PHARMACOKINETICS OF PRAZIQUANTEL IN HEALTHY-VOLUNTEERS AND PATIENTS WITH SCHISTOSOMIASIS

The pharmacokinetics of a novel praziquantel preparation (Distocide®) were investigated in Sudanese patients with hepatosplenic schistosomiasis and in healthy volunteers, and compared with those of Biltricide®.The results of the first study indicated greater (P <0·05) plasma concentrations of Biltricide® at 1·5, 2, 3 and 5 h after administration than with Distocide®; plasma elimination half-lives (t1/2) were not significantly different. In patients with hepatosplenic schistosomiasis, higher plasma levels of Distocide® were noted (P < 0·05 at 8 h) compared to healthy controls; however, due to wide inter-individual variations, there were no significant differences in maximum plasma concentration, time to maximum plasma concentration, area under the plasma concentration curve (AUC), volume of distribution, or clearance; t1/2 was greater (P < 0·05) in patients (11·9 ± 5·4 h) than controls (2·3 ± 0·4 h). In the presence of food, higher plasma concentrations of Distocide® occurred compared to the fasting state; AUCs were greater (P < 0·01) in both food groups, although the values of t1/2 were shorter. The lower plasma levels and longer duration of action of Distocide® may be advantageous in reducing side effects and prolonging exposure of the schistosomes to the drug. © 1990, Royal Society of Tropical Medicine and Hygiene. All rights reserved.