Laboratory and clinical studies of loracarbef

Kotaro Mitsutake, Yuko Yoshitomi, Yoshitsugu Miyazaki, Haruko Matsuda, Yasuhito Higashiyama, Shigefumi Maesaki, Masanori Iwamoto, Kenichi Tanaka, Hironobu Koga, Shigeru Kohno, Kohei Hara, Chikako Mochida, Kazuyuki Sugawara, Mitsuo Kaku, Tohru Morikawa, Yuichi Inoue, Naofumi Suyama, Kouichi Watanabe, Kiyo Fujita, Tetsuro KandaMasao Nakatomi

Research output: Contribution to journalArticlepeer-review

Abstract

A newly developed oral carbacephem, loracarbef (LCBF), was evaluated in vitro and in vivo in comparison with cefaclor (CCL), cefixime, cefotiam and amoxicillin. The results were as follows. 1. Antimicrobial activity: Minimal inhibitory concentrations (MICs) against 419 clinical isolates including 12 different species were determined by the microbroth dilution method. LCBF showed good antimicrobial activity against gram-positive and -negative bacteria except methicillin-resistant Staphylococcus aureus, Enterococcus faecalis, Pseudomonas aeruginosa and Acinetobacter anitratus. The MICs of LCBF were almost the same as those of the first-generation oral cephem, CCL. 2. LCBF concentration in plasma and sputum: Two patients with diffuse panbronchiolitis were given 200 mg or 400 mg of LCBF orally, and its concentrations in plasma and sputum were measured at intervals using HPLC. The peak concentrations of LCBF in the serum and sputum of a patient administered 200 mg were 8.34 and 0.47 μg/ml, respectively, and those of a patient administered 400 mg were 16.1 and 0.36 μg/ml, respectively. From these data, it was suggested that LCBF had good penetration into the blood and lung. 3. Clinical efficacy and adverse reaction: Twenty-one patients with respiratory tract infections were treated with LCBF, and the overall efficacy rate was 65% (good in 13, fair in 3, poor in 4, not evaluable in 1). Stomach discomfort was observed as a side effect.

Original languageEnglish
Pages (from-to)235-241
Number of pages7
JournalChemotherapy
Volume41
DOIs
Publication statusPublished - 1993 Jan 1

ASJC Scopus subject areas

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

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