Digestive Diseases and Sciences

, Volume 36, Issue 12, pp 1673–1679 | Cite as

Effects of H2-receptor antagonists on gastric alcohol dehydrogenase activity

  • Joan Caballería
  • Enrique Baraona
  • Ramón Deulofeu
  • Rolando Hernández-Muñoz
  • Juan Rodés
  • Charles S. Lieber
Original Articles


Inhibition of gastric alcohol dehydrogenase (ADH) activity by cimetidine results in elevated blood levels of ethanol after moderate consumption. To search for alternative H2-blockers lacking such an effect, we compared cimetidine, ranitidine, nizatidine, and famotidine. They inhibited rat gastric ADH noncompetitively, with aKi for ethanol oxidation of 0.68 mM for cimetidine, 0.5 mM for ranitidine, 1 mM for nizatidine, and 4.5 mM for famotidine. These concentrations are higher than therapeutic plasma levels, but intracellular concentrations in the gastric mucosa (assessed with [3H] cimetidine and [14C]famotidine) were at least 10- and 2-fold greater than in the blood, respectively. These results suggests that, given at therapeutic dosesin vivo, the degree of inhibition by cimetidine and ranitidine should be significant and comparable, that by nizatidine should be smaller, and that by famotidine should be negligible. These drugs also exerted either mixed or competitive inhibition of rat hepatic ADH, but the effects of cimetidine and famotidine were observed at concentrations unlikely to occurin vivo. Thus, in alcoholics and in social drinkers who require treatment with H2-receptor antagonists, famotidine might be preferable to the other H2 blockers tested.

Key Words

H2-receptor antagonists cimetidine ranitidine nizatidine famotidine ethanol stomach alcohol dehydrogenase 


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Copyright information

© Plenum Publishing Corporation 1991

Authors and Affiliations

  • Joan Caballería
    • 1
  • Enrique Baraona
    • 1
  • Ramón Deulofeu
    • 1
  • Rolando Hernández-Muñoz
    • 1
  • Juan Rodés
    • 1
  • Charles S. Lieber
    • 1
    • 2
  1. 1.Alcohol Research and Treatment CenterBronx Veterans Affairs Medical Center and Mount Sinai School of Medicine (CUNY)New York
  2. 2.Liver Unit and Biochemical LaboratoryHospital Clinic i ProvincialBarcelonaSpain

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