Drug Groups

approved

Description

Bupranolol is a non-selective beta blocker without intrinsic sympathomimetic activity (ISA), but with strong membrane stabilizing activity. Its potency is similar to "propranolol":http://www.drugbank.ca/drugs/DB00571.

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.

Toxicity

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

Affected Organisms

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

Protein Binding

76%