Exelon (rivastigmine tartrate)
Company: Novartis Pharms
Approval Status: Approved July 2007
Treatment for: Alzheimer's and Parkinson's disease-related dementia
Areas: Neurology
Possible similar drugs: Exelon
| General Information | Clinical Results | Side Effects | Mechanism of Action | Literature References | Additional Information |
General Information
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.
Clinical Results
FDA Approval
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.
Side Effects
Adverse events associated with the use of Exelon patch may include, but are not limited to, the following:
- Nausea
- Vomiting
- Diarrhea
- Depression
- Headache
- Anxiety
- Anorexia
- Weight loss
Mechanism of Action
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.
Literature References
Wesnes K Rivastigmine tartrate with a focus on dementia associated with Parkinson's disease. Drugs of Today 2007 Jun;43(6):349-59
Lefèvre G, Sedek G, Jhee SS, Leibowitz MT, Huang HL, Enz A, Maton S, Ereshefsky L, Pommier F, Schmidli H, Appel-Dingemanse S Pharmacokinetics and Pharmacodynamics of the Novel Daily Rivastigmine Transdermal Patch Compared With Twice-daily Capsules in Alzheimer's Disease Patients. Clinical Pharmacology and Therapeutics 2007 May 23
Moretti R, Torre P, Vilotti C, Antonello RM, Pizzolato G Rivastigmine and Parkinson dementia complex. Expert Opinion on Pharmacotherapy 2007 Apr;8(6):817-29
Winblad B, Cummings J, Andreasen N, Grossberg G, Onofrj M, Sadowsky C, Zechner S, Nagel J, Lane R A six-month double-blind, randomized, placebo-controlled study of a transdermal patch in Alzheimer's disease--rivastigmine patch versus capsule. International Journal of Geriatric Psychiatry 2007 May;22(5):456-67
Dujardin K, Devos D, Duhem S, Destée A, Marié RM, Durif F, Lacomblez L, Touchon J, Pollak P, Péré JJ Utility of the Mattis dementia rating scale to assess the efficacy of rivastigmine in dementia associated with Parkinson's disease. Journal of Neurology 2006 Sep;253(9):1154-9
Wesnes KA, McKeith I, Edgar C, Emre M, Lane R Benefits of rivastigmine on attention in dementia associated with Parkinson disease. Neurology 2005 Nov 22;65(10):1654-6
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
Additional Information
For additional information regarding Exelon patch or Alzheimer's and Parkinson's disease related dementia, please visit the Exelon web page.
The FDA drug information shown here is licensed from Thomson CenterWatch. The information provided here is for general educational purposes only and does not constitute medical or pharmaceutical advice which should be sought from qualified medical and pharmaceutical advisers.
