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

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-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.

• Authors: P L Anderson, S E Noormohamed, K Henry, R C Brundage, H H Balfour Jr, C V Fletcher
• Journal: Pharmacotherapy (Pharmacotherapy) Vol. 20 Issue 8 Pg. 917-22 (Aug 2000) ISSN: 0277-0008 [Print] United States
• PMID: 10939552 (Publication Type: Clinical Trial, Journal Article, Research Support, U.S. Gov't, P.H.S.)

Chemical References

• Anti-HIV Agents
• Glucuronides
• Zidovudine

Topics

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