A Tex t B o o k o î

T \ ll -

S t, ic tly A sP e r S y lltıb tıs P r e s c p ib e d jo r B P h a r n ıa c

飞
y
S e ıłıe s te ı
'
V by P ı a ey C o ı
ıtır n ı ın c iı ofı ııd ia . N e w D e ı hi

￠
* . į1
ic
r
\
D r P ra g iA ro ra

D r Va ru n A ro ra

D a v in de r K u m a r

久 二二、 么 躪 鼬ぐ
产

P e e Ve e (R e g d )

Scanned by CamScanner
 C O N T EN T S

C h a p te r 1 A n ti H ls ta ın l
n ee 1 24
H is ta m in e 1 H i
s ta m in e r e c e t
p o r s a n d th e ir d is tr ib u tio n 2 , c la s s ific a
,
tio n o f a n tih i
s ta m in e s 3 H 1
, R e c e p to r A n tih is ta m in e s (p ir s t G e n e r a tio n )
3, Se c o n d G
e n e r a tio n H 1
r e c e p to r s a n ta o n is t 1 4 H 2 R e c e to r A n ta g o
n is t 1 7 r G a s t i g i p
r c P r o to n P u
m p In h ib ito r s (P P I) 2 0
C h a p te r 2 A n tin e o la s tlc A
p g e n te 25 50
A 1k y la tin
g A g e n ts 2 6 , M e c h a n is m o f A c tio n o f A lk la tin
C r o s s lin k in w ith y g A g e n ts 2 6
g s e c o n d G u a n in e 2 8 N it
r o g e n M u s ta r d 2 8 , N
itr o s o u r e a s
3 1 , A z ir id in e 3 2 ,
s , A r y ls u l h o n a te s 3 3 A n tim e ta b o lite s 3 3 F o lic a c id
p , ,
a n a lo
g u e s 3 3 . P u r in e A n a lo g u e s 3 5 . p w w d in e A n a lo u e s 3 9 , A n tib io t
ic s 4 1 , A n th r a c c li y g
y n e s 4 2 , m a n t p r o d u c ts 4 5
C h a p te r 3 A n ti A n g in a l
63 51
V a so d iı
a to r s 52, A
y l N itr ite 5 2 , N itr o g ly c e r in 5 2 , p e n ta e r y th r ito l
m
T e tr a n itr a te 5 4 , Is o
s o r b id e D in itr a te 5 4 D i
5 8 , B e r id tl H d r ł
, p y r id a m o le 5 5 , V e r a p a m il
p y o c ū o r id e 5 8 , D iltia z e m H y d r o c h lo r id e 5 9 , N ife d ip in e
5 9 ı A m lo d i in e 6 0 F l
p e o d ip in e 6 0 , N ic a r d i in e 6 1 N im o d i in e 6 2
,
p p
C h a p te r 4 D iu re t ic s 64 7 9
C a rbo n ic A n h y d r a s e In h ib ito r s 6 5 , T h ia z id e D itır e tic s 6 8 , S tr u c t u re A c
tiv ity R e la tio n s h ip (S A R ) 6 9 ı L o o )
p D iu r e tic s (H ig h C e ilin g D iu re t ic s
7 2 , P o ta s s iu m S p a r in g D iu r e tic s 7 4 , 0 s m o tic D iu r e tic s 77
C h a p te r 5 A n ti H y p e r te n s iv e D 80 97
ru gs
D iu tic s 8 1 , C tr a lly A c tin g A
re en
g e n ts 8 2 , G a n g lio n ic B lo c k in g A g e n ts
84, A d re n e r g ic N
e u r o n B lo c k in g A g e n ts 8 5 , Adrenergic B ı o c k e rs 86ı
D ir e c t V a s o d ila to r s 8 8 , A n g io te n s in C o n v e r tin E (A C E)i
g n z y m e
to r s 9 0 , A n g io te n s in II r e c e p to r a n ta g o n is t 9 2 , A n t iA d r e n e r ic D r u s
g g
o r A d r e n e r g ic R e c e p to r B lo c k e r s 9 3

C h a p te r 6 A n tia i r h y th m ic D r u g s 98 105

Q u in id in S u lp h a te 9 9 , P r o c a in a m id e H y d r o c h lo r id e 1 0 0 . P h e n to in S o
e
y
d itım 1 0 1 , T o c a in id e 1 0 2 r M e x ile tin e H y d r o c h lo r id e 1 0 2 , A m io d a r o n e
1 0 3 , L o r c a in id e 1 0 3 , S o ta lo l 1 0 4
C h a p te r 7 A n tih y p e rı
ip id e m ic a g e n ts 106 112
S ta t in s 1 0 7, L o v a s t a t in 1 0 8 , C lo fib ra te 109, C h o le s t y r a m in e 110,
C o le s tip o l 111
C h a p te r 8 C o a g u la n ts an d A n tic o a g u la n ts 113 12 o
A n tic o a g u la n ts 1 1 5 i O r a l a n tic o a g u la n ts 1 1 5 ı W a r fa r in 1 6 , M en a d io n e
1 1 A c e to m e n a d io n e 1 1 8 i A n is in d io n e 1 1 8 , C lo p id o g r e l 1 1 9
H F a ih ır e
C h a p te r 9 D ru gs U se d In C o n g e s tiv e e a rt
12 1 12 5
1 2 2 , D ig ito in 122, N e s ir itid ė 123, B 123, T
D ig o x in x o se n ta n e z o se n ta n
124

Scanned by CamScanner
 12 6 135

8 C a r d ia c g ly c o s id e s 1 2 8 , B ile a c id s 1 2 8 , G
o n es 12 ,
12 4 S e x h o r m f s te r o id
S te r o ls 0
13 , P h a r
l
m a c o lo g ic a l r o e o s 132
e c h a n is
m
ro te iŊ ı m
p 13 & 14 6
N l
o ın e n c a
h ır e
l1 s te r o id a l B n o r ie n ta ū
h yd _ w b, ą q
a p te r o n o n re p re s e n ta t io
a f s te r o id lv ro car n
ħJn m e n c la tu r e o q ◆p r p n r h p m q n ç e ◆ A

14 1 14 7 167
ıo n e s
12 Sex H om
4 8 , T e s to s te r o n e 1 5 2 r
Æ a p te r
h o rm 1 4 8 , A n d r o g e n s classification
o n es
M a le s e x i l 1 5 9 D ie th y ls t ilb e s tr o l 1 6 0 ,
t d io l 1 5 8 0 e s t r o
e 154, E s ra
, ,
國 Na n d r o lo n
'
1 6 1 , P r o g e s te r o n e 1 6 3
p r o g e s te r o n e s
1 6 8 1 73
il D y s ń ın c tio n
D r u g s fo r E r e c t e
C b a p te r ß
D y s ħın c tio n 1 6 8 , E r e c tile d y s ħr n c tio n a n d P D E in
C a u s e s o f E r e c tile
1 7 0 , S ild e n a fil c itr a te 1 7 1 , T a d a la ftl 1 7 1
M b ito r s m e c h a n is m
174 180
C h a p te r 14 0 r a l C o n tr a c e p tiv e
1 7 6 , N o r g e s tr e l 1 7 7 , L e v o n o r g e s tr o l
C h o o s in g a p ill 1 7 5 , M ife p r is to n e
178
C r tic o s te r o id s 181 195
C h a p te r 1 5 o

18 6,
C o r tic o s te r o id s D r u g s 1 8 3 , In h a le d a n d In tr a n a s a l C o r to s te r o id s
Im p o r ta n c e o f C o r tic o s te r o id s 1 8 H y r o c o r t s o n e
d i 1 9 0 , C o r t s o n e 1 9 0,
i
p r e d n is o lo n e 1 9 1 , B e ta m e th a s o n e 1 9 4 D e x a m e th a s o n e 1 9 2

C h a p te r 1 6 T h y r o id an d A n tith y r o id D ru gs 196 205

C f h y p e r th y r o id is m 1 9 9 , L th y r o in e 2 0 0 , L th T in s o d iu
a u ses o x } o n e m
2 0 1, P r o r a c il 2 0 4 M
or lio th jir o n in e so d iu m p y lth io u e th im az o le 2 0 3
A n tid ia b e tic A g e n ts 20 6 233
C la s s ific a tio n o f a n tid ia b e tic a g e n ts 2 0 9 , 0 r a l h
y p o g ly c e m ic d r u g s 2 0 9 ,
In s u lin 2 09 , S u lfo n y lu r e a s 2 1 0 , S u lfo n lu r e a m e c h
y a n is m o f a c tio n 2 1 1 ,
S tr u c u tr e a c tiv it r e la tio n s h i 2 1 2 G lu
y p , c o s id a s e in h ib ito r s 2 1 3
,
M e g litin id e s n o n s u lfo n lu r e a in s u li
y n s e c r e ta g o u e s 2 1 4 , B i u a n id e
g g s 2 1 5,
O r a l h yp o l c e m ic d r u
g y g s 2 1 9 , T o lb u ta m id e 2 1 9 , G lim e p ir id e 2 2 2 ,
R o s ig lita z o n e 2 2 4 R
e p a g lin id e 2 2 5 , N a te li id
e 22 6, A c r a b o s e 2 2 7,
,
V o g ilo b o s e 2 2 8 g n
L o c a l nesthetics
2 34 2 55
SUrgcal a r e a n eed lo ca l an es th e tic s 2 3 5 , c h e m is t
ry fo r d e s ig n in g lo c a l
tio r o f l
oċ ala n e s th e tic s 2 3 i L o lan
ca a e s th e tic s d r u s 2 4 0 C
g r o c a in e 24 o,
24 3 , B
en zo c
a jn e 24 4 , B

ajn ? u ta m b e n 2 4 5 B
e n o x in a te 2 4 7
, T e tr a 2 4 8,
' ,
tid O c a i c a in e
n , 2 5 0 , D ib 箇
u c a in e h d
y r o c łū o r id e 2 5 2

勇
一

Scanned by CamScanner
 鼯
鲥

飞
O B JE C T ı
V E S

t a m in e
p to r s a n d th e ir d i
re ce
s tr ib u tio n
Sification o f a n tih is ta m in e
s
* H 1 R e c e p to r A n tih i
s ta m in e s
( ir s t G e n e r a tio n )
F
* S e c o n d G e n e r a tio n H 1
re ce t
p o r s a n ta g o n is t
* M a s t c e ll s ta b iliz e r s
H 2 - e c ep t or A n t ag o n i st
G a s t ri c Pr o t on Pu m p
Inh i bi tor s ( pp I)

E SËR o D u c T ro N I
A n ti h is t a m in e s a re th e d h ic h o tın te r a c t th e tio f h is ta m in in th e b o d y
ru gs w c a c n s o e

H is ta m in e is re le a se d b y th e in te r a c tio n o f a n t ig e n s w ith Ig E an tib o d ie s o n th e s u r fa c e o f

m as lls (ty p e o f w
t ce h ite b lo o d c e ll a n d is
a p a r t o f th e im m iın e s y s te m w h ic h c o n ta in s m a n y

g r a n u le s r ic h in h is ta m in e a n
h
d h e p a r in ) T e a n tig e n s a r e p r o te in s o r p o ly s a c c h a ń d e s o b
ff e tc T e y s tim u la te a n tib o d y
h
ta in e d fr o m v a r io u s s o u r c e lik e d u s t p o lle n g r a in s fo o d s tu , ,

b li a n d a r e o f fo u r
i th e b o d y T h e a n tib o d ie s a ls o k n o w n a s im m u n o g lo u n s
pro d u c b o n n ib l fo r a lle r g ic p h e n o m e n o n
t es ie Ig G , Ig M , Ig A a n d Ig E in w h ic h Ig E is r e s p o n s e
yp

T A M

；， 围 曜 to e x t，
二
二日
d,
c o n s tr ic
tio n
D r" " ・ ・・

tp u t
c a r d ia c
o u
In cre a se
th e r ab o v e e
ffe c ts " re
th e s e c J " h ere a s o
r e c e p to r
" ・・
w
In c r e a s e H
m e d ia te d b y ,
tio n s are
G a s tr ic a c id se cre

H , r e c e p to
rs
m e d ia te d b y

Scanned by CamScanner
= a * s

A n tl

C L A
I S S ıF I C A T I O N O F A N T ıH ıs T A M ıN E S

V
H R e c e p to r A t aıg o n i e t A t a g o n is t
z R p to
r n H e c e r n

V G a s t r ic A c id I n h ib i M r e
1 ı
r
F ir t G tio n & * F a m o t id i n e
s e n e r a S e c o n d G e n e r a tio n
«Ĵ m e t id in e

A m in o a ık y l e t h e r
e g F e x o fe n a d fn e
R a n i t id in e
D ip h e n h y d r a ııt in
A s t l e
e g e H ? N iz a t i d in e
T e r ie n a d in e
D ip h e n h y d ń n a t e H ? P r to n P I n h ib it o r s
【m a t a d ln e
o t ım p
B r o m o d i p h e n h y d r a m in e O le
D e s lo r a ıa d in e
e & m e p r a z o
D o x y la m in e s u c c i n a t e E r a z o ıe
C e t r iz in e
s o m e p
a e m a s t in e ń i m e r a t e
ız v o c e tr i z in e
e
D ip h e n y l p y r a lin e H C I
A c r iv a s l in e
R a ı e
P a n もo p r a z o ı
e
E th y l e n e d ia m in e s
ıe in H C I V
e g T r ip e n n a m e

P y r i ıa in M le te
m e a a
H 3 R e c e p to r A n ta g o n is t
M e p y r a m in e
e T h io p e r a m id e
A n ta z o lın e p h o s p h a te
o b e n p r ob i t
T h o ru y la m in e
v e r o n e

厂
p ip r a z in e s
e g C y l iz in e H a
c
C h lo r c y c ıi z i n e H C ı
M e c ıiz i n e H C I
B u c li z in e H a
M a s t c e ll s M b ili z e r

e g o o m o s o ä u m

P N d r o m il s o d iu m
p y la in e o c
* o m e s
L d x a m id tr o ın e l h a ın i n e
g P h e n ir a m i n e M le
e a a te o o e

C h l o r p h in r a m in e M a ıe a te
D e x c h lo r p h in a r a m in e M a le a te
P y r r o b u ta m in e P h o s p h a te
T ń p r o li d in e H C I
D im e t h in d e n e M a le a te
P h e n im d a m in e T a r ır a t e

P h e n o t h ia z i n e

e g P O m e t h a z i n e H C I
T r im e p r a z in e ıa r tr a te
M e t h d il a z in e + ï r h 9 ł

P h e n o t M a z in e a n a lo g s

e g Q rp r o h e p t a d in e

A z a ta d in e M a le a te

Scanned by CamScanner
 PJ A 不回 赠 ßo o 8 o f 쁘뇹비钰炳a ï C h
뺀 セトIł
r・
g\ąi (
二
虿
.. m
,
e
˜
b a s ic
・c tiï iv R e lı
tr iıc tu r e o
s
f H
d o m ħ印 侈A 只)

,
a n ti M s
d r u g s js
R
/
>
ş
C C N
\ R
Ī Ať

Ať A ry ・ o r A rJď m e th y l g r o tqp

x 0 c n
N Ķ R B a s ic te m in a l a m in e gr ou p

1) Leith o fm a in

M ost o f th e an tih is ta m in es d r u g s ħa v th y le n c h a in
e e e w h ic h is re q u ir e d fo r m ax jm u rn
e c o q p Tħe c h a in c a n be s a tu ra te ￠ u n s a tu r a te d or so m e tim
e g C y d iz in e
es p ar t o f a r in
g s y s te m
Fo r

c }d iz in e
C H a

ベゴ
ー

辷
，

， .' '
" '
' ' . . . .

酽 剧目胃日冒 ；
島姓 麗W LLLLLLLL
Scanned by CamScanner
 靱
g
-
; T e x ￠ßo o * o f M ・d r s ta m ı
tl H ı n e
' T
1
围困园丁鼬曲厂
PU A A n

U
T
'

g"primarily by
歹毒
d '" "
oū 6.
' "
' t " u sE ' . ' ' " ' " ss .
. a. -

。 2 It h a s a ls o fo u n d to a id in tr e a tm t o f e ar co n

く
en
g e s tio n

.
。。 。. ・・,
。。。。。，・・・・
3 It is u se d fo r 'ym
p t' " ti" " tm e. t o f . " " . M d . E r tig o m u se d by￡ s

Ę} .
'. " 。 , e a se

?
'"b

Ţ D ip h e n h y d ra m in e
3) D o x y la m in e Su c c c in a te

h ic h is s o lu b le jn w a te r a n d d a r k e n s
h ite a y s e p o w d e r w
r ıo p e ıtie ı It o c c u I s as w

lig h t It is s to r e d in eı idosed lig h t r e s is ta n t c o n ta in e r It is w e ll a b s o r b e d

e x o s u r e to
p t d in u r in e a s m e ta b o lite c o n ju g a e
on t
e x te n s iv e ly m e ta b o lis e d a n d s e c r e e
fro m G J T It ĵ s

]ly d cau se
tU P A C N am e N N d im e th y l 2 (1 p h e n y l l p y l iid in 2ylqoxy! e e s u c c ĵn a te
r e c e p to r c e n m an
a ls o a n ta g o n is e
w a te r a lc o hol an d c h lo r o fo r m It is r e a d ily a b s o r b e d b y th e G I T It is m e ta b is e d ĵ m liv
oı er
、
if*e a y iı aĖe d o x y e
oxyı
。 by y to c h r o m e p 4 5 o
c en z y m e a n d e x c r e te d in u r in e a s N d e s m e th ı
d to tr e a t a lle rg ic d itio n lik e u r tic a r ia c o n u c tilń tis
j pm r itic an d r h iin itis
1 n js u se con s
N O x id e a n d d id e s m e th y l d o x y ı
a m in e a s m e ta b o ı ite s
d tr e a tm fm tio s ic kn
2 R ph e js a ls o u se d in p r e v e n tio n an en t o o n e ss
M e ch an is m o f A c tio n It a c ts by co m p e titiv e ly in h ib itin g M s ta m jn e a t rece p to i s
3 A s it c ro s s b lo o d b r a in b a r r ie r an d ca u se s e d a tio n so it can be u se d in tr e a tm en t o f ł$ l
U ses
in s o m n ia
1 It is u se d in th e co m b in a tio n to tr e a t n a u s e a an d v om itin g in p r e g in a n cy
d It is a ls o u s e d fo r t m e n t o f p a r lc in so n d is e a s e d u e to its an tim u s c a r in ic p r o p e r ty âf į
2 It can be u se d as a sh o r t te r m se d a tiv e

3 It is u se d in co m b in a ū on w ith o th e r d Jn g s to tr e a t a lle r g y a n d co ld
2 ) D im e n h y d ıiru te . l d d e in a n a lg e s ic
4 It is a ls o u se d in co m b in a ū on w ith p a r a c e ta m o an co e as an

H . Fu
CÏ C 1e m a s« n e m e r a te

，
，

CH 3

，
h y d r o g e n fu m e r a te

，
d m e ta b o lis e d b y th e 】 iv e r b y in o n o l
id ly b s o r b e d fr o m th e G I T a n of
a s tin e is e n tr e s e a c h
ra p a
w a te r c le m h t h i a l c
id e c o n ju g a te It a s w o c r
d id e m e th y la tio n a n d e x c r e te d a s g lu c u r o n
￥ l Ä\ ii 1
lu te c o n fig u r a tio n
"
ï
h ic h h a s th e (R ) a b s o
1
w

解 į
Scanned by CamScanner
 v

ta m In
A tıtl q e

)Ţ d
lo rcy c liz in e H y d r o c h lo t td
n ch e
e s e le c ti
ve l

く
；
r Ţ í・
, b u se d fo r tre a - - to f a lim
n e r Bic a c tiv iw
Iıa y fe v e r an d co m m o n
co ld
,
ニト ・ ・・ ・ 。
，

i i ,
à ' ' " ų n g in tic h o li

tU P A C N am e 1 (4
。
c h lo r o
p h e n y 1) p h m y lm th y ıĻ m th y lp ip r a z in
e e e h y d r o c h lo ń d e

nR Ac N am e 4 D ip h e n y lm e
・・
二仁
th o x y l
p
m e
二T
th y l p ip e r id，
u in
hyd
in e ，
o w
r o c h lo r id e

d e r th a t is so lu b le in w a te r
re a

U se s
d ily
n o r c h lo r c y

M
a b
c liz in e

e ch a n
s o rb e

is m
d

o
a

an
fte r
d
f A c«o n
o ra

a ls o
l a d m in is tr a tio n a n đ
m e ta b o lis e d b

It ac t as H
,
m e ta b o lis e d b

y N o x id a tio n
R
y

e c e p to r a n ta g o n js t
Nemethylation to fo rm

o fí w h ite c ry s ta
e
m p e ltie ı it is hite o r s # g h tly
a w
t c o n ta in e r L ik e th e r a n tih is ta m in e s it is u s e d fo
d in tig h d y closed lig h t r e s is ta n 1 d
o tr itic s d is o r d e r s c a r ia
r pn r h in itis 1Jr ū an
or a lc o h o L It is s to n e
i fo r H p to bu t do t th e r a lle rgy p to m
e tin g w ith M s ta m n e
re c e r n o o sym s
M b c h a n is n ı o f A c tio n I t a c t b y c o m p ,

d d b M ta m in e a lo n e 2 It h a s a ls o so m e lo c a l a n e s th e tic tic h o ı
in e r g ic a n d tis e r o to n erg c i p r o p e r tie s an d
re p o
i n s e s p r o u c e y s an an

can be u se d as an an tie m e tic s

U be s
1 It is u sed fo r s y n ıp to m a tic īe lie f o f r h in itis p r u r itic a n d h a y fe v e r 8) M e c liz in e H y d r o c h lo r id e

s a lt (P ip r in h y d r in a te ) a s a n in g r e d ie n t n p r e p a r a t o
i i n o f
2 It is a ls o u s e d a s ? e ı
e o ? te
CH
lie f o f m d c o l&
gh an c o zıu n o n a
re u

3 It c an a】
so be u se fu l in th e tr e a tm en t o f pa r】
dn s o n is m
H N
D CH z H C\

6) T d p d tm a m itıe H y d r o c h lo d d e

Cl
ı ı
ı ? e r a E in hy
tU p A C N am e 1 [(4 C h lo r o p h e n y 1) p h e n y lm e th y lì Ļ (3 m e th y lb en z y 1) p iı e

dro c h lo r id e

f th e N m e th y l g r o p It is w e ll a b s o ib e d a n d d is tr ib u te ă
m e th y l b y l g r o u p in p la c e o
en z
n N A c N am e N Nimethyl N fp h e n y ]m e th y J) N p y r id in 2 y le th a n e 1 2 d ia m in e
th r o u g h o u t th e b o d y a n d m e ta b o liz e d in
liv e r It is e x a e te d u n ch .
i
G e d in fe c e s a n - W
lite s a r e fo u n d in u r in e

i i a n a n ta g o n is t o f H r e c e p to r s 1t a 】
so a ct a s dop
M e c h a n is m o f A c tio n M e c h z n e s ,

in e a n ta g o n is t a n d a n tic h o lin e r g ic

its lo n g la s tin g an tie m e tic e ffe c t :;

1 It is u se d fo r

fo r tr e a tm en t o fń au sea a n d m o tio n s ic ı
m e ss o r verso
2. It is p r im a r ily u s e d

itic s k in d is o r d e r s
3 It is a ls o u s e d in p r u r

Scanned by CamScanner
A

1 l )
n t ıH

T r
ls

ip
ta m

r o lld in
ın e

e H y ? o c h lo r id e
J H
"
く C H ,
* ， 。

H 3 C

I U P A C N 2 [3 (P y li d in
n o h y d r a t e
a m e r r o l y 1) 1 p t o ly lp r o p l e n y 1] p y F , d in e h y à r o c h lo r id e
m o

S y n th e s i s

C I

O H

T ip o lid i n
W
r e <
C H 2 C H 2

P r o p e r ti e s I t is w h ite t 】】i n d
c r y s a e p ith li g h t
d in l
o w e r w a s u n p le a s a n t o d o r It is s o lu b le in
w a t e r a n a c o h o l a n d i ts s o lu ti o lk 】i n to li t
n s a r e a a e m u s It is r a p id ly a b s o r b e d ĵ n G I T
a n d g e t m ta b li d t b y la te d
e o s e d
o a c a r o x e r iv a t iv e w h i c h a c c o m t s fo r a b o u t h lf th d
a e o s e
e x c r e t e d in th e u r in e

m i n e c h a n i s m o f A c « o n lt a c t a s H 1
r e c e p to r a n ta g o n is t a n d b lo c k th e a c t io n o f M s t a

;
U s e s T r ip r o l i d in e is u s e d to tr l th
c o n o e s W p to m s a s s o c ia t e d w i th a u e r g ie d
t im e s c o m b in e d w ith o t h e r ld d t id
s a n
S o m
c o r u g s o p r o v e g e n e r a l r e l ie f f o H li k
r u e s y m p to m s

m P h q n ln d a m in e T a r tr a t e

n n n u

C H 3

Scanned by CamScanner
 J 1
1 4 ) T r lm e p r a z ln e T a r tr a te (A lhnlne)

C H 2 C H C Hぎ N
ノ
3 HOH
X C H a
C H C 0 0 H
3

IU P A C N am e 10 [3 (d im th y la
m in o ) 2 m e th
y l p r o p y l] p e h n D th ia z in e ta r tr a te
e

P r o p e r tie s It o c c u r s a s a w h ite o r o ff w h ite a s ta ]]in e o w d e r th a t is h

y p eeı y s o lu b le in
w a te r a n d in a lc o h o l It is w e ll a b s o r b e d in th e d i e s tiv e tr a c t a n d
g m e ta b o lis e d b y liv e r
M e ch a n is m f a c tio n
o Tep ra zi ne a n ta g o n is e s th e a c tio n s o f M s ta m M e b y b in d h g a t
H ,
rece p to r

U ses

1 It is u se d as an an tip r u r itic

2 It a ls o ac t a s a se d a tiv
e h y p n o tic a n d a n ū e m e ū c fo r m o tio n s ic la ı e ss
3 In R u s s ia it is d fo r th e tr e a tm e n t o f a i ıx ie t d is o r d e r s
u se
y p e r s o n a lity d is o r d ers o r
o rgan ic m o o d d is o r d e r s

ĺĺĺ444111Ș
Scanned by CamScanner
 !ğ 4
ı į ・ ・
鑾巍巍 鑿
A n ıtım l
«ıH ı T

.
,. °

仁 .

d w e ig h t g a in in
h a e tite a n
a le a s e t e pp
iaı p o r te
d ro h
J h u s A th is ? u g is Æ

ri

ı6 ) A ıa tid in e M a le a te

i
a ın j n 1 (4 flu o r o b e n z -
y 1) 2 1(1 (4 m e th o x y ph e n y D ￠ p ip e r id y i

ï p e r tie s It is w h ite n u ffy þ

r o o w d e r in s o lu b le in w ą te r s o 뇨山1e in o r g a n ic s o lv m t s u c h

as e th l D Ą F D M S O It is s to r e d in w e ll c lo s e d li h t r e s is ta n t c o n ta in e r I t is r a p id ly
a n o
g
a bso rbe d b y G I T

M e ch a n is m o fA c tio n A s te m iz o le is a s e le c tiv e H re c e p to rs a n ta go n is t
,

U ses It is u se d fo 1e r g y s y m p to m s p a r tic u la r ly r h in itis a n d c o

tr e a tm e n t o f a 】
r n ju đ iv itis
It h a s n o lo n ge r u se n o w d u e to its c a r d ia c to x ic ity i e It c a u s e s a i r h y th ï n ia s
:: [5 6 ] c y c lo h e p ta
th y lH ip e r id y lid e n e ) 5H b e n
n » AC N a m e 6.1111-61 m e z o

(12 4b) p yıid in e m a l e a

P ıo p e H ie ı m i d m g Ė h ic h 1ń u 2) L o ra ta d in e
a】
so p h e n o thia z in e a n a lo g in w su a to m is re p la ce d by
s a ? r a te d e ū }đin id g e a n d g n itr o g e n is 呷 la c e d b y carb o n a to m

It is i & b 】
jg h t a ea m c o lo r p o w d e r w h ic h is s to r e d in w e ll c lo s e d c o n ta in e r I t is
s o lu b le h h a v in g m e ltin
N a ta
g p o in t 15 2 15 4 C It is w e ll a b s o r b e d o r a lly a n d

M ed u m is m o f 勇则由o n » is a
potent re c e p to r an ta g o it
n s

f ti
1 ħis ï Ħł To r ' '
ų p e r r e s p dr a tm y m u c o sa l c o n g e s tio n ĵ n a lie ı ic N
g r h in itis
2 n is n ç w łfo r ? e r e lie f f
o n a sa l c o n g e s tio n a n d e u s la h i
an T B C O O C H zc H
c co n g e s tio n s

G EN E RA T ı n Æ A c N a m e Ethyl-Ļ(Oro-5 y d i c 1 1 H bm z o [5 6 ]c y c lo h e p ta L1tpyridĵ n
oN H ? C E PTO RS A N T AG O
, N 1 1 y lid e n e ) 1 P ip e r id in e c a ib o x y la te
T ħe n H jo r s id e e a e c t o f Jir s t b u t so ıu b le in
p r o p e r « e s L o r a ta d in e is w h ite to o ff w h ite p o w d e r in s o lu b e n w a e r
g e n e r a tio n l i t
an ta g o n is t is d a tio n b e c a u
se se th e y cro ss th e
a c e to n e a lc o h o l a n d c h lo r o fo r m I t is r a p id ly a b s o r b e d a fte r o r a l administratiı i an d
m e ta b o lis e d b y O d e m e th y la tio n a n d d e c a r o x y a
b l ū o n to fo r m d e s lo r a ta d in e w h ic h is ' T

A te ın a s p o n s ib le fo r a n tih is ta m in ic a c tiv ity

s z o le e a n d T e rfe n a d in f M s ta m jn e a t p Ġ
e w ere d e v e lo
ped w jth la r e r N M h ec i anf A tio n
sm L o r a ta d in e c o m p e titiv e ly a n ta g o n is e a c tio n o
o c
g te r tia r
y am in e su b s titu ts
Canvascuıar hodiq v a r io u s
en
r ip h e r a lH rece p to r s
ın n
i a ıte r tia ı
y a m f ie o r
n e w er a
a s a s u bs tit
g e n ts w
u en to f
ith
polargroup c o n n e c te d e ith e r to th e te r
u se t s e o r in c o m b in a tio n
u s E d a lo n
w ith p s e u d o e p h e d l in e su fa e fo r i e ]ie f
】 t Ofse
one o f th e d e r y th e m a
aro m a tic r in s w so n a i a lle r g ic r h in itis p n H iń s u r tic a r ia a n Ê; {ţ F ť )
g e r e d e v e lo e d
p Jh ese
1 ￡

◆ °

k
.
i
į
Scanned by CamScanner
 bo ok q m @ d lc m ? l c h e m ł
u a te x t
￠
st
2 yıł ą A l
n ti H ï s ta m ĺ n e

cr om o l yn so d i um

Ç7
刃 '" N

ţ
' " " .

