In vitro antimicrobial activity of me1207 and its therapeutic efficacy in respiratory infections

Akira Watanabe, Yoshihiro Honda, Yutaka Tokue, Naoto Kitamura, Satoru Shoji, Hiroaki Kikuchi, Masakichi Motomiya

Research output: Contribution to journalArticlepeer-review

Abstract

ME1207, an ester derivative of ME1206, has been developed in Japan as a new cephem for oral use. We measured the in vitro antimicrobial activity of ME1206 by the broth dilution method and evaluated the therapeutic efficacy of ME1207 in respiratory tract infections. The minimum inhibitory concentrations (MICs) of ME1206, cefixime (CFIX), cefteram (CFTM), cefaclor (CCL) and ampicillin (ABPC) against 20 strains each of methicillin-sensitive Staphylococcus aureus (MSSA), methicillin-resistant Staphylococcus aureus (MRSA), Haemophilus influenzae and Pseudomonas aeruginosa, and 18 strains each of Escherichia coli, Klebsiella pneumoniae, Enterobacter cloacae and Serratia marcescens were determined by the micro-broth dilution method using the Dynatech MIC 2000 system. As shown by the MICs, ME1206 was more active than the other agents against MSSA. All agents tested had no potent activity against either MRSA or P. aeruginosa. Against H. influenzae and Enterobacteriaceae, ME1206 was somewhat more active than CFTM, but less active than CFIX. Daily dose of 300 mg (11 cases) or 600 mg (21 cases) of ME1207 were given orally to 32 patients for 3 to 14 days (mean: 10.5 days): 1 patient with acute pharyngitis, 2 with acute bronchitis, 8 with chronic respiratory infections and 21 with acute pneumonia. The clinical efficacy was excellent in 9, good in 19, fair in one and poor in one. Two cases were excluded from the clinical evaluation; one case because of Mycoplasma pneumoniae pneumonia and the other because of only two days treatment to develope adverse reactions. Fourteen causative organisms were identified 1 strain of S. aureus, 4 strains of Streptococcus pneumoniae, 1 strain of Streptococcus pyogenes, 3 strains of Branhamella catarrhalis, 4 strains of H. influenzae and 1 strain of P. aeruginosa. Eleven of 13 strains, against which the bacteriological effects could be evaluated, were eradicated. Nausea was observed in one patient. Eosinophilia was observed in three patients and an elevation of transaminase was observed in two patients, but these returned to normal after completion of the therapy. From these results, we conclude that ME 1207 is one of the most useful cephem agents for oral use as first choice drug in the treatment of respiratory tract infections in out-patient clinics.

Original languageEnglish
Pages (from-to)316-326
Number of pages11
JournalChemotherapy
Volume40
DOIs
Publication statusPublished - 1994 Jan 1
Externally publishedYes

ASJC Scopus subject areas

  • Pharmacology (medical)
  • Infectious Diseases
  • Pharmacology
  • Drug Discovery
  • Oncology

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