ADRENERGIC ANTAGONISTS adrenergic blockers 1 Nonselective 2 Selective
ADRENERGIC ANTAGONISTS
α – adrenergic blockers 1. Nonselective 2. Selective phentolamine, tolazoline, phenoxybenzamine α 1 – blocker prazosin, doxazocin, terazosin, tamsulosin, indoramin b) α 2 – blocker yohimbine 3. Miscellaneous ergot alkaloids a)
Pharmacological actions
Cardiovascular effects blocks α 1 receptor vasodilatation ↓ peripheral resistance ↓ venous return & CO HYPOTENSION
Cardiovascular effects HYPOTENSION stimulate baroreceptor reflex sympathetic discharge stimulates 1 receptor TACHYCARDIA
Cardiovascular effects blocks α 2 receptors promotes neuronal release of NE TACHYCARDIA
Other effects Nasal stuffiness -due to vasodilatation & congestion of nasal mucosa ? Miosis - due to loss of tone of radial muscle of iris ? Improved urine flow - due to smooth muscle relaxation of bladder & prostate ? Failure of ejaculation & impotence - due to inhibition of contraction of vas deferens & ejaculatory ducts ? Nausea, vomiting, diarrhea - due to ↑ in gastric secretions ?
Adverse effects Palpitation N Postural hypotension N Nasal blockade N Diarrhea N Impotence N Edema N
Phenoxybenzamine ¬ Nonselective ¬ Used α blocker in pheochromocytoma, secondary shock, peripheral vascular disease Hypotension N Flushing N Tachycardia N N Nasal congestion
Phentolamine l Non selective l Shorter duration of action l Pheochromocytoma, control of hypertension due to clonidine withdrawal, cheese reaction…
Prazosin Ø Selective α 1 blocker Inhibita phosphodiasterase - vasodilation Ø Used in hypertension & CHF Ø Postural Hypotension N Flushing N Tachycardia N N Nasal congestion
Tamsulosin w Selective α 1 A blocker w Used in Benign Prostatic Hypertrophy (BPH) Failure of ejaculation N Dizziness N
Why Tamsulosin is preferred over Prazosin in BPH even though both are selective α 1 blockers?
Therapeutic uses l Pheochromocytoma l Hypertension l Benign hypertrophy of prostate l Peripheral vascular disease
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