LABORATORY AND CLINICAL STUDIES ON CEFOTAXIME

• Published in: CHEMOTHERAPY Vol. 28; no. Supplement1; pp. 406 - 435
• Main Authors: NAKATOMI, MASAO, NASU, MASARU, SAITO, ATSUSHI, TSUTSUMI, TSUNEO, HIROTA, MASAKI, IZUMIKAWA, KINICHI, IWASAKI, HIROMARO, SHIGENO, YOSHITERU, TOMONAGA, AKIMITSU, TANAKA, HIKARU, NAKASONE, KEISHUN, HARA, KOHEI, MOCHIDA, CHIKAKO, SAWATARI, KATSUHIKO, IORI, FUMIAKI, HAYASHI, Ai
• Format: Journal Article
• Language: Japanese
• Published: Japanese Society of Chemotherapy 01.01.1980
• ISSN: 0009-3165; 1884-5894
• DOI: 10.11250/chemotherapy1953.28.Supplement1_406

Laboratory and clinical studies were made on cefotaxime (HR 756, CTX), a new cephalosporin antibiotic with the following results. Cefotaxime was compared with cefazolin (CEZ), cefamandole (CMD), cefotiam (CTM), cefmetazole (CMZ), ampicillin (ABPC), ticarcillin (TIPC), chloramphenicol (CP) and sulbenicillin (SBPC) in antibacterial activity against 22 standard strains and 950 routine clinical isolates. The minimum inhibitory concentration (MIC) of cefotaxime against gram-positive cocci was higher than those of CEZ, CMD, CTM and CMZ. Cefotaxime showed lower MICs against gram-negative bacilli than these drugs tested excluding P. maltophilia and Flavobacterium spp. Cefotaxime was administered to three patients at a dose of 1, 000 mg and two patients at a dose of 2, 000 mg by intravenous drip infusion for one to two hours, and peak serum levels of 52-67 μg/ml and 92-127 μg/ml were obtained at the end of infusion, respectively. Urinary recovery rate after injection of 1, 000 mg was 57.3%. The peak sputum concentration was 0.07 μg/ml in the sputum of a patient with chronic bronchitis due to H. influenzae 2-3 hours after infusion of 1, 000 mg, and H. influenzae began to decrease in number from 108-109/ml and was eliminated from the sputum around 5-6 hours after injection. P. maltophilia was not eliminated from the sputum of another chronic bronchitis patient as though cefotaxime penetrated into her sputum at the peak level of 0.04 μg/ml after injection of 1, 000 mg. The peak sputum concentration of 0.2 μg/ml was assayed 1-2 hours after the end of infusion of 2, 000 mg. Cefotaxime was given to a total of 29 patients-17 with pneumonia, 7 with chronic bronchitis, 1 with lung abscess, 1 with P. T. B. and 3 with pyelonephritis-by intravenous drip infusion for 6-18 days. Eighteen out of 22 patients evaluable responded effectively to cefotaxime treatment for an efficacy rate of 81.8%. Total 10 cases showed the following adverse reaction of the drug: transient chills, and high fever at an early stage after starting i. v. treatment in 6 cases, eruption with or without itching in 3 and a slight elevation of S-GOT and S-GPT in 1.