Kanto J, Aaltonen L, Erkkola R, Aärimaa L
Acta Anaesthesiol Scand. 1984 Feb;28(1):116-8. doi: 10.1111/j.1399-6576.1984.tb02024.x.
Midazolam, the new investigational 1,4-benzodiazepine derivative with highly water-soluble salts, was studied as an anaesthesiological adjuvant in 11 patients undergoing elective caeserean section under epidural analgesia. I.v. administered midazolam, 0.075 mg/kg after delivery, caused a rapid and marked sedative effect, lasting for about 2-3 h. Short-lasting anterograde amnesia of about 30 to 60 min was reported as well. The serum levels of the parent drug and its active metabolites were determined in six cases by a radioreceptor assay and pharmacokinetic parameters were calculated on the basis of these levels by a two-compartment open model. Up to 3 h after midazolam administration, good correlation between the sedative effect and serum drug levels was found. The rapid but short-lasting action can be explained by the pharmacokinetic parameters of midazolam: a short distribution phase half-life (4.19 min), and a short elimination phase half-life (67.85 min) due to a high clearance value (13.18 ml/min/kg) and a moderate distribution volume (1.20 l/kg).
咪达唑仑是一种新型的研究用1,4 -苯二氮䓬衍生物，其盐具有高度水溶性。我们对11例在硬膜外镇痛下接受择期剖宫产手术的患者进行了研究，将其作为麻醉辅助药物。分娩后静脉注射0.075 mg/kg的咪达唑仑，产生了快速且显著的镇静效果，持续约2 - 3小时。还报告了约30至60分钟的短暂顺行性遗忘。通过放射受体分析法测定了6例患者母体药物及其活性代谢物的血清水平，并基于这些水平通过二室开放模型计算了药代动力学参数。咪达唑仑给药后3小时内，发现镇静效果与血清药物水平之间具有良好的相关性。咪达唑仑快速但短暂的作用可以由其药代动力学参数来解释：分布相半衰期短（4.19分钟），消除相半衰期短（67.85分钟），这是由于清除率高（13.18 ml/min/kg）和分布容积适中（1.20 l/kg）。
