Ethanol, Acetaldehyde, Acetate, and Lactate Levels After Alcohol Intake in White Men and Women: Effect of 4-Methylpyrazole

Background: 4‐Methylpyrazole (4‐MP), a selective inhibitor of alcohol dehydrogenase (ADH), recently has been approved for clinical use in humans. The objective was to evaluate the use of 4‐MP in human alcohol research and to study the effect of 4‐MP on various parameters of alcohol metabolism during alcohol intoxication. Methods: 4‐MP (10–15 mg/kg orally) or placebo was given in double‐blind fashion to 22 premenopausal women, 12 of whom were using oral contraceptives, and 13 men followed by intake of alcohol (0.5 g/kg orally) or placebo. Results: A 30% to 40% decrease in the ethanol elimination rate was observed in the different groups during pretreatment with 4‐MP. The alcohol‐induced increase in plasma acetate was partially inhibited by 4‐MP. A significant positive correlation was observed between the effect of 4‐MP on the alcohol‐induced lactate and acetate elevations. The acetaldehyde was nondetectable (