Gastroprotective drugs

In a comparison of oral sustained-release morphine (mean 94 mg/day) and hydromor-phone (138 or 206 mg/day) with regard to nausea, vomiting, and constipation, in patients receiving opioids for cancer pain, morphine provided better pain relief at lower doses (after accounting for dose conversion) but was associated with more nausea, constipation, and higher consumption of antiemetic and gastroprotective drugs [104 ]. 

Targownik LE et al The relative efficacies of gastroprotective strategies in chronic users of non-steroidal anti-inflammatory drugs. Gastroenterology 2008 134 937. [PMID 18294634]... 

A number of experimental studies have been performed looking at the gastroduodenal damaging effects of non-steroidal antiinflammatory drugs (NSAID) such as indomethacin [193]. In these studies, orally administered 5-methoxyflavone inhibited indomethacin-induced leukocyte adherence to mesenteric venules, suggesting a role of inhibition of leukocyte adherence in gastroprotective activity of this flavonic compound. 

Schmeda-Hirschmann, G. and Yesilada, E. (2005). Traditional medicine and gastroprotective crude drugs. /. Ethnopharmacol. 100, 61-66. 

An illustration of the essential steps in inhibition of acid secretion by PPIs with pantoprazole as an example. The drug is administered in a gastroprotected formulation and is absorbed in the duodenum or is administered in a reconstituted IV formulation. The acidic, membrane-enclosed space of the active parietal cell s secretory canaliculus accumulates the PPI approximately 1,000-fold (pH 1.0, pKa of drug approximately 4.0) due to protonation of the pyridine. After intramolecular transfer to the N of the benzimidazole, rearrangement of the molecule occurs to form first the cationic thiophilic sulfenic acid and then the sulfonamide, either of which reacts rapidly with cysteines on the luminal face of the pump. 

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