Pharmacokinetic Interaction between Saquinavir and Cyclosporine
Authors: Kees Brinkman
Journal: Annals of Internal Medicine (1998)

Letters1 December 1998Pharmacokinetic Interaction between Saquinavir and CyclosporineKees Brinkman, MD, PhD, Frans Huysmans, MD, PhD, and David M. Burger, PharmD, PhDKees Brinkman, MD, PhDUniversity Hospital Nijmegen; Nijmegen, the NetherlandsSearch for more papers by this author, Frans Huysmans, MD, PhDUniversity Hospital Nijmegen; Nijmegen, the NetherlandsSearch for more papers by this author, and David M. Burger, PharmD, PhDUniversity Hospital Nijmegen; Nijmegen, the NetherlandsSearch for more papers by this authorAuthor, Article, and Disclosure Informationhttps://doi.org/10.7326/0003-4819-129-11_Part_1-199812010-00022 SectionsAboutFull TextPDF ToolsAdd to favoritesDownload CitationsTrack CitationsPermissions ShareFacebookTwitterLinkedInRedditEmail TO THE EDITOR:An HIV-positive kidney transplant recipient who was receiving cyclosporine and prednisone started zidovudine and lamivudine therapy shortly after kidney function had stabilized. When protease inhibitors became available, saquinavir was added; levels of both drugs were monitored.Without saquinavir, the cyclosporine trough levels in this patient were stable at a dosage of 150 mg twice daily (150 to 200 µg/L). Within 3 days after saquinavir therapy began at a dosage of 1200 mg three times daily, the patient reported fatigue, headache, and gastrointestinal discomfort and the trough level of cyclosporine tripled to 580 µg/L. After cyclosporine and saquinavir ...References1. Merry C, Barry MG, Mulcahy F, Ryan M, Heavey J, Tjia JF, et al. Saquinavir pharmacokinetics alone and in combination with ritonavir in HIV-infected patients. AIDS. 1997; 11:F29-33. Google Scholar2. Sonneveld P, Durie BG, Lokhorst HM, Marie J, Solbu G, Suciu S, et al. Modulation of multidrug-resistant multiple myeloma by cyclosporin. Lancet. 1992; 340:255-9. Google Scholar3. Washington CB, Duran GE, Sikic BI, Blaschke TF. Saquinavir is a high affinity substrate for the multidrug transporter, P-glycoprotein [Abstract]. Clin Pharmacol Ther. 1997; 61:193. Google Scholar4. Kim RB, Fromm MF, Wandel C, Leake B, Wood AJ, Roden DM, et al. The drug transporter P-glycoprotein limits oral absorption and brain entry of HIV-1 protease inhibitors. J Clin Invest. 1998; 101:289-94. Google Scholar5. Lee CG, Gottesman MM. HIV-1 protease inhibitors and the MDR1 multidrug transporter. J Clin Invest. 1998; 101:287-8. 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