Abstract
Pharmacokinetic and clinical studies of temafloxacin (TMFX), a new pyridonecarboxylic acid antibacterial agent, were performed, and the results obtained were as follows:
1) Pharmacokinetic study
Serum and sputum levels of TMFX were measured in three patients with chronic pulmonary emphysema treated with 150mg (1 patient) or 300mg (2 patients) orally. The peak serum levels were 1.36, and 2.47 and1.70μg/ml, 4, and 2 and 4 hours, respectively, after administration. The peak sputum levels were 1.33, and 1.79 and 2.43μg/ml, 4, and 2 and 4 hours, respectively, after administration. The ratios of peak sputum levels to peak serum levels were 97.8, and 72.5 and 142.9%, respectively.
2) Clinical study
Eleven patients with respiratory tract infections (RTIs)(acute bronchitis 3, chronic brochitis 2, bronchiectasis 2, acute pharyngitis 1, acute tonsillitis 1, pneumonia 1, chronic pulmonary emphysema 1) were given 300 or 600mg per day orally for 7-17 days. The clinical efficacy rate was 63.6%. Ten of the thirteen causative organisms (3/3 Haemophilus influenzae, 2/2 Moraxella catarrhalis, 1/2 Staphylococcus aureus, 1/2 Streptococcus pneumoniae, 1/2 Pseudomonas aeruginosa, 1/1 Klebsiella oxytoca, 1/1 Enterobacter cloacae) were eradicated.
No subjective side effects were observed, while transient, slight elevations of laboratory test values (GOT, GPT, BUN) were found in 3 patients.
Based on these results, we concluded that TMFX is an effective and useful oral antibacterial agent for the treatment of RTIs, particularly those caused by H. influenzae and M. catarrhalis.
