lbc buis ofl001tion of sdn.'tivc agonist and antog,mist thcn1e nrc o_f two trrS': C. I -> ' Conslrictian o f pupil is seen cao.aing mio,is which is due w the contraction
N.., These -
Mediates ,k-cld:IJ m~
--
- , in skdccol mll5dc end pl3ll'S -
Stimulu,,d by phen>1 trimeth)'I ..,,.._jun, and blocked hy d-tubocurarinc.
l--.
.;.;;ction. ;- II,.)
,)
.)

of circular fibres cf sphincter papillae by reducing the in1noc:ulw tension.

• Conttaction o f ci\i:uy m uscle and the ~ taxation or suspensory ligaments of
the lens will reduces the ocular lemion •
It causes inc:n:115e in the thickness and dcctcasc In the focal length of the
•
Ni<: Preseuc in the gang]ioaic cdls and adtezul mcdullacy..cclls..12inal00rd and ~erUiJL
;__11 _) lens - spasm o r occommodutioo
~--.)
areas oflnin. - -
NICOTINJC ACTIONS:
Stimulated by dimethyl phenyl pipcn.zium and blockl'<l by hexruncthoniurn. ~.JII ., A. AUTONOM lC GANGLIA : Ach induces pngliooic stimulation due to the
increased
output of Acb aod NA &om parasympat hetic IIDd sympatbctie nerve endings.
.• .,)
~--•-,
I. CHOLINE FSTt:RS: Eg: As:rM ~olinc
• It increases lhe blood pn:ssurc due lo peripheral vasoc:oostriction.
~
PHARMACOLOGICAL ACTIQNS: B. Sl<.ELETAL MUSCLES : Stimulation or somatic nerves iocluces the cootraction of
Oq,a,ding upoo the type of n:ccptor l.brough which ii iJ mediated the actions or Ach sk.cletal muscle.
are cm:goriscd as mu,carioic or mcotinic. • A very hif>i concentration of Ach at m)'OtlCUr.il jUDCl.ion causes the paralysis of
, .) skeletnl muse\.,,,.
r-- -
-
MlfSCARl ,cJC ACTIONS :
A. DE.ART: A~ shows the hypcpolarisaliun of 1he SA node and dccrcu a in the
d~ti_o n. decrcues the impulse gcnentiou.
Effec:t ofAc:b-on the bean is due to vagu.~ slimulanon.
•
c- •
c -• ~.)
.>
• Intra arterial injection of Ach to the bronchial artery produCl:OI fasciculatio ns of
THERAPEUTIC USES:

skcle1al muscle followed by prolonged weakness.

c-• -;)
•
•
-
It causes bndycardia and cardiuc m-est
Decreases the· co111ta dici~usclc ( • ionouopic effect) nntl causes
AV blocbdc. --
~-•,)
c.----,)
• Ach choline is not used for aoy therapeutic pw,,ose.
• Ach substitutes like Mc:1hacbolinc, carl>hachol, bclhaoac:hol arc 11.~cd.
~--••·
• Bcthanacol is used for post- open11ivc paraly\ic ilcus, abdominal distensi on, relief of
• 'Veiiiriaiar contractility is NJuced. gastric atony, urin11ry retention. congenital mega colon.
• In;;;;;;; the conduction ofvcl~ity ofutria.
~ ADVERSE EFFECTS:
,-,--•--~
,)
~
B. BLOOD VESSELS: Ach dilaus the blood vessds of i kin and 11ucou1 membrane. Flushing
•
.- W1iciiiMJ rcc:cptors a"!_stimnlatcd the ~
dotbelial cc].s releuse nitric oxide
~
it • Salivation
which caiuses~ ar rdaxatiun. If the mdotbclium is tlumngcd tl\en
• Sweating
caases VIISQl!ar contraction.
• Bradycria
J=e
• II also dilates coronary arteries.
• Hypotcnsioo
~ -~
• When ii ;.. adminisl«o d Uttough IN route ft SOMc or warmth in skin,
• Syncope
lbn,bbing headache is seen.
C. SMOOTH MUSCLES : tone and rhythmic activi1y of smooth • Bm11chill spasm
. ~ e a ororr and cau.~~7 is1s. - c~ . !-,-Ocaasion ally cardiac nnhythmiu s.
• Cc,nlrac:15 smoolh mwcclc of gall bladder.
CO~IC ATION S:
• Contracts dctrusor muscle of urinary bladder.
•
- -- - -
~bronchial smooth muscle andciiu5C8lironchospasm
··- - - •
-
!fyperlhyroidism
 ..
p• · , - .
,~ ,\
; •)
; ,)
• 8nindual asthma
~ -~
l'IIAMMACOl.(K;! CAI, AC-I Ull'l!I:
~-v
• Pq,ric ulcc,-
.C..~,)
• The phann.1cnlui;kol 1(1iuru, o f 111t<,pinc and ac:opolmlinc: arc simillt except that
• 1'l)'t'CU'dJJ\l mft11e1i"n.
Alloplnc la CNS stim111ant whcreu Scopol1mine iA CNS depressant .
• si1e af choline, c.<tcra.•c •11J h1'\lmh"" 11 1<1 a~c-lic nuid
• Allopinc h.u longer dura1fon of acti,m than tlw of scopol.mine.
• II ~'<!UCC\ tern~• ,nhiNbon llf the C"IIZ\'nlC. ,. u I . SECRETIONS: The bc11"'1onna albloids reduce the ,cac:lio,u of the exocrine glands
• •
l=1o·c:rs,1,tc llh<lline CS!\'n.<cs \\ill «-mt-inc •only with the cs1c1i~ site of 1I,c cho inc
cstcnuc and the C$lcric site ,nil~ r'bospboryla1t\l.Thr hydroly"s . Of ..,_"'111101}'
•"-
1RIC\1 c•j c~tcpt lhe production of mllk.
/ Salivary secretion•: Atropioc blocks the wala)' salivary secrdions and _c a~
site is slow a n d ~ im,,'Cffil,lc inhibition of the cnz)'mc.
Q • l art anti-<hallner,:ic. Cbssify them. '£l<plaln th• pllannacology of atropine
; ,) dryness or mulllh and difficulty in swallowing.
., • Cutrlc ncnllons: It red~~- voiume of pstric juic:e "1d total acidity of
g11.'ltric socn:tlons.
._.)
~ .
Anll-dloli~c arc ihe drugs • ·hich block the ~•lions of Ach on nutonomic efferents It also reduces the secretions ofmucin and gastric enzymes.
~. J
and in lhe CNS c.,cned lhrough muscarinic rccq,1ors. ,- • Other ucreriaas: lt reduces the secretions of nose, mouth, pharynx and
■.
-- ~
C
~-•.
Atropine is lhc prototype of ibis group and is highly sclcclivc form~nic rea:plnrs. bronchi 11 also reduces lhe sweat secretions in low doses.
,,.._ '..) 1. SMOOTH MUSCLES:
CLASSITICATIO:O.: • Ctr: Atropine reduces lhe tone and moulity of all !he plll'.lS of the gut showing
I
~~ anlispusmodie effect. 1t blocks tbevagus nerve stimulation.
•.
A. Nalur.ll albloids: AlrOpine, hyosciuc (scopol~c)
•-.)
, B. Semi synlbdic derivlllivcs: Homacropine, Atropine mclhonitrntc, Hyo14cine butyl ) • Biliary tnid:Atropinc bas weak spasmodic action on biliary tract and gall
'- bromide. bladder. - - -- • '
~ C. Synthetic compounds: • Urinary tract Atropine reduces normal as well as drug induced un:ter.il
I. M)'llrialics: Cyclopen1alonc. Tropic amide
2. Anli-sec:mory- Antispasmodics:
L Qoalf:mlU:y amines: Propanthclcne, Oxyph~'tlooium

~
. _.)
~

.)
peristalsis. In thmp...-utic: doses it reduces lhc tone of fundus of the bladder and
enhances the tone ohrigonal sphindcr ca1Lscs unnary n:1ention.
• Rronchil: Alropine relaxes the smooth muscles of bronchi w1d b1oucbioles. l\
( b. Tertiary ammcs: Dicycloamine. Oxybutynin
C ■ ..) relieves b1onchoc:onstriction produced by the cholincrgic drugs. Since, it dries
up lhe seaetions ii is not rccommcm\cd in bronchial asthma.
Anti-parl.illsonism drug:s: Trihcxypbcnidyl, Procyclidlne, Biperidin
■ ..)
.
• IJ1£ru1: No significant effect on tone and motility of uterus smooth musclc.
ATROP11''E:
C 3. EYE:
"■ .·\) • On low inslillution 11ll'01)ine produces mydriasis by blocking the c110\inergic:
L Two importa.nt alkaloids Anti-parkinsonism dru&S: Tnliexypbonidyl,
" -na\>~ -----
•- ,)
Procyclidine, Oipcridin.
_.) • II paralyses the ciliary smooth muscles which causes ti&)11cning of suspensory
• orBdladonna are Atropine and Sa>polamine
" ligament, results in flattening oflens with inc:r~~ its-focal lc;gfu
,.~. _:,
• Atropine is an ester or aromatic organic acidcalled tropic acid wilh an complex organic
• Because of sphincter -paralysis 11,e individual cannot constrict Ille pupil foT
base atropine
" • .3 viewing lhc objects clearly or .i n response to hril!,ht light. This is called as
l\lECRA."llS~I OF ACTION: ~ paralysis of accommodation or cycloplcgia..
• LoC!ll instillation of 1o/o all'opinc drops causes ma.xi.mum mydriatic effect
•
•
The .Belladonna all(aloiils blocks the mll.'icurinic cftects of Ach.
'The antag0aism between lhi: Ach and mtropinc is c1.1111pctiti11e type which is revmed by
C.. ,_!'!ithin 3 ~_min and_TCCovery ~ ~ ~1in 7•10 _?;-ys and lll&x_im~
,:~ ~ ; cy~lo~llhin 1-3 days. recovery within 7-11 days.
increase in Ille concentration of Acb at mu~carinic neuro effector site.
'.l. CAR.Dlo'VAs°CULAR SYSTEM: - -
• Atropine is more effective in blocking th.!, c!fi.'CIS ofi\ch than the effects of cbolioergic
• 111 therapeutic: dos1.-s atropine reduces heart rate , ll,is effect is fol\owe_d ~
nerve stimulation. = - - -
~ycudia particularly tn young individuals. - -
• ~ ~ d r u g that isrcqnin:d for nerve blockadevarL~J!'Q111.orM11 tooigan.
lncm!$C irt lll~}1Clll(fuLis_ 4~e
• Salivuy or bionclual ~ n s are sensitive to atropin~ blocbd~ wbile ~ SIIIJI..Otlt
muscle oflhe OIT, eye, anil the heart ere less eff~l~
~ . ·-·
- . . . .'11
•
_.
pacemaker.
to l>l_!)ck,ing_of M2 receptors ln the SI\ nodal
· -- - - - -
• Jn !argcd~5_'."5 atropine blocks tl,e nicotinic llCtions of A~~~Dl!l!!,!~_l~f~~a.
\J i"~-t r/) 1ii cf(; ...1 {Vcud,. l 1~
 .. -,
... "'
~ . ,t
• In 1h
n"l'<'ul•~ .i.,,.,. ~1n,.,00 "'mrl,'1.-1)' ,.,,u111
h, ..., m1I • &.'IOOlilol i<1fl lllkl
m 1 • l'IC'l'1• 1 · : I \)
J. M1ilr.ln1J1.ll!lll.ml29Juia;. _!! ~
J..'= dalat,c,,n .,, culall".'<lt
11,,.
hyr,,,.,.,,..., ea,~«-1 h,•rh.,liu,ri.,r •~"1'Mn.1<I , _ I , ~ lls in 1ln-'f'lno tlu.,ih nml
;I" • Due to m ydria11cpnw ,aty ( d1lm oo <tfpup
,l)a11 opme o u,c,d indJC lra1c mcfll
In 1,,\fc
.:_ I v irilia, lri<loc yclh b.kcn lilll.
inll.wncd nn& ICW -. o f ins and cil..r y body
.
h~l''la\.<>,m.
.:.1 \) Atropine nxluccs the paiD by rclu in1
plr.C,oncdioa c,( www ,,oda ti"" -,uo
pia.
5
0'1'T R.'\I l'-'TR\'01.IS SYSTEM :
• I n lhmif'C'\lbc ck'>C< ,1 cusc s
• n,iJJ $1imuli tion of ,-.gal nuclei ond highe
r
-
-l~
• UIOd in IRalmcn& ot q,:Jo plcgja . Eaaa
4. il.6.. t&EANAP.S'.UJfflel,1!!DlCADQN:
ml llled lOmia before pn,:n l macs
tbcsi L
.. \.)
:1
C"C'n'bn,J <Ulln::. _!..-PN: anaa lhdic dnip an adminislc
and ina-cssc in nJC and deplh of ilc pnea l ~ may pn,ducc unplm
sad.
~.- -Jl y i1 rioou a:s breJ)'CM\h• -•- lfae of uropi ne w!1h - inila lll YObl
TC:$piranon. ION: throat •
• ID itt'tic doses Atr0rine r roduc<:s cxcita
lion. :-I .\.) S. CARDJO v ASCl/1,,U CQND[IlONS:
rigidi ty i n ~ bloclc clue ID Yap! adivity.
In modcra1e doses 11 controls I l l e = and y Alropinc ii weful In aboli shing AV
~J~ ..,,.-, U111:ful in countering 1bc syneope and
lm,dy,:adiL
AO\ fE;
parentcnl site of administration ml 6'11111 IIUICIII ...l "' 6. IJRINARY INCONTINENCE:
..-·~Various synlhctlc:substiwtca llkodicyclo
minc , oxybu1ym, -ma l to rcdu ceun mble
• Atmpiru, obsa vcd &om GIT. from
mcmbr:inc.
;.i ~ d1.11U1or contnctioos.
• Pwy de 1oxi6 cd in li\'er and J)31'1ly cxcrt
tcd unchanged in kidneys J..:) CONTRA INDICATIONS:
• Plas m.tv.i 4 bows
• Cros s the plnocntal bAnitT" and is s«rcl
ed in milk anJ saliva. ~ ?.,)
;L
Atropmc should administered with caution
yPal icnts over the age of 40 as it prccip

in
il31c an anaclc of ac:utE a,ojc sti"" &laucoma.
_,_....lacliYiduab with ailu-ged prost ate
as rac:nlion of urine may dcwl op.
~~
ADV ERSE REA CH ONS: reduces secretions .
n, bluning or _,. OvoDic: lung condition - drying and
owing, 1achycudi1, fever, c:onsdpalio
•_. Dl)n css of mouth. difficult in swall ,,> Coagative heart failure •
,~sion, men tion of urine in ddcrs. r--- Pyloric obstnic:tioa, aodi o span .
• l'r<.-cipi101cs glaucoma in elders.
nctivitis and swellio, of eye Ilda.
:..i..~ 3. Wlia t are sym pthomlm elkL Class
ify them. F.llpllla Ille pbar m1t olo1Y
or
~
• ,,, AUer-gic reactions like dermabtis, conju adnu llne.
SYMPAmOMIMMETICS OR ADR ENl '.RGIC DRUGS
PREP,\RA TIONS ANO DOSAGE: AIII:
ut.~ ufb11l1sdonna hn mimic the respo nses obtai ned ~ a ,esut,
of
/' .Belladonna dry e:xtracl - I% of lhe alkalo /Syinpalhomimetic m the mu~ that
.,,,.• BcU3donna tincture - Dose: 0.6-2ml. c llimullllion or sympatbdic OI' ~ c
nc:m:s.
in an inlaa orpa rtially substilulcd l-NH
, ) llJ'OUP 111\d
s or in powder form.. I>- . 0.2S-2mg. ~ 3 ~ j orityortbcsosubslancesc:onta
• Alro pine Sulph~te - Orally 0.5mg tablet es.
bmce me also called a, symp athomimctic amin
~
{
• Atropine eye oin1mc:n1- I ¾
inc sulphate jq Sm!: Doe 0.2S-2mg SCIIM
• AITOpinc sulphate injcc1inn :0.Smg of allOp
cus smC AnoN:
~
THERAPRUTIC USES: A. Tbcn peat ic clam ficatio11:
blood pressure: Eg: noradrenaline,
1. Adrcnagic: drugs used for msma
I . Gastmintesrinal Colic : metaramlnol, phanylcp,ncpnne.
colic pain. lnotr opic actions on the bean : Eg:
dnpaminc, llt1bu1aminc,
~
~ Controls hype r motility and 2. · Those used ftw
:,- Consti1>3tion due to spastic slate
of bowd is relieved. e.
isopraalill
~
Conlrols spasticily induced by lead and
molphinc. · amphclamine, dcxtro amplietlll!line,
~ 3. Those used a , _ t N ~
2. 0 1her colic..~: mcth}4phcaidate. • - -
trca1mcniof bi!ilr y colic,
• Administered along with morphine in !ht =e
4. Thol · :
• Atropine along with ~ hine is u
sed~ L on«k divc jJ atimullll!S: Eg: ~ inc, isopmialinc
Atro pine sho\Ys lhc rcl_~ anr cffcctOAb
iadderWIIJ,
•
 c~ •
C. 11111 -.)
C. . . __,
C. . . --> OP ADR r.NA UN! t A."'10 NA:
truno l. 1CltNlallnc. PllA RMA COI. .OCt CAL Acn ONS
b. Sdc- cn, •e f\, bloc l.as: q : ..Sbu C. . -,~
Eg: ldrm ahno . ~ n e ltaznl;,..,, phcoyl and II •s,:,nisL
Adrcn•linc lets u ■ _.se lecl i,c a
r.
J
.j
~
(

