Pfizer, Inc., (formerly Wyeth Research), Collegeville, PA 19426, USA.
Expert Opin Drug Metab Toxicol. 2010 Dec;6(12):1565-74. doi: 10.1517/17425255.2010.535810. Epub 2010 Nov 11.
genetic and pharmacologically-driven variations in common mechanisms involved in the disposition of antidepressant medications may contribute to variable interpatient response. This review describes the pharmacological properties underlying the safety and efficacy of desvenlafaxine, a second-generation serotonin-norepinephrine reuptake inhibitor (SNRI).
literature published between January 2006 and September 2010 evaluating desvenlafaxine was reviewed.
Desvenlafaxine therapy is initiated at the therapeutic dose (50 mg/day) without a need for dose titration. Desvenlafaxine metabolism and distribution are not appreciably affected by altered function of cytochrome P450 (CYP) enzymes or permeability glycoprotein (P-gp). Desvenlafaxine has clinically insignificant effects on the activity of CYP and P-gp. The efficacy of desvenlafaxine in treating major depressive disorder has been established. Adverse events are characteristic of the SNRI class. Notably, the rate of discontinuation due to adverse events with the 50 mg/day recommended therapeutic dose is comparable to that seen with placebo.
incremental benefits with desvenlafaxine, derived from straight-forward dosing, a simple metabolic profile and lack of interaction with active transporter P-gp and CYP enzymes may contribute to more consistent response, good tolerability and lower incidence of drug-drug interactions with concomitant medications.
在涉及抗抑郁药物处置的常见机制中，遗传和药理学驱动的变化可能导致患者间反应的差异。这篇综述描述了去甲文拉法辛的药理学特性，去甲文拉法辛是第二代 5-羟色胺-去甲肾上腺素再摄取抑制剂（SNRI）。
本文综述了 2006 年 1 月至 2010 年 9 月发表的评估去甲文拉法辛的文献。
去甲文拉法辛治疗以治疗剂量（50 毫克/天）开始，无需剂量滴定。去甲文拉法辛的代谢和分布不受细胞色素 P450（CYP）酶或渗透性糖蛋白（P-gp）功能改变的明显影响。去甲文拉法辛对 CYP 和 P-gp 的活性没有明显的临床影响。去甲文拉法辛治疗重度抑郁症的疗效已得到确立。不良事件是 SNRI 类药物的特征。值得注意的是，由于不良事件导致的 50 毫克/天推荐治疗剂量的停药率与安慰剂相似。
去甲文拉法辛具有增量效益，源自简单的给药、简单的代谢谱以及与主动转运蛋白 P-gp 和 CYP 酶无相互作用，这可能有助于更一致的反应、更好的耐受性和与伴随药物相互作用的发生率降低。
