Clinical progress of proton pump blockers

Clinical progress of proton pump blockers
Core Tips: Clinical Review of Proton Pump Blockers in Medical Review Shandong Heze Dizhi Public Hospital (274001) Zhang Ying Lu Jiarui Proton pump blockers (PPI) have unique mechanisms, high specificity, and strong acid suppression. It has been widely used in the clinic for a long time and has achieved universally recognized efficacy. It has been developed to the second

Clinical Review of the Progress of Proton Pump Blockers in Heze Prefecture, Shandong Province (274001) Zhang Ying Lu Jiarui Proton pump blockers (PPIs) have unique mechanisms, high specificity, and strong acid suppression, and they have a long duration. It has been applied to the clinic and has achieved a recognized therapeutic effect. It has been developed to the second generation. The first generation was represented by comepraaole (Ome), and the second generation was a third generation of lansoprazole (Lrn). There are currently three generations of panupmzole (Pan) pharmacologically. Clinical application. The efficacy and adverse reactions have both commonalities and characteristics, and are summarized below.

1 pharmacological effects 1.1 secretion of gastric acid and pepsin secretion proton pump blocker is a weakly basic drug, the original drug activity is minimal, absorbed into the blood and transported to the gastric mucosal wall cells, and ultimately reach the secretion tube and acidic cavity, where The study of pH in Sakamoto, a healthy person, showed that 20mg of this product was taken orally before going to bed, and its gastric protein secretion inhibition rate was 39% at night at 8h. 13. Pan is a synthetic dialkoxy pyridine substitute at pH 3 Under the condition of 5-7.0, it is more stable than the monoalkoxy substitutions Ome and Lan, and the bioavailability is increased by 7 times. Only the pH of the second generation PPI-Lan introduces fluorine into the molecular structure, which has the pylorus-killing screw. The role of bacteria. However, some people think that Lan can only temporarily inhibit the growth of Helicobacter pylori, the eradication of Helicobacter pylori still need to be combined with antibiotics.

1.3 Affecting Gastrointestinal Hormone Levels Ome significantly inhibits gastric emptying and postprandial gall bladder contraction in healthy people. It raises the level of serum gastrin, serum cholecystokinin levels, and pancreatic polypeptide. There was no significant change in insulin levels.

Taking a regular dose of Lan does not affect postprandial gastric emptying and gallbladder. Secreted by the pancreas.

2Clinical application of 20mg orally once a day for 8 weeks to treat reflux esophagitis, cure rate was 88%. If you use cisapride in combination with oral administration 3 times a day for 12 months, the cure rate is 94%, and it can be effective Prevent recurrence. The cure rate of Lm30mg/d for reflux esophagitis is similar to Ome, but the symptoms are eliminated quickly. The cure rate of refractory esophagitis with the same dose of Lm was comparable to Ome 40 mg/d. Corinaldesi et al. compared the efficacy of Pan and Ome in the treatment of 1 and 111 grades of reflux esophagitis. Pan 40 mg was given orally once daily, Ome 20 mg was given orally once a day, and the cure rate confirmed by endoscopy at 4 weeks was approximately 78.4%. Both groups experienced rapid relief of symptoms and there was no statistically significant difference in remission time.

2.2 Peptic Ulcer The daily cure rate of duodenal ulcer and gastric ulcer after oral Ome 4w is 90%-97%, which is much better than that of H2 receptor antagonist, sucralfate, colloidal quinone, and large dose of antacid. The efficacy of the agent. For patients with H2 receptor antagonists that have been refractory to duodenal ulcer for 6 weeks, switch to 20 mg once per day for oral administration once a week, and the cure rate is 80% for 4 wks. Lrn pyridine ring 4 side chain introduces fluorine and has trifluoroethoxy The substituents make the bioavailability of this product 30% higher than that of Ome, and it is more lipophilic. Under acidic conditions, it can rapidly produce bioactive substances through the parietal cell membrane and exert its efficacy. Ogawa et al. (1995) demonstrated that Lan 30mg/d orally was comparable to Ome oral, and the cure rate Lan was higher than Ome at 2w and was the same at 4w. Lan is safe and effective in the treatment of gastric ulcer, and it can be used as one of the first choice for treating gastric ulcer. Clinical studies have shown that there is no significant difference in the cure rate between Pan 40mg/d and Ome 20mg/d for duodenal ulcer, but the pain symptoms of this product are eliminated quickly in the first 12 days and the two are the same after 2 weeks. The same method used for gastric ulcer control, Pan4w cure rate is higher, 8w cure rate is similar.

2.3 peptic ulcer with Helicobacter pylori infection peptic ulcer with HP infection does not cure HP infection, peptic ulcer is difficult to cure, but also inevitable relapse in vitro experiments show that HP is sensitive to more than 50 kinds of antimicrobial drugs, but most in the body can not In order to eradicate HP infection, even if HP turns negative after treatment, it is easy to re-infect in the short term after drug withdrawal. However, PP.24 Zhuo-ai Syndrome Pan 60mg/(i oral treatment Zhuo-Ergill's syndrome, has a good effect. It was also reported that rice with this product 3Qng/d oral 2-3w treatment of this disease in 3 cases, cure The rate is 100%. 25 Upper gastrointestinal bleeding intravenous injection of Pan / d continuous intravenous infusion of phlegm so that the pH value in the stomach is maintained at more than 6.0 æ›° in this pH environment can make fuller play the role of coagulation mechanism.

3 adverse reactions PPI core imidazole ring, can induce or inhibit the activity of hepatic cytochrome P450 enzymes, thereby affecting the metabolism of other drugs. Ome and Lan have this side effect and one of Pan's greatest features as a third generation PP is that it does not interact with hepatic cytochrome P450 enzymes and the adverse reactions are mild.


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