5. llios c, wrcd in allcr pc rc:ac:tion•:

6. l lll'llle U$«1 fnr local ''UOCOnstn
q,hn ne
B. Thes e dng s •~ also d.... n,,,s
I. Cat<'Chola m,nc s: Adn:nolin
2. Non -a.tc cboh unin cs: Eph<

u :

ctw err« t: Es: ad!UIIIUM,, """

e, NA, Oopa mina .
drinc ,

C..
c., . II ·u
c. lll'u
~
~ Noradrenaline Ids -
-1. CVS :
ac.lectlvely n a IOII ~
A. BLU lT: Adr 11imul■tcs 11
contraction end

aai,nuL
1'tCC p10n of ~ and iDa-e
lhe coaduetion vtloaty.
✓ I t alao increa:ics card !~ outpu
t by .-in & vm ~el ion

asa 1he n1e, fon:a of

Oms lncn:uill& the
3 "" • .,v - . s tt1\IDl and i.n creu ing the force
or aria! coolnil:UoD.
cardia in rcsporue to carotid simas.
C.
1'
CAT ECB OLA M11 ''ES:
d atccbo1311'
· --C · cl---'
• 1incs m uuc the symp athet
ic n1:urol111111onl bWIS mitia s like
0 PllllUnc, . the main hann one a( adn,n aJ

NA and
medu lla Ilka ac!Rnaline me! synlb
dic: c.·• -..l- . )
c -•
✓ Adr abolillbes lhc n:111:ll vagal bn,dy
✓ lt enhances conduetion ecruss \he
✓ NA does not increases Ille ~ 1111e
AV node and prod uce ventrlcwar
11fflhymias.
in• iacact lllimal but h:Nls 10 pn,clu
c,c bndy canli a
c-• -..l
c activlly.
~ due to compeosatory VIISCUlar reftc,,
~ mpound 1"'pr cn:tl ine. SSU RE:
_.8 - BLO OD VES SEL S AND BLO OD PREu, membnoc arc coasaictell 'by A.di and
~--=-•-~
Cl.
r . ► U ~ ~anun
l D F ACT IONadio :}
n by direc t jp(,m dion 1'Qlh rcccp
uns tc,ca1cd oa the • Bloo d vessels or skin and omco
~
.c:; ' es prod uce their
Cate cbol
- NA. of
-=-,.)~
\,)
~~-
111
cclJ membrane.. of skcletru muscles on aeco\11
i n ~ (mtcilatioP) or Adr dl\ntes the blood vessels
&ad drug com biaat ion is cilh« 1111
~
1" • by
► The ow com e of this rece ptor Iowa s the diulo lic blood pregsurc
.
.....
dccreru;c ( inhibition ) in the tiuuc
ity.
activ prq, ond ma~ of beta ttecp lOtS. il
pc:r iph~ actions.
V
► Th~ e arc two n:cp lors a and
II ,
;~ Increase in 'lhe systolic blood pressure
ucctl 'by the modctatc doses of
prod
~--•-=,.),.,).)
clfec ts of c:atccbolamincs. • RIC \s called
a recc:p10r stim uluti on-c xciw ory Dlpha receptors. This t<:SpO
.-h B rcccplOc stim ulati on- inhlbitocy effec
► a ■drencrgic rttp

ts of catccbolmdnca.
ton ,. re of rwo tn,a end s. a,
Adr often rollowed by stiroufating
as biphasic response.
a rise in bolh systo lic md dias.tolic
blood
I r ~
a-
,z adre gerg ic ~ G ; BR ac:icacx,,y in
natun: and act da.rougb G-prolien
( G,) • NA in an intact animal produces
► rea:p1o11
ci, pressuree.
~· , .... ,.
..
-- iated with rclle1t brtod)'canlia.
conccntralion of calcium by
-,.-)
~-.~ • NA induced bypc rta,s ion is. assoc
.
,... . ■
(
way , increases the lntlllaellulac now in man
~ ► Act through IP, DAG path significant red\K:tioo. in lbc bloo d
• Bolh Aclr and NA p«>duces a
'
-:. . ) ~
7 . the activ1nion of pbospbolip■se-Ccalciwl1 will eccou.ots for lhe ~timulating dfco ts of
CIIZ)lfflC. BP.
even in doses thal have no effect on
p
~ 1-, ► The inae3$C in the intn cdlu lar • ll reduces tow peripheral resistance
.
-i. ptor s.
agcr us !hat biod 10 01 rece coupled receptors by Adr also n~ the sy1tollc blood
PJCSSurc
J ] ~
through inhibitory 0- protein (01) C-:11·~· ) •
d vesstls ond
r-
;
..,
'. .t ~,.,
►
►

Alpb a2 adrc nerg ic receptors aet

inhibiting adco ylcy clase and redu
The se rece ptors activ ate G-p otim
ces the c:yclic AMP.
gared potasaium clwmels.
c - -,, • Both Adr and NA amsmct lhe hepatic and mesentcric bloo
raise lhel)ONl venous PR:U\ll'C.
pressure is raise d by bolh more by
Mr.
► TI1e activ ation of a, m:ep lors
ill the adreac::rgic nerves inhibits NA
rel1:11.Se wbere as
ing factor(
c ·' -.> • Pulmonary encr ial and venous
Adr on moderale doses increases the
caebra\ blood f\ow and 01tygcn
activ ation of vascular m:eplOrS
cause the release of endothelium relax •
~{
. ,;_-1
►
EDR F) which brin gs about vaso
a.
b.
Bd111 n:cep«ors -

diJalion.
Del a regp l9r1 an: sub divided illlo
dlree sub types:
se.
myocardial llimulalion 1111d rerun relea le vasodilation, uterine
BeU2 receptors- bronc:biaJ ~.:e iax
a1i on, skeletal musc

" .. . . 3
C. ..a _l
~
l, SMOOTH MUSCLES:

consumplion.
A. BRO NCP II: Adr by its beta tceq
smooth muscles.
)lor agonis1ic 11ctivi1y it rcla1tes the
. _
bronchial
_. __
~
rding 10 the
ls lo the catecholamines varies acco
{ <
t- rcla utio n.
c. Bc:1a3 rccc plon - Brown and whil
e adipose tissue, rcgalalcs NA indu
ced chilllges in B. lJTE1lUS: 11ic=poose of the ulel\
, -presence or abSl.-nce of gcs\3lion, perio
d of
species, the -pbu a of oestrous cycle
;} ~
..
· . •
-·-
ener gy meta boli sm.
aors by stimulating the adai yl cyclase gestation and the dose administaal. or all the fllctors.
, ► Reta. ad by srim ulat iaa Ille G-pulim ( (is) rccep u:d by these compounds irrc~pct\\vc
• The I'll ulau s is rel1u
Intracellular cyclic AMP levels. is stimulated 10 con1rac1 by
enzyme. llus results in dlerileofdle • 11ie human non-pregnant uterillG strip
by sLimul1lio1 protein 1ti nose.
,: ' s.,- nic cyclic AMP acta 10 die cell fimdions adrenaline.
►
J
..,,l
l1 u
 <'~ - ' -
~.- tlll'
r . I',\
c. Ill \
• In t~ 1.,,, mon1h llf t'ff'l!ll.tne)' ..ltfflahnc ,t\h,blts utcriuc
,'\!11tr..11MIS o1MI c.. • \,)
cau.!IIQ utmnfl' ttl1, .al•"'I\. C. . v
4, Clanlry 111111,nthlytlc. ~•pl■I■ tllt pll■rmacol"10'
of IMt,i blocken.
itJ "'"tlloty. ,
C. GI r : A.tr and NA ttl "' lhl- _,,h m11Jelcs o f the It'll
0 . OTltE k SMCXl TII l\l l 'sc:-Lt:s: Adr c,,ntm,1.1 the
1ml ~luce
rn.,,11.,t,,r n1u....:le .,r 1110 hnlf c.. lll v ), i\n,: /\drencrejc bluclccra ore the drug, wbidt 111tagc,ni,.,.
lh11 r,<eq)IM action ofadrenalioe
3

fulhcle.
• • t'c,n1ne1, the ,-c,,e,tl srh,n.'1"1' and tho lri11llno rclnxa tho
· £\ 1':: S),,•l'Olhc-ci.: l<limwlltic,n r...its in n,ydruuis due
dctnl"'r muscle.
toount111Ction <>fn,dial muscles
o f the ins. Adr on toric&J odminlstnlion do not rc&dily pcndnltC
rod
S into the C)'Cball. It
and glaucomolo\lS GY':'

c.. •
)
C.C.,.. ... \v
\.)
v

Md otha rdalod drugs.

► 'lllc,w, drug.t may either block a or I} n:ccpwn or both.
a. adrrHr pc ltloclwi& •SC-II
► 'fbcsc arc lhc drugs which inhibit ad,..,..gjc ~ medlllCd
n:ceptor1 wi1h affcc1ing those m«lialod tlwugb Pn:c,q,IOB.
lhlo11p, Cl lldn:nugj~
P uccs IIINcn tc n-ductio n in inlnlncl1l1r pressure in nonn•l CLASSIFICATION:
o(respin,tloo. (liven 111
◄. RESPI RATIO N: Adr as a brondio Glal(lf and wait stimubn t I. Non -selective a 4drcnergjc blacken :
IV both Adr and NA induce •I""""!, Adr in aerosol form
VCSS5~ llnd rcli~cs bronchial congestion.
S. METAROL IC [ F'FECTS: Adr inaascs bl-1 sup: 1cm.

constric!S lhc pull'!,onllI)'

bl()C)d luctntc,.!!!d p!Pl[lt•
C.-
.
c • v
v
,
a .phnlo alkyl wnlnes: DibcnamiDc, pbenollybcnzammc.
b. N,uural and hydrogenated ago1 albloicls: EtgOlmtine, Ergotox
ine.
-~ ,
2. Selective ci, adn:oagjc blocltas:
Im: f3lty Acid cona:nt ralioo and ICNIII p0tmi ~ levels.
;;dim, ,- ....
6. CNS: ~~ cross the BBR Adr prowccs 011, 1rcmor, stupor, vomiting. ltld
. --..,)
~
Quinaiolincs: Pn:wsin, ter1120sin, doumsi n, lndonm inc.
3. Selective n: blockers: Yohimbinc.
-
rcsllC!l.~ncs$.
by 11d on both sides of
7. SKELE TAL ~WSC LE: Skdcbl muscle contmclion 11-a drenerg lc blocke n
.
ncuromUKUlar junction. ~ II
.-\) These are I.be ~ which inhioits lhc a d ~ c
mediale d
►
:~ ■ "
re,poDSC S
rs ..Uercic bronchospn!im.
8. ANTI- ALLER GI C ACTIO N: Adr releases the malinto
ns from sa!Jv4,Y gland. receptors.
.- .-\)
9. M ISCEL LANEO US: Adr produces thiclc viscid secretio
> All I} bloclu:ni are competi tive blockers.
of their rnpid inactivulion in
ADM[ : C 31c:cl,olanincs arc not administcn:d onlly bcausc
the gut and in the l iver. Ct.ASS IFICATION:
On in lubtion of Adr or isoprcnaline oerosol~ snull qu40ti1i
es ore absorbed in
d '- ~~ l. Non•sclcctive(lh and lb )
"'- •-
: l'ropranolol, sotolol. timolol
systemic circulolion. ~ L Withou t intrinsic sympalhomimcl.ic activity
Adr and NA arc mclllboliscd by catc~J !lc!}ly l tronsf,
•
n ~es (COMT) an ,..
·- b. With intrinsic sympathomimcl\c activity: Pindolo l
•-,~.)
mono amino oxidase s (MAO). c. Additional fl blocking a1.1ivily: Labetalol, carvcdllol.
2. Cardio se!ec:tiv e (ll l ,: Metaprolol, Atcnolol, Accbutolol
ADVE RSE EFFEC TS: 3. Selective (~11: Butoxomine.
• Aw- sic causes p11lpi1111 ion, throbbing hcadnch e and 11cmors.
c.:~•-.)
~ .
P1t0 PRONOLOL:
•
•
NA i/v causes anxiety, pallor and head ache.
Both Adr and NA i/v causes increase in BP, sub-nrac
ventricular aaythmias, and pulmonary edema.
hnoid haemorrhage,
•-- .)
(;
~ I _J
PRARJIIACOLOGICAL ACTIONS:
I. CVS:
the card,ac outpuL
A. Hl!ART: lt tcduccs the heart rate, fOfllC of 1.-untrnctions and
TUERAPEUTIC US ES:
ADRE NALINE is used in the trcalmCOt of
~--~:, It prolon p lhe syst~ uciqg ,_the conduc ti~n.
Due lo 1cdoction in the oxygen consumption eart and the
aortic pressure is
• Aoaphy factic shock
• Bronchial aslhmo
<;·•-
■ J
reduced.
It increases lhc rcfraelo ry period of myocar dial fibres
automallcity due to this it CMISeS dea-casc in depolarisatlcm.
and reduces the
• "Cardiopulmonary tesuscillllinn
;- Conlrol ofhlemorrbage. • · •
~■ - J In ~ u s e s the di!,~c prcssi on and increas
sta!,ili,atimL.dJeef:. -
es membrane
• NA is used in the tre:llmt-'fll ofshoclc; control BP, 00rrcclion ofhypov
alcmio
c! ~ II blocks the stimul ~c:tjon _of llkcnggj_c d~l!f ~~~
calcium.
~f diRo:itin ~
-
 <~ .
c - - -,,
r•-
C 1111 ,,
C. . . \.) by reducing the: li1$1 pus
n. BLOO
N .
DVESSELS: tllockn L....lil:ab.!a and cmscs 611.loJll'..
111111
· • Pruprnnolol in1.-.cucs the blonvallalnhty of c.bkirpmmazine
r~•n.,ei elT~ on 1114'<'d Y<'SSclJ<. but"" 1'1'"°'1P 11<bni1tis1n1ti"" or. i;roJ Y C • u ll~holi am.
Rcduca t NA release &om lhc symrathc11o 1mninals co1~•c.,
ttc:cplo rs.
·
hRed~ . rcnm rdcasc from the kidney causes marted
)'peftCO st\'CS

Ille blocltaJe or II
p '
fall i.o B m
C.. \.)
C. . . \.)
c• v
AOVl!RSI! l!FFECTS:
•
•
•

Increases myocardial insufficiency by pm:ipitating Cl IP and

Bradycuclia.
Chronic obstructive: lung diseases.

edema.
2 · RES l'IRAT ORY TRAc n II ~ e s the brondilal rcsistanCC
S)'Inpathetic bmnchodJlntion is olinima l - c. ·• .) •
•
Prinzmetal angina.
Ttredness, dcacasc exercise capacity.
Asth miiis rn~- ~ ... .)
.,_, ~ C .
3. CNS: Longte rm 0 f rroi,ran olol, cailr.ll efrcc:IS like behavioural changes. forget,.,......., • Coli.I hands and feet
mares:--- --- -- c-• -.)
.
.-
increas ed drea ming •~,
• Periphc:ral vascular diseases.
tic as WI oftidocaino.~ • GI upsd
4· LOCA L ANAE STHET IC ACTION: Potent local an.csthe
~ecaus c ofirrirant prope:rty it is not used Lhmpeulically as
a local an_!!~sthctic. c · --'- .;,)") • Lacie of drive.
Jit inCTCase.s illfplimia lfcc
S. Meubo lism: By blockin g adrcoag ic ally inducat hpolysi • Nigblma n:S ·
futty acid levels.
A plasma triglyceride level, CDUHDL ntio is increased.
II inhibits the glycog aiolysi , in the heart, $1cde141 muscles and
in liver.

c- -
;.._ .-,)
,. • ---.:i
• Forgcllulness
• 'Rardyh allucina tions.
THERAPEUTIC USES:
-,.. _.=-.-~.>
;~
No etTect on ooanaJ blood sugar levels. arrythm iu
Prolonged therapy reduces the carbohy drate tolcnnc e. • Used in the trealmcn t of hypertension, angina pectori.s, cardiac
6. Ske.lct:il muscle: JI inhibitJ • ~ i i r c e s e d trern0rs~ • Myocardial infraction. l'heochromocytoma, thyrotollicosis
Oow.
Reduces the exetcis e capacity by /l mediated incrcoscd blood • Migranc, anxiety, glaucoma, c:anliom}vpathy.
7. EYE: Reduc a the sc:cretions of aquoous humour. .-r■
liiir.iocular tension is reduced .
~ f w : t ~ri.
8. UTERU S: R~~ .ofl,tm•s is bl~cd by pmpran
olol.

