Betaxolol

Betaxolol is a selective beta1 receptor blocker used in the treatment of hypertension and angina.[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		By mouth, ocular
ATC code
Legal status
Legal status
  • In general: ℞ (Prescription only)
Pharmacokinetic data
Bioavailability89%
MetabolismLiver
Elimination half-life14–22 hours
ExcretionKidney (20%)
Identifiers
  • (RS)-1-{4-[2-(cyclopropylmethoxy)ethyl]-
    phenoxy}-3-(isopropylamino)propan-2-ol
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
  • 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)

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

Medical uses

Hypertension

Betaxolol is most commonly ingested orally alone or with other medications for the management of essential hypertension. It is a cardioselective beta blocker, targeting beta-1 adrenergic receptors found in the cardiac muscle. Blood pressure is decreased by the mechanism of blood vessels relaxing and improving the flow of blood.[3]

Glaucoma

Ophthalmic betaxolol is an available treatment for primary open angle glaucoma (POAG) and optical hypertension. Betaxolol effectively prevents the increase of intracellular calcium, which leads to increased production of the aqueous humor. In the context of open angle glaucoma, increased aqueous humor produced by ciliary bodies increases intraocular pressure, causing degeneration of retinal ganglion cells and the optic nerve.[4]

Furthermore, betaxolol is additionally able to protect retinal neurones following topical application from excitotoxicity or ischemia-reperfusion, providing a neuroprotective effect. This is thought to be attributed to its capacity to attenuate neuronal calcium and sodium influx.[5]

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

Side effects

The adverse side-effects of betaxolol can be categorized into local and systemic effects.[4] The local effects include:

Systemically, patients taking betaxolol might experience:

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.

Society and culture

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.
  3. "Betaxolol: MedlinePlus Drug Information". medlineplus.gov. Retrieved 2023-01-12.
  4. Tajran J, Goyal A (2022). "Betaxolol". StatPearls. Treasure Island (FL): StatPearls Publishing. PMID 32491793. Retrieved 2023-01-12.
  5. Wood JP, Schmidt KG, Melena J, Chidlow G, Allmeier H, Osborne NN (April 2003). "The beta-adrenoceptor antagonists metipranolol and timolol are retinal neuroprotectants: comparison with betaxolol". Experimental Eye Research. 76 (4): 505–516. doi:10.1016/s0014-4835(02)00335-4. PMID 12634114.
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