Nexium for sale
Development NEXIUM (esomeprazole) – a vivid example of the company “AstraZeneca, aimed at ensuring all patients with diseases of the digestive tract kislotozavisimymi best means of pharmacotherapy. Studies on the development of the drug lasted for more than 10 years, and the creation NEXIUM (esomeprazole) has confirmed the position of the company “AstraZeneca” as one of the world leaders in producing products for use in nexium side effects gastroenterology.
NEXIUM – the first proton pump inhibitor (PIT), which is a pure isomer, and all other IAS are a mixture of isomers (racemate).
In common nomenclature, a pair of optical isomers are designated as R (rectus – from the Latin. “Direct”, “R” denoting a clockwise rotation) and S (sinister – from the Latin. “L” denoting counterclockwise rotation). These designations refer to the location of chemical groups around the special atom in a molecule. NEXIUM – is S-stereoisomer of omeprazole. The important thing is that he is a new chemical entity and, thus, a new nexium generic pharmaceutically active substance.
Following oral administration NEXIUM absorbed in the small intestine and enters the systemic circulation, is transported to the action – the parietal cells of gastric mucosa, and by diffusion accumulates in the lumen of the secretory tubules. Here NEXIUM transformed into an active form – sulfenamid, so that it becomes possible to its binding to thiol groups of cysteine in the proton pump and inhibition of H + / K +-ATPase, which leads to blockage of generic nexium secretion of hydrochloric acid in the stomach.
The mechanism of action Nexium such as omeprazole and other IAS, but compared with them, it provides a more pronounced control of acid, as confirmed by its greater clinical efficacy (Thitiphuree S. et al., 2000).
Since NEXIUM – pure isomer, it has a better nexium coupons pharmacokinetic profile than omeprazole and other IAS (Andersson T. et al., 2000). NEXIUM distinctive feature is its higher bioavailability. Metabolism during the initial passage through the liver and NEXIUM, and other isomers (R-isomer) by two isoforms of hepatic enzyme cytochrome P450 – CYP2C19 and CYP3A4. It is important to note that the ratio metabolised by CYP2C19 NEXIUM significantly lower (73%) than the R-isomer (98%). In addition, clearance NEXIUM lower than that of omeprazole and R-isomer (Abelo A. et al., 2000; Horai Y. et al., 2001).
Pharmacokinetics NEXIUM less subject to individual variations in comparison with that of omeprazole. This is a side effects of nexium positive quality NEXIUM shows a decrease interindividual variability in the control of acid and, consequently, to increase the predictability and reliability of clinical pharmacotherapy with the use of the drug.
Thanks to the improved pharmacokinetics NEXIUM antisecretory effect is more pronounced, manifest faster and more stable compared with that of omeprazole (Rohss K. et al., 2000). Prove a more pronounced antisecretory effect NEXIUM compared with other IDU (omeprazole, pantoprazole, lansoprazole, rabeprazole) in patients with gastroesophageal reflux disease (GERD) (Rohss K. et al., 2001).
Results of clinical studies have shown high efficiency NEXIUM in the treatment of GERD. According to clinical trials, NEXIUM superior to omeprazole in the application as an initial treatment to eliminate acute erosive reflux esophagitis, the elimination of heartburn and other symptoms of GERD (Kahrilas PJ et al., 2000; Richter JE, et al., 2001). Similar results were obtained in the study of similar design when used as a comparison drug lansoprazole (Castell D. et al., 2001). Long-term maintenance treatment after successful initial therapy, including daily use NEXIUM in half the daily dose to prevent the recurrence of esophagitis was effective on these two clinical trials of similar design (Johnson DA et al., 2001; Vakil NB et al., 2001).
From the standpoint of improving tactics maintenance side effects of the drug nexium therapy of GERD, are critical results of a clinical study of the effectiveness NEXIUM with endoscopically negative GERD in application “on demand”. Symptomatic therapy NEXIUMOM “on demand” (half the usual daily dose – 20 mg every 3 days or less) provided a better quality of life compared with control patients who received placebo and had access to antacid medications (Talley NJ et al., 2000, 2001).
Thus, the use of NEXIUM “on demand” ensures an adequate long-term self-monitoring of symptoms and endoscopic negative GERD can be considered as an alternative to traditional continuous long-term acceptance IAS or intermittent use of H2-receptor blockers.
Eradication of H. pylori, treatment and prevention of recurrence of Helicobacter-associated peptic ulcer – a very topical and important issue of modern gastroenterology. In the eradication schemes, along with antimicrobial agents as basic drugs used IAS.
Of particular interest is the use of such schemes as a basic means Nexium. His performance in the 7-day schemes antihelikobakternoy therapy was studied in two randomized, double-blind studies, included 450 patients with peptic duodenal ulcer in the phase of remission or with relapsed disease (Tulassay Z., Kryszewski A., Ditc P., 2000). Patients assigned NEXIUM or omeprazole 40 mg / day and amoxicillin 2000 mg / day and clarithromycin 1000 mg / day for 7 days. Then, patients with relapse of peptic ulcers treated by the scheme with omeprazole, omeprazole monotherapy was carried out as early as within 3 weeks, and patients receiving NEXIUM, during the same time assigned to placebo. After 4 weeks after the cessation of any therapy of H. pylori eradication rate according to the breath test and histological examination was 86, and 88% in patients with recurrent peptic ulcer treated NEXIUM and omeprazole, and scarring of the ulcer occurred in 91 and 92% respectively. Patients with peptic ulcer in remission phase of H. pylori eradication rate was 89.7 and 87.8% respectively.
According UV Vasilyeva et al (2002), there is no need to continue antisecretory therapy after eradication triple therapy using NEXIUM in patients with peptic duodenal ulcer.
Thus, triple therapy using NEXIUM within 1 week contributes to eradicating H. pylori in peptic duodenal ulcer in 86-90% of cases and does not require further antisecretory therapy. Such effectiveness of therapy exceeds a threshold value (80%) eradication rate, which determines the possibility of using the scheme as first-line therapy antihelikobakternoy (Current European concepts in the management of Helicobacter pylori infection – The Maastricht Consensus Report Gut, 1997).
NEXIUM well tolerated and has an optimal safety profile. Side effects associated with its use are not common, usually mild and transient, do not depend on the dose.
The main advantages NEXIUM:
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NEXIUM helps to heal erosions in reflux esophagitis faster and more effectively than omeprazole;
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NEXIUM provides faster and more persistent the symptoms of GERD have a larger number of patients with reflux esophagitis than omeprazole;
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daily intake NEXIUM highly effective for preventing relapse of reflux esophagitis. Almost all patients achieved a stable remission, they are well tolerated in treatment;
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NEXIUM highly effective as initial therapy for treatment of GERD without esophagitis;
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efficiency NEXIUM opens up the possibility of a new approach to long-term symptomatic treatment of GERD patients without esophagitis. NEXIUM – the only IAS, which can be recommended for admission “on demand” to relieve recurrent symptoms;
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triple therapy using NEXIUM as a basic tool for 1 week ensures eradication of H. pylori infection and promotes healing of peptic ulcers of the duodenum without the need for follow antisecretory therapy.
