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Details

Stereochemistry ABSOLUTE
Molecular Formula C18H29NO3
Molecular Weight 307.4278
Optical Activity UNSPECIFIED
Defined Stereocenters 1 / 1
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of LEVOBETAXOLOL

SMILES

CC(C)NC[C@H](O)COC1=CC=C(CCOCC2CC2)C=C1

InChI

InChIKey=NWIUTZDMDHAVTP-KRWDZBQOSA-N
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/t17-/m0/s1

HIDE SMILES / InChI

Molecular Formula C18H29NO3
Molecular Weight 307.4278
Charge 0
Count
MOL RATIO 1 MOL RATIO (average)
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 1 / 1
E/Z Centers 0
Optical Activity UNSPECIFIED

Description

BETAXON™ is a trade name for levobetaxolol hydrochloride ophthalmic suspension 0.5%, which is indicated for lowering intraocular pressure in patients with chronic open-angle glaucoma or ocular hypertension. The brand name Betaxon is discontinued in USA, but generic versions may be available. Levobetaxolol is a cardioselective (beta-1¬ adrenergic) receptor-blocking agent that does not have significant membrane-stabilizing (local anesthetic) activity and is devoid of intrinsic sympathomimetic action. Animal studies suggest levobetaxolol (S-isomer) is the more active enantiomer of betaxolol (racemate).

Originator

Approval Year

Targets

Primary TargetPharmacologyConditionPotency

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
BETAXON
Primary
BETAXON

Cmax

ValueDoseCo-administeredAnalytePopulation
4.7 ng/g
1 drop 2 times / day multiple, ocular
LEVOBETAXOLOL plasma
Oryctolagus cuniculus
0.5 ng/mL
1 drop 2 times / day steady-state, ocular
LEVOBETAXOLOL plasma
Homo sapiens

AUC

ValueDoseCo-administeredAnalytePopulation
10.4 ng × h/g
1 drop 2 times / day multiple, ocular
LEVOBETAXOLOL plasma
Oryctolagus cuniculus

T1/2

ValueDoseCo-administeredAnalytePopulation
1.6 h
1 drop 2 times / day multiple, ocular
LEVOBETAXOLOL plasma
Oryctolagus cuniculus
20 h
1 drop 2 times / day steady-state, ocular
LEVOBETAXOLOL plasma
Homo sapiens

Funbound

ValueDoseCo-administeredAnalytePopulation
48%
1 drop 2 times / day multiple, ocular
LEVOBETAXOLOL plasma
Oryctolagus cuniculus

Doses

AEs

Overview

CYP3A4CYP2C9CYP2D6hERG

OverviewOther

Other InhibitorOther SubstrateOther Inducer

Drug as victim

Sourcing

PubMed

Sample Use Guides

In Vivo Use Guide
The recommended dose is one drop of BETAXON™ (levobetaxolol hydrochloride ophthalmic suspension) 0.5% in the affected eye(s) twice daily. In some patients, the intraocular pressure lowering responses to BETAXONTM Ophthalmic Suspension may require a few weeks to stabilize.
Route of Administration: Other
In Vitro Use Guide
Unknown
Substance Class Chemical
Record UNII
75O9XHA4TU
Record Status Validated (UNII)
Record Version