Exelon (rivastigmine tartrate) is a cholinesterase inhibitor. The exact mechanism of rivastigmine's action is unknown, however it is thought to exert its therapeutic effect by enhancing cholinergic function. It inhibits the cholinesterase enzyme from breaking down acetylcholine, increasing both the level and duration of action of the neurotransmitter acetylcholine.
Exelon is specifically indicated for the treatment of mild to moderate dementia of the Alzheimer’s type and for the treatment of mild to moderate dementia associated with Parkinson’s disease.
Exelon patch is supplied as a 4.6 mg or 9.5 mg patch designed for transdermal administration. The recommended initial dose of the drug is 4.6 mg/24 hours. If treatment is well tolerated after a minimum of four weeks, this dose should be increased to 9.5 mg/24 hours, the recommended effective dose.
FDA approval of Exelon was based on the results of a single controlled trial in Alzheimer’s Disease as well as on three controlled trials of the immediate release capsule in Alzheimer’s Disease and one controlled trial in dementia associated with Parkinson’s Disease.
International 24-Week Study of Exelon Patch
This randomized, double-blind trial enrolled 1,195 subjects who were placed in one of the following cohorts: Exelon Patch 9.5 mg/24 hours; Exelon Patch 17.4 mg/24 hours; Exelon capsules 6 mg BID or placebo, for 24 weeks. The trial was divided into a 16-week titration phase followed by an 8-week maintenance phase. The primary endpoints included improvement from baseline in cognitive performance, assessed with the cognitive subscale of the Alzheimer’s Disease Assessment Scale (ADAS-Cog) as well as the ability of Exelon patch to produce an overall clinical effect, assessed using the Alzheimer’s Disease Cooperative Study - Clinical Global Impression of Change (ADCS-CGIC). At 24-weeks the differences in the mean ADAS-Cog change scores for the Exelon-treated subjects compared to the subjects on placebo, were 1.8, 2.9, and 1.8 units for the Exelon Patch 9.5 mg/24 hours, Exelon Patch 17.4 mg/24 hours, and Exelon capsule 6 mg BID groups, respectively. The mean differences in the ADCS-CGIC scores for the comparison of subjects in each of the Exelon-treated groups with the subjects on placebo, was 0.2 units. Both endpoints reached statistical significance compared to placebo.
Adverse events associated with the use of Exelon patch may include, but are not limited to, the following:
Exelon (rivastigmine tartrate) is a cholinesterase inhibitor. The exact mechanism of rivastigmine's action is unknown, however it is thought to exert its therapeutic effect by enhancing cholinergic function. This is accomplished by increasing the concentration of acetylcholine through reversible inhibition of its hydrolysis by cholinesterase. Thus, rivastigmine’s effect may lessen as the disease process advances and fewer cholinergic neurons remain functionally intact.
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Cummings JL, Koumaras B, Chen M, Mirski D; Rivastigmine Nursing Home Study Team Effects of rivastigmine treatment on the neuropsychiatric and behavioral disturbances of nursing home residents with moderate to severe probable Alzheimer's disease: a 26-week, multicenter, open-label study. The American Journal of Geriatric Pharmacotherapy 2005 Sep;3(3):137-48
Desai A, Grossberg G Review of rivastigmine and its clinical applications in Alzheimer's disease and related disorders. Expert Opinion on Pharmacotherapy 2001 Apr;2(4):653-66
For additional information regarding Exelon patch or Alzheimer's and Parkinson's disease related dementia, please visit the Exelon web page.