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JAC Advance Access published online on November 1, 2002
Journal of Antimicrobial Chemotherapy, doi:10.1093/jac/dkf232
© 2002 by The British Society for Antimicrobial Chemotherapy
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© 2002 The British Society for Antimicrobial Chemotherapy

In Brief

Pharmacokinetics of saquinavir co-administered with cimetidine

Marta Boffito 1*, Pierluigi Carriero 2, Laura Trentini 3, Riccardo Raiteri 3, Stefano Bonora 3, Alessandro Sinicco 3, Helen E. Reynolds 4, Patrick G. Hoggard 4, David J. Back 4, Giovanni Di Perri 3

1 Infectious Diseases Unit, University of Torino, Torino; Roche, Monza, Italy
2 Roche, Monza, Italy
3 Infectious Diseases Unit, University of Torino, Torino, Italy
4 Department of Pharmacology and Therapeutics, University of Liverpool, Liverpool, UK

* Corresponding author. E-mail: martalbb{at}hotmail.com.

Received 26 June 2002 ; revised 2 September 2002 ; accepted 6 September 2002

Abstract

The present study evaluated the effect of cimetidine, a histamine H2 receptor antagonist able to inhibit cytochrome P450 metabolism, on the steady-state pharmacokinetics of saquinavir soft gel. Twelve healthy volunteers (eight males and four females) participated in an open-label, double-phase pharmacokinetic study. Volunteers took saquinavir soft gel 1200 mg three times a day for 13 days and then saquinavir soft gel 1200 mg twice a day with cimetidine 400 mg twice a day from day 14 to 26. The pharmacokinetics of saquinavir on days 13 and 26 were compared. All 12 volunteers completed the study. The association of cimetidine with saquinavir soft gel 1200 mg twice a day resulted in a significant increase in saquinavir AUC0-24 (120%; P = 0.023) and Cmax (179%; P = 0.019), whereas Ctrough did not differ significantly (32% increase; P = 0.272). Increased exposure to saquinavir was observed in healthy volunteers after co-administration with cimetidine. The most significant increase involved Cmax. Further pharmacokinetic studies in HIV-infected subjects are warranted to confirm the boosting effect of cimetidine and to investigate any impact that the increase in saquinavir Cmax may have on intracellular accumulation of the drug.

Keywords: saquinavir, pharmacokinetics, cimetidine, protease inhibitors
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