Mather L E
University of Sydney at Royal North Shore Hospital St Leonards, Australia.
Minerva Anestesiol. 2005 Sep;71(9):507-16.
Isomers are molecules that have the same number of the same kind of atoms arranged in different ways. There are two major categories of isomers: constitutional (or structural) isomers and stereoisomers. Stereoisomers have identical sets of atoms that are configured in the same positions but are arranged differently spatially. Enantiomers are stereoisomers bearing a mirror image relationship. The pharmacological complication caused by drug racemates is that their component enantiomers usually have different pharmacodynamic effects and different pharmacokinetic properties. Enantioselective pharmacology can occur at any site in the body where a drug interacts with an endogenous chiral centre. The purpose of this presentation is to give some examples where drug chirality is pharmacologically significant to potency, uptake, distribution and elimination. The chosen examples were the anesthetic drugs, thiopentone and bupivacaine.
同分异构体是由相同种类的原子以不同方式排列而成且原子数量相同的分子。同分异构体主要分为两大类:构造(或结构)异构体和立体异构体。立体异构体具有相同的原子组,这些原子在相同位置构型相同,但在空间上排列不同。对映体是具有镜像关系的立体异构体。药物外消旋体引起的药理学并发症在于其组成对映体通常具有不同的药效学效应和不同的药代动力学性质。对映体选择性药理学可发生在体内药物与内源性手性中心相互作用的任何部位。本报告的目的是给出一些药物手性在效力、摄取、分布和消除方面具有药理学意义的例子。所选择的例子是麻醉药物硫喷妥钠和布比卡因。