A review of rivastigmine: a reversible cholinesterase inhibitor

Rivastigmine tartrate is a reversible cholinesterase inhibitor indicated for the symptomatic treatment of mild to moderate dementia. It was approved by the US Food and Drug Administration for the treatment of Alzheimer's disease (AD) on April 21, 2000.

The purpose of this review was to summarize the background on dementia of the Alzheimer type and the pharmacokinetic properties, efficacy and tolerability profiles, clinical applications, adverse effects (AEs), drug interactions, and pharmacoeconomics of rivastigmine.

A literature search was conducted using MEDLINE (1995-2002), EMBASE Geriatrics and Gerontology (1995-2002), the National Institutes of Health Alzheimer's Disease Education and Resource Center Combined Health Information Database, and Google. Search terms included rivastigmine, Exelon, ENA 713, and ENA-713. The bibliographies of retrieved articles also were searched for relevant articles.

In clinical trials, rivastigmine has improved or maintained cognitive function, global function (ie, activities of daily living [ADLs]), and behavior in patients with mild to moderate AD for up to 52 weeks. AEs are generally mild to moderate and primarily affect the gastrointestinal (GI) tract. Clinically significant drug interactions with rivastigmine have thus far not been reported. Treatment with rivastigmine for up to 2 years may reduce the cost of caring for patients with AD. Cost savings are minimal during the first year, particularly for those with mild disease, but increase during the second year of treatment. Cost savings occur earlier for those with moderate AD. Most savings are realized from a delay in the need for institutionalization.

Rivastigmine has been shown to improve or maintain patients' performance in 3 major domains: cognitive function, global function (ADLs), and behavior. The efficacy and tolerability of rivastigmine have been proved by numerous clinical trials, with the most prominent AE being GI irritation.