The use of acetylcholinesterase (AChe) inhibitors seems to be a promising therapeutic strategy against cognitive impairment of Alzheimer's disease (AD). We evaluated the safety and the efficacy of two AChe inhibitor agents, donepezil and rivastigmine, in the treatment of mild to moderately severe AD. Twenty-seven patients were recruited for the study. They met DSM-IV criteria for uncomplicated AD and NINCDS-ADRDA criteria for probable or possibile AD of mild to moderate severity. Mini mental state examination (MMSE) scores of 10-21 at screening were required. Patients' age was between 53-77 years. Sixteen patients were treated with donepezil, 5 mg/day, and 11 subjects received rivastigmine, 6-9 mg/day for 30 weeks. The rating instruments used were the MMSE, the cognitive subscale of the AD assessment scale (ADAS-Cog), and the physical self-maintenance scale (PSMS). The assessment was carried out at baseline and at weeks 6, 12, 18, 24, and 30. The results demonstrated the positive effects of these agents on the cognitive and functional pictures in patients with mild to moderately severe AD. The adverse events related to treatment were generally not troublesome, and were of short duration (nausea, vomiting, dizziness, and diarrhoea).