Drug metabolism and pharmacokinetics of praziquantel: A review of variable drug exposure during schistosomiasis treatment in human hosts and experimental models

Grace Zdesenko, Francisca Mutapi

Research output: Contribution to journalReview articlepeer-review


Background: Schistosomiasis control is heavily reliant on the drug praziquantel (PZQ),which is used as preventative chemotherapy as part of national helminth control strategies. Given the heavy reliance on PZQ for mass drug administration, there has been considerable research on the potential for parasites developing resistance to the drug resulting in decreased drug efficacy. However, there have been comparatively fewer studies of other factors that can potentially alter PZQ efficacy. Here we investigate whether host PZQ metabolism contributes towards variable cure rates. We evaluate factors that can influence the metabolism of PZQ and the resultant effect on the efficacy of PZQ treatment, to determine factors that potentially influence an individual’s response to praziquantel treatment.

Methodology/Principal Findings: The literature search was directed at published studies from three online databases: Web of Science, PubMed, and EMBASE. The search terms for the review comprised of [(praziquantel OR PZQ) AND (schistosom* OR bilharzia) AND (pharmaco*)] and included studies evaluating praziquantel metabolism. Publications were categorised into pharmacokinetics, drug-drug interactions, pharmacogenetics, and metabolite analysis. Forty publications describing human and experimental studies fitted the inclusion criteria and were subjected to data extraction and analysis. The analyses showed that variable exposure to PZQwas associated with alterations in the liver’s capacity to metabolise PZQ and observed drug-drug interactions. Other factors influencing the efficacy of PZQ were brand, formulation, and co administered food. Although some work has been performed on metabolite identification, there was minimal information on PZQ’s metabolic pathway, and no pharmacogenetics studies were identified.

Conclusions/Significance: The study indicated that in both human and experimental studies alterations in the liver’s capacity to metabolise PZQ, as well as drug-drug interactions, affected systemic levels of PZQ that could result in variable cure rates. The study confirmed previous findings of higher antischistosomal activity of (R)-PZQ enantiomer when administered alone compared to the racemate at the same dose, as well as improved efficacy when the drug is administered with food. The study also highlighted the need for more comprehensive studies of the PZQ metabolic pathway and PZQ pharmacogenetic studies in humans.
Original languageEnglish
JournalPLoS Neglected Tropical Diseases
Publication statusPublished - 25 Sep 2020


  • praziquantel
  • PZQ
  • schistosomiasis
  • bilharzia
  • drug metabolism
  • pharmacokinetics
  • pharmacogenetics
  • drug-drug interactions
  • metabolite


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