- Molecular NameBuspirone
- SynonymBuspirona [INN-Spanish]; Buspirone; Buspirone HCL; Buspironum [INN-Latin]
- Weight385.512
- Drugbank_IDDB00490
- ACS_NO36505-84-7
- Show 3D model
- LogP (experiment)2.63
- LogP (predicted, AB/LogP v2.0)2.58
- pka7.2
- LogD (pH=7, predicted)1.67
- Solubility (experiment)N/A
- LogS (predicted, ACD/Labs)(ph=7)-4.14
- LogSw (predicted, AB/LogsW2.0)1.41
- Sw (mg/ml) (predicted, ACD/Labs)0.01
- No.of HBond Donors0
- No.of HBond Acceptors7
- No.of Rotatable Bonds6
- TPSA69.64
- StatusFDA approved
- AdministrationN/A
- PharmacologyA psychoactive drug and pharmaceutical medication of the piperazine and azapirone chemical classes. It is used primarily as an anxiolytic, but also to a lesser extent as an antidepressant.
- Absorption_value100.0
- Absorption (description)It is rapidly absorbed after oral administration; peak plasma concentrations occur after about 40 to 90 min.
- Caco_2N/A
- Bioavailability3.9
- Protein binding95.0
- Volume of distribution (VD)5.3 L/kg after a 20 mg intravenous dose
- Blood/Plasma Partitioning ratio (D_blood)N/A
- MetabollsmIt undergoes extensive first-pass metabolism primarily by oxidation and bioavailability is therefore low. Metabolism is probably mediated by CYP3A4. Most metabolites are inactive, although oxidative dealkylation produces 1-(2-pyrimidinyl)-piperazine which is about 20 to 25% as potent as the parent drug. The major metabolite is 5-hydroxybuspirone which may be oxidised further to many more metabolites and its glucuronide conjugate.
- Half life2.4 h
- ExcretionThe metabolites are excreted mainly in urine (65%); some are also excreted in faeces (35%). Less than 1% of a dose is excreted as the unchanged drug. It is not removed by haemodialysis.
- Urinary Excretion<0.1
- Clerance28.3 ml/min/kg
- ToxicityOral, rat LD50 = 136 mg/kg. Symptoms of overdose include dizziness, drowsiness, nausea or vomiting, severe stomach upset, and unusually small pupils.
- LD50 (rat)N/A
- LD50 (mouse)N/A