Betaxolol information

Betaxolol
Clinical data
Trade names	Kerlone
AHFS/Drugs.com	Monograph
MedlinePlus	a609023
Pregnancy; category	AU: C; ;
Routes of; administration	By mouth, ocular
ATC code	C07AB05 (WHO) S01ED02 (WHO);
Legal status
Legal status	In general: ℞ (Prescription only);
Pharmacokinetic data
Bioavailability	89%
Metabolism	Liver
Elimination half-life	14–22 hours
Excretion	Kidney (20%)
Identifiers
	IUPAC name (RS)-1-{4-[2-(cyclopropylmethoxy)ethyl]-; phenoxy}-3-(isopropylamino)propan-2-ol;
CAS Number	63659-18-7 ;
PubChem CID	2369;
IUPHAR/BPS	549;
DrugBank	DB00195 ;
ChemSpider	2279 ;
UNII	O0ZR1R6RZ2;
KEGG	D07526 ;
ChEBI	CHEBI:3082 ;
ChEMBL	ChEMBL423 ;
CompTox Dashboard (EPA)	DTXSID2022674 ;
ECHA InfoCard	100.113.058
Chemical and physical data
Formula	C18H29NO3
Molar mass	307.434 g·mol−1
3D model (JSmol)	Interactive image;
Chirality	Racemic mixture
	SMILES O(CCc1ccc(OCC(O)CNC(C)C)cc1)CC2CC2;
	InChI 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 ; Key:NWIUTZDMDHAVTP-UHFFFAOYSA-N ;
	(verify)

Betaxolol is a selective beta₁ receptor blocker used in the treatment of hypertension and angina.^[1] It is also a adrenergic blocker with no partial agonist action and minimal membrane stabilizing activity.^[2] 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.

It was patented in 1975 and approved for medical use in 1983.^[3]

^ 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.
^ "Google Scholar". scholar.google.com. Retrieved 2023-12-26.
^ Fischer J, Ganellin CR (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 461. ISBN 9783527607495.

[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] "Google Scholar". scholar.google.com. Retrieved 2023-12-26.

[3] Fischer J, Ganellin CR (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 461. ISBN 9783527607495.

Betaxolol information

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