LAUSR

This study evaluates the influence of pregnancy and HIV infection in conjunction with the use of cART (raltegravir, lamivudine, tenofovir disoproxil fumarate) on intestinal P-gp and hepatic OATP1B1/1B3 and/or BCRP drug transporters activity using rosuvastatin (OATP1B/BCRP) and fexofenadine (P-gp) probes. Single oral doses of 5 mg rosuvastatin and 60 mg fexofenadine were administered to women living with HIV under cART in the third trimester of gestation (n = 15) and postpartum period (n = 10). A control group of 12 healthy non-pregnant women also was investigated. PK parameters were estimated by using a non-compartmental method and evaluated using t-test (p<0.05). The rosuvastatin AUC0-last value was higher at third trimester of pregnancy [19.5 (16.8 - 22.3) ng*h/mL] when compared to postpartum [13.3 (9.3 - 17.5) ng*h/mL], while the fexofenadine AUC0-last values did not differ between the third trimester of pregnancy [738.0 (611.4 - 864.6) ng*h/mL] and postpartum period [874.9 (408.2 - 1342.0 ng*h/mL). The rosuvastatin AUC0-last values did not differ between healthy non-pregnant women [13.8 (10.0 - 17.6) ng*h/mL] and women living with HIV at postpartum period [13.3 (9.3 - 17.5) ng*h/mL], as well as the fexofenadine AUC0-last values did not differ between the two investigated groups [603.6 (467.5 - 739.7) ng*h/mL versus 874.9 (408.2 -1342.0) ng*h/mL]. It is suggested that gestation inhibits the hepatic OATP1B1/1B3 and/or BCRP activity but does not alter intestinal P-gp activity. It was not observed the influence of HIV infection in conjunction with use of cART (raltegravir, lamivudine, tenofovir disoproxil fumarate) on OATP1B/BCRP and intestinal P-gp activity. This article is protected by copyright. All rights reserved.