Betaxolol

Betaxolol
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
    PubChem CID
    IUPHAR/BPS
    DrugBank
    ChemSpider
    UNII
    KEGG
    ChEBI
    ChEMBL
    ECHA InfoCard 100.113.058 Edit this at Wikidata
    Chemical and physical data
    Formula C18H29NO3
    Molar mass 307.428 g/mol
    3D model (JSmol)
    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.
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