Ezoprole Drug Interactions

Antiretroviral Drugs: Concomitant use of atazanavir, nelfinavir, rilpivirine, saquinavir or raltegravir with PPIs is not recommended. Esomeprazole is expected to substantially decrease atazanavir, nelfinavir, and rilpivirine plasma concentrations, which may result in loss of therapeutic effect and development of drug resistance. In contrast, coadministration of saquinavir or raltegravir with PPIs is expected to increase saquinavir or raltegravir concentrations, which may increase toxicity and require dose reduction.
pH-dependent Drugs: Esomeprazole may reduce the absorption of drugs where gastric pH is an important determinant of their bioavailability. As with other drugs that decrease intragastric acidity, the absorption of drugs such as ketoconazole, atazanavir, nelfinavir, iron salts, erlotinib, and mycophenolate mofetil (MMF) may also decrease, while the absorption of drugs such as digoxin may increase during treatment with esomeprazole.
Digoxin: Coadministration of digoxin with esomeprazole may increase the systemic exposure of digoxin. Therefore, patients should be carefully monitored when digoxin is taken concomitantly with esomeprazole.
Mycophenolate mofetil (MMF): Coadministration of esomeprazole in healthy patients and in transplant patients receiving MMF has been reported to reduce the exposure to the active metabolite, mycophenolic acid (MPA), possibly due to a decrease in MMF solubility at an increased gastric pH. The clinical relevance of reduced MPA exposure in organ rejection has not been established in transplant patients receiving esomeprazole and MMF.
Drugs Affecting/Metabolized by Hepatic Microsomal Enzymes: Esomeprazole is metabolized in the liver through CYP2C19 and CYP3A4. Drugs known to inhibit CYP2C19 or CYP3A4 or both (e.g., clarithromycin and voriconazole) may increase the plasma concentrations of esomeprazole by decreasing the rate of its metabolism.
In contrast, drugs known to induce CYP2C19 or CYP3A4 or both (e.g., rifampicin and St. John's Wort) may decrease the plasma concentrations of esomeprazole by increasing the rate of its metabolism.
Diazepam: Concomitant administration of esomeprazole and diazepam may decrease diazepam clearance by 45%.
Warfarin: Increased international normalized ratio (INR) and prothrombin time have been reported in patients receiving PPIs and warfarin concomitantly. Since such increases may lead to abnormal bleeding and even death, patients being treated with PPIs and warfarin should be monitored for increases in INR and prothrombin time.
Tacrolimus: Concomitant administration of esomeprazole and tacrolimus may increase the plasma concentrations of tacrolimus. The plasma concentrations and creatinine clearance of tacrolimus should be monitored. The dosage of tacrolimus may be adjusted if necessary.
Citalopram, Imipramine, Clomipramine, Cilostazol and Phenytoin: Concomitant administration of esomeprazole (a CYP2C19 inhibitor) with drugs that are metabolized by CYP2C19 (e.g., citalopram, imipramine, clomipramine, cilostazol, and phenytoin) may increase the plasma concentrations of these drugs. Dosage adjustment is recommended.
Clopidogrel: Concomitant use of esomeprazole with clopidogrel reduces exposure to the active metabolite of clopidogrel and decreases platelet inhibitory effects.
Citalopram/Escitalopram: Coadministration of esomeprazole with citalopram doubles the AUC of the S-isomer of citalopram (escitalopram) but did not affect its R-isomer. Dosage adjustment of citalopram/escitalopram may be necessary.
Drugs that Cause Hypomagnesemia: Possible increased risk of hypomagnesemia; Monitoring of magnesium levels prior to and during PPI treatment should be considered in patients expected to be on prolonged PPI treatment or who take PPIs with medications such as digoxin or drugs that may cause hypomagnesemia (e.g., loop or thiazide diuretics).
Methotrexate: Concomitant administration of PPIs and methotrexate, primarily at high doses, may elevate and prolong serum levels of methotrexate and/or its metabolite hydroxymethotrexate, which may lead to methotrexate toxicity. Temporary PPI withdrawal may be considered in patients receiving high-doses of methotrexate.
Sucralfate: Concomitant administration of esomeprazole with sucralfate resulted in delayed absorption and decreased bioavailability of esomeprazole. PPIs should be administered at least 30 minutes before sucralfate.
Cisapride: Concomitant administration of esomeprazole with cisapride increased the AUC of cisapride by 32% and prolonged the elimination half-life by 31% but no significant increase in peak plasma concentrations of cisapride.
Laboratory Interactions: During treatment with antisecretory drugs, chromogranin A (CgA) increases due to decreased gastric acidity. The increased CgA level may interfere with investigations for neuroendocrine tumors. Esomeprazole treatment should be stopped 14 days before CgA measurement to avoid this interference.