Betaxolol

Betaxolol 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 affinity 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
Clinical data
Trade namesKerlone
AHFS/Drugs.comMonograph
MedlinePlusa609023
Pregnancy
category
  • AU: C
Routes of
administration		oral, ocular
ATC code
Legal status
Legal status
  • In general: ℞ (Prescription only)
Pharmacokinetic data
Bioavailability89%
MetabolismLiver
Elimination half-life14–22 hours
ExcretionKidney (20%)
Identifiers
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.113.058
Chemical and physical data
FormulaC18H29NO3
Molar mass307.434 g·mol−1
3D model (JSmol)
ChiralityRacemic mixture
  (verify)

It was patented in 1975 and approved for medical use in 1983.[2]

Medical 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

Contraindications
  • Hypersensitivity to the drug
  • Patients with sinus bradycardia, heart block greater than first degree, cardiogenic shock, and overt cardiac failure

Side effects
See also: Beta blocker

History

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.

Brand names

Brand names include Betoptic, Betoptic S, Lokren, Kerlone.

See also

References
  1. 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. S2CID 46962082.
  2. Fischer J, Ganellin CR (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 461. ISBN 9783527607495.
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