Deng Chaoyi, Liu Jin, Zhang Wensheng
Department of Anesthesiology, West China Hospital, Sichuan University, Chengdu, China.
Laboratory of Anesthesia and Critical Care Medicine, National-Local Joint Engineering Research Center of Translational Medicine of Anesthesiology, West China Hospital, Sichuan University, Chengdu, China.
Front Pharmacol. 2022 Jul 1;13:923353. doi: 10.3389/fphar.2022.923353. eCollection 2022.
Among the advancements in drug structural modifications, the increased focus on drug metabolic and pharmacokinetic properties in the anesthetic drug design process has led to significant developments. Drug metabolism also plays a key role in optimizing the pharmacokinetics, pharmacodynamics, and safety of drug molecules. Thus, in the field of anesthesiology, the applications of pharmacokinetic strategies are discussed in the context of sedatives, analgesics, and muscle relaxants. In this review, we summarize two approaches for structural optimization to develop anesthetic drugs, by designing prodrugs and soft drugs. Drugs that both failed and succeeded during the developmental stage are highlighted to illustrate how drug metabolism and pharmacokinetic optimization strategies may help improve their physical and chemical properties.
在药物结构修饰的进展中，麻醉药物设计过程中对药物代谢和药代动力学性质的日益关注带来了重大发展。药物代谢在优化药物分子的药代动力学、药效学和安全性方面也起着关键作用。因此，在麻醉学领域，药代动力学策略在镇静剂、镇痛药和肌肉松弛剂方面的应用得到了讨论。在本综述中，我们总结了两种通过设计前药和软药来开发麻醉药物的结构优化方法。文中突出了在开发阶段失败和成功的药物，以说明药物代谢和药代动力学优化策略如何有助于改善它们的物理和化学性质。
