Ceftizoxime (FK749) に関する基礎的・臨床的研究

書誌事項

タイトル別名
  • LABORATORY AND CLINICAL STUDIES ON CEFTIZOXIME (FK 749) A NEW CEPHALOSPORIN ANTIBIOTIC
  • Ceftizoxime FK749 ニ カンスル キソテキ リンショウテキ ケ

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Laboratory and clinical studies on ceftizoxime (FK 749), a newly developed cephalosporin derivative, were carried out with the following results.<BR>The in vitro antibacterial activity of ceftizoxime against 22 standard strains and 763 routine clinical isolates including gram-positive cocci, Enterobacteriaceae glucose non-fermentative gram-negative bacilli and Haemophilus species was compared with that of cefazolin, cefotiam, cefamandole, cefmetazole, ampicillin and piperacillin. Ceftizoxime was less active against Staphylococcus aureus and Staphylococcus epidermidis than cefazolin, cefotiam, cefamandole, cefmetazole but was the most active of the antibiotics tested against Exherichia coli, Klebsiella aerogenes, Enterobacter cloacae, Enterobacter aerogenes, Citrobacter freundii, Protaus vulgaris, Pr. mirabilis, Pr. rettgeri, Pr. inconstans, Serratia marcescens, Haemophilus parainfluenzao and H. influenzae. Ceftizoxime was also given to ten healthy adult volunteers in single doses of 250 and 500 mg in a cross over study.<BR>Mean peak serum levels were 14.3μg/ml at a dose of 250 mg and 27.0μg/ml at a dose of 500mg. Urinary recovery rate for both doses was about 80 per cent for 6 hours after the end of intravenous drip infusion.<BR>Peak serum levels of ceftizoxime were 84-101μg/ml after intravenous drip infusion of 1 gram, and 90-210μg/ml after intravenous drip infusion of 2 grams. Urinary recovery rates were 68.3-95. 6 per cent.<BR>Peak sputum levels of ceftizoxime were 0.29-1.8μg/ml in the 6 patients with chronic bronchitis after intravenous drip infusion of 1-2 grams.<BR>Biliary level of ceftizoxime after intravenous drip infusion of 2 grams was about 0.07μg/mI. HaemoPhilus influenzae in the sputum of a patient with chronic bronchitis began to decrease from the initial 108 cells/nil to 104 cells/ml for the first 10 hours after intravenous drip infusion of 1 gram, and peak sputum level was 0.29μg/ml in this patient. This organism was eliminated from the sputum on the second day of treatment.<BR>Pseudomonas aeruginosa isolated from the sputum was stable at about 105 cells/ml throughout the treatment period.<BR>Twenty-eight patients with pulmonary, pleural, urinay, biliary or peritoneal infection were treated with ceftizoxime by intravenous drip infusion. Twenty one of the 27 patients responded satisfactorily to the tettment and the effectiveness rate was 77.8%.<BR>One strain of Streptococcus pneumoniae, 1 of β-Streptococcus, 7 of H. influenzae, 2 of E. coli, 2 of Kl. aerogenes, 1 of Ent. aerogenes and 2 of Ps. aeruginosa were eliminated and the bacteriological efficacy rate was 83.3%. Serum transaminase value increased slightly in one patient.

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