Betaxolol

Betaxolol
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
Pregnancy category	AU: C US: C (Risk not ruled out)
Legal status	℞ (Prescription only)
Routes of administration	oral, ocular
Pharmacokinetic data
Bioavailability	89%
Metabolism	Hepatic
Biological half-life	14–22 hours
Excretion	Renal (20%)
Identifiers
CAS Number	63659-18-7^Y
ATC code	C07AB05 S01ED02
PubChem	CID 2369
IUPHAR/BPS	549
DrugBank	DB00195^Y
ChemSpider	2279^Y
UNII	O0ZR1R6RZ2^Y
KEGG	D07526^Y
ChEBI	CHEBI:3082^Y
ChEMBL	CHEMBL423^Y
Chemical data
Formula	C₁₈H₂₉NO₃
Molar mass	307.428 g/mol
Chirality	1 : 1 mixture (racemate)
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^Y Key:NWIUTZDMDHAVTP-UHFFFAOYSA-N^Y
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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

↑ 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.

External links

Kerlone prescribing information

Beta blockers (C07)

β, non-selective	Alprenolol Bopindolol Bupranolol Carteolol Cloranolol Mepindolol Nadolol Oxprenolol Penbutolol Pindolol/Iodopindolol Propranolol Sotalol Tertatolol Timolol

β₁-selective	Acebutolol Atenolol Betaxolol Bevantolol Bisoprolol Celiprolol Epanolol Esmolol Metoprolol Nebivolol Practolol S-Atenolol Talinolol

β₂-selective	Butaxamine

α₁- + β-selective	Carvedilol Labetalol

^#WHO-EM ^‡Withdrawn from market Clinical trials: ^†Phase III ^§Never to phase III

Drugs used for glaucoma preparations and miosis (S01E)

Sympathomimetics

Parasympathomimetics

muscarinic	Aceclidine Pilocarpine

muscarinic/nicotinic	Acetylcholine Carbachol

Acetylcholinesterase inhibitors	Demecarium Ecothiopate Stigmine (Fluostigmine Neostigmine Physostigmine) Paraoxon

Carbonic anhydrase inhibitors/
(sulfonamides)

Beta blocking agents

Prostaglandin analogues (F_2α)

Other agents

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