Efavirenz-Based Antiretroviral Therapy but Not Pregnancy Increased Unbound Piperaquine Exposure in Women during Malaria Chemoprevention.

ABSTRACT: Dihydroartemisinin-piperaquine (DP) is highly effective for malaria chemoprevention during pregnancy, but the standard dosing of DP that is used for nonpregnant adults may not be optimal for pregnant women. We previously reported that the pharmacokinetic exposure of total piperaquine (PQ; both bound and unbound to plasma proteins) is reduced significantly in the context of pregnancy or efavirenz (EFV)-based antiretroviral therapy (ART). However, as PQ is >99% protein-bound, reduced protein binding during pregnancy may lead to an increase in the pharmacologically active unbound drug fraction (f_u), relative to the total PQ. We investigated the impact of pregnancy and EFV use on the f_u of PQ to inform the interpretation of pharmacokinetics. Plasma samples from 0 to 24 h

SUBMITTER: Hong H 

PROVIDER: S-EPMC10112216 | biostudies-literature | 2023 Apr

REPOSITORIES: biostudies-literature