Adverts

Open Access Articles- Top Results for Bupranolol

Bupranolol

</th></tr></th></tr>
Bupranolol
File:Bupranolol.svg
Systematic (IUPAC) name
(RS)-1-(tert-butylamino)-3-(2-chloro-5-methylphenoxy)propan-2-ol
Clinical data
AHFS/Drugs.com International Drug Names
Oral, topical (eye drops)
Pharmacokinetic data
Bioavailability < 10%
Protein binding 76%
Metabolism First pass elimination > 90%
Half-life 2-4 hours (plasma)
Excretion > 88% renal (as carboxybupranolol)
Identifiers
23284-25-5 7pxN
C07AA19
PubChem CID 2475
IUPHAR ligand 550
DrugBank DB08808 7pxY
ChemSpider 2381 7pxY
UNII 858YGI5PIT 7pxY
KEGG D07590 7pxN
ChEMBL CHEMBL305380 7pxY
Chemical data
Formula C14H22ClNO2
271.78298 g/mol
 14pxN (what is this?)  (verify)

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

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, ed. (2007). Arzneistoff-Profile (in German) 2 (21 ed.). Eschborn, Germany: Govi Pharmazeutischer Verlag. ISBN 978-3-7741-9846-3.