- Molecular NameBetaxolol
- SynonymBetaxolol HCL; Betaxololum [INN-Latin]; Betazolol
- Weight307.434
- Drugbank_IDDB00195
- ACS_NO63659-18-7
- Show 3D model
- LogP (experiment)2.81
- LogP (predicted, AB/LogP v2.0)2.97
- pka9.4
- LogD (pH=7, predicted)0.57
- Solubility (experiment)0.451 mg/ml
- LogS (predicted, ACD/Labs)(ph=7)-0.15
- LogSw (predicted, AB/LogsW2.0)2.52
- Sw (mg/ml) (predicted, ACD/Labs)0.89
- No.of HBond Donors2
- No.of HBond Acceptors4
- No.of Rotatable Bonds11
- TPSA50.72
- StatusFDA approved
- Administrationoral, ocular
- PharmacologyA selective beta1 receptor blocker used in the treatment of hypertension and glaucoma.
- Absorption_value90.0
- Absorption (description)Betaxolol is completely absorbed after oral administration.
- Caco_2-4.52
- Bioavailability85.0
- Protein binding55.0
- Volume of distribution (VD)8 L/kg; reported as 4.9, 6.0 and 9.8 L/kg for single doses and 7.7 to 8.8 L/kg for repeated doses.
- Blood/Plasma Partitioning ratio (D_blood)N/A
- MetabollsmPrimarily hepatic. Approximately 15% of the dose administered is excreted as unchanged drug, the remainder being metabolites whose contribution to the clinical effect is negligible.
- Half life14~22 h
- ExcretionThe primary route of elimination is hepatic metabolism and urinary excretion. About 15% of a dose is excreted in urine as the unchanged drug but the majority is oxidatively metabolised to inactive and weakly active metabolites, including α-hydroxybetaxolol. There are no active metabolites of clinical importance. It has high lipid solubility and crosses the placenta. It is distributed into breast milk where higher concentrations have been achieved than in maternal blood. It is not removed by dialysis.
- Urinary ExcretionN/A
- Clerance0.28 L/h/kg.
- ToxicityOral LD50s are 350 to 400 mg betaxolol/kg in mice and 860 to 980 mg/kg in rats. Predicted symptoms of overdose include bradycardia, congestive heart failure, hypotension, bronchospasm, and hypoglycemia.
- LD50 (rat)N/A
- LD50 (mouse)N/A