Esomeprazole magnesium enteric-coated tablets

1. Pharmacodynamic properties Esomeprazole is the S-isomer of omeprazole. It reduces gastric acid secretion through a specific targeted mechanism and is a specific inhibitor of the proton pump in parietal cells. The R-isomer and S-isomer of omeprazole have similar pharmacodynamic properties. 2. Site of action and mechanism Esomeprazole is a weak base that is concentrated and converted into an active form in the high acid environment of the acid secretory microtubules of parietal cells, thereby inhibiting the H/K-ATPase (proton pump) at this site, inhibiting both basal and stimulated gastric acid secretion. 3. Effect on gastric acid secretion After oral administration of 20 mg and 40 mg of esomeprazole, it takes effect within one hour. Repeated administration of 20 mg once a day for 5 consecutive days, measured 6 to 7 hours after taking the drug on the 5th day, the average peak acid secretion caused by pentagastrin stimulation was reduced by 90%. Patients with symptomatic GERD took 20 mg and 40 mg of esomeprazole orally every day. After 5 days, the average time of intragastric pH 4 in 24 hours was 13 hours and 17 hours, respectively. The proportion of patients who maintained intragastric pH 4 for at least 8 hours, 12 hours and 16 hours was 76%, 54% and 24% at 20 mg of esomeprazole, and 97%, 92% and 56% at 40 mg, respectively. Using the AUC parameter instead of plasma drug concentration can show the dose-effect relationship between gastric acid secretion inhibition and drug exposure. 4. Therapeutic effect of inhibiting gastric acid Clinical studies have shown that the healing rate of patients with reflux esophagitis taking 40 mg of esomeprazole for 4 weeks is about 78%, and 93% after 8 weeks. After one week of treatment with esomeprazole 20 mg twice a day combined with appropriate antibacterial drugs, the eradication rate of Helicobacter pylori is about 90%. After one week of eradication treatment, patients with uncomplicated duodenal ulcers no longer need to use acid suppressants alone for subsequent treatment to heal ulcers and eliminate symptoms. 5. Other effects related to the inhibition of gastric acid During the treatment with antacids, the decrease in gastric acid secretion will lead to an increase in serum gastrin. In some patients treated with long-term esomeprazole, an increase in eosinophils (ECL cells) was observed, which may be related to the increase in serum gastrin levels. During the long-term treatment with 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 in nature and are considered reversible.

The active ingredient of this product is esomeprazole magnesium.

This medicine is enteric-coated tablets. 20mg is light pink, 40mg is pink, both are oblong biconvex.

Gastroesophageal reflux disease (GERD) 1. Treatment of erosive reflux esophagitis 2. Long-term maintenance treatment to prevent recurrence in patients with cured esophagitis 3. Symptom control of gastroesophageal reflux disease (GERD) 4. Combination with appropriate antimicrobial therapy to eradicate Helicobacter pylori, heal duodenal ulcers associated with Helicobacter pylori infection, and prevent recurrence of peptic ulcers associated with Helicobacter pylori

Tablets should be swallowed whole with liquid and should not be chewed or crushed. For patients with difficulty swallowing, tablets can be dissolved in half a cup of carbonate-free water (other liquids should not be used because the enteric coating may be dissolved), stirred until the tablet is completely disintegrated, and taken immediately or within 30 minutes, rinsed with half a cup of water and then drunk. Micropellets should never be chewed or crushed. For patients who cannot swallow, tablets can be dissolved in carbonate-free water and administered through a gastric tube. It is important to carefully check the suitability of the selected syringe and gastric tube. Preparation and instructions for use are as follows: Administration through a gastric tube: 1. Place the tablet in a suitable syringe and add about 25ml of water and 5ml of air. Sometimes 50ml of water is needed to prevent the tube from being blocked by the micropellets. 2. Immediately shake the syringe for about 2 minutes to dissolve the tablet. 3. Point the syringe tip upward and check that the tip is not blocked. 4. Insert the syringe into the tube and hold it in this position. 5. Shake the syringe so that the tip is facing down. Immediately inject 5-10ml into the tube. After injection, turn the syringe over and shake it. (The syringe tip must be kept pointing upward to avoid clogging of the tip). 6. With the syringe tip pointing downward, immediately inject another 5-10 ml into the tube, repeat this step until there is no liquid in the syringe. 7. If you need to wash off the remaining residue in the syringe, repeat step 5 and add 25 ml of water and 5 ml of air to the syringe. Sometimes 50 ml of water is needed. Gastroesophageal Reflux Disease (GERD) 1. Treatment of erosive reflux esophagitis 40 mg once a day for four consecutive weeks. For patients with uncured esophagitis or persistent symptoms, it is recommended to take the medicine for another four weeks. 2. Long-term maintenance treatment to prevent recurrence in patients with cured esophagitis 20 mg once a day. 3. Symptom control of gastroesophageal reflux disease (GERD) 20 mg once a day for patients without esophagitis. If the symptoms are not controlled after 4 weeks of medication, the patient should be further examined. Once the symptoms are eliminated, subsequent symptom control can be achieved by on-demand therapy, that is, 20 mg orally once a day when needed. 4. Combined with appropriate antibacterial therapy to eradicate Helicobacter pylori: Esomeprazole magnesium enteric-coated tablets 20 mg + amoxicillin 1 g + clarithromycin 500 mg, twice a day for 7 days.

