Betaxolol

Betaxolol

Clinical data
Trade names	Kerlone
AHFS/Drugs.com	Monograph
MedlinePlus	a609023
Pregnancy category	AU: C
Routes of administration	oral, ocular
ATC code	C07AB05 (WHO) S01ED02 (WHO)
Legal status
Legal status	In general: ℞ (Prescription only)
Pharmacokinetic data
Bioavailability	89%
Metabolism	Hepatic
Elimination half-life	14–22 hours
Excretion	Renal (20%)
Identifiers
IUPAC name (RS)-1-{4-[2-(cyclopropylmethoxy)ethyl]- phenoxy}-3-(isopropylamino)propan-2-ol
CAS Number	63659-18-7 Y
PubChem CID	2369
IUPHAR/BPS	549
DrugBank	DB00195 Y
ChemSpider	2279 Y
UNII	O0ZR1R6RZ2
KEGG	D07526 Y
ChEBI	CHEBI:3082 Y
ChEMBL	ChEMBL423 Y
CompTox Dashboard (EPA)	DTXSID2022674
ECHA InfoCard	100.113.058
Chemical and physical data
Formula	C18H29NO3
Molar mass	307.428 g/mol g·mol−1
3D model (JSmol)	Interactive image
SMILES O(CCc1ccc(OCC(O)CNC(C)C)cc1)CC2CC2
InChI InChI=1S/C18H29NO3/c1-14(2)19-11-17(20)13-22-18-7-5-15(6-8-18)9-10-21-12-16-3-4-16/h5-8,14,16-17,19-20H,3-4,9-13H2,1-2H3 Y Key:NWIUTZDMDHAVTP-UHFFFAOYSA-N Y
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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
• 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

• Levobetaxolol
• Cicloprolol

External links

• Kerlone prescribing information