Semen and serum pharmacokinetics of zidovudine and zidovudine-glucuronide in men with HIV-1 infection

Study Objective. To characterize the concentration-time profiles of zidovud ine 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 intensiv e pharmacokinetic study on day 1. Over the next 8 days, a dose administrati on and timed single-sample strategy was employed to determine serum and sem en concentration time profiles simultaneously. Measurements and Main Results. Zidovudine and zidovudine-glucuronide concen trations were uniformly higher in semen than in serum except at 1 hour afte r the dose. The median area under the curve ratio (semen AUC(0-48):serum AU C(0-infinity)) was 3.31 for zidovudine and 15.04 for zidovudine-glucuronide . Conclusion. Zidovudine and zidovudine-glucuronide reach high levels in semi nal plasma relative to serum. The virologic, pharmacodynamic, and public he alth implications of distribution to this compartment require further study .