Esomeprazole Sodium for Injection

Pharmacological action: This product is a specific inhibitor of the proton pump in gastric parietal cells. Esomeprazole is the S-isomer of omeprazole. It reduces gastric acid secretion by specific proton pump inhibition. The R-isomer and S-isomer of omeprazole have similar pharmacodynamic properties. Esomeprazole is a weakly alkaline drug. It is concentrated and converted into an active form in the high acid environment of the acid secretory microtubules of the parietal cells, thereby inhibiting the H/K-ATPase (proton pump) at this site, and inhibiting both basal gastric acid secretion and stimulated gastric acid secretion. Patients with gastroesophageal reflux disease (GERD) took 20 mg and 40 mg of esomeprazole orally every day. After 5 days, the average time for maintaining gastric pH 4 within 24 hours was 13 hours and 17 hours, respectively. The effects of oral or intravenous administration of esomeprazole are similar. The relationship between gastric acid secretion inhibition and drug exposure after oral administration can also be shown by AUC (area under the blood concentration-time curve). Patients with reflux esophagitis took esomeprazole 40 mg orally for 4 weeks, and the healing rate was about 78%, and 93% after 8 weeks. During antacid treatment, decreased gastric acid secretion can lead to increased serum gastrin. In some patients treated with long-term oral esomeprazole, an increase in enterochromaffin-like (ECL) cells was observed, which may be related to the increase in serum gastrin levels. During long-term use of antacids, there have been reports of a certain degree of increase in the incidence of gastric glandular cysts. These reactions are physiological reactions after significant inhibition of acid secretion, which are benign and reversible. Toxicity studies In conventional single and multiple dose toxicity studies, teratogenicity and mutagenicity and other preclinical related test studies, there is no evidence that esomeprazole is particularly harmful to humans. Carcinogenicity studies of oral racemic mixtures (omeprazole) in rats found hyperplasia of enterochromaffin-like (ECL) cells and carcinoids in the stomach. These effects are secondary to the continued reduction in gastric acid production and significant hypergastrinemia, which are seen in rats after long-term use of gastric acid secretion inhibitors. Lowering stomach acidity with any means, including proton pump inhibitors, can increase the number of bacteria in the stomach (which normally reside in the gastrointestinal tract). Treatment with proton pump inhibitors may result in a slightly increased risk of gastrointestinal infections (such as Salmonella and Campylobacter).

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

This product is white or off-white freeze-dried block or powder.

1. As an alternative therapy for gastroesophageal reflux disease when oral therapy is not applicable. 2. For low-risk patients with acute gastric or duodenal ulcer bleeding (endoscopic Forrest grade LLC-Ⅲ) who are not suitable for oral therapy.

1. For patients with gastroesophageal reflux disease who cannot take oral medication, it is recommended to intravenously inject or drip 20-40 mg of this product once a day. Patients with reflux esophagitis should use 40 mg once a day; for symptomatic treatment of reflux disease, 20 mg should be used once a day. This product should usually be used for a short period of time (no more than 7 days), and once possible, it should be switched to oral treatment. 2. For patients with acute gastric or duodenal ulcer bleeding of Forrest grade llc-Ⅲ who cannot take oral medication, it is recommended to drip 40 mg of this product once every 12 hours for 5 days. Dosage method Injection: The intravenous injection time of the prepared solution should be at least 3 minutes. Infusion: The intravenous drip time of the prepared solution should be within 30 minutes. Instructions for use The preparation of the injection solution is for intravenous injection by adding 5 ml of 0.9% sodium chloride solution to the vial of this product. The preparation of the drip solution is for intravenous drip by dissolving 1 vial of this product in 100 ml of 0.9% sodium chloride solution. The prepared liquid for injection or infusion is a clear solution that is colorless to very slightly yellow and should be used within 12 hours and stored below 30°C. From a microbiological point of view, it is best to use it immediately. Incompatibility The degradation of the prepared solution is highly dependent on the pH value, so the drug must be used according to the instructions for use. This product can only be dissolved in 0.9% sodium chloride for intravenous use. The prepared solution should not be mixed with other drugs or used in the same infusion device.

In clinical trials of oral or intravenous esomeprazole and in post-marketing studies of oral administration, the following adverse reactions have been identified or suspected. These reactions are classified according to the frequency of occurrence as follows (common >1%, <10%; infrequent >0.1%, <1%; rare >0.01%, <0.1%; very rare <0.01%). 1. Eyes: Occasionally: blurred vision. 2. Ears and labyrinth: Occasionally: vertigo. 3. Skin and subcutaneous tissue: Occasionally: dermatitis, pruritus, rash, urticaria; Rarely: alopecia, photosensitivity; Very rare: erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis (TEN). 4. Skeletal muscle, connective tissue and bone: Rare: arthralgia, myalgia: Very rare

1. Patients who are known to be allergic to esomeprazole, other benzimidazole compounds or any other ingredients of this product are contraindicated. 2. This product is contraindicated for use in combination with nelfinavir; it is not recommended to be used in combination with atazanavir or saquinavir (see [Drug Interactions] for details).

Precautions for children: Children should not use this product because there is no relevant data. Precautions for pregnancy and lactation: There is limited clinical data on the use of esomeprazole by pregnant women. Animal experiments have not shown that esomeprazole has direct or indirect damage to the development of animal embryos or fetuses. Animal experiments with racemic mixtures (omeprazole) have also not shown that it has direct or indirect harmful effects on animal pregnancy, delivery, or postnatal development of the fetus. However, pregnant women should use this product with caution. It is not clear whether esomeprazole is excreted through human milk. No relevant studies have been conducted in lactating women, so this product should not be used during lactation. Precautions for the elderly: Elderly patients do not need to adjust the dose of this product.

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.

Keep in a dark place and sealed at a temperature below 30℃.

40mg (calculated as C17H19N3O3S)

24 months

AstraZeneca Pharmaceutical Co., Ltd.

• Founded in:

  1993-10-26

• Address:

  No. 2 Huangshan Road, New District, Wuxi

• Tax NO.:

  91320214607915071G

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  $191.2 million

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