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
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
DescriptionCurator's Comment: description was created based on several sources, including
http://www.accessdata.fda.gov/drugsatfda_docs/label/2010/021114s003lbl.pdf
Curator's Comment: description was created based on several sources, including
http://www.accessdata.fda.gov/drugsatfda_docs/label/2010/021114s003lbl.pdf
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 Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: CHEMBL213 |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Primary | BETAXON Approved UseBETAXON™ (levobetaxolol hydrochloride ophthalmic suspension) 0.5% is indicated for lowering intraocular pressure in patients with
chronic open-angle glaucoma or ocular hypertension. Launch Date2000 |
|||
| Primary | BETAXON Approved UseBETAXON™ (levobetaxolol hydrochloride ophthalmic suspension) 0.5% is indicated for lowering intraocular pressure in patients with
chronic open-angle glaucoma or ocular hypertension. Launch Date2000 |
Cmax
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
0.5 ng/mL |
1 drop 2 times / day steady-state, ocular dose: 1 drop route of administration: Ocular experiment type: STEADY-STATE co-administered: |
LEVOBETAXOLOL plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FASTED |
T1/2
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
20 h |
1 drop 2 times / day steady-state, ocular dose: 1 drop route of administration: Ocular experiment type: STEADY-STATE co-administered: |
LEVOBETAXOLOL plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FASTED |
Doses
| Dose | Population | Adverse events |
|---|---|---|
0.5 % 2 times / day steady, ophthalmic Recommended Dose: 0.5 %, 2 times / day Route: ophthalmic Route: steady Dose: 0.5 %, 2 times / day Sources: |
unhealthy, 1 - 6 years Health Status: unhealthy Age Group: 1 - 6 years Sex: M+F Sources: |
Other AEs: Eye disorders NEC, Bradycardia... Other AEs: Eye disorders NEC (6 patients) Sources: Bradycardia (1 patient) |
AEs
| AE | Significance | Dose | Population |
|---|---|---|---|
| Bradycardia | 1 patient | 0.5 % 2 times / day steady, ophthalmic Recommended Dose: 0.5 %, 2 times / day Route: ophthalmic Route: steady Dose: 0.5 %, 2 times / day Sources: |
unhealthy, 1 - 6 years Health Status: unhealthy Age Group: 1 - 6 years Sex: M+F Sources: |
| Eye disorders NEC | 6 patients | 0.5 % 2 times / day steady, ophthalmic Recommended Dose: 0.5 %, 2 times / day Route: ophthalmic Route: steady Dose: 0.5 %, 2 times / day Sources: |
unhealthy, 1 - 6 years Health Status: unhealthy Age Group: 1 - 6 years Sex: M+F Sources: |
PubMed
| Title | Date | PubMed |
|---|---|---|
| Levobetaxolol (Betaxon): in vitro pharmacology, intraocular pressure lowering activity and autoradiographic localization of beta-adrenoceptors in human eyes. | 2001 |
|
| Levobetaxolol (Betaxon) and other beta-adrenergic antagonists: preclinical pharmacology, IOP-lowering activity and sites of action in human eyes. | 2001 Aug |
|
| Levobetaxolol-induced Up-regulation of retinal bFGF and CNTF mRNAs and preservation of retinal function against a photic-induced retinopathy. | 2002 Apr |
|
| Metipranolol attenuates lipid peroxidation in rat brain: a comparative study with other antiglaucoma drugs. | 2003 Oct |
|
| Binding affinities of ocular hypotensive beta-blockers levobetaxolol, levobunolol, and timolol at endogenous guinea pig beta-adrenoceptors. | 2004 Apr |
|
| Effectiveness of levobetaxolol and timolol at blunting retinal ischaemia is related to their calcium and sodium blocking activities: relevance to glaucoma. | 2004 Feb 15 |
|
| Levobetaxolol hydrochloride: a review of its pharmacology and use in the treatment of chronic open-angle glaucoma and ocular hypertension. | 2007 Jun |
|
| Efficacy of brinzolamide and levobetaxolol in pediatric glaucomas: a randomized clinical trial. | 2008 Jun |
Patents
Sample Use Guides
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
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Preferred Name | English | ||
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Official Name | English | ||
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Common Name | English | ||
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Common Name | English |
| Classification Tree | Code System | Code | ||
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NCI_THESAURUS |
C29576
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ACTIVE MOIETY
SALT/SOLVATE (PARENT)
