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Betaxolol

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Betaxolol
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Systematic (IUPAC) name
(RS)-1-{4-[2-(cyclopropylmethoxy)ethyl]-
phenoxy}-3-(isopropylamino)propan-2-ol
Clinical data
Trade names Kerlone
AHFS/Drugs.com monograph
MedlinePlus a609023
  • AU: C
  • US: C (Risk not ruled out)
  • (Prescription only)
oral, ocular
Pharmacokinetic data
Bioavailability 89%
Metabolism Hepatic
Half-life 14–22 hours
Excretion Renal (20%)
Identifiers
63659-18-7 7pxY
C07AB05 S01ED02
PubChem CID 2369
IUPHAR ligand 549
DrugBank DB00195 7pxY
ChemSpider 2279 7pxY
UNII O0ZR1R6RZ2 7pxY
KEGG D07526 7pxY
ChEBI CHEBI:3082 7pxY
ChEMBL CHEMBL423 7pxY
Chemical data
Formula C18H29NO3
307.428 g/mol
 14pxY (what is this?)  (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

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. PMID 2202584. 

External links

See also

Levobetaxolol