Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0038358 (gastric ulcer)
 5,179 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Rabeprazole, a new proton pump inhibitor, was studied in patients with acid-peptic-related diseases (duodenal ulcer, gastric ulcer, GERD) in three placebo-controlled, double-blind, randomized clinical trials. Men and women over the age of 18 were enrolled if the presence of an active duodenal or gastric ulcer or erosive or ulcerative esophagitis was confirmed on upper gastrointestinal endoscopy. Patients were randomly allocated to either placebo or rabeprazole 20 mg or 40 mg in the duodenal and gastric ulcer protocols or to placebo or rabeprazole 10 mg, 20 mg, or 40 mg in the GERD protocol. All doses of rabeprazole in all three studies were statistically significantly superior to placebo in healing acid-related lesions. There were no treatment differences between the rabeprazole doses in healing active peptic lesions. The incidence of positive [13C]urea breath test for H. pylori was 53% in patients with duodenal or gastric ulcers. H. pylori status was not effected by treatment with rabeprazole.
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PMID:Rabeprazole in treatment of acid peptic diseases: results of three placebo-controlled dose-response clinical trials in duodenal ulcer, gastric ulcer, and gastroesophageal reflux disease (GERD). The Rabeprazole Study Group. 959 Apr 13

Rabeprazole is an inhibitor of the gastric proton pump. It causes dose-dependent inhibition of acid secretion and has a more rapid onset of action than omeprazole. Duodenal ulcers healed faster after treatment with rabeprazole 20 or 40 mg/day than placebo or ranitidine 150 mg 4 times daily and at a generally similar rate to omeprazole 20 mg/day in patients with duodenal ulcers; rabeprazole was similar or superior to these agents in relieving symptoms. Rabeprazole 20 and 40 mg/day healed gastric ulcers faster than placebo, and rabeprazole 20 mg/day healed ulcers at a similar healing rate, to omeprazole 20 mg/day in well controlled 6-week studies. Gastric ulcer symptom relief with rabeprazole was similar or superior to that provided by omeprazole or placebo. In 8-week studies in patients with gastro-oesophageal reflux disease (GERD), rabeprazole 10, 20 and 40 mg/day were more effective than placebo, rabeprazole 20 mg/day was more effective than ranitidine 150 mg twice daily, and rabeprazole 20 mg/day was similar in efficacy to omeprazole 20 mg/day. Symptom relief with rabeprazole in 8-week trials in patients with GERD was superior to that provided by placebo, and similar to ranitidine or omeprazole. Rabeprazole was similar to omeprazole and superior to placebo in both maintenance of healing and prevention of symptoms in patients with healed GERD in 1-year studies. One-week triple therapy with rabeprazole 20 mg twice daily plus 2 antibacterial agents achieved > or = 90% Helicobacter pylori eradication, but, as would be expected, a regimen of rabeprazole 20 mg twice daily plus 1 antibacterial agent was less successful. The drug was as effective as omeprazole and lansoprazole as part of triple therapy for H. pylori eradication. Rabeprazole successfully reduced acid output to target levels and prevented further pathological changes in 10 patients with Zollinger-Ellison syndrome. Usual dosages of rabeprazole are 20 mg/day for 4 weeks to treat duodenal ulcers, 6 weeks for gastric ulcers and 8 weeks for GERD, although some patients with duodenal ulcer may respond to a 10 mg/day dosage. For long term maintenance of GERD healing, 10 or 20 mg daily doses are adequate. Patients with hypersecretory states may need individualised dosages starting at 60 mg/day. The drug was well tolerated in clinical trials, with headache, rash, infection, diarrhoea and flu syndrome as the most common adverse events. In conclusion, rabeprazole appears to be a well tolerated proton pump inhibitor with a rapid onset of action and a low potential for drug interactions. The drug may be used to achieve healing and the relief of symptoms of duodenal ulcer, gastric ulcer and GERD, maintain GERD healing, and can form part of effective regimens to eradicate H. pylori.
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PMID:Rabeprazole: a review of its use in acid-related gastrointestinal disorders. 1055 40

