Bupranolol

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Bupranolol
Bupranolol.svg
Clinical data
AHFS/Drugs.com International Drug Names
Routes of
administration
Oral, topical (eye drops)
ATC code
Pharmacokinetic data
Bioavailability < 10%
Protein binding 76%
Metabolism First pass elimination > 90%
Elimination half-life 2-4 hours (plasma)
Excretion > 88% renal (as carboxybupranolol)
Identifiers
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
Chemical and physical data
Formula C14H22ClNO2
Molar mass 271.78298 g/mol
3D model (JSmol)
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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.

Uses and dosage[edit]

Like other beta blockers, oral bupranolol can be used to treat hypertension and tachycardia.[citation needed] 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.[citation needed]

Pharmacology[edit]

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.[citation needed]

Adverse effects, contraindications, interactions[edit]

Adverse effects, contraindications and interactions are similar to other beta blockers.[citation needed]

References[edit]

  • Dinnendahl, V; Fricke, U, eds. (2007). Arzneistoff-Profile (in German). 2 (21 ed.). Eschborn, Germany: Govi Pharmazeutischer Verlag. ISBN 978-3-7741-9846-3.