'
~-•=·j
C ■- j

j C:ONTRAINDJCATIONS:
• Bronchial asthma
• Partial and complete heart block
• C-orona.ty artery disease.
ADME :
• Well absorb ed through oral administration.
•
•
•

Low bioavailability due lo high first pass metabolism fn

Oral: parenteral ratio-40: I
the .liver.
They are Jipoph ilic and penetrate into lhe brain e~ily.
~ .-_,d. -~
r; • - ~j S. Classify aktlelal muacle relaxan ts. Explain the pharm: u:ology
Am: f\KP UAL MUSCLE RELAXANTS
Skeletal muscle relaxants are lhe drugs that acl peripherally nt

of d-tuboc urarioe .
neuromuscular junction/muscle
fibte itselfor centrally in cen:brospinal axis to reduce muscle lone
and cause p ~.
•
•
•

Metabolism depends on hepatic blood flow

Exaded through the urine as glucoranidcs.
More lhaD 90% bound 10 plasma prolcins.
DRUG INTERACTIONS:

c·•
(a; -
...
~ -• -,
~ .)
-J
CLASSIFICATION:
l. Peripherally acting drugs
A. Neuromuscular blockers :
& AV node conduction. • Non-depolarizing blockers:,
• When used along with digitalis, verapamil reduces 1he SA ~ -J ► Lonpcting-dlubocurmine,pancuranium,doxacurium,pipecuronium
cs.
Delays rea,va y from hypoglycaemia due to Insulin and oral.antidiabcti
~ .. I_
rium.
• ► Intermediate acticlg-Vecuronium,;atr,curium, cistr.lcur ium,,ocu
lhc blockade of
•PheJJylcphrinc, ephedrine: will increases the blood pressure due lo ► Short actinc• Miv;acunn1um:
•
sympalbdic vasodi lalion. ___
Jndomethacin and NSA IDS will incrca.~es 1he aotfhypertensive actions
_ ..- ...
ofpblockers. c.! ~ • Depolarizing blocker, : Succinyl choline:, dccamcthorium.
2. Directly acring dlUgs: Eg: Dantrolcne sodiam,quinine.
• Cimeudinc will inhibit ptopranolol metabolism.·
flow.
• PropnUIOlol retards lignocaine metabolism by reducing hepatic blood
 ,...- ,
. .·,"'
; , j 1
tl -tut>o..unirfnc-(J'n,rorn,.. dnu;l:
:1v Al)MI !;
This is the dc.,tro .
chond .
. ·11111 alhloid obfaint"d &otu plwll
rot.:IIOfY q11,1rcmary ammoru
~I V • l>•tubo curarin c being I qua,\CfflAt)' ■ll)UWIUllm.CO
IJlpound not -~ from !he GIT.
~i,J!d ro'!.! omcn to:rm , ,.......J \) • The drug !J wcll_ahs(ul!_ccl on 1M acfminlsfration and
widely dlS1nbutc:d in tlsrucs.
·-
· of action : - • On IV administration o.ftll~p eutic ;i;,; skd&
l -;;u,clcs_paraly,Sis wilh.niboc!!!3rinc
,.._
Mech musm
• D-tuboc:unuine combines wilh lhc nicotiniC ~or s
on tho motor end plote ... '-' Williino ne tcrone onilliill'm in and pea cffcc:t i.s obwnc
d wilhin five 10 ,cvco min and
action pmist within 60-100 min.
and blocks the action or Acb by compclilive blocb
de t' · \) _.l 1dmin~~tn1io_n parentally is eliminated IIIIChanged
in urine wii1:in 24hn.
crgic receptors at
Competitive blodcas hmvc the affinil)' towards NM cbolin • 33~
• u 'ibe dNg cannot cross ~.!!! p_l~ barrier.
•
muscle end pl3re
NM RCcp ton is ■ proldn with S sub units (o2,ll,s.1,6)
which are arraoged
~
,. ~, •
ADVERSE EFFECTS:
•
in n>5ette surrounding ,odiwn c:bamiel.
T• -u a subuniis amy two Ach binding sites, tJiese
hove neptiv cly charged
... ~) L!-- R)'Jl()xia and respiratory paraly,is.
,.. • Hypotcnsioa
subunits which combined with Ach-opc:niag of sodium
channel. ,._ ~)
• Most or lhe compctilivc block m have rwo or more quartc
nal}' W atoms
,. ,'I _
,. •
• Regurgitation of £11~lric juice.
OcsopbagQ! sphinc!a paralysis.
which provid e attractioo 10 !be same site .
e with rccq>lor
~
• Ada i.e relc:a,ed io the motor tnd plate is not able to combin
Ill gcncrate ac:tioo potential .
,. I~
! ~
·-
Preparalioo and dos-se:
• Tubocwurinc injection in 10 ml and 20 111! vials contain
ing 3mglml dose 6-10
...,_ g and action
.,J
.....
• D-tubocurarinc nxtuces lhe frequency or ·channel openin
potential rcduocs a1 aitical levels , it is unable
lo trigger the action poten tiol .
e· -
~ -- -.) •
mg Iv initially
Dimdbyl tuhocururinc iodide - rv initfol dose 3mg follow
ed by tmg aftci-15
muscle !ails to mntruct i=-o sc 10 nerve.impulse .
~ -- ~ -.) min.
,-. I. .
~
~---
...... PHARMACOI.OGICAL ACTIONS : ,- l~
'" __ Therapeutic uses:
:._J
.,;.,,----1. SKELETAL MUSCELS:
• d-tubcx."llririae on parcnlflll admirustratioo i11itial1
y produces molor -,"
C'. ~
• Adjuvants ann~slhllSIR
• Electro coavul~ive therapy
wcalcness ronowed by naccid paralysis I • Spastic disorders
rs and eyes are
• small ntpidly moving muse!~ of the lingers , toes.ca
tasks and
~I ..> •
effected first milking ii impossible ro perform dekcalc motor C . .> 5 INlrks
wing .
producingcf.iplopia , slurred spccch ind dlfticuhy in swallo
I:
• !he muscles of limbs , neck Md trunk ore
affo~led later followed by ,.. I .,;-«i plala in dcl•il about tbe tttholqutt or local
anaesthesia.
..f' intcrcosral mmclc:s
"' I ., Ans: TECHNIQUF..S OF LOCAL A.NAESffiESIA.
~· hypoxia
,:;;
,. • finally diaphragm rs paralysed and ut:lllb occurs from
recovers first and small
"! 3 I. SURFACE ANAESTill:S JA:
ctics 10 muco\lS membrane
J • recov ery occurs io reverse order the diaphragm • II is produced by topical application of surface anacslh
muscles recovering later. ~ :,
..J'"" ./·2. Autonomic ganglia: • J
and abraded slcin.
• Only the superficial layer is anaesthetised.
I • In the doses used clinica lly ,d-rubocumine can
produce partial
t-J ~ • Onset and duration or action depends on the site, lhe
Jrug 11nd its ~vnccnt1111ion .
J blockade of borll autonomic ganglia and odrcnol medul
in fa1J in BP.
la and results
-
:J
~
• EO: Lidocaioe spniye d in lbc ihroat acts in 2-S
~0-45 min.

min and produces anaesthesia in

J J. HiJtamine release:
• JI cen produce hisfam ioe rrJP.:litP from tissue by
acfing tlir~t ly on ~ • The absorptiOfl of soluble maeslhdics is rapid from
2. INFILTRAT ION ANAE STIIE.~lA:
mucous mc:mbranc.
• mast cells. _--~
sed salivary
~ • Dl1111c: solutios;s of LA is iofilh'atcd under the skin in \he
ation, blncks
area of opa
• This mny ocaisionolly cnuse bmac hosp ~, increa sensory nerve endings.
trachea bronchial and gastric acid sectt1ioll.i-(_)
..--i- -- 1··
 ,\
,,
I
.. ,
I
j$ •hnrtcr. I
I -r1,,11
I 'u .. , ,\
• On.-tct Cl( " ·11,,n •~ 1mn'K'\hM'" :tm
• •
,0-1so1111n. the lowwJiJDbr,. pc!ui• )oY(ci _
.
<'- 1• .. · · as. and hydroccl l • SpinDI 11111CS1~i• It ulCd r,,, opcr.uona 011
• Et: udoc :ionc :-3~ nnn. lluro,-aCJtlll like i11..:i$ltlP.~ c..,a s,~- ed c. ICdioB.
ln 61in,a, 011 is usc,d fi>1 minor .,pcr:111t>ns
'V •bdomcn. pro,t!llcctnmy, ftlldUrc scttin.J,. and -
• Lnrscr amounr ofL-\ ,s miu, ml c.mir
. a
rod rothcllmlanae:st lS • I
,.
.,, ltsad~vcfg~~
i. lliua rcr.
- -
-ioD wilboul loss of
• It d,lCS fK'I :i rr~-. """'" S)~n ns. ~ good -lgc si• 11114 mllldc rda.
3- DUCTION
COl'\Th .
BLOCK:
· · · · i.,
___,, so tbllt the area distal to mJcctio11
•
..\\ ii.
consciousness. re- problcma.
' ,\
-
.r
C, LA IS laJCCfc,d 3roun
d ncn·c uuu,.' S
. iii. Cardiac, renal and pulmonary d i - poMS
an3c:sthctist'd and p.v.ilys~d. .00 ....,. •onlhcdurarion ofactton. •·· ,)
,....__. r• . .
~ ,ce o ,..,\ and , rs c:on,~•llr:111
.1--A..-
COMPLICATlONS OF Sl'INAL AN!.
STHESI.A:
~ and iscbm1ta
"'.. "'
• Lldocai.nc sho" 'S immaliarc action so
it is commonly used, is rare, maintains brealbmg. Ifhyp olms
ion
ting LA M>CUIIIICOusfy.
t._Respiratory pvalysls:more it lead to rapir atory s-a i,-.
.'\. FIEl D BLOCK: Ir is producal by injec J
of respira!Oly centre is
inlc: ralm l - 1 a , coug)iillg and
,. ,,
/ • II bloc:Jcs all the ncm:s in particular lidd. ) Due ta paralysis of alan al abdominal and
ft is daae in hcmiorrliapby, appeadicec
tomy, dental procedures, scalp ~
~ I1 puImonary comp1·1cat1· ous can occw-.
•
of sympadidic --'r ic:t or OUlfl aw of
stitching, and opcrntjons on fore ums
and le~. B. Hypoteanon: It is due to bloc bdc
bcalt.
,,-, • larger area can be 11111csthetiscd with lcssa
' drug compucd to infiltration.
ting the LA aroUDd the appropriate nerve
J~ blood veuc b decreased VCOOIIS return to
ft: Beadach,: ia due 10 seepage of CSF.
B. IVER \'E BLOCK: Ir is produced by injec neuro logic al complication rauhin&
,",.) in
trunk or flc.TIJ.s.
• Muscles supplied by the injected nave
plCJCus are paralysed.
at...
.J
, D. Canela equlaa l}'Dd nnM: Rare
f prolonged loss of contr
ol over bladder and bow
"E. Septic mcalngitb: du~ to injection intro
d spbi ndm.
duce d during hanb v puncture.
the drug aod the area to be covered
• The laten cy of anxsthcsia dcpcods on minal opcralioo it is clue to n- initiation
OD
'" ·..)
~ Na■- ud vomJliDg: after abdo
by diffusion. .J.. abdominal viscera.
• Eg; Lidocai.nc:- intercostal nerves arc
anacslhetised within 3 mm. but ~ -..) r
5. EPID URA L ANAESTHESIA:
bronchilll plexas block m11y l31ce 15 min
. .. ,,)
,-l.
• The spinal c:ord dur&l spac e is filled
with semi liquid fat through which nerve
..-l
of the plexus and larger volumes ...L;)
• Flooding technique is used for bloc:hge d.
root slml
011 nerve roots and small runounlS
-.-~
< ..
ue l'cquircd.
• Frequently pt.Tfonncd nerve blocks arc
lingu al, intcrcostol, ulnar, sciatic, ;)
• lA is injected in this SJ)IICe ac primarily
pendn1Cd into intcrvertcbral foramina
J categories dcpcoding on the site of
\' J
y . ,,· femoral, hronchial plexus, trigeminnl, facial
, and phn:nic. Epid tnl anaathc:sia can be divided into
~
•
.,... / \"" on eye, limbs, abdominnl wall
\• • Used for 100/h c:xlrlletion, operation • -action.
cic region. Epidural space in thi1
r;>""' . ,·;r,.,"' 'v" fractu res, lrnuma on n"bs. ~ >"'lborac:ic: Injection is made in the mid thora
region is narrow amal1 wlumcs of drug is
requiied. Used generally for pain
4. SPL"IAL ANAESTlfESJA:
~
~
,t ~✓~
,../ .,}..
• The LA is injected in the sub arachnoid
rbe end of spinal cord.
space betw«n L 2-3 and L 3-4, below reliali>Uowing thoracic:/ upper abdomina
~ Lumbar: Relatively larp

l SUf&Cl'Y.
volumes of drug are 11ccdcd because
space is wide. tt pl'OINCeS anaesthe,ia of

