Population pharmacokinetics of esomeprazole in patients with preterm
preeclampsia
Abstract
Esomeprazole is a proton pump inhibitor being investigated for treatment
of preeclampsia. Esomeprazole pharmacokinetics during pregnancy is
unknown. We used data from 10 pregnant patients with preterm
preeclampsia, and 49 non-pregnant individuals to develop a population
pharmacokinetic model of esomeprazole. A two-compartment model described
the data well. In pregnant patients after single dose, clearance was
42.2% (14.9%– 61.6%) lower compared to non-pregnant, most likely due
to downregulation of CYP2C19. In non-pregnant after repeated dosing,
clearance was 54.9% (48.2% – 63.5%) lower in extensive metabolizers
and bioavailability was 33% (10.0% – 52.0%) higher compared to
single dosing, which could be due to autoinhibition of CYP2C19.
Esomeprazole pharmacokinetics during pregnancy appears to be more
dependent on CYP3A4.