Venlafaxine (VFX) is a serotonin and norepinephrine reuptake inhibitor chiral drug used in therapy as an antidepressant in the form of a racemate consisting of R‐ and S‐VFX. The two enantiomers of VFX exhibit different pharmacological activities: R‐VFX inhibits both norepinephrine and serotonin synaptic reuptake, whereas S‐VFX inhibits only the serotonin one. R‐ and S‐VFX are metabolized in the liver to the respective R‐ and S‐O‐desmethylvenlafaxine (ODVFX), R‐ and S‐N‐desmethylvenlafaxine (NDVFX), and R‐ and S‐N,O‐didesmethylvenlafaxine (NODVFX). The pharmacological profile of ODVFX is close to that of VFX, whereas the other two chiral metabolites (NDVFX and NODVFX) have lower affinity for the receptor sites. The pharmacokinetics of the VFX enantiomers appear stereoselective, including the metabolism process. In the past 20 years, several studies describing the enantioselective analysis of R‐ and S‐VFX in pharmaceutical formulations and its chiral metabolites in biological matrices were published. These methods encompass liquid chromatography coupled with UV detection, mass spectrometry, or tandem mass spectrometry, and capillary electrophoresis. This paper reviews the published methods used for the determination of the individual enantiomers of VFX and its chiral metabolites in different matrices.

中文翻译：

---

文拉法辛及其活性代谢物的对映选择性分析：分离方法学综述。

Venlafaxine（VFX）是5-羟色胺和去甲肾上腺素再摄取抑制剂手性药物，用于治疗抗抑郁药，其消旋体形式为R-和S- VFX。VFX的两种对映异构体表现出不同的药理活性：R ‐VFX抑制去甲肾上腺素和5-羟色胺突触的再摄取，而S ‐VFX仅抑制一种血清素。R-和S- VFX在肝脏中代谢为各自的R-和S - O-去甲基文拉法辛（ODVFX），R-和S - N-去甲基文拉法辛（NDVFX）和R-和S - N，O-去甲基文拉法辛（NODVFX）。ODVFX的药理特性与VFX接近，而其他两种手性代谢物（NDVFX和NODVFX）对受体位点的亲和力较低。VFX对映异构体的药代动力学表现出立体选择性，包​​括代谢过程。在过去的20年中，一些研究描述了R和S的对映选择性分析‐药物制剂中的VFX及其在生物基质中的手性代谢物已发表。这些方法包括液相色谱，紫外检测，质谱或串联质谱以及毛细管电泳。本文回顾了已公开的用于测定不同基质中VFX及其对映体的手性异构体的方法。