Department of Anaesthesiology, Medisch Spectrum Twente, Enschede, The Netherlands.
Clin Drug Investig. 1998;16(3):241-50. doi: 10.2165/00044011-199816030-00008.
The aim of this investigation was to compare the clinical effects and pharmacokinetics of lidocaine and prilocaine in two groups of 15 patients undergoing axillary brachial plexus anaesthesia.
The study had a randomised design. Patients were allocated to one of the two groups of 15. Each group received either lidocaine (600mg = 2.56 mmol/L + 5 mg/L adrenaline) or prilocaine (600mg = 2.72 mmol/L + 5 mg/L adrenaline), injected over a period of 30 seconds. Onset of the surgical analgesia was defined as the period from the end of the injection of the local anaesthetic to the loss of pinprick sensation in the distribution of all three nerves.
The mean onset time of surgical analgesia of both lidocaine and prilocaine was 10 minutes. Lidocaine was biexponentially eliminated with a rapid elimination phase half-life (t((1/2)alpha)) of 9.95 +/- 14.3 minutes and a terminal elimination phase half-life (t((1/2)beta)) of 2.86 +/- 1.55 hours. Lidocaine was metabolised to MEGX (monoethylglycylxylidide); time to reach maximum plasma concentration (tmax) 2.3 +/- 0.8 hours; maximum plasma concentration (C(max)) 0.32 +/- 0.13 mg/L; t((1/2)beta) 2.4 +/- 2.4 hours. Lidocaine total body clearance was 67.8 +/- 28.8 L/h. Prilocaine was rapidly and biexponentially eliminated with a t((1/2)alpha) of 9.4 +/- 18.4 minutes and a t((1/2)beta) of 2.12 +/- 1.28 hours. The total body clearance of prilocaine (150 +/- 53 L/h) was higher than that of lidocaine (p = 0.0255). Both compounds demonstrated a comparable volume of distribution (Vd), while the volume of distribution at steady-state (V(ss)) and the volume of distribution in the second compartment (V(beta)) values of prilocaine were a factor of 1.6 higher than those of lidocaine (p < 0.001). Both compounds showed a comparable t((1/2)alpha) (p > 0.8) and a comparable t((1/2)beta) (p = 0.26).
Following axillary administration, lidocaine and prilocaine demonstrated similar pharmacokinetic behaviour and could therefore be used as the clinical preference for this regional anaesthesia technique.
本研究旨在比较利多卡因和丙泊酚在两组接受腋路臂丛神经阻滞麻醉的 15 例患者中的临床效果和药代动力学。
本研究采用随机设计。患者被分配到两组中的一组 15 例。每组均给予利多卡因(600mg = 2.56mmol/L + 5mg/L 肾上腺素)或丙泊酚(600mg = 2.72mmol/L + 5mg/L 肾上腺素),在 30 秒内注射完毕。手术镇痛的起始时间定义为局部麻醉注射结束至所有三支神经分布区针刺痛觉丧失的时间。
两组利多卡因和丙泊酚的平均手术镇痛起始时间均为 10 分钟。利多卡因呈双指数消除,快速消除相半衰期(t((1/2)alpha))为 9.95 +/- 14.3 分钟,终末消除相半衰期(t((1/2)beta))为 2.86 +/- 1.55 小时。利多卡因代谢为 MEGX(单乙基甘氨酰二甲酰胺);达峰时间(tmax)为 2.3 +/- 0.8 小时;最大血浆浓度(C(max))为 0.32 +/- 0.13mg/L;t((1/2)beta)为 2.4 +/- 2.4 小时。利多卡因的总清除率为 67.8 +/- 28.8L/h。丙泊酚快速双指数消除,t((1/2)alpha)为 9.4 +/- 18.4 分钟,t((1/2)beta)为 2.12 +/- 1.28 小时。丙泊酚的总清除率(150 +/- 53L/h)高于利多卡因(p = 0.0255)。两种化合物的分布容积(Vd)相似,而丙泊酚的稳态分布容积(V(ss))和第二隔室分布容积(V(beta))值均比利多卡因高 1.6 倍(p < 0.001)。两种化合物的 t((1/2)alpha)(p > 0.8)和 t((1/2)beta)(p = 0.26)相似。
腋路给药后,利多卡因和丙泊酚表现出相似的药代动力学行为,因此可根据临床需要选择该区域麻醉技术。