PHARMACOKINETIC ASPECTS OF THEOPHYLLINE IN PREMATURE NEWBORNS
PHARMACOKINETIC ASPECTS OF THEOPHYLLINE IN PREMATURE NEWBORNS
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DOI：
10.1056/nejm197608192950803
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发表时间：
1976-01-01
影响因子：
158.5
通讯作者：
NEIMS, AH
中科院分区：
文献类型：
--
作者：
ARANDA, JV;SITAR, DS;NEIMS, AH
为了进一步研究茶碱在早产儿体内的药代动力学特征，采用高压液相色谱法测定了6例3-15天龄窒息早产儿静脉输注茶碱后的血药浓度。茶碱的表观分布容积为0.690 ±。0.095 l/kg（平均值±. SE），该值与儿童相似，但半衰期（30.2 ±. 6.5（1）时间是9倍。血液清除率（17.6 ±. 2.3血浆清除率（100 ml/kg·h）低于幼儿血浆清除率（100 ml/kg·h）。在总血浆浓度为17毫克/升时，56.4 ±. 3.8和36.4 .+-。3.8%的茶碱与成人或足月脐带血浆蛋白结合。胆红素和茶碱不竞争血浆蛋白。计算表明，5.5 mg/kg的负荷剂量和1.1 mg/kg/8 h的维持剂量率将达到并维持8 mg/l的平均血药浓度（血浆中约为10 mg/l）。
To characterize further the pharmacokinetics of theophylline in premature infants, its concentration in blood was measured by high-pressure liquid chromatography after i.v. infusion given to 6 apneic premature newborns 3-15 days of age. Theophylline''s apparent volume of distribution was 0.690 .+-. 0.095 l/kg (mean .+-. SE), a value similar to that of children, but the half-life (30.2 .+-. 6.5 h) was 9 times longer. Blood clearance rate (17.6 .+-. 2.3 ml/kg per h) was lower than plasma clearance rate (100 ml/kg per h) of young children. At a total plasma concentration of 17 mg/l, 56.4 .+-. 3.8 and 36.4 .+-. 3.8% of the theophylline was bound to adult or full-term cord plasma proteins, respectively. Bilirubin and theophylline did not compete for plasma protein. Calculations suggest that a loading dose of 5.5 mg/kg and a maintenance dose rate of 1.1 mg/kg per 8 h would achieve and maintain a mean blood concentration of 8 mg/l (about 10 mg/l in plasma).