Eichelbaum M
Dr Margarete Fischer-Bosch-Institut für Klinische Pharmakologie, Stuttgart, Federal Republic of Germany.
Biochem Pharmacol. 1988 Jan 1;37(1):93-6. doi: 10.1016/0006-2952(88)90758-7.
The examples discussed demonstrate the importance of stereoselective drug metabolism and raise the question of whether the therapeutic use of racemic drugs is still justified. There is no straightforward answer to this question. If only quantitative differences in therapeutic activity exist and the less active enantiomer is not predominantly responsible for side effects, the therapeutic benefit gained by using the more active enantiomer is only marginal and does not justify the substantial increase in costs involved in manufacturing such a drug preparation. However, if stereoselectivity in therapeutic activity is pronounced and adverse drug reactions are caused mainly by the less active isomer then an isomeric pure drug preparation should be used.
所讨论的例子证明了立体选择性药物代谢的重要性，并提出了外消旋药物的治疗用途是否仍然合理的问题。对于这个问题没有简单直接的答案。如果仅存在治疗活性的定量差异，且活性较低的对映体并非主要导致副作用，那么使用活性较高的对映体所获得的治疗益处仅为边际效益，并不足以证明生产这种药物制剂所涉及的成本大幅增加是合理的。然而，如果治疗活性中的立体选择性很显著，且药物不良反应主要由活性较低的异构体引起，那么就应该使用纯异构体药物制剂。
