Bupranolol
File:Bupranolol.svg | |
Systematic (IUPAC) name | |
---|---|
(RS)-1-(tert-butylamino)-3-(2-chloro-5-methylphenoxy)propan-2-ol | |
Clinical data | |
Routes of administration | Oral, topical (eye drops) |
Pharmacokinetic data | |
Bioavailability | < 10% |
Protein binding | 76% |
Metabolism | First pass elimination > 90% |
Biological half-life | 2-4 hours (plasma) |
Excretion | > 88% renal (as carboxybupranolol) |
Identifiers | |
CAS Number | 23284-25-5 |
ATC code | C07AA19 (WHO) |
PubChem | CID 2475 |
IUPHAR/BPS | 550 |
Chemical data | |
Formula | C14H22ClNO2 |
Molar mass | 271.78298 g/mol[[Script error: No such module "String".]] |
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Bupranolol is a non-selective beta blocker without intrinsic sympathomimetic activity (ISA), but with strong membrane stabilizing activity. Its potency is similar to propranolol.
Contents
[hide]Uses and dosage
Like other beta blockers, oral bupranolol can be used to treat hypertension and tachycardia. The initial dose is 50 mg two times a day. It can be increased to 100 mg four times a day. Bupranolol eye drops (0,05%-0,5%) are used against glaucoma.
Pharmacology
Bupranolol is quickly and completely absorbed from the gut. Over 90% undergo first-pass metabolism. Bupranolol has a plasma half life of about two to four hours, with levels never reaching 1 µg/l in therapeutic doses. 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.
Adverse effects, contraindications, interactions
Adverse effects, contraindications and interactions are similar to other beta blockers.
References
Dinnendahl, V, Fricke, U, ed. (2007). Arzneistoff-Profile (in German). 2 (21 ed.). Eschborn, Germany: Govi Pharmazeutischer Verlag. ISBN 978-3-7741-98-46-3.
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