Ö 6 CH H C H
2
Ť z
o 0

O H

tU p A C N a ın e : D is o d iu m 1 3 b is (2 « a rb o x
ŕ
y c h r o m o n 5 y lo x y ) 2 h y d r o d o x yp o p a n e
p r o p e r tie s It is a w h ite h y g r o s c o p ic c T y s ta llin e p o w d e r th a t is s o lu b le jn w a te r It is
ta s te le s s b u t s lig th ly b itte r a fte r ta s te It is p o o r ly a b s o r b e d fr o m
G I T b u t r a p id ly a b
f i h l i T h i d i t d h g d in u r in e a n d in ie c e s
s o r b e d b y th e u n g s a
l t e x c r e e u n c a n e
ter n a a o n s r u g s

M e c h a n is m o f A c tio n It in h ib its d e g r a n u la tio n o f m a s t c e lls th u s p r e v e n tin g th e r e

le a s e o f M s ta m in e a n d le u k o tr ie n e s It a c ts b y in h ib itin g c a lc iu m
i r ıf l
H ta o n is t
r e c e p to r a n g
M e c h a n is m o f A c tio n 16 a c ts as , U s ės
itc h in g
symptoms lik e y n o se ,
r u iu ı eye sn e e z
d fo r p r o p h y la c tic t o fb ro n c h ia l a s th ın a
u se c e tr iz in e is u sed fu ie v e a lle ï g ï
r e】 1 N e c r o m o ly n
b u liz e d so d iu m is u se m an a ge m en

a n d b ro n c h o sp a sm
i n īm g e
2 Its n a s a l s o lu tio n is u se d fo r a lle rg ic r h in itis

4 ) L e v o c e tr iz in d to tr e a t a lle rg ic co n u c j tiv itis a n d k e r a titis

e 3 Its e ye d ro p s a re u s e

is tıs e d to tr e a t M s ta m in e r e la te d s y m p to m s lik e
4 0 ra l concen trate o f cro m ly n s o d iu m
o

Hu s h in g v o m itin g u r tic a r ia a n d itc h in g

HCI
C HzCHźO C HzC0 0 H
IH 2
R EC E PT O R IWTAGO
ti o f M s ta m in e a t H 2 r e c e p to r
b lo c k e r s a r e a g r o u p o f m e d ic in e th a t b lo c k t e a c o n
h
H
s to m a c h ıh e r e fo r e th e s e
z
f
h T h is d e c r e a s e th e p r o d u c tio n o a c id in
n N AC N 4 2 t4 Įm p r e s e n t in th e s to m a c x c e p t O m e tid in e a ll H ,
p hıe n y ])p h e n y l m J
e th y l P ip e r a z in e l y 1] e th o x y
am e E
o ro
i d d d l l
d r u g s a r e u s e d in th e tr e a tm e n t o f g a s r c a
a c= t n u o e n a u c e r
tic a d d d ih y d r o c h lo r id e lik e h y p o te n s io n h e a d a c h e
a n ta g o n is ts a r e w e ll to le r a e
t d a n d h a v e c o n m to n s id e e ffe c ts
POPerties n is Ie v o r o ta to ly e n a n tio m f c e tr iz in d The ą b l k s r e d u c e th e v o lu m e o f g a s
It is d ia r r h o e a c o n s tip a tio n d iz z in e s s a n d ? e n e s s
h ite o c e r
er o e a w u in e p o w d e r
c r y s ta
th a t is w a te r s o lu b le It is th in y tim e s m o r e a c tiv e tha n k tio d d is s o c ia te s m o r e tr ie u ic e s e c r e te d a n d h y ? o g e n io n c o n c
en tr a tio n o f g a s tr i c ju ice
s lo w ly fr o m H
n an m er an j
« ece
p to r s It is rap id ly a bs o rbe d fte r i a d m in is tr a tio d p ity r e la tio n s h ip )
a o o r ly
, ora n a n S A R (S tr u c tu r e a c tiv
metabolis e d in u rin e
ti n le d to tfie d is c o v
M e c h a n is m f A c tio n G u a n y l h is ta m in e h a v in g p a r tia l a g o n is t a n d w e a k a n ta g o n is t a c o
o ıe v o c e lr iz in e js a c tiv e tof
seı
e n a n tio m e r o f c e tr iz i
a te w h ic h f H 2 r e c e p to r a n ta g o n is t d r u g s It a c t a s a
lea d in th e d is c o v e r y a n d d e v e lo p m e n
e c tiv e ly b in d ı
o H
n e ra ce m e ry o
r d a n ta g o n is e th e ff
e c e p to r a n
, e e c t o f M s ta m in e ta is ts
U se ı
ts n ew er H re c e p to r an go n
u se s a re s im ila r to c e tr iz in Ĺ ,
e e u s e d fo r a ll
e e z in
s ıı
& itc h in g e tc
e rgy s m
y p to m s lik e r u n o se
n n y

IM A s T c E LL
STMILIZER i
NH 2 in e
G u a n y lh is ı
a m

t o r y c e ll l
} p e s a s so c ia te d w ilh
an d a s th m a

Scanned by CamScanner
 吧

w a s m one p o te n t th a
n paï ıt G
ı uu ı lh is
y
ta n u n e m
d 孟小 ・一 一 ・
・
。
。 。 。。
。 。， 嬲
j e les ï a ıa c tiv i j S y n th e s is

NH C H a
C H s C O C H C 0 0 C zH s
cH2N H
C H z c H ac H z H N N
ļ i
attlų
V

" y bU t
X
~
į ・ } :
H ac C H z O H
HSCH z CHzNH z

HaCcHzscH2CH2NHCSCHs C H aN H
\ iz
n
tİ d in
= øa a ı z
)
C im e e
. i
H Ń ŕ4
CM e üdin e V
fiv e s a
w a e s Jn e s iz e d w ħic h a ıe m o r e a c tiv e th a n c im e ig h tly s o lu
s】 b le ĵ n a te r
tid in p o w d e r th a t is
w
e For p p e r« e s It is h ite to ff w h ite c r y s ta llin e
ex am
p le ro a w o

' " . °'

ÏT
" °
x y
' " I '" . ' " '' " ' ' " n ta g o n is t ' ' e" '" " '
N S0 NH
.", ' CH2 C H 2 2 M ..
2
fı
a n iūd i
ne N H2 U se s C im e ū d in e is u se d in ĥ e a tm en t o f g a s tr ic an d du o d e n a l u lc e r s

an ta g o n is t d
ru gs a re d 2/ F a m tid in e § $ į:
'
i!
￡
1) a tid in e s a iı
】e d as ı
o
m e e 0 1lo w s

厂
。 く に
二

胪 シ
聞 。 -
대나 。。
、
뇨
。

N CH cH
i th y le n e )a m h o ]th ia z o 1 4 1
y 1) 3 11[ 2 [(d ia m n
z S
C H aH z tU p A C N am e N (A m in o su lp h o n o m e

di
n
I
_ C V ・
mhyl125-ı
nethyljmidazo'-yl
,

￡
i i phbxide
e

XXĹCHşĤ X, ĥ P X V . H
'
m e th
y ltM o ) e th y lj g u an i ł . ..
d fr o m th e G 1 T d its fa ın o tid in e
an
fr o m lig h t F a m o tid in e is in c o m p le te ly a b s o r b e t ĵ n G u a n id in e
l b io is o te r e o f c im e tid in e th a t c o n a
i h i
e ta b o iite e x c r e te d in u in e
m
It is a t a z o e

gro u p

Scanned by CamScanner
 o' " dr ' " '
Eį egį ''tú
■ I .

. o f gm
h i- d d"d . U U J~ Ī p e r tie s It is a w M te to o ￡ f w M te c r y s ta U jn e p o w d e r th a t is v e r y e liB h tly
智 . . w a te r It is r e a d ily a b s o r b e d a n d m e ta b o lis e d b O d e m e th la tio n m e th y ıo id a tio n i
a ıd
y y x

:i
fo n e

M M . d. . H ıd ıo a l" ł? fA
M e c h a n is m o tio n
c O ın e p r a z o le is a s e le c tiv e a n d ir r e v e r s ib le p r o to n p u m p in h ib i
to r It in h ib its H /K A T P a s e s y s te m a n d d e c r e a s e a c id s e c r e tio n
U ee :O m e praz o le is u s e d in tr e a tın e n t o f p e p tic u lc e r g a s tr o e s o p h á g e a l r e H u x d is e a s e
I
E lis o n s yn d r o m e an d e r o s iv e e so p h a g itis :K ľ 1 q

2) L an so p r a z o ıe

钾
V
R
い '
・・ ゴ飞
H z C F B
R a n itid in e lik e th e r d r u g s in h i i þe a( tio n f h is ta m in
M e c h a n is an o f A c tio n o l
e a tH
r e c e p to r
z tU p A C N a m e (R S ) 2 ([3 m e th y l Ļ (2 2 2 trifluorcethoxy) p y r id in 2 y l]m e th y l sulfiny
d d u o d e n a l u lc e r 1 H b e n z o [d lim id az o le
Ue R a n itid in e js u se d fo r tr e a tm en t o f g a s tric an

p r o p e r tie e It is a w h ite to b r o w n is h w h ite o d o r le s s a ry s ta 】 】in e p o w d e r th a t js p r a c &

lly in s o lu b le in w a te r It is a r a c im ic m ix tu r e o f d e x la n s o p r a z o le an d le v o la r ıs o p r a z o ı
e in
ca
l is r e a d ily a b s o r b e d a n d m e ta b o lis e d ĵ n to its
w h ic h d e x la n s o p r a z o le is a c tiv e L a n s o p r a z o e
EOWCROï tm JM P 】N H Ï M T
P【
s u lfo n e a n d h y d r o x y m e ta b o lite s

M ech an is m o fA c tio n Its ac tio n is s im ila r to o m e p r a z o le

llin g e r E llis o n s y n d r o m e (tu f s to a ch w h ic h re su lt s p e p tic u lc e r ) an d

u se d in Z o m o rs o m

G a s te r o e s o p h a g e a l r e flu x d is e a s e (s t o m a ch co n te n t r is e u p in to eso pha w w h iċ h re su lt

h e a rt b u m c h e s t p a in v o m itin g

3) R a b e p r a z o le
i
ノ飞
. '

c H

" .
P m e th y 1
th y l] P y r id ĵ n 2 y 1】 lfin y ll
y p ro p o x y) 3
su
tU p A C N a m e (R S ) 2 [[4 (3 M e th o x m e

1H b e n z o td ] im id a z o le
i h w h ite s o lid w h ic h is v e r y s o lu b le
p r o p e r tie s R a b e p r a z o le is a w h ite to s lig h tly y e l o w s
l
h i f a n d in s o lu b le ĵ n e th e r a n
d hex an e
in w a te r m e th a n o l r e e y s o u
f l l b le in e th a n o l c o r o o r m

T h i th b li a c id th io e th e r
It is a b s o r b e d a n d m e ta b o lis e d in liv e r b y o x a o i d t i n o e e r c a r o x y c

e te d in u r in e
it m e ta b o lite s a p p r o x 90 % o f d r u g is e x cr
g lu c u s o n id e a n d s u lfo n e a r e s an d the'Stoma ï
w /K A T p a s e p u m p in s
M e c h a n is m o f A c tio n R a b e p r a z o le in h ib its
a c id tio
su p r e s s th e se cre n

į - )

Scanned by CamScanner
Scanned by CamScanner
 E Ę
rŢ È a

A N T I N EO p LA ST ı
C -

A G E N T S "
I C

( ÐB J E C T M
A l ky l at ing Ag e n t s
M e c h a n i sm of Ac t ion A1 ky l at ing Ag m t s
of

C r o s s ı nk i i ng wi th se c o n d Gu a n i ne
A n t ime t ab o l ites

:X H . M is c e lla n eo u s A g e n ts

E Sū R o D u c T rm
A n tin e o p la s tic a g e n ts a re u sed to tr e a t th e ca n cer g ro u p o f d ių p a s e m o h l
C a n ce r is a

in g a n a b n o r m al an d u n c o n tr o lle d c e ll d iv is io n in ın o s t o f th e n o r m a l b o d y c e 】 1s T h is n e w
c e il g r o w th in v a de th e s u r r o m d in g s tr u c tu r e s T h e c a n c e r ın a y b e b e n ig n a n d m a lig n a n t
B e n ig n tu m o rs do n o c a tio n s in th e b o d y ) b u t m a tig
o t m e ta s ta is e (s p r e a d o f c a n c e r to o th e r ı

n an t do m e ta s ta is e C a n c e r is c la s s ifie d a c c o r d in g to th e ty p e o f c e ll in w h ic h n e w g ro w th
O C C U RS a s

1 .
C a r c in o m Th is ty p e o f c a n c e r d e r iv e d fr o m
a e p ith p li《l c e 】】s T h is g r o u p re p r e s e n ts
n e a r ly a ll th o s e in b r e a s t, ltın g , p r o s ta te , c o ı
o n an d m a re a s c a n c e r

2 S a rco n a
ı ıh is ty p e o f m a lig n a n t ttım o r a r is e s fr o m tr a n s fo r m e d ce lls o f con n ec tiv e

tis s u e T h is tu m o r is m a d e o f c a r tila g e , fa t, v a s c u la r , c a n c e llo w bo n e an d he m a to p o i

e tic tis s u e s

3 L e u k e m ia d L y m p h o m a ıh e s e tw o m a 】
an ig n a n t o r s d e r iv e d {r o m h a e m a to p o ie tic
(b lo o d c e ll fo m g ) ıh is tu m o r m a tu r e in ly n tp h n o d e s a n d b lo o d r e s p e c ū v e ı
y Lyn
p o m a s a r e H o g k in L y m p h o m a a n d th e n o n H o d g lc in L y m p h o m a s T h e e n la r g e d
h d
L y m p h n o d e s a r e u s u a lly p a in le s s
4 .
G e rm c e ll tu m or lt is d e r iv e d fr o m g e r ın c e lls It m a y be m a lig n a n to r b e n ig n G
c e lls n o rm a u y fo u n d in th e o v a ry a n d te s tis
5 B 1a s to m a It is co m m o n in ch ild r e n It is a tu m o r th a t resem b le s a n im m a h ır e o r

em b r o y n ic tis s u p h r o b la s to m a m e d u u o b la s to m a a n d r e tin o b la to m a
e Ex am p le s m e n e ,

C a n c e r c a n b e tr e a te d b y m a n y w a y s in c lu d in g c h e m o th e r a p y , s u r g e r y , r a d ia tio n th e r a p y
a n d n e o pı a s tin g a g e n ts T h e a n tin e o p la s tic a g e n ts a r e th e s p e c ia liz e d d r u g s u s e d p r im a r ily
to tr e a t c a n c e r T h e fir s t a n tin e o la s tic a e n ts w e r e u s e d i n 1 9 40 s , w h ic h w e r e m a d e n a h ı
p g
r a lly o r s n th e tic a ll A ti l ti t b d a o n e o r in c o m b in a tio n w ith o th e r
l
y y n n eop as c a吕 e n s ca n e u se
a n tin e o p la s tic d r u s T h e s e d r u s d e s tr o
g g y th e c a n c e r c e lls b u t h a v e s o m e s id e e ffe c ts lik e
n a u s e a , h a ir lo s s m o u th u lc e r a n d lo w e r in
, g o f th e b lo o d c e ı ls
A n tin e o p ıa s tic a s e n ts h a v e d iffe r e n t m o d e o f a c tio n a n d th e ir e ffe c t d e p e n d s u po n cy
to to x ic a c tio n w h ic h is s e le c tiv e fo r b e n ig n c e lls i e R a p id u y d iv id in g c e lls

Scanned by CamScanner
Scanned by CamScanner
Scanned by CamScanner
 e q o fM e di
ı ì
ęu A w n ti N e o a s tı
pı c A ge n ts
A

m u ta tio
n s
to
n u c te o đd e s le a d ji ıg
fm
f th e
c) B y in d u c tio n o ispg o
M ec h a n is m o fA c tı
o n 1ť a c ts by a u cy la tio n a lte fs th e n u cı
e o tid e gu a n in e by ca u se s

wwn ament
)
(Tel1iymhom
i es u
h
'
f m y c o d s fu
o
f b
th e lp h a 1_ i" d "nly in th " f. ltip le y e l' m d ca í c in o' "
rea s
t
u se d
N b can cer
e " ' " . ? o u m "
2 f r o s ta te
is u s e d in tr e a b n
en t o p
Jts e s o g e n a n a lo gu e
3
2 n is a ls o u se d to tr e a t o cu la r re tin o b la s to m a (r e tin a ca n ce û
2 ) C y c lo p h o ıp h a m id e

4 ) C h l0 bu il
f? c H z c H 2C ï : f H '"fy'Ę Í ,: f : ram c

ー
N
貨 /，ふ イ 武
ı H
C H a C H aU l

in 叩 e rhy d r o 132 o x a z a p h o s p h o r in a n e
n ÆA c N am e (R s ) 2 B is (2 m o ro e th y l) am
4 14 B is (2 c h lo r o e th y 1)a m in o ]b u ty r ic
phen yı a c id
Iu p A c N a ın e

n y gm ec u p ıĽ u ıw w
d fr o lig h t I t is r a p id ly a b so rb e d fr o m th e G 1 T ar id m e t a b o lis e d in iv e r in to its
ı
t. Te m

a c e tic a c id m u s t a r d (a c tiv e ta b o lite )

Ph en yı
m e

m u s ta r d m e ta b o lite s F u r th e r cyclophosphami,
to ? x icp h o s p h o ra m id e a n d n on n itr o g e n
by e n z y m a tic o x id a to in g iv e s 4nxocyphosphamide a n d ca rbo x y p h o s p h a m id e a s in a c tiv e lic a tio n an d dam a g e th e D N A in a ce ll
m a b o lite s
eı
U ses

1 C h lo ra m bu c il is m a in ly u se d in chro n ic ly m p h o c y tic le u k e ın ia
m u s ta r d fa im s D N A (T o ss li田田 b e tw een an d w ith in D N A s tr a n ds a t gu an in e N 7 p o s itio n s
c a r c in o m
2 It b e u se d fo r n o n H o d g k in ly m p h o m a p o ly c y th e m ia o a l ia n a
can

1 C y c lo p h o s p h a m id e is use d in th e tr e a tm t o f ly n ip h o m e s o lid tu
en as so m m o rs an d
B )
2 It ĵ s u se d to tr e a t rh e u n ıa to id a r th r itis d s th a t in c lu d e itr o N o ) gr o u p An d àu re a
s e v e re m u ltip le s c le r o s is m in im a l c h a n g e d is N itr o s o u r e a s a r e c la s s o f co m þo u n a n so
e a se a n d w egen eť s
gra n u lo m a to s is

S tr e p to m y c es a chro m o
i th e n a tu r a l a n tib io tic o b ta in e d fr o m gm es
e g o r y w h e r e a s S tr e p to z o ta c in s
3) M e lp h a la n an d C 1ū o r o z o to c in a r e la te d c o m p o u n d h a s b e e n p r e p a r e d

M e ch a n is m o f A c« o n
c a ib o c a ūon h ic h a r e s tr o n g
N itr o s o u re a s u n d e r g o n o n e n z y m a tic b r e a k d o w n to fo r m s w
/ B F u r th e r itr o
￠
tt d a lk y la te p u r in e a n d p ln im i in e
d b ases o fD N A n so u re a s
e c tr o p h ile s
r
eı an can

E . C X
Y Ţ :
D N A r e p a ir E n \ es

ŢŢ
e o f Pr°
h '

Ţ
w c

.' " ch is p r a c tic a ll

y

Scanned by CamScanner
A n ti N ・o pı e A w
a * tı n tł

'
' ' ' " ı i_ It a c ts o n Tpo=Onofguanin=beseoı
'DNÀ_
8 r o w th b y c ro s9 ıın kł
n g w th D N A d o
ł u b le h e ħx su an ds so h a t th e c e o s c a n
ı n o \
W
dı v ld e

U sc s

1 T h io te p a ı s u se d In th e b ea M rm t o f v a r fo ı
= s o lid tıım o ￠s n d
i o d i n g b r e ıs ł, o m y am d
b la d d e r c a r c in o m a
2 T h io te p a is a ls o u se d h th e lıe a b n m lof v a r io ı
ıs

D ) A R Y LS U LP H O N A TES

The m o s t im p o r ta n t m e m be r o f th is g ro u p is B u s o 】】
B u s u lfa
ı n

C ĺ O ıO C H l W ? i q o s o ı
IU p A C N am e l , Bu ta n ed io l d im e th a n e s u 】P m m a

in w a te r It is s to r e ig h t
d in ı r e s is ta n t co a iıw r
n ı

B u su lfa n co n ta in s tw ıa b ile m e th a n e s u lfo ıī a te g łu u p s (O S O z CıŁ

o } a » d ni d b o p p t e
d s o f a fo u r c a r b o n a lk y l c h a in B u s u lfa n h y d m ı ys ed m m
& e s w a n a g ro u p s
en

an d c a r b o n iu m io n s
B u su lfa n is m e ta b o lis e d in liv er by gıutathi ((Ä I ï ) « w p ı
ne an ı 8
te tr a h y d r o th io p h e n e tetrahydrothiopheıie12de su fo ı
ı a n e an d as

in a c tiv e m e ta b o lite s
M e ch an is m f A c tio n
o Its ın e c h a n js m i n v ı ııe c ıo s s h ik in g b e tw e e n g n e an d
d b y a n S F P r e a c tio n in w h ic h n u c ıe o p h ū e g tıan i
n e a s c a rb o n
a d e n in e in te r s ta n
a g e c an n o t b e r e p a d b y elm
s y la te le a v in g g r o u p T h is ty p e o f d a ırı
ar
a d ja ce n t to m e

m e cha n is m
U B lfa n h a s a s e le c tiv e im » v e e fle c t o n b on e m a F n » It is u se d to
se u su m u n osu p p te s
tr e a t c h r o n ic g r a n u lo c y tic le u k a e m ia

Æï M E ï A B
ite is a s u b s ta n c e th a t r e p la c e s o r in M b iķ a s p e c itic ın e ı a b o lile O n te r m e d Ļ
n tim e ta b o ı
A
n or m a l c m a r ın e ta b o lic
a te d p r o d u c t o f m e ta b o lis m ) o f a c e ll th u s in te r fe r e s w ih
an

d
ħın c tio n In o th e r w o r s a n m e a ti t b lit v n t b i o s y n a n ￠ıU t i ı i s a n ofn ı
o e s p r e e
S o d u e to ib
a r m e ta b o lite s A n a n tim e ta b o lite is s im iı a r in s tn łc h ır e ło a
æ llu ı
s tr u c tu r e s im ila r ity a n tim e ta b o lite s r c ıd ilv incorpora
in to D N A o r R N A a n d in te r fe r e
w ith c e llu la r h ı n c tio n F o r e g A n tifo ı a te c o m p e tit \ e y
i r l in h ib it th e fo lic a d d a n d p r o d u c e
t i o x c e ffe c ts o n c e lls i c th e s to c e ll t o w th a n d c e ll d iv is io n y p 吕
A ) F O L ıC A C ıD A N A LO G U E S
a c id b y th e d ih y d r o fo la te
F o lic ac id B e ts re du d in to te tr a h y d r o fo \ic m
ce
en z ym e

h ym id ln e d so m e a m in o a c id s
e c e s s a r y fo r th e s y n th e s is o f F u r in es ı an
re d u c ta s e T H F is n

