Proton-pump inhibitor

Proton pump inhibitors (PPI) are used for people with ulcers and for treatment of heartburn and other symptoms of gastroesophageal reflux disease (GERD), a condition in which backward flow of acid from the stomach causes heartburn and possible injury of the esophagus. GERD has an estimated prevalence of 10-20% in the Western world [32] and proton pump inhibitors are the mainstay of GERD therapy. One study [33] estimated that GERD was prevalent in 7 million insured people in the U.S. at an incremental health cost of 23 billion. Using a 4% work productivity loss, the cost estimate increases to 32 billion. 

Omeprazole can be made by reaction of a substituted diaminobenzene to make the benzoimidazole [38]. Alkylation of the thiol gives the sulfide which is then oxidized to the sulfoxide, omeprazole. The omeprazole can be separated into the two enantiomers. Preferably, asymmetric oxidation of the sulfide is done to selectively prepare the S enantiomer, esomeprazole. 

The primary H2 blockers used to control gastric secretions are listed in Table 27-1. Cimetidine was the first H2 blocker to be widely used as an antiulcer agent. Newer drugs such as famotidine, nizatidine, and ranitidine appear to be at least as effective as cimetidine they differ from one another primarily in their phar- 

Cimetidine Tagamet 300 mg 4 times each day with meals and at bedtime, 400 or 600 mg in the morning and at bedtime, or 800 mg at bedtime 

Omeprazole (Prilosec) was the original PPI this drug is now joined by esomeprazole (Nexium), lansoprazole (Prevacid), pantoprazole (Protonix), and rabeprazole (AcipHex) (see Table 27-2). All of these drugs are similar, with selection often depending on cost, availability, and the drug interaction potential of each agent.15 Likewise, nonprescription forms of certain PPIs are now available, and these forms offer a convenient, 

Generic Name Trade Name Treatment Healing Maintenance Prevent Recurrence Treatment Healing Maintenance Prevent Recurrence 

Treatment of H. Pylori Infection in Gastric Ulcer Disease 

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Moreover, receptors also control gastric acid release, although some marked species dependence is noticed (8). However, appHcation of agonists in this area does not seem to be probable the antagonists and the proton pump inhibitors serve quite weU. 

Antacids are neutralizing agents. Examples are magnesium hydroxide, magnesium trisylicate and aluminium hydroxide. Prior to the introduction of histamine-H2 receptor antagonists and proton pump inhibitors, they were the standard drugs for the treatment of duodenal/ peptic ulcers. Today their clinical use is limited to the treatment of dyspepsia and the symptomatic relieve for patients with peptic ulcers. 

Proton Pump Inhibitors and Acid Pump Antagonists... 

Cytochrome P450 2C19, also termed S-mephenytoin hydroxylase, is a mixed-function oxidase localized in the endoplasmic reticulum which is responsible for the biotransformation of S-mephenytoin, some barbiturates, almost all proton pump inhibitors such as omeprazole, diazepam and others. 

Proton Pump Inhibitors and Acid Pump Antagonists retinoid X receptor (RXR) and is also activated by various lipophilic compounds produced by the body such as bile acids and steroids. PXR heterodimerized with RXR stimulates the transcription of cytochrome P450 3A monooxygenases (CYP3A) and other genes involved in the detoxification and elimination of the... 

Proton Pump Inhibitors and Acid Pump Antagonists. Figure 1 Irreversible proton pump inhibitors (PPIs). 

Proton Pump Inhibitors and Acid Pump Antagonists. Figure 2 Chemical mechanism of irreversible PPIs. PPIs are accumulated in acidic lumen and converted to active sulfenic acid and/or sulfenamide by acid catalysis. These active forms bind to extracytoplasmic cysteines of the gastric H.K-ATPase [3]. 

Shin JM, Cho YM, Sachs G (2004) Chemistry of covalent inhibition of the gastric (H+,K+)-ATPase by proton pump inhibitors. J Am Chem Soc 126 7800-7811... 

Shin JM, Sachs G (2002) Restoration of acid secretion following treatment with proton pump inhibitors. Gastroenterology 123 1588-1597... 

Shin JM, S achs G (2004) Differences in binding properties of two proton pump inhibitors on the gastric H+,K+-ATPase in vivo. Biochem Pharmacol 68 2117-2127... 

Helicobader pylori hydrochloric acid hypersecretory paralytic ileus photophobia proton pump inhibitor... 

The proton pump inhibitors are particularly important in the treatment of Helicobacter pylori in patients with active duodenal ulcers. Helicobacter pylori (H. pylori) has been implicated as a causative organism in a type of chronic gastritis and in a large number of cases of peptic and duodenal ulcers. 

The proton pump inhibitors suppress gastric acid secretion by blocking the final step in the production of gastric acid by the gastric mucosa... 

The proton pump inhibitors are used for treatment or symptomatic relief of various gastric disorders, including gastric and duodenal ulcers, GERD, or pathological hypersecretory conditions. Painful, persistent heartburn 2 or more days a week may indicate acid reflux disease which can erode the delicate lining of the esophagus,... 

The most common adverse reactions seen with the proton pump inhibitors include headache, diarrhea, and abdominal pain. Other less common adverse reactions include nausea, flatulence, constipation, and dry mouth. 

The proton pump inhibitors are contraindicated in patients who have hypersensitivity to any of the drags. Omeprazole (Pregnancy Category C) and lansoprazole, rabeprazole, and pantoprazole (Pregnancy Category B) are contraindicated during pregnancy and lactation. The proton pump inhibitors are used cautiously in older adults and in patients with hepatic impairment. 

PROTON PUMP INHIBITORS. The adverse reactions of the proton pump inhibitors are usually mild. The most common adverse reactions associated with file proton... 

Intravenous H2-receptor antagonist (preferred) or intravenous proton pump inhibitor (PPI)... 

Proton pump inhibitors (consider ql2h dosing for better pH control)... 

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