Betaxolol

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Betaxolol
Betaxolol structure.svg
Betaxolol ball-and-stick.png
Clinical data
Trade names Kerlone
AHFS/Drugs.com Monograph
MedlinePlus a609023
Pregnancy
category
  • AU: C
  • US: C (Risk not ruled out)
Routes of
administration
oral, ocular
ATC code
Legal status
Legal status
  • In general: ℞ (Prescription only)
Pharmacokinetic data
Bioavailability 89%
Metabolism Hepatic
Elimination half-life 14–22 hours
Excretion Renal (20%)
Identifiers
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
ECHA InfoCard 100.113.058
Chemical and physical data
Formula C18H29NO3
Molar mass 307.428 g/mol
3D model (JSmol)
  • Interactive image
Chirality Racemic mixture
  (verify)

Betaxolol (trade names Betoptic, Betoptic S, Lokren, Kerlone) 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 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

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.

External links

  • Kerlone prescribing information
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