Morton W A, Sonne S C, Verga M A
Department of Hospital Pharmacy Practice and Administration, University of South Carolina Institute of Psychiatry, Charleston, USA.
Ann Pharmacother. 1995 Apr;29(4):387-95. doi: 10.1177/106002809502900410.
To introduce the new antidepressant venlafaxine. Basic pharmacokinetic data and clinical trials are reviewed, as well as adverse reactions, drug interactions, dosing guidelines, and therapeutic considerations. The article also discusses several pharmacotherapy issues and how venlafaxine compares with other available antidepressants.
A MEDLINE search was used to identify pertinent literature, including reviews.
As this is a relatively new agent, all available clinical trials were reviewed.
All clinical trials that were available prior to submission for publication were reviewed. Preliminary trials and unpublished reports were not reviewed.
Venlafaxine hydrochloride is a structurally novel agent that has recently been approved in the US for the treatment of depression. This unique antidepressant blocks neuronal reuptake of norepinephrine, serotonin, and, to a lesser extent, dopamine. Venlafaxine and its major active metabolite, O-desmethylvenlafaxine, exhibit linear kinetics with an elimination half-life of 5 and 11 hours, respectively. Venlafaxine has been evaluated in 7 clinical trials for the treatment of depression. These have consisted of 2 open trials, 3 double-blind, placebo-controlled trials, and 2 double-blind trials where venlafaxine was compared with trazodone and imipramine. All 7 trials have established efficacy for venlafaxine using standard psychiatric rating scales to measure change of depressive symptoms. The usual daily dosage ranges from 75 to 225 mg/d in 2 to 3 divided doses, with a maximum daily dosage of 375 mg/d. The drug's adverse effect profile differs somewhat from other more specific serotonin reuptake inhibitors in that it appears to cause dry mouth, somnolence, and elevated blood pressure as well as nausea, headache, and dizziness.
Although venlafaxine has recently become available for use as an antidepressant in the US, few clinical trials have been conducted to help the practitioner evaluate its place in the treatment of depression. There are no comparative trials of venlafaxine with the serotonin specific reuptake inhibitor antidepressants, which are rapidly becoming the newest comparative standard. The clinical place for venlafaxine in the treatment of depression has yet to be determined.
介绍新型抗抑郁药文拉法辛。回顾其基本药代动力学数据、临床试验，以及不良反应、药物相互作用、给药指南和治疗注意事项。本文还讨论了几个药物治疗问题以及文拉法辛与其他现有抗抑郁药的比较情况。
使用MEDLINE检索来识别相关文献，包括综述。
由于这是一种相对较新的药物，对所有可用的临床试验进行了回顾。
对提交发表之前所有可用的临床试验进行了回顾。未回顾初步试验和未发表的报告。
盐酸文拉法辛是一种结构新颖的药物，最近在美国被批准用于治疗抑郁症。这种独特的抗抑郁药可阻断去甲肾上腺素、5-羟色胺，以及程度较轻的多巴胺的神经元再摄取。文拉法辛及其主要活性代谢物O-去甲基文拉法辛呈现线性动力学，消除半衰期分别为5小时和11小时。文拉法辛已在7项治疗抑郁症的临床试验中进行了评估。这些试验包括2项开放试验、3项双盲、安慰剂对照试验，以及2项将文拉法辛与曲唑酮和丙咪嗪进行比较的双盲试验。所有7项试验均使用标准精神科评定量表来测量抑郁症状的变化，从而确定了文拉法辛的疗效。通常每日剂量为75至225mg/d，分2至3次服用，最大日剂量为375mg/d。该药物的不良反应谱与其他更具特异性的5-羟色胺再摄取抑制剂有所不同，因为它似乎会导致口干、嗜睡、血压升高以及恶心、头痛和头晕。
尽管文拉法辛最近在美国已可作为抗抑郁药使用，但进行的临床试验很少，无法帮助从业者评估其在抑郁症治疗中的地位。目前尚无文拉法辛与5-羟色胺特异性再摄取抑制剂抗抑郁药的对比试验，而后者正迅速成为最新的对比标准。文拉法辛在抑郁症治疗中的临床地位尚未确定。
