Effect of widely used combinations of antiretroviral therapy on liver CYP3A4 activity in HIV‐infected patients

摘要: Aims To evaluate the effects of combined antiretroviral drugs (HAART) on liver CYP3A4 activity using [14C-N-methyl]-erythromycin breath test (ERMBT). Methods HIV-infected patients (31 women, 30 men) with mean (± SD) age 38 ± 9 years were enrolled and underwent complete clinical laboratory evaluation. Patients divided into five groups treated two nucleoside analogues (NAs) one following: nelfinavir alone (n = 13), any ritonavir-boosted protease inhibitor (n = 8) or without (n = 13) nevirapine, nevirapine (n = 15), a third NA (n = 12). Three four ERMBTs performed 7 days prior to (D−7) at beginning treatment (D0), D14 (only for taking nevirapine) D28. Results Mean baseline displayed high interindividual variability (47%) but low intraindividual (15%). Women had 30% higher ERMBT values than men [2.7 ± 1.3 vs. 1.9 ± 0.7; 95% confidence interval (CI) 20.5, 49.5; P = 0.003]. The data correlated body weight, α- β-globulins alanin aminotransferases (0.10 < rs < 0.20; P < 0.01). Whereas no effect activity, nelfinavir-based drug regimens inhibited it by 69% (95% CI 64.7, 72.9; P = 0.005) 93.3, 96.7; P = 0.001), respectively. Conclusion Evaluation HAART may aid in preventing inappropriate HIV-infected patients.