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口服抗酸剂对静脉注射依诺沙星处置的影响。

Effect of oral antacids on disposition of intravenous enoxacin.

作者信息

Nix D E, Lebsack M E, Chapelsky M, Sedman A J, Busch J, Norman A

机构信息

Center for Clinical Pharmacy Research, State University of New York, Buffalo School of Pharmacy.

出版信息

Antimicrob Agents Chemother. 1993 Apr;37(4):775-7. doi: 10.1128/AAC.37.4.775.

Abstract

The effect of an intensive aluminum-magnesium hydroxide antacid regimen (Maalox TC) on the disposition of intravenous enoxacin was studied in six male and six female volunteers. A single 400-mg dose of enoxacin was administered intravenously over 30 min on two occasions separated by a 1-week washout period. Thirty milliliters of Maalox TC was administered at -8, -2.5, -0.5, 1.5, 3.5, 5.5, 7.5, 9.5, 11.5, 13.5, and 15.5 h relative to the start of one enoxacin infusion. The enoxacin dose in which antacid was coadministered was randomly selected. Fourteen plasma samples were collected over 24 h, and urine was collected in two divided intervals over 48 h. Enoxacin concentrations in plasma and urine samples were determined by high-performance liquid chromatographic assays. The intensive antacid regimen did not change the total clearance (P = 0.058) or steady-state volume of distribution (P = 0.516) for enoxacin. However, the nonrenal clearance and half-life were significantly altered (P < 0.05). The mean nonrenal clearance increased from 13.27 +/- 3.33 to 15.68 +/- 2.35 liters/h (18.2%) following the antacid regimen. This effect of antacid is unlikely to be of clinical significance. Enoxacin may be administered intravenously, but not orally, without regard to antacid treatment.

摘要

在六名男性和六名女性志愿者中研究了强化铝镁氢氧化物抗酸方案(氢氧化铝镁混悬液)对静脉注射依诺沙星处置的影响。在两次给药之间有1周的洗脱期,每次静脉注射400mg依诺沙星,给药时间为30分钟。相对于一次依诺沙星输注开始的时间,在-8、-2.5、-0.5、1.5、3.5、5.5、7.5、9.5、11.5、13.5和15.5小时给予30毫升氢氧化铝镁混悬液。与抗酸剂同时给药的依诺沙星剂量是随机选择的。在24小时内采集14份血浆样本,并在48小时内分两个时间段收集尿液。通过高效液相色谱法测定血浆和尿液样本中的依诺沙星浓度。强化抗酸方案未改变依诺沙星的总清除率(P = 0.058)或稳态分布容积(P = 0.516)。然而,非肾清除率和半衰期有显著改变(P < 0.05)。抗酸方案后,平均非肾清除率从13.27±3.33升/小时增加到15.68±2.35升/小时(增加18.2%)。抗酸剂的这种作用不太可能具有临床意义。静脉注射依诺沙星时可不考虑抗酸剂治疗,但口服时则不然。

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