Loperamide: studies on its mechanism of action.
Open Access
- 1 August 1981
- Vol. 22 (8) , 658-662
- https://doi.org/10.1136/gut.22.8.658
Abstract
The effects of loperamide on net solute and water absorption, and prostaglandin E2 (PGE2) and cholera toxin-induced secretion were studied in the rat jejunum using an in vivo steady-state perfusion technique. Loperamide stimulated absorption of fluid, electrolytes, and glucose and reversed PGE2 and cholera toxin-induced secretion to absorption; this opiate analogue had no effect on cholera toxin stimulation of adenylate cyclase activity or the rise of tissue cyclic AMP (cAMP) concentrations. The opiate antagonist, naloxone, reduced the antisecretory effects of loperamide without affecting tissue levels of cAMP. These results indicate that loperamide inhibits PGE2 and cholera toxin-induced secretion, and that this phenomenon is independent of any direct effect that cholera toxin has on the adenylate cyclase system. The action of naloxone suggests, but does not prove, that loperamide exerts its effect via opiate receptors.This publication has 20 references indexed in Scilit:
- Effects of Prostaglandins and Cholera Enterotoxin on Intestinal Mucosal Cyclic AMP AccumulationJournal of Clinical Investigation, 1974
- Effect of Prostaglandin E1 on Glucose, Water, and Electrolyte Absorption in the Human JejunumGastroenterology, 1973
- Studies on the effects of unconjugated dihydroxy bile salts on rat small intestinal function in vivoBiochimica et Biophysica Acta (BBA) - Biomembranes, 1972
- The effects of different bile salts on the absorption of fluid, electrolytes, and monosaccharides in the small intestine of the rat in vivoGut, 1972
- Intestinal Adenyl-Cyclase Activity in Canine Cholera: Correlation with Fluid AccumulationThe Journal of Infectious Diseases, 1972
- Inhibition of glucose absorption by prostaglandins E1, E2 and F2αJournal of Pharmacy and Pharmacology, 1972
- Stimulation of intestinal mucosal adenyl cyclase by cholera enterotoxin and prostaglandinsJournal of Clinical Investigation, 1971
- Cholera enterotoxin—Recent investigations yield insights into transport processesThe American Journal of Medicine, 1971
- Effects of Prostaglandins, Theophylline, and Cholera Exotoxin Upon Transmucosal Water and Electrolyte Movement in the Canine JejunumGastroenterology, 1971
- Interrelationships between the absorptions of glucose, sodium and water by the normal human jejunum.1969