Abstract
The proton pump inhibitors (PPIs) lansoprazole (LPZ) and omeprazole (OPZ) have been widely used for more than 20 years in the treatment of acid-related diseases such as gastro-duodenal ulcers and reflux esophagitis. Both LPZ and OPZ are derivatives of 2-[(2- pyridylmethyl)sulfinyl]-1H-benzimidazole, but LPZ has a trifluoroethoxy group in the molecule which seems to provide unique pharmacological properties in addition to its anti-secretory effect. For example, the anti-secretory effect of LPZ in rats was roughly 2 times greater than that of OPZ but the anti-ulcer effects were more than 10 times stronger than those of OPZ in rat models of reflux esophagitis, indomethacin-induced gastric antral ulcers and mepirizole-induced duodenal ulcers. It has also been reported that LPZ has acidindependent protective effects on the gastrointestinal mucosa, anti-inflammatory effects, and anti-bacterial effects on Helicobacter pylori. In contrast, recent advances in endoscopy have revealed that non-steroidal anti-inflammatory drugs (NSAIDs) often cause ulcers not only in the stomach and duodenum, but also in the small intestine in humans. Anti-secretory drugs such as PPIs and histamine H2-receptor antagonists (H2-RAs) are commonly used for the treatment of upper gastrointestinal mucosal lesions induced by NSAIDs. However, the effects of these drugs on NSAID-induced small intestinal lesions are still not fully understood. In this article, both a brief history of the discovery of LPZ and the unique pharmacological properties of LPZ independent from its anti-secretory action are reviewed, and the effects of PPIs and H2-RAs on NSAID-induced small intestinal lesions are discussed.
Keywords: Helicobacter pylori, histamine H2-receptor antagonist, indomethacin, lansoprazole, NSAID, omeprazole, proton pump inhibitor, small intestinal ulcer, gastro-duodenal ulcers, reflux esophagitis
Current Pharmaceutical Design
Title:Discovery of Lansoprazole and its Unique Pharmacological Properties Independent from Anti-secretory Activity
Volume: 19 Issue: 1
Author(s): Hiroshi Satoh
Affiliation:
Keywords: Helicobacter pylori, histamine H2-receptor antagonist, indomethacin, lansoprazole, NSAID, omeprazole, proton pump inhibitor, small intestinal ulcer, gastro-duodenal ulcers, reflux esophagitis
Abstract: The proton pump inhibitors (PPIs) lansoprazole (LPZ) and omeprazole (OPZ) have been widely used for more than 20 years in the treatment of acid-related diseases such as gastro-duodenal ulcers and reflux esophagitis. Both LPZ and OPZ are derivatives of 2-[(2- pyridylmethyl)sulfinyl]-1H-benzimidazole, but LPZ has a trifluoroethoxy group in the molecule which seems to provide unique pharmacological properties in addition to its anti-secretory effect. For example, the anti-secretory effect of LPZ in rats was roughly 2 times greater than that of OPZ but the anti-ulcer effects were more than 10 times stronger than those of OPZ in rat models of reflux esophagitis, indomethacin-induced gastric antral ulcers and mepirizole-induced duodenal ulcers. It has also been reported that LPZ has acidindependent protective effects on the gastrointestinal mucosa, anti-inflammatory effects, and anti-bacterial effects on Helicobacter pylori. In contrast, recent advances in endoscopy have revealed that non-steroidal anti-inflammatory drugs (NSAIDs) often cause ulcers not only in the stomach and duodenum, but also in the small intestine in humans. Anti-secretory drugs such as PPIs and histamine H2-receptor antagonists (H2-RAs) are commonly used for the treatment of upper gastrointestinal mucosal lesions induced by NSAIDs. However, the effects of these drugs on NSAID-induced small intestinal lesions are still not fully understood. In this article, both a brief history of the discovery of LPZ and the unique pharmacological properties of LPZ independent from its anti-secretory action are reviewed, and the effects of PPIs and H2-RAs on NSAID-induced small intestinal lesions are discussed.
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Cite this article as:
Satoh Hiroshi, Discovery of Lansoprazole and its Unique Pharmacological Properties Independent from Anti-secretory Activity, Current Pharmaceutical Design 2013; 19 (1) . https://dx.doi.org/10.2174/1381612811306010067
DOI https://dx.doi.org/10.2174/1381612811306010067 |
Print ISSN 1381-6128 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4286 |
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