Nexium, Esomeprazole An Overiew

Nexium [Esomeprazole] is a bis (5-methoxy-2-[(S)-[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]sulfinyl]-1H-benzimidazole-1-yl) magnesium trihydrate, developed and marketed by AstraZeneca This compound helps is in reducing or rather inhibits gastric acid secretion. Esomeprazole is the S-isomer of omeprazole, which is a mixture of the S- and R- isomers, meaning it is one of the two stereo-enantionmers in omeprazole. Esomeprazole was the third biggest selling pharmaceutical drug in the world for 2005, totaling US$ 5.7 billion in sales. Nexium [Esomeprazole] is a proton pump inhibitor that suppresses gastric acid secretion by specific inhibition of the Hydrogen/Potassium-ATPase in the parietal cells of the gastric mucosa. Nexium [Esomeprazole] is mainly indicated in acid-peptic disease [APD]/ gastro-esophageal reflux disease. [GERD] It is supplied as delayed-release capsules for oral administration or in packets for preparation of delayed-release oral suspensions. They are also available in the form of injections for intra-venous use. As with all proton pump inhibitors, which are acid labile, Nexium [Esomeprazole] should also be swallowed unbroken/crushed. Gastro-esophageal reflux disease: Commonly known as ‘heart burn’ which I am sure everybody must have suffered from it, at least once. When we eat food, the food passes down the esophagus and then into the stomach where it is broken down/digested by the acid present in the stomach known as gastric acid. The walls of the stomach, meaning the gastric mucosa is well equipped to handle this gastric acid. This acid cannot regurgitate into the esophagus normally, however, at times it does enter the esophagus where it breaks down the food if present. But, the esophageal mucosa is not programmed to handle the gastric acid and hence it causes an irritation which we term as heart burn or gastro-esophageal reflux disease. Now, if everyone suffers from heart burn then why do we need to prevent it? What harm is it going to cause? According to doctors, it is quite normal to get heart burn once a while, however if there is an increase in the number of episodes, specifically two times in a week in spite of taking medications or changing diet then this is a cause of concern. The main cause of concern is that over a period of time, this acid erodes the esophageal mucosa leading to a condition known as erosive gastritis. What prevents the acid from regurgitating into the esophagus? There is a sphincter between the esophagus and stomach known as the lower esophageal sphincter which prevents the regurgitation by acting as a valve. This vale is tightly shut and opens only when it has to pass food to the stomach. If this valve is not closed /shut properly then it will lead to regurgitation. Spicy food, fried food, obesity, smoking, alcohol wearing tight garments also aid in regurgitation Indications and dosage: Indications: - Gastro-esophageal reflux disease - Healing of erosive esophagitis - Maintenance of healed erosive esophagitis - Eradication of Helicobacter pylori in combination with appropriate antibacterial regimens - Pathological hypersecretory conditions like Zollinger-Ellison Syndrome Dosage: Adults: Erosive Esophagitis- healing: Nexium [Esomeprazole] 20mg to 40 mg once a day for 4 to 8 weeks is recommended in the healing of a diagnostically confirmed case of Esophagitis. In the event of patients not showing signs of full healing of the lesions, the regimen of Nexium [Esomeprazole] 20mg to 40 mg should be repeated for another 4 to 8 weeks. Maintenance of healed Erosive Esophagitis: Nexium [Esomeprazole] 20 mg daily is indicated in the maintenance of healed erosive esophagitis. This is to be followed for not more than 6 months since controlled studies did not extend beyond six months. Symptomatic GERD: - Nexium [Esomeprazole] 20 mg daily for 4 weeks is indicated for treatment of heartburn and other such symptoms associated with Gastro-esophageal reflux disease. If the symptoms do not resolve by 4 weeks then a repeat in the regimen is recommended by additional 4 weeks. Risk reduction of NSAID associated gastric ulcer: Nexium [Esomeprazole] 20mg to 40 mg daily for up to 6 months is recommended Helicobacter pylori Eradication to Reduce the Risk of Duodenal Ulcer Recurrence: Triple therapy of Nexium [Esomeprazole] along with amoxicillin and Clarithromycin is indicated in the treatment of patients with Helicobacter pylori infection and Duodenal ulcer disease [active or within past 5 years] - Nexium [Esomeprazole] 40 mg once daily for 10 days - Amoxicillin 1g twice daily for 10 days - Clarithromycin 500 mg twice daily for 10 days. Pathological hypersecretory conditions like Zollinger-Ellison Syndrome Nexium [Esomeprazole] is indicated as a long term drug for the treatment of some pathological hypersecretory conditions, like Zollinger-Ellison Syndrome. However, the dosages of Nexium [Esomeprazole] in patients with pathological hypersecretory conditions vary from patient to patient. Thus, the dosage regimens should be adjusted to individual patient needs. Pediatric: Age less than 11 years: - Short term treatment of symptomatic Gastro-esophageal reflux disease: 10mg once daily for up to 8 weeks. - Healing of erosive esophagitis: Weight less than 20 kg: 10 mg once daily for 8 weeks Weight more than 20 kg: 10 mg or 20 mg once daily for 8 weeks. Age between 12 to 17 years: - Short term treatment of symptomatic Gastro-esophageal reflux disease: 20mg or 40 mg once daily for up to 8 weeks. Safety and effectiveness of Nexium [Esomeprazole] for the treatment of symptomatic gastro-esophageal reflux disease in patients less than 1 year of age have not been established. Also, safety and effectiveness of Nexium [Esomeprazole] for pediatric uses other than that for the treatment of symptomatic gastro-esophageal reflux disease have not been established. Nexium [Esomeprazole] should be taken at least 1 hour before meals. I.V. Injection: Nexium [Esomeprazole] I.V. for Injection is indicated for the up to 10 day [short-term] treatment of Gastro-esophageal reflux disease in adult patients who have a history of erosive esophagitis as an alternative to oral therapy in patients when therapy with Nexium [Esomeprazole] Delayed-Release Capsules is not possible or appropriate. When oral therapy is possible or appropriate, intravenous therapy with Nexium [Esomeprazole] I.V. for Injection should be discontinued and the therapy should be continued orally. Contraindication: Hypersensitivity e.g. angioedema and anaphylactic reaction/shock Special precautions: - nursing mothers - pediatric patients - For patients with severe liver impairment [Child Pugh Class C], do not exceed the dose by more than 20 mg. - pregnancy - age more than 60 years Side Effects: - headache - diarrhea - abdominal pain - nausea - flatulence - dry mouth - constipation - increased: - creatinine, uric acid - increased or decreased hemoglobin, white blood cell count - increased bilirubin, alkaline phosphatase, ALT, AST - hypokalemia - hyponatremia - hyperkalemia - hypernatremia - Altered thyroid function tests. Drug Interactions: Nexium [Esomeprazole] may interfere with the absorption of drugs where gastric pH is an important determinant of bioavailability like: – ketoconazole, iron salts, digoxin. It may reduce the plasma levels of atazanavir. Nexium [Esomeprazole] should be used only for the conditions, dosages, and durations specified in the Prescribing Information or by your physician. Nexium information located at Genericsmed.com site References: - Drug Today, July-September 2005 Edition, pg 472 - Pharmacology and Pharmacotherapeutics, R.S.Satoskar, S.D.Bhandarkar, S.S.Ainapure, Revised 17th Edition, pg 604 - http://www.purplepill.com/index.aspx - http://www.nexium-us.com/ - http://en.wikipedia.org/wiki/Esomeprazole - http://www.rxlist.com/cgi/generic/esomeprazole_pi.htm - http://www1.astrazeneca-us.com/pi/Nexium.pdf

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