药物动力学和临床哌醋甲酯的有效性。
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Kimko HC,交叉JT,硬饼干
药物动力学和临床哌醋甲酯的有效性。
Pharmacokinet。1999年12月,37 (6):457 - 70。doi: 10.2165 / 00003088-199937060-00002。
- PubMed ID
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10628897 (在PubMed]
- 文摘
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哌醋甲酯规定在美国超过90%的儿童被诊断为儿童注意力缺陷多动症(ADHD)。尽管ADHD已被广泛研究,使用哌醋甲酯在ADHD仍然提出了一系列尚未解决的问题,包括其药效学特征(药物浓度效应关系)和长期治疗对患者的精神病理学的影响。本综述的目的是提供一个分析pharmacokinetic-pharmacodynamic属性和治疗的有效性哌醋甲酯可以帮助回答这些问题。哌醋甲酯有两个手性中心,但该药物用于治疗包括只有threo一双对映体。比l-enantiomer d-threo-Methylphenidate力更大。哌醋甲酯是管理经历立体选择间隙的外消旋混合物。哌醋甲酯是一种短效的兴奋剂的作用持续时间1到4小时和药代动力学半衰期为2到3个小时。口服后最高药物浓度发生在大约2小时。哌醋甲酯从胃肠道吸收,容易传递到大脑。哌醋甲酯对短期有效的治疗儿童多动症。 Its mechanism of action is not understood, but may be associated with its influence on multiple neurotransmitters, especially the release and reuptake of dopamine in the striatum. There is marked individual variability in the dose-response relationship for methylphenidate, and therefore dosage must be titrated for optimal effect and avoidance of toxicity in each child. It is unclear whether this variability is predominantly pharmacokinetic or pharmacodynamic. If variable stereoselective metabolism occurs clinically, therapeutic drug monitoring of methylphenidate will require the application of chiral assay methods for the analysis of the active component, d-threo-methylphenidate. It is difficult to predict which children will have a favourable response to methylphenidate. Nonetheless, several studies have been published linking the severity of ADHD in children with improved clinical response to methylphenidate. The use of individual single-blind medication trials may be a practical solution to this problem. Additionally, the targeted condition warrants careful consideration, since different conditions (e.g. misbehaviour or poor academic performance) may require different regimens. Further studies of the relationship between the pharmacokinetic and pharmacodynamic properties of methylphenidate are required to allow the development of optimal dosage regimens.
