| Author/Editor | Dajani, EZ | |
| Title | Misoprostol: pharmacology, pharmacokinetics and mechanisms of action | |
| Type | članek | |
| Source | Exp Clin Gastroenterol | |
| Vol. and No. | Letnik 1, št. 2 | |
| Publication year | 1991 | |
| Volume | str. 97-105 | |
| Language | eng | |
| Abstract | There is substantial evidence supporting a role of prostaglandins (PGs) in physiological mechanisms important in maintaining the mucosal integrity of the gastrointestinal (GI) tract. Thus, it is postulated that natural prostaglandins could be used therapeutically in acid peptic disorders. However, problems of selectivity, metabolic instability and oral inactivity precluded their clinical use. These limitations were resolved by the development of a synthetic prostaglandin E1 analog, misoprostol. Animal and human studies demonstrated that misoprostol possesses potnet gastric antisecretory properties against basal, nocturnal and stimulated (meal, histamine, tetragastrin) gastric secretion. The inhibition of gastric secretion is characterized by suppression of volume, acid, pepsin and total acid output, in a dose-dependent manner. Unlike nonprostanoid gastric secretory inhibitors, misoprostol does not influence either the fasting or postprandial serum gastrin. The gastric antisecretory effects of misoprostol are not a consequence of reduction of mucosal blood flow, nor a consequence of altered mucosal barrier functions, but mediated via a direct effect on parietal cells. Misoprostol possesses mucosal protective properties against injury to the gastroduodenal mucosa induced by non-steroidal anti-inflammatory drugs (NSAIDs), bile acid and ethanol. The basic for the mucosal protective property of misoprostol is not fully known, but laboratory and clinical evidence indicates a direct effect on mucosal blood flow, enhanced mucosal restitution, enhanced mucosal barrier stability and enhanced mucus and bicarbonate secretion. Misoprostol is quickly and extensively absorbed following oral administration. It is rapidly metabolized to many polar metabolites by pathways similar to other fatty acids in virtually every cell and is excreted by many different pathways. There are no significant pharmacokinetic ineractions with several pharmacological classes of drugs.(trunc.) | |
| Descriptors | ALPROSTADIL GASTRIC MUCOSA ANTI-ULCER AGENTS INTESTINAL MUCOSA |