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

Pharmacotherapy. 2000 Aug;20(8):917-22. doi: 10.1592/phco.20.11.917.35263.


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-infinity) 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.

Publication types

  • Clinical Trial
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Adolescent
  • Adult
  • Anti-HIV Agents / blood
  • Anti-HIV Agents / pharmacokinetics*
  • Area Under Curve
  • Glucuronides / blood
  • Glucuronides / metabolism
  • HIV Infections / blood
  • HIV Infections / metabolism*
  • HIV-1*
  • Humans
  • Male
  • Semen / metabolism*
  • Zidovudine / blood
  • Zidovudine / pharmacokinetics*


  • Anti-HIV Agents
  • Glucuronides
  • Zidovudine