Karolinska University Hospital, Karolinska Institute, Department of Neurobiology, Care Sciences and Society, Division of Alzheimer Neurobiology, Novum, 4th Floor, Room 4F23:10, 141 86, Huddinge, Stockholm, Sweden.
Expert Opin Drug Saf. 2010 Jan;9(1):167-76. doi: 10.1517/14740330903439717.
Cholinesterase inhibitors are the mainstay of symptomatic therapy for Alzheimer's disease (AD). Rivastigmine, an inhibitor of both acetylcholinesterase and butyrylcholinesterase, is available as a transdermal patch and in oral forms. It is also approved for the treatment of Parkinson's disease dementia (PDD) in many countries. The objective of this article is to review the safety and tolerability profile of transdermal and oral rivastigmine in AD and PDD patients.
Articles were identified by searching MEDLINE in July 2009 using the terms rivastigmine, Exelon, ENA 713 and clinical trial. All double-blind, placebo-controlled randomized trials in which rivastigmine monotherapy was administered to AD or PDD patients for longer than 2 weeks were included.
This article provides a comprehensive summary of currently available safety data on rivastigmine.
The main adverse events reported with rivastigmine therapy are gastrointestinal in nature. However, the transdermal patch appears to reduce these side effects, allowing more patients to access higher therapeutic doses. Overall, the safety profile of rivastigmine is favorable and the improved tolerability offered by the rivastigmine patch suggests that transdermal delivery may be the best way to deliver this drug in AD and PDD patients.
胆碱酯酶抑制剂是阿尔茨海默病（AD）症状治疗的主要药物。 他克林是乙酰胆碱酯酶和丁酰胆碱酯酶的抑制剂，有透皮贴剂和口服制剂。它也被许多国家批准用于治疗帕金森病痴呆（PDD）。本文的目的是回顾 AD 和 PDD 患者中使用透皮和口服 Rivastigmine 的安全性和耐受性概况。
通过在 2009 年 7 月使用 Rivastigmine、Exelon、ENA 713 和临床试验等术语搜索 MEDLINE 来确定文章。所有 Rivastigmine 单药治疗 AD 或 PDD 患者超过 2 周的双盲、安慰剂对照随机试验都被包括在内。
本文提供了 Rivastigmine 现有安全性数据的综合总结。
与 Rivastigmine 治疗相关的主要不良事件是胃肠道性质的。然而，透皮贴剂似乎减少了这些副作用，使更多的患者能够使用更高的治疗剂量。总体而言， Rivastigmine 的安全性良好， Rivastigmine 贴剂提供的更好的耐受性表明，在 AD 和 PDD 患者中，透皮给药可能是递送这种药物的最佳方式。
