Journal of Antimicrobial Chemotherapy (2001) 48, 351-354
© 2001 The British Society for Antimicrobial Chemotherapy
Antiretroviral drug concentrations in semen of HIV-infected men: differential penetration of indinavir, ritonavir and saquinavir
a PHLS Antiviral Susceptibility Reference Unit, Division of Immunity and Infection, University of Birmingham; b Department of Sexual Medicine, Birmingham Heartlands Hospital, Birmingham; c Department of Pharmacology & Therapeutics, University of Liverpool, UK
Variable drug penetration of antiretroviral drugs into the genital tract may contribute to the differential evolution of HIV and the emergence of drug resistance. This, in turn, may have an impact on the sexual transmission of resistant HIV in patients treated with antiretroviral drugs. We have measured concentrations of the HIV-1 protease inhibitors indinavir, ritonavir and saquinavir in the blood plasma (BP) and seminal plasma (SP) of 23 HIV-1-positive men. Forty-five time-matched blood and semen samples were obtained. SP concentrations of indinavir exceeded the EC95 of indinavir, corrected for protein binding, of 42 ng/mL at all time intervals. In contrast, the median ritonavir and saquinavir SP concentrations were below the relevant EC95 at all times post drug ingestion. The median SP:BP concentration ratios for indinavir were 0.6, 0.8 and 1.4, respectively, at 0–2, 2–6 and 6–8 h post-drug ingestion. In contrast, the median SP:BP concentration ratios at 0–3, 3–9 and 9–12 h post-drug ingestion were <0.02, <0.04 and <0.04, respectively, for both ritonavir and saquinavir. These differences justify further study of HIV-1 evolution and development of resistance in the genital tract of men taking these anti-HIV drugs.
* Correspondence address. PHLS Antiviral Susceptibility Reference Unit, Division of Immunity and Infection, The Medical School, University of Birmingham B15 2TT, UK. Fax: +44-1926-741115; E-mail: s.taylor.1{at}bham.ac.uk
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