epidurll\
lowu abdomen, 11clvis and hind
in the caudal cquinl:,
~
• The primary silc of action is nerve roo1
lhetised and par a!~ limbL
~~ • Lower abdomen and hind limbs arc anacs Caudal: Injection is tuven in sacral aina
l. Produces anaesthesia of l)Clvic ad
volume and speed ofinjcction, specific vagfoal delivery, anorecta\ and
• Leve l o( anaesthesia depends upon the _. pcrilllll tegion. Used mostly for
patient
graviry of drug solution and posture ofrhc genitourinary operations.
or isobaric lo CSF.
• The drug solution should be hyper baric 6. JNTAVENOUS REGIONAL ANAESTH
ESIA:
e ofposture after IOmin . of toumiquc:t occluded limb such that tlj
• n,e level of011ocsthcsia docs not change within ~g • It consisls of injection of LA in a vein ·us~ues
depends on the dnig used and its drug diffuses from peripheral vucu lar
bed lo non- vucu lar includiJ
. -- • The duration of spin11I anacslhcsia
· • · • • - · -·
conccn1ra1ion. nave ending.
• Addition -of 0.2-0.4- mg of IKhnuline lo LA prolongs·spinal anaesthesia
• Rep,nal analgesia is producr.d within 2-5
min.
min and lasts till S-10
oboul I/3 rd. paedic procedures,
• II is llllillly Ulfld for upper limb and ortho
 )
)
)
.rc ,,fhi&h ~ ~ c i1y,
'' i,.,•au
8ur1•n~.111ne ,h,,11 1,1 ,,.~ t,e n1111lo)" ) me 1o eilher_
a clcpcnde 11pot1 1ypica1 ~rmK
al r-s,a
• D I ~ o:r myw,sthcnia pavi -
~ nco sli~ lnc or cdrophooium, e stralg!la wbicb
gnu i,e IM- lmpro.cmclll orm mcl
of ,pht drln r, ~
I ts bf genus _Ep h~ ~ • Adminiatration or 1-1.5 mg of-U
· los11 for J-41n.
l . Exp laio tJ,,. pba rmuo l~ cainie drcc u
. ol,tsincd &om !hep mnaodLbell adrcocrgic rece ptor s and a whh DOOllipninc ~ 1hc maa
.,,d ~ •Atropine sulphale 0.6mg 1M Ilon
An.s: E1'11£DRl;\'E: Ir is ..n alk4J
· ubrcs both al~
- c $OIi! of Ach.
Pba rn,, .<-ologkal actions: Eph.
.,Jrin
nss-
J
relcuses Na'from the ncn-c.- eodi TR.EATM.!NT~.
. contn1ciion .-
. . and increase in lho clll'dloc
outpu1. ~ in die tn: atm mt of~ p-n
s.
.,,..1 . CVs: lncmose:s 1the furcc ofmyocanlW
lnaases BP duc to pcnpbcritl'
'aS(M.'!OOStnCUOR _,,,, nsc. f
th ~
• Neostigmine is formedyused
Bc:cause ofiu short duralloo of acdo
a, d.R ii a.......,._. oflD lcna cc, WWDg alld
side c&d s -
•
. 11. ~ ihe presser •-r - o muscles, wtn log of muscles, agen ts 1ri1h
mt duntian of adioa and low u
c,rcd adm inis tnno o _ smooth m11$clCS, uterine smo t) ambenonium.
• Rc:p utcs bro ~tal fbladdo-. pn,ferred. Eg: Pridostiginine and 30m in amd while on oral
I 2. Srnooth muscles: Rclr lleosbgimae appears with in
sphmcrer ~ ~
iety
. the restlessness, insomnia, anx • , • The effect of p,,m iten l
.., in= rs rhe tone of rrigonc and. tiCd0$CS ti C4USC:S •
poly S}'Dap(1c ~ o n proclucC$ a resp
onse wilb io l br.
h , cmiscs the monos)'llllpllc uid • pjri d -,f g · 1& )0-6 0mg ,
' .
J. CNS: Stunufar cs CNS at I mpt
IJ'on ors and inac ase in mcn
u. .
l:i.l ld!V lty. 11111 ~ • The lbc:npy is initiated
by Dmlligimae 7.5 -10.5mg.
y ~ 'IJlllil lhe
'1"' ~ a time and lbc dose gnd mll
__,, 1 ambaloni11m 2.5-Smg oral ly at
n:flc.~C$ of spu ul cord. ·...>
. . .--v-- n. mllXimllDI benefit is obtained. 3-4h n!y orally or
~
ctabolic rate and oxygen consum
ptio cstenscs are 11SUally administered
,s. . . h • The rcv111n1nle anticholinc
t. 4. Eye: prodUCC$ mydnll!,hed rin e~~ I em
ll' S. Met abo lic dftc ts: Ep
ADI\TE: Absorbed on om! udnuntsln
, • RC$istanr to MAO
lbon
-,.~ puen lall: , to ensure smooth and
• 80-90% of fflCOYelY occms in
S1lS1ained effect.
2S% of individuals.
is u.,ed in its mmagement in lhe
oosc o[25-100mg once
~• De aminared in hv~T.
15% is eliminated in urine io an
uncb11Dgcd form.
,.
!.l
•,-)
• J>ra!nisolooe a g)ucocorticoid
a day.
as ll.alhioprinc used as an adju11m
t thm py in tesis tant
__, • Other immWIOSllppR$Sml suc:h
: I S-60mg oral ly. j.,.
edrine hydrochloride tnblcl 30mg, dose casca.
Prc p»r alio ns and dosa,:c: eph
Eph edri ne hydrochloride eHx
ir- 15mglml, dose: 5- IOml.
...
' ,_)
' ;) 4.. Wri te ID detall lbol lt die dns
p ■ttl111 oa glaucoma.
3. Exp laill ;,. drta iJ abo ut lllt
drugs acting on myu rbcn ia gra
vis.
t:, Allr . DRUGS USED IN JBI
Df.ATMENT OF Gl,A\lCOMA.
unu eate d il lead s lo
TR£ATMF,NT OJ,' MYAESTHE
NJA GR AV IS, ch intraocular tens ion is raised, if
Ans : DRUGS USED IN TRF. • Olauc:om• Is • condition I.a whi
ress ive we akn ~ of
'~ optic neuropathy with loss of optic
nUflle.
ri1.td by easy fatigllbility and prog
~
n.
• Myasthmia gravis is charaac: • ThJS may be accompanied with
loss oflltripberal and later centnl visio
stria rcd muscle. a ~oss ofv isi~n is
seen.
• II is M autoimmune_disorder
: cau se< iJ.i x.l b~~ of postsynap
JiC.D.eptO!JlUSCUll!L ~ • Most forms of g l
b) clos ed angle c) cooge11ital d) drug indu
ced.
Ach receptor comple~.
• e n - is classified into a) opm angle da ~c om a is due lo
e are degraded and cleared mach
faster than ~ • Etiology of primary gl 1~
b not lcn o~ but ~n
Recepto rs in the my ~c niu_uscJ in t i ~ neuro vuculllrization
and ~gment dispcm;ion synd rom e.
•
normally.
Ach may be reduced lo 70-90%.
tat • Elfflted ialr l ocullll' pnlSUft'; an
be reduced by :
Number ofavailable rcccprors for 2w of~__,_
• o lna as ing th eo ut _!!
ger hypel))lasia or lhYmnrna eous humour by lhc ciliary bod y.
• Many palienrs with this diirordcr may atu o Dea-easing the prodaclion of
aqu
of Ill ·
rome (Lamhcn-Eaton-;}_..,romc) a ormmunc n re • :
• Ano ther myasrhcnic synd • sm..tll cell car~ino na oftheJun "" gs. • In, acutt ......,..;tt da n5 Thi s blockade by iris results in
occurs ,n. asso . . w11l1
c10t1on 1 • ·- · · - _ .•.,... _ o .l'he uis is
probably bloc:b_the lnlbecular specc.
• The 11utoa11tibo.dies nre dirc,,ted lo rhe
_tlll.ci11m .~.:::.j
·- '·
:-lhe
e tem
.
nnals with the
~ - - • tbc intrlnC:Ula pressure
producin& severe pain nausea and ol\c:
n loss
. the ~ch release from nerv-e tccm -=L . '~-m nerv
ioals.""" - - ··- - -
decrease m . . . . . . . lo opti cllm phy.
• Myaslbenia can also be induct-d•
by pcn~illamilll: dUri th e trcatmcn1 of rheumatoid
ng
arthritis and wilsons rlis~
 ....-,,
""""\---, ~,. ,)
;,:1 --.~)
~ · - i, • pn"fCfTl.'II
• · - - -
o h s • "'"hea l <"Ill ~ An.I• r,k,"'1'4!10 • ,ch l'h•
- - --- - ~ m111111il~
Adjuv:ml$ such .u a."1&1'.<'lami<lc-11tC l'fllJ'I" )~ in aa ~
lrclllln< 'tlL
•
0
may be infused IV 10 lf,,.,ir !Or.
,. I V
...:i \)
/ • ..-Chro
-
0

0 Once the :,cute 111.1d: 11 a.,ntml lN surga')' ii advised.

m·e( ,...,"d <'-a ngl<"} Jlrnnk i:l1•N>m!..i,
It DCC'\fs pcmw, cnt clruJ lb(npy.
°
Couse of aui~ IOP is 1101 known.
,..I ~
... r~
M .,,pl1h1 the al«p1 Involved ill tllt •••ro llumonJ tru,inl nlell of
NEU RO IIQMORAL TRANSMISSION Of A/'115
► Transm ission of nerve impulse ■croa 1.he synaps e in call'II

ANS.
and pcripha11 nc:rvom
~ <>f the dccltnod in vision is l!nllltllll diagnosis is delqed. ,. . v
"- lhc SY111f1K c:lcft.
0
syste m= as• result of.!J.._cutO humoral tmrmut lEr lllbllmcc into
• l\fajor goals of drug tb,r2py !ff; - , . to ,.. v ~ Dubois suggested that junctional 1ransm1ssion c:owd 6c c:idw:r chania
l or el"Strical
!OP bdow which furtha- optio naw dam•F is unlikely ,. '· of c:umal DCM:
0 To rruiint.:un :in
• v 4 JCunhe> molor end plats of the 1kcldal muscle was c:x:ilal a aRSU11
0

0
oa:ur.
To rc:sct the !OP lo a lowwr level.
To minimi se lbc local and systemic side clTccls ofiMdn
lP. . -v~
'
f
impulse.
Langley- Prr:smce of excitatory or in1u1,itary substana:s in the effo:dO
► Lowci - Vagu1 i.alul>itcd by heart by a cbcmlcaJ trarumi1
1tr A ~ choline
r cdJ
.
o To cdua1e the r,3ricn1 llbout the disease. ~ !
He perfuR d the heart of frog. He allowed the l)C!filsion fluid
fiom a fiog bccl IO cmne
• Trurm ~,:
0 The inililll aim is lo achieve 20-50% ,eduelioa ill IOP wilh mc,clu:a
ticm. ....I,)
I .J
in contact wilh the S(.-COnd frog heart. Vogo stimulation of the
donar fros will produces
clonar &op. He proposed the mm of
The P~ gla~ analog ues~ ,iho drugs initially once• day. ~ cardiac ancst in bolb lbe r«ipicnt BIid lbc
0
~ - a fluid. tbe subslanc:c
.. -> recipient heart is due 10 substance tdeased &om the pafusio
o Beta adn-oa '!!ic bloc:tea, timolol are u,ed.
initlal.ly called vagostuCf. Thm it is called a, acecy1 choline.
o ClJ adrcnergi c ~ni.st are less clfecti,~·ihan timolol. ,..J
o AccL1Zol3:!11ide, 1 c■rbooic anhydruc is used orally in ■ dose of 0.2S-
inlulri~ ... . ~
l gm daily in divided amounts.
o Topical carbonic ■ohydrase inhibitor prepantioos liko
Doaolamide and
...
- l.
,.)
NEUROTRANSMITTERS:
,l- Acetyl choline
Briozolarrude can cause less loxiciry and are prcfc:md.
...- l.,.) 8:• Adttnaline
...- L..)
glaucoma. , C. Nora,:IJq]alne
o Rt.-vcrsible an1i-choline ~erase gives satisfactonly n,sults io ,, D. Dopamine.
!bey may impair
o Miotics should be avoided io patients with c,WIIC t beQuSe
vision.
...,-I__. ,) AO."T YL CHOL INE (Ach):
- ----- ---
o Beta adrencrgic bloc:tas may cause cardio\lllCUl~andrespiratQJY
side_eficds.
~l • It is recognised 'by Ille scie n ~
---rf' isan mc:,-of choline.
Drugs used io glaucoma:- ;J--, :.,'' is synthesised in the nerve fibre by the combination
of choline from lhe
• ·n1ose which iucrcases Ilic outflow of aqueous humour: ;-i-., cxlnc:dlular Duid with ICCf}'I group of acetyl oo-A
/ Cbolinergic ageots (M'IOlics) a: PiJoc:arpinc ~ drops 0.25-4 %. I • Ach is 51oted in the synaptic vesicles and Is release d ~
/ Cholinesterase inl1ibl1ors ex: l'hysosligminrt 0.25% oinlmenl. ;--· :, • Acb is IIIClaboliscd by the enzymes like •~Jcbo line est~'IC
and butyryl choline
o ProstJlgladin analogues ex: lAcanopo&C 0.OOS': ' e)'C drops.
• T'sc which decreases production of llflUCOUS humour by the
ciliary body
~ - Non selectiv e beta blodas ex: TIIIICllol O.zs.-0.5% eye drops
·:;)
,-I
.,
... -
- -
esl!en! eS. I
ADR!NALINE, NOR ADRF.NALINE, DOPA ML'IIE :
o Sclccti ve Bela adrenagic bJockm ex: Betuolol. ,--------~ ---
• These an: called as catecbolamlnes. 1
y Non selectiv e adreatrgic: against ex: adrmaline 1-2% eye drops. • Praent in the high cooccntrations in t~tenn inal axons of the
neurons. )
o Carbonic anhydnise inlJJ'bilon: ·~
. __ • ~ ~~rs &i from the~ ~ call~ e!!cnylalanine.
' • Topical ex: Brillzolamick. . .:.. ~
• Phmyfalanine undergoes hydroxylation· in the presence of
hydroxylascs and
• Syslemic ex: ICdalolaniide. • foJDIS tyrosine which OD fuitiia~~r11 1io11 in the presence
ofhydroxylasc:_s
l'onns di bydroxyp_henylalanine ~ -DOPA un~ergocs the ~C:8~~~y_lation
 ~
,v-
.> ~r~
C. -
C. -

-
c._. ,,_)
,.\
,)
---
'
1r .~ •
\9·
\.. .,.. .
rn the P""'"""" oroorA. J"""'bo1.lc~ anJ f,,..,,.. ,1<•1"'"'
i,,o. ,,..0 ~,u~no
h \roit)llnlll'°'
<:. _. ,\,) · of nerve im.,u\scs
► Loc11I •n•cothc1la. l,1n,;k the, 11£'M"alloo rwd e<.1nd..ct&00 r· at all part:!
orlhc 111:umn wllffl they come In contact without c:.ousing structunl damage: 1il50
" )~~ .,,..r
. ,. ~ ~, ,,,r· lhnl is formed is l lnr«I in 1hc C}1l'f'l"<nL Ol'11'11nin_cs ~.,:,,ll,..,.
:,nd fOnn$ Nor ~nlinc wln<'h on fu&thcr mclh)•~ion f.m - -- ':-• ·v ► They ore nol only net on 11e11:,«y nave■ but when epplied to mixed IICUfOD It -·
affects motor impul,n resulting in rnuaculwr para!~
'--.
NA nnJ Adr N"Cstrored in Ll~~ lm,~~ul~_) c;. • \\ ► CLASSIFICATION: -- - -
v"'' I. Injectable anacslbctic:s:
S-0:PS INVOLVED lN NEl!RO UUJ\IORAL TRANSMISSION: C . \ )
~i=
a. Low potency, s1,ort duration:
A, IMPULSE CONDUCTION: cg: Procaine, Chloroprocalne.
1 ,\
In the resting membrane -1ium is present oursidc lhc cell ond lhC Po C -. b. Intermediate potency and dUllllion: ,;:-
present inside the cc:U. Stimulation of electric impuls-• In lhc cell causes sudden 1nc:reasc
d' • h - .
,n
.0 nsD'loVC cl. . u Eg: Lidocainc, Priloc:aitle.
c. 1-ligb potency, loogduration:
,) \..
,--
so ,um ID I e axo~ mcn~l'lll'I" thi.• is due dq,olnrisation ofthe cell. 1bc potasstU'."° ' tential
o ul of the ceU cnusmg hypcrpolariSDtion. The potential genttalcd is +20IIW, Acl10R po
C • __v Eg; Tetracaine, Bupivacainc, Ropivacaine, and OU,ucaine.
■-~
·-
generates in the ceU which ncllwlcs ionic chaoncls at the next excitable p$IS oflhe inetnb~C. 2. Surface anaesthetics:
C -~ a. Soluble: t.- f,
B. TRANSMITTER RELEASE: Eg; Cocaine, Udocaine, Telracainc, BeooxiDate.
__, • .... _,., junctional
u . .
,.t:'W'Otnmsmtllcrs (excitatory and iohibitorY) me SID""' ID - .r•·. cd - . I ,.) b. Insoluble: ·
ncrYe endings in the ston1gc vesicles N=·eimpulse gcoCllllcdwill pt0motcs lhcv~cles7'us. -
with axonal membrane~e calcium ·=IIY lakes placAI. then all the contcnlS of the _vcs!cle w'.IL
~·· I -. ).
(" Eg: Renzocaine, Oxetha7.ine
► Local anaClllhctics arc high lipid and low wat~ublc will-not be useful for the
be exuded otil from the synaptic cleft. .Proteinsukesynaprot1gmin, synaptobn:~, n~rciun transportation lhrougb the aqueous pbllSCI surraundingthe na-ve fibre.
arc locarcd'in lhcvcsicul.v and the axonal membranes are participal~ in lhe :f\J..,;aoo. wilh lhe ~(~ ► Local anaesthetic,~ consists oflhn:e parts: ·
axonal membnlllCS by cxoc::ytos:is. c-1 \) i.)
ii.)
Hydrophilic amino group
lntcnnctliate chain -
C. TRANSMITTER ACTION ON POOOSTJUNCTIONAL MEMBRANE: c- -
The relea.scd transmitter combines with. the specific r,:ceptor.; on post !UJ)c~onal ,_I _..> ►~e
....) A iit.>fil,liilic ~gmup.
the -presence of amino nitrogen these are the bases and fo_rm salts with the acids,
membrane depends OD excitatory post junctional polenlial and inhlbilory postJUllCIIOnRI
-I ~ ►t Jf the tissue pH is alkaline the free bases is· liberated and vro<1.uce the phannacolog\C1ll
potential (EPSP and lPSP).
EPSP and IPSP arc due to depolarisation and hypcrpolarisa1ion of the memb18J1,C. Due
to the presence of EPSP and JPSP nerve impulse is gc11er.itcd in lhe cell.
~ ---
~.:.~
:.1_~
action oflhe tissues.
►, Majority oflhc clinically useful local anaesthetics are nitTOgcn nitrogen containing
compounds either in the form of esters or amides.
~ ... ~
D. TERMTNATION OFTRAJIIS~ll'J"I'.ER ACJ'ION: j.' Ester- linked local anaesthetics: Cocaine. procaine, chloroprocaine,let:racainc,
Combination with lhc receplor lhe NT either mll)I degrad~IJY or ll can either~ bcn1.oc:aine
taken up bythe_POSlj~onal neurons_by uef~e.mcc~ms, 'ii.) Amide linked loc:al anaesthetics: Lidoca\ne, bupivacaine.. Oibucaine.
~I..:, MF.CHANISM OF ACTION:
~
E. UPTAKE .MECHANISMS:
q_
'"J 3 ► Local anaesthetics block the generation and the conduction of the neTVc impulse.
UPTAKE J: Pick.ing 11p of ca1cdiolamine's liom cittraccllular spBCe by adrcoergic
c-1..~ ► The blockade results from lhe biochemical changes caused by U1e drug on the
o neurons and by the o1nl neuronal cells.
lJ1'TAKE 2: Picking up of NT by the effeclor cells in pcripher.il tissues like vasc..-ular
smooth muscle, hcut and exocrine glnnds. ~'-.
~-,,
~ t .
► Local anaesthetics like procaine prevent the increase in pc:nneabilily of the cell
mcmb- to sudiwn ion which is lhe fim event in dcpolansauon. Thus an action
is~ . - --- -·-- ··
► ~
l)Otcnlial
6. What are local IUlaadadlcl• C11ulfy them wilh cx:tmplcs. Wrile the. ml!chanism
or actio• or loc•I auestbedcs. :..L, a
The action :::the-process of depolarisation leading the failure of propngalion·ot .
C I-'
~
►. Ans: Local aoaeslhdics are the drugs which upon topical application or local impu!Se without affecting resting potcntilll is known as Mcmbrano 1tnbilising dfe'11.
injection cause irrevasible loss of sensation, especially of poin, in a restricted area of ► Smaller nerve fibres presents as a g,-eatet surface area-per unit volume of action 1\1an
large fibres. Small fibres are blocked first.
1he body.
► Vari~rcs are bloc~d in lhe follow~_g manner.
 Chl pttr lV

