Gastroprotective agents

Nissinen, E., Linden, I-B., Pentilla, K.E., Ranta, S. and Pohto, P. (1991). Antioxidant properties of the gastroprotective agent nitecapone. Gastroenterology 100, A133. 

The analgesic effects of NSAIDs are attributed to inhibition of the COX-2 enzyme, whereas the negative GI effects are due to inhibition of COX-1.28 Patients taking oral anticoagulants, those with a history of peptic ulcer disease, or others at high risk for GI complications may be considered candidates for a COX-2 inhibitor or a combination of a nonselective NSAID with a gastroprotective agent such as a proton pump inhibitor (PPI). Because most PPIs are available by prescription only, such patients should be referred to a physician. 

The N-H bond of amides has a pKa of 15-18, an acidity comparable to alcohols and protection of the N-H bond by JV-benzylation is a common ploy. Schemes 8.181 and 8.182 exemplify catalytic hydrogenolyses of N-benzylamides, which were steps in syntheses of Huperzine A71 and AI-77-B (gastroprotective agent),385 respectively. However a number of authors have commented that N-benzylamide groups can be difficult to hydrogenolyse (see below) and therefore these examples may represent particularly favourable cases,... 

Nonselective cyclooxygenase NSAlDs significantly increase the risk of gastric irritation and peptic ulceration. Coprescribing with a gastroprotective agent such as a proton pump inhibitor may be beneficial." Patients with SLE taking NSAlDs may experience... 

It is used orally as a potent gastric antisecretory and gastroprotective agent. 

Masclee GM, Valkhoff VE, van Soest EM, Schade R, MazzagUa G, Molokhia M, et al. Cyclo-oxygenase-2 inhibitors or nonselective NSAIDs plus gastroprotective agents what to prescribe in daily clinical practice Aliment Pharmacol Ther July 2013 38(2) 178-89. 

Cinnamomum cassia (Chinese cinnamon), a species containing numerous flavonic derivatives (epicatechol, epicatechol-O-glucoside and dicyclic-O-glucosides), has been used in traditional Chinese medicine for its analgesic, antipyretic and tonic properties [90]. The aqueous extract showed an effect comparable to cimetidine, a potent antisecretory agent, preventing the ulceration induced by stress and cold, and contrarily to cimetidine, it inhibited the ulceration induced by serotonin. It also reduced the secretion of acid and pepsin and increased the mucosal blood flow. Similar gastroprotective results were obtained in other experimental models, such as in the lesions induced by phenylbutazone and oral administration of ethanol. 

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