ArticlePLoS neglected tropical diseases2016
Pharmacokinetic Study of Praziquantel Enantiomers and Its Main Metabolite R-trans-4-OH-PZQ in Plasma, Blood and Dried Blood Spots in Opisthorchis viverrini-Infected Patients.
Article in PLoS neglected tropical diseases, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.
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Who cites it
10 citing papers in PubMed, 22 citations in OpenAlex.
- In vitro and in vivo human metabolism and pharmacokinetics of S- and R-praziquantel.Pharmacology research & perspectives · 2020Trial
- Extrapolation of praziquantel pharmacokinetics to a pediatric population: a cautionary tale.Journal of pharmacokinetics and pharmacodynamics · 2018Trial
- N- and O‑Prenylated Quinolones: Syntheses andACS medicinal chemistry letters · 2026Article
- Analytical and Clinical Validation of Assays for Volumetric Absorptive Microsampling (VAMS) of Drugs in Different Blood Matrices: A Literature Review.Molecules (Basel, Switzerland) · 2023Review
- Effect of pharmacogenetic variations on praziquantel plasma concentration and safety outcomes among school children in Rwanda.Scientific reports · 2023Article
- Pharmacokinetics of Ascending Doses of Praziquantel in Adults Infected with Opisthorchis felineus in Western Siberia, Russian Federation.Antimicrobial agents and chemotherapy · 2022Article
- R-praziquantel integrated population pharmacokinetics in preschool- and school-aged African children infected with Schistosoma mansoni and S. haematobium and Lao adults infected with Opisthorchis viverrini.Journal of pharmacokinetics and pharmacodynamics · 2022Article
- Optimal single sampling time-point for monitoring of praziquantel exposure in children.Scientific reports · 2021Article
- Opisthorchis felineus genes differentially expressed under praziquantel shed light on the nature of tegument disruption and indicate the adaptive role of cGMP-dependent protein kinase.Parasitology research · 2020Article
- Slow-release praziquantel for dogs: presentation of a new formulation for echinococcosis control.Infectious diseases of poverty · 2017Article
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Authors and funding
8 authors at 3 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
backgroundPraziquantel (PZQ) is the treatment of choice for infections with the liver fluke Opisthorchis viverrini, a major health problem in Southeast Asia. However, pharmacokinetic (PK) studies investigating the disposition of PZQ enantiomers (R- and S-PZQ) and its main metabolite, R-trans-4-OH-PZQ, in diseased patients are lacking. The implementation of a dried blood spot (DBS) sampling technique would ease the performance of PK studies in remote areas without clinical facilities. The aim of the present study is to provide data on the disposition of PZQ enantiomers and R-trans-4-OH-PZQ in opisthorchiasis patients and to validate the use of DBS compared to plasma and blood sampling. METHODOLOGY/PRINCIPAL
findingsPZQ was administered to nine O. viverrini-infected patients at 3 oral doses of 25 mg/kg in 4 h intervals. Plasma, blood and DBS were simultaneously collected at selected time points from 0 to 24 h post-treatment. PK parameters were determined using non-compartmental analysis. Drug concentrations and areas under the curve (AUC0-24h) measured in the 3 matrices were compared using Bland-Altman analysis. We observed plasma AUC0-24hs of 1.1, 9.0 and 188.7 μg/ml*h and half-lives of 1.1, 3.3 and 6.4 h for R-PZQ, S-PZQ and R-trans-4-OH, respectively. Maximal plasma concentrations (Cmax) of 0.2, 0.9 and 13.9 μg/ml for R-PZQ, S-PQZ and R-trans-4-OH peaked at 7 h for PZQ enantiomers and at 8.7 h for the metabolite. Individual drug concentration measurements and patient AUC0-24hs displayed ratios of blood or DBS versus plasma between 79-94% for R- and S-PZQ, and between 108-122% for R-trans-4-OH. CONCLUSIONS/SIGNIFICANCE: Pharmacodynamic (PD) in vitro studies on PZQ enantiomers and R-trans-4-OH-PZQ are necessary to be able to correlate PK parameters with efficacy. DBS appears to be a valid alternative to conventional venous sampling for PK studies in PZQ-treated patients.
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