lOMARKS,

1. Wha t are antl-cplleptlcs. Classlry them

. Explain the pharmacology of J>henytoin.
Ans. These arc the drugs used in the treatment of
epilepsy or epileptic seizures.
CLASSIFICATION:
~-eeYCJ!tics arc cla~ ecl based upc,n their Ulf&
banisms niaclio.ns:
1. Those act through the neurons) excitability
by delaying the recovery from inactivation
ofsodium channels
Eg: Phcnytoin, Carbamazepine, Lamotrigioe.
2. Those actW ~ca sing the low thrcsholj.calci
um.@ ~ the_thalamic neurons
Eg: Ethosuximide.
3. Those act simi~arly t~ ~th phenytoin and etho
suxinpde
Eg: Valproic acid.
4. Those act by enhancing inht'bition througll
OABA.
• Acting ihrougb_09A related --,t ors
Eg:.Barbitwates, benmdiaz.epines.
• ~ relcasin&.GABA-fmm nc:ur...cll!ll.~gs
Eg: GABApentin
• By inhibiting GABA trm•11ppinas~
Eg: Vigabatrine
• By inhibiting.{lABA..ceuplakG__
--- ,-----··
Eg: Tiagabine
5. Those that inhibit excitatory neurotraosmittas:
Eg: Lamotriginc
6. Miscellaneous: Leveteracetin, Ac:ew.olamid
e.
PHENYTOIN ~ll EN YL HY DA NT O~
MECHANISM OF ACTION:
• Mainly acts on affecting the voltage dependen
t sodium ion channels.
...,A"" It acts..on..allnMOnal..mem
bnmes ingndjng peripheral nerves as welJ as non-
excitable and excitable membnncs.
• lt~ ~t h~ ~ of seizwa in the brain and shortens duration
of after
dis chi r~.
• It causes dose dependent block of sodi.um
channels bY, !educing the sodium ·
00nc:eotration leading to a reduction in parox
al de larisation · PS) "'
• It e post tetamc potcntiation (PTP) which is resp
onsible for the
-----
seizure. .
• PTP is not involved in the genesis of pitet mal epile
in this condition. -- - --·-
--· -·
psy and hence it is not used

• It increases the brain levels of GABA as well

as 5-HT and homovallmic acid.
 ., c,,--'-11111' '
. ~ '-
•"
~
r ' ~ ,\
t}
'Z
'
;: PHARJIUC'OLOGICAI. AMIONS:

,.
~
C
---~
- ~~
7• TV.l(ATO()F.NIC:ftv: Cauoc foetal hyd.,,.ma oynd•Off!~tin&.lil'.I trimcslc:r of
prcgnoncy. II &how■ midline hypoplasia, ptons; wide snoutb, inter q,icanthic folds,
il
• I. CNS: It in=a.•es the antitriltptic .._-ti<,n ..-i1hout causing lhc Jrow,ine.'IS,
~-~ short ncci:. mild webbing or neck, llholt plMilml!,d, hypc,plutic nails.
Some childm, may develop lic61t defedS, miaoc,,:phaly lllll mental S1Jb
< Onsd <-f acti<'n is sJ<,w throuJ:h IV injection.
Action persi~ foe k•ns time after cessatfon ofdicrnpy.
• 2. CVS: Phcn)1oin dc,pn,s:scs \'a\lnCUIIU' autM1atidry.
0e.."l'CaSCS the «•nJu.."tion velocity t,,,twm1 vcntricul11r m,rcs.
~ dur.ttion of action potential.

C:. ·~
C. - ~
C • .,)

nonm,lilics.
8. MISCELLANEOUS: Mcploblutic ~ blood dncr.i.asis, ;,plastic anaemia and
agranulocyt~is.
DRUG IN'l1!!RACTIONS:

·· - - - - -
Shom,as QT intcn,1J i11 electrocardiogram.
AJmini$tcml otally 100-200mg41imts dailysupres,es thecc~IS. 1. lsoniozid, cimetidine, colrimaxazole and coumarin anticoa:gulaols imumlS ph\.'Dytoin
C - -~
c-·. ,.)
c- ■ ~
I.age tv ck,- it causes hypolcnsiaa, AV bloclc, cardiac Dll'C$L metabolism due in<:reue in the plasma levels llllld toiticity.
ADMF.:
2. Folic acid during its chronic administralion redua:s efft:Cti'Y'Cl1a$ oFphalytoin.
3. Ph~yt~n <X>_!!!P~~~-~h as sulphonamides,~-• and vitamin 812
..~-•··.:,
( • Slowly and ,'llriably lhsod>ed &om the guL rot binding with plasma proteins.
• Reaches peak pluma conantnnon in 3-12 hrs after ingestion. 4. Riliun~in and eth~deaeases plasma ph,:nytoin because of hepatic cnzym"
• 70-95% bowidi lo plasma prolcins iniliiclion.
• M~:iholiscd by Pan hydroxylation in liver.
• Cooceotrated in bile, rc.~b~ from inlC$hllC as parahydroxyphcnol. ~· ·
~ ~
.J THETRAPEUTIC USES:
• Plasma h12 is 2-4hrs :,_;rn:a1men1 of gramlmll epilepsy
~ . i.)
.•
• 94~'of lhc diii_g is cxa,:ted through urine within 48bts. •_,.,Psyclion,otor seizures
• Ifcauses hepatic microsomal cnzym~ue1ion. - c- • . ;) ~,,. Focal cortical cpikp,iy
c ■:~
..,,, Slatus epileptictlS
ADVERSE EFFECTS: ~- .Cardiac arrythmias
l. latolennn,: U 1ticarial, scalarifonn and measles like skin rashes mny occur. _. ~ • • UtK.'<I io treatment of neuralgia
Skin reactions may be accompanied with Jymphadenopalhy, hq,atomegaly, und
jaundice.
2. CNS: Mild roxi city ca~ ~wsincss, &tigue, headache and confusion. ·
.-■ -->
l.r .
.
. • - In diabetic neuropalhy.
2. Whal are sedative- hypaotics. Classify lhcm. Explain the pharmacology or
Large doses it causes vcstibulocerd,ellar syndrome which is charPcteriscd by c-~ ~diMCpam
vertigo, al&Xia, nystagmus, dys.uthia.
Ocular pain wilh bluning of visio11, ddusion.s, halludnations. ,c-~ Ans. SEDATIVE; A drug lhat subdues the excitement and calms lhe subject without
inducing sleep though drowsine:1s may be produced. -
Rarely behavioural changes may O(X:Uf.
c ·~
~
3. GIT: Alkalinity of lhc drug causes nausea, vomiting. • HYPNOTICS; A d111g that induces and m~'!!.ai!!J! lt1c.slcep whiclt is similnr to nonnal
4. FACE AND GUMS: Hyperplasia ar~ hYPmrophy of the gums with cJerna and arousablc sl°"'P·
bleeding. • Sedative hypnotics arc geiieral CNS depressant drugs with time and dose relation ships.
Long lerm pbcnytoin therapy causes hypertrophy of facial, subcutaneous tissue, ;C - ~ • 1bo$e dnies which ha11e quicker onset, shorter durati,o n t111d steeper dose response
hypenrichosis end ooarscning of facial fcarurcs- pl1cnytoin facics.
.~ curves are liypnoh"c!ls. · - -
• Slowiy"aci"'i;,-g dru;·;ith flatter dose response curves arc acdati~.;;;~'l
S. ENDOCRINE EFFECTS: Hypcrtrichosisin children.
Hyperglycaemia and osteomalacia
Rarely, hyperglycaemic, hyperosmolar, non-keiotic coma.
c-S • _...sc4~v~drug reduces e>tcilemenl, calms ihe
L.. aiwP.I~_;
CLASSIFICATION;
,_ . - - --
patient
-·
-and is commonly 11RCd as an
6. ENZYME INDUCl'ION: · Ac.:elenllcs mel.abolism of vitamin-O, folate L Selective benzodiattpine OABA-A reaplor agonist~:
gluooc:oltic:oids, ~ I Sleroids, thyroxin,OC pill;, doxycycline. • L Benzodiucpines: Di87.epam, oxazc:pam, lora1.epam.
b. Non- benzodiazepines; Zopiclom; zalpidem, zalq,lon
IL N011- selective, non-ben7.0dia.o:cpine GABA-A receptor ag1mists
 r - ~,
~· UII
r,. '.,-'
(. ~
C. - v
• It is sq,an, lcd by simrle distilla tion ~
) . (;VS:
• Colourless, volntilc, i11011mmable liquid. C !II" • Drinkin g wine have • can f~v e
ec1iv,ty due 10 clc,v•1i on of IIOL
cholC$1 cTOI levcl1 and 1nh1bit,.,.n of platele t a,;tivat
ion.
_,, Ncutrnl spirit contai ns 9().QS¼ of almhol. C. . . \) • Alcohol may relieve w,ginal poun.
w,\h hypert ension .
C. . . \.) • Regular con~umption of alcohol is iusoe1a1cd
dial fun..'1ion.
• Small amounts of alcoh o l • - lhe myocu
Pl IARM AC OLOO ICAL ACTI ONS:
II
C.
and precip itates any,hm ias.
c. v • Alcohol effects the coodUC11on system of heart
by depres sing vasomo t01'
• Appliocl locally ii evapo r:ues quickl y. • In moder ate doses ii cauxs dilation o f skin vessels
in TCducing the lcmpc ralute in fever. C. • \.) centre- flushing and feeling of warmth_
• It hos cooli11& and refreshing elTcc:t and is used
In concentrations of 40-50 ,~ it has Nbcfacicnt
e ~ and mild irritant action. • Prevents cutaneous vasoco nwidio o on ci<J)OSllfC to
cold.
• '-1
ent, germicidal 111d irritant. 1lliy centres causing
• In higher concen tration s it ads IS an astring • Taken in conccnlnated folffl stimulitcs the mcdul
incn:a.ses cardiac
• Alcoh ol in the conccntrutioo of70% acts IS an
anti~ tic. increase in the blood pressure, accelerates the bcmt.
C - ~
1/IT~ output.
~-· -·~
Talcm orally it gives local feeling ofwan nth. C - ~ 4. LIVER ;
~
• lt .:auses dose related toxic effects.
• lnaa.s cs lhe saliv:u y secretions.
• lnitant action o o gastric mucos a - arpcti zer.
• 7~1(1"/4_of 50ml alcoho l will ina-eases the
gasiric scaeri oos by rcle4sing ", • Common effects are farty infiltration and bepalO
are due to impaired gl)"007. ncogcncsis, glycog
meply. These effects
en depict ion, n:duced
synthesis of albumin and transferrin, diminisbcd
fatty acid oxidation,
hiam ne and gastiin from stomach_
• > IS%- incrca s~mo tility and secretions. e • ·.-~ increased synthesis ofVLD L
• Ac:ule alcohol coosumptioo inhibit s hepatic
m\croSQfflal CYP4SO
c ■"
and intestinal juices.
• >20% • decrea ses enzym e activi ty of gastric enzymes.
■-v
• > 40"/4 • Toxic effect on gastri c mucos a. • Chronic alcohol consumption increa ses the nte of
metab olism of drug)!
2 . CNS: r----, C such as pheoobarbitone, warfarin and steroids.
■. ·"
bcpatomegaly.
• Primarily acts as Q!S dcpr t.Ssa n~ • Lllrge quantities of lllcoho\ causes hypoglycaemia and
inhibit ing NMDA rcccptOl'll, effects C
~ ~ Acts by enhancing the inhibitory GA BA by
~ ■ -"
5-HT, nor adrena line and 5. KJONEYS
die functi oning of recept ors l ike dopamine, • Alcohol increases output of 'llrine due to tubula r reabso
q,tion of water
" ■- ~
•.--~
endorp hins.
ioczgic pathw ay that projec ts • Increases excret ion of mngne;ium and calcium.
~ The pleasurable effects are mediated by a dopam • Decreases lhe excretion of potassiwn.
ffects like eating, sex ontl
~~
from the ventnll and trigeminal area. The ph:asu mblee 6. TF.RATOGENIC EFFECTS:
mnsumptioo of substa nces of abu..;e arc increased. • Drinking during pregnancy causes damage to the
foetus.
• Long tc:rm expos ure to alcohol brings chang
es in neuronal systems which is due
ors and excitatory glutam inergic
~ • It causes fOdal alcoholic syndrome which
is charac1eriscd by characteristic
tion, mental deficiency.
to die regula tion of inlnl>ito_ry GADA recept facial appearance, purentmil onset of growth retarda
-(; .
~
<; • .) Moderate consumption during pregna ncy causes
•
low binh weight and
m:q,to rs. and hypera ctivity ufCN S.
• Sudden with drawl of alcoho l cause s excita lioo
• Alcohol reduc es ";sual activity 311d interferes with
muscular coordination in ■:· 3 spontaneous abortion.
7. SKEU ITAL MUSC LES:
small doses. :, • Reduces lhe muscle slrength
activity of brain such as
• It impails lhe ability of brain to coord jnate motor • lm:vm iblc damaac to muscle tissue_
typing, standing and band steadi ness. 8. Miscellanmus:
senses of proportion.
W-1111 increasing consumption, the individulll losscs all
•
of self -control.
c·-•
C - -~ • It is aphrodisiac drug (sexu3l stimulant)
testosterone levels, impotence,
•'
• Difficulty in speech, unsteadinesa of gait, complete loss • Chrooic alcohol ingestion causes reduction in
ia, leucopocnia, dccrea~c
• Large quantities can cause unconscious ness. sterility, 8Yf18ecomastia. prostatic congestion, anaem
• .Jtespinition becom es slow and face becomes
pale and psynotic blood pressure c .- . ') in T-cell s,Jiyp erlipid aemia , hypcNrcaenaemia, pana-e
atitis, hepati c cinhosis.
&Ila. c..• .--.
~ ADME:
• In epileptics alcoh ol precip itates convulsions,
duodenum and small intestine.
• Ethyl alcohol is rapidly absorbed from the stomach,
 , -- 1!!111111,
• . J'
·,- 'II
c--. . ,<~
C. fll!IIIIII
C. . . \)
~
Reller of ,nxlcty ind •Pl"ct,.,,.i,, n preopcnti•,cly ■nd
1
- ~~
: ;"'SQ'lltion is ~cla)1'd in the p~,re nf ~'Id in ~•nm,h. • 10 ,,.~;litale smoolh
~ mctnhohs<J by Sl"tric and h~tic akM.11 dc:h)-dn •~ fflt)'IIIC. C: incluctioo.
• ~bured through body ,.,1cr and •tnmf hi CI\U)' Ilk....,
• II IS CJ<cn,ted by kidneys lllld lurigs. c.. . . \) • Amncala Cor ~ ■nd post-opcrulive evcnll.
• Supplement analgesic action to anar1the1ia.
T IIERAPElTTIC USC:S: C. . . \.I • Anlicmctic effect extending lo the po!lt -opcntive period.
• Dcacu: addiry and volume or gastric jUKlC.
• In the symptomatic trealmfflt of f-t-va-. C. . . v
• In the prevention of~-.. Different drug,,,: .
• As an antiseptic C. . . \.) Opioid,: Morphine or pdhidioe (.SO· I 00mg) i/m relieves anxiety and appreb~1o n
.~v
L
• As 111 appetizer. nf the op,r.atitw,, prodt.,u pro- and post· c,pcnlM aalgesia, !IDOOlhm i~ctJon,
• Methyl alcohol poisoning C. - ~ . reduce the dose of anaesthetic required, suppl- of poor a:nacs1heuc, pro-
C . .... \) opmtive restlessness is required.
• Wash out phenol during accidental skin ClOlllaminarion.
Dlsadvantagt1: Decrea.'!es respiratioo, interferes with pupillary sil!II' of
-~. .
• locnl injection-neuralgia. C
anacslhesia, may cause fall in BP, cao precipitate asthma.
S marb
~ ~) ► Lack of amnesia, flushin& delayed garuic emptying and ln1iuy spasm.
► MOTphine particularly cauaes constipation. vomiting and urinary
I. Expl~iu in detail abo11t 1111ges of gencnl anacstlesla.
Ans: General ~aesthetics : These are ~ which bring about the loss of scnsatioos,
parttcwarly pun along willl l'M:nlole loss or coesciousnc:ss.
~~ . -,)
n:tcnlion.
► Use of opioids is rcslricted to those having pre,<,penti\'C pain.
b. Scdatiw- antianxi,cty drugs:
■:·v
~ ,.. ► Benzodim:cpines like diazepam (5-10mg) or Loruepa:m (2mg/kg) aare used.
Stages of ceaenil 9uestllesl1; C ► They produce·tranquillity and smoolllen induction.
There arc four stages ofgeneral anaesthesia.
to
C ■:v ► They can be used lllong with pethidine or fentanyl fur a variety of minor
surgical aud mdnscopic procedures.
a. Stage-I: (Stage of llla!gcsia): It is !he: beginning of anaesthetic inhalation. Lasts up
loss of consciousness. Pain is abolished. Patient remains consciou.~. Patient can hear C ■ V ► Promcthozi.ne (50mg 1/M) is an 1111lihistaminic wilh sedative anti emetic and
-.■:~_\)
antic:holinergic propa1ies causes 11.:!IS respiratory depression.
and sec, feels lilcc dn:am lite state. Amnesia develops by the end of this staee. ReflcKes
and respiration are 110I1111I.
C c. Anri cholinc:rgjC$:
~... ► Atropine;' hyoscinc (0.6mg IM/IV) arc used primanly to reduce salivary and
b. Stage-II (Stage of delirium): This stage st.arU from a loss of consciousness to regular
~!ration and excitemml Patient may shout, strugcle and hold the breath. Muscle
tone incrc:ascs, jaws m: dosed, brealhing is jaty, vomiting and involunta!)' ruicluritioo
are-.
c. Stage-lIJ (Stage of surgical anaesthesia):

