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They are the most potent inhibitors of acid secretion available. The group followed and has largely superseded another group of pharmaceuticals with similar effects, but a different mode of action, called H 2-receptor antagonists. These drugs are among the most widely sold drugs in the world, and are generally considered effective. [3]
All of these drugs inhibit the gastric H,K-ATPase by covalent binding, so the duration of their effect is longer than expected from their levels in the blood. [ 76 ] Targeting the terminal step in acid production, as well as the irreversible nature of the inhibition, results in a class of medications that are significantly more effective than H ...
Cimetidine was the prototypical histamine H 2 receptor antagonist from which later drugs were developed. Cimetidine was the culmination of a project at Smith, Kline & French (SK&F; now GlaxoSmithKline) by James W. Black, C. Robin Ganellin, and others to develop a histamine receptor antagonist that would suppress stomach acid secretion.
Some chemicals found in trace amounts in food, as well as some dietary supplements, have been shown to inhibit 5-LOX; these include baicalein, caffeic acid, curcumin, [3] hyperforin and St John's wort. [8] [9] [10]
Proton pump inhibitors (PPIs) block the gastric hydrogen potassium ATPase (H + /K + ATPase) and inhibit gastric acid secretion. These drugs have emerged as the treatment of choice for acid-related diseases, including gastroesophageal reflux disease (GERD) and peptic ulcer disease. PPIs also can bind to other types of proton pumps such as those ...
Cimetidine has been shown clinically to reduce the clearance of mirtazapine, imipramine, timolol, nebivolol, sparteine, loratadine, nortriptyline, gabapentin, and desipramine in humans. [25] Cimetidine inhibits the renal excretion of metformin and procainamide, resulting in increased circulating levels of these drugs. [16]
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