Antiretroviral drug concentrations in semen of HIV-infected men: differential penetration of indinavir, ritonavir and saquinavir
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 meas...
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| Veröffentlicht in: | Journal of antimicrobial chemotherapy 2001-09, Vol.48 (3), p.351-354 |
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| container_title | Journal of antimicrobial chemotherapy |
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| creator | Taylor, Stephen Back, David J. Drake, Susan M. Workman, Judith Reynolds, Helen Gibbons, Sara E. White, David J. Pillay, Deenan |
| description | 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 |
| doi_str_mv | 10.1093/jac/48.3.351 |
| format | Article |
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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.</description><identifier>ISSN: 0305-7453</identifier><identifier>ISSN: 1460-2091</identifier><identifier>EISSN: 1460-2091</identifier><identifier>DOI: 10.1093/jac/48.3.351</identifier><identifier>PMID: 11532998</identifier><identifier>CODEN: JACHDX</identifier><language>eng</language><publisher>Oxford: Oxford University Press</publisher><subject>Adult ; Anti-HIV Agents - pharmacokinetics ; Antibiotics. Antiinfectious agents. Antiparasitic agents ; Antiviral agents ; Biological and medical sciences ; HIV Infections - metabolism ; HIV Protease Inhibitors - pharmacokinetics ; Human immunodeficiency virus 1 ; Humans ; Indinavir - pharmacokinetics ; Male ; Medical sciences ; Middle Aged ; Pharmacology. Drug treatments ; Ritonavir - pharmacokinetics ; Saquinavir - pharmacokinetics ; Semen - metabolism</subject><ispartof>Journal of antimicrobial chemotherapy, 2001-09, Vol.48 (3), p.351-354</ispartof><rights>2001 INIST-CNRS</rights><rights>Copyright Oxford University Press(England) Sep 2001</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c450t-3ab6ff841fb0764d13d9e1ee4a944878625c7354564c5b2254181243eb31973e3</citedby></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,776,780,27901,27902</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=1113549$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/11532998$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Taylor, Stephen</creatorcontrib><creatorcontrib>Back, David J.</creatorcontrib><creatorcontrib>Drake, Susan M.</creatorcontrib><creatorcontrib>Workman, Judith</creatorcontrib><creatorcontrib>Reynolds, Helen</creatorcontrib><creatorcontrib>Gibbons, Sara E.</creatorcontrib><creatorcontrib>White, David J.</creatorcontrib><creatorcontrib>Pillay, Deenan</creatorcontrib><title>Antiretroviral drug concentrations in semen of HIV-infected men: differential penetration of indinavir, ritonavir and saquinavir</title><title>Journal of antimicrobial chemotherapy</title><addtitle>J. Antimicrob. Chemother</addtitle><description>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.</description><subject>Adult</subject><subject>Anti-HIV Agents - pharmacokinetics</subject><subject>Antibiotics. Antiinfectious agents. Antiparasitic agents</subject><subject>Antiviral agents</subject><subject>Biological and medical sciences</subject><subject>HIV Infections - metabolism</subject><subject>HIV Protease Inhibitors - pharmacokinetics</subject><subject>Human immunodeficiency virus 1</subject><subject>Humans</subject><subject>Indinavir - pharmacokinetics</subject><subject>Male</subject><subject>Medical sciences</subject><subject>Middle Aged</subject><subject>Pharmacology. 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Antiinfectious agents. Antiparasitic agents</topic><topic>Antiviral agents</topic><topic>Biological and medical sciences</topic><topic>HIV Infections - metabolism</topic><topic>HIV Protease Inhibitors - pharmacokinetics</topic><topic>Human immunodeficiency virus 1</topic><topic>Humans</topic><topic>Indinavir - pharmacokinetics</topic><topic>Male</topic><topic>Medical sciences</topic><topic>Middle Aged</topic><topic>Pharmacology. Drug treatments</topic><topic>Ritonavir - pharmacokinetics</topic><topic>Saquinavir - pharmacokinetics</topic><topic>Semen - metabolism</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Taylor, Stephen</creatorcontrib><creatorcontrib>Back, David J.</creatorcontrib><creatorcontrib>Drake, Susan M.</creatorcontrib><creatorcontrib>Workman, Judith</creatorcontrib><creatorcontrib>Reynolds, Helen</creatorcontrib><creatorcontrib>Gibbons, Sara E.</creatorcontrib><creatorcontrib>White, David J.</creatorcontrib><creatorcontrib>Pillay, Deenan</creatorcontrib><collection>Istex</collection><collection>Pascal-Francis</collection><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>Bacteriology Abstracts (Microbiology B)</collection><collection>Biotechnology Research Abstracts</collection><collection>Industrial and Applied Microbiology Abstracts (Microbiology A)</collection><collection>Toxicology Abstracts</collection><collection>Virology and AIDS Abstracts</collection><collection>Technology Research Database</collection><collection>Environmental Sciences and Pollution Management</collection><collection>Engineering Research Database</collection><collection>AIDS and Cancer Research Abstracts</collection><collection>ProQuest Health & Medical Complete (Alumni)</collection><collection>Algology Mycology and Protozoology Abstracts (Microbiology C)</collection><collection>Nursing & Allied Health Premium</collection><collection>Biotechnology and BioEngineering Abstracts</collection><collection>MEDLINE - Academic</collection><jtitle>Journal of antimicrobial chemotherapy</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Taylor, Stephen</au><au>Back, David J.</au><au>Drake, Susan M.</au><au>Workman, Judith</au><au>Reynolds, Helen</au><au>Gibbons, Sara E.</au><au>White, David J.</au><au>Pillay, Deenan</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Antiretroviral drug concentrations in semen of HIV-infected men: differential penetration of indinavir, ritonavir and saquinavir</atitle><jtitle>Journal of antimicrobial chemotherapy</jtitle><addtitle>J. Antimicrob. Chemother</addtitle><date>2001-09-01</date><risdate>2001</risdate><volume>48</volume><issue>3</issue><spage>351</spage><epage>354</epage><pages>351-354</pages><issn>0305-7453</issn><issn>1460-2091</issn><eissn>1460-2091</eissn><coden>JACHDX</coden><abstract>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.</abstract><cop>Oxford</cop><pub>Oxford University Press</pub><pmid>11532998</pmid><doi>10.1093/jac/48.3.351</doi><tpages>4</tpages><oa>free_for_read</oa></addata></record> |
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| source | Oxford University Press Journals All Titles (1996-Current); MEDLINE; Elektronische Zeitschriftenbibliothek - Frei zugängliche E-Journals; Free Full-Text Journals in Chemistry |
| subjects | Adult Anti-HIV Agents - pharmacokinetics Antibiotics. Antiinfectious agents. Antiparasitic agents Antiviral agents Biological and medical sciences HIV Infections - metabolism HIV Protease Inhibitors - pharmacokinetics Human immunodeficiency virus 1 Humans Indinavir - pharmacokinetics Male Medical sciences Middle Aged Pharmacology. Drug treatments Ritonavir - pharmacokinetics Saquinavir - pharmacokinetics Semen - metabolism |
| title | Antiretroviral drug concentrations in semen of HIV-infected men: differential penetration of indinavir, ritonavir and saquinavir |
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