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Adrenergic receptor antagonists

- Adrenergic receptor antagonists Non-selective - blockers Phenoxybenzamine, phentolamine Selective 1- blockers Doxazosin, prazosin, terazosin Tamsulosin-Selective 1A-blocker -Adrenergic receptor antagonists Non-selective -blockers Nadalol, pindolol, propranolol, timolol Selective 1-blockers Acebutolol, atenolol, esmolol, metoprolol - and -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 1 and 1receptors Adverse effects due to blockade of 2 and 2 receptors

- Adrenergic receptor antagonists


Non-selective - blockers
Phenoxybenzamine Non-competitive - receptor antagonist vascular resistance, BP Relaxes smooth muscles in bladder neck and prostate
Phaechromocytoma - hypertension

Phentolamine Competitive - receptor antagonist Vasodilation, vascular resistance, BP


Necrosis and ischaemia

A/E- reflex tachycardia, dizziness, headache, nasal congestion

Selective 1- blockers
Doxazosin, prazosin, terazosin, silodosin, tamsulosin, alfuzosin, trimazosin Orally administered Relax smooth muscles in bladder neck and prostate obstruction to urine flow Relax vascular muscles, vasodilation and BP Rx of BPH, hypertension A/E Hypotension, dizziness, oedema

Doxazosin - Hypertension and benign prostatic hyperplasia (BPH) Silodosin - Benign prostatic hyperplasia Prazosin - Hypertension Alfuzosin - Benign prostatic hyperplasia Terazosin - Hypertension and BPH Tamsulosin - Selective 1A-blockerBenign prostatic hyperplasia

1A,- prostate) 1B blood vessels)

Tamsulosin
relatively selective for 1a-adrenergic receptors, which are (mainly present in the prostate). Hence, it may have a more selective action in BPH with minimal effects on blood pressure

Silodosin
high affinity and selectivity for 1A adrenergic receptors which ensures that it works quickly and effectively to relieve the symptoms of BPH. low affinity for 1B receptors (in the blood vessels) hence low incidence of orthostatic and vasodilatory side effects.

-Adrenergic receptor antagonists Non-selective -blockers


Nadalol, pindolol, propranolol, timolol 1-blockade Heart -ve chrotrophic, dromotrophic , ionotropic Kidney - renin secretion Eyes - aq. humour secretion 2-blockade Bronchoconstriction Mask signs of hypoglycemia

Non-selective -blockers contd.


Pindolol, Acebutolol - Intrinsic sympathomimetic activity (Partial agonist activity) Pindolol, propranolol- membrane stabilizing activity Timolol - aq. humour secretion

Pindolol-hypertension Propranolol-hypertension, cardiac arrhythmias, subaortic


stenosis, tremors, migraine, thyrotoxicosis, MI, phaechromocytoma, anxiety

Nadolol - hypertension, angina Timolol - hypertension, migraine, glaucoma

Selective 1-blockers (Cardioselectve 1-blockers)


Acebutolol, atenolol, esmolol, metoprolol Produce less bronchoconstriction
Cardiovascular disorders

- and -Adrenergic receptor antagonists


Carvedilol Blocks 1, 1, 2 Vasodilative effect, cardiac overload and increases CO in patients with heart failure Labetalol Nonselective -blocker & selective -blocker 1-blockade - HR, CO 1-blockade - PVR
hypertension

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