~ -•~
<:· • ---~
-.
bronchial secretions.
► The aim of their use to prevenl vagal bradycardia and bypolensio n and
prophyluis of laryngospasm.
► Hyosane in addition produces amnesia and antiemetic effect.
► They should not use in febrile patients.
This stage starts &om onset of respiratioo and ends by the cessariuo of sponlaneous
brathing. It is divided into four planes:
Plane I: Roving of eyeballs is seen. it ends when the eyes are fixed.
cl'
.--l ► Dryness or mouth in pre- and post- operative may be distressed.
d. Nturoleptia:
► Chlorpromazine (2 5mg), trifluopernzinc ( 1Omg),halopcridol (2-4mg) 1/M are
Plane II: Loss oflaryngeal and corneal reflexes.
Plane 111: pupils 11811 dilaliJw. light rcn~ lost c-•-
~
c-1
-
J
used.
► They cause anxiety, smoothen inductinn and antiemelic action.
.c-•,.,
Plane N: lotercostal paralysis. shallow abdominal respiration, dilated pupils are seen.
d. S1age N (Stage ofmedullary plltll!ysis): ~ .> ► Involuntary movements and muscledystoni a can occur especially in children.
e. H2 bloclccn:
II slarts from lhe cessalion of breathing and a11l by failure, of circulation J~d deorh\ )
' - - . "-· ► Patients widc:rgo prolonged operations like caC$arcan section, obese patients
Pupils lie dilaled;-pu&e is tliread and BP is reduced. - .
:, and increased risk of gastric n:gularions and pnannonia.
2. !Iplaill 1be pn mNSdldic medicalif f la deb ii.
~ at
► Raniridine (150mg) or famotidine (20mg) gi~cn night before and in I.he
~.~
Ans. Pre anaesthetic-medication refers to lhc use of drugs before anaesthesia to make momina benefit by raising the ph of gastric juice which reduces the volume
pleasuR: IJld safe. and chances of regurgitation.
The aims are:
~ '1:°'°" pump inhibitors like the omepra7.ole / pantoprazole is an alrc:mative.
f. AnlllllllCl!cs:
~
 ~
,--\ J
► Metoc~opmm.ide 10.20mg l/M ly rrropcn1tivdy is effective in reducina post·
operaltvc vomiting.
i;
► Combined use of mctocloprnmidc and H2 blocltm more offe,:live.
► Domperidonc is more efTt.-cth-e 111d does not produce oxlnl pyramidal effects.
► ?'1~ansetron +SmgW ly is ro-s to be highly cfTec:tivo in reducing
1nadt.'tlce of post anaesthetic nous.:a and vomiting.
3. Write a note 011 dlsulfiram .

.~---'.->
C. •
" \)
.\)
'""'.. . \J
, =•\)
• Drugs acts on the CNS either directly or reflexly.
Neurochemlcal transmission of CNS:
•
•

Communication within the mammalian nervous system may be due to

the chemical messengers.
Neurosccretion is the fundamental property of the neurons which is due
Ans. DISULFlR AM
'-·• -=v to the chemicals released at neuronal endings.
• II is also called as tclTll ethyl thiuram sulphide.
• 1 t is used in the treatment of alcohol dependence. C.-- :" • The impulse gcncratioo in the neurons is takes place by three processes:
A. Ncurotransmissioo
• Theropy is initiated after alcohol has not been CODsumed for at least l2hrs.
• Tn:atroentisinitiatcd with 500mgofs inalolbeb 1-2 wecb i>llowedby 125-lSOm&
OD as maintenance dose up to 1 ~ - ~: B. Neuromediation
C. Neuromodulation
• Aftt.-r o week therapy small amount of alcohol is given to the palients to pn,dUC9 IIWC
reactions sucb as Oushing. perspiration. palpilatioa, - - , wmiting and docnae in
;j'~ • Neurotraumlssloa: It is a process by which an impulse is transmitted
across the synapse in between the two oc:urons. Neurotransmitters arc
:-:~
blood pressure. •
released in the synaptic cleft either stimulate or inhibit the post synaptic
• Sevt.TC reactions may occur even v.ith the first dose ordisullinm lhc belbllelll lholaW neurons.
be carried out in a hospital
• Neuromedialion: Elicitation of post synaptic responses · from the
MECHANISM OF ACTION: This drua inhsl>ils alddlyde dcbydiogm ue ad 'blocb
rdeascd neurotransmitters through secondary messengers like Camp,
oxidation or aldehyde fonncd during metabolism of llkx>bol. ll Ibo labibits duplminc bcla ~ Cgmp and iooositol phosphate.
oxida~c.
~ • Nearomodulation: Occurs at pre and post synaptic neurons to regulate
I\DM£: G iven orally, slowly absorbed from the gut and IPdaboliwd slowly.
the release of neurotransmitters modulate post synaptic excitability.
ADVERSE EFFECTS: Dmwsiness , nausea, vomiting. ~ c:nmps. &dg,-tity,
metallic taste in mouth, acidosis.
DRIIG INTERACTIONS: II inhibits metabolic dcpaclalioa ol Wllfmm, llloopliylline.
--· 'V
S. Explaia the DeU'Olnn1mitten of CIIS.
Am: NEUROTRANSMITfERS:
beo1.oc1i:v,cpeocs, carbamazep inc, phenytoin.
CONTRAfNDICATIONS: llcpatic and circulatory diseases, unc:onlJOlled dilMlil mcllit1II, • The CNS has both excitatory and inhibitory neurotransmitters
alcoholics. They are I. Amines, 2. Amino acids, 3. Peptides.
4. Explain the n~uro hun1e>ral tn■umulon of CNS.
• Amines: Acctyl choline- excitatory and inhibitory
Nor adrenalin~ excitatory aod inhibitory
Ans: Anatomically nervous system cian be divided into two divisions: Dopamine- inhibitory
I . ·n1e ccnrral nervous system
S-IIT- excitatory and inhibitory
Histamine- inhibitory.
2. The peripheral nervous system.
• CNS will regulate the functions like circulation, diaestion aJK! ft!lpimtiOA • Amino acids: lrglutamic; acid and aspartic acid- excilatory
GABA- inlul>itory .
and modifies tbc processes like feeling, attilude. lhoqlil and memory. -
• Peptides- Substancc-P- excitatory
• Major divisions of CNS are cerebrum, cerebellum, brainstem and spinal
. ::_ • - ~- _ (;bol1:CYStoltinin~ Inhibitory and excitatory.
cord. Billions of neurons are lhe functional units whicharcconcemed with
1. GABA: Major iniiibitory amino acid neurotransmitter in brain.
spccialiscrl functions like motor activity, perception and n:gulationofbody
~yad,uiud t'OD'I glutamate in the presence ofan enzyme called glutamic
fu nc tio ns.
acid decuboxylasc. It binds either to GABA-A or GABA-0 receptors.
 a. GABA -A: These are inotropic receptors which regulates the calciuIIl
channels. It is composed of a, p, y subunits.
a,f3 subunits- responds to barbiturates but not benzodiazepines.
'Y subunit - Benzodiazepine receptors.
b. GABA-B: Metabotropic receptors belong tog-protein couple d recepto r
family.
2. Glutam ate and aspart ate: Excitatory amino acid neurotransmitters. High
concentrations are presen t in various parts of the brain.
• Glutam ate is released from presynaptic nerve terminals and binds to
severa l glutamate receptors. The glutamate receptors are ionotropic
recepto rs act by increasing the sodium and calcium levels cusing
depolarisation.
• Two ionotropic glutam ate receptors are
a. N-Methyl-D -Aspa rtate (NMDA) receptors.
b. Non-N MDA receptors.

· - - 4.
101\IARKS
1• What
are Anti psychotks. Classify thrm. Ex11laln the pharm acolog
y of
Phtno thlazincs.
Ans: These are the drugs majorly used in the major psychosis like schizophreni
depressive psychosis. a and manic-

• These arc also called as neurolcplics or major tranquilizers which acts

by reducing
agitation and disturbed behaviour associated with delusions, halluc
inations in
schizophrenia.
CLASSIFICATION:
• Phenothiazincs: Chlorpromazinc, trifluoro promazine.
• Rauwolfia alkaloids: reserpine.
• Butyrophenones: Haloperidol, trifluperidol.
• Di phenyl butyl piperidines: Pimozide, penfluridol.
• Thioxanthines: Chlorprothixenc, flupcntixol.
• lndole derivatives: Molindonc, oxyperitine.
• Dibenzodiazepines: Cloupine.
• Substituted benzamides: Sulpride
• Miscellaneous: Risperidone.
PHENOTHIAZINE COMPOUNDS:
Most widely used compounds in major psychosis.
MECHANISM OF ACTION:
• Phenolhiazines and other antipsychotics produce beneficial effects on three
major
integrating systems of the brain.
1. Mesolimbic system
• Mcso cortical system
2. Hypothalamus.
• These drup may cause
1. Blockade of mainly the post synaptic dopaminergic (02)
receptors and to a
smaller extent on 5-HT receptors.
2. Modify the functions of mesolimbic system.
3. Reduce the incoming stimuli by acting on brain stem reticular fonnat
ion.
• The therapeutic efficacy of antipsychotics is related to ability to
bind and block the
dopaminc:rgic D2 receptors in mesolimbic system,
• Blockade of dopamine action in .corpus striatum is responsible for
extrapyramidal
symptoms often as~a tcd with antip~ychotic df:1gs.
PHARMACOLOGICAL ACTIONS: . ·
t. Behavioural and CNS actions:
• Oilorpromazine administered to ·nom1al monkey, the animal loses
its
IIBlessiveness and interest to the surroundings, Shows indifference
in
hlppe ninp around, lack of initiative, not attack ·spontaneously
and sits
aalianlcss.
 ' ri I
11111•11is1cml
~ F,11 ~ tcmpct"•turc regulation, rcspin tory
• Ne, chun!,'<' m thr ,1.1.- ,,1" '4l <'fillnc.,• an,l r.>n~,.
1111'1'}:<'dO, ~

,11,nr,,, wh<'n"'
(. JIii \; 4. C:NS: Ep11l'fl11c "'"'""v111on
"nt,c~ blumng of
'• tl,, tuibanec in
.
t
,t,1<.hyc.rJ,a. c,111.iupu •~·n
paralytu: ileus difficulty in
•
• Chl<>rrn•m.,.inc. 1,1,..,h the C\•n.h11,,,1,~Ia,,.,,1.,11,-c
"'' '"'"5C~. 1
.
c. NI\> mc.,ul
0
· • -
1111
1nictu11tinn. inl,ibitton of c1acul" n, JIO'lura
•
_,v~:- ':'
Ih
ypo
letmo
th.rorn.......,.opa..'11ia, aplastic
. ,v
i•S)-Ch<"11111or sluwt'. 1!• ulocyl oSIJ, ~ r
• In paltm ls 1nth mo,,v pJ~,-h.,,i, ;1 pn'Cluo.-cs ·
S. llacrnnro1cttc Ny,tcm and 1· - Auran
an~kly, wi1hout ctTcctrnl! (. . . . I.I cc gabctorrhoea.
cm.11i,,n;,J '/UCSthlmn~ J,nunufl<>n of • .
011ucm1a. intra h~tic obstruc:hvc 1aunJ,cc.Gynocc:oma.slia. UTlpo1m '
wal:.-fulnC$$.
. . \.1 6. f:11r.locrinc and mc1;,bolic disturbilnc:~:
"
~
c.~,
2. CNS: menstruul irrcgulllrities.
cs ,tntc of c~tukpsy ~f
• Diminuri,,n of SJ'(•nl3oa.,us fflQlor a,1ivity pn>duc
various posture;, and rcrmnn rRF.PARI\ TION AND DOSAGE:
ho.ty and hmhs "hkh arc m,>tlul11tcd into " . . ' \J 2S,SO, I OO mg tablds
1m.rn<>l,1liSC'd fur J'NIM!,'t.'d rcri<>ds.. • Chlorpromazinc hydrochloride tablets: I0,
• P<1tcnliation <>f 3Ction of an:llgcsiC$ drugs. Dose: 25-100mg.
Prolm1i:ation of Phmobatbitonc $1oq,s . • Chlorpromazinc injection 2Smw'ml
-~-~·;
•
• lnducli<>n of slcqi with slow wave J'l3llcm, on EEO.
c- - . ,, Dose: 1/M 2S-50 mg.
ns.
lmpro1'Cll'lfflts of cx,gnith-c a/Id intclkcfu:ll funcrio
~
•
• Shows ;inti emetic actions.
c -~ ' TIIERAPEUTIC USES:
J. ANS; • Treatment of schizophrenia
• Accts as autonomic suppressant. • Manic depressive psychosis
the actions of adrena line
Due 10 alpha adttnc rgic blod:ing :tetion ii blocks • Hutchinson's disease
•
and nor-adrenaline.
c· .. -,> • Anticmctic
• Ccntn l depressant action on hypothal:1111us. c_l('u • Anti-hiccup.
■ \I
4. C\'S:
~ .- ."
t.:d prcssor rcflcltes, it cau$CS DRUG JNTERACTIONS;
• Due to the inhibi tion of cmtn lly mcdia C dep r=t effects.
ngs lhe CNS
orthosl3tic bypotmsion 's ml txhycardia in elders
. • Barbiturates, morphine, pethidine, alcohol will prolo
'".-'---"~
• Dilates the blood vessel's directly. • MAOI precipitates bizarre reactions
blunting of Twaves in ECG. olcnsive action.
• It C3LISC$ prolooAAlion of QT-interval and • Gu1111ethidine, clonidine causes neutralisation ofhyp
(;'
S. H)'poth3lamic and Endocrine systcmi:
in the pharmacology of caffr lnc.
.---- ~
ion. produces amenorrhoea,
• It m!uccs oestrus cycles, bloclcs ovulat
•
galactorrhoea due to increase in serum prolactin
It blocks rhc release of Growth Hormones.
levels.
~ - _,
2. Define CNS stimulants. Classify them. Expla
Ans: CNS STJMUI.ANTS
~c--_,,,··-.)3,
• RcdUl.u libido in men.
(;'
• The drugs thnt will stimulate CNS are called
as CNS stimulants.
ng up those who have been
ADME; • They are called a~ Analeptics which means picki
of administration.
cast down.
• Well absorbed thruugh oral and pan:nh:ral routes ratory centre.
local irrit.:llion. • Analcptics will stimulate CNS particularly respi
• When administered dlrough 1/M route causes
• Distriburcd in all body tissues. CLASSIFICATION:
onidc conjugation. Sulphonalion,
• Mc1abolised in the liver by hydroxylation, glucur
dcmethyl:ition. I. Those acting directly on the CNS:
alkaloids, amphetam ine,
A. Predominantly cortical stimulants: Xanthine
ADVERSE EFFECTS:
mcthylampbetamine, pipradrol.
t dcnnalilis. rurcly yellowish brown or Picrotoxin, pentylenetetrazol,
I. Intolerance: J>holoJC11Silivlty reactions, contac B. Predominantly mcdullary stimulants :
rmenl, nc:11r blindness.
purple discolour.Ilion of exposed sltin. Visual impai camphor, carbon dioxi de, nikethamide.
tmnors, aldncsia, rigidity, excessive
2. Extrapyrmnidal efftcts of partinsonisn1 like
salivation.
C. Predominantly spinal stimulants: Strychnine.
onium, veratrium,
J. Bcba~iollllll changes: drowsiness, impaired
psychomotor functi on, restlessness. 2. Those which stimulate CNS renexly: l.obetine, amm
excitement, psychotic reactions. confusional states
. nicotine.
 Xnnc hinc a lk11loi ds: Caffe ine, thC'Oph, lllnc-,
• \\'hen 1rca1c J w ith ni1nc ac iJ -
• X a nthos - yellow in Gn-ek . ·
n·II,",.
chc-oh1·.. mlnc-
n.·i-iJuc. ·

