Department of Anesthesiology and Intensive Care, Charité University Hospital Berlin-Campus Benjamin Franklin, Hindenburgdamm 30, D-12203 Berlin, Germany.
J Antimicrob Chemother. 2011 Oct;66(10):2330-5. doi: 10.1093/jac/dkr282. Epub 2011 Jul 5.
To assess the pharmacokinetics of moxifloxacin in morbidly obese patients.
Twelve morbidly obese patients (2 male/10 female, age 25-61 years, weight 98-166 kg, body mass index 43.0-58.2 kg/m(2)) scheduled for gastric bypass surgery were treated with 400 mg of moxifloxacin orally once daily for 3 days and with 400 mg of moxifloxacin intravenously on day 4 (day of surgery). Pharmacokinetic analysis was performed on day 1 and day 4. Specimens of small intestine, greater omentum and subcutaneous adipose tissue were collected intraoperatively 1.8-3.7 h after moxifloxacin infusion. Moxifloxacin concentrations were determined by HPLC.
The plasma pharmacokinetics (mean ± SD) was comparable to historical data in normal-weight subjects. Oral bioavailability was 79.6% ± 11.5%. After intravenous administration, plasma clearance was 9.6 ± 2.0 L/h, volume of distribution was 165 ± 30 L and area under the curve was 43.7 ± 11.8 mg·h/L. Linear regression analysis showed the volume of distribution to be better correlated with ideal body weight, lean body weight, fat-free mass or height (R(2) = 0.60-0.67, P = 0.001-0.003) than with total body weight (R(2) = 0.46, P = 0.015). Whereas mean tissue concentrations in small intestine (6.99 ± 2.34 mg/kg) were twice the concomitant plasma concentrations, the concentrations in greater omentum (0.801 ± 0.168 mg/kg) or subcutaneous fat (0.638 ± 0.180 mg/kg) were only one-quarter of those.
The pharmacokinetics of moxifloxacin is not significantly affected by morbid obesity. No dose adjustment seems to be necessary in this particular population.
评估莫西沙星在病态肥胖患者中的药代动力学。
12 例病态肥胖患者（2 男/10 女，年龄 25-61 岁，体重 98-166kg，体重指数 43.0-58.2kg/m2）接受莫西沙星 400mg 口服，每日 1 次，连续 3 天，第 4 天（手术日）给予莫西沙星 400mg 静脉滴注。第 1 天和第 4 天进行药代动力学分析。在莫西沙星输注后 1.8-3.7 小时手术期间采集小肠、大网膜和皮下脂肪组织的标本。通过 HPLC 测定莫西沙星浓度。
与正常体重受试者的历史数据相比，血浆药代动力学（均值±标准差）相似。口服生物利用度为 79.6%±11.5%。静脉给药后，血浆清除率为 9.6±2.0L/h，分布容积为 165±30L，曲线下面积为 43.7±11.8mg·h/L。线性回归分析显示，分布容积与理想体重、瘦体重、去脂体重或身高的相关性优于与总体重的相关性（R2=0.60-0.67，P=0.001-0.003）。尽管小肠组织中的平均浓度（6.99±2.34mg/kg）是同时期血浆浓度的两倍，但大网膜（0.801±0.168mg/kg）或皮下脂肪（0.638±0.180mg/kg）中的浓度仅为其四分之一。
莫西沙星的药代动力学不受病态肥胖的显著影响。在这一特定人群中似乎不需要调整剂量。
