Alteration of Early-Phase Piperaquine Disposition by Concurrent Administration of Clarithromycin in Healthy Volunteers
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Date
2024
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Advances in Pharmacology and Clinical Trials
Abstract
Malaria and Helicobacter pylori infections are some of the most prevalent infectious diseases causing thousands of deaths
worldwide. Concurrent infections can exacerbate co-morbidities or make worse the management of malaria. Drug-drug
interactions arising from activities of CYP450 during concurrent management of the co-infections could worsen management
challenges and therapeutic outcomes. Fifteen healthy volunteers were administered single oral dose of P-Alaxin© consisting
piperaquine (960 mg) and dihydroartemisinin (240 mg). Following a five-month wash out period, clarithromycin (500 mg)
was administered twice daily for five days. A single dose of P-Alaxin© was administered on the 3rd day. Blood samples were
collected within 48 hours and analyzed for plasma levels of the administered drugs using RP-HPLC methods. The Tmax was
5.2±2.11 h vs 5.47±2.56 h and did not vary significantly p>0.05. However, Cmax and AUC0-48, of piperaquine when concurrently
administered with clarithromycin increased significantly (179.41±56.35 ng/ml vs 478.99 ± 148.86 ng/ml; 37,644.56 ±
16.716.95 vs 104,098.47 ± 53.311.57 ng/ml*h respectively (p<0.05).quine during concurrent administration could be a
pointer to major drug interactions that may manifest during full course of management of the concurrent infections.
pharmacokinetic parameters in the early phase metabolism of piperaquine during concurrent administration cou