Scanned by CamScanner
A n ti N e o p ıa s t ıc A g ・ n t a 屬
S y n t h e s i s

H 2 N
・
Ī į H 2
y
C H 2 B '

P a r a a m ın a t e d 2 & D ib r o m o
P y ń m l d ln e P ro p ïo n a ld e h y d e

N H

H O O C C H

V C + h C H a C 0 0 H

M e u to ır e x a l e

p ti I t is ll t o r a g e b r o w n c r y s ta llin e h y g r o s c o p i c p o w d e r W h ic h is p ï a c
r o p e r e s y e o w o n

ti c a lly in s o lu b l e in w a t e r b u t s o l u b l e in d il u t e s o lu t i o n s o f m in e r a l a c id s a 】k a li h y d ı o x id e s

a n d c a r b o n a t e s i t is r e a d ily a b s o r b e d in l o w d o s e s i t p o o r ly c r o s s e s b l o o d b r a i n b a n i e r i t
i s c o n v e r t e d in t o i t s 7 h y d r o x m e t a b o li t e s in M g h d o s e

m e c h a n i s m o f a c t i o n m e t h o t r e x a t e in h ib it s t h e w w w e d ih y d r o f o ıa t e r e d u c la s e th u s

p r e v e n t s t h e f o r m a ti o n o f T H F
U s e s

1 M e th o t r e x a t e i s u s e d t o t r e a t p s o ń a s is a c u t e lw p h o b la s t ic le u k a e ın ia a n d d ıo r i o c a r c i
n o m a

2 I t h a s a ls o b e e n u s e d a s a n n
i ım r u n o s u p p r e s s a n t

3 I t i s a l s o u s e d t o t r e a t r h e u m a t o id a r t h r i t is in f la m m a b o r y m y o s i t is l u p u s b r e a s t n e c k
a n d lu n g c a n c e r

B ) P U R ıN E A N A L O G U E S
P u r i n e s t r u c t u r e c o n t a in i n g a n a l o g u e s a r e m e r c a p t o p u r in e t h i o g u a n in e a n d a z a th i o

p r i n e T h e s t r u c t u r e o f t h e s e a n a l o g u e s a r e s im il a r t o h y p o x a n th in e a n d g u a n i n e T h e s e

a n a l o g u e s h a v e s u lfh y d r y l / th i o l g r o u p a t p o s it i o n 6į o f th e p u rn i n e

r e s p e c t i v e ly
a ì J i ? r

・
Scanned by CamScanner
Scanned by CamScanner
C ) P Y R ıM ıD ıN E A N A L O G U E S
P y r im lo g u e s a r e t h e c o m p o u n d s t h a t in h ib i t t h e e ıız y m e t h y ın i d y la te s y n th e ta s e ,
i d in e a n a

e n z y m e r e s p o n s ib le f o r c o n v e r s i o n o f 2 d e o x y u r id y li c a d d t o t h y m i d y li c a c id f o r D N A
'

s y n t h e s is I n o th e r w o r d s p y r im id in e d e r iv a ti v e s b lo c k t h e a c t io n o f t h w d y la te s y n th e t a s e
(1 S ) a n d in h b
i it t h e s y n t h e s is o f D N A

th t s p la y im ı t h
e sy s te m s a n p o r ta n t r o e in r e p li c a t io n a n d c e ll d i v is io n t s w w w e is
e
ib le fo d t iv t h y la t io f d U M P (d P h o s p h a t e ) t o y ie ld
re sp o n s r r e u c e m e n o e o x y U ń d in e m o n o
d T M P (d e o x y 1h y m i d in e M o n o P h o s p h a te ) w h ic h is u s e d f o r th e s y n t h e s is o f D N A
th e c la s s ic a l e x a m p le s o f t h is c a te g y 5 H d l, f lo id in d b in
o r m e u o ro u r a x u r e a n c y ta r a e

H O H z H O H z

Ħo x u r id ı
n e

5 f lu o r o u r a c il is d e s ig d to b lo k th
n e c e c o n v e r s io n o f u r id i n e to th y m i d in e T h e 5 F lu o r o
u r a c il i s d iff e r fr o m u r a c il t i t io 5 h
a p o s n flu in
p la c e
w e r e o r e a to m r e th h y d
il
e r o g e n a to m o f
u r a c T h e c a r b o n f lu o r in e b d is tr o n
o n s g e r a n d le s s s u s c e p t ib le t o e n z t ic ıe a
c o m to b h y d
y m a c v a g e a s
p a r e c a r o n r o g e n b o n d
O n p a r e n tr a l a d m i n is t r tio f fı
a n o o x u r i d in e it c o n v e r ts in t o it s t iv e
a c m o n o p h p h te
,
d ń tiv e h ic h o s a
e v a w is p o te n t c o m t i t iv e in h i b it o
p e r o f T S e n z y m e

a s . X t io . . . . . _ ń b o s e o r d e o x y r ib o s e m o ie t y h a s p r o d u c e d u s e ń ll d r u g s s u c h
S tr tu ll y
u c r a
y t a r a b in e is c y t o s in e a r a b in
c
in d
o s e s te a o f r ib o s e s u T h ly d i ff e
e n c e in s tr c tu e is t h e e g e r e o n r
p im e ń c h y d r o x y l g r o
u r
u p a t 2 '

p o s it i o n o f p to s e
m u s t b e c o n v e r t e d in t o i ts m o n o n h n n h = t o
e n s u g a r C y a r a b in e
r l

Scanned by CamScanner
Scanned by CamScanner
 H \z T R z

D r 彆 N a ・ e 四 国 国 ı 図 生 困 风
D o x o r u b i c in C H 0 0 H H O H H
3

D a u n o r u b ic i n C H 0 H H O H H
3

E p ir u b i c i n C H O O H O H H H
,

Id a r u b i c in H H H O H H

O c 4
H s ı C F a
V a lr u b ic in C H O H O H
.

D o x o r u b ic in a n d d a u n o r u b ic i n d if f e r o n ly b y a s in g le h y d r o x y l g r o u p a t p o s iti o n b u t
t h e y h a v e ? f e r e n t c li n i c a l a c ti v ity D a n t ır u b i c in h a s b e e n u s e d in t h e t r e a t m e n t o f a c u te
le u k a e m i a s w h e r e a s d o x o r u b i c in h a v e c y t o t o x ic a c t iv i ty a g a i n s t a w id e r a n g e o f s o li d t u m o u l s

1 ) D a u n o r u b i c i n

T h i s a n tib i o tic i s o b t a in e d fr o m s t r e p t o m y c e s p e u c e t iu s o r S c o e r u le o n ıb id ū s

P r o p e ń i e s I t is a n o r a n g e r e d h y g r o s c o p ic a y s t a 】】i n e p o w d e r w h ic h i s ħ e e ly s o l u b le in
w a t e r s t o r e d i n a i r t i g h t c o n t a in e r a n d p r o t e c te d fr o m li g h t I t is r a p id ly m e t a b o l is e d in li v e r
d t e d i t it s h y d l d b i in o l w h ic h th e b k th
a n c o n v e r n o r o x y a n a o g u e a m o r u c ń u r r e a t o e a g ly
c o n e I t is e x c r e t e d in u r in e a s u n c h a n g e d d r u g
M e c h n i s m o f A c ti o n D a u n o r u b ic i n in t e r a c ts i th D N A b in t e l t io d in h ib it
w y r c a a n a n
th e m a c r o m o l e c u l a r b io s y n th e s i s a n d in h i b it t h t o is n h i h l il s in
s e p o o m e r a s e w c r e a x s s u p e r c o
D N A t r a n s c r ip t i o n

U s e D a u n o r u b i c in is u s e d f o r a c u t e m y e l id le k i h i lo g le k i
o u e m a c r o n c m y e e n o u s u e m a
a c u t e lm y p h o c y ti c le u k e m i a n d k a i
a p o s s s a r c o m a

2 ) D o x o r u b i c in
D o x o r u b i c in is o b t a i n e d f o m S t iu S l b id
r p e u c e s o r c o e r u e o r u u s

s to r e d in a ir t i g h t c o n t a i n e r I t i s g iv e n in t r a v n e o u s ly a n d m e ta b o li s e d in l iv e r in to i t s a c t iv e
m e t a b o li t e d o x o r u b i c in o 1 I t is m a in ly e x c r e t e d in b il e

Scanned by CamScanner
A n il N e o p la ı t lc A g * n u

U s e s

1 It is u s e d in th e tr e a tm e n t o f c a r c h o m a o f h e a d n e c k c e r v ix v u lv a a n d p e n is
,

2 I t is a ls o e ffe c t iv e in H o d g k in s a n d n o n H o d g k i n s ly n ıp h o m a a n d g e r m c e ll M m o u r s

o f t e s t is a n d o v a r y

m N T P R O D U C T S I
H e r b a l m e d i c in e s a r e im p o r t a n t i n th e p r e v e n tio n a n d t r e a t m m t o f c a n c e r D r u g s d e
ń v e d f r o m p l a n t s a r e o f g r e a t i n t e r e s ts a s s y n t h e ti c d r u g s h a s v a r i o u s u n d e s ir a b le s id e

e ffe c ts P l a n t d e ń v e d d r u g s h fe w
a e r
v o r n e
o s i d e e ffe c ts C a n c e r c e u s a r e s t ıs c e p tib l e t o

c h e m o th e r a p e u ti c d r u g s b u t th is ıe d to d if f e r e n t ty p e s o f t o x ic i t i e s i n e b o d y T o a v o id
t h e s e p r o b le m s n o w a d a y s v a ū o u s th e r a p ie s fo r th e tr e a b n e n t o f c a n c e r u s e s p la n t d e r i v e d
r o d u c ts T h e r e a r e f o u r ty p e s o f p la n t p r o d u c ts u s e d a s a n ti c a n c e r T h e s e a i e
p
a ) V in c a a lk a lo id s (V in c r is ū n e a n d V in b l a s t ii n e )
b ) E p ip o d o p h y llo to x in s (E t o p o s id e a n d T e n ip o s i d e )
c ) T a x a n e s (P a c li t a x e l)
d ) C a m p to te c in d e r i v a tiv e s (C a m p t o t e d n a n d ir i n o t e c a n )
V i n c a A l k a l o i d s : T h e s e a lk a l o id s a r e is o la t e d fr o m th e p a in ń Ĥ n
i p la n t (C a th a r a n th m

r o s e u s ) V in c a r o s e a

T h e s e a lk a lo i d s h a v e t w o b a s ic m o i e t ie s

1 ) C a th a r a n t h i n e (I n d o l e c o n t a in in g m o ie ty )
2 ) V in d o li n e (I n d o li n e c o n t a in in g m o ie ty )
V in c r i s tin e a n d V in b l a s t in e a r e m o s t c o n u n o n ly u s e d a ık a l o id s in c a te g o r y
t h e b a s ic s t r u c h u e o f v in c a a lk a l o id s is

° H
r Ţ ・ 2 H s

H Ķ

H C O

V in i t in R \
H O
c r s e R ?
W R ?
W
V in b la t in R r
H 3 f W
s e R z R W

Scanned by CamScanner
A n '" N " \ A g ' "

ıß } tď # Ą ı ņ n N E o u s / W
1 J L I Ð P ı « \ ı ı ı

C l N H s
\ J ł
P t

C I N H s

IU p A C N a m e C is D ia n u n in e d ic h ] o r o p l a t im ım ä j

in i t ig h in d te c t d fr m li g h t I t is e ffe c tiv e b y in tr a v m o u s
in w a te r k e p t a r t c o n t a e r a n p r o e o

山 村 村 s t r a t io n a n d e x c r e te d in u ū n e
a
C i s p l a t in d D N A b y t h r o s s l in k s o r its a c ū o n is s im il a r
M e c h a n i s m o f A c ti o n a ın a g e e c

t o a l k y l a t in g a g e n ts

d in t m ts f i e r s in c lu d e t e s ti c u l a r c a n c e r e s o p h a g e a l
U s e I t is u s e t r e a e n o v a r o u s c a n c

b in h ım o r s o v a r i a n c a n c e r h e a d a n d n e c k c a n c e r b r e a s t c a n c e r
c a n c e r r a , ,

2 ) M it o t a n e

团 团团 国画 四 国 团 团
C I

I U p A C N a m e 1 ,
1 (D ic h l o r o p h e n y 1) 2 ,
2 d ic h l o r o e th a n e

ti I t is h it lo l d h i ltin g p o in t 1 7 1 t o 1 7 2 F I t is l e s s
p r o p e r e s a w e c o r e s s p o w e r a v n g m e

lb l e in w a te r b u t s o lu b le i n e t h a n o l c a r b o n t e t r a c h l o r id e a n d is o c t a n e o n o r a l a d m in i s tr a
s o

t io n m i to t a n e i s m e t a b o li s e d in liv e r a n d c o n v e r te d in t o it s d ic h l o r o p h e n y la c e t ic a c id o r its

m o n o a n d d ih y d r o x y la t e d d e r iv a t iv e s

M e c h a n i s m o f A c « o n I tS m e c h a n iis m o f a c tio n i s u n ım o w n b u t it i s b e li e v e d th a t it
d ifi t h ip h l t b l is f te r o id s a s w e ll a s d ir e c tly s u p p r e s s in g th e a ? e n a l
m o e s e p e r e r a m e a o m o s

c o r t e x

U s e M i to t a n e is d e r iv a t iv e o f d ic h l o r o d ip h e n y l t r ic h l o r o e th a n e (D D T ) w i th a n t i a d r e n o

c o r tic o id p r o p e r ti e s I t i s u s e d in t r e a t m e n t o f a d r e n o c o r t ic a l c a r c in p m a a n d c u s h in g s s y n

d r o m e

Scanned by CamScanner
了
區區電国 園
国
V. .Dilat.. W ibire . dNl￠
r.t. )

m d- Ch- d E】
ba .

Anw pectoris also know n as m yocardialischaem ia in w hichflow ofbloodto the heart

is notable to m eetthe m etabolic dem an ds ofthe heartfor oxygm This condition occurs due
to one or m ore ofthe hearts arteries are narrow ed or blocked The sym ptoı ns in clu des
'
.

severe su bstem alP radiati ngto the leftshoulder an d alongthe Oexor surface ofthe left

aīnt Angi
.
na is a sign thatsom eone is atincreased risk ofheartattack cardiac u restor
,

sudden cardiac death .

ns in the follow in gm anner

Angina is categorisedon the basis ofits cause and sym ptoı
nenta1stress or physim l
1 Classicalangin a In this type anginalattaçk occurs due to ı
.

exertion The depression ofST \ entoccurs in ECG

. .

2 Unstable angina Blockage ofcoronary artery (atherosclerosis disease)is the m ain

.

factor for an gina and attack occurs by vasospasm .

3 Varien tan gina Itoccurs due to vasospasm ofcoronalyvessels gen eranyin the m om
.
-

in g and m ay n otbe associated w ith severe atherosclerosis The elevation ofST se

.

m entoccuRs in ECG The drugs used in the treatm entofangina \ toris are dassffied
.

as follow s

AN了IAN GINAL DRUGS

Scanned by CamScanner
A n il A n g ın a ı

n itr ic a c id a n d s u lp h u r ic a c id

ÝH P "
ÝH P N C
C H O H q ・
?H O N q
C H P H C H O N C
G ly c e r in N it r o g ly c e r in

N o g ly le il ith b u r n i n g ta te It is th ic k
p p e r tie s
r o i tr c e ń n e is a c o ıo u r s s o w a s w e e t s

b le e x p l o s iv li q u i d h ic h is li g h t ly lu b le in w a te r b u t s o l u b le in o r g a n i c s o lv e n ts
f la n u n a e w s s o

r a p i d ıy a b s o r b d ír o m r a l m e ll s b y G I T N i tr o g ly c e r in is m e ta b o lis e d b y
It is e o u c o s a a s w a

i to i t d d i i t te d iv t iv T h e s e d e r iv a t i v e s h a v e le s s
r e d u c t a s e e n z y m e n s m o n o a n n r a e r a e s

v a s o d il a t i n g p r o p e r t y th a n t r in itr a t e

M e c h a n i s m o f A c tio N i t r o g ly c e r i n
n is c o n v e r te d N itr ic
to O x id e (N O ) w h ic h a c tiv a te
la d t i ın
la te th e t h e s is o f G ħæ h ic h t h e n a c t iv a t e s ie o f p
y la t s e s s y n c w a s e r s r o
g u a n e c y c a n u

t e in k in a s e d e p e n d e n t d e p h o s p h o r y l a t io n s o f t h e m y o s in lig ht
c h a in o f s m o o th m u s c le s T h e

b e n t r e ıe a s e o f c a l c i t ı ın io m r e s u l ts in th e r e la x a t io n o f s m o o th n iu s c le c e lls a n d v a
s u q s e u

s o d ila ti o n

fmių ii
ı r it e s a n d mN it r a te s l

N O
G T P
P te in k in G
r o a s e
G C u a n y ıc y c ıa s e
( In a c t iv e ) A c t iv e (G C ) ( in a c t iv e )

C G P

P r o te in k in a s e
(a c t iv e )

y M o c in L C
I M y o s in L C
p h o s p h a te ,
(C o n tr a c t io n ) (R e la x a t io n )

ls e s

1 It is u s ed in th e tr e a m te n t o f a n g in a p e c t o r is ,
h e a r t f a il u r e a n d m y o c a r d ia l in fa r a c tio n
in th e fo r m o f s u b li n g u a l t a b le t , in t r a v e n o u s ly a n d tr a n s d e r m a l p a tc h e s a s it r a p id ly
a b s o r b e d b y th e s k in

2 I t h a s b e e n u s e d a s a g e l a t in iz e r f o r n itr o c e ll u l o s e a n d a s a p r o p e ll a n t li k e c a r d it e a n d
b a llis ti t e

Scanned by CamScanner
 t l A n g ln a l
A n

b id e d in itr a t e is s y n t h e s iz d b in t le la d h y ? tio f o r b i « O l in t o
I s o s o r e y e r m o c u r e a n o

b id e b 1 ħ ır i c a c id a d ń th in te r a c t io f h b ix t u f
y l
s u n t e o
is o s o r y ır e r n o w o y ? o x g r o u p s y ın r

a c id a n d s u l fu ń c a c id
n i tr ic
p r t ie s I t is a w h i te c r y s t a l l in d lig h t ly lu b le in te r I t is e x p io
r o p e e p o w e r ,
v e r y s s o w a

d s e n s i tiv e to h e a t s o it is d ilu t e d i th la t i to ı th ita b le in e r t

s iv e a n w c o s e m a n n o r a n y o e r s u

t I t is s to r e d in tig h t ly c lo s e d l ig h t r e s is t a n t c o n t a in e r b e lo w 1 5 o
c I t ın a y c o n t a in 1 %
d ilu e n

n i u m p h o s p h a te a s a s t a b il i z e r
a in t m
o

I s o s o r b id e d in i tr a te i s r e a d ily a b s o r b e d fr o m o r a l m u c o s a s k in a n d G L T I t i s m e t a b o lis e d
d e n i t r a t io n i n t o I s o s o r b id e 2 m o n o n it r a t e a n d is o s o r b id e 5 m o n o n itr a te B o th m e ta b o
b y
h a v i n g v a s o d il a tin g a c t iv ity a n d le s s lir t ta b l is th ĵ o T b i d e d in it r a t e
l it e s a r e s p ? s m e o m a n s o s

h i f A ti o I b id d in
M e c a n s m o c n s o s o r e d in i tr a te a c ts s im il a r t o n i tr o g ly c e l i n e b y p r o u c g
N o
U s e s I t i s g iv e n a s s u b l in g u a l o r c h e w a b le t a b le t in t h e t r e a t m e n t o f a c u t e a n g in a l
k I t is n o t e ffe c tiv e o r a lly b e c a t ıs e o n s e t o f a c t io Ė o m 1 5 t o 3 0 m in u t e s I t h a s
a t ta c n r a n g e s

a ls o b e e n a p p l ie d t o p ic a ll y a n d c a n b e g i v e n b y in t r a v e n o u s in ń r s i o n

D I P Y R ıD A M O L E
5 )

中
团 团 团 团 团 团 团 团 ■ 冒 网 团 团 C H 2 C H 2 0 H
ノ

ī +
y k
N
c . . c H . O H
H O H C H C

H O H
z

C H
2

C
\
/
N A N A N

z 2

I U P A C N
Ů
a m e 2 2 2 2 [ (4 8 D ip e p r i d i n o p y r i m id o [5 4 d ]p y r i ın i d i n e 2 ,
m y l)
d in it r i o l] t e t r a e t h a n o l
P r o p e r ti e s : I t i s a b r ig h t y ll c r s t l lin e d in l b le in t I t is in m
e o w y a p o w e r s o u w a e r c o

p le te ly a b s o r b e d f r o m G I T I t i s m e t a b o li s e d in li v e r b y g lu c u r o n i d a t io n a n d e x m t e d i n
t h e b ile
M e c h a n i s m o f a c « o n D ip y r id a m o le a c t b y t w o m e c h a n is m s

a ) I t i n h ib its t h e p h o s p h o d ie s t e r a s e e n z y m e th a t n o r m a lly b r e a k d o w n c A M P i h d c G M P
b ) I t in h ib it s t h e c e ll u la r r e u p ta k e o f a d e n o s in e in to r e d b lo o d c e 】1 s , e n d o th e li a ı A n d
p la t e le t s le a d in g t o in c r e a s e d e x t r a c e ll u l a r c o n c e n t r a t io n o f a d e n o s in e

U s e s

1 I t is u s e d t o d il a t e t h e b lo o d v ė ş s e ıs w i th c o r o n a r y h e a r t d is e a s e

2 I t is a ls o u s e d to lo w e r p u lm o n a r y h y p e r te n s io n

Scanned by CamScanner
Scanned by CamScanner
A n tl A n g ın i ı

3 ) D ıL T I A Z E M H Y D R O C H L O R ID E
O C H a

Ð V
O
,
H c Ł

C H a
/
ėH z C H 2 F
C H a

p r o p e r tie s I t i a a w h i t e c r y ß t a ] ] i n e p o w d e f ı f r e e l y a o l u b ]e i n w a te r a n d a to r e d in w e n
c l o s e d l i g h t r e s is t a n t c o n t a i n e r I t i8 r a p id l y a b a o r b e d a n d m e t a b o l is e d b y f ir a t p a s $
l ia m b y d e a æ t y l a t i o n , o x id a t i v e O a n d N e m e t h y ıa t i o n s a n d g a tio n o f p h e n o ł ic m
艸 e

t a b o li t e a o f t h e v a r io u s m e ta b o lite s d e a c e t y l d il t ia z e m i s p h a n i ia c o b g i c a l l y a c t i v e

M e c h a n is m o f A c t io n I t i n h ib i t s t h e i n f l u x o f e x t r a c e l l u l a r C a c r o s s m y o c a r d ia ı a n d
v a s c u la r s m o o th m u s c le b y i n h ib i t i n g i o n « o n t r o l g a t e d c h a n n e ı o r i n t e r f e r in g w i łh th e r »

le a a e o f c a l c i u m f r o ııı s a r c o p 】 a a m i c r e t i c u l u m w h i c h r e s u l t s i n d i l a t i o n o f c o t i【M a ı y a n d r y
te m ic a r t r i e s
U s e I t is t m e d to tr e a t h y p e r t i o n a n d a n g n ia p e c to r is

4 ) N ıF E D ıP IN E

I u p A c N a m e : D im e th y 1 2 6 d im e t h y l 4 (2 nitrophenyl1 m y d r o p y r i d i n e 3 c a p
b o x y la te
P r o p e r t ie s : N i f e d ip in e is a y e llo w c r y s t a llin e p o w d e Ļ p r a c t ic a l l y in s o ıu b l e in w a te r
a n d p r o te c t e d fr o m li g h t I t is n o t a n it r a t e b u t i ts itr g r o is ti a l f o r its a n ? n g in a l
n o u p e s s e n
e f fe c t I t is a b s o r b e d e f f ic i e n t l y a fte r o r a l a d m in is t r a tio n a n d m e ta b o lis e d b y l i v e r in t o i ts
in a c t iv e m e ta b o l it e N i f e d ip i n e is e x c r e t e d tr f h d d in in
a s a a c e s o u n c a n g e r u g u r e

m e c h a n is m o f a c t io n l ts a c t io n is s im il a r to o th e r c a lc iu m c h a n n e l b lo c k e r s i e it
in h ib i t s th e in f l u x o f c a lc i u m io n s th r o u g h L ty p e c a lc iu m c h a n n e ls
U s e s

1 It is ū s e d in m a n a g e m e n t o f h y p e r te m io n It h a s n o a n t ia r r h y th m ic a c ti v i t y
2 I t is d
u s e in p r o p h y la x is o f a n g in a p e c to r is

Scanned by CamScanner
Scanned by CamScanner
M U L T ıP L E C H O ıC E q U E S T IO N S

Q 1 M e c h a n is m o f a c t io n o f n itr a te is
a ) S t im u a lt e s g u a n y la te c y c la s e b ) Þ b ıo c k e r s

c ) C a ıc i u m c h a n l b lo k d ) ib i ts
I h p h d
n e c e r s n o s p h o ie s tr a s e
:
Q 2 T h e a n ti a n s i n a l d r u g th a t i n h ib it s p h o ı p h o d ie ı tr a s e i»
a ) N ife d i p in e b ) ls o s o r b id e d in i tr a te
c ) D ip y r id a m o le d ) A ir i
s p n

9 W n ic h o f th e f o ll o w in g d g b t t d il to
Q r u e o n 吕 o v a s o a p

a ) D ip y r id a m o le b ) 】s o s o r b id e d in it r a te

c ) V e r a p a m il d ) B o th a ) a n d b )
4 W W C h o f th e f o u o w in g a n ti g in l d f l f t t t f id ia
Q a n a r u s u s e u o r e m e e n c y r e a m e n o c y ı n e p o o n
in 8
a ) A s p ir in b ) A m y l n itr ite

c ) D in r id a m o le d ) G ly c e r y l tr in i tr a t e

Q 5 W h i c h o f th e f o ll o w in g la ihydro p W iđ in e d e d v a t i v
a ) N ic o r a n d il b ) N im o d ip i n e

c ) F e lo d ip i n e d ) B o th b ) a n d c )
6 W H ic h o f th e f o l l o w i n 8 s t a t t i f l i i tr t
Q e m e n s a s e o n o r g a n c n a e

a ) ıh e s e g e n e r a t e th e t ın s t a b l e n it r a t e s a l ķ in s it u

b ) O r g a n ic n it r a t e s a r e lipid s o lu b le a n d a r e w e ll a b s o r b e d th r o u g h t e s k in
c ) ıh e y p r e v e n ts o r r e t e r s e c o r o n a r y a r t e r y s p a s m

d ) ıh e s e c a n b e a d m in is te r e d b y s u b l in g u a l r o u t e

Q 7 M o s tly c a l c i m c h a n n e l b ıo c k e r a c t b y in h ib i t in 8 in f l w o f C a
a
i o n u g h
a ) p t y p e c a ıc i t ım c h a n n e ı b ) T W p e c a l c i c h a n n e l
c ) L ty p e c a lc it ım c h a n n e l d ) N t w e c a l c i t ım c h a n n e l

