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Dr. dr. Mgs. Irsan Saleh, M.Biomed
Dept of Pharmacology
FK Unsri
ANIAD!"N"!#I$ D!U#S
%Sympatholytics,
Adrenolytics&
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1) 1& 2 )
BopindololEsmolol
Oxprenolol
PindololPropranolol
Sotalol
Timolol
Carvedilol(antioxidant)
Labetalol
& )
Beta-blocers (anta!onists)
"ceb#tolol"tenolol
Betaxalol
BisoprololCeliprolol
$etoprolol
%ebivolol
Selective %on selective $ixed
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-blockers with ISA%intrinsic symatho'
mimetic acti(ity& or partial agonists)
Ace*+tolol, $eliprolol, -prenolol, Pindolol-blockers with membranostabilizing
activity) Ace*+tolol, $ar(edilol,
-prenolol, Propranolol
First pass effect%hepatic meta*olism, p.o.
*ioa(aila*ility //0&) -prenolol, Pindolol,
Propranolol
Lipophilic drugs) more of *eta'*loc1ers
ydrophilic drug) Atenolol
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Lipopilic -blocers (e'!' propranolol) are
ell absorbed rom te !#t* b#t #nder!o
extensive irst-pass metabolism in te liver*
it considerable variabilit+'
,+dropilic
-blocers (e'!' atenolol) areless completel+ absorbed rom te !#t and
are eliminated #ncan!ed b+ te idne+'
Te dose ran!e to maintain eective plasmaconcentrations is narroer tan or dr#!s
ic #nder!o metabolism and te clinical
response is more predictable'
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Selective 1-"drenoceptor "nta!onists
$etoprolol
"ceb#tolol
"tenolol
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Main effects of *eta'*loc1ers
Antihypertensi(e effect
Antitachyarrhythmic effectAntianginal
%antistenocardic& effect2An-iolytic3 effect
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"nti+pertensive eect
Blocade o 1-adrenoceptors in te eart
and red#ction o te eart rate and
m+ocardial contractilit+'Blocade o renal #xta!lomer#lar 1-
receptors ic red#ces renin secretion'
Blocade o pres+naptic
2-adrenoceptors ic inibits exoc+tose o %"'
Carvedilol and labetalol also bloc
-receptors and prod#ce vasodilation'
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"tenolol
Bisoprolol
$etoprolol
%ebivolol
Propranolol
1.2-blocin!
activit+-blocers
1//0
2/2
1*
S e l e c t i v i t +
(//34/.min)
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Heart Arterioles
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Antitachyarrhythmic effect
of the *eta'*loc1ers5ed#ce te rate
o spontaneo#s depo-
lari6ation o sin#s and "7 nodal tiss#e
8ndiations9S7 and ventri-
c#lar tac+arr+tmias'
( c"$P)
- atenolol* pindolol* propranolol
- only antiarrhytmic action9 esmolol and sotalol
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"trial l#tter it a :91 cond#ction ratio'
Esmolol
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"n!ina pectoris is a s+mptom o
reversible m+ocardial iscaemia and ismost re;#entl+ experienced as cest pain on
exertion* ic is relieved b+ rest'
Pain is te conse;#ence o an imbalancebeteen ox+!en s#ppl+ and ox+!en demand in
te iscaemic area
o m+ocardi#m'
"ntian!inal
(antistenocardic) eect
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2An-iolytic3 effectof 4'sympatholytics
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"dverse reactions o -blocers
Blocade o
1-receptorsma+ ca#se
brad+cardia* "7 bloc* eart ail#re'
Blocade o 2-receptorsma+ ca#se
broncospasm* cold extremities*
intermittent cla#dication (red#cin!
periperal blood lo) and +po!l+cemia'
C%S eects9sleep dist#rbance* dreams
and all#cinations (more common it
lipopilic dr#!s ic cross te BBB)'
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Blocade o posts+naptic 1-receptors
loers blood press#re b+9
Loerin! tone in arteriolar resistance vessels'
=ilatin! veno#s capacitance vessels* ic
red#ces veno#s ret#rn and cardiac o#tp#t'Selective 1-adrenoceptor anta!onists spare
te pres+naptic 2-adrenoceptors and do
not prod#ce relex tac+cardia'
Posts+naptic 1-blocers
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Posts+naptic1-blocers
=oxa6osin
Pra6osin
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Pra6osin 3 indications9
- "rterial +pertension- Con!estive cronic eart ail#rePotentiall+ beneicial eect9 an increase
in ,=L and a red#ction in tri!l+cerides'"dverse reactions("5s)Post#ral +potension d#e to veno#s
poolin! (tis can be tro#blesome ater
te irst dose)
Letar!+
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Alf+5osin %6atral S!7
&, Do-a5osin, ams+losin %mnic7
&
Selective postsynaptic alpha-!"-blockers#
*loc1 alpha'89'receptors into the smooth
m+scles of the prostate gland, and theprostatic part of the +rethra.
Indication)
hyperplasiaof prostate
gland
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Carvedilol (antioxidant)
Labetalol"rterial +pertension
Cronic eart ail#re
Contraindication9
- cor p#lmonale
$ixed beta- & alpa-anta!onists
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Centrall+ actin! dr#!s ("nti+pertensive action)
2-a!onists
81-a!onists
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Clonidine ( ,Cl)
xerostomia (dr+ mo#t)itdraal penomenon
sedation
post#ral +potension
Te stim#lation o pres+naptic
2-receptorsin C%S inibits %" release* red#ces s+m-
patetic inl#ence on te vasomotor centre>
red#ces periperal arterial and veno#s tone'
a)2-a!onists(< t1/2: 23 times daily p.o.)
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The site of action of :'methyldopaappears
to be inthe brain rather than in the periphery.Systemically administered -methyldopa rapidly
enters the brain, where it accumulates in
noradrenergic nerves and converts to-methylnorepinephrine.
Released $-methylnorepinephrine
from thenoradrenergic nervesactivates CS !-adrenoceptors whose function
is to decrease sympathetic out"ow.
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$lonidine
$'methyl'N"
(+)
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The stimulation of I1-receptors:
in C%S red#ces s+mpatetic toneand loers blood press#re>
in idne+ inreases secretion o "%P
$oxonidine
5ilmenidine
b) 81(8nosin-1)-a!onists( t1/2: 1 time daily p.o.)
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"drener!icne#ron
blocers?#anetidine5eserpine
%#mero#s"5S 5
a#(
ol)ias e r
pe nt i
na
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"drener!ic ne#ron blocers
Tese dr#!s #se te active transport
mecanisms or monoamines to
acc#m#late in te adrener!ic nerve
terminal' 8nside te cell te+ prevent
te release o %" rom vesicles'