Pharmacokinetic properties of benzodiazepine hypnotics.
The kinetic properties of three benzodiazepine hypnotics are reviewed. Flurazepam serves as a precursor for at least two rapidly appearing and rapidly cleared metabolites that may contribute to sleep induction and are nonaccumulating. The final metabolite of flurazepam (N-desalkylflurazepam), however, has a long half-life and accumulates during repeated dosage. Temazepam has a relatively slow rate of absorption and an intermediate half-life in the range of 10 to 20 hours. Triazolam has an intermediate rate of absorption; due to its ultrashort half-life (1.5 to 5 hours), triazolam is a non-accumulating hypnotic. Taken together with sleep laboratory studies and clinical trials, knowledge of the kinetic profile of benzodiazepine hypnotics can assist in evaluating their clinical benefits and disadvantages.
D000042:Absorption; D000367:Age Factors; D014151:Anti-Anxiety Agents / Q000378:metabolism*; D004305:Dose-Response Relationship, Drug; D005260:Female; D005479:Flurazepam / Q000031:analogs & derivatives / Q000378:metabolism*; D006207:Half-Life; D006801:Humans; D008297:Male; D012737:Sex Factors; D012890:Sleep / Q000187:drug effects; D013693:Temazepam / Q000378:metabolism*; D014229:Triazolam / Q000378:metabolism*
D014151:Anti-Anxiety Agents; D014229:Triazolam; C033473:didesethylflurazepam; D013693:Temazepam; D005479:Flurazepam