Frampton_2014_Drugs.Aging_31_639

Rivastigmine is unique among cholinesterase inhibitors commonly used in the treatment of mild to moderate Alzheimer's disease (AD) in that it is available as a transdermal patch formulation (Exelon((R)) patch, Rivastach((R)) patch, Prometax((R)) patch). The patch is applied once daily and, in the EU (and US), is available in three sizes: 5, 10 and 15 cm(2) (releasing 4.6, 9.5 and 13.3 mg rivastigmine/24 h, respectively). In the phase III OPTIMA trial, patients with mild to moderate AD who experienced functional and cognitive decline on the 10 cm(2) patch-the recommended maintenance dose-gained additional benefit when their dose was increased to the 15 cm(2) patch. For example, 15 cm(2) patch recipients showed significantly less functional and cognitive decline than 10 cm(2) patch recipients after 24 weeks of double-blind treatment. Patients receiving the 15 cm(2) patch also showed significantly less functional, but not cognitive, decline than those receiving the 10 cm(2) patch after 48 weeks of double-blind treatment; as such, OPTIMA only met one of its two co-primary endpoints. The 15 cm(2) patch was generally well tolerated; although more 15 cm(2) than 10 cm(2) patch recipients reported adverse events (e.g. nausea and vomiting), fewer 15 cm(2) than 10 cm(2) patch recipients discontinued treatment due to adverse events. By further slowing functional deterioration without markedly compromising tolerability, increasing the transdermal rivastigmine dose to the 15 cm(2) patch has a favourable benefit-risk profile-and therefore represents a valid option-in the treatment of patients with mild to moderate AD who have previously experienced functional and cognitive decline while receiving the 10 cm(2) patch.