Betaxolol

Betaxolol
Systematic (IUPAC) name
1-{4-[2-(cyclopropylmethoxy)ethyl]phenoxy}-3-(isopropylamino)propan-2-ol
Identifiers
CAS number	63659-18-7
ATC code	C07AB05 S01ED02
PubChem	2369
DrugBank	APRD00245
ChemSpider	2279
Chemical data
Formula	C18H29NO3
Mol. mass	307.428 g/mol
SMILES	eMolecules & PubChem
Pharmacokinetic data
Bioavailability	89%
Metabolism	Hepatic
Half life	14–22 hours
Excretion	Renal (20%)
Therapeutic considerations
Pregnancy cat.	C(AU) C(US)
Legal status	℞ Prescription only
Routes	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

• Kerlone prescribing information

See also

Levobetaxolol