SAFETY AND PHARMACOKINETICS OF A SINGLE ORAL DOSE OF AMISULPRIDE IN HEALTHY ELDERLY VOLUNTEERS

Objective: Amisulpride is a substituted benzamide neuroleptic, which b inds selectively to dopamine D-2 and D-3 receptors, mainly in the limb ic structures. States of delusion and agitation occur frequently in th e population aged more than 65 years, especially in demented patients and this sometimes requires the use of neuroleptics. The objectives of this study were to determine the safety and the pharmacokinetic profi le of 50 mg of amisulpride administered orally as a single dose to eld erly volunteers. Methods: Twenty healthy volunteers (10 men and 10 wom en) aged 65-79 years were included in this open trial. Frequent measur ements of blood pressure and heart rate were made and ECG and blood sa mples were performed up to 72 h after drug intake. Results: The overal l clinical and cardiovascular safety was satisfactory. The mean C-max of the racemate amisulpride in elderly people was 64.1 +/- 6.7 ng.ml(- 1), and was not different from the value of 56 +/- 4.1 ng.ml(-1) in yo ung subjects. As with the C-max, the mean values of t(1/2) and AUC in elderly people (15.6 +/- 1.3 h and 667 +/- 51 ng.ml(-1).h, respectivel y) were not different to values observed in young subject (respectivel y 11.7 +/- 0.5 h and 603 +/- 25 ng.ml(-1). h). Conclusions: A single o ral dose of amisulpride was well tolerated and showed a similar pharma cokinetic profile in healthy elderly and young subjects. However, thes e findings should be confirmed after multiple dosing in a larger popul ation in order to establish the lack of need of dosage adjustment in t his elderly population.