Kartela Farmakologia II

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12

12

12

. 12 1g.
12 ,
12 .
(). "
" (
).
12 + " " + , 12 .
( )
12
( ).
, , Crohn,
.
.
12. 12
.

, ,
.

.
12,
12
( ...).
2-3 .

. , 12 .
. , .
. .
. 1mg 2-3
5 . 1mg 3 .
1mg 3
.

(Lidocaine, lignocaine)

.
. :
Purkinje
,
.
. .
. /2 . /2 7-8
.

,

5-10 . O /2 1-2 .
(70% ) (
MEGX GX)
.
. ( , ,
), ( ).
.

Adams-Stokes,

Wolff-Parkinson-White,


().
.

. >5mcg/ml,
, , , , ,

, .

9mcg/ml ,

. .
() .
. , ,
, , , .

,


.
. , ,
.
. .
( ) .
. 1mg/kg 25-50mg/ ,
5 . 200-300mg.
14mg/ .

(.. ) 200-300mg
10% . 1mg/kg
30mcg/kg/. 1-2g
1 5% ( 500ml
) . Xylocaine.
( ).

(Gluceryl trinitrate, nitroglycerin)

cGMP.

c-GMP
. (
.)


.
. , .

. /2 3 .
.

.
. ( ), ,
( ), (
), Raynaud. ,

,

.
.
. , ,
, , .
. (50%
) , ,
( ),
, , (
, , ).
. , .

.
.

6 .

. .
(Viagra)
.
, , .
(, , ..)
.
( ). .
. ( ) 0,3-1mg
1-3 30-60 .
5-20mcg/ (crescendo)
.
2,6-6,4mg 2-4 / .
0,1 0,8mg/ 1
( , ) 12 . 2,5-5cm
( ) 4-8
. Nitrolingual spray, inj. Nitrong tabl .., Minitran, Nitro-Dur, Transiderm-Nitro
patches ..

(Nifedipine)

(Prizmental ),

Raynaud,
. ,
. -.
90%.
:
. L ,
. .
. , shock, .
. O , , (
), (), ,

(, , , ,
..), (, , ), (,
..), , , , , ,
, , ,
( -).
1 ,
.
( ) .
.
. , , ,
, , .
( 30 ) .
. H ( )
.

.

CYP3A4 .
.
,

. .
. ,
.
.
. Raynaud 5-20mg 3/ .
( )
. 20mg 2/
.
.

5,

10,

20mg.

10, 20mg 20mg. 100 g/ml


. Adalat, Glopir, Coracten tabl, caps

(Heparin)

standard (

.. 3.000-30.000 Da), , - .
.
, ,
, , , , ()
.
(...)

4.000-6.000 Da.

... ,
( 12 ). a
,
+ ( + 5-) (
), standard
18 ,
.. ,
a.
(H-5) + = ( )
(... H-5) + = ( )
( )

a =

(H- +5) + = ( )
( ) + =
(... H-5) + = ( )
( )

= -

10

... :
( standard
), (
), 4 (2-3
), 1-2 (..
, ).
, () -Xa .
APTT ( ) .
, ...

.

.
( ).
. /2
30 1,5 .
APTT ( ).
E. ,
, (bypass),
, ,
, .
. , ,
, , , .
. ( 10%)
,

, ,

. .
.
(1mg 100 ,
50mg). (
)
, (, , ,
NSAID, ), .
.

(, , ..), .
.

standard (heparin-induced

thrombocytopenia HIT), ,
, .

11

5 .

150.000/mm3

IgG
4, Fc
.
.
Bivalirudin
GP IIb/IIIa.
. , NSAID,
.
.
5 . (<100.000) .
( )
. , . .
... . .
(enoxaparin)
.
()
, , .

in

vitro

.
. mg.
. 5.000
15.000 /12 ( 20.000
/m2 ) 0,9% NaCl ( )
APTT ( ) KCCT (
-). APTT KCCT 4-6
1,5-2,5 .
5.000 8-12

.
().
1 ( , ).
.

5.000 25.000/ml

(Heparin/Leo) 5.000 , 25.000/ml (Calciparine).


2.000, 2.500, 3.500, 5.000, 10.000
25.000 . ( Clexane, Fraxiparine, Innohep, Logiparin, Fragmin ..)

12

(Warfarin)

36-48 . .
,

. .


,
,
,
.
, , ,
,
, ,

, , ,

.

. , ,
, , , ,
(
/ ).
C V VIII,
. (
, C,
S, C Va
VIIIa. C, 1-).
() 5mg
, , VII.
>50

13

.
( ), .
.
( , ),
(, , ,
, , ..),
(, , , , ,
, ..), , ,
, , , , NSAID,
..

