OBJECTIVE: This study was done to determine the placental transfer of the human immunodeficiency virus protease inhibitor lopinavir with ritonavir. STUDY DESIGN: Twenty-five human cotyledons that were obtained after uneventful pregnancies and deliveries were perfused in an open double circuit with lopinavir (1099-10,606 microg/L) and ritonavir (254-1147 microg/L) at various albumin concentrations (2, 10, and 40 g/L). RESULTS: The fetal transfer rate of lopinavir, when combined with ritonavir, was 23.6% +/- 6.9% at an albumin concentration of 2 g/L. The fetal transfer rate decreased to 20.7% +/- 10% at an albumin concentration of 10 g/L and to 3.3% +/- 0.5% at an albumin concentration of 40 g/L. CONCLUSION: The placental transfer of lopinavir, a highly protein-bound molecule, was compatible with passive diffusion of the unbound fraction. Even at physiologic maternal albumin concentrations, the amount of drug transferred into the fetal compartment was well above the 50% inhibitory concentration.
OBJECTIVE: This study was done to determine the placental transfer of the human immunodeficiency virus protease inhibitor lopinavir with ritonavir. STUDY DESIGN: Twenty-five human cotyledons that were obtained after uneventful pregnancies and deliveries were perfused in an open double circuit with lopinavir (1099-10,606 microg/L) and ritonavir (254-1147 microg/L) at various albumin concentrations (2, 10, and 40 g/L). RESULTS: The fetal transfer rate of lopinavir, when combined with ritonavir, was 23.6% +/- 6.9% at an albumin concentration of 2 g/L. The fetal transfer rate decreased to 20.7% +/- 10% at an albumin concentration of 10 g/L and to 3.3% +/- 0.5% at an albumin concentration of 40 g/L. CONCLUSION: The placental transfer of lopinavir, a highly protein-bound molecule, was compatible with passive diffusion of the unbound fraction. Even at physiologic maternal albumin concentrations, the amount of drug transferred into the fetal compartment was well above the 50% inhibitory concentration.
Authors: C Vinot; L Gavard; J M Tréluyer; S Manceau; E Courbon; J M Scherrmann; X Declèves; D Duro; G Peytavin; L Mandelbrot; C Giraud Journal: Antimicrob Agents Chemother Date: 2013-01-07 Impact factor: 5.191
Authors: Leonardo Pinto; Priya Bapat; Fernanda de Lima Moreira; Angelika Lubetsky; Ricardo de Carvalho Cavalli; Howard Berger; Vera Lucia Lanchote; Gideon Koren Journal: Pharm Res Date: 2021-04-06 Impact factor: 4.200
Authors: Sreeja Sudhakaran; Craig R Rayner; Jian Li; David C M Kong; Neil M Gude; Roger L Nation Journal: Br J Clin Pharmacol Date: 2007-12-17 Impact factor: 4.335
Authors: Pierre-Francois Ceccaldi; Laurent Gavard; Laurent Mandelbrot; Elisabeth Rey; Robert Farinotti; Jean-Marc Treluyer; Sophie Gil Journal: Obstet Gynecol Int Date: 2009-05-18