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        Esomeprazole sodium

        Anti-ulcer drug Pharmacokinetics Indications Drug Interactions Dosage Side effects Precautions Uses
        Esomeprazole sodium
        Esomeprazole sodium structure
        CAS No.
        161796-78-7
        Chemical Name:
        Esomeprazole sodium
        Synonyms
        Esomeprazole Na;EsoMeprazole sod;ESOMEPRAZOLE SODIUM;Esomeprazoleandsalts;(S)-OMeprazole sodiuM;(S)-Omeprazole Sodium Salt;Esomeprazole sodium impurity;Calcium Folinate Leucovorin Calcium;Sodium (S)-6-methoxy-2-(((4-methoxy-3,5-dimethylpyridin-2-yl)methyl)sulfinyl)benzo[d]imidazol-;5-Methoxy-2-((S)-((4-methoxy-3,5-dimethyl-2-pyridyl)methyl)sulfinyl-1H-benzimidazole sodium salt
        CBNumber:
        CB7123722
        Molecular Formula:
        C34H36MgN6O6S2
        Formula Weight:
        713.12
        MOL File:
        161796-78-7.mol

        Esomeprazole sodium Properties

        Melting point:
        156 °C (approx)

        Esomeprazole sodium Chemical Properties,Uses,Production

        Anti-ulcer drug

        Esomeprazole Sodium is the sodium salt form of esomeprazole. It is a commonly used anti-ulcer drug, which was first successfully developed by the Swedish company Astra Zeneca first. It belongs to a proton pump inhibitor. The proton pump inhibitor is the primary choice for treating peptic ulcer, gastro-oesophageal reflux disease and other acid-related diseases. Currently commonly clinically used PPI include five kinds: omeprazole, lansoprazole, rabeprazole, pantoprazole and esomeprazole. As the first PPI, the omeprazole’s drug efficacy in treating acid-related diseases has been widely recognized. Esomeprazole is the S-isomer of omeprazole, which can reduce gastric acid secretion by specific targeting mechanism. It is the specific inhibitor for the proton pump inhibitor in the parietal cell. Owing to the metabolic advantage of esomeprazole, it has a higher bioavailability and more consistent pharmacokinetics than its counterpart, omeprazole sodium, increasing the drug that reaches the proton pump. Its role of gastric acid control is much better than other proton pumps inhibitors such as lansoprazole, pantoprazole, and rabeprazole.
        In animal experiments, this product has a dose-dependent inhibition of the Na+/K+ ATP enzyme activity of the isolated rabbit parietal cells with an IC50 of 60 μmol/L. Its efficacy is greater than omeprazole (IC50: 100 μmol/L). Meanwhile, esomeprazole sodium can inhibit histamine-induced 14C aminopyrine accumulation in isolated human parietal cells. Its effect intensity is 2 times of omeprazole.
        Intravenous or intestinal injections of esomeprazole sodium to the experimental fistulization rats can inhibit gastric acid secretion caused by histamine with the ED50 were 0.24 and 0.43 mg/kg, respectively. For omeprazole with the same way of injection, the ED50 is 0.30 and 0.68 mg/kg, respectively.
        Using esomeprazole sodium in the gut of pylorus ligated rats enteral use esomeprazole sodium can reduce the basic amount of secreted gastric acid with potency three times larger than that of omeprazole. The drug can prevent and treat the stress or alcohol-induced gastric damage of experimental rats, also can prevent and treat the gastric lesions induced by acetic acid and indomethacin. Its ED50 values ??were 1.6 and 5.5 mg/kg, respectively. From the above results, the efficacy on ulcers of esomeprazole is greater than that of omeprazole.
        In addition, experimental data has also shown that when esomeprazole sodium is combined with penicillin and clarithromycin, it can be effectively applied for treating the duodenal and peptic ulcers caused by H. pylori infection.
        The above information is edited by the Chemicalbook of Dai Xiongfeng.

        Pharmacokinetics

        After intravenous injection of 5mg/kg 14C-labeled esomeprazole sodium into the SD rats, the half-life of the plasma concentration for female rats is 7.3 h, and 17.4 h for female rats. It can be rapidly absorbed through oral administration. Its plasma level exhibits bimodal peaks at 1h and 4h after taking drugs, respectively. The biliary drainage experiments of rats found that the absorption process after administration have a duration of 24 h or more. The order of concentration of drug in different organs is as below: liver> kidney> lung> blood> fat. For oral administration, the drug is mainly excreted through feces. The pharmacokinetics curve of esomeprazole is linear. When increasing the dose, the AUCs and cmax concurrently increase, while tmax, CL and half-life still keep constant.
        Esomeprazole sodium has a relative low toxicity. LD50 of rat through oral administration is greater than 5g/kg. For intraperitoneal administration, the LD50 is also over 2.5g/kg. Canine can take a dose 10mg/kg dose per day continuously for 28 d with no obvious abnormalities observed. For rats subjected to continuous medication for 13 weeks at a dose of 80 mg/kg, all the physiological parameters were not changed. The toxicity amount is over 320 mg/kg. In general pharmacological experiments, this product has a extremely small effect on the cardiovascular and autonomic nervous system. It only has a slight effect on the central nervous system at high dosage.

        Indications

        For the treatment of Gastroesophageal reflux disease (GERD)-erosive reflux esophagitis.
        Used for long-term maintenance therapy for cured esophagitis patients to prevent recurrence.
        Symptomatic control of gastroesophageal reflux disease (GERD).
        Heartburn and combined with other appropriate antimicrobial therapy for totally eradication of Helicobacter pylori-induced gastric and duodenal ulcers.

