indication

Used to manage hypertension and tachycardia. Also used to treat glaucoma.

pharmacology

Bupranolol is a competitive, nonselective beta-blocker similar to propanolol without intrinsic sympathomimetic activity.

mechanism of action

Bupranolol competes with sympathomimetic neurotransmitters such as catecholamines for binding at beta(1)-adrenergic receptors in the heart, inhibiting sympathetic stimulation. This results in a reduction in resting heart rate, cardiac output, systolic and diastolic blood pressure, and reflex orthostatic hypotension.

toxicity

Symptoms of overdose include bradycardia, cardiac failure, hypotension, and brochospasm.

biotransformation

Over 90% undergo first-pass metabolism. The main metabolite is carboxybupranolol, 4-chloro-3-[3-(1,1-dimethylethylamino)-2-hydroxy-propyloxy]benzoic acid, of which 88% are eliminated renally within 24 hours.

absorption

Quickly and completely absorbed from the gut with less than 10% oral bioavailability.

half life

2-4 hours