Rivastigmine. A review of its use in Alzheimer's disease

Drugs Aging. 1998 Nov;13(5):391-411. doi: 10.2165/00002512-199813050-00005.


Rivastigmine (SDZ ENA 713) is a carbamylating, long-acting reversible and noncompetitive carbamate acetylcholinesterase inhibitor that is indicated as an oral treatment for patients with mild to moderately severe Alzheimer's disease. The drug has been evaluated for this use in 3 well designed, adequately powered, phase II/III, 26-week clinical trials that included a total of 1479 rivastigmine and 647 placebo recipients. Most of these patients had concomitant disorders that were being treated with numerous other drugs. Individual and pooled results of these trials indicate that rivastigmine 6 to 12 mg/day usually produces cognitive, global and functional changes that indicate significantly less deterioration than was observed with placebo in patients with mild to moderately severe Alzheimer's disease. Individual results of the 2 pivotal trials and pooled analysis also show that, compared with placebo recipients, significantly more rivastigmine 6 to 12 mg/day recipients respond to therapy. Indeed, after 26 weeks of therapy in the 2 pivotal trials, significantly more rivastigmine 6 to 12 mg/day than placebo recipients achieved clinically meaningful improvements as defined by 3 separate response criteria. The lower dosage range of 1 to 4 mg/day was not as effective as 6 to 12 mg/day, as measured using these criteria and other efficacy parameters. 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. Unpublished data from 3989 patients indicate that rivastigmine and placebo were associated with similar incidences of serious adverse events and changes in laboratory parameters, ECG and cardiorespiratory vital signs. The most common events were gastrointestinal, central and peripheral nervous system and whole body adverse events. However, compared with placebo, rivastigmine more commonly caused adverse events resulting in treatment withdrawal. These events were most frequently gastrointestinal and were more common in women.

Conclusion: Rivastigmine is a useful option for the treatment of patients with mild to moderately severe Alzheimer's disease. Although only short term (6- month) comparisons with placebo are available, given the lack of established treatment options it should be considered for first-line use in this population.

Publication types

  • Review

MeSH terms

  • Alzheimer Disease / drug therapy*
  • Animals
  • Carbamates / adverse effects
  • Carbamates / pharmacology
  • Carbamates / therapeutic use*
  • Cholinesterase Inhibitors / therapeutic use*
  • Clinical Trials as Topic
  • Drug Interactions
  • Humans
  • Learning / drug effects
  • Neuroprotective Agents / therapeutic use*
  • Phenylcarbamates*
  • Rivastigmine
  • Sleep / drug effects
  • Substance-Related Disorders


  • Carbamates
  • Cholinesterase Inhibitors
  • Neuroprotective Agents
  • Phenylcarbamates
  • Rivastigmine