Betaxolol
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| Clinical data | |
|---|---|
| Trade names | Kerlone |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a609023 |
| Pregnancy category | |
| Routes of administration | oral, ocular |
| ATC code | C07AB05 (WHO) S01ED02 (WHO) |
| Legal status | |
| Legal status |
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| Pharmacokinetic data | |
| Bioavailability | 89% |
| Metabolism | Hepatic |
| Biological half-life | 14–22 hours |
| Excretion | Renal (20%) |
| Identifiers | |
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| CAS Number |
63659-18-7  |
| PubChem (CID) | 2369 |
| IUPHAR/BPS | 549 |
| DrugBank |
DB00195 |
| ChemSpider |
2279 |
| UNII |
O0ZR1R6RZ2 |
| KEGG |
D07526 |
| ChEBI |
CHEBI:3082 |
| ChEMBL |
CHEMBL423 |
| Chemical and physical data | |
| Formula | C18H29NO3 |
| Molar mass | 307.428 g/mol |
| 3D model (Jmol) | Interactive image |
| Chirality | Racemic mixture |
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Betaxolol (trade names Betoptic, Betoptic S, Lokren, Kerlone) is a selective beta1 receptor blocker used in the treatment of hypertension and glaucoma.[1] Being selective for beta1 receptors, it typically has fewer systemic side effects than non-selective beta-blockers, for example, not causing bronchospasm (mediated by beta2 receptors) as timolol may. Betaxolol also shows greater affininty for beta1 receptors than metoprolol. In addition to its effect on the heart, betaxolol reduces the pressure within the eye (intraocular pressure). This effect is thought to be caused by reducing the production of the liquid (which is called the aqueous humor) within the eye. The precise mechanism of this effect is not known. The reduction in intraocular pressure reduces the risk of damage to the optic nerve and loss of vision in patients with elevated intraocular pressure due to glaucoma.
Betaxolol was approved by the U.S. Food and Drug Administration (FDA) for ocular use as a 0.5% solution (Betoptic) in 1985 and as a 0.25% solution (Betoptic S) in 1989.
Clinical uses
- Oral: for the management of hypertension
- Ophthalmic: for the management of glaucoma
- the drug seems to have an effect of neuroprotection in glaucoma treatment
Dosage
- Oral: The initial dose in hypertension is ordinarily 10 mg once daily either alone or added to diuretic therapy.
- Ophthalmic: The recommended dose one to two drops in the affected eye(s) twice daily.
Contraindications
- Hypersensitivity to the drug
- Patients with sinus bradycardia, heart block greater than first degree, cardiogenic shock, and overt cardiac failure
See also
References
- ↑ Buckley, MM; Goa, KL; Clissold, SP (July 1990). "Ocular betaxolol. A review of its pharmacological properties, and therapeutic efficacy in glaucoma and ocular hypertension.". Drugs. 40 (1): 75–90. doi:10.2165/00003495-199040010-00005. PMID 2202584.