DiPadova C, Roine R, Frezza M, Gentry R T, Baraona E, Lieber C S
Section of Liver Diseases and Nutrition, Bronx Veterans Affairs Medical Center 10468.
JAMA. 1992 Jan 1;267(1):83-6.
To determine whether the H2-receptor antagonist, ranitidine, which is a potent inhibitor of gastric alcohol dehydrogenase activity in vitro, increases the bioavailability of orally administered ethanol (0.3 g/kg of body weight) and to compare the resulting blood alcohol concentrations with those of two other H2-antagonists, cimetidine and famotidine, the latter of which does not inhibit gastric alcohol dehydrogenase.
For each of the H2-receptor antagonists, a different group of subjects was used. In each group, a paired design was adopted with each subject serving as his own control.
Hospital laboratory.
Normal, healthy men aged 24 to 46 years.
Eight men were treated for 1 week with ranitidine (300 mg/d), six with cimetidine (1000 mg/d), and six with famotidine (40 mg/d).
Peak blood alcohol concentrations, areas under the blood alcohol curve, first-pass metabolism, and bioavailability of orally consumed ethanol.
Relative to baseline, ranitidine increased the mean peak concentration and the area under the curve of blood alcohol concentrations by 34% (P less than .05) and 41% (P less than .01), respectively. First-pass metabolism of ethanol was decreased from 70 +/- 10 to 31 +/- 9 mg/kg of body weight, with a corresponding increase in ethanol bioavailability of 79.6% to 92.6%. By comparison, cimetidine had even a greater effect on blood alcohol levels, while famotidine had no significant effects.
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.
确定H2受体拮抗剂雷尼替丁（在体外是胃酒精脱氢酶活性的有效抑制剂）是否会增加口服乙醇（0.3 g/kg体重）的生物利用度，并将由此产生的血醇浓度与另外两种H2拮抗剂西咪替丁和法莫替丁的血醇浓度进行比较，其中法莫替丁不抑制胃酒精脱氢酶。
对每种H2受体拮抗剂使用不同组的受试者。在每组中，采用配对设计，每个受试者作为自己的对照。
医院实验室。
年龄在24至46岁之间的正常健康男性。
8名男性接受雷尼替丁（300 mg/天）治疗1周，6名接受西咪替丁（1000 mg/天）治疗，6名接受法莫替丁（40 mg/天）治疗。
血醇峰值浓度、血醇曲线下面积、首过代谢以及口服乙醇的生物利用度。
相对于基线，雷尼替丁使血醇浓度的平均峰值浓度和曲线下面积分别增加了34%（P<0.05）和41%（P<0.01）。乙醇的首过代谢从70±10降至31±9 mg/kg体重，乙醇生物利用度相应从79.6%增至92.6%。相比之下，西咪替丁对血醇水平的影响更大，而法莫替丁没有显著影响。
应警告接受雷尼替丁或西咪替丁治疗的患者，在饮用在无此类治疗时被认为安全的乙醇量后可能出现功能损害。
