Mandrioli R, Forti G Cantelli, Raggi M A
Faculty of Pharmacy, Alma Mater Studiorum--University of Bologna, Department of Pharmaceutical Sciences, Via Belmeloro 6, 40126 Bologna, Italy.
Curr Drug Metab. 2006 Feb;7(2):127-33. doi: 10.2174/138920006775541561.
A review with 103 references. Fluoxetine is the parent drug of the SSRI (selective serotonin reuptake inhibitor) antidepressant class, and is still one of the most highly used drugs of this class world-wide. Fluoxetine now has largely (albeit not completely) substituted older and less safe drugs such as tricyclic antidepressants. Different cytochrome P450 isoforms are involved in the metabolism of fluoxetine, however, the main active metabolite, norfluoxetine, is produced by the CYP2D6 action in the human liver. In this paper, the main metabolic characteristics of fluoxetine will be reviewed, with particular attention paid to the role of cytochrome isozymes. The pharmacological interactions of the drug will be overviewed, especially those concerning other drugs used in psychiatric clinics, such as antipsychotics and antidepressants and the relationships between pharmacological interactions and cytochrome activity will be discussed. Recently, much attention has been drawn to the therapeutic drug monitoring (TDM) of fluoxetine, and in particular to the analysis of fluoxetine enantiomers for which enantiomeric separations and enantioselective metabolism will also briefly be mentioned.
一篇有103篇参考文献的综述。氟西汀是选择性5-羟色胺再摄取抑制剂（SSRI）类抗抑郁药的母体药物，至今仍是该类药物在全球范围内使用最为广泛的药物之一。如今，氟西汀已在很大程度上（尽管并非完全）取代了如三环类抗抑郁药等较老且安全性较低的药物。不同的细胞色素P450同工酶参与氟西汀的代谢，不过，主要活性代谢物去甲氟西汀是由人类肝脏中的CYP2D6作用产生的。本文将对氟西汀的主要代谢特征进行综述，尤其关注细胞色素同工酶的作用。该药物的药理相互作用将进行概述，特别是那些与精神科临床使用的其他药物（如抗精神病药和抗抑郁药）相关的相互作用，并将讨论药理相互作用与细胞色素活性之间的关系。最近，氟西汀的治疗药物监测（TDM）备受关注，尤其会简要提及氟西汀对映体的分析，包括对映体分离和对映选择性代谢。
