- Molecular NameAlprazolam
- Synonymalprazolam; TUS-1
- Weight308.772
- Drugbank_IDDB00404
- ACS_NO28981-97-7
- Show 2D model
- LogP (experiment)2.12
- LogP (predicted, AB/LogP v2.0)2.45
- pka6.2
- LogD (pH=7, predicted)2.43
- Solubility (experiment)Insoluble
- LogS (predicted, ACD/Labs)(ph=7)-4.15
- LogSw (predicted, AB/LogsW2.0)0.03
- Sw (mg/ml) (predicted, ACD/Labs)0.02
- No.of HBond Donors0
- No.of HBond Acceptors4
- No.of Rotatable Bonds1
- TPSA42.55
- StatusFDA approved
- AdministrationN/A
- PharmacologyA short-acting drug of the benzodiazepine class. It is primarily used to treat moderate to severe anxiety disorders and panic attacks, and is used as an adjunctive treatment for anxiety associated with moderate depression.
- Absorption_value90.0
- Absorption (description)Readily absorbed after oral administration
- Caco_2N/A
- Bioavailability88.0
- Protein binding71.0
- Volume of distribution (VD)0.72 L/kg
- Blood/Plasma Partitioning ratio (D_blood)N/A
- MetabollsmHepatic, via Cytochrome P450 3A4. The major metabolites are α-hydroxyalprazolam, 4-hydroxyalprazolam (both active), and a benzophenone derivative of alprazolam.
- Half life12 h
- ExcretionAbout 80% of a dose is excreted in the urine in 72 h of which 11% is unchanged drug, 15% is α-hydroxyalprazolam, and 9% is the benzophenone metabolite. Small amounts of desmethylalprazolam and 4-hydroxyalprazolam are also excreted in the urine. About 7% of a dose is eliminated in the faeces.
- Urinary Excretion20
- Clerance0.74 mL/min/kg.
- ToxicityOral, mouse: LD50=1020 mg/kg. Symptoms of overdose include confusion, coma, impaired coordination, sleepiness, and slowed reaction time.
- LD50 (rat)N/A
- LD50 (mouse)N/A