- Molecular NameClonazepam
- SynonymChlonazepam; Clonazepamum
- Weight315.716
- Drugbank_IDDB01068
- ACS_NO1622-61-3
- Show 3D model
- LogP (experiment)2.41
- LogP (predicted, AB/LogP v2.0)2.57
- pka1.5, 10.5
- LogD (pH=7, predicted)2.57
- Solubility (experiment)Insoluble
- LogS (predicted, ACD/Labs)(ph=7)-4.12
- LogSw (predicted, AB/LogsW2.0)0.03
- Sw (mg/ml) (predicted, ACD/Labs)0.02
- No.of HBond Donors1
- No.of HBond Acceptors6
- No.of Rotatable Bonds2
- TPSA90.29
- StatusFDA approved
- AdministrationOral, I.M., I.V, sublingual
- PharmacologyA benzodiazepine derivative with anticonvulsant, muscle relaxant, and anxiolytic properties.
- Absorption_value100.0
- Absorption (description)Rapidly absorbed after oral administration with peak plasma levels found after about 4 h.
- Caco_2N/A
- Bioavailability98.0
- Protein binding86.0
- Volume of distribution (VD)3.2 L/kg
- Blood/Plasma Partitioning ratio (D_blood)N/A
- MetabollsmThe major metabolic reaction catalysed by cytochrome P450 isoenzyme CYP3A4, is reduction of the nitro group to 7-aminoclonazepam, followed by acetylation to 7-acetamidoclonazepam; 7-aminoclonazepam is slightly active and is found in plasma at concentrations similar to those of clonazepam. 3-Hydroxylation of clonazepam and its two metabolites may also occur, followed by conjugation with glucuronic acid or sulfate.
- Half life23 h
- ExcretionClonazepam crosses the placental barrier and is excreted in breast milk. Less than 1% of a dose is excreted unchanged in the urine in 24 h. Urinary excretion accounts for up to 70% of a dose, as both free and conjugated metabolites, over a period of 7 days, of which about 50% consists of 7-aminoclonazepam and 7-acetamidoclonazepam.
- Urinary Excretion<1
- Clerance1.55 ml/min/kg.
- ToxicityToxicity is associated with plasma concentrations greater than 0.1 mg/L.
- LD50 (rat)N/A
- LD50 (mouse)N/A