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米那索龙的临床效果与药代动力学。亚麻醉输注方案。

Minaxolone, clinical effects and pharmacokinetics. Subanaesthetic infusion regimen.

作者信息

Mather L E, Seow L T, Gourlay G K, Roberts J G, Cousins M J

出版信息

Anaesthesia. 1981 Jun;36(6):586-91. doi: 10.1111/j.1365-2044.1981.tb10321.x.

DOI:10.1111/j.1365-2044.1981.tb10321.x
PMID:7270827
Abstract

Minaxolone, infused at a constant rate of 0.01 mg/kg/min produced drowsiness followed by a sleep-like state from which subjects could be easily awakened. After the infusion was stopped, initial recovery was rapid, and completed within 45 minutes. The ability to produce this state rapidly and reversibly would have great value in outpatient surgery, short operative procedures and for basal sedation during procedures performed under regional anaesthesia. In common with many intravenous induction agents, involuntary skeletal muscle movement and twitching during the latter part of the infusion regimen was observed in some subjects. The rapid recovery was consistent with the pharmacokinetic characteristics of Minaxolone, i.e. high total body clearance (near or even exceeding that of indocyanine green) and rapid redistribution. However, renal clearance of unchanged Minaxolone was negligible.

摘要

米那索龙以0.01毫克/千克/分钟的恒定速率输注会导致嗜睡,随后进入类似睡眠的状态,在此状态下受试者很容易被唤醒。停止输注后,最初的恢复很快,在45分钟内完成。快速且可逆地产生这种状态的能力在门诊手术、短小手术过程以及区域麻醉下手术期间的基础镇静中具有很大价值。与许多静脉诱导剂一样,在部分受试者中观察到输注方案后期出现不自主骨骼肌运动和抽搐。快速恢复与米那索龙的药代动力学特征一致,即全身清除率高(接近甚至超过吲哚菁绿)且再分布迅速。然而,未改变的米那索龙的肾清除率可忽略不计。

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