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Nexium Side Effects and Dosages

5/16/2016 12:07:56 PM
Nexium Side Effects and Dosages

Nexium history begins in 1979, when AstraZeneca company was synthesized omeprazole. Today, there are 5 generations of these drugs. Of particular interest today is esomeprazole developed by AstraZeneca and presented at the pharmaceutical market of United States the original drug Nexium. Its special and unique is that it is the first pure optical isomer among PPIs (S-stereoisomer of omeprazole); all the other members of this group are a mixture of S- and R-isomers (racemates). This achieves improved pharmacokinetic profile and significant increase in bioavailability of the drug that provides the best suppression of production of hydrochloric acid by the parietal cells of the stomach.

Nexium Dosages

When comparing the use of omeprazole and esomeprazole 20 mg for 5 days, it was found that the area under the curve "concentration-time" in the first case was 70% more. This is because the S-stereoisomer of omeprazole are less metabolized by the cytochrome in the liver and has a smaller clearance in comparison with R-isomer. This feature should be considered further because CYP2C19 gene polymorphism in the population significant enough that it does not allow to predict with great accuracy the effectiveness of PPI metabolized by this enzyme, and determines the presence of individuals that are resistant to these drugs. With the advent of Nexium was able to solve the problem.

Nexium Side Effects

In a study on the use of esomeprazole and 20 at a dose of 40 mg / day for 5 days in patients with gastro esophageal reflux disease (GERD), pH values higher than 4.0 for a longer time than with omeprazole therapy in a dose of 20 mg / d. On the 5th day the average daily pH value in the treatment of esomeprazole at both doses was also higher than when using omeprazole
Identical results were obtained when comparing the efficacy of esomeprazole 40 mg / day omeprazole 40 mg / day in patients with GERD. When using esomeprazole pH greater than 4.0 for a longer time than with omeprazole 40 mg. On the 5th day the pH was maintained above 4.0 for over 12 hours, respectively in 88 and 77% of patients treated with esomeprazole and omeprazole.
Effectiveness in lowering gastric acidity as compared with esomeprazole. The daily intake of esomeprazole 40 mg / day provides a better control of gastric acid secretion compared with lanzoprazol at a dose of 30 mg / day.
In a study of the use of esomeprazole and pantoprazole 40 mg / d in patients with GERD daily average pH was 4.7 vs. 3.7 (p <0.001), respectively. On the 5th day of intragastric pH value greater than 4.0 for 12 and 16 hours at 90 and 50% of the volunteers esomeprazole group and only in 30 and 10% of pantoprazole group.

Clinical efficacy of Nexium

Control of gastric acidity level
The efficacy of Nexium to control the increased secretion of hydrochloric acid was studied in an open multicenter study (duration 12 months), which includes patients with Zollinger-Ellison syndrome and idiopathic gastric hyperacidity. Initially used 40 mg esomeprazole dose 2 times a day, that is increased if necessary. Monitoring of gastric acidity was conducted on the 10th and 20th day, and at 3, 6 and 12 months after initiation of treatment. Fully was treated 21 patients, 17 of which received 6 months at an initial dose Nexium, y 3, it was increased to 80 mg two times a day and 1 - 80 mg three times a day. The effectiveness of this therapy (normalization of acidity) was 94% in group 1 and 100% - in the 2nd and 3rd. At 12 months, 16 patients received an initial dose Nexium, 4 - 80 mg 2 times a day and 1 - 80 mg three times a day. Efficacy in group 1 was 88%, and in the 2nd and 3rd - 100%. With respect to reducing gastric acidity, particular interest is a study that compared the efficacy of esomeprazole with PPI drugs of all generations. In patients with GERD used esomeprazole 40 mg / day, omeprazole 20 mg / day, lansoprazole 30 mg / day, pantoprazole 40 mg / d, and rabeprazole 20 mg / day for 5 days. Monitoring of gastric acidity in a 1 st and 5th day.
The results of these studies demonstrate the high efficiency of Nexium to control the level of stomach acidity.

