Pharmacokinetics and Drug Interactions of the Sedative Hypnotics

Sleep complaints are common among patients and may be associated with mild to severe clinical symptoms. The use of hypnotic agents to improve the onset and quality of sleep has a history dating back centuries. Currently, several benzodiazepines and nonbenzodiazepines are widely used as sedative-hypnotic drugs. The pharmacokinetic and pharmacodynamic profiles of these agents vary substantially, allowing them to be chosen for different clinical situations and tailored to specific sleep complaints. The short-acting benzodiazepines and benzodiazepine agonists have become the most widely prescribed sedative hypnotics because of their short to ultrashort half-life and low tendency to impair cognitive and psychomotor performance on the day following nighttime use. In the current review, we summarize the pharmacokinetic and drug interaction profiles of the Food and Drug Administration-approved benzodiazepine sedative hypnotics: estazolam, flurazepam, quazepam, temazepam, and triazolam. In addition, alprazolam is included because of its popularity for this use, and two benzodiazepine receptor agonists, zolpidem and zaleplon, are reviewed. The presented data will provide clinicians with insight into the pharmacokinetic profiles of several popular sedative hypnotic agents and provide guidelines to help them recognize or avoid drug interactions. Psychopharmacology Bulletin. 2003;37(1):10-29.