Bupranolol
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| Clinical data | |
|---|---|
| AHFS/Drugs | International Drug Names |
| Routes of administration | Oral, topical (eye drops) |
| ATC code | |
| Pharmacokineticdata | |
| Bioavailability | < 10% |
| Protein binding | 76% |
| Metabolism | First pass elimination > 90% |
| Eliminationhalf-life | 2-4 hours (plasma) |
| Excretion | > 88% renal (as carboxybupranolol) |
| Identifiers | |
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| CAS Number | |
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| IUPHAR/BPS | |
| DrugBank | |
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| CompTox Dashboard(EPA) | |
| Chemical and physical data | |
| Formula | C14H22ClNO2 |
| Molar mass | 271.79g·mol−1 |
| 3D model (JSmol) | |
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Bupranololis a non-selectivebeta blockerwithout intrinsic sympathomimetic activity (ISA), but with strong membrane stabilizing activity. Its potency is similar topropranolol.
Uses and dosage
[edit]Like other beta blockers, oral bupranolol can be used to treathypertensionandtachycardia.[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 againstglaucoma.[citation needed]
Pharmacology
[edit]Bupranolol is quickly and completely absorbed from the gut. Over 90% undergofirst-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 acarboxylgroup –, 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]Further reading
[edit]- Dinnendahl V, Fricke U (2007).Arzneistoff-Profile(in German). Vol. 2 (21 ed.). Eschborn, Germany: Govi Pharmazeutischer Verlag.ISBN978-3-7741-9846-3.