Abstract
One likely mechanism of virological failure is poor antiretroviral drug diffusion in sites of viral replication such as the genital tract. We measured antiretroviral drug concentrations in blood and semen in 13 HIV-infected men failing treatment. Enfuvirtide did not cross the blood-testis barrier, whereas tenofovir accumulated in semen. Unlike indinavir, semen concentrations of lopinavir, amprenavir, saquinavir and efavirenz were ineffective. These are worrying findings, because suboptimal semen drug concentrations may enhance the risk of sexually transmitted drug-resistant HIV variants.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Adenine / analogs & derivatives*
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Adenine / pharmacokinetics
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Adult
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Alkynes
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Anti-HIV Agents / pharmacokinetics*
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Benzoxazines
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Blood-Testis Barrier
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Cyclopropanes
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Enfuvirtide
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Genitalia, Male / metabolism*
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HIV Envelope Protein gp41
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HIV Fusion Inhibitors / pharmacokinetics
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HIV Infections / drug therapy*
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HIV Protease Inhibitors / pharmacokinetics*
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HIV-1*
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Humans
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Male
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Middle Aged
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Organophosphonates / pharmacokinetics
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Oxazines / pharmacokinetics
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Peptide Fragments / pharmacokinetics
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Tenofovir
Substances
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Alkynes
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Anti-HIV Agents
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Benzoxazines
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Cyclopropanes
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HIV Envelope Protein gp41
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HIV Fusion Inhibitors
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HIV Protease Inhibitors
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Organophosphonates
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Oxazines
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Peptide Fragments
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Enfuvirtide
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Tenofovir
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Adenine
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efavirenz