Guay David R P
Department of Experimental and Clinical Pharmacology, University of Minnesota, Minneapolis, MN, USA.
Consult Pharm. 2012 Dec;27(12):857-67. doi: 10.4140/TCP.n.2012.857.
Vilazodone (VIIBRYD, Trovis Pharmaceuticals; New Haven, Connecticut, also known as 659746, EMD68843, SB-659746-A) is a newly introduced antidepressant that has taken approximately a decade from its discovery to approval by the Food and Drug Administration. This paper will review the chemistry, pharmacodynamics, pharmacokinetics, clinical efficacy, tolerability, drug-drug interaction potential, dosing, and administration of this agent.
Medline/PubMed/IPA/EMBASE databases were searched using the terms "vilazodone," "659746," "EMD68843," and "SB-659746-A." All English-language papers from 1985 to April 2012 were reviewed for relevance. Bibliographies of all papers were reviewed to identify further papers.
All English-language papers from 1985 to present appearing in these searches were reviewed for relevance to this paper. In addition, their bibliographies were reviewed to identify any papers not identified in the searches. Data are expressed as mean or mean ± standard deviation, unless otherwise noted.
Vilazodone is the first combined selective serotonin reuptake inhibitor (SSRI)/5-HT1A receptor agonist antidepressant. Vilazodone must be administered with food to optimize bioavailability. The primary route of elimination is metabolism followed by excretion of metabolites. Advancing age and renal and hepatic impairment do not alter its disposition. Early phase II clinical trials were unable to demonstrate antidepressant efficacy. However, later phase III trials using 40 mg daily doses were able to demonstrate superior efficacy compared with placebo treatment. Adverse events, warnings, and precautions mirror those of other SSRIs.
Although there are theoretical reasons why 5-HT1A agonism may be a desirable additional property in antidepressants, there is no evidence to date that vilazodone has any advantage over existing post-tricyclic antidepressants. It has a narrow therapeutic dosing range whose upper boundary is close to that producing intolerable gastrointestinal and central nervous system adverse events. Further research will clarify and refine the role of vilazodone in the management of psychiatric disorders.
维拉唑酮（商品名：VIIBRYD，Trovis制药公司；位于康涅狄格州纽黑文，也称为659746、EMD68843、SB - 659746 - A）是一种新推出的抗抑郁药，从发现到获得美国食品药品监督管理局批准大约花费了十年时间。本文将综述该药的化学性质、药效学、药代动力学、临床疗效、耐受性、药物相互作用潜力、给药剂量及用法。
使用“维拉唑酮”“659746”“EMD68843”和“SB - 659746 - A”等检索词对Medline/PubMed/IPA/EMBASE数据库进行检索。对1985年至2012年4月期间所有英文文献进行相关性审查。对所有文献的参考文献进行审查以识别更多相关文献。
对1985年至今在这些检索中出现的所有英文文献进行相关性审查，以确定与本文的相关性。此外，对其参考文献进行审查以识别检索中未找到的文献。除非另有说明，数据以均值或均值±标准差表示。
维拉唑酮是首个兼具选择性5 - 羟色胺再摄取抑制剂（SSRI）/5 - HT1A受体激动剂特性的抗抑郁药。维拉唑酮必须与食物同服以优化生物利用度。主要消除途径是代谢，随后是代谢产物的排泄。年龄增长以及肾、肝功能损害不会改变其处置方式。早期II期临床试验未能证明其抗抑郁疗效。然而，后期使用每日40毫克剂量的III期试验显示与安慰剂治疗相比具有更优疗效。不良事件、警告及注意事项与其他SSRI类药物类似。
尽管从理论上讲，5 - HT1A激动作用可能是抗抑郁药中一项理想的附加特性，但迄今为止尚无证据表明维拉唑酮比现有的三环类后抗抑郁药具有任何优势。它的治疗剂量范围狭窄，其上界接近产生难以耐受的胃肠道和中枢神经系统不良事件的剂量。进一步的研究将阐明并完善维拉唑酮在精神疾病治疗中的作用。
