Nix D E, Norman A, Schentag J J
School of Pharmacy, State University of New York, Buffalo.
Antimicrob Agents Chemother. 1989 Jul;33(7):1006-8. doi: 10.1128/AAC.33.7.1006.
A study involving 25 health male volunteers was conducted to evaluate the effect of lomefloxacin on the pharmacokinetics of theophylline. The mean age was 22.4 +/- 3.0 years, and the mean weight was 77.3 +/- 7.7 kg. A single 6-mg/kg aminophylline dose was given intravenously on study days 1 and 15. The subjects received a 400-mg lomefloxacin dose (four 100-mg capsules) on study days 9 through 15. No treatment was given on study days 2 through 8. Thirteen blood samples were collected within 24 h after each aminophylline dose. Theophylline concentrations in serum were measured by enzyme immunoassay (EMIT). The mean aminophylline dose was 437 +/- 36 mg, equivalent to 344 mg of theophylline. Multiple doses of lomefloxacin had no effect on the area under the concentration-time curve from 0 h to infinity, maximal concentration, or clearance of theophylline from serum. There was a slight increase in the theophylline half-life from 6.72 +/- 1.63 to 7.02 +/- 1.37 h after lomefloxacin dosing (P = 0.04); however, the change was clinically insignificant. No change in theophylline dose is required when lomefloxacin therapy is instituted in a patient receiving theophylline.
一项涉及25名健康男性志愿者的研究旨在评估洛美沙星对茶碱药代动力学的影响。平均年龄为22.4±3.0岁,平均体重为77.3±7.7千克。在研究的第1天和第15天静脉注射单次6毫克/千克的氨茶碱剂量。受试者在研究的第9天至第15天接受400毫克洛美沙星剂量(四粒100毫克胶囊)。在研究的第2天至第8天未进行治疗。每次氨茶碱给药后24小时内采集13份血样。血清中的茶碱浓度通过酶免疫测定法(EMIT)进行测量。氨茶碱的平均剂量为437±36毫克,相当于344毫克茶碱。多次给予洛美沙星对茶碱从0小时到无穷大的浓度-时间曲线下面积、最大浓度或从血清中的清除率没有影响。洛美沙星给药后茶碱的半衰期从6.72±1.63小时略有增加至7.02±1.37小时(P = 0.04);然而,这种变化在临床上无显著意义。在接受茶碱治疗的患者中开始使用洛美沙星治疗时,无需改变茶碱剂量。