(, ), , ,
..
NSAID .
. , , (
VIII).
.
.
. (Panwarfin tabl.) 10mg/ 2
(PT)
1 .
PT 2-2,5
3-4 ( ,
, ).

PT (.. 10-15

) 2 2,
8 . 39mg/.
:
<65 * INR 2,0-3,0

65-75 INR 2,0-3,0



>75 INR 2,0-3,0
* : , ,
, , , .

14

(Furosemide frusemide)

. NaCl
Henle. 0,5-1 30 .
(
). /2 2 .
, ( ,
), , ,
( ).

, ,

, , , ,
, , . , , , ,
.
. . .
.
.
( , , - ),
,
, , ,
, ,
, .
.
. , o
. , 3 4.
. 20-80mg 1-2/.
. () 20-40mg
500mg 4mg/. (spray)
2 30-60 . Lasix

15

(Enalapril)


. .

.

.
,
.
.
, , , ,

, ,
. (
) ( 1:1000,
0,3-0,5ml ).

(0,9% NaCl) 000,8-1,2 mg.
. To
.
.
(
, 2,5mg),
.

NSAIDs .
.
.
.
( ..) .
2,5mg 10-20mg/. Renitec tabl.
16


Hsp90 (heat shock
protein). ,
(Hsp90) -
DNA
( , GRE) -.
(..
, A2 ..) .
(),

( ), ,

().
( ,
o, , , ),
, , , ,
, T4 T3
TSH. .
,

/2 .


25
20
5
5
4
4
0,75
0,75
2

/2 ()
90
30
60
120-200
80-180
250+
300
100-200+
200

"

"
"
"
"

45-80%), 90%,


.
.

17


( ) .

( , , ).

(
), , , .
, ,

.. .
. 12, ,
, , .
. , , (
), , ,
( ), ,
, , .
Cushing*, ,
( >15mg/ ),
( ), ( ,
).
.
,

( ,

, , , ..).
, ,
24, /2 .
-
.

1mg

, ,
24 . ' ,
9.00 . (
).

.
. .
,
, ,
. '

18

,
3-10 . .

.
, , , ,
, , , .
. .
. (, ...), ,

.
(, ) ( 2 ), (
).
.
.
.

19

(Ranitidine)

, 2-.
2-
. 5-10 .
(50%)
1-2hr .
. 25%
. ,
. 1/2 2hr.

12, , Zollinger-

Ellison, .

, ,

.
.
(3%). (<1%), , , , , , .

, , , ,
, , -GT .
, , .
.
.

.
. 150mg 2
300mg 4-8 .
150mg .

Zollinger-Ellison 150mg 3 (
900mg/24). 2-4mg/kg/ 300mg/.
150mg 150mg/6.
150mg 2 (
50mg 40-60 ). . 50mg/6-8
. 25mg/ 2 6-8
. Zantac tabl 150mg, 300mg, inj 25mg/ml. Baroxal tabl 150mg. Ptinolin tabl 150mg ..

20

(Omeprazole)

H pH .
30-40% .
( 70%) . /2 0,5-1
,
/2 3 .
3 .
.

12,

, Zollinger-Ellison, NSAID,
.
. .

, , , , ,
, , .
( ). ,
. .
.
( C) , , , ( ).
. pH

, , , , 12,
, ).
P450.
, , , , tacrolimus.
. , 20mg/ 8
12 4 . 20mg
4 4 .

Zollinger Ellison 20-120mg/24 . >80mg

, -. 1/2 .
Losec tabl, inj.

21

(Loperamide)

.

.
( 40%) . /2 11 .
( )
.
. , 38oC.
, <2 .
.
, , ,
(, )

. ,

) .
. , . .
. .
.
. 4mg (2 ) 2mg (1 )
16mg ( 812mg). 48 .
4-8 1mg X 4/.
2-4mg X 2/ . Imodium caps.

22

(Ampicillin)

. . Gram+
Gram-. - .
. Gram +/-.
. , ,
, (
) Gram+.
, 50% 10-15%
.
.
H. Influenzae .

.
, .
.
(sulbactam) ,
, (bacteroides fragilis)

.
.
. .
. , ,
(

AIDS),
. .
. .
. .
. .
. /2 .

23

. .
1 2 .
.
.
.
. . 500mg-1g X 3-4/. 50-150mg/kg/
3-4 .
Caps, syrup, susp, inj Pentrexyl, Ampicipen ..

24

(Cefuroxime)


. ,
vulgaris,
(, ,
).
.
. (cefuroxime axetil)
. .
/2 80 .

