Betaxolol

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Betaxolol
Betaxolol structure.svg
Betaxolol ball-and-stick.png
Names
Trade namesKerlone
  • (RS)-1-{4-[2-(cyclopropylmethoxy)ethyl]-
    phenoxy}-3-(isopropylamino)propan-2-ol
Clinical data
Pregnancy
category
  • AU: C
Routes of
use
By mouth, ocular
External links
AHFS/Drugs.comSystemic: Monograph
Eye: Monograph
US NLMBetaxolol
MedlinePlusa609023
Legal
Legal status
  • In general: ℞ (Prescription only)
Pharmacokinetics
Bioavailability89%
MetabolismLiver
Elimination half-life14–22 hours
ExcretionKidney (20%)
Chemical and physical data
FormulaC18H29NO3
Molar mass307.434 g·mol−1
3D model (JSmol)
ChiralityRacemic mixture
  • O(CCc1ccc(OCC(O)CNC(C)C)cc1)CC2CC2
  • 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 checkY
  • Key:NWIUTZDMDHAVTP-UHFFFAOYSA-N checkY
  (verify)

Betaxolol is a medication used to treat hypertension and glaucoma.[1]

It is a selective beta1 receptor blocker. It is thought to work by reducing the production of aqueous humor within the eye.

Betaxolol 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

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.

External links

Identifiers: