Inoue K, Kera Y, Kiriyama T, Komura S
Jpn J Pharmacol. 1985 May;38(1):43-8. doi: 10.1254/jjp.38.43.
Alcohol-sensitive Japanese subjects with facial flushing and an increase in heart rate during ethanol intoxication exhibited marked individual variation in accumulation of acetaldehyde. This variation correlated well with the intensity of the above mentioned physiological responses. Oral pretreatment with 10 mg/kg 4-methylpyrazole, which inhibited the ethanol elimination rate by 15-25%, strongly suppressed both acetaldehyde accumulation and the associated responses. Under this condition, the sensitivity to acetaldehyde appeared to be reduced, and the correlation between the acetaldehyde level and the physiological responses disappeared. The effectiveness of even a low dose of 4-methylpyrazole suggests its clinical usefulness for alleviation of acute acetaldehyde toxicity in alcohol-hypersensitive Japanese individuals as well as in disulfiram-treated alcoholics.
对酒精敏感的日本受试者在乙醇中毒期间出现面部潮红和心率加快，其乙醛蓄积存在明显的个体差异。这种差异与上述生理反应的强度密切相关。口服10 mg/kg 4-甲基吡唑进行预处理，可使乙醇消除率降低15%-25%，能强烈抑制乙醛蓄积及相关反应。在此条件下，对乙醛的敏感性似乎降低，乙醛水平与生理反应之间的相关性消失。即使是低剂量的4-甲基吡唑也有效，这表明它在减轻酒精过敏的日本个体以及接受双硫仑治疗的酗酒者的急性乙醛毒性方面具有临床应用价值。
