Betaxolol
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| Betaxolol
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| Systematic (IUPAC) name | |
| 1-{4-[2-(cyclopropylmethoxy)ethyl]phenoxy}-3-(isopropylamino)propan-2-ol | |
| Identifiers | |
| CAS number | |
| ATC code | C07 S01ED02 |
| PubChem | |
| DrugBank | |
| Chemical data | |
| Formula | C18H29NO3 |
| Mol. mass | 307.428 g/mol |
| SMILES | & |
| Pharmacokinetic data | |
| Bioavailability | 89% |
| Metabolism | Hepatic |
| Half life | 14–22 hours |
| Excretion | Renal (20%) |
| Therapeutic considerations | |
| Pregnancy cat. | |
| Legal status |
℞ Prescription only |
| Routes | oral, ocular |
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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. 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
Dosage
- Oral: The initial dose in hypertension is ordinarily 10 mg once daily either alone or added to diuretic therapy.
- Ophthalmic: The recommended dose is 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
External links
See also
Beta blockers (C07) | |
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| Non-selective β antagonists | Metipranolol • Nadolol • Oxprenolol • Penbutolol • Pindolol • Propranolol • Tertatolol • Timolol • Sotalol |
| β1 antagonists (cardioselective) | Atenolol • Acebutolol • Celiprolol • Betaxolol • Bisoprolol • Esmolol • Metoprolol • Nebivolol |
| Mixed α1/β antagonists | Carvedilol • Labetalol |
Synonyms / Brand Names:
The content of this page is taken from the FDA package insert for this drug and should not be edited.
Acknowledgement and Attribution Regarding Sources of Content
Some of the initial content on this page may be incorporated in part from copyleft sources in the public domain including wikis such as Wikipedia and AskDrWiki. Drug information for patients came from the The National Library of Medicine. Infectious disease information may have come from the Centers for Disease Control (CDC). Differential Diagnoses are drawn from clinicians as well as an amalgamation of 3 sources: 1.The Disease Database; 2. Kahan, Scott, Smith, Ellen G. In A Page: Signs and Symptoms. Malden, Massachusetts: Blackwell Publishing, 2004:3; 3. Sailer, Christian, Wasner, Susanne. Differential Diagnosis Pocket. Hermosa Beach, CA: Borm Bruckmeir Publishing LLC, 2002:7 .