GERD

In an 8-week, multicenter, randomized trial comparing the efficacy of Nexium 40 mg / day and omeprazole 20 mg / day for the treatment of GERD in 2425 patients with negative serological tests for H. pylori. (J. Richter et al., 2001). After 4 weeks from the start of treatment in the group of esomeprazole therapy efficacy was significantly higher compared to the group of omeprazole (81.7 and 68.7% respectively). After 8 weeks of treatment the number of these drugs Nexium healed patients in the group it was also higher.
Efficacy in treating GERD esomeprazole 40 mg daily dose as compared with lanzoprazol 30 mg / day (D. Castell et al., 2002). The test was conducted among 5241 patients with endoscopically proven erosive reflux esophagitis. It has been shown that the effectiveness of the treatment duration Nexium 4 and 8 weeks were higher as compared with lanzoprazol treatment over the same period [3].
In a study in the use of Nexium "on demand" mode, 6-month duration of the main task was to determine the effectiveness of preventive treatment for GERD maintenance using esomeprazole (N. Talley et al., 2002). Patients in an amount of 721 individuals with GERD endoscopically negative divided into 3 groups: esomeprazole 20 mg / day, 40 mg / day or placebo. At the same time patients could refuse the proposed treatment in the case of its ineffectiveness. Both doses of esomeprazole were significantly more effective compared with placebo. About 90% of patients completed the 6-month course of treatment Nexium Group, noting the positive dynamics and quality of life, while in the placebo group, discontinuation rates exceed 40%. Thus the majority of patients treated with Nexium, not indicated in the subsequent claims by the upper gastrointestinal tract.
In the two trials with similar designs and the task was to determine the effectiveness of preventive treatment for GERD maintenance using esomeprazole. High effectiveness was demonstrated in Nexium half the daily dose (20 mg) for the prevention of GERD recurrence after successful seed treatment conducted.
Based on the results of these studies, we can talk about high efficiency of Nexium, not only in the treatment of GERD, but also in the prevention of its recurrence. Symptomatic therapy Nexium "on demand" can serve as a more effective and safe alternative to the standard long receiving PPIs previous generations.

Helicobacter ulcer

The randomized multicenter trial compared the efficacy of omeprazole and Nexium in 374 patients with clinically active duodenal ulcer, an infectious nature which breath test has been confirmed. Patients received esomeprazole 20 mg 2 times a day, or omeprazole in the same dose and 1000 mg amoxicillin twice daily 2 and clarithromycin 500 mg 2 times a day for 1 week. In the group of omeprazole after 7 days of monotherapy with this drug continued for another 3 weeks, and patients receiving esomeprazole, administered a placebo for the same period. Endoscopic control of the state of the ulcer was carried out after 4 and 8 weeks after initiation of treatment. Thus ulcer healing rate was comparable in both groups and after 4 weeks reached 74 and 76%, and after 8 weeks - 87 and 88% in the first and second groups, respectively, indicating the high efficiency of Nexium Helicobacter in the treatment of peptic ulcer. The weekly rate of application of esomeprazole allowed to achieve results similar to 3-week course of treatment with omeprazole.
Efficacy of esomeprazole has been studied in two studies in the schemes Helicobacter therapy. The first study involved patients with acute exacerbation of peptic ulcer disease, and in the second - to remission. Treatment regimens were similar in this previous study. After 4 weeks after cessation of therapy frequency eradication of H. pylori in patients with exacerbation of peptic ulcer, Nexium treated for 7 days and omeprazole for 28 days, according to the breath test and histological examination was 86 and 88% respectively and the scarring of the ulcer was observed in 91 and 92% of cases. Patients with peptic ulcer remission in H. pylori eradication rate was 89.7 and 87.8% in the group of omeprazole and esomeprazole, respectively.

Conclusions

Esomeprazole (Nexium) - is the first proton pump inhibitor synthesized in the form of optical isomers. This feature of the drug makes it possible to eliminate the main disadvantage of IPP - considerable variability of metabolism. Esomeprazole (Nexium) in clinical studies, omeprazole was superior to other drugs STI Group for efficacy in the treatment of acid the main diseases of the upper gastrointestinal tract and thus well tolerated. The use of Nexium allowed to offer patients a new efficient scheme for the prevention of recurrence of GERD. All this makes Nexium drug of choice among PPIs.