Q 8 V e r a p a m il b e ıo n g s t o

a ) 1 4 d ih y d r o p y r id i n e b ) B e n z o th ia z e p in e

c ) P h e n y l a lk y l a m in e d ) N o n e o f a b o v e

Q 9 T h e s e c o n d g e n e r a ti o n d ih y q >o p y r i d in e d r u g a a r e

a ) A m i lo d ip in e b ) I s r a d ip in e

c ) N i c a r d ip in e d ) A ll o f a b o v e

Q 1 0 W h i c h o f th e f o ll o w i n g d r u B i s n o t b e t o n 吕 ti s e c o n d g e n e r a ti o n d ih y d m p y r i d in h

a ) N if e d ip in e b ) I s r a d ip in ė
c ) F e lo d ip i n e d ) N im o d ip in e

A N S W E R S

Scanned by CamScanner
D lu re tlc s į iį gi!g
s o rb e
d is d is ta l c o n v o lu te d h l b u le b y c a tio n e x c h a n g e w h ic h is u n d e r th e c o n tr o l o f a ld o s t e r

o n e
T h e la s t a n d f in a l s it e w h e r e th e s o d iu m io n s r e a b s o rp « o n t a k e s p la c e is c o lle c tin g

H e re , s o d iu m io n s fr o m r e n a l t u b u la r flu id is c h a n g e d fo r p o t a s s im io n s a n d to a
tu b u le e x
t w it h h d
y r o g e n io n s fr o m b lo o d
le s s e r e x te n ,

Tı te h ı u
b le n o r m a lly r e a b s o r b o v e r 9 0 % o f t h e g lo m e r u la r lil te r a te ,
th e re s t o f til e fııt e r a te

a n d
t u b u la r s e c r e tio n s p a s s in t o th e b la d d e r a n d a r e v o id e d a s u ï in e

c LA S S ı
F IC A T IO N
l ifie d fo llo
D iu r e t ic s a r e c a s s a s w s

D I U R E T IĊ S

1
C a r b o n ic T h ia z id e s L p D iu r e ti c s o r
o o P o ta s s iu m
A n h y d ra s e C h lo r t h ia z id e H i g h C e iıin g D iu r e ti c s S p a ıi n g D i u r e ti c s
I n h ib i to r s H y dr o c h lo r th ia z id e F u r o s e m id e S p i r o n o la c t o n e
A c e t a z o ıa m i d e H y? o flu m e t h ia z id e B u m e ta m id e T r ia ın e te r e n e
M e th a z o la m i d e yclothiazide E th a c r y n ic a c id A ın ilo ń d e
D ic h l o rp h e n a m id e B e n d r o ñ u a z id e

P ly th i a z id e
o O s m o t ic D i m e ti c s
In d a p a m id e M a m ito
ı l
C h l o r ta h d o n e U r e a
Q u in e th a z o n e G 1y c e r o l
M e to la z o n e l s o s o r b id e

IA ) C A R B O N IC 劇 酬 前丽 開 A S R 弱酉露面鬨 了了丫百日 叼
Scanned by CamScanner
 It h a s a ls o b e e n u s e d in th e t r e a e n t o f '
. d (d js o , d ' " f In n " " ]
.
3
i k e s s a n d n e u r o m u s c u la r r
a ttitu d e s c n d

強纛難縈聾看猕 は 吧
ー 一 。 ti i
锄 SW c tu r e A c « v ity R e la o n a h ip (S A R )

1 Th e m u b s titu te d s u lp h a m o y l g r o u
p is e ss e n tia l fo r th e äc tiv ity ・
a re
ca te g y
or l
lp h a m h
a tta c e d to tic r in
to th is T he o y g r o u p m u s t aro m a g
bo n " '
2 su
å be lo n gin g
g T
h e d ru
r u gs
f th e a c e ta z o la m id e s r in g n itr o g e n y ie ld s
'
riı
ı S u b s tittıtio n o f a m e th y l gro u p on on e o s
3
h ic h a ls o r e ta in c a r b b n ic a n h y ? a s e n i h ib it r a c tiv ity
m e th a z o la m id e w o
i de
n A c e tu o la n ı NHCO CH3
N HlSCz

e ta m id e rr ļ o !
{

iadjaz0l2 y1)a c
:

M ph a m
5 su 】 o yı
1..tħ
n ÆA c N a m e

S yn th e s is NHCO CHg
HS
NH2
C H l 3 m e th y l 1,thiadiaz0l 2 y lid e n e ] a c e ta m id e

\
(
IU ? A C N a m e N [5 (a m n o s u p o n y )
Hs i l h
uj lid h a v in g m e ltin g p o in t 2 13 5 o c It is fr e e ly s o lu b le in
p r o p e r tie s It is w h ite c r y s ta n e s o
th a z o la m id e is w e ll a b s o r b e d fr o m th e G I T w
h e n g iv e n o r a lı y Iť s m e ta b o lis ın
w a te r M e
d n ta in e r s a t 1 5 to
°
d i ll l
t o f e x c r e tio n is u n k n o w n It s h o u ld e s o r e
b t n w e c o s e c o
H ・ a n d ro u e

3 0 °C
i h ib ito r in th e c illia r y m u s c le
M e ch a n is m o f A c tio n p o te n t c a r b o n ic a n h y d r a s e n
It is a
tio n b y s lo w in g th e fo rm a tio n o f b ic a ŕ b o n a te
w h ic h r e s u lts in d e c r e m e a q u e o u s h u m o r s e c r e
C IS O z NHCO CHa w ith s u b s e q u e n t r e d u c tio n
in s o d itım a n d flu id tr a n s p o r t
io n s
U ses
1 It is u se d as a d iu re tic

2 It is u s e d in th e tr e a tm en t o f g la u co m a '
rv

NHa a c tiv ity

a n tin e o p la s tic /
.
3 It is a ls o h a v in g ť
f

A c e ta z o la m id e
Pertieı 1t ís a w hite a y s m 】in e p o w d e r , s 】
jg h tly s o lu b le in w a te r It is
a fta
ra pid ly a b s o rbe d
o ra l a d m in is tra tio n It is n o t m e ta b o lis e d a n d e x c r e te d u n c h a n
e d in
g u r in e
M e c h a n is m ofA ? on
1 Jt in h ib its c a r b o n ic a n hy? c a u s in g r e d u c tio n o f hy ? o
a se
P o rt in the tu b u le lu m g e n io n s fo r a c tiv e tr a n s
en w H ch le a d s to e x c r e tio n f bic a r b o n a te s o d itım
o
a n d w a te r , , p o ta s s ium
Z M e a n tic o n v u ķ a n t i
a c t v it o f th is d
hıy dra s e in the C N S
y ru g d e e n d s
p o n d ir e c t in h ib iti
hic h d e a e a s e cabon o n o f c a r b o n ic a n
, w
d io x id e te n s io n in h
t e p u lm o n a r a lv e o li i. T" t
U ie l :
O x y g e n te n s io
n y IU P A C N a m e 4,5-dicı dorc1 b e n z e n e d is u lp h o n a m id e " - " .

d h i p 22 8 5 C , s lig h d y
t o
P r o p e r tie s It is a w h ite o r a ı m o s t w h ite c r y s a
t llin e p o w e r a v n g m
1 It is u s e d in th e ı 】 k a lin e s o ıu tio n It is fr e e ly
c h a r a c te r is tic o d o r , p r a c tic a ly in s o lu b le in w a te r a n d s o lu b le in a
r e a lm e n t f
o g la u c o m
? ￡ţ:į s
-x3
a an d
se d '
1】
" '" .. . s o lu b le in p y r id in e , 1 N N a O H , in a lc o h o l a n d in 2 N s o d iu m c a r b o n a te s o lu tio n Its a b s o r p
' ' " t f. .
tio n , m e ta b o lis m a n d r o u te o f e x c r e tio n is n o t w e ll k n o w n
回国团团■
M e c h a n is m o f A c « o n Its a c tio n is s im ila r to a c e ta z o la m id e b u t c a u s e s e x c r e tio n o f le s s
; y n &
b ic a r b o n a te a n d m o r e c h lo r id e io n s a lo n g w ith s o d iu m io n s
四国■国虹匠
；

Scanned by CamScanner
D łu r ı u c ı

U C T U R E A C T I V IT Y R E L A T ıO N S H IP (S A R )
s T R

A t it io n 3 th e s u b s t it ti o n o f a 】k y Ļ c y d o a 】k y ! h a 】o a 】k y l a n d o r a R y l g r o u p s g iv e
p o s u

o te n t d iu r e t ic c o m p o u n d F o r e g C y c lo p e n th ia z id e
p

달し
X
: c H

C y c ı
o p e ra t h i a z id e

M d fo P ły t h i a id e
it io d 3 g h ly
2 t o z
S u b s tit u t io n a t p o s n a n g iv e s p o t e n c o m p o u n r e &

ł g N C H a
C H 2 s C H 2 C F 3

P o ı
y t h la z id e

3 S u b s t ih l ti o n o f a u r y l g r o u p a t p o s i t io n 4 g iv e s in a c t iv e c o m p o u n d
4 S u b s tit u t io n a t p o s i t io n 6 w i th c h lo r in e b r o m in e o r f lu o r in e g iv e M g h ly a c t iv e c o m

p o u n d F o r e g H y d r o f lu m e t h ia z id e

F
b H y d ro f lu m e l h ia z id e
・

5 A t i ti o 7 fr lp h (W S O ) is l fo d iu
p o s n e e s u a m o y l g r o u p z
e s s e n t ia r ï e t ic a c t iv i ty

Scanned by CamScanner
p ıu r e t ıc s

h lo r th i id e is u s e d d iu t ic d t ih te iv I t is a ls o u s e d t0 m a l ıa g e
U s e
C o a z a s r e a n a s a n a n y p e r m e

f lu i d a s s o c ia te d w ith c o n g e s tiv e h e a r t f a ih ır e /
e x c e s s ć

2 ) E
o t W
h i= a z i d e

N H S 0 !į : Ĥ i
Z 2 ・

į : c ı
A N

N 6 h lo o 3 d i h y d r o 2 H 1 2 4 b e . T h ia d ia z in e T s U ip h . n a i d e 1 1 d i o x
I U p A C a m e c r , , ,

d is h ite o s t h it t u in d e r li g h t l y
s s o lu b ıe in w a te f ,
r ti e s m s r u g w o r w e c r y s a e p o w
p r o p e
b d b t t
l t io f lk li h d id I t i f a ir ly r a p i d ly a b s o r e u n o
l u b l e i n d ilu t e s o u n s o a a y r o x e s s
s o
i " T

h l th ia z id b t it is e p o tm t th e
h i s m o f A c ti o n I ť s a c ti o n is s im il a r to c o r o e u ın o r
M e c a n

X X d ' ' " u r e tic o r a s a n a n t ih y p e r te n s iv e d r u g ' " S g i v e n w ith p o t ' " "

s io n

2 A b t h ia d i in 7 lp h id
f ıu th y 1 2 H 1
D ih n a ın e
y d 6
A C N 3 4 tń e n z o a z e s u o
I U P a m e r o o r o m e

1 ,
1 d i o x id e

h i te 】m h ite t a 】l i n d c ū c a 】l y in lu b le in t e r it
p e r tie
P lt is t s o w a
r o s a w o r a o s w c r y s e p o w e r p r a

is f a ir ly id ly b b d lly d d t b o lit e w h ic h b in d s t o th e r e d b lo o d
r a p a s o r e o r a a n p r o u c e s a ın e a

c e ll s I t is e x c r e t e d in u r in e \ ・

M e c h a n i s m o f A c tio n S im il a r to c h lo r o t h ia z id e

U s e I t is u s e d a s a n a n t jh y p e r te n s iv e a n d d i u r e t ic

4 ) C y c l o th ia z iđ e

: Į
ī i
Scanned by CamScanner
Scanned by CamScanner
d ir
§i

Scanned by CamScanner
 1
m 。 f沁 回国 国 国 团

Iu p A c N a m e 2 A ,
7 Tńamin &Phen y]Tete ńdine
p r o p ń i e s It is a w e a k b a s e I t is a y e u o w a y s t a l lin e p o w d e r .
s h g h a y s o ıu b ıe jn w a te r , ıū e p t
w e ll c lo s e d lig h t r e s is t a n t c o n t a in e r It is a b o u t 5 0 % a b s o r b e d w h e n g iv e n o r a u y e x te n
in ,

ly e ta b o l is e d a n d is e x c r e te d u n h g d in in d m e 吕e ķ m e ta b o li s ?
s iv m c a n e s o
e u r e a n

h is m o f A c tio n Its ti o is im il a to A ilo ń d h y d h lo r i d

M e c a n a c n s r m e r o c e

U s e It is u s e d a s 出 u r e t ic in t r e a tm e n t o f r e fr a c to r y o e d e m a

E ) O S M O T İ C D IU ? T IC S

O s m o tic d iu r e tic s b y in c r e a s in g
a c tsth e o s m o t ic p r e s s u r e o f t u b u la r ū u id T h e s e a g e n ts a r e

ħ e e ıy f tl t e r a b le a g lo m
t t h
e n d u s a n d e h a v e li m ite d t u b u la r r e a b s o r p t io n W h m th e s e a g e n ķ

a r e a d m in is te r e d in h ig h c o n c e n t r a ti o n , it r e s u lts in p a s s in g o f l a r g e q u a n t it y o f w a te r fr o m

th e b d y o in t o th e t u b u le a n d th is r e s u lt s in d i ıır e s is S o m e e x m a p le s o f o s m o t ic d iu r e tic s

in c lu d e U r e a M a n n it o l S o r b i to 1 Is o s o r b id e a n d G 1y c e r o 1 Is o s o r b id e a n d g ıy c e r o l a r e u s e d
m a in ly in g la u c o m a T h e s ite o f a c tio n o f o s m o tic d iu r e t ic s is p r o x im a l tu b u le , lo o p o f H e n te
a n d c o ll e c t in g t u b u l e

1 ) M a n n it o l
C H 2 0 H

H O C H

H O C H

H C O H

ĮX
H

I U P A C N (2 R 3 R , 4 4 5 R ) H
a m e e x a n e 1 2 3 ,
4 3 ,
6 h e x o l
P r o p e r ti e s It is a w h i te c r y s t a l li n d fr ly lu b le in te It is b b d in ll
e p o w e r e e s o w a r a s o r e s m a
t fr G i r A f t e r i n tr a v e n d is t r it is d
in t io n p id ly
a m o u n o m o u s a m a r a e x c r e te in th e u r in e
I JR

1 M a n n ito l is u s e d a s d ia g t ic t f k id ħ c t io
n o s a g e n o r n e y m n

2 I t is o fte n u s e d in th e t f b l d
m a n a g e m e n o c e r e r a o e e m a

3 It is u s e d to in c r e a s e u r in e v o lu m e in ti e t ith te l f a il u
p a n w a c u r e n a r e

Scanned by CamScanner
 A n tih y
p e r te m iv e D m gņ
: Į
r \ u p
4
tic s C en tr a lly A c tin g A
D iu r e g e n ts A d re n e r g ic N e u r o n
d iu r e tic s M th y ld o p a
1 1lia z id e
e
B lo c k in g A e n b
g
į} Loo d iu r e tic s
p
Ĵ ł G u an a be? A c e ta te
A g e n ts
G u a n e th id in e M o n o su lp h a te
G an g ıio n ic u o c lj n g
r A d rH ï e ï g ic N e u ro n B ı A g e n ts ': : '
.
e s u ]p h a "

侧
O\C。
EnzymemcE)1nhiMtD。 G ang li。
圧 ck . .、 P A ? en er
国
g ic B 1o c k u s
国 团团国 !
D ir e c t V d ila to
ec e p M r
r ı an t ag o n i st T
i mo
as o m
n g i oū e n s i n 1 r i me t a p h a n T l oı
D ia z id e
A dre n e r g ic R ece p to r B to c k e r s o x
tiA dm e rg ic ugs or M e c a m y la m in e A te n o lo l
￠ A n H y d r a la z in e
Î L a b e ta lo l
i M ĵ n o x id iı
E sm o lo l

Ê. ïį th e h e a r t 1
r '' " ţ \

: E n z ym e
Ô
In h ib it o rs (A C E ) L o s a r ta n T e r a z o s in

T im a z o s in

il V a ls a r ta n D o x a z o s in
E n a lp r
0 tw o c a tęg o r ie s ī e p r im a ıy o r e s s e n tia l h yp e r te n s io n in h ic h th e f h yp
w ca u se o e r tm C d e s a r ta n
is t Jm o w d d a ıy h }p
io n L is n o p r il an
n o n an se co n e r te n s io n in w h ic h ca u se is k n ow n

T e lm is a r ta n
be b d iv id e d h to
Q u in a p ń 1H C 1
su mū d (9o to 1 04 n m iH ) m o d e r a te (105 t 1 14
g o m m H g)a n d se v ere h B en a z ep ń1
te n s io n (12 o to ı 4o n m ı H g ) B e n ig n h yp e r
y p e r te n s io n in w h ic h th e d ia s to lic b lo o d r e s s u r e in
is p
a ea s e s a m a or j ıis k fa c to r ı
o r c o n e s tiv e h e a r t fa il
g u re t k s ro d
e an c o r o n a r y a r te r
y d is e a s e
Se v e r a Į Ta a o īs Ju be e n
ve c o n s id e r e d w h ch m a y c a u s es th e h y p e r te n s io T h e re
n m a y be ; D İU R E

loexcreteadequatedaÐ
amountofsaı
tand w a te r
i'FĦ ' X X X ï ï '
. '"

li】
ce
"

n a u se a
a " "

c o n s ti a tio n
p
,_ e g r a d u a lly

h ea d a che e tc
Ţ r te n s i-
- fo llo w

#￡ Iu re ti s (s e e ch a p te r 4 o n D iu re tic s )

Jt s h o u ld
Ħ o d u c e lo w e r c a illa r
p y r e s is ta n c e w ith o u t lo w e r in
g th e c a r d ia c o u tp u t
国 国區 。

团团■國■崇一 デ 強孰

Scanned by CamScanner
 e rt» n s iv D
A n tıH y p
e ru gs

s yn th e s is

Hacour cHzcoċ " .

T
Ho

f c a n p h w w c
'

M e th y \d o o p a te H O CH 2
ţ C O ロH !

i
M e lh w do pa
p ro p er tie s It is h ite o r a lm o s t w h ite c r s ta 】
a w 】in e p o w d e r fr e e ly s o lu M e w a te r a n d
y
s h o u ld
b e p r o te c t e d fr o m lig h t It is a n e th y l e s te r o f m e th y l d o p a a n d is p r e fe r ie d fo i

ţ
s u s e It is m e ta b o lis e d in th e C N S a n d a b s o ŕ b e d b
' in tr a v en o u y a n a m in o a c id i a c tiv e
' t
p o rt sys e m
M e c h a n is m o fA c« o n lt c o ıw e r ts in to a m e th y l n o r a dm a ain e w h į c h is p o te n t % a drm er

i
g ic a g o n s t r n i Ð. t
_ :ı
U s e It is u se d as an an tih y p e r te n s iv e a ge n t ・

o n id in
2) C ı e H y d r o c h lo r id e

m . Nm .
U M , m ßd . p a le w a m c u o ıid ,

IU p A C N am e 2 [(2 6 D ic h lo ro ) a m jn
p h e n yı o ] 2 im id a z o 1ĵ n e hydiodoride
p r o p e r tie s It is a w h ite o r a lm w p d e r fr e e ly s o lu b le in w a te r a n d i
o st h ite c r y s ta llin e ow

b d fr o m th e G I T a n d e x c r e te d in th e u r in e
s to r e d in w e ll c lo s e d c o n ta in e r It is w e ll a b s o r e
d
o r m e ta b o lite s i e p A y l o x y
d o n id in e a n d its o
a s u n c h a n g e d d r u g a n d p r o d u c e s tw o m a j

g lu c u ro n id e s
CN S h ic h lts in
e r g ic r e c e p to r in
re su
M e c h a n is m o fA c tio n It a c ts b y s tim ula tin g a j a d r e n w

tflo w fr o m th e C N S
d e c r e a s e in th e sym p a th e tic o u

ı
国团团团团团匯乡夏差 摹私・兹 ，
刍四国国四国团团国匿趙
Tį īį

Scanned by CamScanner
 e r te n a ı D
n tıH yp v e

區
ru ıı
A

m A D RE N
IĈ N E U R 쿄
o N B LO C K I
N G
l
T ıle d r u g s b e o n g in s to th is c la a s a
re r e s e r
AGEN
p in e
guaneMid gu m d re ı
j b e th a n id ĵ ıı
e an d
1) G u an ï th id ln e M o n o su lp h a te

q
bm A «e tM e
C m
C H 2C H
2 50 4

H c H3c o o Iu p A C N am e 1 [2 (P e r h y d r o a z a c in l yı
)e th y ı
1 gu a n id iī ı
e m o n lp h a te

Ħ
u s u

n Jp A c N am e
tchiorobmzylidene)amínoJ g u a n jd i n e m o n o a c e ta te

a Ħ ń ile o r a lm o s t w
It h ite a T a e s o lid h a v in g m e ltin g p o in t 2 2 7 c
M i e i an d
M h is ın c tio n
o f A G u a n ith id in e is t k
i t ly 25 % a b s o r b e d fr o m G İ T a n d m e ta b o lis e d b y th e li ec an
en u p b
n b le in Ħ a
so i Ē is Fp
a ï o x m a e
v er
th e
a
y th e a d r m e r g ic n e u r o n s w h e r e it r
p la c e s p in e p h r in e w h ic h r e s u lts in r a d u a i
n o re
M e c h a n is m o f A r t im I t a d s b y s tim u la tin g o-adrenergic r e c e p to r s w h ic h T e s u lts jn a
d l in h ib its th e r e le a s e o f n o r
g d e p n o t ı u i n e in iıs s to r a g e
s ite s It a s o e p in e p h r in e w h e n s m
o e a se d \ \ etic V to tħe h e a r t lc id n e y a n d p e r ip h e r a l v a s c u la tu r e y p a ū w tic f f i a r e s b m u la te d
T h e a d m in is tr a tio n o f d iu r e tic s w ith g u a n ith id in e is n e
c e s s a r y s in c e h
U ıe lt js ts e d m ū e a t h ig h b 】 o o d p n e ss u re i h id i i i d y p o tm s iv e e ffo a o f
gu a n t n e s a s s o c a te w i th s o d im a n d w a te r r e te n ū o n

U se s

1 It is u se d in tr e a tm
en t o f h
y p e r te r ıs io n
@ O M C B L O C K IN G A G E N
GA N GLı
2 It is a ls o d in th e to p ic a l tr e a b n e n t o f o
u se
p e n a n g )e g la u c o m a

二 二二
˜ ・ ― ― ' 一 p u ls e s "
隷 嚣y
. " e ' .. Pa ' " 3 G u a n ith id in e e h a s b e e n d to tr e a t d u o n ic
s n ip a 一 p a in c z u s e d b y c o m p le x r e g io n a l p a ĵ n
s y n d r o m e (p a in o f th e b o d
y u s u a J1y s ta r ts Er o m m g an d đ a n g e s to s k ĵ n
r e le a s e

Jo n g tr r
fr o m th e
p o s t g a n g lio n ic s y m p a th e tic n e r v e e n d in g s G . ^ g Į i. N i. B l. E k e
d ıie b 如 云 to x ic it a n d d e v e lo m e n t f
n ow
r. Ar a n d b o n e s)

y p o r e s is ta n c e a s w e ll a s e
iT a tic a b
s tn p tio n ir o an G L T B u t th e
y a re u se d ı o r s h o r t te r m tr e a tm e n t o f h e r te n s io n a s s o i
w ith d is s e a in y p c a te d 2)R e s e i p in e
g a n e n T s m o i a T r im e la p h a n is th e d r u o f h i
g c o c e w h ic h is u s d
d u c e c o n tr o J transient ħ e to p r »
}p o te n s im Į t is g iv e n b
d r u g is M e c a m y s lo w in tr a v e n o u s in fu s io n T h e a n j
o th e r
ŕ

H 3
ca l
Ħ

Y ıH a
y l 1 1 1 7 a d im e th o x y 1 8 P (3 4 5 tr im e th h o x y b e n z o y lo x y ) 3 0
IU P A C N a m e M e th 20a -

y o h im b a n e 1 6 0 c a r b o x y la te

P r o p e r tie s It is a n a lk a lo id o b ta in e d fr o m R a u w o u ia s p e c ie s It is a w h ite o r s lig h tly y e llo w

u ı>

c r y s ta l w h ic h d a r k e n s o n e x o s u r e to lig h t a n d p ra c tic a lly in s o lu b le in w a te r I t is s to r e d in

M eca m
y la m in e p

Scanned by CamScanner
 Y
:

k
.

'
{

'"
H . H3
,
éH C H ' NHCH

d d c e c a r d ia c tp u t s y s to ū c a n d
p to ï s in b r o n c h i a n r e u
ou
m u s c le a n d a ls o w ith Pz a dren o rece

d is a to lic b lo o d p r e s s u re an d in c r e a s e p e r ip h e r a l v a s c u la r r e s is ta n c e
U se s
:
'
鷺蕊裳に黑ぽ
。 m ed ' " t h yp˜ i o d 他p 。
ザ 翩 章节
_ä Y °.
' "
"

is u se d ' ' . Tr e in fa n . ..
3 Its g e l f. R m "
;

豬
˜
Scanned by CamScanner
 LįĮĮ!
i

j
°
T
m
\
' " ' "
;
į . ・
D ru * s
Į L A 式会社 A n tı
ĎI? C T V A S 0 D
不ゼ芬鳥
圖
二 豪
台文卫認才； ' '
忑 二广 て 1
'
趨路国國認
' '

慧二ご
'" .

