Lopez-Pousa_1999_Neurologia_14_180

AIM The cognitive deficiency of Alzheimer's disease is attributed to a dysfunction in the cerebral cholinergic systems. Current drug treatments are directed at stimulating cholinergic transmission. The aim of this study was to evaluate the latest cholinergic drugs available an those about to appear in the market. METHODS: A review of the most recent studies published regarding the physiopathology of Alzheimer disease and the results following treatment with donepezil, rivastigmine and metriphonate was carried out. RESULTS: Donepezil is a specific, reversible acetylcholinesterase inhibitor of close to 100% absorption and a half-life of 70 h, achieving stable concentrations at approximately 3 weeks. Patients treated with a single daily dosis of 5 or 10 mg improve in the ADAS-Cog scale. The medication is initiated with a dosis of 5 mg/day. Rivastigmine is a competitive, pseudoirreversible inhibitor with a half-life of 2 h, although it acts for approximately 10 h. The Adas-Cog scale and the CIBIC-Plus improve in patients treated with a daily dosis of 6 or 12 mg taken in two doses. Administration should be initiated at low doses (3 mg/day) which are progressively increased. Metriphonate is a prodrug of short life which inhibits acetylcholinesterase through a metabolite (DDVP) with a half-life in the circulation of 2 h. Improvement is observed in the ADAS-Cog scale and the CIBIC-Plus and in behavior disorders at doses of 0.3 and 0.65 mg/kg/day. Doses between 30 and 60 mg/day are effective.
CONCLUSIONS: Different studies carried out with the acetylcholinesterase inhibitors donepezil, rivastigmine and metriphonate have been effective in the control of the cognitive symptoms of Alzheimer disease in the initial or moderate phases of the disease.