Adrenolytics jurusan pendidikan dokter umum fakultas kedokteran universitas sriwijaya

7/25/2019 Adrenolytics jurusan pendidikan dokter umum fakultas kedokteran universitas sriwijaya

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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'

Adrenolytics jurusan pendidikan dokter umum fakultas kedokteran universitas sriwijaya

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