Slaughter R L, Edwards D J
Department of Pharmacy Practice, College of Pharmacy and Allied Health Professions, Wayne State University, Detroit, MI 48202, USA.
Ann Pharmacother. 1995 Jun;29(6):619-24. doi: 10.1177/106002809502900612.
Successful application of information on cytochrome P450 to prevent drug interactions and improve the therapeutic risk: benefit ratio can occur only if we know which enzyme is responsible for the metabolism of a drug. Until recently, this information was not usually available when new drugs reached the market. It is not enough to know the fraction of a dose metabolized versus excreted unchanged or the metabolic pathways by which a compound is degraded. Studies conducted during drug development must identify the enzyme or enzymes involved in the metabolism of new drugs. In addition, the ability of new drugs to inhibit or induce the activity of the key P450 enzymes must be known if we are to take full advantage of our current knowledge of how the cytochrome P450 system works.
只有当我们知道哪种酶负责药物代谢时,细胞色素P450信息才能成功应用于预防药物相互作用并改善治疗风险效益比。直到最近,新药上市时通常还没有这些信息。仅知道药物剂量中经代谢与未经变化排泄的比例或化合物降解的代谢途径是不够的。药物研发过程中进行的研究必须确定参与新药代谢的一种或多种酶。此外,如果我们要充分利用目前对细胞色素P450系统工作方式的了解,就必须知道新药抑制或诱导关键P450酶活性的能力。