ArticleJournal of acquired immune deficiency syndromes (1999)2008
Differential extracellular and intracellular concentrations of zidovudine and lamivudine in semen and plasma of HIV-1-infected men.
Article in Journal of acquired immune deficiency syndromes (1999), 2008. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 26 papers, 1 of them a synthesis that pooled it.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
26 citing papers in PubMed, 1 synthesis or guideline pooled it, 44 citations in OpenAlex.
- Pharmacokinetics of Antiretroviral Drugs in Older People Living with HIV, Part II: Drugs Licensed Before 2005.Clinical pharmacokinetics · 2024Pooled it
- Decay kinetics of HIV-1-RNA in seminal plasma with dolutegravir/lamivudine versus dolutegravir plus emtricitabine/tenofovir alafenamide in treatment-naive people living with HIV.The Journal of antimicrobial chemotherapy · 2023Trial
- Emtricitabine seminal plasma and blood plasma population pharmacokinetics in HIV-infected men in the EVARIST ANRS-EP 49 study.Antimicrobial agents and chemotherapy · 2015Trial
- Anogenital HIV RNA in Thai men who have sex with men in Bangkok during acute HIV infection and after randomization to standard vs. intensified antiretroviral regimens.Journal of the International AIDS Society · 2015Trial
- Contemporary antiretroviral pharmacology in the male genital tract: implications for HIV treatment and prevention.Antimicrobial agents and chemotherapy · 2026Review
- Effect of in vitro exposure of first-line antiretrovirals on healthy human spermatozoa on kinematics and motility.International urology and nephrology · 2025Article
- Article
- Testicular disposition of clofarabine in rats is dependent on equilibrative nucleoside transporters.Pharmacology research & perspectives · 2021Article
- Review
- Differential extracellular, but similar intracellular, disposition of two tenofovir formulations in the male genital tract.Antiviral therapy · 2019Article
- Antiretroviral Therapy and Alcohol Interactions: X-raying Testicular and Seminal Parameters Under the HAART Era.European journal of drug metabolism and pharmacokinetics · 2018Review
- Population Pharmacokinetic Modeling of Tenofovir in the Genital Tract of Male HIV-Infected Patients.Antimicrobial agents and chemotherapy · 2017Article
- Pharmacokinetic Modeling of Lamivudine and Zidovudine Triphosphates Predicts Differential Pharmacokinetics in Seminal Mononuclear Cells and Peripheral Blood Mononuclear Cells.Antimicrobial agents and chemotherapy · 2015Article
- Maternal and fetal zidovudine pharmacokinetics during pregnancy and labour: too high dose infused at labour?British journal of clinical pharmacology · 2014Article
- Xenobiotic transporter expression along the male genital tract.Reproductive toxicology (Elmsford, N.Y.) · 2014Article
- Pharmacokinetics of antiretrovirals in genital secretions and anatomic sites of HIV transmission: implications for HIV prevention.Clinical pharmacokinetics · 2014Review
- Basolateral uptake of nucleosides by Sertoli cells is mediated primarily by equilibrative nucleoside transporter 1.The Journal of pharmacology and experimental therapeutics · 2013Article
- Antiretroviral bioanalysis methods of tissues and body biofluids.Bioanalysis · 2013Review
- Article
- HIV-1 treatment as prevention: the good, the bad, and the challenges.Current opinion in HIV and AIDS · 2011Review
Corrections and comments
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Authors and funding
9 authors at 4 institutions in 3 countries.
Funding
Abstract
objectivesTo quantitate extracellular and intracellular zidovudine (ZDV) and lamivudine (3TC) concentrations in blood and semen of HIV-1-infected men.
design: Nonblind, single-center, open-label pharmacokinetic (PK) study in 14 subjects receiving ZDV plus 3TC.
methodsPaired blood and semen samples were obtained during 1 intensive visit and 3 single time point visits over 2 weeks. Extracellular ZDV and 3TC concentrations were measured in blood plasma (BP) and seminal plasma (SP), and intracellular ZDV and 3TC triphosphate (TP) concentrations were measured in isolated mononuclear cells using validated methods. HIV-1 RNA was measured in blood and semen. PK parameters were estimated using noncompartmental analysis.
resultsMedian (interquartile range [IQR]) SP/BP area under the time-concentration curve over the 12-hour dosing interval (AUC0-12h) ratios for ZDV and 3TC were 2.28 (1.48 to 2.97) and 6.67 (4.10 to 9.14), respectively, whereas individual SP/BP concentration ratios ranged from 1.9 to 91.4. Intracellular median (IQR) SP/BP AUC0-12h ratios for ZDV-TP and 3TC-TP were 0.36 (0.30 to 0.37) and 1.0 (0.62 to 1.30), respectively, whereas individual SP/BP concentration ratios ranged from 0.11 to 2.9. HIV-1 RNA was undetectable in both compartments.
conclusionsZDV and 3TC SP exposures are 2- to 6-fold greater than BP exposures. Seminal ZDV-TP exposures are approximately 40% of those found in peripheral blood mononuclear cells (PBMCs), whereas 3TC-TP exposures are similar to PBMC exposures. PK variability makes individual SP/BP ratios a suboptimal surrogate for genital tract exposure.
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What OpenQuestion holds
Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.