- Molecular NameLorazepam
- Synonym(+/-)-Lorazepam; L-Lorazepam Acetate; O-Chlorooxazepam; O-Chloroxazepam
- Weight321.163
- Drugbank_IDDB00186
- ACS_NO846-49-1
- Show 3D model
- LogP (experiment)2.45
- LogP (predicted, AB/LogP v2.0)2.52
- pka1.3, 11.5
- LogD (pH=7, predicted)2.52
- Solubility (experiment)0.08 mg/ml
- LogS (predicted, ACD/Labs)(ph=7)-3.56
- LogSw (predicted, AB/LogsW2.0)0.02
- Sw (mg/ml) (predicted, ACD/Labs)0.09
- No.of HBond Donors2
- No.of HBond Acceptors4
- No.of Rotatable Bonds1
- TPSA61.69
- StatusFDA approved
- AdministrationN/A
- PharmacologyLorazepam's principal use has been in treating the symptom of anxiety.
- Absorption_value95.0
- Absorption (description)Readily absorbed after oral administration.
- Caco_2N/A
- Bioavailability93.0
- Protein binding91.0
- Volume of distribution (VD)1.3 L/kg
- Blood/Plasma Partitioning ratio (D_blood)N/A
- MetabollsmHepatic glucuronidation
- Half life14 h
- ExcretionAbout 75% of a dose is excreted in the urine as the inactive glucuronide conjugate within 5 days (up to about 50% in the first 24 h) and 14% is excreted as conjugates of minor metabolites which include ring-hydroxylation products and quinazoline derivatives; only negligible amounts are excreted as free lorazepam; about 7% of a dose is eliminated in the faeces. Lorazepam is a metabolite of lormetazepam.
- Urinary Excretion<1
- Clerance1.1 ml/min/kg
- ToxicityPlasma concentrations of 0.3 to 0.6 mg/L were reported in 3 subjects suffering toxic effects after the ingestion of overdoses of lorazepam; the estimated amounts ingested were 100 and 120 mg in 2 of the cases. The subjects recovered within 24 to 30 h [M. D. Allen et al.,Am. J. Psychiatry,1980, 137, 1414–1415].
- LD50 (rat)N/A
- LD50 (mouse)LD50=3178mg/kg