Semen and Serum Pharmacokinetics of Zidovudine and Zidovudine‐Glucuronide in Men with HIV‐1 Infection

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Abstract
Study Objective. To characterize the concentration‐time profiles of zidovudine and zidovudine‐glucuronide in semen and serum of men infected with the human immunodeficiency‐1 virus (HIV‐1). Design. Open‐label observational study. Setting. University‐affiliated teaching hospital and research center. Patients. Four asymptomatic HIV‐1‐infected men. Interventions. Zidovudine administration was followed by an 8‐hour intensive pharmacokinetic study on day 1. Over the next 8 days, a dose administration and timed single‐sample strategy was employed to determine serum and semen concentration time profiles simultaneously. Measurements and Main Results. Zidovudine and zidovudine‐glucuronide concentrations were uniformly higher in semen than in serum except at 1 hour after the dose. The median area under the curve ratio (semen AUC0–48:serum AUC0–∞) was 3.31 for zidovudine and 15.04 for zidovudine‐glucuronide. Conclusion. Zidovudine and zidovudine‐glucuronide reach high levels in seminal plasma relative to serum. The virologic, pharmacodynamic, and public health implications of distribution to this compartment require further study.

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