哌甲酯在多动症儿童中的药代动力学
Pharmacokinetics of methylphenidate in hyperkinetic children.
作者信息
Hungund B L, Perel J M, Hurwic M J, Sverd J, Winsberg B G
出版信息
Br J Clin Pharmacol. 1979 Dec;8(6):571-6. doi: 10.1111/j.1365-2125.1979.tb01046.x.
Abstract
1 Pharmacokinetic study has been carried out following oral administration of 10-20 mg of methylphenidate hydrochloride to four behaviorally disorders children. 2 It is indicated that the drug is metabolized to ritalinic acid with an apparent plasma half life of 2.5 h. 3 The variability in magnitude of plasma concentration seems to be due not to its metabolism to ritalinic acid but due to the variability in the apparent volume of distribution. 4 The brief half life of methylphenidate which parallels the short duration of action of methylphenidate in behaviorally disordered children may be explained in part by its low protein binding which results in high percentage of free drug being made available for metabolism to pharmacologically inactive metabolites.
摘要
- 对四名患有行为障碍的儿童口服10 - 20毫克盐酸哌甲酯后进行了药代动力学研究。2. 结果表明，该药物代谢为哌甲酯酸，血浆表观半衰期为2.5小时。3. 血浆浓度大小的差异似乎不是由于其代谢为哌甲酯酸，而是由于表观分布容积的差异。4. 哌甲酯的半衰期较短，这与它在患有行为障碍儿童中的作用持续时间短相平行，部分原因可能是其蛋白结合率低，导致高比例的游离药物可用于代谢为药理活性较低的代谢产物。
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