Академический Документы
Профессиональный Документы
Культура Документы
(Sympatholytics,
Adrenolytics)
Dr. dr. Mgs. Irsan Saleh, M.Biomed
Dept of Pharmacology
FK Unsri
Beta-blockers (antagonists)
Selective
Non selective
1)
1 & 2 )
& )
Bopindolol
Esmolol
Oxprenolol
Pindolol
Propranolol
Sotalol
Timolol
Carvedilol
(antioxidant)
Labetalol
Acebutolol
Atenolol
Betaxalol
Bisoprolol
Celiprolol
Metoprolol
Nebivolol
Mixed
Metoprolol
Acebutolol
Atenolol
Antihypertensive effect
Blockade of 1-adrenoceptors in the heart
and reduction of the heart rate and
myocardial contractility.
Blockade of renal juxtaglomerular 1receptors which reduces renin secretion.
Blockade of presynaptic 2-adrenoceptors
which inhibits exocytose of NA.
Carvedilol and labetalol also block
-receptors and produce vasodilation.
Selectivity
-blockers
Atenolol
Bisoprolol
Metoprolol
1/ 2-blocking
activity
15
50
Nebivolol
25
293
Propranolol
1,9
(5565/min)
Heart
Arterioles
Antitachyarrhythmic effect
of the beta-blockers
Reduce the rate
of spontaneous depolarization of sinus
and AV nodal tissue
Indiations: SV and ventricular tachyarrhythmias.
( cAMP)
Esmolol
Antianginal
(antistenocardic) effect
Angina pectoris is a symptom of
reversible myocardial ischaemia and is
most frequently experienced as chest pain on
exertion, which is relieved by rest.
Pain is the consequence of an imbalance
between oxygen supply and oxygen demand in
the ischaemic area
of myocardium.
Anxiolytic effect
of -sympatholytics
Postsynaptic 1-blockers
Blockade of postsynaptic 1-receptors
lowers blood pressure by:
Lowering tone in arteriolar resistance vessels.
Dilating venous capacitance vessels, which
reduces venous return and cardiac output.
Selective 1-adrenoceptor antagonists spare
the presynaptic 2-adrenoceptors and do
not produce reflex tachycardia.
Postsynaptic 1-blockers
Doxazosin
Prazosin
Prazosin indications:
- Arterial hypertension
- Congestive chronic heart failure
Potentially beneficial effect: an increase
in HDL and a reduction in triglycerides.
Adverse reactions (ARs)
Postural hypotension due to venous
pooling (this can be troublesome after
the first dose)
Lethargy
Carvedilol (antioxidant)
Labetalol
Arterial hypertension
Chronic heart failure
Contraindication:
- cor pulmonale
2-agonists
I1-agonists
Clonidine
-methyl-NE
(+)
b) I1(Inosin-1)-agonists
(> t1/2: 1 time daily p.o.)
Adrenergic
neuron
blockers
Guanethidine
Reserpine
Numerous
ARS
Rauwolfia serpentina