Department of Neurology, Nova Southeastern University, FL, USA.
CNS Neurosci Ther. 2010 Spring;16(1):51-60. doi: 10.1111/j.1755-5949.2009.00119.x.
Oral cholinesterase inhibitors (ChEIs) are associated with side effects such as nausea and vomiting. The use of transdermal patches for ChEI delivery may help to minimize these problems. The objective of this review was to consider available data from patients switching from oral ChEIs to transdermal rivastigmine treatment, and to suggest practical guidelines for patients wishing to do this. Literature database and reference list searches were performed to identify suitable publications. Data from two clinical trials and a series of open observational studies, in which patients were switched to the rivastigmine patch from oral rivastigmine, donepezil tablets, or galantamine, were evaluated. Adverse events were tabulated. In the studies reported here, nausea was reported in up to 3.2% and vomiting in up to 1.9% of patients switching to the rivastigmine patch from oral rivastigmine. Similar rates (up to 3.8% of patients for nausea and 0.8% of patients for vomiting) were reported when switching to the rivastigmine patch from donepezil tablets, and no nausea or vomiting was reported in a case study of patients switching to the rivastigmine patch from galantamine tablets. Switching regimes used in clinical trials appeared well tolerated. Data support recommendations for patients on high rivastigmine capsule doses to switch directly to the 9.5 mg/24 h rivastigmine patch, while those on lower oral rivastigmine doses should start on the 4.6 mg/24 h patch for 4 weeks before increasing to the 9.5 mg/24 h patch. This latter regimen is recommended for patients on other oral cholinesterase inhibitors if switching is medically indicated or requested by the patient or the caregiver.
口服胆碱酯酶抑制剂(ChEIs)会引起恶心和呕吐等副作用。使用透皮贴剂递送 ChEI 可能有助于最大限度地减少这些问题。本综述的目的是考虑从口服 ChEI 转换为透皮 Rivastigmine 治疗的患者的现有数据,并为希望进行这种转换的患者提出实用指南。进行了文献数据库和参考文献列表检索,以确定合适的出版物。评估了两项临床试验和一系列开放观察性研究的数据,其中患者从口服 Rivastigmine、donepezil 片剂或加兰他敏转换为 Rivastigmine 贴剂。列出了不良事件。在报告的这些研究中,从口服 Rivastigmine 转换为 Rivastigmine 贴剂的患者中,有高达 3.2%的患者报告恶心,高达 1.9%的患者报告呕吐。从 donepezil 片剂转换为 Rivastigmine 贴剂时,报告的恶心发生率相似(高达 3.8%的患者恶心,0.8%的患者呕吐),而从 galantamine 片剂转换为 Rivastigmine 贴剂的病例研究中则没有报告恶心或呕吐。临床试验中使用的转换方案似乎耐受性良好。数据支持建议高 Rivastigmine 胶囊剂量的患者直接转换为 9.5mg/24h Rivastigmine 贴剂,而低剂量口服 Rivastigmine 的患者应先开始使用 4.6mg/24h 贴剂 4 周,然后再增加到 9.5mg/24h 贴剂。如果转换是医学上需要的,或者患者或护理人员要求转换,建议其他口服胆碱酯酶抑制剂的患者使用这种方案。