_, -.
-=--
C ~ - ••
C. IJ!.
r~...
C. FIi IJ
C. Mil \1

, ~,:
~-~
A . 111•:Al tT: S1imu l;in1 action on myocardium
ralc, force of c<intr:1t-tir,n, myoc,mlllll oxyge n con~
umptl on. .
• L,,rgc do.'ie!I ur caffeine cau'4.: palp_itations, tachyc

th
~how, ; incr~-.e in c heart
.
ardia'. cardiac
rdium .
n - C':tffdne
,irrythmias and positive chrono1rop1 c effect on myoca
• Coffe e- gri nding lhc seeds ofC':tlT<•a nrnhic C. !II ll
ing of the
nc and :;mall amN!lllS of • Increase in the force or contractions cause,; better empty
..
• Tea - Lea\'c s of Th<.':1 si1wns is - C'nffd
tbco bro mine and throph ylline . c.. PIii \ J heart and venous pressure.
• Coca- Seeds o fTh<'Clhwma eOC<)3· Caffei ne and
thet)b wmine . c.Ill..,, B. DLOOD VF.SS F:LS: Direct action on vascu lar
smooth muscle causes
l\lEC IIAN IS l\l OF ACTION:
C.
,, the peripheral vasodi lation
C
,,
... • It l.lilatcs the coronaries and increases the blood
flow.
.~ ·-•-~--~~.
• l\ kth yl xanthinc.s acts by many ways: • It increases cerebral vascular resisiance by reduc
ing the CSF
I . By inhibiting cyclic nucleotide phosphodie
sterase which prevents
pressure- relief of migraine headache.
the conversion of CAM P to siAM P.
.. • h causes the relaxation of pulmonary arterioles
by reduc ing the
ses the levels of
\\ nen methyl xanlhincs are administered they increa
CAM P.
r spaces.
~ ~
pulmonary arterial pressure.
• II increases the blood pressure by stimulant action
on vasom otor
2. Chan ges in the distribution of calcium in i;tracellula
3. By bloct..;ng adenosine receptors.
,, center.
C ■ -u 6: KIDN EYS: It increases the urinary output.
PnAR \lAC OLO GIC. ~L ACTIONS: C ' ·· Theophy\line> thcobromine> caffeine.
hial smoo th musc les.
I. C~S: Caffe ine posses most significant action
on CNS follow ed by ■ u 7. SMOOTII MUSCLES: Caffe ine relaxes the bronc
pi\oca rpinc and in
1hcophyllioe and theobromine.
C ■---u • It abolis hes the bronc hospa sm by histam ine,
cerebral cortex. C. • • .., anaphylactic shock conditions.
• At threshold doses of caffei ne; it stimulates the 8. VOI. UNTA RY l\lUSCLl!:S: lt streng thens the
contraction and increa se in
.
• In large doses it stimulates the mcdullary cortex the metabolism and fatigue of skeletal muscl
es. lt increases the
• rn toxic doses it causes the convulsions. C. -
--~
•.--~
~ contractility of the diaph ragm.
ne increases mental
2. CER EBR AL COR TEX: In small doses caffei
'" · ·-\)
secretions.
9. MISC ELl.A NEO US: It increa ses the gastric acid
es the reaction time,
alertn ess, delay s fatigue and drowsiness, reduc
~c-11...~
• Dasal metabolic rate is increased.
rencx.
impro ves moto r activity and augm ents conditioned • Thcop hyllin e elevates the plasma renin activity.
• It increa ses the physi cal perfo nnanc e. routes of admin istrat ion.
• In large doses (> 300 to 500 mg) it cause s irritab
jljty, nervousness, ADME: Readily absorbed on oral, rectal and parenteral
(; .)
confu sion of thought, insom nia, heada che, tremors. byllin e, 3% of theob romin e
• A fier absor ption 17¾ of caffei ne, 20¾ of thcop
lsions. (; • . ..>
• In toxic doses it causes focal and generalised convu are bound to plasma prote ins.
c--CI•~.,
vasomotor, and vagal
J . MED ULLA : In large doses it stimulates respiratory, • Metabolised in the liver by methy \ation and oxida
tion.
centres. • Plasm atl /2 is2-1 2 hrs
more in marked
• Caffe ine induced respir atory stimu lation is
~.~
ADVERSE EFFECTS:
indivi duals .
se in the blood deliri um, ringin g of ears,
• Stimu lation of the vasom otor centre cause s increa l. CNS: Confu sion, tremo rs, insom nia, excite ment,
press ure and brady cardia. heada che, tachy pnoca , tachy cardi a, cmesi s, fever.
reflex excitability of spina l pain, hacmatemc sis
4. SPIN AL CORD: In large doses it increases the 2. _GIT: llype racidity, nausea, vomi ting, epigastric
cord.
5. CVS: Thcophylline ha!! more action on CVS.
 ~ fll '\Il
C.
C. . . . \)
card ial puin, h is tem,~d as
3· MI S~E LL AN rOU S: Diz ziness, hypotcnsion , seve re pc1i • Rarely morphine produce,
a S<--n,ic o r anxi<.-ty or fear whic
C. . . \)
tion , con vuls ions , sho ck. Jysphorfa. •
vcn rnc u la r fibr illat ion , deh ydra C. . . \) hine is c:har ecte rised by drowsine ss,
difficulty
• ScJu1ioo n inducccl by the morp
SAG E: hy.
in lhe cionc:cntra1ion and mental apat similar ti tl1osc oblerved during natural
PRE PAR AT ION S ANO DO c.. . . 0
600 mg oral ly • Lurgc doses $lcc-p with EEO changes
I. Caf fc!° e c ilra te : d ose: J20- e: 250 -500 mg. c. . . . v sleep. vag;il and
·.l·lt,
ate amp oule s-25 0mg /ml.: dos oough ccnt cn and stimulut~ the
l . Caf feine and sod ium bc nzo • Deprcs.ses the respiratorY and
C. • \.I oculomotor centres and the CTZ.
Tllf -:IU PEU TIC USES:
re, bronchial c.- . , li C. Respiration:
e depress all phas es of respir31ory
activ ity. It acts
raine, acute lcll ventricular failu
......
• l'hetaJlCUriC doses of morphin
CNS srimulan t. trea tme nt of mig b y:
a s1 h111a , diu reti c, hyp erte ns ion. 1. Direct dcpr,-ssant action on
respir.itory ccnh c and
ation .
inso nism. Explain the phllmlllco
opa.
logy of L-D ased plasma carb on dioxide concentr
J. Clas sify the drugs actin g on
park C
C
,,. 2. R,-ducing ils sen.\itivity to incre
• Causes bronchoconstriction alon
g with the histWT1ine.
C.. -.U
c, breathin g Is cnli rely maintaine
d by hypo xic
Ans: ~ ·' ·
• With the toxic dose s o r mol'phln lls in Cheyna
lain the phannacology of morphine. aort ic chcmoreceptor.1. This rcsu
4. Classify opioid analgesics. Exp
ch relieves rhe pain.
~ -.. driv e mediated by co.ro tid und
stokes respiration. Inhalation of pure
o,i;ygen at this stage aboli shes
the hypoxic
Ans : Analges ics are the drugs whi
•
• Analgesics M C clas.,ilicd ns n arco
rics 1111d non-narcotics.
word opioid refe rs to the prod ucts
obtained from opium
~
•
-- \J
drive and produces apnoea.
D. Pl PILS: produces the characte
ristic pin poin t pupils. Causes mios
is.
on of the ehcmo
0 1'10 11) ANALGESICS; The e produces vomiting by stimulati
F.. Nausea and cmesls: Morphin
•
u
pop py.
• ll1e tcnn opio id rcfors to don
ate all natural, semi-synthetic, synt
morphin i: l ike actions i.e., relie
ves pain and depress ion of CNS
.
hetic drugs which have
otics beca use they induce skep.
C
C
. . _V
rece ptor trigg er zone (CT Z)
vomiting cc:ntre.
F. COUGH SU PRESSIO:-.: Dep

in med ulla. ln larg e dOSC$ morp

resses the cough reflex as a reswt

hine depresses the

of depression or the
.~•"
• The se drugs M C :ilsc called as nan: cough centre. nucleus and cauM.-S
CLA SSI FICAT ION: stimulates the mcdullary vai;al
• G. Vagus sllmut:allon: Morphine
luids: morphine, codeine
I. Natural 1lku bradycardia. Therapeutic doses
~ -~
inc.
acetyl morphine (heroin), Pholcod s rcflcit c1tcitubilily of spinal cord.
..
2. Semi-synthetic opiates: Di H. Spinal rord : Morphine increase
fcntanyl, methadone, tramadol. nt incrcuse in CSF preS\urc.
3. Synthetic opiates: Peth idin e, of morphine may produce II signitico
m and used as sulphate or hydrochl
oride. ~ \)
I. lllis«llaneous: Morphine pmd
uccs a rclcuse of A.OH wilh n:su
ltant ,h:crc11se in
alkaloid of opiu etics in p11tien1s
MORPHINE: It is an important
' ~ urinary output Administratio n
with congestive heart foilurc.
of morphine rcducC11 efficacy or diur
PHARMACO LOGICAL ACl"IO
I . CNS:

NS:
A. A~,UG ESI A: Mo,phinc
produces relie f of pain in a dose that usually docN
not cause
'c· I .l ..) 2. GIT: Morphine induces vigorous
sphincters.
spasm of smooth muscle of hut, ilco
mov ements.

co\ic and anal

• It reduces propulsive peristaltic an,\
■ ·~
arly cvidcnl in the du,>d1,."1lum
'.
mot or in coordination. effect on pin • Spasmogcnic action is pan icul
phine ond its 01111logucs have little
• In the sub DJ111cRfhctic doses mor csscd. large intestine.
1t, pain arisi ng from tissu es is supr <; , ...,
prick sensation and its withdrawn rcllc saliva, gaslric: acid and intcstinul
. g continuous and dull poin.
efTcclivc in rclic·vin • Decrease in the secretio n of
• In moderate doses morphine is
• In Jary crdo scs relie ves shar
• Morpiinc raises the pain thre
p caused by trau ma.
shold and there by rcducipg 1M prec
ipitatioQof C' i:! secretions.
• Desiccation or faeces, abolition
of tbe periSlaltic mov eme nts, 11n·
ofsphincters especially anal sphinct
cn.
ration or morphine should rccci
poin.
al reaction to pain.
• Patients on long tcnn administ
• Morphine produces the emotion high fibre diet and laxative such
as Senna regularly.
nosis: prcssun: by prod ucin g a spnsi
13. Eup hor ia. Scd11tfon and hyp euphoria • Morphine increases the intra biliary
e produces a sense of well being-
• With therapculic do11c:s morphin and aid11 the of sphincter of oddi.
ic withdraw! ad nighl n:sponsc
• Euphoria cfiminutcs fc:ar, p,rn
ana lges ic nction of morphine
 ,-
..
' I . ' I
(. . . lj
' I • ,r U1L-n>9 n111I
(. 1111 ·_.
ti ,oun •nal~~le, ..,,b11vc and euphurie
J . O • h r-r sn,oof h n1u.uln: ~-1,,,1,h1nC' r"~hh"'C'$ 1111 •""~'(' m I K" h'llt. '
d,·INS<•r musdc of l>l•ld,..-. The , '"'"'"' ,phin,-irr •~ ,,,.11111~1cJ. II nl:-<• l'""luccs "" (. " • 1 n lcrunca developed 10 rc,p1r,afut Y c-pre> •
111crc.1'<<" in the ton,• o(hmn.-h, an,I hl\,t'k'h1<1lc,<,
-1. C\'S: thernpcuric Jo.<elt ,,( m<'r)'h111c, hmvc n,·i:ligil>lc ,·ff•"'"" the tn),,.,nnlium, hi,><
,<I
C. . . ~ c ffccls of morphlnc.
h , ,h 1 ,v.1nc:, • MAO 1nh1b11ors,
01wc; trrn :kAC.TIONS: CNS dcprC'.\~:tnlS, P """
pn:ssurc nnd heart ntc. Mufl'h1nt' """''"-cs di lllth>n of rc,n11hcrnl "'"°'I wssds C. . . V ..., • rrecu
lricyclic ontidcprcssanrs enhance the _..auvc"'
nf mofl)hine.
p:trticul:irly culMcoUS M,-..,J ,..,,...,15, T,"ic J,,_...::s produces hyr<>tcnsiun.
5. .' IELIRO ENDOC Rll\"t-: .!-\ .STT.\i: 111<'fl'hine acts in the h~1X•tholo1nus onrl inhibits C. . . \J
TIIERAPl,:UTI C ust:S:
rile rclc3SC ofGnR II at>d CRH. h d"-ttASCS the con..'Clllrntio~ off-SH, Lit. 1\CTII. II c.. • \)
increases the pla.<mm nin......-ntr:ltion o( probctin.
ofinfections.

. ..
6. li\li\lUNE SYSTEIII: Ir suprc,<><'S the immune fun-,1ion.• and incrcnsc the sus-,cpubihty
7. 1\1£TA0OLISM: it m:!u,'CS the m<'l3bolic rJtc when there is slight fall in rcmpcr~ture.
It reduocs the re,;pir:110,y rntc. musculo.r activity 11nd periphc.-al vaso<lilotion.
C.
C • \J
'>
•
•
•
•
•

Relief of pnin.
In the trcatmcnl of acule ventriculur failure.
Scd11tion and alcq,.
As o pre anoesrhe11c medication.
Produces constipation
.
C • -·~ , • As II anaesthetic
AD.\IE:
C - -~.
• Given omlly. morphine is absorbed. Bioav11ilubility oforJI od01inistr11tion is
2~0•~- Ir also be administered rectally. Given subcutaneously produces
~ · ·'.:
-,
S mark$.
I. F.xplain In detail about opioid antagonists . . .
wialgcsic emu ..;th in I S-20 min and reaches pc:3lc plasma concentration f" t; Ans: Toe drugs that antagonises the cffcctS of morphine and other op101d analgesics
60-90 min. Gi,-en intra\'enously produces immediate effect. .
• Circulates in the plasma partly bound 10 plasma proteins 1111d partly in C • :u and act by competitive antagonism arc opioid anragonislS.
They arc clas3ifk-d GS
free fonn. c ■~ a. Pure antagonists : oaloxone, naltrexone.
b. Partial agonisL<: of nalorphim: type: nnlorphine. levcll11Tl'han.
• It crossc::s lhe placenl:il barrier readily and secreted in the milk.
!'.·felabolised in the liver
C ■ ·u c. Partiul agonists of morphine type: propinom& profodal.
c ■~
•
• Plasma t l/2 is 2hn.. NALAXONE: N-Allyl analogue of oxymorphone - pure antagonist.
c ■u
.-\i
• Excn,ted through urine.
• It an111goniscs the respiratory dcpress.i.nt action of morphine nnd othCT opioids.
PREPARATIO NS A.'11D DOSAGE: • (liven orally, only 1/50 as potent when given pnrcntrally.
C • 1mg given IN sly hlocks the effects of25mg of heroin.
• Tincture of opiu~ydrochl oric solution- I O"/o0piwn I I ¾morphine. Dose: 0.3-2ml.
C" • •." • Completely metabolised in the liver.
• Cblorodyne- chloroform and m orphine tincture contains 0.0229o/oof morp.hine
• Available in 1ml vials containing 0.4mglml.
hydrochloride. Dose; 0.J-0.6ml. C" . -~ • Drug of choice in opioid poisoning.
..-.ll
• Morphine solutions: Dosc-10-JOmg.
• Administered as 1/V bolus in a doi.e of0.8-2.0mg every 2-3min to the maximum
• Morphine hydrochloride stdphote solution : Dose: I 0-20rng SIC or 1/ M . ·.:,
C · dose of 10mg.
ADVERSE EFFECTS:
•

