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)

We tested the hypothesis that the gastric H+/K+ adenosine triphosphatase inhibitor, omeprazole, because of its different mode of action and pronounced inhibitory effect on gastric acid secretion, may be more effective in peptic ulcer that is refractory to histamine H2 receptor antagonist treatment than continuing the same therapy. Altogether 107 patients (duodenal ulcer, n = 88; prepyloric ulcer, n = 14; gastric ulcer, n = 3; mixed sites, n = 2) with refractory peptic ulcer - that is ulcer unhealed after at least two months' treatment with cimetidine 0.8 g or 1 g daily or with ranitidine 0.3 g daily - were randomly allocated to receive either omeprazole 40 mg daily (n = 54) or to continue treatment with the same H2 receptor antagonist and at the same dose (n = 53) for up to eight weeks. The patients in the two treatment groups were well matched demographically. Healing by 'intent to treat' analysis was as follows: at four weeks, omeprazole 46 of 54 (85%), H2 receptor antagonist 18 of 53 (34%) (p less than 0.0001); and at eight weeks, 52 of 54 (96%) and 30 of 53 (57%) respectively (p less than 0.0001). One patient was lost to follow up but of the 22 patients whose ulcers were shown to be unhealed at endoscopy after receiving continued H2 receptor antagonist treatment, 21 healed in four to eight weeks when changed to omeprazole. Daytime epigastric pain cleared at four weeks in 43 of 47 (91%) patients on omeprazole and in 32 of 46 (70%) on H2 receptor antagonists (p=0.01) and relief of all dyspeptic symptoms occurred in 39 of 47 (83%) and 23 of 45 (51%) (p=0.0009) patients respectively. Adverse events occurred in 11 of 54 (20%) patients on omeprazole and in 12 of 35 (34%) on cimetidine but in none on ranitidine. The events were mild and none required treatment withdrawal. The commonest event in patients on omeprazole was loose stools or diarrhoea (n=5). Omeprazole was significantly better than continued H2 receptor antagonist treatment for the short term management of refractory peptic ulcer as judged by healing rate and pain relief, and it was safe.
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PMID:Treatment of refractory peptic ulcer with omeprazole or continued H2 receptor antagonists: a controlled clinical trial. 162 76

Omeprazole is the first of a new class of gastric antisecretory drugs, proton pump inhibitors. It inhibits the H+,K(+)-adenosinetriphosphatase enzyme of the gastric parietal cell, resulting in potent, long-lasting suppression of basal and stimulated acid secretion. The drug is currently approved for treatment of gastroesophageal reflux disease and Zollinger-Ellison syndrome. In clinical trials, treatment with omeprazole results in rapid healing of duodenal ulcers; it is also effective in treating gastric ulcer disease. It is uniformly well tolerated without significant adverse effects, although animal studies linked profound long-term suppression of gastric acid secretion with the development of gastric carcinoids. Potential future uses include the prophylaxis of ulceration secondary to stress or use of nonsteroidal anti-inflammatory drugs, and the prophylaxis of recurrent peptic ulcer disease.
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PMID:Omeprazole: a new drug for the treatment of acid-peptic diseases. 193 56

Since their introduction in 1976, and until recently, the H2-receptor antagonists have been the 'state-of-the-art' gastric acid inhibitors, but the advent of omeprazole, the acid pump inhibitor, has necessitated a reassessment of therapy for acid-related diseases. In making this reassessment, the following therapeutic goals should be considered: rapid and reliable therapeutic effect, safety, simple treatment regimen, resolution of recurrence, and cost-effectiveness. Extensive clinical evidence indicates that omeprazole offers an advance over the H2-receptor antagonists in achieving these goals. A series of meta-analyses shows that omeprazole gives more rapid symptom relief and more reliable healing than H2-receptor antagonist, ranitidine, in uncomplicated duodenal ulcer (DU), in uncomplicated gastric ulcer (GU) and in reflux oesophagitis (RO). By contrast with the H2-receptor antagonists, refractoriness leading to failure to heal is virtually unknown with omeprazole. Omeprazole also fulfils the goal of therapeutic safety, and this has been documented in extensive short- and long-term clinical and laboratory studies. Omeprazole has a simple treatment regimen: 20 mg once daily is recommended in the routine treatment of DU, GU and RO. As a result of its high therapeutic success rate, omeprazole is also cost-effective. Taking all these factors into account, it is concluded that omeprazole approaches the therapeutic targets set for the treatment of acid-related disorders.
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PMID:Treatment of acid-related disorders with gastric acid inhibitors: the state of the art. 198 62

