Hamunen K, Maunuksela E L, Seppälä T, Olkkola K T
Department of Ophthalmology, University of Helsinki, Finland.
Br J Anaesth. 1993 Dec;71(6):823-6. doi: 10.1093/bja/71.6.823.
We have studied the pharmacokinetics of i.v. and rectal pethidine in 20 children age 4-8 yr undergoing ophthalmic surgery. After i.v. administration, the clearance of pethidine was mean 10.4 (SD 1.7) ml kg-1 min-1, volume of distribution at steady state 2.8 (0.6) litre kg-1 and elimination half-life 3.0 (0.5) h. After rectal administration, plasma pethidine concentrations varied greatly and peak concentrations appeared late, at 147 (44) min. The mean systemic bioavailability after rectal administration was approximately 55%. Because the bioavailability of rectal pethidine varies greatly, this route is not encouraged in the management of acute pain.
我们研究了20名4至8岁接受眼科手术的儿童静脉注射和直肠给予哌替啶后的药代动力学。静脉注射给药后,哌替啶的清除率平均为10.4(标准差1.7)毫升/千克/分钟,稳态分布容积为2.8(0.6)升/千克,消除半衰期为3.0(0.5)小时。直肠给药后,血浆哌替啶浓度差异很大,峰值浓度出现较晚,在147(44)分钟时出现。直肠给药后的平均全身生物利用度约为55%。由于直肠给予哌替啶的生物利用度差异很大,在急性疼痛管理中不鼓励使用该途径。