Betaxolol

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Betaxolol
Betaxolol structure.svg
Betaxolol ball-and-stick.png
Systematic (IUPAC) name
(RS)-1-{4-[2-(cyclopropylmethoxy)ethyl]-
phenoxy}-3-(isopropylamino)propan-2-ol
Clinical data
Trade namesKerlone
AHFS/Drugs.commonograph
MedlinePlusa609023
Pregnancy cat.C (AU) C (US)
Legal status Prescription only
Routesoral, ocular
Pharmacokinetic data
Bioavailability89%
MetabolismHepatic
Half-life14–22 hours
ExcretionRenal (20%)
Identifiers
CAS number63659-18-7 YesY
ATC codeC07AB05 S01ED02
PubChemCID 2369
IUPHAR ligand549
DrugBankDB00195
ChemSpider2279 YesY
UNIIO0ZR1R6RZ2 YesY
KEGGD07526 YesY
ChEBICHEBI:3082 YesY
ChEMBLCHEMBL423 YesY
Chemical data
FormulaC18H29NO3 
Mol. mass307.428 g/mol
 YesY (what is this?)  (verify)
 
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Betaxolol
Betaxolol structure.svg
Betaxolol ball-and-stick.png
Systematic (IUPAC) name
(RS)-1-{4-[2-(cyclopropylmethoxy)ethyl]-
phenoxy}-3-(isopropylamino)propan-2-ol
Clinical data
Trade namesKerlone
AHFS/Drugs.commonograph
MedlinePlusa609023
Pregnancy cat.C (AU) C (US)
Legal status Prescription only
Routesoral, ocular
Pharmacokinetic data
Bioavailability89%
MetabolismHepatic
Half-life14–22 hours
ExcretionRenal (20%)
Identifiers
CAS number63659-18-7 YesY
ATC codeC07AB05 S01ED02
PubChemCID 2369
IUPHAR ligand549
DrugBankDB00195
ChemSpider2279 YesY
UNIIO0ZR1R6RZ2 YesY
KEGGD07526 YesY
ChEBICHEBI:3082 YesY
ChEMBLCHEMBL423 YesY
Chemical data
FormulaC18H29NO3 
Mol. mass307.428 g/mol
 YesY (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. 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[edit]

Dosage[edit]

Contraindications[edit]

External links[edit]

See also[edit]

Levobetaxolol