裟二名北裳ゴエ竺只
9Į ， .˜ 一

d p眾
。,

麗
。 . ..

l ズt l
。。 。 is ın o f A c « o n ī
It m a t b y a c tio n o ń
ressu r e ech a y
。 n ac
l in b lo o M th e la r g e c o d u c ta n c a lc im a c ßv a d
i h ia ts h a n ce
re s u
iu m c h an n e l o r a c tio n on r b o n ic a n h d
o es w o ta s s
ca
y r a s e in a ııo o h ) ) /
u sd e \
p m
1
u se s
1t is u se d a s v a so d ila to r in tr e a tm f h y p e r te n i
:
en t o

Ii
s on iT f
. E d to co u n te r h y p o g l c e m ia in d i
y sease s ta te lĵ k e in su Ľn o m a .
a c tin v a so d ila to r s
s id e a r e ų p ic a J d ir e c t g

】) H y d ła Ja z in e H y d r o c h lo ī id e
:
Ń y
N
v
N H z

团团园圃四回国
CI
cĮ : i y
NH2 t J \
J y )H

z in o p h th a la z in e h y d r o c
1 H yd ra h lo r id e
tU p A C N am e
6 (P ip e r id in 1 y 1) PWmidine2,4-diaminb3-oxide
Iu p A c N am e
d e r iv a tiv e Į t is a w h te o r a
i lm o s t w h ite c ly s ta llin e p o w d
n o p e r tie s It is p h
a th a la z in e er
M in f tr ia m in o p y r im id in e s y s te m 1t is a w h ite o r a in n o s t
id iıis N id e
p r o e r tie s o x o x o
s o Ju b le in w a te r a n d s to r e d n w e
i ll c lo s e d c o n ta in e r I t is r a p id ly a b s o r b e d fr o m G I T a n d p
b le in w a te r a n d s to r e d in w e ll c lo s e d lig h t r e s is ta n t
d er s lig h tly s o lu
c r y s ta p llin e o w
w h ite
u n d e rg o es ir s t p a s s m e ta b o lis m b y a c e ty la tio n a n d e x c r e te d in u r in e a s g lu c u r o n id e ın b
ı i ll b b d f th e G 1 T a n d m u s t b e m e t a b o lis e d b y h e p a
t \c
i e r It s
c o n ta n
w e a s o r e r o m
ta b o lite b li i g o n id e c a n tu
i i
t a n s fe r a s e to a c t v e m n o x
s u lp h o r
id il s u lp h a te b u t m a io r m e ta o te s u c u r

M echan is m o f A c tio n Į t is a s s u m e d th a t h y d r a la z in e a c ts b y d ir e c t R e la x a tio n o f v a s c u la r ı f

It is e x c r e te d in u r in e in its m e ta b o ite o r m
g a te i v a s c u la r
s m o o th m u s c le Jt a ls o lte r s th e c e llu la r c a lc iu m m e ta b o lis m a n d in te r fe r e w ith th e c a lc iu m i 1 t a c ts b y o p e n in g A T P s e n s itiv e p o ta s s iu m c h a n n e ls n
M e c h a n is m o f A c t o n
a

m o v em en t w ith in th e v a s a ıla r s m o o th m u s c le th a t a r e r e s p o n s ib le fo r c o n tr a c tio n lls

o o th m u s c le ce
sm
U s es
U ses
1 Jt is u se d to tr e a t M g h b lo o d p r e s s u re an d h e a r t fa ilu re id e ly d in tr e a tm t f h a ir lo ss
p ic a lly it is
u se en o
T o w

2 It is u se d in co m b in a tio n w ith is o s o r b id e d in itr a te fo r tr e a tm en t o f co n g e s tiv e H e a rt

fa ilu re
darci th e r a p y
3 It is n o t a ïir s t U n e th e r a p y fo r h y p e r te n s io n b e c a u s e it in c r e a s e s c a r d ia c o u tp u t an d
p la s m a re n in c o n c e n tr a tio n w M c h r e s u lts in flu id r e te n tio n
N itr o p r ııs id e
4 ) S o d ilm
2 ) D ia z o x id e
N a tF e (C N )sN 0 1 2H z D
z

o n tr o s y l fe r r a te m
i d ih y d r a te
IU ? Ac N a ın e S o d iu m p e n ta c y a n de
C 1 ts e o u s s o lu tio n
s o lu b le in a te r a qu
d d is h b r o w n p o w d e r fr e e ly
w
p r o p e r tie s It is re

HCI d e ta b o ūsed
d m in is tr a tio n an m
id a n d n itr ic o x id e a fte r a
fr o lig h t It is c o n v e r te d in to c y a n e
m
e n tia l fo r its an tih w e r te n s iv e
Ha i t
T h e n itr o s o m o e y i s e s s
b y th e liv e r y ie ld in g th io c y a n a te
ıU P A C N am e m 3 th y l 2 H
XĪ yd.
o ro m e 1 4 4 ben z o th ja d ia z in e 1 1 d io x id y l'
"

Y
"
e °' " - tiv a te s gu an
i. m o f A c tio n It is m e ta b o lis e d .. ' " w
.n

h d u r a tio n o f
tin i e
g h y p o te n s v
a g e n t W it a
a s a sh o r t a c
u se 1t is u se d in s e v e r e h y p e r te n s io n
a cū o n 1 to 1 0 m in u te s

T ī§
į
Scanned by CamScanner
 u n te B y in d u c in g v a so c o n s
tr ic tio n th is h o m io n e re s u lts in an in c re a se in b l' "
˧ ,

.
d v o lu m e an d v a sc u la r r e s is ta n
b lo o ce
w
h ic h r esu lts in in c re a s e
äo n ď d iu m w
! R e a b s o lp
so

e le v a te
b lo o d p le ss u 「e 勉力团团

(1 4 am in o ac id s )
A n g io te n s in o g e n
Lo w b lo o d p r e s s t ır e
R e n in
M
L O W so d iu m e x c re tio n C H , C H ıC H , C N N H ı

Decapeptide In ac tiv e )
A n g io te n s in I
A C E シ 田o 1ın d in lu n gs
M a le r e p r o du c tiv e t is s u e )

A g io te n s in /
n e

ero n

A g io te n s in m
n sm e tio n

(H e p ta e p tid e ) 3) E n a a p r il M
ı aıe a te

p e r ip h e r a l O H
N +
tio n

11
a r e te n
O c 3

į
R e s is ta n ce
ł ・
H yp e r te n s io n H 2c H 2
H yp e r te n s io In ac tiv e P e p tid e
F ia g m en ķ
IW ? 0 8°

İ
Y tıL Ţ
.
ll L d .. ..
b . N y \ 3 p h e n y l p r °f y
in Mb i tor s

E n a lp ī il R a m i r i】
p
co m p
et

B e n
itive l y bi nd s w i th

Q u in a p r il FOSinop
AC E an d inh i bi t t s a ti

d T r a n d o la p r il
i ty an d ' "t h' .
ţ
A
n ÆA C N "
. d , a t,
" īN 1S ) 1 E th . x y ..

, , an

Scanned by CamScanner
ン
ー

c H o
ー
っ
0

C = O

H C H 2

O C 2 H 5

C a n de s a r ta n
i łm q

T e lm is a i飞a n

ANT?NERGIC D RU G S o R A D ? N E R G IC ? C EPT O R B t Ħ ņ
Scanned by CamScanner
 ! y ?
區
冒
国

P ro pa n o \o \
!įv

CH
/ 3

X
ļ .
cH a

N a d o lo \

& C H C H 2N H

+lt: q
C H2 H, .C < \ CHs

. N C
A rn o lo l

P in d o lo \

Scanned by CamScanner
 )a 8 )7
)a 2 )ä 1

s r o ta l d o s a v
\
i tc e r iD )a
n a tr a s im le T )c n o e to n a e t r
r ! ţ￠ iW 3Q
ľ b a fo ı]A )d
'
ev o
n a tr a s o L )a lo lo m iT d n a en id M te n a u G
fJ a tr a s e d n a C )b Q đp la n E lid ix o n iM en id in o 1C fo se su dn a n o
to ig n 21 itc a fo se är e p o r p
n a e hT m s in a h c e m
tp e c e r 11 n i
sn e e r u tc u r ts e tit
g a tn a ro W 2Q
s ile ıa ts in o
:į : į Į ś/
lir p o t p a C )c s s a Jc
: e v o b a fo n A )d h c a e fo s e r u tc u r ts o w t ev ig d n a n o it a c ifis s a lc r ie h t h tiw s tn e g a e v is n e tr e p }ht itn A n ia lp x E 1Q
lir p o n s iL )
Į a
a lln jD
\ť
:
g u r d o tp si g o f e
n iw o 1ı ht fo en o S N O IT S E U Q R E W S N A G N O L
etatńplanE fo
ig n A )c
\\ 5 e to
m n is n
Ju n in e R )d
ig n A
,
n is n e to
1
c in w o1 Q lid ix o n im dn a e n iz a la r d y h ]o lo n a p o r p p o t p a c fo e r u tc u r ts e h t e tir W 6Q
į o p se r 8 i e d itp e p
g n iw o o f
1ı e h t fo h
a n o ū ibc sn o c o sa v to f e lb im s r o tib jh n iE C A n o e to n tr o h s e tir W 5Q
Tn O ū n e te i a N dn
e d ir o lh c o r d y h e ta p o d ly h te m fo s ise h lm g e h t e v iG 4 Q
iz a la r d y H )
a
en
Į o lo n e tA U 9 Q s in a h c e m s lí n ia lp ciE ?s ī o tib ih n i E C A e ia ta h W : 3 Q
h c ih w g u r d h T
e n o itc a fo m
y b e l c s u m h lo o m s r a lu c s a v e h t x a le r y ltc e r id 2 Q
川 叩 tp a c fo
ū a id e m m u in a h c e m s s u c s iD
iz a la r d y h d n fo
n o n o itc a
si e d o c 出 吐 fn m ez a itliD )c en a
lo lo n e tA )d Q
iG ? s tn e g a evittepyhitna e r a ta ? M 1
lp m
s ti e v
en id in o C )a
ı se axe e lb a tiu s h tiw n o ita c ifis s a lc
lim a p a r e v )b
g n iw l lo f e h t fo en O 8 Q S N O IT S E U Q R E W S N A T R O H S
ia r g o s la o
r e ts u d d n a en im n i d e su
b h ca d a e h
e n iz a la r d yH )c
n is o z a m ir T )d
T )a
5 N O TT S E U O W E ıV E R
n is o z a re
n is o z a x o D U ,
g o la n w e hT 7 Q
si n is o z arp fo e u a e o s
lb u ı re ta

)d ts in o g a tn a e n o r e ts o d 1A )c
)b d n a )a h to B

s c ite r u id p o
p y h itn
o L )b
s c ū e ıı1id
s c ite r u

n o m
id
m o
ed iz a ih T )a
c ts o m eh T 6 Q ダ
m aı
si tn e g a e v is n e tr e a n a sa d e su
e v o b a Eo llA )d lir p im a R )c lo lid e v r a C H v
:

p o t p a C )b lir p la n A )a
5 Q
m aı
si EC A e ? tib ih n i s g u r d ev is n e tr e p y h itn a e h T

P
e v o b a fo U A )d lo lo x a t e B )c

::
lo lo r p o te M )b
e r a ls i s r e k co lb c ig r e n erda Þ ev
ı
o lo

itc e le s
n e tA

e hT
)a
4 Q
CH HC
ī
n a tr a s o L )d lid ix o n iM )c
ť
lo lo m s E )b en ip e d e fiN )a
r sa h e l a ıu s o t yı
ıa c ip o t l Jń e a r 1 g u i d e v is n tıe p y h itn a g n iw 9 Q
e o u o f e h t fo e n 0
l im a p a r e V )d
e d is s u r p o r tin m u id o S )c
n a t r a s )b )a
lid ix o n iM
tg u r d o rp a s 2 Q
i g n iw o u o f e h t fo h C W W

ı1 e l c u n eı
o z a r te t e v a
h g g n iw 1 Q
o ı
ıo f e h t fo h c in w
S N o IT S E U q O H C
EC ı TL U M
ELP ı

g u rD e v ı tn A
pyH ı
s s n e tr e

Scanned by CamScanner
 '
t v
E c T ı
þ
ţ
Q u in id in e S u lp h a te
ť 1 t
o c a i n a m i d e Hy d r o c h l or i de §
. .
D ii 呷 yr a m id e r h 呷 h a le 梆 7 \ < 9
11 I
m en y tu in S o d iu m ł
N T

L id o c a in e H y d ro c M o r id e

T o c a jn id e Ni
: l H
M ex ile tin e H y d r o c h lo r id e ţ &
:
A ın io d a r o n e

: L o rc a in id e q r r
S o ta lo l C la s s I a C la s s Ib C la s s l c

Q u in id in e L id o c a in e E n c a in id e
lik e tr a c ts w h e n a n e le c tr ic a l im
H ea rt is a m īrs d e an d it w o r ks a pu m p H e art co n p u ls e p r o c a in a m id e P h e n y to in F 1e c a in id e
ıO m th e S A n o d e m o v e s a c r o s s it T ħe h e a r t p u m p s a n d b e a ts a t a r e g u la r p a c e a s lo n g a a T o c a ir rid e P
D is o p } r a m id e ro p a İe n on e
e le c tr ic al im p u ls e s tr a n s m its a lo n g iŁN o r m a l h e a r t b e a t is 6 0 10 0 tim e s p e r m in u te T h e te r m
a r r h y th m ia is a s ia te o f a b n o r m a i h e a r t r h tlm i a n d is c o n s is ts o f ir r e g u la r h e a r t r a te (b e a t
y )
a n b n o r m a ır p u la r it o r s o m e tim e s d is tu r b a n c e ĵ n th e c o n d u c tio n o f e le c tr ic a l iın p u ls e w H h
g y c
ca u ses \ in th e a c tiv a tio n o f a tr ia an d v en tr ic le s A r r hy th m ia u ltim a te m a k e s th e h e a r t
ı
le s s e fó c ie n t A rr h y th m ia a r is e s d u e to v a r io u s r e a s o n s hke
it 2 tia n g in a l d r u g s )

￡
lo l (R e fe r to u n an
) D is tu r b a n Ç pro pra n o
a ce jh th e g e n e r a tio n o r co n d u c tio n o f e le c tr ic a l im p u ķ e t' b lo c \ç s th . K ? c h a n n e ls m d p r o lo ° g §1l '
t T h' '" ge n
Cı' ' " II A g e n '
b) ln so m e d is e a s e d s ta te lik e
y o c a r d ia ıis c h e m iá h e a r t d is e a s e 】
m ik e h y p e r te n s io n e tc
T h e se d ru gs h a v e n o
e ffe c t o n N a c h a n n e ls Th ese a g ėn ts p T o lo n g s
16 e QT
"
'

A n tia r r h y th m ic d r u s a r e th e a e n ts w h ic h h e l s to r e u la te th e ir r
g g p g e g u la r h e a r t b e a ts +ı
a n d s lo w s d o w n th e h e a r t T ħe s e d r l b lo c k e r s đbtocJs m o ￡C a
h e a g e n ts a r e c a lc ilJm c h a n n e
an
u g s e ffe c ts e le c tr ic a l im
p u ls e c o n d u c tio n th r o u g h th e c la s s 1v A g e n ts T e s
h e a r t a n d e x c ita b ilit o f th e h e a r t A n tia r r h i l dr u gs)
y w w c d r u g s a c ts b y b lo c k in g N a a n d C a 2 + io n io n Fo r ex am p i e V e r a p a m ĵ l (R e fe r to a n tia n g n a
cha n n eı s o f th e m
s
y o c a r d iu m a n d in c r e a s e s th e tim e r e q u ir e d ı o r r e s to r a tio n a fte r a c tiv a tio n
D e p e n d in g u o n th e m o d e o f a c tio
p n a n tia i r h y th m ic d r u s a r e b r
g o a d ly c la s s iíie d in to liv e V a r io u s a n tia r r h y th m ic a g e n ts are
c la s s e s Th ese are Į f
!
C la s s I T ħe s e a g e n ts in te r fe r e ith N D \N E S U L P H A T E
N ı
t) q u ı
w a c h a n n e ls
C la s s I ıT ħe s e are p a dren e rg ic b lo c k e r s
C la s s m T ħe s e a ffe c t K e l s
C la s s ı
v m e c a lc iu m cha n n e l b lo c k e s
C la s s V a re m is c e lla n
d a c t b y m e c h a n is e o u s an
m o th e r th a n th e
a b o v e fo u T c la s s e s
C la s s I a g e n ts T h e s e a c ts b bl
y o c k in g N a + c h a n n e ts T h
bra n e s ta b iliz in g a e n ts T h e s e d e s e a r e a ls o k n o w
g ru gs d e cre a s
e s th e flo w
n a s m em
o f N a + in to th
e c e lls a n d h l in e ps

Ý
国画鼗粼 簸 ï
，
獺驪殲殲翻籤
Scanned by CamScanner
 ı ı
r fa
s e s
d e đ e a
th e s
is h ı
s p
+
B r N a N H z C C H
g » t ı]H

2 B ro m o p y r id i n e
C N
C N

c e to n it r lt e
p h e n y ıa

N H H S 0
O 2
2 4

D iis o p y ra m id e

U s e s

1 It is u s e d in th e tr e a t n n e n t o f v ? io u s ty p e s

2 It is a ls o u s e d in th e m a n a g e m e n t o f a tr i a l { ib

4 P H E N Y T O ıN S O D ıU M

O N a

Scanned by CamScanner
 ￠U A T M B O O k o f M e d ıc ï n a ı

t io o f a c t io n p o te n t ia l a n d h
th e d u r a n a s '
ħ is f A c t io n It d e a e a s e s " k
M m o f le
T
« ı n e

o n h e in i t ia t io n o f d e p o la r is a t io n
ľ c t

Ì , b p r im a r il y u s e d " " t ie p ū e p ? h th e tr e a t m e n t o f " " ty p - o f s e ih l l

ų
t a b s e n c e s e iz u r e s
e t cc e p
f r d ia c a r r h y h li n ia
】s d in th tr e a t m e n t o c a
2 I t is a o u s e e

R E F E R T O L O C A L A N A E S T H
5 ) L ıD O C A ıN E H Y D R O C H L O R ID E (P L E A S E E T ıC S
)
6 ) T O C A ıN ıD E

N H 2

H 3 C

N (2 6 d im th y lp h y l)
n Æ A C N a m ė 2 a m in o p r o p io n o 2 6 x y li d i d e o r e e n a la n in a m id e
m p e r t ie s I t is h i te s o li d h in g a m e l t in g p o in t o f 2 4 6 2 6 6 o
C 1 t is s lig h t l lu b ı
a w a v y s o
e
in te It t b li t jn th l iv to g iv in a c t iv e m e ta b o li t e s
w a r g e t s m e a o e e e r e

M e c h a n is m o f A c t io n It la r g e ly a ffe c ts N a c h a n n e ls b y b in d in g to th e in a c ti v e s t a te o f
N a c h a n n e ls a n d d e c r e a s e s th e a c t io n p o te n t ia l

U s e s

1 It is u s e d a s a lo c a l a n a e s t h e t ic

2 It is u s e d a s a n a n t ia r r h w W c

3 I t is a 】s o u s e d a s a s o d iu m c h a n n e l b lo c k e r

7 ) M E X I L E T ıN E H Y D R O C H L O R ID E

H
L ą łj : į ( ? Ļ1 1
i ￠
N H 2

H 3 C
H C I

IU ? A C N (W
a m e )) [2 (2 M im e th y lp h e n o x y ) 1 m e th y l e th y 1J a n jn h y d h l ń d
e r o c o e
ħ o p e r ti e s l t is m
a w te o r a 】m o s t w h i te t a l lin d
c i y s e p o w e r fr e e ly s o lu b le in w a te r it
g e ts m b o 】i s e d i n
e ta th l iv
e e r to g iv e a n u m b e r o f in a c t iv e m e ta b o ıi t e s It m u s t b e s t o r e d in a
Cl os ed o n t a i n e r te c te d fr
p r o o m li g h t

爨里 ■
Scanned by CamScanner
 b e lo įį 1
p ro p a fe n o n e n g e to v \

H ac i M ec h a n is m o f a c « n n o f s o ta 10 l is : Į XU
a ) B10CJS N a ch an n e l b ) B 1o d W ċ h a r ın e l
2 y la m in o )e th y l]P h e n y 1J m e th a n
cs

d x 2 (p r o p a n
(R S ) N [4 61 h y r o y
e l
) B lo c k s C ch a n n e d ) B10d«ers
IU p A C N am e c a

in a m e ltin g p o n
j t o f 2 0 6 2 0 7 C It is s o lu b le in w a te r l b)K ? ha n l
r ıo p e r tie s It is a w h ite s o lid h a v g )C ch an n e
a a c n e
:
i h u r in e
te d u n c h a n g e d n
t e
l d )N f abo v
c) N ť ch a n n e
It is n o t m e ta b o lis e d a n d is e x c r e
on e o e

m ila r to A m io d a r o n e
i i i e It in c r e a
o f a c tio n s s se s T h tia ırh y th m ic d r u g w iı
h lo c a l a n aes h e«c
ı ac ū o n is
M e c h a n is m o f A c tio n lts m e c h a n is m
e an
Q 7
i l id e { ; r tť T : ŕ ī
: T i
d ia c a ti p te n t a
a) v jl b)p ro c a in a m .
th e r e p o lu is a tio n p h a s e o f c a r
o n o erap am
c
t : ! 1
i n a n g in a d ) D ig o x in
u ses It is u se d in th e tr e a tm f c a r d ia c a rT h y th 】m ia h y p e r te n s o
en t o p e c to r is c) E n ca in id e

0 n e o h
f ı e o w in g h
fo 1ı av e su lp h o n am id e c h a r a c te r
Q 8 1 t ļ
ta lo l b ) Q u in id in e su lp h a te f ;
a ) So

R E V IE W Q U E S T IO N S
fĵ ĵ g < A N SW E R S

S H O R T A NSW ER Q U E S T IO N S
Q 1 W n a t a re an lia r r h y th m ic d r u g s ? W rite th e ir c la s s ific a tio n w ith ex am p le s
Q 2 W r ite \ th e s is o f D ü s 叩 戸 a m id e n
Į !

Q 4 W rite a s h o r t n o te o n c la s s m an tia r r h y th m ic a g e n ts
Q 5 D is c u s s m e c h a n is m f a c tio n f d a s s I a g e n ts a n d h o w th e s e a r e ń ir tħe r a c c o rd
o o c la s s ifie d
Ĵ n g to th e m o de o f a c tio n ?

= x e ı. v e , x d.

Scanned by CamScanner
 S ta tin (H M G C A du
m a s o re c ta s e iııh ib ito ı8 )
ım 1 e g M a s ta tin s iın v a s ta tin M e v a s ta tin
F ib r a te s (F a b ń c a c id deń v a tiv e s) e
g C 1o fib r a te c ip r o fib r a te
s a tin s
B ile a c id b in d in
3 g r e s in s c o le s ty r a m in e N ic o tiŊıic a c id c o \e s ū p o l
LO ï a s ta t in
G u g u lip id
F ib r a læ
?o ra te
M is c e D a n eo u s
A n tih y p e d ip id e m ic A g e n ts
cnolese
C o le s tip o ı

(f i S ta t in s F ib ra te s M is c e \ıa n e o 1ıs

C 1o ĥ b r a te le s t rr a m in
!' i i ;
t Ė o m h m i g theitegńty
o f th e c e ll w a ll H ig h 'e v e ls o f L o v a s ta tin Æ o e
q

o f h e a r t d is e a s e s Atherosclerosis ß ta tin C ip r o fib r a te N ic o tiï ıic a c id

; : ö tn o l (z u s E s atherosclerosis w h ic h js l h e m a j
o r c a u s e
a S im v a s
+ ť i
c c u m u la tio n a n d d e p o s itio n o f fa t d
i o f a r te r ie s d u e to a G fib r o z ĵl le s tip o l
1 s ø te h ì M c h th e r e is h a r d e n n g b M e v a s ta tin em C o
ği f d i m a n d la r g e e s A lo n g w ith th e h t d e p o s its th e r e is
a cm
p o s its in th e in tim a o m e u tin F fib r a te G g u u ip id
ib r o u s tis s u e s D u e to th is d e p o s itio n th e r e is
en o
A to r a v a s ta u
m u la tio m o f c h o le s tæ o l c e llu la r w a s
te s a n d ı
l ti i o f th e a r te r ie s H y p e r lip id e m ja is B fib r a te
d e m ea s e in th e lu m e n o f th ę a r t y th is r e d u c e s e a s c y Ħu v a s ta tin en z a

id in th e fo r m o f lip o p r o te m
in w h id r th e r e is in c r e a s e d p la s m a le v e ls o f lip s tin
se ń v a s ta
is th e r o o t c a u s e o f v a r io u s h e a r t p r o b le m s a s ít c a u s e s a
th e r o s c le r o s is L i i
i W p f
id s 1R e tr ig ly c e r id ie s a n d c h o Į e s te r o l c ir c u la te d ín th e b lo o d in th e fo r m o f L ip o p r o te in s
・

Ii p o p r o te in s a r e la r g e p a r tic le s (s lo b u le s ) c o n ta in in g a n o n p o la r c o r e s u r r o u n d e d b y a p o la r
c o a t o f 声 呷 細 lip id s D e p e n d in g u p o n th e s iz e a n d d e n s ity a m o u n t o f tr ig ly c e r id e s a i ıd o w n a s H M G C o A r e d u c ta s e in h
a ls o ı ib ito ï s a s th e s e d r u g s d e a ce a s e s e
T hese are m
c h o le s te r o l e s te rs h tħe c o r e JPOProteins a r e c la s s ffie d in to s ix c la s s e s ū tiv e ly in h ibitin g 11 e e n z p n e
le ve ls o f L D L an h
c o l e d
s te r o l in th e p a b y c o m p e

ta s e is th e e n z y ın e ir ı v o b r e d in M e
l M y io Ðıia on s ao w est y Iip o p r o te in s )
d e n s iı T r a n s p o r t T G (tr ig ly c e r id e s ) o b ta in e d C o A (3 h y d r o x y 3 m e th y g u a r y
l l t l co en z ym e A ) r e d u c
i t s e n t in m æ oA
tio m
b io s y n th e s is o f c h o le s te r o
l s ta tĵ n s h a v e th e s a m e la c to n e m o e y a s p r e

h t r s ite a n d c a iJs e s n
I M b itio n O f 1l e
Z V LD L N b y 【 D e n s ity Ľ ip o p r o te iıu ) Tra n sp o r t T G i
s ta t n s i ts e ıf b in d s to t e r e c e p o
o w
s y n th e s iz e d jn th e liv er r e d u c ta s e e n z y m e
so

3 Ci
n lo m ia o n rem n an ts F o rm ed fr o m C h y lo m ia en z y ņ re
on s & V I D L (a fte r lo o esin g tr ig lyc e s te r a t 14
e r id e s ) de f h e x a h y d r o n a p h th a le n e r in g w ith a m e th y l b u ty r a te
S ta tin s a re m a u p o
d ID L a n 【 e m ıe d ia te D e n s it L i o r o te i
y p p n s) F o r m e d fr o m C h io m ie r o n s & V L D L
fa ń e r lo o e in g iıig ly c n id e s ) y
5
6
L D L ? w D e n s it Ľ i o r
h d l m ig h
y p p o te iıu ) F o r m e d fro m ID L
densiy l ip o p r o te in s ) s yn th e s jz e d in th li
W X N A D pH (N ic o tin am id e A d e n in e D in u d e tid e P h o s p h a b ) '" "

h e lps in b a m o r tin e v e r & s m a ll in te s tin e it

p g c h o le s te r o l fr o m tis s u e s to th e liv e r

Scanned by CamScanner
 B o o R o fM e d - In a l
P /A 7m

ı A ,ï ￠
Am y ßh m lc D ru g=

' H a Jf R e d u c e d
ıi v&
HM G C
H
o A
;o r a c
- M
tiv a
ch
X , 九\
te s it w h ic h in tu m
・
r e Bu tts in
. h"
ı s . .
M a t e s o n w į ıh .

