Alzheimer Research Forum Overview of Exelon (rivastigmine)

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Name: Exelon™

Other Names: Rivastigmine tartrate

Therapy Types: pharmacological

Mechanisms: cholinesterase inhibitors

Development Status: approved in U.S.

FDA Phase: FDA approved

Primary Medical Role: Treatment of mild to moderate dementia of the Alzheimer's type.

Role in Alzheimer's Disease: It improves cognition, participation in activities of daily living, and global evaluation ratings in patients with mild to moderately severe Alzheimer's disease.

Pharmacological Role: A phenyl-carbamate derivative, a brain-selective acetylcholinesterase inhibitor, thought to selectively target hippocampus and cerebral cortex. Studies in lesioned rats indicate that ENA-713 ameliorates impairment of ChAT activity. Rivastigmine preferentially inhibits the G1 enzymatic form of AChE, which predominates in the brains of patients with Alzheimer's disease (AD).

Side Effects: At the high dose of 12 mg.day (note, in this study, 10% of the patients discontinued the study on the medication because of severe nausea and vomiting). Nausea (40% vs. 10% placebo); dizziness (40% vs. 30%); fatigue (25% vs. 0%); myalgia (20% vs. 0%); urinary incontinence(20% vs. 0%); sweating (10% vs. 0%); vision disorders (15% vs. 0%). Rivastigmine causes adverse events that are generally those expected from an acetylcholinesterase inhibitor. They are usually mild to moderate, of short duration and responsive to dosage reduction. One case of severe vomiting with esophageal rupture reported to have occurred after reinitiation of treatment at an inappropriate single dose of 4.5 mg following an interruption of treatment for eight weeks.

Evidence pro its efficacy: In two large multicenter clinical trials, rivastigmine 6- 12 mg/day was superior to placebo on three cognitive and functioning scales (p<0.001).

Dosage: Up to 12 mg/day. See notes below.

Companies: Novartis Pharmaceuticals Corporation

Notes: In a letter from Novartis Pharmaceuticals Corporation, posted on the FDA web site, the letter stated, '..to reduce the possibility of severe vomiting in patients who have interrupted Exelon therapy for longer than several days, treatment should be reinitiated with the lowest daily dose.' See Medline Plus Drug Information: - Rivastigmine [MedMaster] and Rivastigmine (Systemic) USP DI.

References

Kumar V, Anand R, Messina J, Hartman R, Veach J. An efficacy and safety analysis of Exelon in Alzheimer's disease patients with concurrent vascular risk factors. Eur J Neurol. 2000 Mar;7(2):159-69. Abstract

Grossberg GT, Stahelin HB, Messina JC, Anand R, Veach J. Lack of adverse pharmacodynamic drug interactions with rivastigmine and twenty-two classes of medications. Int J Geriatr Psychiatry. 2000 Mar;15(3):242-7. Abstract

Rivastigmine for Alzheimer's disease. Drug Ther Bull. 2000 Feb;38(2):15-6.

Birks J, Iakovidou V, Tsolaki M. Rivastigmine for Alzheimer's disease. Cochrane Database Syst Rev. 2000; (2):CD001191.

Jann MW. Rivastigmine, a new-generation cholinesterase inhibitor for the treatment of Alzheimer's disease. Pharmacotherapy. 2000 Jan;20(1):1-12. Abstract

Sim A. Rivastigmine: a review. Hosp Med. 1999 Oct;60 (10):731-5.

Rösler M, Anand R, Cicin-Sain A, Gauthier S, Agid Y, Dal- Bianco P, Stähelin HB, Hartman R, Gharabawi M. Efficacy and safety of rivastigmine in patients with Alzheimer's disease: international randomised controlled trial. BMJ. 1999 Mar 6;318(7184):633-8. Abstract

Spencer CM, Noble S. Rivastigmine. A review of its use in Alzheimer's disease. Drugs Aging. 1998 Nov ; 13(5):391-411. Abstract

Habucky K, Tse FL. Disposition of SDZ ENA 713, an acetylcholinesterase inhibitor, in the rabbit. Biopharm Drug Dispos. 1998 Jul ;19(5):285-90. Abstract

Farlow M, Anand R, Messina J, Hartman R, Veach J. A 52- week study of the efficacy of rivastigmine in patients with mild to moderately severe Alzheimer's disease Eur Neurol. 2000;44(4):236-41. Abstract

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