• Intolerance: Tiierapeuric doses causes tremors :ind delirium. Olhcr effects include
allergic skin rashes, pruritis, dermolitis.
CNS; Dysphoria, mental clouding, vertigo, n3useo and vomiting, headache and

C
C
cl~
-~ •
•
IN dose in children is \Omeglkg.
Naloxone injected 1/V reported to oorrect the hypotension observed in shock.
NALARPIUNI!:: N-Allyl nor morphine.
■-,
• Semisynthctic congcm,T of morphine.
fatigue.
C • Used mainly in the treatment of acute morphine poisoning.
• Rc.q,iralory dcprc:ssion in small dose,.
~-:•"'.,°
• By itself acts as parti11\ agonist, produces analgt.-sia and respiratory depression.
• Consllpatfoa: abdominal distension :ind increased pressure in hilinry tract.
llypotension: i.s due lo peripheral vasodilalion.
C ,4 • When adminislcrcd along with morphine it displaces the morphine from the receptor
•
site reversing the morphine action.
• Urim11y n:tcntion.
• On the foelus: during pregnancy cau.!1,-s depression of foetal respirarion. PIIAR'.\1ACOLOGICAL ACTIONS:
Tolerance: Repeated ad111inis1ra1ion of morphine develops rolerance.
•
~-.a:! 1. When administered without prior medlc:ation with marphine:
.\l
-I
• IJ
.
•
• u
•
I '-'

"U
,,
\I
•

•
•
•

AOH'. NSf,. Ht:C-T'lt

.,...,,c,,.
M Ii.i> ►' Hf.C- I 'I 1,,11 ,,..,.., 11,.,...,,..,,., "'"~•a. mu..:ulat "'""
Allt'fj(ft rc:JKhon,, hlurrcd ._,,.,,.-.. 11J+1c,"or1~. p,lyun•
I.ARC.~ l>OS ►'.S cc,ebt-llor ala.,•. q,,lq,<•f''"" 1e1rutes, hyp<~cn,11X>.~ ECG
(,'IIHONIC AOM INISTRA'TION 19,11te l•-'"""1""'· hypolh yro,d,sm.
1
ch nngn. cardio•....:ular, renal, bt;1.1n J.un• S,: Reversible """'"'~"
EI\TIIHVOTOXKITY; Emhryr,lu ~ic. tnae.»e in the: ruk or ~~ns anoma y

k ~ • ucmon
.
1
.

•
Ul
foc1us.
I ti •
TllEHAPlc:UTIC USES:
To prevent recurrence of mania and depressive c:pt,....Jo tn bipolar di:loOfdcts.
I t• • To trc.11 acute episodes of mania
,~
.I t • To trc::11 alcohol dcpc1ldcnce.
DRUG INTERACTIONS: .
It • When a,dministcrcd along with phenothiazincs increa.sc:s I.he risk o f c:xtrapyramidal
•
effects.
\\lbcn administ~-rcd along with lhiazide or loop diurt:tics it =
the: IMS of sodiwn
1 .. and im:reases the chloride levds.
,.,
/u
•
•
•

When administered along with NSAIDS reduces the renal clear.mce o flithium..
Lilltlum induces the insulin induced hypoglycaerniil-
DOSE:
Lithium carbonate dose: 600mg thrice daily
~ • Maintenance dosc-300-400mg ,...,;ce daily.
u •
3. E.xplain, the pharmacology of tricyclic antidepnssanu OR imipramine.
l u
Ans: ll\TTPRAM INE: A di benzazcpine dcri\'ativc.
-U
MECHANISl\1 OF ACTION:
~ \)
• The drugs that modify depression or mania have distinct effects on metabolism
~ of S-HT, noradrenaline and dopamine.
• N'onna!ly, a large proportion of S-HT /Noradrenaline liberated at nerve ending.s
~
on its storage sit<.'S.
....) • Tricyclic antidepressants
Arc the potent inhibitors of neuronal nor adrenaline and 5-ITT
r.J rcuptake in brain causing an increase in noradn.'tla\ine and 5-HT in
.._, the synaptic cleft.
Variable blockage of u1 and ll!Ss extent to a,z adrcnergic receptors.
"
• PHARMACOLOGICAL ACTIONS:
• Anti- cholinergic properties.
• Behavioural effects; It produces anli -depressant clTect like I~\ I PRAMlNE: A di ben1-az.cpine
•
I

derivative.
MECHANISM OF ACTION:
• • The drugs that modify depression or mania have distinct clT~cts on metabolisr
of5-HT. noradrenaline and dopamine.
••
 f:
(
.,.. \,)
cf\'C c11tll••t!" C. - ,.
'\ I •1111
• Non11ully. a 1-lrt:c rn,,,,rth ,n ,,r ~•ltT N,1n1,h'-"nnlmr hl't.._·nh. ·111 ~:MAl'l-:U l'IC U!'.t.S:
on irs sh.1mgc ~1tc-$~
I ~-1Ir
C. 1111 v • Mental 1kprc:,.,.,n
• Tnc)"l, c nn1iJ,1>!'<'!<-<.1m~
• Art' the J"<)l~\I 111h1bih•t'!C ,,r n,·un•nal nor n,hcn:11il an~_,,
lC r In C. , . v • Acute pnnic attncka,
n.• uprak<' ,n l>t·ain c,..1.,i1t1t an in.."ff'ILSC in 1111r:><ln.~t11l11
1c nml
~ JIii ll • nocturnal encurii,
bulirnia ncrvosa- ovcrutin g
C..
the nn:1rc1c ckft. •
, l1
Vnn~bl e 1,1.,.,i..ai;c of a , and k-ss '"tent 10 u, BJrcncrg ic receptor$ C. • • Deaffcrenlalton pain
C.
Anti• cholincr gic pn'P"f11 cs. • Chronic fatigue syndrom e
V
nin reuptak c inhibito rs.
PH.-\ Ri, L.\COL OGI CAL ACTIO ~S: C t1 4. Ell plain che pharma colo,:y orSell~ cline or selec1lv e seroto
MA OI re
~-rse the
C.•.
.
hkc
I. lkba, iour»I df'ttts: It pn>duces anti -d41>n:s:s:ant dfttt t1 Ans: SEl,EC TIVE SERAT ONIN REUPT AKE t::'iHIB ITORS
ines.
d,1 n·cs..•ant acnon of r"C:Scrpine "ithout restorin g br:rin monmuu
2. CNS: C • t1 Eg: Fluoxetine, llouxamine, ~-rtraline.
light headed
o I 00 mg in normal subjects causes drowsiness. feeling of t, • Selectively inhibit S-HT reupt.lke.
nc::ss. D,•gree of sNbtion enhance s the sleep. '
o Lem O'S the threshold of seizures.
. difficulty in
~ C • • t. Advant11ges:
o R~:1tc d administration of the drug cau.~cs sedntion effects li'kc bradyca rdia.
roncentr:1tion, thinking.
blurred ,-ision.
~. t: • Less rnuscorinic effects, less sedation . fewer cardiov ascular
hypoh.-nsion.
3. A,-.s: Anti ch9linergic effects like dryness of mouth, ooostipation, C .. U
■. u
palpitation. Al>ME:
ADM"E :
C
C \
■ _u •
•
Well absorbed or.11ly
Metabolised and eliminated slowly
• Given orally, well absorbe d.
with plasma proteins. ~ ■ -u
\
~."
• HisJily lipopbilic distribu ted in all tissues by strongly binding Al>VER SE EFFEC TS;
amim:.
• Convert ed in the liver to its active metabolite clc:smcthylimipr <;. • 4'., • Nausea, vomitin g, bitterness, insomn in, headach e, erectile
dysfunc tion. decreas e in
un dia~s cd bipolar
libido, decreas e in sexual thought and desire, mania with
~.
• Metabolised in liver and kidneys .
depression.
ADV.ERSE EFFEC TS: on, insomn ia, sweatin g,
• It causes with drawl symptom s like anxiety, agitatio n, confusi
I. ,\JJergk effects; urticaria, skin rashes, pruritis, pholoscnsitivity
. c;;- • " tremor, shock li'ke symlrome. _
.-
C. ~
accommodation, tachycardia.
2. Anlimu.scarinlc effects; Dryness of mouth, difficul ty in \) • Autono mic sympto ms like nausea, salivati on, diarrho ea,
abdomi nal pain, flushed skit
ejaculation, rnrcly
difficuh y in micturi tion. impotence, constipation, delayed
hyperpy rcxia, glaucom a, enJargc d prostr-dlC. ~ •
hypenh cnnia.
Neurom uscular symptom:; like hyperre flcllia, shiverin g, twitchin
g, rigidity .
, tremors , muscle jerking.~,
3. CNS: feel ing of tirednes s, lethargy, headache, sedation
ataxia, hypel1hcnnia, confusi on, psychosis.
~ THERAPEUTIC USES:
4. CVS: PosturaJ hypoten sion. cardiom yopathy , heart
failure, inverted or flattened T
cardiac arrythmias, heart C ■. ,:> • Manic phase of dipolar depress ion
wave, prol()ngation of QT interval , depress ed ST segment,
CI"'
failure.
5. J\Jlscellaneous: Cholest atic jaundic e, agranul ocytosis , edema,
peronea l palsies.
6. Acute poisoni ng: hyperpy rexia, hypertension, convulsions,

unilateral and bilulcro\

coma, metabol ic acidosis.
C. c ■ 3
'l
•
•
Obsessi ve compul sive disorde r
High risk of suicide.
PREPA RATlcO NS AND DOSAG F.;
upto 20mg once in several v
-3 Flouxet ine 20mg once a day in the mornin g, in crease the dose
.
ORI.JG fNTER ACTIO ~S : maximu m dose: 80mg daily.
tions. C •
MAOJ enhance s the effects ofphcnothiazin es and thyroid prcpnni
•
c• 3 S. Explain the pbarmJ11col~ of halluci nogens .
•
• Hyperte nsive effect o f guancth idine and ITI\.'Camylamine are
reverse d
It polcnl iates the nclions c,fNora drenalin e, adrenaline and phenyic
phrinc.
-~ Ans: HALLU CINOG ENS OR PSVC HOGE NETIC AGEN
TS.
~ -
 ( _,..
.. I
C ,. . v
• Tii.-:<c urr the Jru~ "1,,.,1, ore cor,1hlr '1f 1•1\,;t11~ing 1'Syd1M
1s, . 'k
,. 5 ·ho<1s h C
c. r11 ..
•
TI IC ,.llil'C'IS"""'"'-"C\'
hy 1h,s drug arc =•~nhhng 11~ rm-c,~ "' 1' )" •
C. 1111 ·" 'rA<:IONP.:
schmiphxnio. Jo 1h,·y ArC cJll,-d AS 1'S)'\'h11111imc1ic. • t'c:ntnlly acting ch<,llm:,icr.s.'IC mh1bi11, r
n.< h•lludnogc11s.
• ThC$c drui;s rrc>Ju,'t' holludn31i<'tt< ~ thc)' Arc c;illcJ C. ... " • It er1h111C(:S chotlnergic tru11,mission in the bnnn.
C l .ASSI FICATIO'II: g. abdominal CTlUJlJ» ,
C. ,. . li • Hut il Is shon acting causes sicJc c1Tcct$ lik.: n.su,iea. vumitin
I. lmi11le deri,•31ives such 3S 1)-scri;ic acill llicrhylnmidc. psilochy
2. Non-inoolic dmvat l\~ MCSOllinc, C;Utnabis.
L YSERG IC AC'ID DI ETll\' L AMIDE :

nc, buf,,1cnlnc
c• vu •
dimho u and hcpatoroxicity.
The newer agents like riva,ligminc, doncpczil. ore better tolctalt
Sclccth·e ccnltal ooticholinestcrascs do not Cllu.se cffccU on
d wi1h side cffcctS.
GIT which arc due to
C.
C. • •
• It is an amine all3foid s}nthcsisoo from crgot. peripheral cholincrgic activity.
C , . lJ
C.
• R<'SCl!tblcs n-gut:uninc so it shows oxytocic property. TI1ey increase acctylcholinc levels in the neurons and produce
good 11:Sponscs.
J\JECIIA \1S1\1 OF ACTION: li •
They lltC DOI lk.-p;itotoxic and arc long acting.
C. ',
~
•
• It blocks pairha al actions of S-HT. Ptcpnrntious: Rivllllligmine- I.S-6mg bd capsules. Donc-.r.~1>il-Sm
g capsules.
• 2-Bromo lyscrgic acid and methyscrgidc nn, powerful
untagonists of 5-HT 0nd li •
I\IEMANTINE
produces negligib le psychomimctic effects. NMDA receptor antagonist useful in p:iricnts with moderate
to severe alzlteilllcn
•
C.
PHARMACOLOGICA L ACTIO NS:
R3pidly absorbed on oral Ddministration ond produces aelions
ot low doses 20- ~ a ··t' disease.
C.
• • Blocks the glutwnalc induced cxotoxicity.
2Smicrogmms.
• lndividunl with LSD shows marked changes in mood imd
emotional oUlbursts. t. • Adverse effects include di.r.zinc:IS IWd headache.
• Used in moderate to severe Al1hcim,:r's disease.
C\'aluation and judgement.
• Blocking effect on perfom1ancc in various 1cst$ designed for ~J • St:11led with Smg OD and increased to I0mg BD.
• S)'fflpath()l11immctic octions include dilolion of pupil,
tachycardia. cremors,
c -■ u • NSAIDS : Small doses of aspirin is used..
piloercction, hypcrglyc,:mia.
ADVERSE F.Fn:crs:
."
c ■"
.".
• Varies from six,-cics to spL•dcs. 7. Write a note on opioid receptors.
• In animals ii causes dc:uh due tu n:spi,atory failure. (;
~
lily chang~-s, chromosomal Ans: OPIOID RECEPTORS:
• In man it causes suicidal tcndencie.~. psychos is, pcrsona
ing with specific receptors
damage. • Morr>him: and och,-r (lpioids c,cert their action by intcruct
DRUG INTERACTIONS: "I u present in lhe neurons in the CNS and peripheral tissues.
• Pht'JIOthiazincs like chlorpromazinc an1agonises the clTcds of LSD
Reserpine potcntialcs the elfeels of LSD.
~ " I. p rectpton:
• It is churactcrist-d by its high affinity for morphine.
c;. "
C.
•
I &2 wtiich a«: found in the:
• Endogt.11ous ligands of the µ r<-ccptM are endomorphins
m:uumolian brain.
\l dynorphins binds to 11
6, Explai n in dt111l about the drugs actiug on AM1el111crs
distHC ,
Other opioid peptides like beta endorphins, enkCJ!halins and
•
c; • ,_) rctl-p:ors with low affinity.
Ans: DRUGS ACTING ON ALZHIEJ\JERS DISEASE. matter, thalamus, nucleus
c; • .,_, • lligh density of µ rcceplors has been detected in gray
erised by impaim1e111 of solitarius, nucleus ambigus.
• Alzheimer's disease is a neurodcgencrutive disorder charact
memory and cognitive functions.
• Other symptoms include depression, anxiety, disturlx.'11 sleep.
loss of ncuruns mainly
c-1" · ?,
• Two types of 11 receptors arc
µ, reccptoQ: Higher affinity to morphine
• 1'111hological features include atrophy of ccrdnal cortc.l and Mediates supraspinal analgesia
c· • Blocked by nalaxanazinc.
cholincrgic neurons in die br.iin. . • :. 3
C 112rcx:c11tors: lower 111linity for morphi ne.
• DRUGS:
I. Choline csterasc inhibitors: Rivosligminc, 1acrinc, doncpc
zil.
t=· • "° Mediates spinal analgesia, respiratory and coll'Stipation.
2. K rc:ccp10,~: This receptor has ltii;h nffinily for kctocycl11zocii
1e and dynorphin A.
2. Noocropic agcnls: pi111cctam, 11Piracctam.
3. NMDA antagonists; Mcmantine
4. Others: riribcdil, ginkgo biloba.
~!: Norbiru1ltrophinaminc is a sdcclivc antagoo ist.
Two sub types arc-Ki and KJ.
Kt mcdiatC11 spinal analgesia
"() §.~
.... _
-I
- .7 7' ~-
r
'JI ii
~
.-:
l<J me di ate s su pr as pi
3. c5 re ce pt or s: M ed
Hi gh af fin ity for en ke
na l analgesia.
ia te s sp in al an alg es ia.
.
ph ali ns
r_,
r. ,
I' ..
•,
I
No rtr in do le is a selec
tiv e an tag on ist I
' . r

' .., I
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