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Chemical Compound Review

AC1O5KIS     (E)-7-[(1S,3S)-3-hydroxy-2- [(E,3R)-3...

Synonyms:
 
 
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Disease relevance of Arbaprostil

  • Failure of a cytoprotective dose of arbaprostil to heal acute duodenal ulcers. Results of a multiclinic trial [1].
  • This trial documents that a 10-micrograms dose of arbaprostil (which may be considered cytoprotective because of its small effect on gastric acid secretion), although safe and associated with no side effects, is not efficacious in healing acute gastric ulcers [2].
  • The data indicate that arbaprostil is a potent, long-acting orally active antisecretory drug that may be useful for the treatment of peptic ulcer disease [3].
 

High impact information on Arbaprostil

  • A report of three multiclinic trials evaluating arbaprostil in arthritic patients with ASA/NSAID gastric mucosal damage. The Upjohn Company Arbaprostil ASA/NSAID Gastric Mucosal Damage Treatment Study Groups [4].
  • A single nighttime administration of arbaprostil seems to be a safe and efficacious agent for the treatment of acute duodenal ulcer [5].
  • This 6-wk trial used an arbaprostil dose of 10 micrograms q.i.d., which has little gastric acid antisecretory activity [2].
  • Subsequently, two trials determined the abortifacient potential of arbaprostil in pregnant women during the first trimester [6].
  • These results indicate that arbaprostil, at either antisecretory or even acid stimulating doses, is effective in preventing the development of acute gastric erosions and in accelerating the healing of chronic gastric ulcers [7].
 

Biological context of Arbaprostil

 

Anatomical context of Arbaprostil

 

Associations of Arbaprostil with other chemical compounds

 

Analytical, diagnostic and therapeutic context of Arbaprostil

  • Endoscopies were performed after 21 and 42 days of treatment, at which times the arbaprostil and placebo healing rates, respectively, were 6/59 (10.2%) and 4/53 (7.6%) on day 21 and 25/59 (42.4%) and 16/50 (32.0%) on day 42 [2].
  • Isolation of plasma components by double antibody precipitation and filtration: application to the chromatographic determination of arbaprostil ([15R]-15-methylprostaglandin E2) [11].
  • The present result suggests that the gastric antisecretory effect of arbaprostil can be mainly explained in terms of the formation of 15(S) after oral administration [12].
  • We inferred the degree of conversion in 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 [13].

References

  1. Failure of a cytoprotective dose of arbaprostil to heal acute duodenal ulcers. Results of a multiclinic trial. Euler, A.R., Tytgat, G., Berenguer, J., Brunner, H., Wood, D.R., Lookabaugh, J.L., Phan, T.D. Gastroenterology (1987) [Pubmed]
  2. A multiclinic trial evaluating arbaprostil [15(R)-15-methyl prostaglandin E2] as a therapeutic agent for gastric ulcer. Euler, A.R., Popiela, T., Tytgat, G.N., Kulig, J., Lookabaugh, J.L., Phan, T.D., Kitt, M.M. Gastroenterology (1989) [Pubmed]
  3. Gastric antisecretory activity of 15(R)-15-methylprostaglandin E2, arbaprostil, in dogs. Takanashi, H., Itoh, Z. Jpn. J. Pharmacol. (1991) [Pubmed]
  4. A report of three multiclinic trials evaluating arbaprostil in arthritic patients with ASA/NSAID gastric mucosal damage. The Upjohn Company Arbaprostil ASA/NSAID Gastric Mucosal Damage Treatment Study Groups. Euler, A.R., Safdi, M., Rao, J., Jaszewski, R., Welsh, J., Le, V., Raskin, J., Fleischmann, R., Razzaque, M., Champion, C. Gastroenterology (1990) [Pubmed]
  5. Arbaprostil [15(R)-15-methyl prostaglandin E2] in a single nighttime dose of either 50 or 100 micrograms in acute duodenal ulcer. Euler, A.R., Bailey, R.J., Zinny, M.A., Brandon, M.L., Rousseau, B., Ferguson, J.P., Wood, D.R., Le, V.H. Gastroenterology (1989) [Pubmed]
  6. Arbaprostil's [15(R)-15-methyl PGE2] effects on intrauterine pressure in the nonpregnant and pregnant human female--a report of four clinical trials. Euler, A.R., Leodolter, S., Huber, J., Lookabaugh, J., Burns, M.D., Phan, T.D., Wood, D.R., Bogaerts, H., Kitt, M. Prostaglandins Leukot. Essent. Fatty Acids (1989) [Pubmed]
  7. Effects of 15(R)-15-methyl prostaglandin E2 (arbaprostil) on gastric secretion and various gastric lesions induced in rats. Okabe, S., Jino, H., Nishida, A. Jpn. J. Pharmacol. (1986) [Pubmed]
  8. Absorption, tissue distribution, and excretion of 3H-labeled arbaprostil in the male rat. Sinha, A.J., Shaw, S.R., Thornburgh, B.A. European journal of drug metabolism and pharmacokinetics. (1985) [Pubmed]
  9. Pharmacokinetic interactions between arbaprostil and aspirin in humans. Hsyu, P.H., Cox, J.W., Pullen, R.H., Gee, W.L., Euler, A.R. Biopharmaceutics & drug disposition. (1989) [Pubmed]
  10. Lack of effect of arbaprostil on the human non-pregnant uterus. Reele, S.B., Euler, A.R., Hanover, C.K., Lookabaugh, J.L. Acta obstetricia et gynecologica Scandinavica. (1985) [Pubmed]
  11. Isolation of plasma components by double antibody precipitation and filtration: application to the chromatographic determination of arbaprostil ([15R]-15-methylprostaglandin E2). Cox, J.W., Pullen, R.H., Royer, M.E. Anal. Chem. (1985) [Pubmed]
  12. Acid-promoted epimerization of arbaprostil, 15(R)-15-methylprostaglandin E2, elicits gastric antisecretory activities in rats. Takanashi, H., Kawabe, Y., Akima, M. Jpn. J. Pharmacol. (1991) [Pubmed]
  13. Gastric antisecretory activity of arbaprostil as affected by gastric pH. Reele, S.B. Dig. Dis. Sci. (1985) [Pubmed]
 
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