Rudolph R L, Derivan A T
Wyeth-Ayerst Research, Clinical Research and Development, Radnor, Pennsylvania, USA.
J Clin Psychopharmacol. 1996 Jun;16(3 Suppl 2):54S-59S; discussion 59S-61S. doi: 10.1097/00004714-199606002-00011.
The tolerability and safety of venlafaxine hydrochloride, a new serotonin and norepinephrine reuptake inhibitor, are reviewed in this article. The data presented here are based on a pool of 3,082 patients who were treated with this agent during clinical trials. Of these patients, 2,897 received venlafaxine for depression; 455 of these patients were treated for more than 360 days. The tolerability and safety profiles of venlafaxine were similar to those previously reported for selective serotonin reuptake inhibitors. Patients receiving venlafaxine experienced nausea, insomnia, dizziness, somnolence, constipation, and sweating more often than did patients receiving placebo but reported anticholinergic events less frequently than did patients receiving tricyclics. This is accounted for by the fact that, unlike the tricyclics, venlafaxine lacks significant affinity for muscarinic cholinergic receptors. Resolution of venlafaxine-associated nausea occurred rapidly in the vast majority of the patients who reported it at the start of therapy. Serious adverse events were rare among venlafaxine-treated patients. A small percentage of the patients given venlafaxine experienced modest but significant increases in blood-pressure readings, similar to those observed among imipramine-treated patients. At mean daily venlafaxine dosages of up to 300 mg, the percentage of venlafaxine-treated patients who had sustained elevations in supine diastolic blood pressure during treatment ranged from 2% to 6%, compared with 2% and 5% among the placebo- and imipramine-treated patients, respectively. All of the 14 patients who took an overdose of venlafaxine recovered without sequelae. Tolerability and safety in the elderly did not differ significantly from that observed in younger patients.
本文综述了新型5-羟色胺和去甲肾上腺素再摄取抑制剂盐酸文拉法辛的耐受性和安全性。此处呈现的数据基于3082例在临床试验中接受该药物治疗的患者。在这些患者中，2897例接受文拉法辛治疗抑郁症；其中455例患者治疗时间超过360天。文拉法辛的耐受性和安全性特征与先前报道的选择性5-羟色胺再摄取抑制剂相似。接受文拉法辛治疗的患者比接受安慰剂的患者更常出现恶心、失眠、头晕、嗜睡、便秘和出汗，但报告抗胆碱能事件的频率低于接受三环类药物的患者。这是因为与三环类药物不同，文拉法辛对毒蕈碱胆碱能受体缺乏显著亲和力。在治疗开始时报告有文拉法辛相关恶心的绝大多数患者中，这种恶心迅速缓解。在接受文拉法辛治疗的患者中，严重不良事件很少见。一小部分接受文拉法辛治疗的患者血压读数有适度但显著的升高，类似于在接受丙咪嗪治疗的患者中观察到的情况。在文拉法辛平均日剂量高达300mg时，接受文拉法辛治疗的患者在治疗期间仰卧位舒张压持续升高的百分比为2%至6%，而接受安慰剂和丙咪嗪治疗的患者分别为2%和5%。所有14例过量服用文拉法辛的患者均康复且无后遗症。老年人的耐受性和安全性与年轻患者相比无显著差异。
