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Session 62 Poster Session
Pharmacokinetics of Antiretroviral Drugs
Session Time: 4:30-6:30 pm
Room 4E-F

  439-W.

Penetration of Lopinavir into the Genital Tract of HIV-1-Infected Men
S. Sankatsing*1, D. Burger2, J. Droste2, S. Jurriaans1, J. Lange1, and J. Prins1
1Academic Med. Ctr., Amsterdam, The Netherlands and 2Univ. Med. Ctr. Radboud, Nijmegen, The Netherlands

Background: Penetration of antiretroviral drugs into anatomical sanctuary sites like the brain and the male genital tract is important, as suboptimal penetration might allow for ongoing viral replication despite systemic virological efficacy. Lopinavir (LPV) is a potent HIV-1 protease inhibitor, but so far there are no data available on its penetration into the male genital tract.
Methods: 14 HIV-1-infected patients who were treated with a LPV-containing regimen for a minimum of 4 weeks were included in the study. Semen samples were obtained by masturbation. The samples were centrifuged for 10 min at 1200 g to obtain seminal plasma (SP). Within 2 hours of semen collection a blood sample was taken for the measurement of plasma LPV.
Results: 4 patients had a plasma LPV concentration below 4 mg/L, the other 10 patients had a plasma concentration above 4 mg/L. The desired plasma concentration is > 4 mg/L. The LPV concentration in SP ranged between 0.046 and 3.9 mg/L (median 0.23 mg/L, IQR 0.15-0.33). There was a weak relation between the plasma concentration and the SP concentration (r = 0.51, p=0.07). The median ratio of the concentrations of LPV in SP and in plasma was only 0.034 (IQR 0.021-0.070). There was no relation between the LPV concentration in SP and the time since medication intake (r = 0.22, p=0.45).
Conclusions: Lopinavir has a poor penetration into the seminal plasma. Whether this will lead to suboptimal suppression of viral replication is currently subject of investigation.

©2002 9th Conference on Retroviruses and Opportunistic Infections