Omeprazole is a specific inhibitor of H+,K(+)-ATPase or 'proton pump' in parietal cells. This enzyme is responsible for the final step in the process of acid secretion; omeprazole blocks acid secretion in response to all stimuli. Single doses produce dose-dependent inhibition with increasing effect over the first few days, reaching a maximum after about 5 days. Doses of omeprazole 20mg daily or greater are able to virtually abolish intragastric acidity in most individuals, although lower doses have a much more variable effect. Omeprazole causes a dose-dependent increase in gastrin levels. Omeprazole must be protected from intragastric acid when given orally, and is therefore administered as encapsulated enteric-coated granules. Absorption can be erratic but is generally rapid, and initially the drug is widely distributed. It is highly protein-bound and extensively metabolised. Its elimination half-life is about 1h but its pharmacological effect lasts much longer, since it is preferentially concentrated in parietal cells where it forms a covalent linkage with H+,K(+)-ATPase, which it irreversibly inhibits. Omeprazole binds to hepatic cytochrome P450 and inhibits oxidative metabolism of some drugs, the most important being phenytoin. Omeprazole has produced short term healing rates superior to the histamine H2-receptor antagonists in duodenal ulcer, gastric ulcer and reflux oesophagitis. It has also been shown to be highly effective in healing ulcers which have failed to respond to H2-receptor antagonists, and has been extremely valuable in treating patients with Zollinger-Ellison syndrome.
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PMID:Clinical pharmacology of omeprazole. 202 1

Omeprazole has been shown to provide more rapid symptom relief and to heal ulcers more quickly and reliably than H2-receptor antagonists in duodenal ulcer, gastric ulcer and reflux oesophagitis. In addition, omeprazole is well tolerated and has a good safety profile. Among the areas for clinical development with omeprazole are the maintenance treatment of duodenal ulcer, treatment of non-steroidal anti-inflammatory drugs (NSAID)-induced gastro-duodenal lesions, maintenance treatment of reflux oesophagitis and the treatment of bleeding ulcer. Two studies of patients with duodenal ulcer have shown that maintenance treatment with omeprazole, 10 mg once daily, was as effective as, or superior to, treatment with omeprazole, 20 mg given on Friday, Saturday and Sunday only, and markedly superior to placebo. In patients with gastric ulcer which developed during treatment with NSAIDs omeprazole, 20 mg once daily, resulted in a higher healing rate than ranitidine, 150 mg b.i.d., both at 4 and at 8 weeks. Reflux oesophagitis is often a persistent condition requiring continuous maintenance treatment. In a recent multicentre trial, a substantially higher proportion of patients remained in remission with omeprazole, 20 mg once daily, than with ranitidine, 150 mg b.i.d. Studies comparing omeprazole and ranitidine (administered intravenously) in patients with bleeding peptic ulcers have also demonstrated the superiority of omeprazole with regard to the control of bleeding and the avoidance of surgery. Further studies are currently underway in this and other related areas.
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PMID:Clinical development programme for omeprazole. 209 16

After pharmacological studies showed that omeprazole had a marked and longlasting inhibitory effect on acid secretion, many clinical studies commenced. In duodenal ulcer, omeprazole in doses of 20-40 mg/day has been shown to give significantly higher healing rates than ranitidine or cimetidine. Omeprazole has given healing rates of 58-83% after treatment for 2 weeks and 84-100% after 4 weeks. A more pronounced effect on the relief of ulcer symptoms has also been observed. Similarly, in gastric ulcer several studies have been performed, all of which have shown higher healing rates with omeprazole both at 4 and 8 weeks. Symptom relief has also been faster and more pronounced with omeprazole. In patients with reflux oesophagitis, omeprazole has been shown to decrease the time with an acid milieu in the oesophagus. In several studies omeprazole in doses of 20-60 mg/day has consistently given healing rates approximately twice those of ranitidine in doses of 150 mg twice daily at 4 and 8 weeks. In addition, there has been a rapid improvement in the symptoms of oesophagitis. Omeprazole has been found to be very effective in the Zollinger-Ellison syndrome, with a prompt effect on acid secretion and symptoms. The accumulated experience exceeds 300 patients. More than 13,000 patients have taken part in the clinical investigations with omeprazole. Neither serious side-effects nor other side-effects which could be ascribed to treatment have been observed. There have not been any clinically significant changes in laboratory variables apart from those which are caused by the decrease in acid secretion.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:Clinical experience with omeprazole: assessment of efficacy and safety. 249 59

