Adam H K, Kay B, Douglas E J
Anaesthesia. 1982 May;37(5):536-40. doi: 10.1111/j.1365-2044.1982.tb01223.x.
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.
在先前报告的临床研究的一个亚组中,检测了单次静脉注射1、2或3mg/kg丙泊酚(得普利麻)后的血药浓度。睡眠时间与剂量之间的线性关系可以用这些剂量下的药代动力学线性来解释。单次注射后,苏醒浓度与剂量无关,平均值为1.04微克/毫升。丙泊酚未出现急性耐受性。重复静脉推注1mg/kg时,睡眠时间最初会延长,但在四次给药后趋于稳定。苏醒浓度与给药次数无关。临床研究结果符合一种分布相非常迅速且消除半衰期短的药物。