Clinically relevant enantiomer specific R- and S-praziquantel pharmacokinetic drug-drug interactions with efavirenz and ritonavir
| Autor: | Nyasha Nicole Kapungu, Comfort Ropafadzo Kanji, Charles Nhachi, Julia C. Stingl, Nadina Stadler, Roslyn Thelingwani, James Hakim, Chenai Sheilla Mutiti, Collen Masimirembwa |
|---|---|
| Jazyk: | angličtina |
| Rok vydání: | 2021 |
| Předmět: |
Drug
Adult Cyclopropanes Male Efavirenz Anti-HIV Agents media_common.quotation_subject RM1-950 Pharmacology 030226 pharmacology & pharmacy 03 medical and health sciences chemistry.chemical_compound Cmin Young Adult 0302 clinical medicine Pharmacokinetics drug‐drug interaction parasitic diseases medicine enantiomer specific Humans Drug Interactions General Pharmacology Toxicology and Pharmaceutics Adverse effect media_common Anthelmintics Cross-Over Studies Ritonavir business.industry praziquantel virus diseases Stereoisomerism Original Articles Crossover study Benzoxazines Praziquantel Neurology chemistry 030220 oncology & carcinogenesis Alkynes Original Article Therapeutics. Pharmacology business pharmacokinetics medicine.drug |
| Zdroj: | Pharmacology research & perspectives 9(3), e00769 (2021). doi:10.1002/prp2.769 Pharmacology Research & Perspectives, Vol 9, Iss 3, Pp n/a-n/a (2021) Pharmacology Research & Perspectives |
| Popis: | 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 The effect of efavirenz and ritonavir on the pharmacokinetics of praziquantel (PZQ) were investigated. An open label, single dose one sequence crossover clinical study with 26 healthy male volunteers was conducted. Efavirenz decreased the AUC of PZQ 4‐fold (p |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|