Esomeprazole sodium

The main ingredient of this product is esomeprazole sodium. The auxiliary materials are edetate disodium and sodium hydroxide.

The main ingredient of this product is esomeprazole sodium. The auxiliary materials are edetate disodium and sodium hydroxide.

The main ingredient of this product is esomeprazole sodium. The auxiliary materials are edetate disodium and sodium hydroxide.

1. Effect of esomeprazole on the pharmacokinetics of other drugs Drugs whose absorption is affected by pH: (1) During treatment with this drug, the absorption of drugs whose absorption process is affected by gastric acid may be increased or decreased due to the decrease in gastric acid. As with other acid secretion inhibitors or antacids, the absorption of ketoconazole and itraconazole will be reduced during treatment with this drug. (2) Omeprazole has been reported to interact with some protease inhibitors, but the clinical significance and mechanism of these drug interactions are not very clear. Omeprazole treatment increases gastrointestinal pH, which may change the absorption of other protease inhibitors. Another possible mechanism is to cause drug interactions by inhibiting the CYP2C19 enzyme. It has also been reported that the serum concentrations of atazanavir and nelfinavir will decrease when co-administered with omeprazole, so co-administration is not recommended. Healthy volunteers taking omeprazole 40 mg once daily and atazanavir 300 mg/ritonavir 100 mg simultaneously can reduce the drug exposure of atazanavir (AUC, Cmax and Cmin are reduced by approximately 75%). Increases in the atazanavir dose to 400 mg also failed to compensate for the effects of omeprazole. Coadministration of proton pump inhibitors (including this product) with atazanavir is not recommended. In healthy volunteers, the coadministration of omeprazole (20 mg once daily) with atazanavir 400 mg/ritonavir 100 mg resulted in approximately a 30% decrease in atazanavir exposure compared to the exposure without coadministration. Coadministration of omeprazole (40 mg once daily) decreased the AUC, Cmax, and Cmin of nelfinavir by 36-39%, and the mean AUC, Cmax, and Cmin of its pharmacologically active metabolite M8 by 75-92%. For saquinavir (concomitantly used with ritonavir), increases in serum concentrations (80-100%) have been reported when used in combination with omeprazole (40 mg once daily). Treatment with omeprazole 20 mg once daily had no effect on the exposure of darunavir (used with ritonavir) and amprenavir (used with ritonavir). Treatment with esomeprazole 20 mg once daily had no effect on the exposure of amprenavir (used with or without ritonavir). Treatment with omeprazole 40 mg once daily had no effect on the exposure of lopinavir (used with ritonavir). Because omeprazole and esomeprazole have similar pharmacodynamics and pharmacokinetic properties, the combination of omeprazole and atazanavir is not recommended, and the combination of omeprazole and nelfinavir is prohibited. Drugs metabolized by CYP2C19: (3) CYP2C19 is the main metabolizing enzyme of esomeprazole. Therefore, when this product is co-administered with drugs metabolized by CYP2C19 (such as diazepam, citalopram, imipramine, clomipramine, phenytoin, etc.), the plasma concentrations of these drugs may be increased and the dose may need to be reduced. Co-administration of 30 mg of oral esomeprazole can reduce the clearance of diazepam metabolized by CYP2C19 by 45%. Co-administration of 40 mg of oral esomeprazole can increase the trough concentration of plasma phenytoin in patients with epilepsy by 13%. Therefore, during phenytoin treatment, when co-administration or discontinuation of this product is started, it is recommended to monitor the blood concentration of phenytoin. Omeprazole 40 mg once daily increased the Cmax and AUCτ of voriconazole (a CYP2C19 substrate) by 15% and 41%, respectively. (4) Clinical trials have shown that patients receiving warfarin therapy who co-administered oral esomeprazole 40 mg had an acceptable clotting time. However, after the launch of oral esomeprazole, there have been reports of clinically significant increases in INR (International Normalized Ratio) in individual cases when the two were co-administered. Therefore, during treatment with warfarin or other coumarin derivatives, it is recommended to monitor the blood concentration of warfarin when co-administering or discontinuing this product. (5) In healthy volunteers, co-administration of oral esomeprazole 40 mg increased the area under the blood concentration-time curve (AUC) of cisapride by 32% and prolonged the elimination half-life (t1/2) by 31%, but did not significantly increase the peak plasma concentration of cisapride. Co-administration of this product does not aggravate the slight prolongation of the QTc interval caused by cisapride alone. (6) Studies have shown that this product has no clinically relevant effect on the pharmacokinetics of amoxicillin or quinidine. 2. Effects of other drugs on the pharmacokinetics of esomeprazole: Esomeprazole is metabolized by CYP2C19 and CYP3A4. Oral administration of esomeprazole and clarithromycin (500 mg twice daily), a CYP3A4 inhibitor, can double the body's exposure to esomeprazole (AUC). The combined use of esomeprazole and CYP2C19 and CYP3A4 co-inhibitors can more than double the exposure of esomeprazole. Voriconazole, an inhibitor of CYP2C19 and CYP3A4, increases the AUCτ of omeprazole by 280%. In the above two situations, the dose of esomeprazole does not need to be routinely adjusted. However, for patients with severe liver damage and those who require long-term treatment, the dose of this product should be considered for adjustment.