利多卡因、普鲁卡因胺和哌替啶在绵羊后肢组织中的体外摄取与代谢

The in vitro uptake and metabolism of lignocaine, procainamide and pethidine by tissues of the hindquarters of sheep.

Upton R N, Mather L E, Runciman W B

Department of Anaesthesia and Intensive Care, Flinders University of South Australia, Bedford Park.

Xenobiotica. 1991 Jan;21(1):1-12. doi: 10.3109/00498259109039445.

Abstract

In vitro studies using tissue slices or tissue homogenates of liver, skeletal muscle, fat skin and blood were conducted to determine whether the uptake of procainamide, lignocaine and pethidine into the hindquarters of sheep was due to distribution or metabolism. Both homogenates and slice preparations of liver showed significant metabolism or uptake, confirming the viability of the preparations. 2. None of the drugs was metabolized in blood and there was minimal uptake of the drugs into the skin. 3. There was metabolism of pethidine in skeletal muscle and substantial uptake of pethidine into fat, indicating that the rapid rate of uptake and prolonged elution of pethidine in the hindquarters was due to both distribution and metabolism. 4. No metabolism of lignocaine in muscle was found, but there was substantial uptake into fat, indicating that the rapid rate of uptake and prolonged elution of lignocaine in the hindquarters was due to its distribution into fat. 5. There was negligible uptake of procainamide into either muscle or fat, presumably due to its relatively low lipophilicity.

摘要

进行了体外研究，使用肝脏、骨骼肌、脂肪、皮肤和血液的组织切片或组织匀浆来确定普鲁卡因胺、利多卡因和哌替啶在绵羊后肢的摄取是由于分布还是代谢。肝脏的匀浆和切片制剂均显示出显著的代谢或摄取，证实了制剂的活性。2. 这些药物在血液中均未代谢，且药物在皮肤中的摄取极少。3. 哌替啶在骨骼肌中发生代谢，且大量摄取进入脂肪，表明哌替啶在后肢的快速摄取率和延长洗脱是由于分布和代谢两者。4. 未发现利多卡因在肌肉中有代谢，但大量摄取进入脂肪，表明利多卡因在后肢的快速摄取率和延长洗脱是由于其分布到脂肪中。5. 普鲁卡因胺在肌肉或脂肪中的摄取可忽略不计，大概是由于其相对较低的亲脂性。