Total, Unbound, Renal, and Hepatic Clearances of Raltegravir and the Formation and Elimination Clearances of Raltegravir Glucuronide in Pregnant Women

• DOI: 10.1002/jcph.2287
• Publication Date: 2023-06-01T11:09:08Z
• Authors: Fernanda de Lima ...; Tiago Antunes Paz; Patrícia Pereira ...; Matheus de Lucca ...; Maria Paula Marques; Adriana Rocha; Geraldo Duarte; Vera Lucia Lanchote
• Keywords: Raltegravir; Glucuronide; Probenecid

This work aimed to evaluate the total, unbound, renal, and hepatic clearances of raltegravir (RAL) formation elimination glucuronide (RAL GLU) in pregnant women living with HIV. The participants received RAL 400 mg twice daily during third trimester (n = 15) gestation, delivery 15), postpartum period 8). Pharmacokinetic parameter values were calculated on basis plasma urine data using noncompartmental methods. for gestation as follows: total clearance: geometric mean, 63.63 L/h (95% CI, 47.5-85.25); renal 2.56 1.96-3.34); 60.52 44.65-82.04); unbound 281.14 203.68-388.05). GLU 7.57 4.94-11.6) 8.71 6.71-11.32), respectively. No differences observed pharmacokinetic parameters between period, except higher (7.57 vs 4.03 L/h) (8.71 4.92 trimester. findings based are consistent an increase uridine 5' diphospho-glucuronosyltransferase isoenzymes activities involved metabolism pregnancy, is a minor route elimination. Compared similar exposure reinforces maintenance regimen including 400-mg oral dose pregnancy.