Rothstein P, Arthur G R, Feldman H S, Kopf G S, Covino B G
Anesth Analg. 1986 Jun;65(6):625-32.
A pharmacokinetic evaluation of bupivacaine was carried out after intercostal nerve blocks performed on 28 occasions in 27 children varying in age from 3 months to 16 yr. Bupivacaine HCl, 0.5%, with epinephrine 1:200,000 was employed. Doses of 2 mg/kg, 3 mg/kg, and 4 mg/kg resulted in peak whole blood arterial bupivacaine (base) concentrations (mean +/- SD) of 0.77 +/- 0.25 microgram/ml, 1.37 +/- 0.23 microgram/ml, and 1.87 +/- 0.53 microgram/ml, respectively. Calculated pharmacokinetic parameters (mean +/- SD) were the following: apparent volume of distribution (VD beta), 2.8 +/- 0.8 L/kg; steady-state volume of distribution (VDss), 2.7 +/- 0.7 L/kg; elimination half-life (t1/2 beta), 147 +/- 80 min; and total body clearance (Cl), 16.0 +/- 7.4 ml X min-1 X kg-1, or 382 +/- 201 ml X min-1 X m-2. Compared with data reported for adult patients, our data indicate that the volume of distribution is greater and clearance is more rapid in children than in adults. The absorption of local anesthetic from the intercostal space appears to be more rapid in children than adults. In an additional group of 11 children, the relationship of the bupivacaine blood:plasma concentration ratio (lambda) to hematocrit was investigated. Hematocrit in this group ranged from 30 to 59, and lambda varied from 0.47 to 0.82. There was a significant relationship between lambda and hematocrit defined by the equation lambda = -0.0079 Hct + 1.028 (r = 0.72, P less than 0.05). Reporting bupivacaine concentration in terms of plasma concentration may introduce an artifact that is dependent on the hematocrit, and we therefore suggest that whole blood concentration values be reported by investigators in the future.
对27名年龄在3个月至16岁之间的儿童进行了28次肋间神经阻滞后,对布比卡因进行了药代动力学评估。使用了含1:200,000肾上腺素的0.5%盐酸布比卡因。2mg/kg、3mg/kg和4mg/kg的剂量导致动脉全血布比卡因(碱基)峰值浓度(均值±标准差)分别为0.77±0.25μg/ml、1.37±0.23μg/ml和1.87±0.53μg/ml。计算得到的药代动力学参数(均值±标准差)如下:表观分布容积(VDβ),2.8±0.8L/kg;稳态分布容积(VDss),2.7±0.7L/kg;消除半衰期(t1/2β),147±80分钟;全身清除率(Cl),16.0±7.4ml·min⁻¹·kg⁻¹,或382±201ml·min⁻¹·m⁻²。与报道的成年患者数据相比,我们的数据表明儿童的分布容积比成人更大,清除率比成人更快。局部麻醉药从肋间间隙的吸收在儿童中似乎比成人更快。在另外一组11名儿童中,研究了布比卡因血药浓度与血浆浓度之比(λ)与血细胞比容的关系。该组儿童的血细胞比容范围为30至59,λ值在0.47至0.82之间变化。λ与血细胞比容之间存在显著关系,由方程λ = -0.0079Hct + 1.028定义(r = 0.72,P < 0.05)。以血浆浓度报告布比卡因浓度可能会引入一种依赖于血细胞比容的假象,因此我们建议未来研究人员报告全血浓度值。