<I>In vitro</I> antimicrobial activity, penetration into sputum and therapeutic efficacy of S-1108 in respiratory tract infections

DOI
  • Watanabe Akira
    Department of Internal Medicine, The Research Institute for Chest Diseases and Cancer, Tohoku University
  • Honda Yoshihiro
    Department of Internal Medicine, The Research Institute for Chest Diseases and Cancer, Tohoku University
  • Tokue Yutaka
    Department of Internal Medicine, The Research Institute for Chest Diseases and Cancer, Tohoku University
  • Kitamura Naoto
    Department of Internal Medicine, The Research Institute for Chest Diseases and Cancer, Tohoku University
  • Shoji Satoru
    Department of Internal Medicine, The Research Institute for Chest Diseases and Cancer, Tohoku University
  • Kikuchi Hiroaki
    Department of Internal Medicine, The Research Institute for Chest Diseases and Cancer, Tohoku University
  • Motomiya Masakichi
    Department of Internal Medicine, The Research Institute for Chest Diseases and Cancer, Tohoku University
  • Konno Kiyoshi
    Department of Internal Medicine, Tohoku Chuo Hospiatal
  • Sayama Tsuneo
    Department of Internal Medicine, Tohoku Chuo Hospiatal
  • Shindo Satoshi
    Department of Internal Medicine, Tohoku Chuo Hospiatal
  • Honma Mitsunobu
    Third department of Internal Medicine, Akita Municipal Hospital

Bibliographic Information

Other Title
  • S-1108の<I>in vitro</I>抗菌力と喀痰内移行および呼吸器感染症に対する臨床効果の検討

Abstract

We measured the in vitro antimicrobial activity, and serum and sputum concentrations of S-1108, a new oral cephem developed in Japan, and evaluated its therapeutic efficacy in respiratory tract infections. The minimum inhibitory concentrations (MICs) of 5-1006, cefixime (CFIX), cefteram pivoxil (CFTM-PI) and cefaclor (CCL) against 20strains each of methicillin-susceptible Staphylococcs aureus (MSSA), methicillin-resistant Stphylococcus aureus (MRSA), Haemophilus influenzae, Escherichia coli, Klebsiella pneumoniae, Enterobacter cloacae, Serratia marcescens and Pseudomonas aeruginosa were determined, . by the micro-broth dilution method using the Dynatech MIC 2000 system. As shown by the MICs, S-1006 was more active than the others against MSSA, H. influenzae and P. aeruginosa. Against Enterobacteriaceae, 5-1006 was as active as cefteram and cefixime. No agents tested displayed potent activity against either MRSA or P. aeruginosa. The concentration of S-1006 in the serum of the three patients with bronchiectasis was highest 2 to 3 hours after oral administration of 200 mg (2.17, 1.08 and 0.66 μg/ml). Thereafter, the maximum concentrations of S-1006 achieved in sputum were 0.04, 0.06, and 0.03 μg/ml, respectively. Thus, the maximum penetration rates were 1.84, 5.56 and 4.55%, respectively (mean: 3.98%). An oral dose of 300-600 mg of S-1108 was given daily to 25 patients for 5 to 15 days (mean: 9.3 days): 4 with acute bronchitis, 5 with chronic respiratory infections, 14 with acute pneumonia and one each with pulmonary tuberculosis and secondary infection in lung cancer. Three patients were excluded from clinical evaluation because one patient was diagnosed as having active pulmonary tuberculosis and two were seen in the outpatient clinic only once. Clinical efficacy was excellent in 2 patients and good in 20 (efficacy rate: 100%). Nineteen strains were identified as causative organisms: 1 strain of S. aureus, 6 strains of Streptococcus pneumoniae, 6 strains of Branhamella catarrhalis, 3 strains of H. influenzae, 1 strain of K. pneumoniae and 2 strains of P. aeruginosa. Fourteen out of 18 strains against which bacteriological effects could be evaluated were eradicated by administration of S-1108. Diarrhea was observed in three patients. Eosinophilia and elevation of transaminase values were observed in four patients each, but the adverse reactions disappeared after completion of therapy From the above results, we conclude that S-1108 is one of the most useful cephems for oral use as an agent of first choice in the treatment of respiratory tract infections in outpatient clinics.

Journal

  • CHEMOTHERAPY

    CHEMOTHERAPY 41 (Supplement1), 217-230, 1993

    Japanese Society of Chemotherapy

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