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The little we know about the pharmacokinetics and pharmacodynamics of praziquantel (racemate and R-enantiomer)

Olliaro, Piero ; Delgado-Romero, Petra ; Keiser, Jennifer

In: Journal of Antimicrobial Chemotherapy, 2014, vol. 69, no. 4, p. 863-870

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    Titre
    • The little we know about the pharmacokinetics and pharmacodynamics of praziquantel (racemate and R-enantiomer)
    Auteur
    • Olliaro, Piero. UNICEF/UNDP/World Bank/WHO Special Programme on Research & Training in Tropical Diseases (TDR), World Health Organization, 20 Avenue Appia, CH-1211, Geneva 27, Switzerland
    • Delgado-Romero, Petra. Department of Preclinical and Medical Affairs, PharmaLex GmbH, Mannheim, Germany
    • Keiser, Jennifer. Department of Medical Parasitology and Infection Biology, Swiss Tropical and Public Health Institute, Basel, Switzerland
    Type de document
    • Postprint
    Langue
    • Anglais
    Publié dans
    • Journal of Antimicrobial Chemotherapy, 2014, vol. 69, no. 4, p. 863-870. Oxford University Press
    Autre version électronique
    Identifiant OAI-PMH
    • oai:doc.rero.ch:299218
    Summary
    Praziquantel has been the mainstay of schistosomiasis control since 1984 and widely distributed since 2006 through ‘preventive chemotherapy' programmes to school-aged children or at-risk populations. In addition, preschool-aged children are now recognized as a vulnerable population and a group for targeted treatment, but they may be difficult to dose correctly with the available product—a racemate, based on the biologically active enantiomer (R-praziquantel) and the inactive distomer (S-praziquantel), which contributes the bitter taste and doubles the size of the tablets. Hence, a paediatric formulation is required, possibly enantiomerically pure. Developing such a product and extending its use to younger children should be pharmacologically guided, but limited data exist on pharmacokinetics and pharmacokinetic/pharmacodynamic correlations for praziquantel. This article presents available data on the chemistry, pharmacokinetics and pharmacodynamics of praziquantel, as well as R-praziquantel, and points to gaps in our knowledge