Department of Basic Sciences, College of Veterinary Medicine, Mississippi State University, MS, United States.
Department of Basic Sciences, College of Veterinary Medicine, Mississippi State University, MS, United States.
Alcohol. 2020 Dec;89:9-17. doi: 10.1016/j.alcohol.2020.03.011. Epub 2020 Apr 4.
Binge drinking is a remarkably prevalent behavior. In 2015, 27% of U.S. residents 18 years old or older reported at least one episode of binge drinking in the previous month. Rodent models for binge drinking are widely used to study the mechanisms by which alcohol causes a variety of adverse health effects in humans. Concerns have been raised that many binge-drinking studies in rodents involve alcohol doses that would be unrealistically high in humans. Allometric dosage scaling can be used to estimate the dose of a drug or chemical in mice that would be necessary to achieve similar biological effects at a realistic dose in humans. However, it has become apparent that no single allometric conversion factor is applicable for all drugs and chemicals, so it is necessary to evaluate each compound empirically. In the present study, we compared the area under the blood alcohol concentration vs. time curve (AUC) and the peak blood alcohol concentration following oral alcohol administration at various doses in mice and humans, using data from previously published studies. The results demonstrated that the oral dose of alcohol must be larger in mice (on a g of alcohol to kg of body weight basis) than in humans to achieve similar alcohol AUC values or to achieve similar peak concentrations in the blood. The dose required in mice was about 2-fold greater than the dose required in humans to achieve similar alcohol AUC and peak concentrations. The results shown here were substantially different from the average 5-12-fold difference between mice and humans calculated in previous studies using agents other than alcohol. Results shown here demonstrate that an empirical approach using data from several independent experiments provides information needed to determine the alcohol dose in mice that produces a similar level of exposure (AUC and peak concentration) as in humans. The results indicate that a single alcohol dose in the range of 5-6 g/kg, a range often used in mouse models for binge drinking, is not excessive when modeling human binge drinking. Results presented here illustrate that in mice both alcohol AUC and peak alcohol concentration correlate well with an important biological effect - activation of the hypothalamic-pituitary-adrenal axis - as indicated by increased corticosterone AUC values.
binge drinking 是一种非常普遍的行为。2015 年,美国 18 岁及以上的居民中有 27%报告在过去一个月至少有一次 binge drinking 行为。用于 binge drinking 的啮齿动物模型被广泛用于研究酒精导致人类各种不良健康影响的机制。人们担心,许多啮齿动物 binge drinking 研究中的酒精剂量在人类中是不现实的高剂量。同种异体剂量标度可用于估计在小鼠中达到类似生物学效应所需的药物或化学物质的剂量,这是在人类中达到合理剂量的实际剂量。然而,很明显,没有单一的同种异体转化因子适用于所有药物和化学物质,因此有必要对每个化合物进行经验评估。在本研究中,我们比较了口服酒精给药后不同剂量下的小鼠和人体内的血液酒精浓度-时间曲线下面积(AUC)和峰值血液酒精浓度,使用了之前发表的研究数据。结果表明,为了达到相似的 AUC 值或达到相似的血液峰值浓度,必须在小鼠中使用比人类更大的口服酒精剂量(按酒精克数与公斤体重比计算)。在小鼠中所需的剂量约为人类所需剂量的 2 倍,以达到相似的 AUC 和峰值浓度。与之前使用除酒精以外的其他试剂进行的研究中计算出的平均 5-12 倍差异相比,这里显示的结果有很大不同。这里显示的结果表明,使用来自几个独立实验的数据的经验方法提供了确定在小鼠中产生相似暴露水平(AUC 和峰值浓度)所需的酒精剂量所需的信息。结果表明,在模型模拟人类 binge drinking 时,5-6 g/kg 的范围内的单一酒精剂量是不过量的,这个剂量范围通常用于小鼠 binge drinking 模型。这里呈现的结果表明,在小鼠中,酒精 AUC 和峰值酒精浓度与一个重要的生物学效应(下丘脑-垂体-肾上腺轴的激活)密切相关,这表现为皮质酮 AUC 值的增加。