Ke J, Tam Y K, Koo W W, Coutts R T, Finegan B A
Faculty of Pharmacy and Pharmaceutical Sciences, Department of Pediatrics, University of Alberta, Edmonton, Canada.
Ther Drug Monit. 1990 Mar;12(2):157-62. doi: 10.1097/00007691-199003000-00009.
We tested the hypothesis that amino acids in a parenteral nutrition (PN) solution would result in the decreased metabolism of a model compound, lidocaine. One bolus infusion of lidocaine HCl (1 mg/kg) was administered to seven healthy subjects in association with each of three nutrient regimens: (a) a standard PN solution, (b) 10% dextrose water (D10W), and (c) a meal (control) containing similar fluid volume and caloric, protein, and sodium content as the PN solution. Intravenous nutrients were infused consecutively in a random order at 1 L/12 h. Intravenous and control studies were performed 28 days apart. There was no significant difference in the means (+/- SEM) of total body clearance [7.70 +/- 0.70 (PN) versus 6.78 +/- 0.79 (D10W) versus 7.86 +/- 0.93 (control) ml/min kg], half-life [74.0 +/- 12.2 (PN) versus 89.6 +/- 4.35 (D10W) versus 79.2 +/- 7.22 (control) min], volume of distribution [0.82 +/- 0.15 (PN) versus 0.88 +/- 0.13 (D10W) versus 0.78 +/- 0.13 (control) L/kg], and the fraction of unbound lidocaine in the serum [0.34 +/- 0.025 (PN) versus 0.36 +/- 0.019 (D10W) versus 0.33 +/- 0.020 (control)] among the three nutrient regimens. The concentration-time course of the active metabolite, N-ethylglycyl-2,6-xylidide, did not differ significantly regardless of the nutritional regimen used. Our study indicates that amino acids used for PN do not have any acute effect on lidocaine pharmacokinetics in healthy subjects.
肠外营养(PN)溶液中的氨基酸会导致模型化合物利多卡因的代谢降低。对7名健康受试者分别给予三种营养方案中的每一种,并同时静脉推注一次盐酸利多卡因(1mg/kg):(a)标准PN溶液;(b)10%葡萄糖水(D10W);(c)与PN溶液具有相似液体量、热量、蛋白质和钠含量的一餐(对照)。静脉营养以1L/12h的速度随机连续输注。静脉研究和对照研究相隔28天进行。三种营养方案之间,全身清除率的均值(±标准误)[7.70±0.70(PN)对6.78±0.79(D10W)对7.86±0.93(对照)ml/min·kg]、半衰期[74.0±12.2(PN)对89.6±4.35(D10W)对79.2±7.22(对照)min]、分布容积[0.82±0.15(PN)对0.88±0.13(D10W)对0.78±0.13(对照)L/kg]以及血清中游离利多卡因的分数[0.34±0.025(PN)对0.36±0.019(D10W)对0.33±0.020(对照)]均无显著差异。无论使用何种营养方案,活性代谢产物N - 乙基甘氨酰 - 2,6 - 二甲基苯胺的浓度 - 时间过程均无显著差异。我们的研究表明,用于PN的氨基酸对健康受试者利多卡因的药代动力学没有任何急性影响。