The following adverse reactions have been identified or suspected in clinical trials of esomeprazole, none of which are dose-related. The following adverse reactions have been observed with the use of the racemate (omeprazole) and may also occur with the use of esomeprazole. 1. Central and peripheral nervous systems: paresthesia, somnolence, insomnia, vertigo. Reversible confusion, agitation, aggression, depression and hallucinations, mainly in patients with severe illness. 2. Endocrine: gynecomastia in men 3. Gastrointestinal: stomatitis and gastrointestinal candidiasis 4. Hematology: leukopenia, thrombocytopenia, agranulocytosis, pancytopenia. 5. Liver: encephalopathy (previous severe liver disease); jaundice or non-icteric hepatitis; liver failure 6. Musculoskeletal: arthralgia, myasthenia and myalgia. 7. Skin: rash, photosensitivity, erythema multiforme, Stevens-Johnson syndrome, toxic epithelial necrosis, alopecia. 8. Other: malaise. Allergic reactions, such as fever, bronchospasm, interstitial nephritis, hyperhidrosis, peripheral edema, blurred vision, dysnoea and hyponatremia.

This product is contraindicated in patients with known hypersensitivity to esomeprazole, other benzimidazole compounds, or any other ingredient of this product.

Precautions for children: Children should not use esomeprazole because there is no relevant clinical research data. Precautions for pregnancy and lactation: 1. There is no clinical data for the use of esomeprazole during pregnancy. Animal experiments have not shown that esomeprazole has direct or indirect harmful effects on embryonic or fetal development. Animal experiments with racemic mixtures have not shown direct or indirect harmful effects on pregnancy, delivery, or postnatal development. However, esomeprazole should be used with caution in pregnant women. 2. It is not clear whether esomeprazole is excreted in human milk. Esomeprazole has not been studied in lactating women, so esomeprazole magnesium enteric-coated tablets should not be used during lactation. Precautions for the elderly: No dosage adjustment is required for elderly patients.

1. Effect of esomeprazole on the pharmacokinetics of other drugs For drugs whose absorption process is affected by gastric acid, the absorption of these drugs may be increased or decreased during esomeprazole treatment due to the decrease in gastric acid. As with other acid secretion inhibitors or antacids, the absorption of ketoconazole and itraconazole will decrease during esomeprazole treatment. Esomeprazole inhibits CYP2C19, which is the main metabolizing enzyme of esomeprazole. Therefore, when esomeprazole is co-administered with drugs metabolized by CYP2C19 (such as diazepam, citalopram, imipramine, clomipramine, phenytoin, etc.), the plasma concentration of these drugs may be increased and the dose may need to be reduced. This should be considered especially when esomeprazole is used for on-demand treatment. The co-administration of 30 mg of esomeprazole can reduce the clearance of diazepam metabolized by CYP2C19 by 45%. The co-administration of 40 mg of esomeprazole can increase the trough concentration of plasma phenytoin in patients with epilepsy by 13%. Therefore, during phenytoin treatment, when esomeprazole is used in combination or discontinued, it is recommended to monitor the blood concentration of phenytoin. Clinical trials have shown that patients receiving warfarin treatment, combined with esomeprazole 40mg, coagulation time is within an acceptable range. However, after marketing, it has been reported that when the two are used together, individual cases have a clinically significant increase in the international normalized ratio (INR). Therefore, when starting to use or discontinue esomeprazole, it is recommended to monitor the blood concentration of warfarin. In healthy volunteers, the co-administration of esomeprazole 40mg can increase the area under the blood concentration-time curve (AUC) of cisapride by 32% and extend the elimination half-life (t1/2) by 31%, but does not significantly increase the plasma concentration of cisapride. The co-administration of esomeprazole does not aggravate the slight prolongation of the QTc interval caused by cisapride alone. (See [Precautions]). Studies have shown that esomeprazole 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. The combined use of esomeprazole and CYP3A4 inhibitor clarithromycin (500 mg twice daily) can double the area under the blood concentration-time curve (AUC) of esomeprazole, but the dose of esomeprazole does not need to be adjusted. 3. Incompatibility None

Seal and store below 30℃.

40mg (calculated as C17H19N3O3S)

36 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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