In c r e a s e d fa tty o x i? tio n a n d lip o p r o te in li

H a) pase a c tin
ity
q
b) In c r e a s e d W D L clearance a n d in c r e a s e d le v e ls f H D L in
H M G c o A o 1h e
i t h l w y
re d u c ta s e
c)
in c r e a s e n e c ea r an ce o f re m n a t
n p a r tic le s h Ī .:

HO O C

之三 二

：
i
! ˜ A ˜ 。˜
,一 一 。 。 。
M ev a ı
o n ic a c id

b lo c
k
O C O R
C [》 z

(A M ox y is o b u ty ń c ac id )

Ħ b r a te s re du ces th e
p la s m a le v e ls o f tr ig ly c e r id e s am ıc h o ı
e s te r ? It a ls o īe du ces li
n e

D L le v e ls an d in c r e a s e s H D L c o n c e n tr a tio n
W

C L O F IB R A T
E i

n ÆA c N am e 8-6 12 4 R J ltetTahydrhydroxy-6-oxo 2 H p )T an 2 y i]e th y 1] 1 n a ph C O O C H 2C H 3

th y J 2 m e th y b u t}r a te
CH a
P ro p e r tie s It is a w h ite m s ta l1in e s o Jid Jt is n on h v e r o s c o p ic in n a tu r e It is in s o lu b le
IU p A C N a ın e E th y l 2 (4 ūoro
cł phen o x y) 2 m e th y lp r o p io n a te
li a soh】 b le in w a te r 1 1 g e b fiy d r o v
p i o p e ń ie s İ t is a cıe a r c o lo u r le s s liq u id v e r y s g h y
i b u trpr ic a c id a ls o \m ow n as d o fib ń c
b lit h l p h e n o x y s o
s e d to g iv e a n a c tiv e e ta o
m e c o r o

.
ıi .
. M t y j'' " g the e? y me . M G - o A re d u c t as e an d in-
M ech an is ın o f A c tio n 1t is an a g o n is t o f p P
AR r e c e p to r a n d c au s es acū v a ūon o f th e

.
T1 " " d ' " trog h ig h p la s . 1" " f c h o l. "
re ce p to r

a , o I U se s
ip o p r o te in e m ia
n h ype rı
t o f ty p e 】
f p la s lip id s ) 1 It is u se d in th e tr e a tm en
a
1 in th e tr e a tm t o f h y p e r tr ig w c e r id e m ia
u s e ft ı
en
2 It is a ls o
r o l a n d lip o p r o
te in s
e ls o f c h o le s te
3 It is u se d fo r c o n tr o llin g th e le v

Scanned by CamScanner
 s e ta r b iF )b
n ita tS )a
n o e to n a e tń W 3 Q a e o h r r a id o tn e n b a e r e
f t ht n i d esu o s la s i t F 3
ts e lo h C a im e a n ie to r p o p ilr e p y h II e p y t fo tn e m ta e h e l łn
1o p its e lo h C d n a en im a re

2 Q l i d e s 】1 s i l1 2
s e it r e p o r p tir W
e ru tc u r ts e
s in a h c e m
lp d e ta v e le
m
ita ts a v o L fo s e su dn a n o itc a fo s le v e l io r e ts e lo h c aı
n sa e h t g n ic u d e r n
e t& r b ifo \C n j d e su s jĒ 1

a n o ū a c ifis s a lc e tń W 1 Q s e sU
t g n o le b g u Jd h c a e fo dn
e r u tc u r ts e n o
id ip il r e w h b n
s sa d a e o
c in a fo
S N O IT S E U q R EW SNA G NOL s d ic a e lib o tn i lo r e ts e lo h c fo m s ilo b a t a c d e s a e r c n i o t g n id a e l i b Ē h n i s j s tla s e ū b fo
n o itp ï o s a e
b R n o in a tla s e lib e h t r o f n o in a 1C fo e g n a h c x e s e s u a c s iıH n o ite ıc x e r ie iH s e su a c

3 Q
h ty h r r a ū W
n
h t y fis s a lC ?s g u Jd ta
c in ï n a era
se lp m ax e ė 1b a tiu s h liw m e
t h g il m o rf d e tc e to r p r e n ia tn oc th g it r ia n i d e r o ts e b* um n r e ta w h
s e ht e tń W 2 Q
en ĵn u r e ts e lo hC d n a lo p its e lo h C e ta r b ifo lC n ita ts a v o L fo e ru tc ıM

tr o h s e tir W 1 Q
s ro tib ih nii e s a tc u d e r A o M H n o e to n
p u o rg ııu ħm u m n a vr a m e ta u q
S N O IT S E U Q REW SN A TR O H S gn a h "
d iw remylopc e n ezn e b l y n i V ・w ts g n iv a h d . n is e r e " in A . is a b ,
ÌÏ :

S N O IT S E U Q W E IV E R

aimetorpopilrepyh fo 2
tn e m ta e r t e h t n id e m o s sd ip il fo s le v e l am sa lp secu d e r tI
s a im eaı
o r e ts e lo h c rep y h fo t n n id esu s i t1 l
em ta e r t e ht

.
į j

en ăm a Ħb s e \o h c fo ta h1sa em as si n o itc a fo m s in a h c e m sł n o itc A fo m s in a h ce M

1
m tI E N ïM A R Y T S E L O H C
r en ia tn oc th g it r ia n id e r o ts e b ts u
u b
m w s d n a r e ta w s bro sb a t lo pĤ e o c
ı
re tà w n ie m s n i s i 61 L ru tm n i ipocsargyh s da e b egn aro ro ey
1】 s i tI se ū re p o rp
h t ta ū ß s
w o
jjlıa d n a e fa s e r a
e se
e n a p o rp yx o 4 2 o ro
r em y lo p cc i tI e ħt
lh c d n ly h te id fo lo h c f o a t e m
ĥ ( a en ĵm a ir te ir e a s
o r e ts e
seh tnys u t sesaeni l
N
厂訂二 z
Hc H C N a avda n ia M s d ic a e lib ero m

Ł
e ı
a e se
hT
v
elbulosniretawerawdnasniseTnonamicaem lo h c f o
ses ae a n
i s d ic a e aB i
t
H
i d ip iI s re v n c l e c
n eh dn a
. m = lp e ht :

y lla c
e se hT
.snisergnidnibddaelibsuoi\.dudni--.
T
e ra s n is e r
o c
TSEL

ą=
L O P ı

s g u rD c ım h t
ıi t n A

Scanned by CamScanner
 B o o '"
pu 咝
运 周团日日目
°

Q U ES T
IO N S
A N T IC
IJ A G U L A N T S 8
>: c H O IC E
M u LT Ip L E
o lib r a
te
b) a

: Ţ- a) C o le s tip °
. .w in g d r u g
ıc b b y
d ) N ia d n
b iiI. " d d j" " 'T

Q '
XX con ect
d m g ls
'' "
h r g 】
e
￡ " " ・
n to a g e l a n d fo r m a b lo o d
ts is a p r o c e s s in w h ic h th e b lo o d g e ts c o n v e r te d i
a ) vastatin d ) A ll o f a b o
ve
C o a g u la n h u m a n s a s it
ım o w n a s c lo ttin g C o a g u la tio n is v e r y im p o r ta n t in
e s s s a ls o
日 月u v a s 妞tin
c lo t
T h is p r o c
I
Į d b l d l f th b d d i i ju r y a n d h e lp s in
o s ta s is i e
t n
ig
r e u c e s o o o s s r o m e o y u ï n g a n
F ib r a [e s a cb by i
a ctv at n in hem i (o b s t r u c tiv e
Q p Æ c e p to ī s l s b
4 U hıe ıťp
r f c o a g u la tio n c a u s e s b le e d in g (h e m o r r h a g e ) o r th r o m o s s
b ve D is o r d e r o
d )N o n e o fa o
c)Bo th a ) a n d b ) i u la tio n fa c to r s o r
d o ttin g
i h is p o ly m ep inlv e d in th e p r o c e s s o f c o a g u a tio n a n d la to w n a s c o a g
v o
A m o n g th e fo llo w in g w h c
a cp
to r s a
fe t d t a c tiv e
r e c u r s o r p r o te in s o r z y m o g e n s a n d a r e c o e r e o a n
Q 5 in n v
T h e s e fa c to r s a r e p
e
b) a io le s ı
yr a m
a) c o le s tip o l fa c to r s o f p ep t id e b o n d s T h e s e 2 \ to g e n s a r e o f tw o t yp e s
d) a o libr a te th e c le a v a g e
c )B o a )a n d b) X fo n n b y X X 1 X n a n d p r e k a l1ik r e in
Z o ge n s F a c to r U (p r o th r o m b in ) V II, M
p ro te a s e y n ı
a)
tic Z y m o g e n s F a c to r V a n d v m
N o n e n z ym a
b)
i d f th e fo m a tio n o f v a r io u s c lo ttin g fa c to r s
lik e n V n IX a n d X
V ita m in K is r e q
u re o r r

5 c) d c lo ttin g fa c to r s a r e
1 a) 2 a) 3 d) 4 a ) V a ń o u s b lo o
It fo r m s c lo t (lib ń n )
a) F a c to r I (F ib r in o 8 e n )
P o ti? o m b i n ) It a c tiv a te s I V X Vn Vm XI
b) F a c to r II ( r
fa c to fv n
F a c to r I I I (T Is s u e th r o m b o p la s tin ) It is a co r o a
c )
F a c to IV (C a lc iu m io n s ) B in d s fa c to r s to p h o s p h o lip id
d) r

V (P r o a c c e le r in ) C o fa c to r o fX
e ) F a c to r

V II (P r o c o n v e r tin ) It a c tiv a te s IX X
f) F a c to r

tih e m o p h ilic fa c to r A ) C o fa c to r o f IX
F a c to V I II (A n
g)
r

,
IX (A tih e m o p h ilic fa c to r B) A c tiv a te s X
?
h) F a c to r n

X (S tu art er fa c to r ) A c tiv a te s II
i) F a c to r po w

b o p la s tin te c e d e n t) A c tiv a te s D(
F a c to r X I (p la s m th r o m an
p a

fa c to i ) A c tiv a te s fa c to r X I V II & Peka】】ilaein

k) F a c to r x II (H a gem a n

iz in g fa c to r ) C
b iı r o s s lin ks w ith fib r e s
l) F a c to r X I II (F ib ń n s ta
;

m ) P r e k a llik r e in (P r e K ) A c tiv a te s x n
lp s in a c tiv a tio fxn & X I
gen ) H n o
n ) H M w K (H jg h m o le c u la r w e i吕h t k in in o e

o ) K a llik r e in (K a ) , ?;( į

P) P la te le t p h o s p h o lip id (P L )

惡 @ r

Scanned by CamScanner
G o ıQ
m IC O A G U L A N T S

th e d h ic h in la t i o t im f b lo o d T h e y a r e
u 1a n ts a r e r u g s w c r e a s e s th e c o a g u n e o
t ic o a g
A n

u ' " a
T h e s e

ty p '
t ic la ts H ń N d in E p a r in
ta b le g g
a n o a u n ' e p a n a r o p a r n o x a
je
.
In c .

a ī ıt i c o a g u la n ts
l -
b ) O r a ï

a r in s e g W a r fa r in
i) C o u m
k ł : l
,
: Í ? : ,
d io e g A n i s in đ i o n e
ii ) I n d a n e n e s

t ic o g u la n ts T h e s e d r u g s a c t b y e i th e r o n e o f th e t o u o w w g m e s ó - -

ta b le a n a
In je c

t th r o m b in in h ib i t i o n
a ) D ir e c

i f X a
) I n h ib i t o
n o
b

: X a . . ' " . " g h t h e p a r in s a T e u s e d . A n in je c ta b le a n t ic o a g u la n ts y

in h i b i t t iv i t y o f th
t c f w h i c h a r e s u lp h a t e d I t b in d s w i th a n ń th r o m b in a n d s e a c
o s
r e s id u e s m
i g h t h e p a r in s a r e f r a g m e n ıs o f
l b l o o d L o w le c u l a r w e
;O m b i n a n d x a I t in h ib i t s c o t t in g

t i c o a g u l a n t a c t iv i t y J h e s e a r e
m

is o
o

l a t e d fr o m h e p a r i n b y g e l f il t r a t i o n c h r o
a r in h a v in g a n
h e p th e p r o p h l i d t a t m e n t
e c ip i t a t i o n w ith e t h a n o l J h e s e a r e u s e d in y a x s a n r e
p h y p
o r r
a to g r a
m
d lm b li s T h e s e a r e a ls o u s e d d u r i n g b l o o d t r a n s
e ın th r o m b o s is a n p u o n a r y e m o m
o f d e e p v

d h a e m o d i a l y s is
ħr s io n a n

LA g c o , g u l. . ì
.
' !
ta b le
Ť O l tic o a g u l a n ts
I n je c s r a a n

H e p a r in L o w m o ıe c u la r !

D a lt e p a r in
w e ig h t C o u m a r in s In d a n e d io n e s
E n o x a p a r in
h e p a ń n s W a r fa r in A n i s in d io n e
N a d r o p a r in
N ic o u m a lo n e P h e n in d io n e
P a m a p a ń n
p h e n p r o c o u m o n C h i. R in d i o n e

D ip h e n a d io n e

Scanned by CamScanner
 ts a n d A n tı
c o a g u ı
a n ts
co a
is
S y n th e s

び二 一 。
ー
な忒 一
口了
M e
sallcyla
m y!
習 i響
。。
上
th e v ita m in K d ep en
v iı
a m in K T h e s e a g e n ts
d e c re a se s d Ēn t
fa c to r V n
ÌX a n d X
ñ je p th r o m o ir
th e s is o f fa c to r ro
d ia n e as b a s ic m o ie ty The se
In d a n r l 3
s Jm a re ı
hav e jī ı
ıin d a n e d io n e a n d its d e r iv a tiv es g
i
o f co u m ar n s
COntract a n a lo g u e s
自团团团■セ明目區团团团团■
W a r la rin

U ses

1 It is u se d in th e t r e a e n t o f d e ep v e in th r a m b o s is

2 It is a ls o u s e d d u r in g su r g ic a l p r o c e d u to p r e v t th r o t s tr o k e in
res en b o s is to p r e v
m m
a tr ia l fib r illa tio n
ï n d a n e 1 3 Ą io n e
d a n tic o a
3 It is u se a s an g u la n t an d re du ce s th e r is k o fe m b o
_
Th w ha v e sam e m e c h a n is m o t a cb o n as m a [ U L U u u y 6 ų i t s th e

ıO N E
nthesis o f fa c to r n W D C& X 2) M EN A D
V a r io u s a n tic o a g u la n t d r u gs a re V it in K 3)
(o r a m

c } 0
H 3
M;
\

IU P A C N am e 2 M e th y ln a p h th a le n e l 4 d io n e

p r o p e r tie s 1 t o c c u r s a s b ń g h t y e llo w c r y s ta 】
s in s o lu b e in w a te r 1t h a s v e ry fa in t a a cid
n ÆA C N am e (? ) Ļ hly d r o x y 3 (3 lT h e n y lb u ty l) ć o u a r jn
ox o m
o d o r It g e ts m e ta b o lis e d in th e liv e r b y g lu c m a n id a ū o n to g v
i e ĵ nacve m e ta b o lite s I t u s t
P r o p e r tie s It js a w h ite p o w d e Ļ h y g r o s c o íc in n a h ır e v e r s o lu b le in
p y w a te r It g e ts be s to r e d in a ir tig h t co n ta in er p r o te c te d fr o m lig h t
m e ta bo ı is e d in th e Į iv e r an d k id n e y s It is u s e d a s a r a c e m ic m ix tu r e b u t its M so m er is m o r e is m fA tio It is ita m in K 3 d is in v o lv e d a s a c o fa c to r in th e tu b o x y la
e ch a n
M o c n a v an c
p o te n t th a n R is o m er
in th e b o d y T h e s e p r o te in ita m in K
M e c h a n is m o f A c tio n
tio n o f g lu ta m ic ac id r e s id u e s o f c e r ta in p r o te in s s a re v
n d e c r e a s e s th e s n th e s is o f
by ta g o n is in
y p r o t}? om b in fa c to r V n IX an d X dep en den t co a g u la tio n fa c to r s n V II M an d X
3: an
g th e e ffe c ts o f v ita m in K .
U ses

1 It is u se d in th e tr e a tm en t o f h y p o p r o th r o m b in em ia

t ĵ n a n iın a l fe e d a s it h a s so m e v ita m ĵ n
2 So m e tim es it is u se d a s a n u tr iū o n a l s u p p le m en

K a c tiv ity

Scanned by CamScanner
 ì yD a c e ta te Iu P A c N am e
(+XS)=ethyİ -2 (2 s y o r o p h m y ts2
Iu ? A c N n e
aı
cetylo,gr-3-methy】
naphthalen (6.7wothieo 13 2 c ıp y ń d ĵ n

d p r o th r o b in d e İ ic ie n d in t h e tiv tio n f p la te le ts
f a n tic o a g u ]a n t jr id u d th e ir
m a c a o
v o lv e
ce an
in th e m a n age m e n t o cy In a g g r e g a tio n
2 n is u sed
U ses

į įį Ĥï￠
İXiiX
ĮĮTTć
4 ) A N '" '" D '" N E

o cHa

,
R E V IE W Q U E S T IO N S
Tu p A c N am e 2methox)iphmyl)indan 1 3 d io n e

y s ta ls to lin e w h ite c r y s ta u in p o w d e r s lig h tly

n o p e r lie s It o c cu rs as p a】
e y ow a e

b le in e th e r th a l d hydrochlo SHO RT A NSW ER Q U EST ı

O NS
sw ee t o do u r in s o lu b le in w a te r an d s lig h tı
y s o lu m e n o a n
:
a c id ı
t g e ls m e ta b o lis e d in th e liv er Q 1 W r ite th e m echan is m o f b lo o d co a g u la tio n
M e cha n is m th e th e s js o Q 2 W nat tic o a g u la n ts ? C la s s ify th e m W r ite a n o te o n Jn je c ta b le an tic o a g u la n b
f A c tio n lt r e d u f a c tiv g u la
H o n fa c to r s lik e n V n
o ces sw ı e co a a re an

IX & X a lo n g w ith a n tic o a g u la n t p ro te in s C an d S I t in h ib its th e i j t a m i n K d e p e n d e n t g a n cm ia Q 3 W ń te th e s? ıc tu r e an d u ses o fw a r fa r in m en a d io n e

c a r b o x y Ja tio n o f p r e c u r s o r
p r o te ir ıs Q 4 G iv e th e s yn th e s is o f w a r fa r in

Scanned by CamScanner
 in
i D igo x I '

L '" -

1ī '
'" h e h e a r t is no t a ble l m .' He m e ta b , lic d e m an d s o f th e h e a r t fo r

ll i
İ\e a rt th a n its p p ly It g e n e r a y o c c u r s n o v e r lo a d e d c o n d itio n s like kidn e y d ise a se
su
th fe c tio n s o f th e h e a r t (e g H IV ) e tc M a jo r c a u se s o f C I a r e m o c a r d ia l
,

ia e m ia , v ir a l in y
a】
l h t b e a t s u n c o n tr o lle d h yp o te n s io n '
n a bn o r m a e a r
"ronary a r e ry dis e a s e M gh
t
in fa rc tio
.
, .

t i l ĥ b r illa tio n a n d v a lv u la r h e a r t d is e a se F o r th e re v e n tio n a n d c o n t l

s su r e a r a p
blo o d pr e , ro

h to u s e a g e n ts w h ic h in c r e a s e s th e fo rc e o f c o n tr a c tio n o f the h e t p
Fw e v e o sitiv e
o fc H
a ar

e n ts a r e g e n e r a lly u s e d f o r t h is p pu r o s e P o s i tiv e in t i
o ro p c a ge n ts a r e th e d r u s
in o tro p ic a g g
th s t en g th o f m u s c le contraction T h e s d i th
w hid l in c
r e a s e s e r e ru g s n c r e a se s e c o n c e n tr a io n
t
ll la r c a lc it ım b y in h ib it in g th e N a
+
K '
A T P a s e e m y m e W it h h
t e in c re a s e in c a l
o f in tra c e
u

t ti o t h e r e i s in c r e a s e in m o d i l
y c a r a c o n tr a c tility M a n y s u bs ta n ce s h a v e
c itū n io n c o
n ce n r a n

d
in o tr o p ic e ffe c ts a n c a r ia c g ly c o s id e s a r e o n e o f th e m
d
po sitiv e
C a r dia c gly c o s id e s a re m a in ly u s e d in th e tr e a tm en t o f h e a r t fa ilu re ı
h e se gly co s id e s
li ill a n d s tr o p a n th u s
a re pre s e n t in d ig ita s , s qu
C a r d ia c gly c o s id e s p r e s e n t in d ig ita lis a r e o b ta in e d fr o m th e D igita lis p u rp u r e a Th e ir
a glyc o n e p a r t is s te r o id a l in n a tu r e

D igita lis la n a ta g iv e s r ic h e r s s o u r c e o
f c a r d ia c g ly c o s id e in c o m p a r is o n to D igita lis
pu rp u re a O n h y d r o ly s is , th e s e g ly c o s id e s g iv e a g ly c o n e a n d s u g a r A gly c o n e m o ie ty is
r esp o n s ib le fo r a n
y c a r d ia c e ffe c t w h ile s u g a r m o ie ty h e lp s in th e so lu b ility a n d d is trib u tio n
o f th e gly c o s id e M a in a l c o n e s
gy p r e se n ť a re
1) D igito x i
g e n in 3 ) D ig o x ig e n in
2) G ito x ige n in
4 ) D ig in a tig e n in
Su ga r m o ie tie s
p r e s e n t a re
ľ "
1) D i ito x o se
:
g

3) G lu c o s e

@r
Scanned by CamScanner
 s t lv e H b a r t F a ilu r e
C o t r g e

ta b lis e d i ıu ı
I t is a w h ite p o w d e r p r a c tic a lly in s o lu b le in w a te r I t g e t s m e o

, ï i o f A c ti o n S a m e a s M ' " f D ig o x in

t o f
ia t h t ın e n

: b in ti it h th d io v ts i e t r e a
IJ ' i n c o m a o n n w o e r c a r a s c u r a g e n n
g iv e n
I t is
t iv e h e a r t f a ilu r e
e s
c o n g
d o w n th e h e a r t r a te in c a s e o f s in u s t a c h y c a r d i a
It s lo w s
2

ıT I D E
E S ıR f h e
a \ N q A h K h h i 1 r o + i r r ıp n « d a t v p e o o r n ıo n

d in t h e t e a t m e n t o f c o n g e s t iv e h e a r t f a ilu r e a t r e s t o r l e r n t a c t i t y
2 It is u s e r

i d il ti o t iu e s is a n d d iu r e s is į į
3 It h e lp s n v a s o a n n a r r

三飞 妇 】 $ t 냐 飞

B O S E N T A N
4 )

(C
. 3 )3 C

I T r P A C N a m e 4 t e r t b u t y l N [6 (2 h y d r o x y e t h o x y ) 5 (2 m e t h o x y p h e n o x y ) 2
(p y r im i d in 2 y l)p y r im id in y l ] b e n z e n e 1 s u lp h o n a m id e

P r o p e r t i e s It is a w h i t e s o li d p o o r ly s o lu b le in w a t e r I t i s m e t a b o lis e d i n t h e li v e r b y
th e e n z y m e c y t o c h r o m e P 4 5 0 a n d g i v e s th r e e p h a r m a c o lo g ic a ll y a c t iv e m e t a b o li t e s I t m u s t
b e s t o r e d i n l d t in r t t e d f li 吕 h t
c o s e c o n a e p r o e c r o m

M e c h a n i s m o f A c ti o n I t is a specific a n d c o m p e ti t i v e a n ta g o n i s t o f E n d o t h e lin r e c p e t o r s

ï
Scanned by CamScanner
 y J)p jn id in Ļ y ljp ja im id in ylJ 5 p r o p a n 2 y lp y r id in e 2 s u lp h o n a m id e

p m p e r tie s Jt js a w h ite so id h a v in g a m o le c ııl? w e ig h t 6 0 5 6 3 g / m o l

M echa n js ń o f A c tio n J t is a n Dn seı

e c tiv e ET an d ET re ce p to r a n ta go n is t 1B) 2 c) 3 A )
. .

tfs e s 1 6 js u se d as a v aso a to r jn tr e a tin g p e o p le

d iı w ith a cu te h ear t fa ilu re

i
:
\ Ew O U E s Tıo N s

Scanned by CamScanner
 E R O ıD
S ;
. Th e fir s t w as th e c lin ic a l 蠶\ .. '
Š
" - . . . ' " c
T
s ig n ific a n t im p r o v e m t in
en
p a tie n ts w ith r h e u Jm a to īd ar th r itis fo llo w in g

he sec on d wa s t he ap p l ica t ion o f es t ro g e n

T an d pr o g e s t in pĺ cp "
tr a c e p tio n dem o n s tr a te d b y P in c u r$ a n d
o f S te r o
id s co n co? ea gu es

d its d ific a tio n

一

ポ万
an n io
b a s is o f s tr u c tu r e
i o f s te r o id s o n
3 A a s s ffic a t o n

虫
S be m ls

穆
ex Ho n n on e s

C a r d ia c G ly c o s id e s į ，

d sex hm o n e
f c o r tic o s te r o id s a
n
4 B io s y n th e s is p r o c e s s o
s B io s Jm t e
h s is (G P C R ) a 1 C d h o l s l h e r e R b e a r s a lip h a tic s id e c h a in s te r o id s co n ta ĵ n u s u a lly
5 M echa n is m fo r S te r o id
o ls [s
te r o id a l
t r o id s t s te r \
h a i ıis m a c tio n o f s e l
e h y d r o x y gr
o u p s a tta c h e d in a lic y d ic lin k a g e
y am p lm o le s te r o
6 p h a r m a c o lq s ic a l m e c o n e o r m o r

\
Z F I,a r m a c o lo g ic a l r o le o s
f te r o id s 团团团团团■画面■目自 i ?

