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 followings were found: 1. 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. 2. 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. 3. 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. 4. The cephem antibiotics elevating the AcH level in the blood all had a (1-methy1-1H-tetrazol-5-yl) thiomethyl group in the 3 position of the aminocephalosporanic acid nucleus. 5. It was though that the disulfiram-like reaction caused by the cephem antibiotics was derived from the elevation of AcH level in the blood. 6. The disulfiram-like reaction was presumed to take place through the mechanism that the antibiotics, when injected intravenously, might be excreted into the bile to be metabolized in the intestinal tract, where they might release TZ, which in turn might inhibit aldehyde dehydrogenase. 7. The patient on treatment with or not more than 7 days after treatment with the cephem antibiotics causative of this phenomenon should refrain from the ingestion of alcohol-containing liquor.
Cefminox (CMNX, MT-141) is a new injectable cephamycin antibiotic, which was studied for its antibacterial activity, absorption and excretion after administration and clinical efficacy of patients with infections. The following results were obtained. 1. Antibacterial activity The antibacterial activity of CMNX against 19 clinical isolates consisting of 11 species made the results that its activity against E. coli, P. vulgaris and C. jejuni was superior to CMZ and CEZ. 2. Concentration in serum and urine CMNX was given intravenously to 3 groups at 20mg/kg by one shot (2 cases), 40mg/kg by one shot (2 cases) and 40mg/kg by 1 hour drip infusion (1 case). The half-lives were between 1.15 to 1.80 hours. We obtained over 70% of its excretion to urine within 6 hours after injection. 3. Clinical efficacy Clinical evaluation was made on a total of 18 patients with various infections, 11 of whom had underlying diseases. The result was excellent in 1 case, good in 11 cases, fair in 2 cases and poor in 4 cases, and the effective rate was 66.7%. 4. Side effect Clinical and laboratory abnormal findings related to CMNX were not found. It is concluded that CMNX seems to be effective and safetive antibiotic in the field of pediatrics.