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Chemical Compound Review

BSPBio_003134     3-[[2- (diaminomethylideneamino)- 1,3...

Synonyms: CCG-40241, CHEBI:178303, NSC-757810, HMS501L07, NSC757810, ...
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Disease relevance of famotidine


Psychiatry related information on famotidine


High impact information on famotidine

  • Comparison of the effects of over-the-counter famotidine and calcium carbonate antacid on postprandial gastric acid. A randomized controlled trial [8].
  • CONCLUSIONS--Recommended over-the-counter doses of famotidine and calcium carbonate tablets have different pharmacokinetic profiles when taken in the postprandial period [8].
  • RESULTS: In 43 patients without gastric neutrophils, ulcers developed in 1 of 14 (7.7%) taking placebo, 2 of 16 (12.5%) taking 20 mg famotidine, and none of 13 taking 40 mg famotidine [3].
  • METHODS: One hundred four patients with rheumatoid or osteoarthritis who had gastroduodenal ulceration received famotidine, 40 mg twice daily [9].
  • METHODS: Thirty-four dysphagic patients with peptic stricture and erosive esophagitis were dilated and randomized to omeprazole 20 mg every day versus H2RA (ranitidine 150 mg twice daily or famotidine 20 mg twice daily) [10].

Chemical compound and disease context of famotidine


Biological context of famotidine


Anatomical context of famotidine


Associations of famotidine with other chemical compounds


Gene context of famotidine

  • Histamine-induced increase of cAMP was inhibited by the H2 receptor antagonist famotidine, whereas induction of IP3 was not observed, making signaling via the H1 receptor unlikely [27].
  • These results suggest that, in addition to the absence of OCT1 in human kidney, a species difference in the transport activity by hOAT3 and rOat3 accounts, at least in part, for the species difference in the drug-drug interaction between famotidine and probenecid [28].
  • Inhibition and substrate specificity of hOCT1, hOCT2, and hOCT3 for ranitidine and famotidine were elucidated in cRNA-injected Xenopus laevis oocytes [29].
  • Ranitidine and famotidine exhibited similarly potent inhibition of [3H]1-methyl-4-phenyl pyridinium uptake into hOCT1-expressing (IC50= 33 and 28 microM, respectively) and hOCT2-expressing oocytes (IC50= 76 and 114 microM, respectively) [29].
  • Famotidine seems to be one of the most potent inhibitors of hOCT3 yet identified [29].

