Journal
PHARMACOLOGY RESEARCH & PERSPECTIVES
Volume 9, Issue 3, Pages -Publisher
JOHN WILEY & SONS LTD
DOI: 10.1002/prp2.769
Keywords
drug-drug interaction; enantiomer specific; pharmacokinetics; praziquantel
Categories
Funding
- Stanford Global Health Equity Scholars Programme [D43TW010540]
- German Federal Ministry of Health, Global Health Protection Programme
- The World Academy of Science [17-464 RG/BIO/AF/AC_ I/]
- European and Developing Countries Clinical Trials Partnership [TMA2016SF-1508]
- AiBST-Chitungwiza Trial Unit
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The study found that efavirenz significantly reduced the AUC of PZQ, while ritonavir only increased the AUC of S-PZQ. Therefore, further investigation is needed for the use of PZQ in HIV patients due to the risk of treatment failure and adverse effects.
We conducted a clinical study to determine the effect of efavirenz and ritonavir on the pharmacokinetics of R- and S-PZQ in healthy male participants. This was toward evaluating the risk of drug-drug interactions, which may occur after PZQ administration to HIV patients on efavirenz or ritonavir containing regimens. A non-randomized, open-label, single-dose, one sequence crossover study with 2 arms was conducted. We gave 26 healthy volunteers a single oral dose of 40 mg/kg PZQ followed by a daily oral dose of either 400 mg efavirenz or 100 mg ritonavir for 14 consecutive days. On day 14, they ingested a single 40 mg/kg dose of PZQ. We measured plasma levels up to 12 h on day 1 and day 14. Samples were analyzed by LC-MS. Pharmacokinetic analysis was conducted in WinNonlin to determine the primary endpoints (plasma T-1/2, C-min, and AUC). Efavirenz had a significant effect on the pharmacokinetics of PZQ (p < .05), reducing the AUC by 4-fold (1213.15 vs. 281.35 h.ng/ml for R-PZQ and 5669 vs. 871.84 h.ng/ml for S-PZQ). Ritonavir had no significant effect on R-PZQ but increased the AUC 2-fold for S-PZQ (p < .05) (4154.79 vs. 7291.05 h.ng/ml). Using PZQ in HIV patients needs investigation, as there is a risk of both treatment failure and adverse effects because of induction and inhibition, respectively.
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