Rivastigmine in the pharmacotherapy of Alzheimer's disease

Rivastigmine, an inhibitor of acetylcholine-esterase,. has been approved for the treatment of Alzheimer's disease (AD). Compared to tacrine, it possesses much better tolerability. It shows no hepatotoxicity and has been reported to inhibit specifically CNS acetylcholine-esterase. The duration of its blocking of acetylcholine-esterase is considerably longer than the detectability of the compound in plasma, properties that led to the term "pseudo-irreversible" to describe the mechanism of action. The efficacy in treating AD patients and the tolerability of rivastigmine has been demonstrated in the ws yet largest clinical trial programme which included a total of 3300 AD-patients. The results suggested that abilities increased and/or that the progression of the disease slowed. In addition, activities of daily living improved. Data of controlled studies are available for a period of six months. and from open extension trials from a period of one year. Tolerability of rivastigmine is good, the main side-effects being gastrointestinal disturbances like nausea or vomiting, presumably caused by enhanced cholinergic transmission. These side-effects can be minimized by slowly increasing the dosage up to the level that is still well tolerated.