Analytical, diagnostic and therapeutic context of famotidine


  1. Famotidine for the prevention of gastric and duodenal ulcers caused by nonsteroidal antiinflammatory drugs. Taha, A.S., Hudson, N., Hawkey, C.J., Swannell, A.J., Trye, P.N., Cottrell, J., Mann, S.G., Simon, T.J., Sturrock, R.D., Russell, R.I. N. Engl. J. Med. (1996) [Pubmed]
  2. Famotidine to prevent peptic ulcer caused by NSAIDs. Graham, D.Y. N. Engl. J. Med. (1996) [Pubmed]
  3. Neutrophils, Helicobacter pylori, and nonsteroidal anti-inflammatory drug ulcers. Taha, A.S., Dahill, S., Morran, C., Hudson, N., Hawkey, C.J., Lee, F.D., Sturrock, R.D., Russell, R.I. Gastroenterology (1999) [Pubmed]
  4. Efficacy and safety of famotidine in the management of benign gastric ulcers. Lyon, D.T. Am. J. Med. (1986) [Pubmed]
  5. Comparison of gastric mucosal surface pH response times after intravenous administration of histamine2-receptor antagonists. Katsu, K., Yabe, S. Clinical therapeutics. (1995) [Pubmed]
  6. An open-label study of the therapeutic efficacy of high-dose famotidine adjuvant pharmacotherapy in schizophrenia: preliminary evidence for treatment efficacy. Rosse, R.B., Kendrick, K., Fay-McCarthy, M., Prell, G.D., Rosenberg, P., Tsui, L.C., Wyatt, R.J., Deutsch, S.I. Clinical neuropharmacology. (1996) [Pubmed]
  7. Review of an extensive worldwide study of a new H2-receptor antagonist, famotidine, as compared to ranitidine in the treatment of acute duodenal ulcer. Bianchi Porro, G., Dicenta, C., Cook, T., Humphries, T.J. J. Clin. Gastroenterol. (1987) [Pubmed]
  8. Comparison of the effects of over-the-counter famotidine and calcium carbonate antacid on postprandial gastric acid. A randomized controlled trial. Feldman, M. JAMA (1996) [Pubmed]
  9. Famotidine for healing and maintenance in nonsteroidal anti-inflammatory drug-associated gastroduodenal ulceration. Hudson, N., Taha, A.S., Russell, R.I., Trye, P., Cottrell, J., Mann, S.G., Swanell, A.J., Sturrock, R.D., Hawkey, C.J. Gastroenterology (1997) [Pubmed]
  10. Omeprazole versus H2-receptor antagonists in treating patients with peptic stricture and esophagitis. Marks, R.D., Richter, J.E., Rizzo, J., Koehler, R.E., Spenney, J.G., Mills, T.P., Champion, G. Gastroenterology (1994) [Pubmed]
  11. Treatment of active duodenal ulcers with famotidine. A double-blind comparison with ranitidine. Rohner, H.G., Gugler, R. Am. J. Med. (1986) [Pubmed]
  12. Cimetidine induces interleukin-18 production through H2-agonist activity in monocytes. Takahashi, H.K., Watanabe, T., Yokoyama, A., Iwagaki, H., Yoshino, T., Tanaka, N., Nishibori, M. Mol. Pharmacol. (2006) [Pubmed]
  13. Hemodynamic effects of quinidine and famotidine in patients with congestive heart failure. Kirch, W., Halabi, A., Hinrichsen, H. Clin. Pharmacol. Ther. (1992) [Pubmed]
  14. Lansoprazole. A review of its pharmacodynamic and pharmacokinetic properties and its therapeutic efficacy in acid-related disorders. Barradell, L.B., Faulds, D., McTavish, D. Drugs (1992) [Pubmed]
  15. Histamine H1 and H2 receptor antagonists accelerate skin barrier repair and prevent epidermal hyperplasia induced by barrier disruption in a dry environment. Ashida, Y., Denda, M., Hirao, T. J. Invest. Dermatol. (2001) [Pubmed]
  16. Negative effects of famotidine on cardiac performance assessed by noninvasive hemodynamic measurements. Kirch, W., Halabi, A., Linde, M., Santos, S.R., Ohnhaus, E.E. Gastroenterology (1989) [Pubmed]
  17. Pharmacodynamics of famotidine in humans. Chremos, A.N. Am. J. Med. (1986) [Pubmed]
  18. Initial 48-hour acid inhibition by intravenous infusion of omeprazole, famotidine, or both in relation to cytochrome P450 2C19 genotype status. Sugimoto, M., Furuta, T., Shirai, N., Ikuma, M., Hishida, A., Ishizaki, T. Clin. Pharmacol. Ther. (2006) [Pubmed]
  19. Postprandial biliary and pancreatic secretion during profound inhibition of gastric secretion in humans. Lanzini, A., Facchinetti, D., Pigozzi, M.G., Wuhrer, A., Saleri, A. Gut (1993) [Pubmed]
  20. Famotidine-associated central nervous system reactions and plasma and cerebrospinal drug concentrations in neurosurgical patients with renal failure. Yoshimoto, K., Saima, S., Echizen, H., Nakamura, Y., Kondo, T., Yagishita, Y., Ishizaki, T. Clin. Pharmacol. Ther. (1994) [Pubmed]
  21. Histamine-induced production of interleukin-1 alpha from murine bone marrow stromal cells and its inhibition by H2 blockers. Tasaka, K., Mio, M., Shimazawa, M., Nakaya, N. Mol. Pharmacol. (1993) [Pubmed]
  22. Comparative efficacy of cimetidine, famotidine, ranitidine, and mylanta in postoperative stress ulcers. Gastric pH control and ulcer prevention in patients undergoing coronary artery bypass graft surgery. Lamothe, P.H., Rao, E., Serra, A.J., Castellano, J., Woronick, C.L., McNicholas, K.W., Lemole, G.M. Gastroenterology (1991) [Pubmed]
  23. Low dose famotidine and cimetidine in single postprandial doses: a placebo controlled comparative study of overnight pH. Reilly, T.G., Mann, S.G., Panos, M.Z., Walt, R.P. Gut (1995) [Pubmed]
  24. Effect of gastric acid suppressants on human gastric motility. Parkman, H.P., Urbain, J.L., Knight, L.C., Brown, K.L., Trate, D.M., Miller, M.A., Maurer, A.H., Fisher, R.S. Gut (1998) [Pubmed]
  25. Influence of histamine receptors on basal left ventricular contractile tone in humans: assessment using the H2 receptor antagonist famotidine and the beta-adrenoceptor antagonist esmolol as pharmacologic probes. Borow, K.M., Ehler, D., Berlin, R., Neumann, A. J. Am. Coll. Cardiol. (1992) [Pubmed]
  26. Pharmacodynamics and pharmacokinetics of parenteral histamine (H2)-receptor antagonists. Ostro, M.J. Am. J. Med. (1987) [Pubmed]
  27. Human skin mast cells express H2 and H4, but not H3 receptors. Lippert, U., Artuc, M., Grützkau, A., Babina, M., Guhl, S., Haase, I., Blaschke, V., Zachmann, K., Knosalla, M., Middel, P., Krüger-Krasagakis, S., Henz, B.M. J. Invest. Dermatol. (2004) [Pubmed]
  28. A species difference in the transport activities of H2 receptor antagonists by rat and human renal organic anion and cation transporters. Tahara, H., Kusuhara, H., Endou, H., Koepsell, H., Imaoka, T., Fuse, E., Sugiyama, Y. J. Pharmacol. Exp. Ther. (2005) [Pubmed]
  29. Differential substrate and inhibitory activities of ranitidine and famotidine toward human organic cation transporter 1 (hOCT1; SLC22A1), hOCT2 (SLC22A2), and hOCT3 (SLC22A3). Bourdet, D.L., Pritchard, J.B., Thakker, D.R. J. Pharmacol. Exp. Ther. (2005) [Pubmed]
  30. Continuous intravenous famotidine for haemorrhage from peptic ulcer. Walt, R.P., Cottrell, J., Mann, S.G., Freemantle, N.P., Langman, M.J. Lancet (1992) [Pubmed]
  31. Use of microbleeding and an ultrathin endoscope to assess gastric mucosal protection by famotidine. Daneshmend, T.K., Prichard, P.J., Bhaskar, N.K., Millns, P.J., Hawkey, C.J. Gastroenterology (1989) [Pubmed]
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