- Molecular NameBrotizolam
- SynonymNA
- Weight393.696
- Drugbank_IDN/A
- ACS_NO57801-81-7
- Show 2D model
- LogP (experiment)2.79
- LogP (predicted, AB/LogP v2.0)2.75
- pka6.2
- LogD (pH=7, predicted)2.75
- Solubility (experiment)N/A
- LogS (predicted, ACD/Labs)(ph=7)-4.45
- LogSw (predicted, AB/LogsW2.0)0.07
- Sw (mg/ml) (predicted, ACD/Labs)0.01
- No.of HBond Donors0
- No.of HBond Acceptors4
- No.of Rotatable Bonds1
- TPSA70.79
- StatusN/A
- AdministrationN/A
- PharmacologyA sedative-hypnotic thienodiazepine drug which is a benzodiazepine analog.
- Absorption_valueN/A
- Absorption (description)Brotizolam is rapidly absorbed after oral administration
- Caco_2N/A
- Bioavailability70.0
- Protein binding92.0
- Volume of distribution (VD)0.40 to 0.77 L/kg
- Blood/Plasma Partitioning ratio (D_blood)N/A
- MetabollsmCompletely metabolised to two major hydroxylated metabolites including 6-hydroxylated brotizolam.
- Half lifeN/A
- ExcretionThe drug is more slowly absorbed in the elderly and metabolic clearance is impaired. The metabolites are excreted in urine as glucuronide and sulfate conjugates, approximately 65%, and in faeces (22%). 2 to 3% of the dose is excreted unchanged. Brotizolam is rapidly distributed throughout the body.
- Urinary ExcretionN/A
- CleranceFor the elderly: 109 mL/min and the young: 40 mL/min.
- ToxicityA 42-year-old man was found dead and a toxicological screening carried out on his blood, urine and stomach contents. In his blood, 10.4 μg/L brotizolam, 3000 μg/L ibuprofen and 130 μg/L dihydrocodeine were found. In his urine, the brotizolam metabolite We 964, α-OH-triazolam, ibuprofen, dihydrocodeine and phenylpropanolamine were found at varying concentrations. Brotizolam and ibuprofen were both detected in stomach contents. It was determined that death occurred due to a combination of these drugs and alcohol poisoning. [T. Saito et al.,J. Anal. Toxicol.,1997, 21, 584–586].
- LD50 (rat)N/A
- LD50 (mouse)N/A