- Molecular NameQuazepam
- SynonymQuazepamum [inn-latin]
- Weight386.8
- Drugbank_IDDB01589
- ACS_NO36735-22-5
- Show 3D model
- LogP (experiment)4.03
- LogP (predicted, AB/LogP v2.0)4.53
- pkaN/A
- LogD (pH=7, predicted)4.53
- Solubility (experiment)N/A
- LogS (predicted, ACD/Labs)(ph=7)-5.75
- LogSw (predicted, AB/LogsW2.0)0.0
- Sw (mg/ml) (predicted, ACD/Labs)0.0
- No.of HBond Donors0
- No.of HBond Acceptors2
- No.of Rotatable Bonds3
- TPSA47.69
- StatusFDA approved
- AdministrationN/A
- PharmacologyA drug which is a benzodiazepine derivative. Quazepam is indicated for the treatment of insomnia including sleep induction and sleep maintenance.
- Absorption_valueN/A
- Absorption (description)Quazepam is rapidly (absorption half-life of about 30 minutes) and well absorbed from the gastrointestinal tract.
- Caco_2N/A
- Bioavailability32.0
- Protein binding95.0
- Volume of distribution (VD)At bedtime, 5 L/kg and in the morning, 8.6 L/kg
- Blood/Plasma Partitioning ratio (D_blood)N/A
- MetabollsmThe active metabolites of quazepam are 2-oxoquazepam and N-desalkyl-2-oxoquazepam. The N-desalkyl-2-oxoquazepam metabolite has only limited pharmacological activity compared to the parent compound quazepam and the active metabolite 2-oxoquazepam. Quazepam and its major active metabolite 2-oxoquazepam both show high selectivity for the type1 GABAA receptors.
- Half life39 h
- ExcretionIt is eliminated both renally and through feces.
- Urinary ExcretionN/A
- CleranceN/A
- ToxicityAdverse events most frequently encountered in patients treated with quazepam are daytime drowsiness (12%) and headache (4.5%). Fatigue, dizziness, dry mouth, dyspepsia have been reported with frequency more than 1%.
- LD50 (rat)N/A
- LD50 (mouse)N/A