Blood disoprofol levels in anesthetised patients. Correlation of concentrations after single or repeated doses with hypnotic activity.

The blood concentrations of disoprofol (Diprivan) after single intravenous doses of 1, 2 or 3 mg/kg have been examined in a subpopulation from previously reported clinical studies. The linear relationship between sleep time and dose could be explained by the linearity of the pharmacokinetics at these doses. After a single injection the awakening concentration was independent of dose, with a mean value of 1.04 micrograms/ml. No acute tolerance occurred with disoprofol. On repeated 1 mg/kg bolus injections the sleeping time rose initially but stabilised after four doses. The waking concentration was independent of the number of doses administered. The clinical findings fitted an agent with a very rapid distribution phase and a short elimination half-life.