| Item |
Information |
|
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 |
| • |
Humans and other mammals |
|
| 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% |