Detail of "85287-61-2"

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Antibacterial activity, absorption, excretion, metabolism, distribution to organs and clinical use in surgical infection of a new cephalosporin antibiotic, AC-1370

Antibacterial activity, absorption, excretion, metabolism, distribution to organs and clinical use in surgical infection of a new cephalosporin antibiotic, AC-1370. Nakayama, Issei; Akieda, Yozo; Kawamura, Hiroshi; Kawaguchi, Hiroshi; Yamaji, Emiko; Ishiyama, Shunji (Sch. Med., Nihon Univ., Tokyo 173, Japan). Chemotherapy (Tokyo), 32(Suppl. 9), 498-517 (Japanese) 1984. CODEN: NKRZAZ. ISSN: 0369-4682. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) Blood levels and urine concns. of AC-1370 [85287-61-2] were detd. by bioassay and HPLC in 3 healthy volunteers after i.v. injection of 1,000mg AC-1370. Peak serum levels of 121mg/mL (bioassay) and 122mg/mL (HPLC) were obsd. 5 min after treatment. Peak urine levels were 8, 167mg/mL (bioassay) and 7,867mg/mL (HPLC). Recovery in urine was 89.8% (bioassay) and 87.1° (HPLC) within 8 h. Pharmacokinetic parameters calcd. from the HPLC assay were K12 (h-,1): 2.86; K21(h-1): 2.79; Kel(h-1): 0.93; T1/2 (b)(h): 1.64; Vd(liter): 12.6; AUC(h×mg/mL): 1.73. AC-1370 was excreted in urine without being metabolized. When 20 mg/kg AC-1370 was administered i.m. to rats, the kidney level of the drug was the highest, followed by those in serum, heart and liver. Clin. response to AC-1370 in 13 cases of surgical infections was evaluated as excellent in 1 case, effective in 8 cases, and failure in 4 cases. No side effect was obsd.

Antibacterial activity of AC-1370 against anaerobes

Antibacterial activity of AC-1370 against anaerobes. Watanabe, Kunitomo; Bunai, Midori; Aoki, Makoto; Kagawa, Kazunobu; Sawa, Kakuyo; Ueno, Kazue (Sch. Med., Gifu Univ., Gifu 500, Japan). Chemotherapy (Tokyo), 32(Suppl. 9), 30-41 (Japanese) 1984. CODEN: NKRZAZ. ISSN: 0369-4682. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) Section cross-reference(s): 10 A bacteriol. evaluation with anaerobes was made of AC-1370 (I) [85287-61-2] as compared with other cephems. I showed a broad antianaerobic activity, its activity against gram-pos. cocci was inferior to that of cefoperazone (II), cefoxitin (III) or cephazoline (IV). Against gram-neg. rods, the activity of I was equal to or somewhat inferior to that of IV, II or III. Among the various species of anaerobes examd., I showed good activity against P. micros and C. ramosum, and less activity against the B. fragilis group, E. lentum, and C. difficile. I was hydrolyzed by b-lactamase derived from B. fragilis and B. bivius, however its hydrolysis rate was less than that of cefmenoxime (V). I showed greater therapeutic effect than V against exptl. polymicrobial infections in mice caused by E. coli and B. fragilis. Appearance of C. difficile in cecal contents was not obsd. when I was administered to mice at a dose of 2mg for 7 days, contrary to the case with cefotaxime and III.