[Comparative analysis of the influence of food and cimetidine in plasma levels of praziquantel]. / Análisis comparativo de la influencia de los alimentos y la cimetidina en los niveles plasmáticos de prazicuantel.

ABSTRACT

Praziquantel (PZQ) is an effective drug for treatment of neurocysticercosis. The drug shows an extensive first-pass effect and therefore plasma levels are low. In order to increase plasma and CSF levels of PZQ other alternatives have been investigated such as the use of PZQ jointly with cimetidine or food. With the pharmacokinetic parameters obtained in these studies, in the present work computer simulations were made in order to predict plasma concentrations of PZQ-administration with cimetidine or with meals under the two treatments currently used ultrashort scheme (three dose of 25 mg/kg given at 2-hours intervals) and the traditional scheme (50 mg/kg/day divided in three dose given at 8-hours intervals for 15 days). The results of our simulations showed that the combination of PZQ with a high carbohydrate diet could be an adequate alternative for clinical therapy. Furthermore a clinical study was performed in 18 patients with neurocysticercosis, which received the ultrashort scheme in fasting state, with cimetidine or with a high carbohydrate diet. The efficacy of the treatment was evaluated by the percentage of disappearance of the lesions and plasma levels obtained in each group. The results showed that a high carbohydrate diet increases plasma levels of PZQ. The results of the clinical study, together with our simulations indicate that the treatment of PZQ with a high carbohydrate diet was an adequate clinical alternative and showed improvement of the effectiveness of PZQ therapy.