Bupranolol

Bupranolol is a non-selective beta blocker without intrinsic sympathomimetic activity (ISA), but with strong membrane stabilizing activity. Its potency is similar to propranolol.

Bupranolol
Clinical data
AHFS/Drugs.comInternational Drug Names
Routes of
administration
Oral, topical (eye drops)
ATC code
Pharmacokinetic data
Bioavailability< 10%
Protein binding76%
MetabolismFirst pass elimination > 90%
Elimination half-life2-4 hours (plasma)
Excretion> 88% renal (as carboxybupranolol)
Identifiers
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC14H22ClNO2
Molar mass271.78298 g/mol g·mol−1
3D model (JSmol)
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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 that is, the methyl group at the benzene ring is oxidized to a carboxyl group , 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, eds. (2007). Arzneistoff-Profile (in German). 2 (21 ed.). Eschborn, Germany: Govi Pharmazeutischer Verlag. ISBN 978-3-7741-9846-3.
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