        Drug Interactions

        Esomeprazole sodium can reduce the absorption of ketoconazole and itraconazole. When combined with the product, we should reduce the dosages of drugs metabolized by the enzyme CYP2C19 such as diazepam, citalopram, imipramine, clomipramine and phenytoin. When combined with the product or stop using this product, we should also monitor the plasma concentrations of phenytoin.
        No interaction between the product and the amoxicillin, quinidine or warfarin was observed. No need for dose adjustment when combined with clarithromycin.
        There is not too much clinical information of excess taking drug. But a single dose of 80 mg of this product has no adverse reactions. This product has no special antidote.

        Dosage

        This product should be swallowed with water, and cannot be taken after chewing or crushing.
        Adults: For treatment of erosive reflux esophagitis: 40mg per day. Continuously take for 4 to 8 weeks. For long-term maintenance therapy and prevention of relapse for cured esophagitis patients, the recommended dosage is 20mg per day. For symptomatic CORD without suffering from esophagitis: 20mg per day. Take it for 4 weeks (If fail to control the symptoms, the patient should subject to further observation). Once symptoms have been got controlled, then the can use the dosage as needed for controlling the future symptom, such as 20 mg per day. For the triple associated therapy used for Helicobacter pylori eradication, prevention and cure of duodenal ulcer caused by Helicobacter pylori, and also Helicobacter pylori-induced recurrence of peptic ulcer: 20mg, amoxicillin 1g and clarithromycin 500mg, 2 times a day, medication for 7d.
        For elderly patients or patients of mild or moderate hepatic impairment, there is no need for dosage adjustment. It should be concerned that the maximal dosage should not exceed 20 mg for patients with severely impaired liver function.
        Children and lactating women are not recommended for taking this drug.

        Side effects

        Common adverse reactions (incidence of 1% to 10%) include headache, abdominal pain, diarrhea, gastrointestinal disorders, flatulence, nausea and vomiting, and constipation. Other adverse reactions (incidence of 0.1% to 1%) include dermatitis, itching, hives, dizziness, and dry mouth.

        Precautions

        Patients who are allergic to Benzimidazole-class drug are not allowed to use esomeprazole sodium. Patients of rare hereditary fructose intolerance, glucose-galactose absorption dysfunction, sucrase-isomaltase deficiency, and also lactation women are not allowed to use this drug.
        Patients who have severe impaired liver or renal function, long-term treatment, malignant warning before using, and pregnant women should use with caution. When any warning symptoms (such as significant weight loss, recurrent vomiting, dysphagia, vomiting blood or black stools) happens, patients should be checked to exclude the possibility of malignant disorders (such as cancer) due to that treatment can worsen the symptoms and delay diagnosis. Long-term user should be regularly monitored.

        Uses

        Treatment of peptic ulcer, gastroesophageal reflux disease and other acid-related diseases.

        Chemical Properties

        Beige Solid

        Uses

        (S)-Omeprazole is the (S)-enantiomer of Omeprazole (O635000) a gastric proton-pump inhibitor. (S)-Omeprazole is more potent that its (R)-enantiomer and is used in the treatment of gastroesophageal ref lux disease as well as gastrointestinal ulcers associated with Crohn's disease.

        brand name

        Nexium (AstraZeneca).

        Esomeprazole sodium Preparation Products And Raw materials

        Raw materials

        Preparation Products


        Esomeprazole sodium Suppliers

        Global( 278)Suppliers
        Supplier Tel Fax Email Country ProdList Advantage
        Shanghai Kaisai Chemical Co., Ltd 021-33516711 , 33516722
        021-33516776 kaisaichem@163.com China 5956 58
        Qufu Haida Tiancheng Biochemical Co., Ltd. 0537-4531868-
        qfhdtc@126.com China 36 55
        Jiangsu Zhongbang Pharmaceutical Co., Ltd 025-87151129
        0086-25- 87151120 sales@chinaredsun.com China 142 58
        Jinan Chenghui-shuangda Chemical Co.,Ltd. 0531-58897066 58897051 58897055 58897087 58897086
        0531-58897093 shenyun@jnchsd.com China 78 62
        Hainan Manfangyuan Pharmaceutical Chemical Co., Ltd. +86 (898) 6651-8050
        +86 (898) 6677-5768 mfy001@hnmfy.com China 85 60
        Hefei Topway Biotechnology Co.,Ltd 0086-551-65326752 14755135869
        0086-551-65326751 sales@ahtopway.com China 76 60
        SiChuang NanBu Honesty Technology Co., Ltd. 0838-5675166
        0838-5675535 nbcxkj@126.com China 695 55
        J & K SCIENTIFIC LTD. 010-82848833- ;010-82848833-
        86-10-82849933 jkinfo@jkchemical.com;market6@jkchemical.com China 96505 76
        Chembest Research Laboratories Limited 021-20908456-
        021-58180499 sales@BioChemBest.com China 5984 61
        BeiJing Hwrk Chemicals Limted 21-51691807-
        021-55236763 peter.shi@hwrkchemical.com; China 14684 55

        View Lastest Price from Esomeprazole sodium manufacturers

        Image Release date Product Price Min. Order Purity Supply Ability Manufacturer
        2019-12-27 Esomeprazole sodium
        161796-78-7
        US $0.00-0.00 / KG 100g 99%+ 5000 KG Shaanxi Dideu Medichem Co. Ltd
        2018-07-27 Esomeprazole?sodium
        161796-78-7
        US $20.00 / KG 1KG 99.90% 20kg career henan chemical co

        161796-78-7(Esomeprazole sodium)Related Search:


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