Dundee J W, Halliday N J, Harper K W, Brogden R N
Drugs. 1984 Dec;28(6):519-43. doi: 10.2165/00003495-198428060-00002.
Midazolam is a short-acting water-soluble benzodiazepine (at pH less than 4), a member of a new class of imidazobenzodiazepine derivatives. At physiological pH the drug becomes much more lipid soluble. Water solubility minimises pain on injection and venous thrombosis compared with diazepam administered in organic solvent. Midazolam is a hypnotic-sedative drug with anxiolytic and marked amnestic properties. To date it has been used mostly by the intravenous route, for sedation in dentistry and endoscopic procedures and as an adjunct to local anaesthetic techniques. It has proved less reliable than thiopentone, but preferable to diazepam, as an intravenous induction agent and is unlikely to replace the other well established drugs. However, due to the cardiorespiratory stability following its administration, midazolam is useful for anaesthetic induction in poor-risk, elderly and cardiac patients. The short elimination half-life (1.5-3.5h) and the absence of clinically important long acting metabolites make midazolam suitable for long term infusion as a sedative and amnestic for intensive care, but clinical trials have yet to be completed. Thus, a combination of properties make midazolam a useful addition to the benzodiazepine group.
咪达唑仑是一种短效水溶性苯二氮䓬类药物(在pH值小于4时),属于新型咪唑并苯二氮䓬衍生物类。在生理pH值下,该药物的脂溶性大大增加。与在有机溶剂中给药的地西泮相比,水溶性使注射时的疼痛和静脉血栓形成降至最低。咪达唑仑是一种具有抗焦虑和显著遗忘特性的催眠镇静药物。迄今为止,它主要通过静脉途径使用,用于牙科和内镜检查中的镇静以及作为局部麻醉技术的辅助药物。作为静脉诱导剂,它已被证明不如硫喷妥钠可靠,但比地西泮更可取,并且不太可能取代其他成熟的药物。然而,由于给药后心肺稳定性良好,咪达唑仑可用于高危、老年和心脏患者的麻醉诱导。较短的消除半衰期(1.5 - 3.5小时)以及缺乏具有临床重要意义的长效代谢产物,使得咪达唑仑适合作为重症监护中的镇静和遗忘药物进行长期输注,但临床试验尚未完成。因此,多种特性使咪达唑仑成为苯二氮䓬类药物中的一种有用补充。