Inhibits acid secretion

It was known that the K+ -competitive imidazopyridine compound, SCH28080, inhibits acid secretion. Then, many reversible inhibitors were developed. These contain protonatable nitrogens but have a variety of core structures such as imidazopyiidines, piperidinopyr-idines, substituted 4-phenylaminoquinolines, pyrrolo [3,2-c]quinolines, guanidinothiazoles, and 2,4-diamino-pyrimidine derivatives. Several reversible inhibitors have been in clinical trials. 

Misoprostol is a synthetic prostaglandin E2 analog that exogenously replaces prostaglandin stores. The minimum effective dose shown to inhibit acid secretion and promote mucosal defense is 400 meg/day. Misoprostol use is limited by a high frequency of bothersome gastrointestinal effects such as abdominal pain, flatulence, and diarrhea. In placebo-controlled studies diarrhea occurred with twice the frequency in the... 

Misoprostol (B) is a semisynthetic prostaglandin derivative with greater stability than natural prostaglandin, permitting absorption after oral administration. like locally released prostaglandins, it promotes mucus production and inhibits acid secretion. Additional systemic effects (frequent diarrhea risk of precipitating contractions of the Liillmann, Color Atlas of Pharmacology (... 

Gastric acid secretion is inhibited in the presence of acid itself. A negative feedback occurs when the pH approaches 2.5 such that further secretion of gastrin is inhibited until the pH rises. Ingested carbohydrates and fat also inhibit acid secretion after they reach the intestines several hormonal mediators for this effect have been proposed. The secretion of pepsinogen appears to parallel the secretion of H+, while the patterns of secretion of mucus and bicarbonate have not been well characterized. 

In contrast, H3-selective histamine agonists inhibit acid secretion stimulated by food or pentagastrin in several species. 

Almost a century ago, in 1910, the Croatian physician Karl Schwarz had formulated the dictum, "No acid - no ulcer , yet 50 years later doctors still lacked the means of effectively inhibiting acid secretion. Inappropriate levels of gastric acid underlie several widespread pathological conditions, including gastroesophageal... 

BY 1023/SK F 96022 INN pantoprazoie, a novel gastric proton pump inhibitor, potently inhibits acid secretion but lacks relevant cytochrome P450 interactions./. Pharmacol. Exp. Ther., 1990, 254(1), 129-135. 

Cells throughout the gastrointestinal tract release somatostatin. Somatostatin inhibits acid secretion in the stomach and it promotes absorption of sodium, chloride and water in the small intestine and colon (Krejs 1986). The somatostatin analogs octreotide and lanreotide have been shown to decrease intestinal secretion in animal models (Botella et al 1993) and in humans with specific metabolic intestinal secretory disorders however, these drugs are not used widely in human medicine. In one study in horses, octreotide was shown to decrease gastric acidity (Sojka et al 1992) but its effects on intestinal or colonic secretion in horses have not been reported. 

Gastric Inhibitory Polypeptide - (G.I.P.) is a 43 amino acid polypeptide released by glucose and fat ingestion. In addition to its insulinotrophic effects in animals and man, G.I.P. inhibits acid secretion in... 

Lloyd KC, Wang J, Aurang K, Gronhed P, Coy DH, Walsh JH (1995) Activation of somatostatin receptor subtype 2 inhibits acid secretion in rats. Am J Physiol 268(1 Pt 1) G102-G106... 

The pathogenesis of peptic ulceration is not yet clear. It could be due to an imbalance between acid secretion and mucosal defensive and/or protective mechanisms, but the association between H. pylori and peptic ulceration has questioned this hypothesis. Therefore, drugs inhibiting acid secretion and/or eradicating H. pylori are of major interest. 

Histamine H2-receptor antagonists inhibit acid secretion by blocking the stimulation of H2-receptors in the gastric parietal cell. They are Cimetidine Nizatidine Ranitidine Roxatidine... 

The Merck group also described (L-643,4A1) as long acting. In the fistula dog using histamine as the stimulant, it is a little more potent than ranitidine, but at 15mg/kg p.o. ( 50xED5q) it inhibited acid secretion by 80% after 24h. At this dose ranitidine s effect had... 

Tricyclic compounds - The therapeutic use of tricyclic compounds such as trlmlpramlne and plrenzeplne has been reviewed. Trimipramlne (50mg nocte) produced similar healing rates to clmetldlne In diiodenal and gastric ulcers, and was effective In maintenance treatment. Tiredness and dry mouth were side effects. The related antidepressant mianserin Inhibited acid secretion In volunteers, 7 but MCI 2016, 21, a... 

Omepra/ole and lansopraznie are inactive at neutral pH. but in acid they rearrange into two types of reactive molecule, which react with sulphydryl groups in the H7K -ATPproton pump) responsible for transporting H" ions out of the parietal cells. Because the enzyme is irreversibly inhibited, acid secretion only resumes after the synthesis of... 

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