Brookie M Best1, Edmund V Capparelli. 1. University of California, San Diego, Skaggs School of Pharmacy and Pharmaceutical Sciences, San Diego, California, USA. brookie@ucsd.edu
Abstract
PURPOSE OF REVIEW: This review briefly outlines the influences of gender and pregnancy on drug disposition, and describes the available antiretroviral pharmacokinetic data and dosing recommendations in these groups. RECENT FINDINGS: Recent studies in pregnant women continue to document altered exposure of different classes of drugs during pregnancy. While new information shows that tenofovir exposure is significantly decreased during pregnancy, the magnitude of the decrease will not likely necessitate dose changes, similar to other nucleoside reverse transcriptase inhibitors. In contrast, standard doses of lopinavir/ritonavir in the third trimester showed markedly decreased exposure, and higher doses of this co-formulated agent should be given to women during the third trimester. Likewise, nelfinavir exposure using the new 625-mg tablets is also decreased during pregnancy, and higher doses should be considered in the third trimester. SUMMARY: The majority of antiretrovirals studied have altered pharmacokinetics during pregnancy. Understanding the extent of these changes is necessary to recommend dose changes during pregnancy when appropriate. The correct dose is critical to maintain efficacy and safety of these agents for both the mother and the fetus. Innovative study designs are needed to facilitate the study of antiretrovirals during pregnancy.
PURPOSE OF REVIEW: This review briefly outlines the influences of gender and pregnancy on drug disposition, and describes the available antiretroviral pharmacokinetic data and dosing recommendations in these groups. RECENT FINDINGS: Recent studies in pregnant women continue to document altered exposure of different classes of drugs during pregnancy. While new information shows that tenofovir exposure is significantly decreased during pregnancy, the magnitude of the decrease will not likely necessitate dose changes, similar to other nucleoside reverse transcriptase inhibitors. In contrast, standard doses of lopinavir/ritonavir in the third trimester showed markedly decreased exposure, and higher doses of this co-formulated agent should be given to women during the third trimester. Likewise, nelfinavir exposure using the new 625-mg tablets is also decreased during pregnancy, and higher doses should be considered in the third trimester. SUMMARY: The majority of antiretrovirals studied have altered pharmacokinetics during pregnancy. Understanding the extent of these changes is necessary to recommend dose changes during pregnancy when appropriate. The correct dose is critical to maintain efficacy and safety of these agents for both the mother and the fetus. Innovative study designs are needed to facilitate the study of antiretrovirals during pregnancy.
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