title: Comparative pharmacokinetics of brotizolam and triazolam in healthy subjects.
abstract: Pharmacokinetics of oral brotizolam (0.50 mg) and triazolam (0.50 mg) were studied in healthy young volunteers. The plasma concentration profile of brotizolam can be described as a one compartmental open model with first-order absorption. The absorption of triazolam was less regular and in half of the subjects was not consistent with first-order kinetics. Inter-individual variability in absorption rate (peak times) was larger for brotizolam. Mean peak times were 1.1 +/- 1.0 h for brotizolam and 1.2 +/- 0.5 h for triazolam. Mean peak concentrations were 7.3 +/- 3.1 ng/ml and 5.0 +/- 3.9 ng/ml respectively. The elimination half-life of brotizolam was twice that of triazolam with mean values of 5.0 +/- 1.1 h and 2.6 +/- 0.7 h respectively. There was no correlation between the half-lives of the two drugs. Protein unbound fraction was similar for triazolam and brotizolam with mean values of 9.9 +/- 1.5% and 8.4 +/- 0.7% respectively.
mesh_terms: D000284:Administration, Oral; D000328:Adult; D014151:Anti-Anxiety Agents / Q000378:metabolism*; D001381:Azepines / Q000008:administration & dosage / Q000378:metabolism*; D005260:Female; D006207:Half-Life; D006801:Humans; D006993:Hypnotics and Sedatives / Q000008:administration & dosage / Q000378:metabolism*; D007408:Intestinal Absorption; D007700:Kinetics; D008297:Male; D011485:Protein Binding; D014229:Triazolam / Q000378:metabolism*
chemical_list: D014151:Anti-Anxiety Agents; D001381:Azepines; D006993:Hypnotics and Sedatives; D014229:Triazolam; C020960:brotizolam