Aspirin increases blood alcohol concentrations in humans after ingestion of ethanol

Article Abstract:

Any drug that is absorbed from the stomach and intestine must first pass through the liver before reaching the circulation. If the drug is metabolized, such as in the liver, before reaching the circulation, there will be less active drug available to exert its therapeutic effects. The decrease in bioavailability, or availability of a drug at its sites of action, due to its metabolism before reaching the circulation, is known as the first-past effect. Ethanol undergoes oxidation, a metabolic reaction, in the stomach, and this reaction was shown to be an important factor in determining the blood levels of alcohol. Fasting, alcohol abuse, and female gender are associated with diminished first-pass metabolism. Certain drugs, such as cimetidine and ranitidine, used to treat ulcers, also affect first-pass metabolism and gastric alcohol dehydrogenase (ADH), an enzyme involved in alcohol metabolism. Treatment with these agents is associated with elevated blood alcohol levels after ingestion of only small or moderate doses of ethanol. Aspirin, which is commonly used to relieve pain and treat rheumatic disorders, can cause adverse gastrointestinal side effects. The effects of aspirin on ADH and first-pass metabolism of ethanol were assessed in five healthy volunteers given 0.3 grams per kilogram of body weight. Ingestion of one gram of aspirin one hour before alcohol intake was associated with higher blood levels of alcohol in the fed state, defined as one hour after a standard breakfast, as compared with levels in the absence of aspirin ingestion. Aspirin was shown to decrease the activity of ADH in the stomach of humans and experimental rats, but not the activity of rat liver ADH. Aspirin had no effect on blood alcohol levels in rats when alcohol was given directly into the circulation. These findings suggest that aspirin increases the blood levels of alcohol in humans by decreasing the metabolism of ethanol by gastric ADH. (Consumer Summary produced by Reliance Medical Information, Inc.)

Author: Baraona, Enrique, Lieber, Charles S., Roine, Risto, Gentry, R. Thomas, Hernandez-Munoz, Rolando

Publisher: American Medical Association

Publication Name: JAMA, The Journal of the American Medical Association

Subject: Health

ISSN: 0098-7484

Year: 1990



Aspirin, Alcohol dehydrogenase, Alcohol dehydrogenases, Stomach

High blood alcohol levels in women: the role of decreased gastric alcohol dehydrogenase activity and first-pass metabolism

Article Abstract:

Differences between the sexes have been observed in the metabolism of alcohol. Women tend to have higher blood alcohol concentrations than men when the same doses are taken. Also, women are more prone to alcohol-related liver disease. Although the liver is the primary site of ethanol (common alcohol) metabolism, local metabolism of alcohol has been reported in gastrointestinal tissue as well. Until recently, the gastrointestinal "first-pass metabolism" of alcohol has not been considered significant. The differences between the sexes were evaluated concerning the gastric oxidation of alcohol. These results were considered in conjunction with the long-term effects of alcohol consumption. This study included 20 men and 23 women; first-pass metabolism was determined after oral and intravenous administration of alcohol. Blood alcohol concentrations were measured and alcohol dehydrogenase activity was evaluated by gastric biopsies. Six men and six women were alcoholics. In the non-alcoholic women, the first-pass metabolism and gastric alcohol dehydrogenase activity were much lower than in their male counterparts, at 23 and 59 percent, respectively. The alcoholic men had lower rates of first-pass metabolism and gastric alcohol dehydrogenase levels when compared with the non-alcoholic men. Alcoholic women had the lowest rates of gastric dehydrogenase activity, and the first pass metabolism in these women was negligible. This provides additional evidence that women have a different and more pronounced physical reaction to alcohol. It was concluded that this vulnerability increases the risk of physical complications in female alcoholics. (Consumer Summary produced by Reliance Medical Information, Inc.)

Author: Frezza, Mario, di Padova, Carlo, Pozzato, Gabriele, Terpin, Maddalena, Baraona, Enrique, Lieber, Charles S.

Publisher: Massachusetts Medical Society

Publication Name: The New England Journal of Medicine

Subject: Health

ISSN: 0028-4793

Year: 1990



Analysis, Measurement, Women, Demographic aspects, Alcoholism, Alcohol, Ethanol, Alcohol use, Blood alcohol

Effects of ranitidine on blood alcohol levels after ethanol ingestion: comparison with other H2-receptor antagonists

Article Abstract:

Ranitidine (Zantac), one of the most frequently-used drugs in the United States, may increase the level of alcohol in the blood by slowing its metabolism. Twenty men took the equivalent of 1.5 drinks of alcohol to measure their baseline blood alcohol levels. They were then given 150 milligrams (mg) of ranitidine twice a day for eight days. On days seven and eight, they were given the equivalent of 1.5 drinks either orally or intravenously one hour after taking the drug with breakfast. The men who drank the solution had higher blood alcohol levels after taking ranitidine than they did at baseline. Those taking alcohol intravenously did not. Six men were then given cimetidine and six famotidine. While cimetidine also caused increased blood alcohol levels over baseline, famotidine did not. Patients taking ranitidine or cimetidine (Tagamet) should be warned of their affects on blood alcohol levels.

Author: Frezza, Mario, Baraona, Enrique, Lieber, Charles S., Roine, Risto, Gentry, R. Thomas, DiPadova, Carlo

Publisher: American Medical Association

Publication Name: JAMA, The Journal of the American Medical Association

Subject: Health

ISSN: 0098-7484

Year: 1992



Antiulcer agents, Ranitidine, Antiulcer drugs, Cimetidine, Famotidine

Subjects list: Physiological aspects, Alcohol metabolism