Abstract
The antibacterial activity, tissue concentration, and pharmacokinetics of levofloxacin (LVFX) were investigated in patients with infections in the fields of dentistry and oral-maxillofacial surgery. The patients included 20 with subperiosteal abscesses, 12 with intraoral buccal abscesses, 12 with postoperative maxillary cysts, 4 with radicular cysts, 8 with maxillary siunsitis, 6 with maxillary or mandibular cysts, 4 with osteomyelitis, 5 with facial abscesses, and 3 with neck abscesses. The drug was administered at a dose of 100mg orally before maxillofacial surgery to 16 patients, and the concentrations in the blood (n=16), oral mucosa (n=16), and maxilla or mandible (n=13) were measured by bioassay 0.5, 1, 2, and 3 hours after administration. A pharmacokinetic study was also performed using a one-compartment model.(1) Of the 74 patients, bacteria were isolated from 69 (93.2%). A total of 184 isolates were obtained, including 86 (46.7%) aerobes and 98 (53.3%) anaerobes. The bacteria isolated most frequently were Streptococcus and Peptostreptococcus. Streptococcus showed an MIC range of 0.2 to 0.78μg/ml, and Peptostreptococcus showed a range of 0.1 to 0.78μg/ml. The mean 90% minimum inhibitory concentration was 0.78μg/ml, and the MIC50 was 0.39μg/ml. LVFX showed good antibacterial activity against these organisms.(2) The blood concentration (n=16) was 0.95±0.1μg/ml (0.5h), 1.29±0.1μg/ml (1h), 0.88±0.1μg/ml (2h), and 0.63±0.1μg/ml (3h). The pharmacokinetic parameters determined by the one-compartment model were as follows: maximum blood concentration Cmax, 1.18μg/ml; half life, 1.37h; area under the concentration-time curve (AUC), above 0.78: 0.53μg·h/ml; and effective time above MIC90: 2.09h.(3) When the drug was administered preoperatively at a dose of 100mg to 13 maxillofacial patients, the oral mucosal concentration was 0.79±0.1μg/g, and the maxillary or mandibular concentration was 0.35±0.1μg/g. Therefore, LVFX produced similar levels in the oral mucosa and serum, but yielded bone concentrations below the MIC.We conclude that LVFX is well absorbed and attains a serum concentration sufficient for a favorable therapeutic effect.
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