Study of molecular mechanisms of formation of hydrochloric acid of gastric juice allowed to reveal its key part – the active secretion of protons, involving the transport of K + which is sold by a special membrane complex – the proton pump. While the formation of protons in different intracellular reactions controlled by different regulatory factors (acetylcholine, histamine, gastrin, prostaglandins, gastrointestinal tissue factor, etc.), the work of this mechanism is practically not related to the physiological regulatory mechanisms.
Therefore, the development of generics that can reduce the activity of ATPase proton pump is an important task of Online Pharmacy Without Prescription. The first proton pump inhibitor was omeprazole (on the Swedish market since 1987), followed by lanzoprazol (1992, France).In 1994, Germany appeared pantoprazole.Recently there have been generics rabeprazole (UK) and esomeprazole (Sweden). Proton pump inhibitors belong to the chemical class of substituted benzimidazole derivatives and have antisecretory effect by inhibiting H +, K +-ATPase (proton pump), parietal cells of gastric mucosa. In the tubules of the gastric glands of the proton pump inhibitors, as a weak base, interact with a hydrogen ion, are transformed into sulfenamidnye derivatives, which form covalent bonds with cysteine SH-groups of H +, K +-ATPase on the surface of the apical membrane of parietal cells facing the lumen of gastric glands , and block the final stage of formation of hydrochloric acid.
Such communication is irreversible, so the duration of proton pump inhibitors depends on the rate of synthesis of new molecules, proton pump, as well as the duration of circulation of the drug in the blood. All connections of this group quickly activated as strongly acidic reaction medium (pH less than 3.0). In less acidic environment (pH ~ 3,5-7,4) Pantoprazole is chemically more stable than omeprazole or lanzoprazol it to a lesser extent, transformed into an active form. Therefore, its inhibitory ability in the reaction from neutral to moderately acidic approximately 3 times less than that of omeprazole. Indian drugs reduce the basal and stimulated gastric secretion regardless of the nature of the stimulus. Their clinical efficacy – the highest among the antiulcer funds.
These generics provide the maintenance of intragastric pH at 3.0 and above for 18 hours a day, which contributes to scarring of ulcerous defect in a short time. Duodenal ulcers cicatrizing for 2 weeks in 60% of patients, for 4 weeks – 96% of patients, observed scarring of the stomach and duodenal ulcers in ranitidinrezistentnyh in 94,4% of cases. Proton pump inhibitors are used during antigelikobakternoy (eradication) therapy. Although their bactericidal effect is debatable, especially as they apply in the granules with a special membrane, which dissolves in the small intestine at alkaline pH, and enclosed in gelatin capsules.
Pharmacological characterization.
Indications: non-ulcer dyspepsia;
* stomach ulcer and duodenal ulcer;
” peptic ulcer;
” stress ulcers;
” erosive and ulcerative esophagitis;
” reflux esophagitis;
” Zollinger-Ellison syndrome;
” multiple endocrine adenomatosis;
” system mastoidoz;
” infection of Helicobacter pylori.
Contraindications:
” hypersensitivity;
” malignant neoplasms in the gastrointestinal tract;
” pregnancy (especially the I term);
” breastfeeding.
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