Alteration of Early-Phase Piperaquine Disposition by Concurrent Administration of Clarithromycin in Healthy Volunteers

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DOI: 10.23880/apct-16000250

Volume 9, Issue 4

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

Keywords: Metabolism; Drug Interactions; Clarithromycin; Piperaquine

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