Description
Misoprostol is a prostaglandin E
1 analog with agonist activity mediated by EP
2, EP
3, and EP
4 receptors. It has been shown to inhibit the formation of gastric lesions in rats (ED
50 = 0.31 μg/kg), inhibit superoxide generation in human neutrophils (EC
50 = 0.35 μM), and relax fetal rabbit ductus arteriosus (EC
50 = 0.36 nM) in a concentration dependent manner. Misoprostol is commonly used in clinical medicine for the prevention of peptic ulcer disease. It has also been used in conjunction with mifepristone (RU-
486; ) for the oral induction of first trimester abortion. Misoprostol contains a C-
1 methyl ester and is readily absorbed and rapidly hydrolyzed in humans to the active free acid.
Chemical Properties
Pale Yellow Gel
Uses
A cytoprotective prostaglandin PGE1 analogue.
Uses
A metabolite of Misoprostol. Cytoprotective PGE1 analog that prevents NSAID-induced gastric ulceration
Uses
Misoprostol Acid is a prostaglandin E1 analog with agonist activity mediated by EP2, EP3, and EP4 receptors. It has been shown to inhibit the formation of gastric lesions in rats (ED50 = 0.31 μg/kg), inhibit superoxide generation in human neutrophils (EC50 = 0.35 μM), and relax fetal rabbit ductus arteriosus (EC50 = 0.36 nM) in a concentration dependent manner. Misoprostol is commonly used in clinical medicine for the prevention of peptic ulcer disease. It has also been used in conjunction with mifepristone (RU-486; ) for the oral induction of first trimester abortion. Misoprostol contains a C-1 methyl ester and is readily absorbed and rapidly hydrolyzed in humans to the active free acid.
Biochem/physiol Actions
Misoprostol is a synthetic prostaglandin E1 (PGE1) analogue use to prevent non steroidal anti inflammatory drug-induced (NSAID) gastric ulcers; as a labor inducing and postpartum hemorrhage treatment agent.
in vivo
Unlike the Misoprostol, Misoprostol acid is detectable in plasma. Misoprostol is a lipophilic methyl ester prodrug and is readily metabolized to the free acid, which is the biologically active form. Misoprostol is used worldwide for a variety of indications in obstetrics and gynecology. Misoprostol has both gastric antisecretory and mucosal protective effects[1].
References
[1] WALT R P. Misoprostol for the treatment of peptic ulcer and antiinflammatory-drug-induced gastroduodenal ulceration.[J]. New England Journal of Medicine, 1992, 327 22: 1575-1580. DOI:
10.1056/nejm199211263272207[2] K T BUNCE. GR63799X–a novel prostanoid with selectivity for EP3 receptors.[J]. Advances in prostaglandin, thromboxane, and leukotriene research, 1991, 21A: 379-382.
[3] E. TALPAIN. Characterization of the PGE receptor subtype mediating inhibition of superoxide production in human neutrophils[J]. British Journal of Pharmacology, 1995, 114 7: 1459-1465. DOI:
10.1111/j.1476-5381.1995.tb13370.x[4] G C SMITH J C M R A Coleman. Characterization of dilator prostanoid receptors in the fetal rabbit ductus arteriosus.[J]. Journal of Pharmacology and Experimental Therapeutics, 1994, 271 1: 390-396.
