Pharmacokinetics of nitrazepam in saliva and serum after a single oral dose.
The pharmacokinetics of nitrazepam in saliva and serum was studied in 12 healthy volunteers after a single administration of a 5 mg nitrazepam tablet. The binding of nitrazepam to plasma proteins was determined 4 hours after the administration by ultracentrifugation. The analysis of nitrazepam concentrations was performed by 63Ni-EC-GLC. The pharmacokinetic parameters were evaluated manually or by AUTOAN-program in serum, and manually in saliva. The concentrations of nitrazepam in serum and saliva correlated significantly (r = 0.472, P less than 0.001, n = 97). The ratio saliva: serum was, however, time dependent. The protein free fraction in serum was significantly higher (P less than 0.01) than the salivary concentration at the same time (4 hours after administration). The peak concentrations in serum and saliva were 40.7 and 1.9 ng/ml (P less than 0.001) and the times to reach the peak maximum 2.4 and 2.5 hours, respectively (difference not significant). The mean half-life of nitrazepam in serum was 30.5 hrs and in saliva 39.9 hrs, the difference being significant at P less than 0.05. The distribution phase parameters, poorly described before, were calculated. The clinical value of nitrazepam analysis in saliva seems to be negligible.
D000284:Administration, Oral; D000328:Adult; D001798:Blood Proteins / Q000378:metabolism; D006801:Humans; D007700:Kinetics; D008297:Male; D009567:Nitrazepam / Q000008:administration & dosage / Q000097:blood / Q000378:metabolism*; D011485:Protein Binding; D012463:Saliva / Q000378:metabolism*; D012471:Salivary Proteins and Peptides / Q000378:metabolism
D001798:Blood Proteins; D012471:Salivary Proteins and Peptides; D009567:Nitrazepam