The effect of midazolam (Hypnovel) administration on antipyrine pharmacokinetics in humans

1. Twelve healthy volunteers were given a standard regimen of oral midazolam (Hypnovel) (15 mg nightly) for 10 consecutive nights. 2. Antipyrine pharmacokinetics were studied immediately before midazolam administration was started, after the dosage schedule had been completed and one week after dosing had been discontinued. 3. No statistically significant changes were seen in the disposition of antipyrine as assessed by the plasma half-lives, areas under the curve and plasma clearances. Therefore, although previous studies have demonstrated that high doses of midazolam induced the drug-metabolising enzymes in laboratory animals, such effects are unlikely to occur in humans being treated with therapeutic doses.