- Molecular NameBromazepam
- Synonym7-Bromo-5-(2-pyridyl)-3H-1,4-benzodiaxepin-2(1H)-one; 7-Bromo-5-(2-pyridyl)-3H-1,4-benzodiazepin-2(1H)-one; Bromazepamum [inn-latin]
- Weight316.158
- Drugbank_IDDB01558
- ACS_NO1812-30-2
- Show 3D model
- LogP (experiment)2.05
- LogP (predicted, AB/LogP v2.0)2.04
- pka2.9, 11.0
- LogD (pH=7, predicted)2.03
- Solubility (experiment)N/A
- LogS (predicted, ACD/Labs)(ph=7)-2.74
- LogSw (predicted, AB/LogsW2.0)0.13
- Sw (mg/ml) (predicted, ACD/Labs)0.57
- No.of HBond Donors1
- No.of HBond Acceptors4
- No.of Rotatable Bonds1
- TPSA54.35
- StatusFDA approved
- AdministrationN/A
- PharmacologyA benzodiazepine derivative drug, developed in the 1970s.
- Absorption_value84.0
- Absorption (description)Well absorbed after oral administration and peak plasma concentrations are usually achieved within 2 h.
- Caco_2N/A
- BioavailabilityN/A
- Protein binding70.0
- Volume of distribution (VD)0.9 L/kg
- Blood/Plasma Partitioning ratio (D_blood)N/A
- MetabollsmBromazepam is reported to be metabolized by a hepatic enzyme belonging to the Cytochrome P450 family of enzymes. In 2003, a team led by Dr. Oda Manami at Oita Medical University reported that CYP3A4 was not the responsible enzyme, seeing as itraconazole, a known inhibitor of CYP3A4, did not effect its metabolism.
- Half life8~19 h
- ExcretionAbout 70% of a dose is excreted in the urine in 72 h, including about 2% of the dose as unchanged bromazepam, about 27% as the glucuronide of 3-hydroxybromazepam, about 40% as the glucuronide of 2-amino-5-bromo-3-hydroxybenzoylpyridine, and less than 1% as 2-(2-amino-5-bromobenz-oyl)-pyridine.
- Urinary ExcretionN/A
- CleranceN/A
- ToxicityIn a 68-year-old woman who was found unconscious and barely breathing, bromazepam intoxication was discovered to be the cause (a serum level of 6 mg/L was detected); normal functions were restored 12 days after the ingestion. [J. Rudolf et al.,Dtsch. Med. Wochenschr.,1998, 123, 832–834.]
- LD50 (rat)N/A
- LD50 (mouse)N/A