More than 13,000 individuals with duodenal ulcer, gastric ulcer or reflux oesophagitis have now taken part in controlled clinical studies with omeprazole. In duodenal ulcer, treatment with omeprazole, 20 mg daily or more, has resulted in healing rates of 58%-83% after 2 weeks and 84%-100% after 4 weeks. In all of these studies, healing rates with omeprazole have been higher than with either ranitidine or cimetidine. Omeprazole has also had a more pronounced effect on ulcer symptoms. Although the first comparative study on gastric ulcer showed only marginally higher healing rates with omeprazole than with an H2-receptor antagonist, later studies have all shown significantly higher healing rates with omeprazole. Healing rates of the order of 70% or more have been achieved within 4 weeks, rising to over 88% after 8 weeks. Symptom relief has also been faster with omeprazole. In both duodenal ulcer and gastric ulcer, almost every patient can be healed, including those resistant to treatment with H2-receptor antagonists. The influence of omeprazole on the healing of reflux oesophagitis has been investigated in several studies comparing omeprazole with ranitidine. Healing rates have been markedly higher with omeprazole in all studies. These unprecedentedly high healing rates (81%-96% at 8 weeks) have also been accompanied by rapid symptom relief. In clinical studies with omeprazole, no clinically significant side-effects which could be ascribed to treatment, nor indeed any serious side-effects, have been observed, neither have any clinically significant changes in laboratory variables been seen. Furthermore, no pathological changes of the gastric mucosa have been detected after long-term treatment with omeprazole.
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PMID:The clinical utility and safety of omeprazole. 257 8

Twenty-seven patients with peptic ulcer (19 with duodenal ulcer (DU) and eight with gastric ulcer (GU] refractory to H2-antagonists were treated with 40 mg of omeprazole once daily for 4-8 weeks, depending on the rate of ulcer healing. Clinical assessment, endoscopy and laboratory tests were performed at entry, after 2 and after 4 weeks, and if unhealed, also after 8 weeks' treatment. Ten healed patients were given a maintenance therapy of omeprazole 20 mg daily for up to 12 months during which the patients returned for endoscopy, gastric biopsy and laboratory tests at 3-monthly intervals. The initial treatment healed 15 of 19 (79%) DU patients in 2 weeks and all DU patients by 4 weeks. Seven of eight (87%) GU patients healed in 4 weeks and only one required 8 weeks' treatment. Symptom relief was rapid, with most patients being symptom-free within the first day of treatment. Six patients received 12 months' continuous maintenance therapy, one patient 9 months and three patients 6 months' treatment. All patients remained in remission whilst on omeprazole therapy. No adverse events were reported throughout the study. There were no clinically significant changes in haematology or blood chemistry after healing or during the long-term treatment. Biopsy samples revealed no histological changes in the gastric mucosa at any stage. Omeprazole 40 mg therefore was found to produce rapid healing and symptom relief in Asian patients with H2-antagonist-resistant peptic ulcers. Maintenance therapy with omeprazole 20 mg daily was shown to be safe and effective in preventing recurrence of peptic ulceration.
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PMID:Omeprazole in acute and long-term treatment of Asian patients with peptic ulcer refractory to H2-antagonists. 257 78

Basal and pentagastrin stimulated gastric acid secretions were measured in 20 patients with duodenal ulcer before and after one week of treatment with oral omeprazole 20 mg daily. Omeprazole markedly inhibited gastric acid secretion in all the patients. The mean basal intragastric pH rose from 1.6 to 6.3, and the BAO and MAO were reduced by 86.9% and 83.9% respectively on day 7 of the study. We also conducted a clinical trial in 63 duodenal and 12 gastric ulcer patients. Each patient received 20 mg omeprazole. 98% of the patients were free of pain within first week of the treatment. After 2, 4 and 6 weeks of treatment, the healing rates of duodenal ulcer were 81.3%, 96.8% and 100% respectively, and those of gastric ulcer were 50%, 91.7% and 100% respectively. The drug was well tolerated and no side effect was observed.
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PMID:[Omeprazole in peptic ulceration: acid inhibition and endoscopic healing]. 263 88

Omeprazole inhibits H+,K+-ATPase, the enzyme responsible for the exchange of H+ and K+ in the final step in the acid secretory process within the parietal cell. It has been shown to produce a marked and long-lasting inhibition of acid secretion with a decrease in 24-hour intragastric acidity after repeated daily dosing. Omeprazole has been shown to give significantly higher healing rates than ranitidine or cimetidine in patients with duodenal ulcer and gastric ulcer. Similarly, a more pronounced effect on ulcer symptoms has been observed. In patients with reflux esophagitis, omeprazole has been shown to decrease the time with an acid milieu in the esophagus. Omeprazole has consistently given about twice as high healing rates and faster decrease in symptoms than with ranitidine. In patients with Zollinger-Ellison syndrome, omeprazole has been found to have a rapid and long-lasting effect on acid secretion and acid-induced symptoms.
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PMID:Clinical utility and safety of omeprazole. 265 79


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