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Adrenergic Receptor Antagonists

Adrenergic Receptor Antagonists

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Published by Patterson Macharia

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Published by: Patterson Macharia on Mar 21, 2012
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Adrenergic receptor antagonists

α- Adrenergic receptor antagonists  Non-selective α- blockers – Phenoxybenzamine, phentolamine  Selective α1- blockers – Doxazosin, prazosin, terazosin – Tamsulosin-Selective α1A-blocker β-Adrenergic receptor antagonists  Non-selective β-blockers – Nadalol, pindolol, propranolol, timolol  Selective β1-blockers – Acebutolol, atenolol, esmolol, metoprolol α- and β-Adrenergic receptor antagonists – Carvedilol, labetalol

Sympatholytics • Drugs that reduce sympathetic activity – Adrenergic receptor antagonists – Ganglion blocking agents – Sympathetic neuronal blocking agents • Therapeutic effects of adrenergic receptor antagonists are primarily due blockade of α1 and β1receptors • Adverse effects due to blockade of α2 and β2 receptors .

reflex tachycardia.blockers • Phenoxybenzamine – Non-competitive α.α. headache. ↓BP – Relaxes smooth muscles in bladder neck and prostate • Phaechromocytoma .hypertension • Phentolamine – Competitive α. nasal congestion . dizziness. ↓vascular resistance.receptor antagonist – Vasodilation.Adrenergic receptor antagonists Non-selective α. ↓BP • Necrosis and ischaemia A/E.receptor antagonist – ↓vascular resistance.

blockers • Doxazosin. vasodilation and ↓BP – Rx of BPH. silodosin.Selective α1. oedema . trimazosin – Orally administered – Relax smooth muscles in bladder neck and prostate – ↓ obstruction to urine flow – Relax vascular muscles. alfuzosin. tamsulosin. prazosin. dizziness. hypertension A/E – Hypotension. terazosin.

Hypertension • Alfuzosin .• Doxazosin .Hypertension and benign prostatic hyperplasia (BPH) • Silodosin .prostate) α1B –blood vessels) .Hypertension and BPH • Tamsulosin ..Selective α1A-blockerBenign prostatic hyperplasia • α1A.Benign prostatic hyperplasia • Prazosin .Benign prostatic hyperplasia • Terazosin .

which are (mainly present in the prostate). .• Tamsulosin – relatively selective for α1a-adrenergic receptors. it may have a more selective action in BPH with minimal effects on blood pressure • Silodosin • high affinity and selectivity for α1A adrenergic receptors which ensures that it works quickly and effectively to relieve the symptoms of BPH. • low affinity for α1B receptors (in the blood vessels) hence low incidence of orthostatic and vasodilatory side effects. Hence.

humour secretion • β2-blockade – Bronchoconstriction – Mask signs of hypoglycemia .↓ aq. pindolol.β-Adrenergic receptor antagonists Non-selective β-blockers • Nadalol. ionotropic – Kidney -↓ renin secretion – Eyes . timolol • β1-blockade – Heart -ve chrotrophic. dromotrophic . propranolol.

Intrinsic sympathomimetic activity (Partial agonist activity) • Pindolol. humour secretion Pindolol-hypertension Propranolol-hypertension. glaucoma . phaechromocytoma.Non-selective β-blockers contd.hypertension. subaortic stenosis. angina • Timolol .membrane stabilizing activity • Timolol -↓ aq. tremors. anxiety • Nadolol . cardiac arrhythmias. Acebutolol . • Pindolol. MI. propranolol. migraine. thyrotoxicosis.hypertension. migraine.

↓ cardiac overload and increases CO in patients with heart failure • Labetalol – Nonselective β -blocker & selective α-blocker – β1-blockade .↓HR.↓ PVR • hypertension . ↓CO – α1-blockade . atenolol. esmolol. β1. β2 – Vasodilative effect.and β-Adrenergic receptor antagonists • Carvedilol – Blocks α1. metoprolol – Produce less bronchoconstriction • Cardiovascular disorders  α. Selective β1-blockers (Cardioselectve β1-blockers) – Acebutolol.

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