ı \H \ )
r y w w
rIN T R OD U C T
\ H \ H

n o ' v
h t a r e fo u n d th r o u g h o u t th e a a 】 C h o le s te ro l
s te r o id s a r e a u n iq u e f c h e m ic a ıc o m p o u n d s t a
c la s s o
c h a s c h o le s te r o
l a n d e r g o s te r o l b ile depen ds po n so u rc e s
f th e r in th r e e d iffe r e n t c a te g o ń
u
l es
d n g d o m A r ıd th is c la s s in c lu d e s s
t
c la s s ifie d u r
e r o s s u
a n d p la n t 】 s te r o ls ar e
i te s r e fe r r e d to Th e
a n c ie n t G r e e k s H p p o c r a
f h im k in g d o m ly o w n as
a c id s a n d s te r o id h o rm o n e s
In t h e l ite r a tu r e o t e
th o s e s te r o ls b ta ĵ n e d fr o m th e an al on al e

Z o o s te r o ls o
k f b il ( h o le ) a n d s o lid
h l s te r o l is d e ń v e d fro m th e G r e e
t e r m s o r e c *

g a u s to n e s a n d th e te r m c o e Ī, g '
l i d h c te r iz e d b p h y t o s te r o ķ
y a p lm ts a r e o w n
h i s c a r a
(s te r o s ) B a s ic a 】1y s te r o id s a r e n a tu r a o r s y n t e t c o r g a n c c o m p o u n
b ta in d l fr o th as
s t r o is o e m e

h i h d in f o u r r in g s in s im ila r m a n n e r T h e s e 4 . phytosterols th o s e
c o m p le x m o le c u la r s tr u c tu r e w 呷 o
c a r e c o s e
1 it s te r o ls
s tig ï ń a s te r o ıs o
e tc
b e m e n e a n d o n e fiv e e r g o s te r o
r in g s c o m p ro m is e d 17 c a r b o n s k e le to n c o n ta in in g th r e e s ix m e m b e r

m e m b e r q rĽ lo e n m e r in g o r s te r o id s c o n ta in e ith e r th e p a r tly o r c o 呷
p
1 刀 山了己叩 e n la Ţ h e n a n th r e n e n u c le u s
le te ly h y d r o g e n a te d

. . "
\
A r
H is to ï ic a l d e v e lo p m e n ts
ĺ \ II
1 1889 B r o w n S e q u a r d p r le p a r e d a te s tic u la r e x tr a c t an d te s te d o n M m se lf re p o r tin g
enhanced í
r e u v e n a tio n
HC

2 D
s te r o
r A d o lf W in d a u
id s tr u c tu r e s
s

an
a G o ttin g e n c h e m is Ļ w o r k e d o n is o la tio n , a s s a s a n d e lu c id a te
y
d r e c e iv e d th e N o b e l p r iz e in 1 9 2 8 fo r h is r e s e a r c h o n th e . M yco s te r o ls . ' '" t, r o ls ob ,
X . th . E i1h e r ye a st . . ' ' " n a'

c o n s titu tio n o f s te r o ls
3 1 92 9 A d o if F B u te n dt a n d Edw
an a rd A D o is y in d e p e n d e n tl r e o r te d th e is o la tio n
y p
o fa n a c tiv e s te r o id h o rm
sex on e E s tr o n e , fr o mth e u r in e o f p r e n a n t w o m e n
g

Scanned by CamScanner
 en d in g w ith a c a rb
ci
m s \

şĝ ĵ
) B io s jm th e s is o f s te r o id s

š
ŕ
H a s tw o p a r ts Ĺ e ou te r c o r te x s u rr o u n d in g c e n tr a lm edu lla T h e o u te r A d r e n a l c o r te x ń u th e r
'
th r e e d iı
ie r e n t M s to ı
o g ic a l z o n e s p ro d u ces a ll s e x h o r m o n es Th e se a r e fo llo w in g s
Z g lo m lo s a
f on a e ru
O<esponsbie fo r th e p r o d u c tio n o f a ld o s te r o n e

R E D U CT A SE
ARo ı
ıA TA S E
H O
0
5 u
0 Ĺ
E S T R A D \o
5 u D IH Y D R O T E S T O S T E R O N E TE STO STER O N E

B o th th e d h a rm on e
jn ito c h o n d ń a f c o r tic o s te r o id s an se x
1 B io s y n th e s is p r o c e s s
m d o
an th e th d o p la s m ic F ig u
sm o o en re tic u lu m F ir s tly re

æ =

穮聂衣 。

Scanned by CamScanner
G P r o te i n M e c h a n is f o r S te id B io s th e s is
m r o s y n

A s in th đo lls b in d i n g f th d
o e r e n c r in e c e th e o e g o n a o tr o p in r e s u lt s in a n it r c
in t r a c llu l a A M P le th r o u
r e 'a
ls g h t iv a t i o f G t e in d a d
e r c v e a c n o a p r o a n e n y l c y c la s e
" e
h

ì T .
A T P

S C C

P 4 5 0
C h o ı
e s te r o l

S e x h a rm o n e a n d c o r o c o 8 te ro ld s

Scanned by CamScanner
 fia r M t h a n i s ın a c t io n o f s t e r o id s

二 p b
皆 n 》 m o m 聞 ı
ıı 心 目 回 国 自 国 n d 目 u ı ı ıM t u g h 自 s m a
し 。
目

汇 三三 T ı i= 《 c i L 目ir id ıe c e p M s c 台 iw 鲫 b h d ın g w l lh t 八 口U

偉
ヂ

l ä i i ļ d ıh e
l a m
ıı
l
*
i
b r s »
t
m
ae B
=
a
ł«
= a w io n o f ħ e g m e
b
ū a
o N
lp ıo
A a
d
n
ı«
d
e
M
ı
e
n
m
g
c ü o n
e r
w i ıh
r ib o
s
n
u
u c
o u
l e ic
1
Wd a d (m R N
￥
n ) L
i
ド
W
わ
产

丈
、

H A M IO N A L R E S P O N S E
O r

P H Y S IO L O G IC A L E F I E C T

p b a n m » c o lo g i c a l o f s lt r o id s

l d d u c t iv e
] E t ı Ea{nogens b io s y n t h e s iz e d j n th e a d r e n a c o r te x a n r e p r o
s r o g e n
h is
a le h w h ic
p r i n c ip a l fe m
n e
o r g a r ıs o f fe m a le s E s t r a d io l is th e s e x o r m o ,

d lo p m e n t
d d in th E s t r a d io l
l p a y e d v i t a l r o l e i n fe m a le s f o r e v e
p r o u c e e o v a r y lp
t io d h e s
a f fe c ts h a n
f d E tr a d io l p r i m a r i ly m a i r a n
o s e c o n a r y s e x o g a n
r s s

Į fe m a 】e s e x u a l d i n a t i o n
.

Scanned by CamScanner
 5 G o n an e 5 9 G o n an e
a

F ig m e 5

C 13 1 u lw i o u t
h y dr o c a r b o n s k e le to n w
iM a m e th yl gro u p a t
t te tr a c y c lic
It is p a re n e s tr a n e
a t C 17 o w n
as
d carbo n su b s titu tio n
th y l t C 10 an n o
Gr o u p a 6)
gtradiol (E ig u ï
m e
a l dnı
a e
f n a tu lh o r m on
(o e s tr a n e ) w ith a n ex am p le o ra

Ci
:
E s tra d lo \
5 p E s tra n e
5 a E s tr a n e

figure 6

X X
wiout c a ib o n
d C 13 b u t

Ţ
at C 10 an
w ith m
g to u p s
e t ır y ı .
The h ydro c a rb o n
d r o s tä n e
n am ed
m
t c 1 7 is
su b s titu tio n a s id e c h a in a

d e r iv a tiv e s (Figure 7 )

巴 魯
一
，

Scanned by CamScanner
 łem B \ o 》( 【 qý ] n) se p a
o Į
o ł Ľ a J aJ a J e s au q u a ą o ıq J o " ,

￡
i
d
t x
ałe" '
Ų4!M U M E L P ? ıe a u e l ų ł l q p
a M o a

[ 】s a 배 p a ų s e p

sn ?p i a sa ųłP U E [ ] saBpaM
([E1] d ) se o 1 p a J J a Ja J a J e
n u P !O J a łS
: ì
ť
ī ī !
q e p a łe )o i s A U a n łg q s
: s n '

ų ąt m u M E ıp aJe au e ld ła A o
a ıı
;!
s
ų 1ţ M 1o s.uĮ I p ĮIo
Ņ ep U 0 31e ł
Y Ħ

ıu ıto ı
ł
U a S a* d a« U O

a ds
»￠ł .
ı[

.
Ţ: i : ;
;;: !
e u B w a lo ųa

u o qn D o ł
dn
e u sĮ ĺ t q
m p
pu e qJ pau ı
a u e lo [ a q ı
x) p q
auełswų p au ïe u å 1m n e lu o a Iz J
e s d n o ß 1Ãq 1
?W q łim u c iq J e r ı

m e su Ĥ 4l '
1 J pu e 01 J ł
a lq n o p 1o u o p e ł
e U W Q J ? p Įs e ų 1ţ m
u o q
o1 J m z g J u a a m ą q p
a
s lo w s ļo suoge!Sap ìe u g q a l qn
o p

- p ue s - u a am ļ a
q s puo
m& oq s a r e' oıa l sa 1 01 p w s e ' âw EN
p ıo ıą s . 1 o
u o q ? lq n o p Į
o J s p !o J q s m w u B !s /J a # a l a ıÐ Áq p a J ı? Į a ı s ! p
B u ţ u ţ e lu

Scanned by CamScanner
 4

B anciC (C 8 an d c 9)
e d r in g s o n e
d ie q u a to r ia l tr a i ıs fu s io n b e tw e e n r in g §
o tw o tr a n s fu s a n d m
f s io n b e tw e e n r in g s C a n d D 1 3
a to r a tr a n s u
a n d d equ
4 « x a a n d ro s t 5 e n 3 o n e
17 ￠ H y d r o x y

F ig u re 15
H

6 A d d itio n a l r in g a ūen

w Hen a n a d d itio n a l r in g in b e tw e e n a n y tw o c a r b o n a to m s o f th e s te r o id r in
g s y s te m n

o 1 th e a tta c h e d s id e c h a in , th e s te r o id n a m e d c y c lo u se d a s p r e fix is p r e c e d e d b y lh e
R
rı
u m bers o f th e p o s itio n s jo in e d b y th e n e w b o n d a n d G r e e k le tte r a P d e n o tin gı

ĤH b o n d u n le s s th a t d e s ig n a tio n is a k e a d y c o n ta in e d in th e

J
n m e
-
r
,
Į .

iı
H

5a
ĺ ig u r e 1 7
r Ħ = 团 = = = ■

っ 币酮 島 阳
Scanned by CamScanner
Scanned by CamScanner
 i

T IO N S
S W ER Q U ES
RT AN
§H O p i s im le s t s te r o id a l s tr u c tu r e ?
n e s
W ic h o f 2 1 c a r b o n c o n ta in in g s te r o id a l s k e le to n
1 ill b e n a m e o
W n atw b y N O R In s te r o id a l n o m e n c la tu r e
2 d o y o u m e an
W hat l a n d a x ia l
3 u a to r ia
W it a t is q
e

4 sh o r t
S te r e o c h e m is tr y o f d o u b le b o n d s
W r ite h t f t r o id s w h e n A d d iı ıi id s
5 so m e e x a m p le s o s e i so m e on a r n g s ħts e d in s te r o
D ra w
6 ? e fo llo w in gs
D ra w
7 A n d r o s ta n e C h o le s ta n e
G o n an e
> P re gn an e
e
E s tr a n

id a l n am e o f g iv en s tr u c tu r e
te r o

廿
W r ite s

ır e 2 4
F ig ı
O N TY P E Q U ES TI
ONS
Tı
tio d does EX P L A N A
fo n an
n a tu r a l c o
rm a n ot t o id s
b a s ic n o m e n c la tu r e o f s e r
n
k e le to n is th e u m e r a te
f th e s te r o id s 1 En
w in o f te r o id s w ith e x a m p le s
tr a d itio n a l d ra g
°S itio n s ili h t te r e o c h e m is tr y o s
t th e B p 9a 14 9 P H g
i l g s
bl tr ip le b d
f s te r o id s c a ffo ld c o n ta in in g d o u e o r o n
s a
sho w th e h y ? o g e n n c la h ır e o
3 E x p la in n o m e
f ū s o f s te r o id s
i e D , K Um n d Boa t c o n o r m a o n
d in m y r e v ie w p a p e r D r a w c h a ir a n
b e e n p u b lis h e 4
bove s te r oid a l c h e m is tıy h a s e n t a p lt e n a n tltr e n e r in g
N o te The id [C Į o p
stemic n o m e ııc īa tu r f t o C h e m ic a l S h łâ ie s 2 0 1 6 4 (3) 126
a
e o S te r o s y c
E S T \o N s
V ıh dp k ı
ıo R l ņł P L E C H O IC E q U
M U LTı
m ar an
0 0 ・
I n tm la tio n a l Į o tłn ta f i s te r o id a ıs k e le to n ?
ıe ir
t】 âe r in a tiÐe s A n H o w ın a n y s ix ın e m b e r r in g p re sen t n
1
B 4
A 5
D 2
C 3
id a l s k e le to n is k n o w n as
2 R in d D in s te r o

A C y c lo p e n ta n e
B C y c lo b u ta n e
C C y c lo p r o p an e

te a o y
s te r o id a ıs k Te to n is represen
3 A bo v e th e p la n e su b s tih ıtio n in

B D ark w e d ge s t ì
C s tr a ig h t u H b o ld lin e [
D N on e o f ab ov e

Scanned by CamScanner
 v es
{ @ b je c t i
?e s
ly 】
o n es
o rm
se x h 1 M a le s e x h o rm on es

2 Fem a le s e x h o rm o n es an d p r o e s te r o n '
g e s

ho m o n es
ı [a n d r o g e n s ]
le s e x
】
[a ın a
1 In tro d u c tio n
2 C la s s ific a tio n o f a n d r o ge n s

> T e s to s te r o n e an d th e ir d e ń v a tiv e s
> T e s to s te r o n e e s te r s d e r iv a tiv es

> A n d ro ge n g o n is ts
a n ta

S te r o id a l d r u g s
o N o n s te r o id a l ilrug
5a re d u c ta s e e \ e in h ib ito r s te r o id s
3 S tr u c tu r e a c tiv ity r e la tio n s h ip o f a n d r o e n
g
4 A n d ro g e n s s e le c te d d r u gs
T e s to s te r o n e

> N an d r o lo n e

[b]fe m a le sex h o rm on es [e s tr o g e n s ]
1 In tr o d u c tio n
2 ? a s s ilic a tio n o f fe m a le s e x h o rm o n es

> E s tr o g e n h o r m on e / s te r o id s
> E s tr o g e n (e s tr a d io l) e s te r s te r o id s
> C on u j g a te d e s tr a d io l e s te r s te r o id s
> N on s te r o id a l e s tr o g e n s (d is tilbe s tro ıd e r iv a tiv e s )
> E s tr o g e n an ta g o n is t (tr ip h e n y le th y le n e d e r iv a tiv e s )
3 E s tr g e n s s e le c te d d ru gs
1) E s tr a d io l
2) O e s tr io l
3) O e s tr io n e

4) D ie th y ls tilb e s tr o l
IC ]P r o
g e s te r o n e s
'

1 In tr o d u c tio n
2 C la s s ific a tio n
o f p r o g e s te r o n '
e s

) .
P r o g e s te r o n e d e r iv a tiv e s
> S y i ıth e tic d e r iv a tiv e s p r o g e s tin s an d n o re th is tir o n e
> P o te n t s y n th e tic n o r e th is tir o n e
k
Scanned by CamScanner
S ı þ
t h e ir d e ıi v ı d v e ı
r ıd
n ￠ a
o ņ
ıe r o
ı
￠t
fr ￠
e

0
0
T e s to s t e r o n e 17 o 【 m e t h y lt e s t o s te r o n e

T e s to s te r o n e 17 0 u n d e c a n o a te T e s to s te r o n e l n c y p io n a te

Scanned by CamScanner
ł = = u z c rp m o n e a c e la u

Scanned by CamScanner
 Ħ

a xf ßo o k 0 fM e d fc m ・l
' "

p y
s ıı

ノ 뇨ノ ヘ
〒 ロ

: O d o To n c
x * lı ￠
ı P
a c tiv e a n
d le s s a n o ro ge n lĻ a ' " ' y [n a n
o re a b oł
A ıı ic
9 IW te s to s te r o n e m

te s to s be r o m e
n ı Ť ï F

二 3
0 tU P A
p ro p e
C N A M E

r tie s A w
17hydroxy-androsten m
h ite o r a lm o s t w h ite
po w
T e s to s te r

der o r
o n e

e O R
Ļ a n d ı1 7
C o ıe s s Crystalsodouess
li h t a n d m o is tu r e Sıoreptote
fr om g
id n u c le tıs in r in g A e n h a n c 8 A C T io N
ia F u s io n i出 h e t e r o c y d ic r in g s y s
..
te m jn bo th e s te r o
o r e a n a b o lic a c tiv e a n d le s
ed t
he MECHAHISM 0 T e s to s te r o n e
m is m o v e d in s id
e ı h e c y to ı
a ī e fo u n d t p o s s e s s m d b in d w ith an d ro ge n p asm to w a Ĺr d s ta ı t
a a b o lic a d iv ily s ta n o øo ļ o ı
o s
tis s u es a n
rece
p to r (A R ) th is r e c e t gp
n
le h e te r o c y c li i i in g A
p o r c o ır ı p e x ım
ı d
o s s e ss in g p } T a z o
c r n g n r ergo es a si
n w ħn d
a iıd r o g e n jc a a ip e d u e t o p
gH
'" " y
W
b o r' ' ? ip tio n al
Ē
n sa
th e a n d ro gen e ffe c ts adi'"y '"nged
du ce s ・
p ro
L U SES
C L IN IC A

1 T e s to s te r o n e s te r o id s are u se d as in h o r m o n e r e la c e m e n t th e r a
id s
p p y [H R T I
"
2 T e s to s te r o n e s te r o are u se d fo r
å m an a ge m en to f a c q u ir e d h
y p o g tm a d ĵ s m
3 T e s t o s te r o n e s te r o id s a re u se d fo r m an a ge m en t o f h y p o g o m a s s o c ia t d
e w 0 3
S E LE C Æ » D R U G S S T A J IIIZ O L O L H IV in fe c tio n

4 T e s to s te r o n e s te r o id s a re u se d fo r an d o p a iıs e
į S T E R U S E IN F E M A L E S
T e s to s te r o n e is a s te r o id s e r h o r m o n e fo u n d in b o th m e n a n d w o m e n In m e n te s to s te r o n e is 1 T e s to s te r o n e s te r o id s a r e u se d fo r m e ta s ta tis (s k e le ta l) c n f th e b r e a s tm
c im o m a o

Produced pńn u w b y Øie L e y d ig (in te r s tilia l) c e lls o f th e te s te s w h e n s tim u la te d w o m en w ho a re 1 5 y e a r s p o s tm e n o a u s a l

by p
Ju te in iz in g h o rn ıo n e In w o n ıe n th e p r o d u c tio n o f te s to s te r o n e o c c u T s d 2 T e s to s te r o n e e s te r s u s e d in c o m b in a ū o n w ith e s tr o in th e
u e to ge n s m m g em e n t
c o n v e r s io n o f T e s to s te r o n e fr o m a n d r o t a s s o c ia te d ith in ho do
s e n e ä o n e (50 % ) w h ic h is s e c r e te d b w m en o p au se w o m en w t r e s p o n d to d e q u a te ly to e s tr o
y o v a r ie s (2 5 % )
n o a ge n
an d aù M (25 % ) th e r a py a lo n e

U O LO G ı
cA L Æ R TA N C E O F T E ST E ST R O N E S EX S ID E E F F E C T S O F T E S T O S T E R O N E
H A RM O N E
T o Pr o m o t e pe n ııal og
￡ Am n e s ia A D is c o lo r e d H a ir D iz z in e s s D r y S ı H ir s u tis m H o s ti】iv Im p a ir e d
en e si s n x ie ty cin
To a in ta in fu
n ı n c tib a】
a Jn 】
a h lra tio n o f s p e rm a to z o a
U r in a tio n P a r e s th e s ia P e n is D is o r d e r P e ń p h e r a l E d e m a S w e a tin & a n d V a s o d iı
aūo n : ı\: \
T o d e v e lo
p an d m a in ta in ■\，
pńm a Jy o f th e m a le r e r o
監
qg a n s o
p d u c tiv e s y s te m
ı Su p p o r ta n d m a in ta in s e c o n d a ry or ŕ th e
ga n s o m a le r e r o
p d u c tiv e s y s te m
i
,
Į

团团团国磷 暮
【 t

Scanned by CamScanner
 .
G th fa ilu d Turner s It is a ls o
F ib r in o g e n ?
'

3 e x ce ss, ro w re an s yn om e

4 so d iu m su lfa te h a s b e e n u se d to p ic a lly jn th e tr e a tm eń t o f corneal

? o lo n e
S p Ja n

6
盆
二 。。 an d " d一 . . 。 m 。 。。 . . 。' " 一 。 , a ˜ ，

ROGENS F E M A L E S E X H A R M O N E /S T E R O ID S

iz e d in th e a d r e n a l c o r te x an d d u c tiv f fe m a le s E s tr a d io l
B io s m th e s
rep ro e o r ga n s o
.
.

'" e x h . R m o n ,. w h ic h is p r o d u c e d in th e o v a ry E s tr a d io ıp la y e d v ita l
ip =
'
r in c
is th e p d e v e lo p m e n t o f s e c o n d a ry s e x o rg a n s E s tr a d io l p r im a r ily a ffe c ts
fe m a le s fo r
r o le
tio n a n
d h e lp s fe m a le s e x u a l d e te r n d n a ū o n
tu r a
m a
L E S E X H A R M O N E /S T E R O ID S C L A S S ? CA H O N
G EN S FE M A
E ST R O

E s tro n e

Ľ s tro
-- E s tra d io ı
E s trio ı
.

s"
K io

Scanned by CamScanner
 B o o k o fM e d ï c ï n ・ı
p U į Te x t
ı
łL

rT:.;' i
:
B w en ho m o n e l ıl=
n id ı

II

0
0
0
E s n a d io l
E s tr o n e

e s te r 则用 阳 id 田
E s 加 号 eııf巴比国 d io n
OH

三三 C H

H 3C °
H O
M e su a n o l
E th in 歹ıF s n a d io t

O (C H 2 )3

H O 0

E s b a d io l 17 9 w km e E s m d io ı119 c y c lo p e n ty lp ro p io n a tt

,
=

Scanned by CamScanner
 k f M
1Į U A T e J rt B o o o e
W a ı
9 ・
9 tł

m a l c y c le a n d s e c o n d á
m a i n i n i n g th e m e n s r y f e iħ
ıo p t o f p u b e r ty a le
in th e d e v e m e n E
th li v r A E s tr o g e n s s u lf a t e d
ł
e a
a r e m e ta b o l is e d in e n E s tr
ĝ c h a r a c te r is t i c s E s tr o g e n s o
g e
te d in t h e u i
Jb r m e d a n d t ], e s e c o n íu g a te s e x c r e r n e a n d
thebile
i? i G lu c u r o n jd e c o n íu g a t e s a r e ,

ıU p A C N A M E E s tr a 1 3 3 (1 0 ) T n e n 3 ,
1 7 P d io t

p R o p E R T I E s w M t h ite o d o u r le s s h y g r o s c 叩 ic s m a ll c r y s t a ls o
e o r c r e a m y w , , r c r y s ta 】
】j n t

o d p c t ic a l Į y in s o lu b le in w a t e s o lu b l e in a c e t o n e d i o x a n a n d in s o lu ti o n s f f ix
p w e r r a , , o e d
Ħ IĶ a FI h y ? o x id e s s p a r i n g ly s o lu b le in v e g e t a b le o i ls S t o r e in a i r tig h t c o n t a in e
, r s a t a

te 呷 e r a t u r e P r o te c t fr o m ıi g h Ł

M E C H A N I S M O F A C H O N E d io l is l is t f
s tr a p o te n t n a t u r a a g o n o G Proteinoupled
E s tr o g e n R e c e p to r (G P E R J E tr a d i o l b d ith to in id th iv t a r g e ts
, s o u n w r e c e p r s e e r e s p o n s e c e l】
s

(e g Fe m a le o qg a n s b r e a s ts ) h e Jp s jn to g la te tr ip ti o n h ic h ta
, r e u g e n e a n s c r w s r t to p r e p a r e

m e s s e n g e r R N A H o r m o n e b d e s tr o to d im iz lo
o u n g e n r e c e p r s e r e ,
tr a n s c a te to th e n u c le u s o f
c e l ls a n d b in d to tr o g le
e s e n r e s p o n s e e m e n ts (E ? ) o f g e n e s B in d in g to E R E a lt e r s th e

tr s c r ip t i o te f f fe c te d
a n n r a o a
g e n e s T h e m R N A in te r a c ts w ith r ib o s o to d ir d t e in s
m e s e s e p r o

Scanned by CamScanner
Scanned by CamScanner
Scanned by CamScanner
Ţtįį ţ / . _ u a t i ım s

a i 】y h b a m a r j n j e đi o n : Ë ţ Į i

Ţ
. A n
Ħ ( f J 5 / j

ļ
ţ į
*
.

p y
v
A

a
s

g in
e
s u

p a r a

a
p p

Į u
o

t io n s

s E
s i Eo ń
c o
e s

n t a in in g m ic r o n is e d p r o g e s te r o n e a r e a ls o a v a il a b le f o r o r a l .

A d v e ıs e E f k c ts

G astrointestinal di s M r b a n c e s

a ín p e t i te or we i gh t
m n g e s ap

H u i d re t en ä o n

O e d e m a , c n e d d o a s m a f me l as m a )

A l ler g i c sk i n ra s h e s

u r t i ca r i a

;
・
1
m e n ta l d e p r e s s io n

Scanned by CamScanner
 B Į Į W D
d itio n th a t be a re s u lt o f n e u ro g e n ic ho rm o n al or
E i e đ Ðe d)function (E D ) is a co n ca n

l d y s fu tio is in a b ility to a tta in a s a tis fa c to r

ī d is o r d e rs M a le se x u a n c n y s e x u al

r e la tio n s h ip ııia y in v o lv e a ck
】 o f e r e đ io n o r p T o b le m s w ith r e le a s e j
e a cu la tio n o r o r a sm
g r tile s c tio ale v en in fı
a in ta in tis fa c to r y se x u a lp e r fo r m a n ce P re m
E e c t ū e d y s ń m đ im ı is th e in a b Ðity to m sa a tu re

r e fe rs tr o lle d q a c u la tio n b e fo o r s h o r tly a fte r en te r in g th e v a g iru

e a c u la tio n
i to u n co n re

R e ta r d e d aculation u su a uy is \ o \ ou s w ith d e la y e d j
e a cu la tio n R e tr o g r a d e D ru g s fo r E re c tile d y s fu

i
e ac u la tio n den o te s b a c k øo w

Nitric O jci? a v o ) p la y s s ig n ilic a n t r o le jn e r e c tile o f p e n is in m a le

ftın c tio n D u r in g th e

回
d d d h lia l c e lls in P D E 5 in h ib ito rs
sexu a l s tim u tu s n i? c o x id e 0 0 ) is r e le a s e d fr o m n e rv e in g
ens a n e n o t e

th e c o ıp ı
ıs cav em o s tım (E r æ tile tis s u e o f th e p e n is ) T his r e le a s e d N O e n h a n c e b lo o d flo w
in to c o «p u s c a v e m o su m o f p e n is an d c a u s e e r e c tio n

国 C A U S E S O F E R E C N LE D Y S F U N W

a n w w w c
ON

f d r u g s fo t u e c tile d y s fu n c ū o n

푀
F ig u re 1 C la s s ific a tio n o
D ia b e te s
S p i na l co r d inj uıy

Scanned by CamScanner
 D O S E T h e ty p ic a l d o se o f S ild e n a fil is 50 m g o r a lly ta k e n l h o u r b e fo r e s e x u a l a c tĵw ity

M e c ħa n is m o f s iï d e n a fil c itr a te

F ig ï ır e 2 ř ih s io lo f E r e c tile d s ń u
y gy o
y r c tio n d p D E in h ib ito r s
an m e ch a n is m

Scanned by CamScanner
 .
Į c)
p u ln
B o th
to n a r

a an
y a r te
d b
fab o v e
r ia l h y p e r te n s io n

d) N on e o

is n o t P D E in h ib ito r
W h ic h o n
e
t
a)
S ild e n a fiı
b ) T a d a la lil

c) T e s to s te r o n e

d) A ce tild e n a fiı

is t en d o c r in e c a u s e fo r E re c tile D y s ħın c tio n

5 W n ic h o n e n o

ı ) D ia b e te s m e llitu s
W ħa t ís e r e c tiı d y s fu
a
e n c tio n ?
2 W ħa t a r e th e b) H y p e r th y r o id is m
ca u se s br
ı e r e c tile d y s fu n c tio n ?

