Abstract
The antimicrobial activity, absorption, elimination and clinical utility of temafloxacin (TMFX), a newly developed quinoline antimicrobial, were determined, and the following results were obtained.
1) Antimicrobial activity of the test drug against clinically isolated methicillin-susceptible Staphylococcus aureus, methicillin-resistant S. aureus, Escherichia coil, Klebsiella pneumoniae, and Pseudomonas aeruginosa was determined.
2) Absorption and elimination: After the test drug was administered orally once to 2 adults (diabetics without infection) at a dose of 150 or 300mg/day and 3 elderly patients without infections at a dose of 300mg/day after fasting, the drug concentrations in serum and urine were determined. The maximum drug concentrations (Cmax) in patients receiving 300mg/day were 3.01μg/ml for the adults and 4.29μg/ml on average for the elderly. The average serum elimination half-times (T1/2) were 6.32 hours for the former and 7.90 hours for the latter, and the drug concentrations were 1.90 and 2.60μg/ml for the two groups of patients after 10 hours. On the other hand, the Cmax for the adults receiving 150mg/day orally was 2.31μg/ml, and the T1/2 was 5.94 hours. The drug concentration was 0.79μg/ml after 10 hours. The rates of recovery in urine were 50.2% and 54.5% after 12 hours following the administration of 150 and 300mg/day, after fasting, respecitvely, and 72.1% after 48 hours following the administration of 300mg/day after fasting.
3) Laboratory tests: Among 12 patients admitted to the study were 5 with pyogenic tonsillitis, 2 with acute pharyngitis, 2 with acute bronchitis, 2 with bacterial pneumonia, and 1 with pulmonary suppuration.
The test drug was effective in all but 1 patient with pulmonary suppuration, the rate of effectiveness being 91.7%. Streptococcus pneumoniae and Streptococcus pyogenes were isolated from 1 patient with acute bronchitis and 2 with pyogenic tonsillitis. The former disappeared after treatment and the latter disappeared in 1 patient, but the other patient was left with the infection after treatment. No objective or subjective side effects, or abnormal laboratory tests were observed during treatment.
The results of this study suggest that TMFX is of use in the treatment of infections in the field of internal medicine.