Acid-related diseases such as gastro-oesophageal reflux disease (GORD) and peptic ulcer are a common cause of morbidity and if inadequately treated can lead to serious complications. The proton-pump inhibitor rabeprazole has been extensively evaluated in well-controlled trials in North America and Europe for the acute treatment of erosive or ulcerative GORD and gastric and duodenal ulcers and for the long-term maintenance of GORD healing. The results show that rabeprazole has a favourable benefit/risk profile for each indication. Rabeprazole 10 and 20 mg given once daily in the morning was highly effective in producing and maintaining healing, providing symptom relief, and improving overall well-being. Healing rates for rabeprazole were equivalent to omeprazole in all indications, and superior (GORD healing and duodenal ulcer healing) or equivalent (gastric ulcer healing) to the histamine 2-receptor antagonist ranitidine. Symptom relief provided by rabeprazole was equivalent or superior to comparator drugs. Rabeprazole was well tolerated in both short- and long-term studies. The incidence of treatment-emergent signs and symptoms related to rabeprazole was low, and these were generally mild or moderate in severity. The overall rate of discontinuations due to adverse events was approximately 3%. There were no deaths related to rabeprazole therapy. These findings indicate a favourable benefit/risk profile for each intended use.
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PMID:The benefit/risk profile of rabeprazole, a new proton-pump inhibitor. 1092 9

Proton-pump inhibitors (PPIs) have revolutionized the treatment of gastroesophageal reflux disease (GERD) and peptic ulcer. To evaluate the efficacy of the new PPI rabeprazole, 12 controlled clinical trials were conducted worldwide-three for each indication (erosive or ulcerative GERD healing, long-term GERD healing maintenance, duodenal ulcer healing, and gastric ulcer healing). Rabeprazole was compared to placebo, the H2-receptor antagonist ranitidine, and the PPI omeprazole. Treatment duration ranged from < or =4 weeks for duodenal ulcer to < or =6 weeks for gastric ulcer, < or =8 weeks for GERD healing, and 1 year for maintenance of GERD healing. Rabeprazole was as effective as omeprazole for each indication and significantly more effective than ranitidine for healing of GERD (87% vs 66%) and duodenal ulcer (83% vs 73%). Rabeprazole was also superior to ranitidine in providing symptom relief, particularly in GERD.
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PMID:Efficacy of rabeprazole once daily for acid-related disorders. 1131 37

Acid-related disorders are caused by an imbalance between acid secretion by the gastric parietal cells and the defensive mechanisms of the gastrointestinal tract to protect against the effects of acid. Therapy for acid-related disorders focuses on the control of acidity. Data collected throughout the last decade have demonstrated that PPIs are the most effective therapy for acid-related disorders: PPIs have proven superior to H2RAs and antacids in numerous studies. Five PPIs are currently available in the United States. While all PPIs exert their effect through the same basic mechanism of action, they do not have the same pharmacologic and clinical properties. All PPIs are effective in healing and maintenance of gastric and duodenal ulcers and GERD. The PPIs differ, however, in their ability to control symptoms rapidly and consistently. Due to its more rapid rate of activation, rabeprazole results in a faster onset of action and faster symptom control than other PPIs. Studies comparing rabeprazole to omeprazole found statistically significant differences in the rapidity of symptom relief in patients with gastric ulcer, duodenal ulcer, and GERD. Rapid symptom relief is important to the majority of patients, as their symptoms have an impact on their quality of life. Rapid symptom relief is also important in an environment where patients self-medicate on demand, depending on daily symptoms. Rabeprazole has also been shown to have a more consistent suppression of acid, including at night. Optimizing therapy with PPIs necessitates consideration not only of healing rates of the different available treatments but also of the rapidity and consistency of acid suppression that translate clinically into symptom relief.
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PMID:Optimizing acid-suppression therapy. 1172 43

Symptom relief is one of the key goals in the management of gastric acid-related disorders such as gastro-oesophageal reflux disease (GERD), including nonerosive reflux disease (NERD), and duodenal and gastric ulcer. Whereas heartburn and regurgitation are classic symptoms of GERD, duodenal and gastric ulcers are associated with epigastric pain. The relationship between gastric acid and the presence of symptoms correlates well in GERD and duodenal ulcer, but not in gastric ulcer and NERD. Nevertheless, in all these disorders, gastric acid is considered a key pathogenic element, and acid suppression remains central to therapy. With their profound, prolonged effect on acid inhibition, proton pump inhibitors are considered the first-choice therapy for these disorders. Rabeprazole is a newer generation proton pump inhibitor that suppresses the gastric proton pump and acid secretion more rapidly than does omeprazole, lansoprazole or pantoprazole. In clinical trial settings, rabeprazole provided fast and sustained symptom relief, which can help ensure patient acceptance of therapy and aid in patient compliance.
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PMID:Review article: relief of symptoms in gastric acid-related diseases--correlation with acid suppression in rabeprazole treatment. 1549 15

