Sánchez-Alcaraz A, Sangrador G, Laguarda M, Quintana B
Department of Pharmaceutical Services, Lluis Alcanyis Hospital, Xàtiva, Spain.
J Clin Pharm Ther. 1991 Jun;16(3):209-14. doi: 10.1111/j.1365-2710.1991.tb00306.x.
Midazolam concentration curves versus time were analysed in 10 otherwise healthy patients (ASA I-II) with inferior limb pathologies. The benzodiazepine was used as an adjuvant agent to epidural anaesthesia in view of its lower residual effect compared with other intravenous benzodiazepines. Midazolam pharmacokinetics in these patients fitted an open two-compartment model. The plasma levels versus time corresponded to a biexponential process with a very rapid distribution phase (t1/2a = 5.7 +/- 2.4 min) and an elimination phase (t1/2 beta = 66 +/- 37 min). Mean values for distribution volumes in the central compartment and extrapolated values were Vc = 0.12 +/- 0.04 l/kg and V beta = 1.28 +/- 0.92 l/kg. This kinetic behaviour explains the rapid but short duration of midazolam action. The induction time, estimated from the start of hypnosis (eye closure), was from 60 to 120 s with i.v. injection. The duration of action for the dose administered was from 15 to 60 min, with plasma levels below 90 ng/ml upon eye opening.
对10名患有下肢疾病但其他方面健康的患者(美国麻醉医师协会分级I-II级)的咪达唑仑浓度-时间曲线进行了分析。鉴于与其他静脉注射苯二氮䓬类药物相比,该苯二氮䓬类药物的残留效应较低,故将其用作硬膜外麻醉的辅助药物。这些患者的咪达唑仑药代动力学符合开放二室模型。血浆浓度-时间曲线符合双指数过程,具有非常快速的分布相(t1/2a = 5.7 +/- 2.4分钟)和消除相(t1/2β = 66 +/- 37分钟)。中央室分布容积的平均值和外推值分别为Vc = 0.12 +/- 0.04升/千克和Vβ = 1.28 +/- 0.92升/千克。这种动力学行为解释了咪达唑仑作用迅速但持续时间短的特点。静脉注射后,从催眠开始(闭眼)估计的诱导时间为60至120秒。给药剂量的作用持续时间为15至60分钟,睁眼时血浆浓度低于90纳克/毫升。