Cephem antibiotics and alcohol metabolism.
Mechanisms of the disulfiram-like reaction of cephem antibiotics were studied. Changes in ethanol (EtOH) and acetaldehyde (AcH) levels in the blood with EtOH loading following daily intravenous administration of cephem antibiotics were determined in rats and the following were found: The daily intravenous injection of cefazolin, cefotiam (CTM), cefsulodin, cefoxitin or ceftizoxime in no way varied the changes in the EtOH and AcH levels in the blood with EtOH loading. The daily intravenous injection of cefmetazole, cefoperazone, cefamandole, latamoxef, cefmenoxime or cefotetan caused the AcH level in the blood to be elevated significantly until at least 8 hours after the EtOH loading, but was inert on the EtOH level on the blood. The daily administration of 1-methyl-2-tetrazoline-5-thione (TZ), a compound having a partial structure similar to those of the cephem antibiotics elevating the AcH level in the blood on EtOH loading, was inert on the EtOH level in the blood but elevated the AcH level in the blood. The daily administration of 1-(2-dimethylaminoethyl)-2-tetrazoline-5-thione (MTZ), a compound having a partial structure similar to that of CTM, was inert either on the EtOH or AcH level in the blood. The cephem antibiotics elevating the AcH level in the blood all had a (1-methyl-1H-tetrazol-5-yl) thiomethyl group in the 3 position of the aminocephalosporanic acid nucleus. It was though that the disulfiram-like reaction caused by the cephem antibiotics was derived from the elevation of AcH level in the blood.(ABSTRACT TRUNCATED AT 250 WORDS)
D000079:Acetaldehyde / Q000097:blood*; D000427:Alcohol Deterrents / Q000494:pharmacology*; D000818:Animals; D001652:Bile Ducts; D002437:Cefazolin / Q000494:pharmacology; D002439:Cefotaxime / Q000031:analogs & derivatives / Q000494:pharmacology; D015310:Cefotiam; D002441:Cefsulodin / Q000494:pharmacology; D002511:Cephalosporins / Q000008:administration & dosage / Q000494:pharmacology*; D000431:Ethanol / Q000097:blood*; D007275:Injections, Intravenous; D008026:Ligation; D051381:Rats; D011919:Rats, Inbred Strains
D000427:Alcohol Deterrents; D002511:Cephalosporins; D000431:Ethanol; D015310:Cefotiam; D000079:Acetaldehyde; D002437:Cefazolin; D002439:Cefotaxime; D002441:Cefsulodin