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[儿童体内茶碱的药代动力学和药效学特性]

[Peculiarities of the pharmacokinetics and pharmacodynamics of theophylline in children].

作者信息

Berdel D, Heimann G

出版信息

Wien Klin Wochenschr. 1984 Aug 31;96(16):616-21.

PMID:6516414
Abstract

Pharmacologically relevant factors such as enteral absorption, distribution, metabolism and excretion are age-dependent. The absorption of theophylline given in aqueous solution to prenatal infants with apnoea is markedly reduced when administered along with the infant's feed. The metabolic pathway of theophylline depends on the age group. Newborn and older infants form the pharmacodynamically active metabolite, caffeine. The main metabolites 1.3-dimethyl-uric acid and 3-methylxanthine are detectable, as in adults, but 1-methyl-uric acid remains below the demonstrable serum concentration level in infants of our study. The elimination velocity of theophylline is also dependent on the age. In order to achieve effective theophylline concentrations in the serum with oral preparations the galenic properties of the sustained-release products are decisive. By contrast, there was no difference between intravenous administration as permanent infusion or bolus injection. The data presented underline that in the treatment of apnea in premature infants as well as in the treatment of asthma in older children individual controls of serum concentrations are required to achieve further improvement of therapeutic success.

摘要

诸如肠内吸收、分布、代谢和排泄等与药理学相关的因素都与年龄有关。给患有呼吸暂停的早产婴儿口服水溶液形式的茶碱时,若与婴儿的食物一起服用,其吸收会显著减少。茶碱的代谢途径取决于年龄组。新生儿和较大婴儿会形成具有药效学活性的代谢产物咖啡因。与成年人一样,可检测到主要代谢产物1,3 - 二甲基尿酸和3 - 甲基黄嘌呤,但在我们研究的婴儿中,1 - 甲基尿酸的血清浓度仍低于可检测水平。茶碱的消除速度也取决于年龄。为了通过口服制剂在血清中达到有效的茶碱浓度,缓释产品的药剂学性质起决定性作用。相比之下,持续静脉输注或大剂量注射之间没有差异。所呈现的数据强调,在治疗早产儿呼吸暂停以及大龄儿童哮喘时,需要对血清浓度进行个体化控制,以进一步提高治疗效果。

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