Pharmacokinetics of praziquantel in healthy volunteers and patients with schistosomiasis

Abstract

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 less than 0.05) plasma concentrations of Biltricide at 1.5, 2, 3 and 5 h after administration than with Distocide; plasma elimination half-lives (t 1/2) were not significantly different. In patients with hepatosplenic schistosomiasis, higher plasma levels of Distocide were noted (P less than 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; t 1/2 was greater (P less than 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 less than 0.01) in both food groups, although the values of t 1/2 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.

Combination Chemotherapy of Schistosomiasis in Laboratory Studies and Clinical Trials

“…Innovative financing models analogous to those put in place by the Medicine for Malaria Venture (MMV), in which academia, the private and public sectors, and the pharmaceutical industries are brought together, are appealing and might represent an VOL. 47,2003 MINIREVIEW 1493…”

A high-performance liquid chromatographic method for determination of praziquantel in rat plasma: Optimization and application to pharmacokinetic study

“…The previous HPLC methods described [6,[8][9][10][11][12][13][14][15] are all based principally on the method developed by Xio et al [16]. However, those methods are rather time-consuming as they involve three-step liquid-liquid extraction procedure.…”

“…A number of analytical methods have been reported for determination of praziquantel in human and animal biological fluids and tissue organ extracts. These methods involve radiometric assay [2], fluorometric assay [3], enzyme-linked immunosorbent assay [4], thin-layer chromatography (TLC), gas chromatography [5,7] and high-performance liquid chromatography (HPLC) [6,[8][9][10][11][12][13][14][15]. Most of the HPLC with UV detection methods described previously are based principally on the method developed by Xio et al [16].…”

Treatment of urinary schistosomiasis: methodological issues and research needs identified through a Cochrane systematic review

“…This calls for well designed trials incorporating also pharmacokinetic assessment, possibly with sparse sampling and population kinetic assessment. These trials should also control for food intake, as the bioavailability of PZQ depends upon taking it with food and the type of food matters (Mandour et al 1990 ;Castro et al 2000). The rationale behind the widely spaced dosing intervals of metrifonate treatment derives from its long-lasting effect on red blood cells and plasma cholinesterases (Plestina, Davis and Bailey, 1972).…”