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生物大分子的有序不对称性使它们能区别象氨基酸和糖这样的单体化合物的光学异构体,而药物的药理活性常与一种异构体有关,但许多药物仍以外消旋体的型式应用。本文从药物动力学和药效学的观点出发,论述了临床常用的外消旋药物及其对映体的临床药理,并指出合理调控药物对映体的比值或单独选用一种活性对映体对减少毒副作用和提高临床治疗效果的重要意义。药物对映体活性的药效动力学差异采用组织灌流技术和在整体动物比较了一系列药物对映体(Enantiomers)的生物活性的大量报道均证明;药物与组织细胞成分间的相互作用具有立体选择性的特性。例如,肾上腺
The orderly asymmetry of biological macromolecules allows them to distinguish between optical isomers of monomeric compounds such as amino acids and sugars, and the pharmacological activity of the drug is often associated with one isomer, but many drugs are still present as racemates The type of application. In this paper, from the point of view of pharmacokinetics and pharmacodynamics, the clinical pharmacology of clinically used racemic drugs and their enantiomers are discussed. The rationale of rational control of the enantiomeric ratio of drugs or the selective use of one active enantiomer To reduce the side effects and improve the clinical treatment of significance. Pharmacodynamic differences in drug enantiomeric activity demonstrated extensively using tissue perfusion techniques and comparing a series of bioactivities of enantiomers in whole animals; the interaction between drug and tissue cell components is stereoscopic Selective features. For example, the adrenal gland