ï j 4 w ri te th e d) s p in a l c o r d in jtır y
į ! ex am
p Je o fp h o sp h o d ie s te r a s e in h ib
ito r s
' . r aw the foılow i ng st tu c t ur es
í . S iı
d e n a f il c itr a te

T a d a la ı
T A N SW E R S 】
tı
R ig h t c ı
in ic a ıu ses an d m e c h a n is m f a c tio n
o o f T a d a la ı
il 1 C 4 C 5 D
2 D 3 B
L O N G Q U E S T IO N S Į şŔ
ī
:į ;

Ī
'

团日■ ''
，
，
国回回哩爨
Scanned by CamScanner
 區
1 In b x 1đ u X
L io n
2 M e c h a n is a n o f a c t io n
3 c o m b in a t io n o r a l c o n h a c e p t iv e s
4 C o m b i r ıa t i o n h o rm o n a l c o n tr a c e p t iv e s [C H C s ]
5 M o o s in g a Ħ ll F lo w c h a r t
6 S e le c te d D lr
u g s

a ) M i fe p r is to n e

b ) N o r g e s h e l
c ) L e v o n o r s e s tr o l
7 Q u e s t io n b a n k
# M C Q S
* S h o r t Q u e s t io n s

# E X p la n a t io n ty p e q u e s t io n s

#< éi T R O D U C T I O N I

(t i n a n c ia l i m p l ic a t io n s p la y a r o le a s w e ll) w h e re p o p u l a t io n c o n tr o l is a g o a l

C o m b in a t io n h o r m o n a l c o n t r a c e p t iv e s [C H C s ] in c lu d e e s tr o g e n s a n d ti n
p r o g e s O R
p r o g e s t in o n ly c o n tr a c e p t iv e s E s tr o g e n s p r e v e n t th e d e v e lo p m e n t o f th e c e n tr a l f o l1ic le b
y
i n h ib i t i n g f o u i c le s t im u l a t in g h o r m o n e (F S H ) s e c r e t io n a n d s t a b iliz e th e e n d o m e t r i a l lin in
g
tu m in i m iz e b r e a k th r o u g h b le e d in g P r o g e s ti n p r e v e n ts o v u l a t io n b y s u p p r e s s i n g l u t e in iz in g

h o r m o n e m s e c r e t io n P y o g e s t in w o r k in c o m b in a t io n w i th e s tr o g e n in C H C s s u c h a s

c o m b in a t io n o r a l c o n t r a c e p t iv e s (C O C s ) fo , rm u la t i o n s

> C o n tr a c e p t iv e p a tc h

> C o n tr a c e p t iv e r in g

一 POgestin o n ly p i ll (P o n
\
一 > D e p o t i n tr a m u s c u la r o r s u b c u ta n e o u s in je c t io n
佷 > S u b d e r m a l ím p la n Ļ a n d a s p a r t o f in tr a u te r in e s y s te m s
排
一

封
@ r
Scanned by CamScanner
 te r in d e v ic e Iu s in tr a u te M
m D in tr a u e e
f p re gn an c y d u r in g 1l e
v en D u s
th r o m b o s is b o lis m PoP teation o

tr a c e p tiv Ę D \ŘT deep

a to r y
d ru gs PE POnaly em
is g İ v en 3 6 to 4 8 h o m s b e fo r e 1h e p r o c e d 】n e
co n
id a l a T ıti in fla n
m
ı m ife p r is to n e
N s A ID s n o n s te r o
s y s te ı
n

yN
i
p r o ge s t n
n n 】
mRGEST

Scanned by CamScanner
国
-
d)
ı
VOrgcaisused
N g t
o r
i
e s r e ı»
n m ai

e )
L
R G EST R O

H 3C
ĝÁ O H
M U l

团团团团■回 团目四国
1 7 0 h y d r o x y 1 7 a p r o p t y n y le s tr a 4 m m 3-o n e
(3 Ľ im e th y la m in o p h e n y l)
119 m
u ) 17PAydraxy-17prop-l w ße s b a - \ n
" e
e th rla m in o n h e n yı
th y la m in o p h e n y D 1 7 p h y d r o x y 1 7 a p r o p
l wylestra+en 3 on e Ī
re n 4 e n
20 yn 3 o n e d) 11 (6 D im e

i o r 1 7 a lp h a p g
E h l 1 7 h y d r o x y 18 1 9 d n M ife p r is to n e is u se d fo r
13 t y P r a c tic a lly in s o lu b le in
IU p A C N o d o u r le s s p
o w der 2
w h ite
r a c tic a lly
A w h ite o r p
pR o pE R H E s f
P r o te c t r o m light a ś)
l o h o l c h lo r o fo r m t Fo r te r in e fib r o id s O e io m y o m
h tly s o lu b le in a c d in tr e a tm u
is tw ic e tim e p o te n t th an
en
is
w a te r s lig
u se
e a n d it M ife p r is to n e

險
r g e s te r o n
o
c )
a c tio n s im ila r to p
M oA vonorgestrol ľ t
e n s tn ıc tu ıe
c e lls include Id e n tify th e B lv
in s id e ta r g e t
.

e n r e c e p to r s
e a n d e s tr o g 0 1
le d w ith p r o g e s te r o n d th e p ih Jitu y
Lev qg e s tr o l c o u p
on o
l n d th e h y p °th a la ï n u s an

c tiv e tr a c t t
h e m a m m a ry g a
fo r
th e fe m a le r e p r o d u th e r a te o f r e le a s e
c o m p le x ) d e c r e a s e s

园
L e v o n o r g e s tr o l c o u p e
l d c o m p le x (L R
\ \
te d a fte r o v u la tio n in h ibitio n Ĵ
re v e n
u te in iz in g h o r m o n
e r u sh N o w p r e gn a n c y p o n o r g e s tr o
\
o v tıla to r y ı b )Ľ e v
i d t
o r g e s tr e l
am o u n
i i in h r e q u r e ) N fa bo v e
d u e to d e c r e a s e s th e r a te o f lu te n z g
o r m o n e o n eĮ o
a d )N
c ) M ife p r is to n e :ïĮ
'

C L IN IC A L U S E S 4 G n R H is
d a s m o s t p o te n t b ir th c o tr o l p ill r e le a s in g h o rm
on e
) h v o n o r g e s u o l is
n
a se
tı a ) G o n a d o tr o p in
(P M S )

거
s tr u a l s y n d r o m e h o rm o n e
b ) L e v o n o r g e s tr o l is u se d in tr e a tm en t fo r p r e m e n b) G o n a d o tr o p in r e la x in g
on e
d Lev o n o r g e s tr o l is u se d in h e a tm e n t fo r E n d o m e b ia l c a n cer
c ) G on a d o tr o p in r e fr e s h in g h o rm
į

d) k v o n o r g e s tr o l is u se d in m a in te n a n ce fo r M e n s tr u a l cycle r e g u la ū o n d) G on a d o tr o p in r e s tin g h o rm
on e
ïľ
3!

習魯畿躡鱸 贓 攙霽 鼽 可 。
俐 歹
Scanned by CamScanner
ť g
】
n trodu ction
1.

C id Cl
orticostero s assification
2.

G1ucocorticoids

M ineralocorticoids

n
i c
ıportan ce ofCorticosteroids
3.

4 SAR o
fCorticosteroids
.

id D
5 Corticostero s rugs
.

H ydrocortisone

cortison e

Prednisolon e

Betam ethasone

> Dexam ethason e

6,
Qu estion ban k
M CQs

> ShortQu estion s

E)q lanation Tiïpe Questions

Scanned by CamScanner
 ￡$ S k o fM e d 1c In a ICh
te o o
p U A Te
x
"
共縈 羞 蝨
.

a t in g '
ifte d as re gu ı
b o lis ın
-

c la b as
, . -

id s are
te m e tı
c
C o r tic
o s te r o hy d tı
b o
tic o ld (c ır
G lu c o c o r

r te x
d re n a t c o a d a p ta t io n
fa o f th e
a
d in s tr e s s
c ic ıta v o lv e
p o r t is o
l is h ı
> c
d pre ssu re
es b lo o
c o r tis o
l in c r e a s
>
ke
N ◆ u p ta
l h e lp s in
a
> c o r tis o

ffe c t in u n u n e s y s te m
a ls o a
> C o r tis o l
Th c o n ce ń tr a t io n s o f tis o l
g /d a y
e c o r
t o f 10 m
d a ta ra e
te d b y b o y la te
T y p ic a n y c o r tis o l is se a e
ıg / d L
(1 6 ı a t 8 A M ) th a n in t h e aftern
b h ig h h th e mo r ni n g
inperiph p a

s e v e r e s tr e s
in s
m a y b e in a e ase

te r o id s C la s s if ic a t io n
C o r tic o s

c o S T E R O ı
C O R T ı D S

l
Scanned by CamScanner
 f l u d r o c o r t is o n e

H 3

M e th y lp r e d n i s o lo n e
d is e a c e ta te
Ħ u r o c o r t o n

B e ta m e th a s o n e
d ıo a te P ıe d n is o n e
M e th y lp r e ııi s o ıi e a c đ

N a m e

'
is lo A c e t a te
p r e d n o n e
H C O C
is lo e S o d P ho s
n e d n o n

O C ,
X N a
・ p r e d n is o lo n e S o d S u c(

b Scanned by CamScanner
 TīĻ ľ

"

.m p
.
Dn
(c o r tis o l) is u n a m ra u y u cL w 6 6
-
le
o c o r tis o
n e
H y?
tiv ity
cc tic o id a c C 4&
d th e d o u b le b o n d b e tw ee n
3 c a r b o n yl g r o u p in C 2 0 , a n
th k e to g ro u p in C
. e
l c o r tic o id s
th g lu c o c o r tic o id s & m in e r a o
n tia l fo r b o
ee sb sむeじ 且
C 5 a re

īł
" L
' H
DH
/
H

n o c o r tic o s te ro id s a n ta g o n ia ta

C O R T IS O L
。
一
" '°
价 ザ
デ
H M o d ific a tio n in R in g A
i n o r c o r tis o lc o m p o u n
f ū n 吕A , p r o d u c e in a c t v e
d
뇨 ヘ
十ペ 鳥 s iz e o
W in
ヘ R e d u c tio n
厂 h e te r o c y c ]ic lik e Z u x acu ru au ・

\L cH3 Is o s te r ic a lly rep la c e m e n t in R in g A '"

ity f th e c o r tis o l
a c e ta te w h ic h h a s 2 5 % a c tiv o

0
,

M e fip ris to n e

Scanned by CamScanner
 ◆ イ
.

i ii

ę
0 O

0
ï n a c t ıv e c o m p o u n d

tis l in c r e s e s its p o te n c y
th y l r in g A o f c o r o a
2 a m e o n

is te t a o g th e h a lo g e n s
t io n b y b r o m in e a t C 2 p o n m n
s u b s t it u
le f u s io n w ith R in g A le a d t o 2 0 0 0 t im
H te t ic r in g i e p y r a z o e s
e r o c y c

t a ls la k in e r a l c o r ti c o id a c tiv i y
te n c y o f c o r t is o l b u o c s m
p o

: : i M o d ilic a ti o n in R in g B
i R p la ith h y d h lo d
e c e m e n t w r o p h o b ic g r o u p s lik e a lk y l o r h a lo g e n s (m e th y l c r o a n

f lu o r o a t 6 a p o s i t io n in c r e a s e th e a c t i v i ty d la i O H o r O a t 6 a
a n p o r g r o u p e -

P o s iti o n d e c r e a s e s th e a c t i v i ty
: i Ĵ

Scanned by CamScanner
 į í! jecti n o

U S E S O F C O R T IS O N E
H I H ıIC A L
C lJ 】
ı

H y d ro c o r tis o n e is u se ħrl a s a n ti in 11a n

C o r tis o n e u n a to r
y an d
3 an ti a 】
1e r
is ħr l in tis s u tr a iu p la n ta ti ń gy a ge n t
o r tis o n e
u se e
4 c o

ħite 5 U s e fu l in ly m p h o p o ie s is [1e u k e m ia s a n d l
p R O p E R H E S H y d r o c o r tis o n e ) A w h ite to p r a c tic a lly w o do u r le s s c r y s ta 1】
jn m p ho n ıa a l ı
e
p o w dH It is to p ic a lly u se d in fo r e cz em a [s k in d ißo r d e r 】
V e ıys * g h d y s o lu b le in w a te r e th e r a n d s o lu b le in c h lo ro fo r m S to r e a t a te m 6
p e r a tu r e o f 25

M Ok H y ? o c o r tis o n e b in d w ith G iu c o c o r tic o id R e c e p to r (G R ) a n d fo r m

e d G R com
h ic h p r o d u c e s p e d lic D N A s e q u e n c e s c a lle d
w
g lu c o c o r tic o id r e s p o n s iv e e le m en ts
p le x
(G R E s)
D N ıS o L \ I
in s id e th e n u c le u s fo r m R N A (tr a n s c r i tio n ) T h e s e c h a n e s i
p g n p r o te in syn th e s is
r e fle c t H
OH

= ıH I
1 H y d r o c o r tis o n e ĵs m a inly r e c o m m e n d e d in H o r m o n alre p la cem t th
p y tH R T 】
en era
2 H y d r o c o r tis o n e h e l s
p in C a r b o h y ? a te
p r o te in m e ta b o lis m an d L ip id
J H 1 H
m e ta b o lis u
3 F o r r e p la c e m e n t th e r a m
p y in c h il? e n m ay b e g iv en 4 0 0 to 8 0 0 ic r o g r a m
m s / k g d a il in
y Ĵ* 1) ļ
P re d n is o lo n e

tu p A c N A M E 11P 17a 21 trMydroxypregna-l,dien-3 2 d i o n e

P ro p e r a e s P re d n is o lo n e A c e ta te A w h ite o r a】
m o st w h ite a cy s ta 1]Ĵ n e p o w d e r p r a ď c a 】
1y
in s o lu b le in w a te r s lig h tly s o lu b le in a lc o hol an d in d ic h lo r ó m e th a n e ī ï o te c t fr o m li h t
g
s lig h tly s o lu b le in a c e to n e a n d in c h lo r o fo r m S to r e a t a te m p e r a h n e o f 2 5
M O A P r e d n is o lo n e b in d s g lu c o c o r ū c o id r e c e to r IG R ıin th e c to la s m a n d s te r o id
p y p
Blu c o c o r tic o id r e c e p to r c o m p le x c a u s e s c h a n g e in p r o te in \ th e s is a n d r e fle c t d e s ir ėd
p h a rm a c o lo g ic a l r e s p o n s e s
C lin ic a l U s e s

1 It is m a in ly r e c o m m e n d e d in H o rm o n a l r e p la c e m e n t th e r a py
2 It h e l d Ľ ip id m e ta b o lis m
p s in C a r b o h y d r a te p r o te in m e ta b o lis m an
3 C o r tis o n e is u d ti a lle r gy a g e n t
s e fu la s an ū in fla m m a to r y a n an
Po )
团团ıÆ " " In s o iu b ı
e i n w a te r s
o u b ]e 3o o m fa
D o se P r e d i
n s o lo n e 2 5 to 6 o m g d a ily in d iv id e d d o s e s
"
}
o co ho s to r e a t a te m
冒 p e r a tu re o f 25°

Scanned by CamScanner
出 j ŢĪ
国
+
th a s o n e b in s gı
d u c o c o r tlc o id r
e c e p to r ÏC R
ıIn th ￠

yť
e
D e xa m
OA r e c e p to r co m p le x c a u s e s c ha n WplAını» ñ d ı￠m rń d
M o id g e ï n p r o te in ı n lh e * l
' o co
r tic y * and r r ñ# rı

■
1uc i a l re sp o n se s

i
c o lo s
g ı c
.
tï ıa
hM
se s
alu

ı åi i tı c
u se d as an ti in fla m m a to r y d r u g w h ic h p r o v id e a re ı
it ıjn
1
It is in H a m m a a on
. d yJ iı t v łfla *
f tihl e bu ou
o t
a r ts

i i i X H K
p
u1 it iss up r e s c ń b e d to d e cc r ew a s e s w e 1
r ib 1in g (e d e m a ) w M
11
'
2 s p e c ific a y d ıa r e ra\o ıd
o . ' " s p in e a n d b r a in tr e a t y «t n ła e c t* d
. ' "
tig h t c o ta in e r s a t a te m p e r a tu r e i th a s o n e is u s e d to tr e a t e y e in H a m m a tio n a n d 】
a ir n
a c e to n e
s to r e in D ex a m e
s o lu b le in a so
p re s a ib e d a *
s p a r in g ly 3
g i c
s te r o
id

l
R E V IE W Q U E S T IO N S
:
ĝĮ i
'

ll _ C A L TIS E S
1 B e la m e th a s o n d iu m p h o s p h a te to p ic a l a n tia lle rg ic
e so
O NS
ES T ı
2 It is ï Ħ Ħ I h ? ı a m m a to r y c o n d itio n s o
f th e e y e s e a r s , o in tm e n t c o n ta in in g 0 1% sH O R T Q U
l
B p ta m e th a s o n e v a le r a te e s te r s is a s o e d in th e tr e a tı n e n t s o fte n in g th e s k in
3 u s
1 w n a t is p h y s io lo g ic a 1 ħr n c tio n s o f M in e r a lo c o r tic o id s

3 H ow m u ch co r tis o l s e c r e te d p er day
T H A S O 4 W h a t is A d d is o n d is e a s e ?

W ha thap pe n e d w hen c a rbo n y ıg r o u p is r e p la c e d a t p o s itio 3in

n c o r to s te r o id s s k e le to ?
W h a t e ffe c t p du d if p o la r g r o u p (O H ) in tr o d u :į
ro ce ced a t p o s itio n 6 a n d T i n i d s
s k e le to n ?
7 D ra w th e fo llo w in g s tr u c tu r e s

> 1 1 P 1 7 a 2 1 tr ih d 14ien 32ione

y ro x yp re gn a

> 90 H u o ro 16 p m e th y l 11 P 1 T 2 1 tr ih y d r o x yp r e g n a 1 m e i 3 2 Æo n e I
D c A iu n c u ls o n e
>
H P AC N AM E 9 a - flu o r u 16 a 11 17 a 2 1 tr ih y d r o x
yp re gn 4 3 2M io n
y l 1 19, 1 7 , 2 1 tr ih d r o
y x yp re gn a 1 , 4 d ie n 3 2 0 d io n e >
, en e

1 l p 17 a 2 1 tr ih d
y 6a th y lp r e g n a 1 4 i e n 3 p M io n
y
į :￠
ro x m e e
8
W r ite in s h o rt d e ta ils o f c lin ic a l u ses o fc o r tis o n e $J :

Scanned by CamScanner
Scanned by CamScanner
 四 ■ 园团 团 s
o ßı
。
t
§yú p
ı
h yp o d fıe a t
intolce
: Eig= lo s s
ńo n s
c o n ım o n i o r w ei ht
g g a in c a u se d by Ta
p Ħ州紐 tf?
p
p a lp ita
d em a
pedale
D ia M ea/ fr e q u e n t b o w e l m o v e m en ķ
p
h e a / lig h t m e n s e s
: deudlon o f th )T m
O
m e n o rr

p T re n ì o r
fa tig u
: ie io d in e th e
a py W ea kn e ss ,

n e ss,
e

ir r ita b iliy , in s o m n ia
ħe N e rv o u s
ı w ı a w
al my
i
th) t
s .
r ui t mR aım i
. C i hıyr o id ? u
h yp o ı
CA U S
ES O F H Y
P E R T H Y R O ID ı SM

C o rs (th y r o
id a d e n o m a , fo llic u la r c a rc in o
m a ), T o x ic m
b y p ih ıita ıy d y s ħm c tio n > Tu m uıtin o d u la r o ite r
g
to x ic d iffu s e g o ite r )c a u se d b
by hy po t ha 】am i c dy s f un c t ion G r a v e s d is e a s e ( y p o ly m o T h is m s in th e ts h re c e t
e ó c ien c y of TR H ca u s e d p or
T x ic u n in o d u a r g o e r (a ķ o k n o w n a s p lu n u n e r d i
D
l it
D GOiminwidisnı Æ u g e m e n t o f T h y r o id G la n d ) o
ith h yp e r th y ro id is m
s e a se )

m g en i ı i nm nıa y
al oe t in ind u c e d > N o d u la r B o ite r w c a u se d by e x o ge n o u s io d in e (a 】
so 】
m om
c as
lo did e d e ó c ie x y jodasedow)
Ex o ge n o u s th yr o id e x c e s s th r o u 吕h s e lf a d m in is tr a tio n (fa ti i
id is m c tou s h
E W in d n oed ljp o ? m
ı yp e rth yr o id is m )
T s in e k in in h ñbiı p in s e c r e tin g o r o f th e p itu ita r
* ım ıh i m i d e ・
ym a se on
\ > T h y r o tr o y
A m io d a m ıe
im a tin ñb, s u n itin ib s «n a ña ı
ıb) > H y d a tid ifo r m m o le w ith se c r e tio n o f a th y r o id « tim u la tin g s u b s ta n c e )
* Be m o tm e
In te r le u k in D ru g in d u c e d (io d id e s , a m io d a r o n e , in te r ı
e u kin interferon lilhiu n i , n ,

h io n a m id e
Eı In 帊 陨凱 m 《ı

od i de s a nd i od i de c o n tai ni ng L i thi um
ı
pH Y S IO L O G IC A
L IM P O R T A N C E O F T H Y R O ID H O R M O N E S
p «e p m im s Thites ,

1 T h c th y m id h o rm o n e s h a v e s tr o n g p h y s io lo g ie i呷 a c to n d e v e lo p m en t gr o w th a n d
M i am p i n
m e ta b o lis m
s
ı
ılfonyl
2 T h e th y r o id h o r m o n e s is a ı
so im p o rta n t b io lo gica l h o rın o n e fo r u s e f e n e r gy
S P P S o f H y p o thp o id is m
T h y r o id h o r m
ı o n es e n c o u r a g e m e ta b o lic a c ū v itie s o f m o s t tis s u e s le a d h g to a n
> w e w a g a in
> Æ igu e in c r e a s e in b a s ıl m e ta b o lic ra te ] h e a t p r o d u c tio n
,
an d in fe r tility
; ļ
> Sı
a gg is h n e s s 3 T h y ro id h o r m o n e s a ls o r e g u la te th e im m u n e re s p o ru e in th e in te s tin e
> m n uh
i an m 4 T h y r o id h o r m o n e s e n c o u r a g e m e ta b o lic a c tiv ities o f m o s t tis s u e s le a d in g to an

> sı
ipalioı
ı in c r e a s e in b a s a l m e ta b o lic ra te
> H a lp e ń o
a r y m en s h ı ds l th [e s se n tia l to th e "
o n e s n e c e s s a ry fo r c h il? e n s n o r m a g ro w
'
5 T h y r o id h o r m
> M p
f
dev e ı
opm en t o f th e fe ta l a n d n e o n a ta l b ra in
ņ n ıp & 】m s o sb w n g do w
i n
y be o n e c a u s e b e c a u s e th y ro id h o rm
m
is tial k
he fu n Ħim and m a i n i
o fa l b o d s s te
y y m a n d m e t b li a
one

o c p ro c e s s e s M A N A G EM EN T O R T R E A T M E N T

h y p e rm e ta b o lic s yn d ro th a t o c c ıu s w iıen
m e

Scanned by CamScanner
 l a ū ó O N IN E S O D Iu M o R LİO T Y R O N IN E S O D IU M
J
" N a
+

S o D IU M 4 0 (4 h y d ro x y 3 io d o ph e n y l) 3 m io d o L t) T o s in e
N A M E
IpAC
Ź X d i' ' "
1 ￥= ,
tm ,
o d o ıır le s s , c r y s ta llin e p o w d e r V e ry s i g h tw
】 so lu b le in

N IS M O F A C T IO N
M EC H A
d iu m is a t h y r o id h o r m o n e I t is u s e d in th e tr e a tm e n t o f hypothï oidism L
n in e s o
L m yr o
i i la r w a y m e c h a n is m o f a c t io n a s h v o th ]iT o x in e L T h y r o n in e
S o d iu m h a s in s m
n ip °n in e
s tim u la t e
s h y p o t h a la m ic , t h y r o tr o p in r e le a s in g h o r m o n e (H U Đ a n d r e le a s e o f
s o d iu m

yrotropin (i e , th y T o id s tim u ıa tin g h o r m o n e [T S H ]] fr o m th e p it u ita r y in r e s p o n s e t o lo w

c c u la tin g
le v e ls o f t h w o i d h o r m o n e T S H in t ıır ıt p r o m o te s h o m o n e s y n th e s is a n d r e le a s e
t i ity
b y in c r e a s in g t h } T o id a c v

C U N IC A L U S E S

1 L Th y r o n in e S o d iu m u s e a lo n e o r in c o m b in a t io n w i th a n t ith y r o id a ge n ts to tr e a t

hyp o th y r o id i s m

2 L Th y ro n in e S o d iu m is m o r e a c tiv e th a n le v o th y r o x in e

3 L Thy in S d iu lo in tr e tm t fo tic la r ly in h yp o th y r o id
r o n e o m u s e a n e a e n r p a r u

(m y x e d e m a )co m a

Scanned by CamScanner
 y L T H IO
U RA r
p

!;
. ir l " th io xo
i 4 (J H ) o
p y r im id n
n e
田

n ÆA C N M «Ė 2 > D ihıw p rw y

d s o lu b le in w a te r Y "c t tr o
an d to th , to u c h S ig h y n

l c o r ìv e r s io n o f T4 T o T b y b lo c k in g id a tio
p e r ip h e r a
Ĵ o x
MOhFopylthiouracil b lo d cs n of

* .
. ,
Ć
CH M CA L US E S

1 P r o p y lth io u ra c iĮ is p r im a r y a n tith }T o id d r u g a r e u s e d fo r h yp er th y r o id is m

1
2 P r o p y lth io u r a d l u s e d fo r tr e a tm e n t o f th y r o id a d e n o m a
"

Ħy v
f X ŃĤ H
ł
'" U ' " v

'
.İ g
Scanned by CamScanner
Scanned by CamScanner
Scanned by CamScanner
Scanned by CamScanner
Scanned by CamScanner
Scanned by CamScanner
Scanned by CamScanner
Scanned by CamScanner
Scanned by CamScanner
Scanned by CamScanner
Scanned by CamScanner
Scanned by CamScanner
Scanned by CamScanner
Scanned by CamScanner
Scanned by CamScanner
Scanned by CamScanner
Scanned by CamScanner
Scanned by CamScanner
Scanned by CamScanner
Scanned by CamScanner
Scanned by CamScanner
Scanned by CamScanner
Scanned by CamScanner
Scanned by CamScanner
Scanned by CamScanner
Scanned by CamScanner