.
6.
, , , . .
.
.
. (cefuroxime axetil) 125-250mg X 2/. ZInnat tabl
750mg-1,5g X 3-4/. 20-30mg X 2-3/. Zinacef inj.

25


, , , ,
, , , . , .
. , 30S
.
.
.

(, , ),
30S ,
-
30S .
. . <10%.
,
. ,
, . /2
5-10

. T/2 2-3 .

8 .
.
7 .
.

Gram+/-, . ,



. .
-.
.

, , Gravis,

( ).
. :
. . . H
. ,
, , .

.
.
.

26

(
), (
), () .
:

. .
( )

( ).

.
,
, .
:

= =

.
:
= = =

. . Ca++
.
.
, .
.
,

, , ,
, , ()
. (
).
(
). 50% 4-6
.
.
7
, , .
1

. ()

27

6-10mg/L 20-40mg/L
. .
. <6
. , .
.

, , ,
, , , , ,
, .
,
.

.

:
. .
. ( ).
. .
+ 50% ( ).

28

(Chloramphenicol)

Gram+/- ,

, , , .

.
( ) .
. 50S ( )
( ).

, .
. 75-90%

( 50-90% ).

60%. . /2 4
. ,
30% . 7090%.
. ( ), (
)
.
. .
.
2
. , >20gr >50mg/kg/,

,
. 1:25.000-40.000 .
.
.
(
) .
75 g/ml : ,

29

, , ,
, , ( 40% ).
(,
Herxheimer*),

, ().
.

(, , ..).
.
G6PD. , .
.

.
. p450
, , ,
.
.
.
.
.
.
. 250mg X 4/. 25mg/kg/.
.
30mg/kg/ >50mg/kg/. Kemicetin inj. caps.

30

(Erythromycin)

.
.
.
. Gram+ , , , ,
, , , , .
. 50S .
.
.
.
.
( ). 70%
. 40% .
. O /2 1,60,7 .
. CYP3A4.
. , , ,
, , , , ,
, (
).
. .
. , ,
.
50 .
.

. .

31

. , 1 3, ,
. .
. p450 (CYP3A4)

( )
,
, , .
.
, , , , ,
( ) , ,
( , ) ,
.,, ( ),
. 1 2
. .
.
.
. 250-500mg X4 / . 500mg-1g 2/.
1%
: 500mg
X 4/ 15 . Erythrocin tabl, oral susp., inj.

32

(Vancomycin) (Teicoplanin)

, Gram+
. .
, .
. .
. 5
12 . 50-60%
, , , .
/2 4-8
2-3 .

.
. (, difficile),


Gram+
.
viridans .
. .
. ( ), .
, .
. (red
man syndrom red neck syndrom) ,
.
,
. ,
(.. ).

33

. (
).

( 60 )

.
, .
.
. .
. .
. 125mg-500mg X 4/ p.os .
. Vancomycin, Voncon inj.

34

(Ciprofloxacin).

Gram+

Gram-

, ),


. -.
. .
70%.
. 10% .
.
300ml/. 24 ,
20-35% 5 .
.
. , , ,
Gram- , , (. avium).
.
. .
<18 .
. .
, . , , ,
, , , .
G .
<1% :
.

.
... , , , , , , ,
, , , , , , , .
.

, , , , ,

, , , , ,
.

35

. , , , .
. , , ,
.
. , , ,
, , , .
.

, , .
. , , , ,
, , .

. , .

.
.

.
. .
. 2
. .

.
.
. .
. .
. . Ciproxin tabl, inj

250-500mgX2, 200mgX2.

250mg 100mg
500mg X 2 5-7

1 . 0,9% NaCl 5%
( 1-2 mg/ml).

(ml/)

30-50

250-500mg/12

<30

250-500mg/18

1-2
5g/ml.

36

+ (TMP+SMZ)

1 TMP:5 SMZ (80mg TMP + 400mg SMZ).


. , , , ,
, .

carinii AIDS,

.
. , .
.

.
, ( , ),
..
(CSM, Committee on Safety of Medicines)
(
, )
carinii. .
. < 2 .
.
. 480mg-960mg X 2/ p.os.
C. carinii AIDS, 120mg/kg/
960mg X2 . Septrin, Bactrimel tabl, susp, inj.

37

(Metronidazole)

.
.
DNA .
. 100%
.
. /2 8-10 .
. , , (gardnerella) ,
(giarda lamvlia), (
), Crohn, ,
( Helicobacter pylori).
. . 1 .
. , , , , ,
, ,
( ), .
.
.
.

. .
.
/2 .
. . .
. .
. .
.
.
. LDL.
.
.
. A 500mg X 3/ 7 .