Control of gastric acid secretion by antisecretory agents has been the cornerstone of therapy in the successful management of all acid-related disorders, including gastro-oesophageal reflux disease (GERD), and duodenal and gastric ulcer. Treatment efficacy has been strongly correlated with degree and duration of acid suppression within the 24-h period and with total duration of therapy. All proton pump inhibitors are highly effective for the healing of ulcers and erosive oesophagitis. All have closely similar mechanisms of action, yet important pharmacological differences exist, which can significantly impact certain aspects of their clinical efficacy. Rabeprazole's rapid activation over a wide pH range may be the explanation for its early onset of effective acid inhibition compared with other proton pump inhibitors such as omeprazole, lansoprazole and pantoprazole. Like rabeprazole, esomeprazole is also a potent inhibitor of gastric acid at steady state, although it is thought that rabeprazole may provide enhanced first-day acid suppression compared with esomeprazole. First-day antisecretory efficacy should produce faster symptom relief, a hypothesis supported by clinical data. Moreover, drugs with pharmacological profiles that include both rapid onset and potent antisecretory effects should help control healthcare costs by reducing the need for otherwise commonly used twice-daily proton pump inhibitor administration.
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PMID:Review article: pH, healing and symptom relief with rabeprazole treatment in acid-related disorders. 1549 16

Rabeprazole is among the most potent proton pump inhibitors (PPI) identified to date and it has been demonstrated that it is effective in such diseases as gastroesophageal reflux disease (GERD), duodenal ulcer and gastric ulcer. There is currently interest in developing a new formulation: rabeprazole sterile powder for injection (RSPI). This investigation was conducted to evaluate the preclinical pharmacokinetics of RSPI in rats and at the same time a comparative study was carried out in dogs between RSPI and Pariet tablets using liquid chromatographic-mass spectrometry analysis. The liquid chromatographic-mass spectrometry method was first conducted and validated as being specific, and having accuracy, precision, sensitivity and a satisfactory recovery. After intravenous administration of RSPI (i.v.: 2, 6 and 18 mg/kg) to rats, no significant dose-dependency was found in the CL (4.20-5.72 l/h/kg), V(area) (d) (0.94-1.32 l/kg), dose-normalized AUC (197.20-245.82 microg/l*h based on 1 mg/kg) and t(1/2) (p>0.05). In the dog, a randomized, open-label, crossover experiment was carried out to show that the mean area under the plasma concentration-time curve (AUC(0-infinity)) after i.v. administration of RSPI was at least four times larger than that following oral administration of Pariet tablet at an equivalent dose but the elimination half-life of these two formulation was similar (p>0.05). The results showed that the pharmacokinetics of RSPI was linear (r(2) = 0.98) in the dose range 2-18 mg/kg and the RSPI had a much higher AUC(0-infinity) and similar t(1/2) values compared with the enteric-coated tablet.
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PMID:Liquid chromatographic-mass spectrometry analysis and pharmacokinetic studies of a novel rabeprazole formulation, sterile powder for injection, in dogs and rats. 1737 59

Rabeprazole is a proton pump inhibitor that can be used in the treatment of acid-peptic-related disorders (gastroesophageal reflux disease [GERD], duodenal ulcer, gastric ulcer, gastric acid hypersecretory syndromes) and Helicobacter pylori. Pharmacodynamic data has demonstrated that rabeprazole, with a high pKa of approximately 5.0, can be activated at a higher pH than other proton pump inhibitors. This possibly results in faster onset of action. Owing to its non-enzymatic pathway of metabolism, rabeprazole is also less influenced by genetic polymorphisms of the CYP2C19, which others proton pump inhibitors are dependent on. In a 2-week, placebo-controlled trial, rabeprazole was both rapid and effective in relieving heartburn on day 1 of therapy and improved other GERD-related symptoms including regurgitation, belching, bloating, early satiety and nausea. For oesophageal reflux disease without erosions both 10 and 20 mg of rabeprazole are equivalent and better than placebo at 2 and 4 weeks. An on-demand approach to non-erosive reflux disease with 10 mg of rabeprazole has also been documented as superior to placebo. Some success in the treatment of extra-oesophageal manifestations of GERD, such as asthma and chronic laryngitis, has also been achieved with rabeprazole. Overall, rabeprazole with very few side effects is a safe and efficacious medication for acid suppression therapy.
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PMID:Rabeprazole: a pharmacologic and clinical review for acid-related disorders. 1923 23