Effects of beta-lactam antibiotics and N-methyltetrazolethiol on the alcohol-metabolizing system in rats.
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概要
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The disulfiram-like effect of various beta-lactam antibiotics containing N-methyltetrazolethiol (NMTT) on the alcohol-metabolizing system was studied using rats. Their administration caused decreased activities in low K<SUB>m</SUB> aldehyde dehydrogenase (ALDH) and acetaldehyde oxidation in the liver, with marked depression from several hours to 2 days after the treatment. Blood acetaldehyde level increased markedly when ethanol was administered 18-24 hr after pretreatment with antibiotics. A similar time course change in the effect was obtained when disulfiram was administered. The following results obtained in the present study indicate that the disulfiram-like effect associated with these antibiotics was not mediated by the whole molecular structures of these drugs: Firstly, the antibiotics were eliminated rapidly from the plasma and liver, and the disulfiram-like effect was followed by a disappearance of the drugs. Secondly, the concentration of antibiotics required to inhibit mitochondrial low K<SUB>m</SUB> ALDH activity in vitro was very high compared with their liver concentration. Thirdly, rapid onset of disulfiram-like effects occurred after administration of NMTT itself, and a pronounced elevation of blood acetaldehyde level was observed when ethanol was administered 3-5 hr after the NMTT injection. Fourthly, almost the same amounts of NMTT were released in the body after the intravenous administration of various NMTT-containing antibiotics, as judged by the urinary excretion. These results suggest that the disulfiram-like effect of beta-lactam antibiotics is mediated by NMTT released from them.
- 公益社団法人 日本薬理学会の論文
著者
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Yoshida Tadashi
Shionogi Research Laboratories Shionogi & Co. Ltd.
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Kawamoto Keiko
Shionogi & Co. Ltd.
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Sugeno Koichi
Shionogi Research Laboratories Shionogi & Co. Ltd.
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OTSUBO Shigemi
Shionogi Research Laboratories, Shionogi & Co., Ltd.
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OGAWA Ayako
Shionogi Research Laboratories, Shionogi & Co. Ltd.
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Matsubara Takashi
Shionogi Research Laboratories
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TOCHINO Yoshihiro
Shionogi Research Laboratories, Shionogi & Co. Ltd.
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TOCHINO Yoshihiro
Shionogi Research Laboratories, Shionogi & Co. Ltd.
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OKAMOTO Joji
Shionogi Research Laboratories, Shionogi & Co. Ltd.
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HIRAI Eizo
Shionogi Research Laboratories, Shionogi & Co. Ltd.
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KAWAMOTO Keiko
Shionogi Research Laboratories, Shionogi & Co. Ltd.
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OKAMOTO Joji
Shionogi Research Laboratories, Shionogi & Co. Ltd.
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HIRAI Eizo
Shionogi Research Laboratories, Shionogi & Co. Ltd.
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SUGENO Koichi
Shionogi Research Laboratories, Shionogi & Co. Ltd.
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