Tolerability of rivastigmine transdermal patch in patients with Alzheimer’s disease: a narrative review

The rivastigmine transdermal patch was developed to provide similar efficacy to oral rivastigmine in the treatment of Alzheimer’s disease (AD), but with improved tolerability. Randomized clinical trials and observational studies reporting on the tolerability of the rivastigmine transdermal patch in patients with AD, identified through a systematic literature search. Rivastigmine was the first cholinesterase inhibitor for which a transdermal formulation was developed; consequently, there is a substantial body of evidence on its efficacy and tolerability. The incidence of gastrointestinal AEs is markedly reduced with the transdermal patch compared with oral rivastigmine, while the efficacy of the patch remains similar to that of the oral formulation. Application site reactions are generally mild and do not cause much discomfort for the patient, and the risk of can be reduced by simple measures such as site rotation and good skin care. Tolerability of the patch improves over time, including at the highest dose level. Overall, the available evidence supports transdermal rivastigmine being generally well tolerated at doses up to 13.3 mg/24 h in patients with AD.

利斯的明（rivastigmine）透皮贴剂旨在实现与口服利斯的明治疗阿尔茨海默病（Alzheimer’s disease，AD）相当的疗效，同时提升患者耐受性。本研究通过系统文献检索，筛选出多篇报道AD患者使用利斯的明透皮贴剂耐受性的随机临床试验与观察性研究。利斯的明是首款研发出透皮制剂的胆碱酯酶抑制剂（cholinesterase inhibitor），因此目前已有大量关于其疗效与耐受性的研究证据。与口服利斯的明相比，透皮贴剂可显著降低胃肠道不良反应（adverse events，AEs）的发生率，同时其疗效与口服制剂保持一致。用药部位反应通常较为轻微，不会给患者带来明显不适；通过轮换给药部位、做好皮肤护理等简单措施，即可降低此类反应的发生风险。随着用药时间延长，透皮贴剂的耐受性会逐步改善，即使在最高剂量水平下亦不例外。总体而言，现有证据支持，阿尔茨海默病患者使用剂量最高达13.3 mg/24 h的利斯的明透皮贴剂整体耐受性良好。