Clinical efficacy of temafloxacin in respiratory infections and its pharmacokinetics in sputum

• Published in: CHEMOTHERAPY Vol. 41; no. Supplement5; pp. 361 - 368
• Main Authors: Tanimoto, Hiroichi, Nakatani, Tatsuo, Narui, Kouji, Nakamori, Yoshitaka, Nakata, Koichiro, Tsuboi, Eiyasu, Sugi, Hiroko
• Format: Journal Article
• Language: English; Japanese
• Published: Japanese Society of Chemotherapy 1993; 公益社団法人 日本化学療法学会
• Subjects: temafloxacin; 呼吸器感染症; 薬動力学的解析; 血清・喀痰中濃度
• ISSN: 0009-3165; 1884-5894
• DOI: 10.11250/chemotherapy1953.41.Supplement5_361

We evaluated the clinical efficacy and safety of temafloxacin (TMFX) in a phase II study in a total of twelve patients with respiratory infections. TMFX was administered orally at a dose of 300mg twice daily in most cases. The time course of the serum and sputum concentrations was evaluated after administering a single 300mg dose to two patients with copious mucopurulent sputum, and pharmacokinetic analysis was also performed. The subjects included one case each of pneumonia, mycoplasmal pneumonia, infected bullae, diffuse panbronchiolitis, and eight cases of bronchiectasis. Clinical response was good in eight cases, fair in two and poor in two. The overall clinical response rate was 67%. Two strains of Haemophilus influenzae were eradicated. Two of the 3 strains of Pseudomonas aeruginosa persisted and one decreased. No adverse effects were observed. The average peak concentration of TMFX in serum was 3.53μg/ml and in sputum 3.72μg/ml. The mean sputum/serum concentration ratio was 106%. The pharmacokinetic parameters in sputum were very similar to those in serum. The results indicate that TMFX penetrates into bronchial secretions well and is useful in the treatment of respiratory infections.