Koizumi F, Ohnishi A, Takemura H, Okubo S, Kagami T, Tanaka T
Department of Internal Medicine, Yamanashi Prefectural Central Hospital, Kohfu, Japan.
Antimicrob Agents Chemother. 1994 May;38(5):1140-3. doi: 10.1128/AAC.38.5.1140.
To ascertain whether monitoring of the concentrations of ofloxacin in saliva during a course of treatment is more suitable and safer than that of its levels in blood, we simultaneously monitored its concentrations in three body fluids (blood, saliva, and expectorated sputum) after a 300-mg administration in 18 patients with chronic respiratory infection. The mean (+/- standard error of the mean) half-lives derived from the three drug level-time relationships were similar: 6.04 +/- 0.58 h for serum, 6.34 +/- 0.63 h for sputum, and 6.61 +/- 0.65 h for saliva. The mean peak concentration (4.06 to 4.53 micrograms/ml) did not differ at the three sites, but the times taken to reach peak concentration in saliva and sputum (3.17 +/- 0.46 h) were significantly longer than that in serum (2.22 +/- 0.28 h). The ratios of the concentrations in saliva and sputum to the concentration in serum increased during the first 2 h and reached 1.0 between 2 and 8 h after administration. They rose above 1.0 16 h after administration: 1.14 +/- 0.11 for saliva and 1.19 +/- 0.10 for sputum. The concentration-time relationship for sputum corresponded closely with the concentration-time relationship for saliva, and an overall significant correlation between the concentrations in sputum and saliva was obtained (P < 0.01). These results suggest that monitoring concentrations in saliva may be more valid, as well as less invasive, than monitoring of the levels in blood for ensuring that the drug concentration reaches its therapeutic level in bronchial secretions.
为确定在治疗过程中监测唾液中氧氟沙星浓度是否比监测血液中氧氟沙星水平更合适、更安全,我们对18例慢性呼吸道感染患者给予300毫克氧氟沙星后,同时监测了其在三种体液(血液、唾液和咳出的痰液)中的浓度。由三种药物浓度-时间关系得出的平均(±平均标准误)半衰期相似:血清为6.04±0.58小时,痰液为6.34±0.63小时,唾液为6.61±0.65小时。三个部位的平均峰浓度(4.06至4.53微克/毫升)无差异,但唾液和痰液达到峰浓度的时间(3.17±0.46小时)明显长于血清中的时间(2.22±0.28小时)。唾液和痰液中浓度与血清中浓度的比值在给药后的前2小时内升高,在给药后2至8小时达到1.0。给药后16小时,它们升至1.0以上:唾液为1.14±0.11,痰液为1.19±0.10。痰液的浓度-时间关系与唾液的浓度-时间关系密切对应,痰液和唾液中浓度之间存在总体显著相关性(P<0.01)。这些结果表明,为确保药物浓度在支气管分泌物中达到治疗水平,监测唾液中的浓度可能比监测血液中的水平更有效,且侵入性更小。