Betaxolol

Betaxolol

drugbox


IUPAC_name = 1- [4- [2-(cyclopropylmethoxy)
ethyl] phenoxy] -3-
(1-methylethylamino)propan-2-ol
CAS_number = 63659-18-7
ATC_prefix=C07
ATC_suffix=AB05
ATC_supplemental=ATC|S01|ED02
PubChem=2369
ChemSpiderID=2279
DrugBank=APRD00245
C=18 | H=29 | N=1 | O=3
molecular_weight = 307.428 g/mol
bioavailability = 89%
metabolism = Hepatic
elimination_half-life = 14-22hours
excretion = Renal (20%)
pregnancy_AU = C
pregnancy_US = C
pregnancy_category =
legal_status = Rx-only
routes_of_administration = oral, ocular

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

* [http://products.sanofi-aventis.us/kerlone/kerlone.pdf Kerlone prescribing information]

ee also

Levobetaxolol


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