The inhibition of first-pass metabolism of ethanol by H2-receptor antagonists: a tabulated review

  title={The inhibition of first-pass metabolism of ethanol by H2-receptor antagonists: a tabulated review},
  author={David E. Moody},
  journal={Expert Opinion on Drug Safety},
  pages={917 - 934}
  • D. Moody
  • Published 2 September 2018
  • Medicine
  • Expert Opinion on Drug Safety
ABSTRACT Introduction: In the 1980s–1990s numerous studies were performed on H2-receptor antagonist inhibition of ethanol first-pass metabolism. Blood alcohol concentrations warranting possible driving under the influence citations in the United States have subsequently dropped from ≥100 mg/dL to 50 mg/dL (Utah in 2019) (30 mg/dL or zero tolerance in some parts of the world). A reexamination of these studies seemed important. Areas covered: Papers were compiled that addressed the effect of… Expand
2 Citations
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In Vivo Interactions Between H2‐Receptor Antagonists and Ethanol Metabolism in Man and in Rats
An increase in ethanol absorption due to cimetidine but not to ranitidine in man at ethanol serum concentrations below 20 m M is suggested, suggesting inhibition of microsomal ethanol oxidation. Expand
Effects of various concomitant medications on gastric alcohol dehydrogenase and the first-pass metabolism of ethanol.
It is concluded that many commonly used medications affect gastric ADH, but that the increase in the actual amount of alcohol absorbed is quite small, and demonstrable only under special conditions. Expand
Effects of ranitidine on blood alcohol levels after ethanol ingestion. Comparison with other H2-receptor antagonists.
Patients treated with ranitidine or cimetidine should be warned of possible functional impairments after consumption of amounts of ethanol considered safe in the absence of such therapy. Expand
H2-Antagonists and Alcohol
There are conflicting data on the existence of significant first-pass metabolism of alcohol (ethanol) in the human stomach and its inhibition by histamine H2-receptor antagonists and the significance of this interaction is not easy to resolve. Expand
Inhibition of gastric alcohol dehydrogenase activity by histamine H2-receptor antagonists has no influence on the pharmacokinetics of ethanol after a moderate dose.
It is concluded that gastric mucosal concentrations of histamine H2-receptor blockers achieved after oral dosing are probably too low to cause significant inhibition of gastric ADH in vivo. Expand
Lack of effect of H2-receptor antagonists on the pharmacokinetics of alcohol consumed after food at lunchtime.
None of the H2-receptor antagonists had any statistically significant effects on any of the pharmacokinetic parameters for alcohol in an open, four-way cross-over study. Expand
Effects of cimetidine on gastric alcohol dehydrogenase activity and blood ethanol levels.
Results indicate that gastric alcohol dehydrogenase activity governs, in part, the systemic bioavailability of ethanol, and systemic effects of alcohol may be exacerbated in patients receiving cimetidine. Expand
Histamine-2 Receptor Antagonists Do Not Alter Serum Ethanol Levels in Fed, Nonalcoholic Men
This study examined the potential interaction of H-2 receptor antagonists with alcohol using a randomized crossover design in which each of 25 participants would be treated with a therapeutic regimen of the four drugs and serve as his own control. Expand
Is there an Interaction Between H2-Antagonists and Alcohol?
  • A. Fraser
  • Medicine
  • Drug metabolism and drug interactions
  • 1998
The relationship between ethanol absorption and gastric emptying raises the possibility that the effects of H2-receptor antagonists observed at very low doses of alcohol may be due to the acceleration of gastric emptied by these drugs. Expand
Effects of H2-receptor antagonists on ethanol metabolism in Japanese volunteers.
The effects of H2-receptor antagonists (cimetidine, ranitidine, and famotidine) on ethanol metabolism were investigated. Neither in aldehyde dehydrogenase (ALDH)-1 deficient subjects nor in thoseExpand