38

. A 250mg X 3 500mg X 2 7 , +/-


.
.
A. A 800mg X 3/ 5
(diloxanide furoate) 500mg X 3/ 5-10
.
. 500mg X 3/ 10 .
. 500mg X 3/ 10 .
. A 2g 800mg X 3/ 3 .
. A 200mg X 3/ 3 .
Crohn. A 400mg X 2/ ( 40mg
500mg X 3/).
(Helicobacter pylori) ( )
500mg 100ml (
14mEq ) . Flagyl caps, susp, sup.vagin . Flagyl I.V. inj

39

().

. E
.
.

.
PPD 2 (),
,
.
. .
.
.
20% .
. .
( )
( ). - ().
(multi-allelic gene locus for
arylamine NAT2). ""
"" . /2 1-3 .
. 5% , , ,
, , ,

(
B6 B6

, 10-50mg/

),

( ),

.
.
. (80-150mg/kg 20-40 300mg)
0,5-3 ,
.

40

. 80-150mg/kg
GABA
.
, . 2-3

.
( ) 1g 1g
( 70-375mg/kg ).
GABA .
,
.
.
. , (
), , , .
.
. P450 (CYP2C9 .. ,
CYP1A2

, CYP3A4 , CYP2E1 ..).

CYP2E1

( -actyll-p-benzoquinone imine
NAPQI

12 ).

.
.

.
, p.os. .
. .
. .
.
. .
. ,
. .
. . 69 . 300mg /. 10-20mg/kg/ ,
( 300mg/).
6 . Dianicotyl tabl 100, 300mg

41

(Rifampicin)


.
. DNA- RNA- (
). .
DNA-.
. p.os.
80%. .
. . 30%.
2 . /2 1,5-5 .
. , , .
. .
. , (<1%), ,
- , , , ( )
. , , ,
, , , , .
"", ,
, ,
20-30%.

, , -

( , , ), .
( 1 ),
, .
. , , , .
. ,

,
,

, , ,

42

.
.
. , ,
, , .
.
. 600mg/ .
500mg.
. 600mg X 2/ 2
.
. 600mg ( ).
Rifadin caps, tabl, sirup. 300, 600mg.
.

43

(Amphotericin B)

.
.
.
. .
.

. .
. . .
.
95% (3% )
. /2 1-2 .
3-7
. .
. .
. , ,
. , , (
), , , , ,
, . ,
. ( ,

).
. .
. .
.
,
(, )
.
.
.

44

. 100-200mg/6 .
1mg 200ml 5%
2-4 . , ,
50mg. , 0,3mg/kg 5% 4-6
1 (5-10mg 500ml dextrose 5% ).
0,1-0,25mg/kg 0,651mg/kg/
>50mg .
1,5mg/kg/. 0,1mg/ml
. H 6-12
1,5-3g. Fungizone I.V.

45

(Ketoconazole)

,
. 100 .
,
.
. 90% .
. (
) /2 1,5-4 ( ).
(85-90%) (10-15%).
. , , ,

.
.
. .
, (, ), , ,
400mg
(, ..). 15.000
50 .
.
.
. 200mg .

. (
, ) .
4-5ml (0,2

HCl)

.
.
, (,
, ), (),
, ( ), ,
( ), , , Tacrolimus.
46

, .
,

H2-, ,

, , , .
. , ,
, -GT . .
. 200mg/ 14
. . Fungoral tabl 200mg, cream, shampoo (2%)

47

(Acyclovir)

. 1 2
- .
(9%), .

. 2 3 .
.
.
,
-GTP DNA

DNA-

.
.
(
)

DNA.
.
DNA- .
. p.os (15-30%).
1/2 . /2 3 (80%)
. .
. , , .
. (<3%)
, , , (
)
( ).
, , ,
. , ,
(9%).

48

2,5mg/mL ,
, (bolus)
,

.

. ,
.
. . <2 .
. .
. .
.
. .
. .
(ml/)

25-50: 12

"

10-25: 24

"

<10:

24

( )
. 200mg X 5 / 5-7 . 3%.
5 . 5%.
5/ 7.
10-15mg/kg X 3 10 .
5mg/kg X 3/
( 1 ) ( ).
. 800mg X4/ 7 . 7,5-10mg/kg X 3/.
, HIV 4
250mgX2 . H
. (
..) gel .
. 10-20mg/kg (
800mg) X 4 /. .
10mg/kg X 3/ (
)
10mcg/ml. ( )
- ( 3 ).
. Zovirax tabl 200, 400, 800mg. 250, 500mg.
3%, 5%, 200mg 400mg/5ml.

49

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