Limited penetration of lopinavir and ritonavir in the genital tract of men infected with HIV-1 in Brazil

Therapeutic Drug Monitoring
Tania R C VergaraPaulo F Barroso

Abstract

The concentrations of lopinavir and ritonavir in seminal and blood plasma and the seminal human immunodeficiency virus (HIV) viral load were quantified by HPLC and the Nuclisens assay, respectively, in a cross-sectional study of 16 HIV-1-infected Brazilian men under stable treatment with a lopinavir/ritonavir containing antiretroviral regimen. Semen and blood samples were collected on 2 occasions: at 6 to 60 minutes before ("trough"), and 5 to 6 hours after ("peak") ingestion of regular doses of lopinavir/ritonavir. Median seminal lopinavir levels were 120.6 ng/mL (range, <20-1481.8 ng/mL) and 233.1 ng/mL (range, 48.4-1133.4 ng/mL) at trough and peak points, respectively. The corresponding values for ritonavir were 9.2 ng/mL (range, <5-47 ng/mL) and 17.1 ng/mL (range, 6.6-66.7 ng/mL). The median concentrations of lopinavir and ritonavir in semen were, respectively, 1.9% to 3% and 3.7% to 4.4% of those measured in blood plasma samples collected within 30 minutes. HIV-1 viral load was detectable in the semen of 2 and in the blood of 6 of 16 patients. These results may have implications for drug-resistant HIV-1 evolution and transmission.

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Citations

Oct 11, 2008·AIDS Research and Human Retroviruses·Joanne SteklerRobert W Coombs
Feb 12, 2013·Bioanalysis·Robin DiFrancescoGene D Morse
Jan 28, 2012·Enfermedades infecciosas y microbiología clínica·Elena López AspirozMaría José García Sánchez
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Sep 21, 2011·Journal of Acquired Immune Deficiency Syndromes : JAIDS·Juan Manuel TiraboschiDaniel Podzamczer

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