In Vivo Interactions Between H2‐Receptor Antagonists and Ethanol Metabolism in Man and in Rats
In Vivo Interactions Between H2‐Receptor Antagonists and Ethanol Metabolism in Man and in Rats
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人和大鼠体内 H2 受体拮抗剂与乙醇代谢之间的相互作用
DOI：
10.1002/hep.1840040623
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发表时间：
1984
期刊：
影响因子：
13.5
通讯作者：
B. Kommerell
中科院分区：
文献类型：
--
作者：
H. Seitz;Siegrid Veith;P. Czygan;J. Bösche;Bernd Simon;Roland Gugler;B. Kommerell
在8名男性志愿者中进行的一项随机安慰剂对照研究中，研究了西咪替丁（1，000 mg/天）或雷尼替丁（300 mg/天）给药7天对单次口服乙醇（0.8 gm/kg体重）后血清乙醇浓度的影响。与安慰剂相比，西咪替丁而不是雷尼替丁使血清乙醇浓度峰值（85.9 ± 3.5 vs. 73.0 ± 3.2 mg dl−1，p < 0.02）和血清乙醇浓度时间曲线下面积（350 ± 19 vs. 304 ± 25 mg dl−1 hr−1，p < 0.05）显著增加。然而，西咪替丁对乙醇消除率没有影响。当静脉注射乙醇（1.0 gm/kg体重）时，西咪替丁不能诱导乙醇代谢的变化。此外，在动物实验中研究了H2受体拮抗剂的作用。雌性Sprague-道利大鼠接受单次乙醇（7或3 gm/kg体重）给药，同时腹膜内注射西咪替丁（120 mg/kg体重）、雷尼替丁（120 mg/kg体重）或等渗盐水。在酒精吸收后，西咪替丁和二甲双胍均显著抑制乙醇消除（3.99 ± 0.39与5.68 ± 0.23 mmol kg−1 hr−1，p < 0.02）和雷尼替丁（4.21 ± 0.14与5.68 ± 0.23 mmol kg−1 hr−1，p < 0.02），但在血液乙醇浓度低于20 mM时则无。这些结果表明，当乙醇血清浓度低于20 mM时，人体对西咪替丁而非雷尼替丁的乙醇吸收增加。在乙醇血清浓度高于20 mM时，两种H2受体拮抗剂均抑制大鼠的乙醇消除，表明抑制微粒体乙醇氧化。
The influence of a 7‐day medication of either cimetidine (1,000 mg per day) or ranitidine (300 mg per day) on serum ethanol concentrations after a single oral dose of ethanol (0.8 gm per kg body weight) was investigated in a randomized placebo‐controlled study in eight male volunteers. Compared with the placebo, cimetidine but not ranitidine produced a significant increase in both the peak serum ethanol concentration (85.9 ± 3.5 vs. 73.0 ± 3.2 mg dl−1, p < 0.02) and in the area under the serum ethanol concentration time curve (350 ± 19 vs. 304 ± 25 mg dl−1 hr−1, p < 0.05). However, the ethanol elimination rate was not affected by cimetidine. When ethanol (1.0 gm per kg body weight) was administered intravenously, cimetidine failed to induce a change in ethanol metabolism. Furthermore, the effect of H2‐receptor antagonists was studied in animal experiments. Female Sprague‐Dawley rats received a single dose of ethanol (7 or 3 gm per kg body weight) together with an intraperitoneal injection of either cimetidine (120 mg per kg body weight), ranitidine (120 mg per kg body weight) or isotonic saline. After alcohol absorption, ethanol elimination was significantly inhibited by both cimetidine (3.99 ± 0.39 vs. 5.68 ± 0.23 mmoles kg−1 hr−1, p < 0.02) and ranitidine (4.21 ± 0.14 vs. 5.68 ± 0.23 mmoles kg−1 hr−1, p < 0.02) at high ethanol concentrations (60 to 20 m M) but not at blood ethanol concentrations below 20 m M. These results suggest an increase in ethanol absorption due to cimetidine but not to ranitidine in man at ethanol serum concentrations below 20 m M. At ethanol serum concentrations above 20 m M, both H2‐receptor antagonists inhibit ethanol elimination in the rat suggesting inhibition of microsomal ethanol oxidation.
西咪替丁减少肝血流量和普萘洛尔代谢。
DOI：
10.1056/nejm198103193041202
发表时间：
1981
期刊：
The New England journal of medicine
影响因子：
--
作者：
Feely,J;Wilkinson,GR;Wood,AJ
通讯作者：
Wood,AJ
西咪替丁对正常志愿者茶碱清除率和半衰期的改变。
影响因子：
39.2
作者：
Reitberg,DP;Bernhard,H;Schentag,JJ
通讯作者：
Schentag,JJ