Abstract
Arbaprostil [15(R), 15-methyl prostaglandin E2] is inactive. In the presence of acid it is converted to the active 15(S) configuration. The degree of acidity needed for the conversion is not known. We inferred the degree of conversionin vivo in man at different gastric pHs by administering arbaprostil to normal volunteers whose gastric pH was maintained constant at various levels by intragastric titration. A pH-dependent inhibition of gastric acid secretion after stimulation with a peptone meal was observed, with 100 μg inhibiting 98% of acid production at pH 2, but only 15% at pH 6. Significant gastric acid inhibition occurred with the gastric pH at, or less than, 5.
This is a preview of subscription content, log in via an institution to check access.
Similar content being viewed by others
References
Newman A, DeMoraes-Filho JPD, Phillippakos D, Misiewicz JJ: The effect of intravenous infusions of prostaglandins E2 and F2 on human gastric function. Gut 16:272–276, 1975
Karim SMM, Carter DC, Bhana D, Ganesan PA: Effect of orally administered prostaglandin E2 and its 15-methyl analogues on gastric secretion. Br Med J 1:143–146, 1973
Kollberg B, Johansson C: The Inhibitory effect of 15(R), 15-methyl prostaglandin E2 and the interaction with atropine on stimulated gastric acid secretion in man. Scand J Gastroenterol 14:337–342, 1979
Karim SMM, Carter DC, Bhana D, Adaikan Ganesan P: Effect of orally and intravenously administered prostaglandin 15(R), 15-methyl prostaglandin E2 (arbaprostil) on the healing of duodenal ulcer. Gastroenterology 83:357–363, 1982
Fung WP, Karim MM: Effect of 15(R), 15-methyl prostaglandin E2 on the healing of gastric ulcers: A doubleblind endoscopic study. Med J Aust 2:127–128, 1976
Gilbert DA, Surawicz CM, Silverstein FE, Weinberg CR, Saunders DR, Feld AP, Sanford RC, Bergman D, Washington P: Prevention of acute aspirin-induced gastric mucosal injury by 15(R), 15-methyl prostaglandin E2: An endoscopic study. Gastroenterology 86:338–345, 1984
Kollberg B, Nordemar R, Johansson C: Gastrointestinal protection by low-dose oral prostaglandin E2 in rheumatic diseases. Scand J Gastroenterol 16:1005–1008, 1981
Robert A, Yankee EW: Gastric antisecretory effects of 15 (R), 15-methyl PGE2, methyl ester and 15(S), 15-methyl PGE2, methyl ester. Proc Soc Exp Biol Med 148:1155–1158, 1975
Merritt MV, Bronson GE: Kinetics of epimerization of 15(R)-methylprostaglandin E2 and of 15(S)-methylprostaglandin E2 as a function of pH and temperature in aqueous solution. J Am Chem Soc 100:1891–1895, 1978
Halvorsen L, Dotevall G, Walan A: Gastric emptying in patients with achlorhydria or hyposecretion of hydrochloric acid. Scand J Gastroenterol 8:395–399, 1973
McCallum RW, Callachan C, Lange R: Abnormal gastric emptying of solid food in patients with atrophic gastritis with or without pernicious anemia. Dig Dis Sci 25(9):717, 1980 (abstract).
Robert A, Kane G, Reele SB: Dose-response inhibition in man of meal-stimulated gastric acid secretion by 15(R), 15-methyl prostaglandin E2, given orally. Gut 22:728–731, 1981
Author information
Authors and Affiliations
Rights and permissions
About this article
Cite this article
Reele, S.B. Gastric antisecretory activity of arbaprostil as affected by gastric pH. Digest Dis Sci 30, 612–616 (1985). https://doi.org/10.1007/BF01308408
Received:
Revised:
Accepted:
Issue Date:
DOI: https://doi.org/10.1007/BF01308408