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监测唾液中拉莫三嗪的浓度。

Monitoring salivary lamotrigine concentrations.

作者信息

Malone Stephen A, Eadie Mervyn J, Addison Russell S, Wright Andrew W E, Dickinson Ronald G

机构信息

Royal Children's Hospital, Brisbane, Queensland, Australia.

出版信息

J Clin Neurosci. 2006 Nov;13(9):902-7. doi: 10.1016/j.jocn.2005.12.037. Epub 2006 Oct 17.

Abstract

Lamotrigine concentrations were measured simultaneously (as far as was feasible) in stimulated and unstimulated saliva samples, and in plasma, from seven adult volunteers over a 32 h period following a single 50 mg dose of the drug, and in 20 children and adolescents during the course of routine antiepileptic therapy. In individuals there was a close correlation between the measurements at least 2 h after ingestion of the drug. Concentrations in stimulated and unstimulated saliva were similar; the stimulation produced little change in the saliva secretion rate. The saliva-to-plasma concentration ratio increased linearly by 0.78% for each 1 mg/L plasma lamotrigine concentration, with a mean value of 48.8% at a plasma lamotrigine concentration of 10 mg/L. With appropriate precautions as to the timing of saliva collections, and a single plasma lamotrigine concentration measurement to calibrate the salivary values in the individual, salivary lamotrigine concentration measurement appears to be a practicable approach to therapeutic drug monitoring. This has significant implications for the elucidation of the pharmacokinetics of lamotrigine in the paediatric population.

摘要

在7名成年志愿者单次服用50毫克药物后的32小时内,以及在20名接受常规抗癫痫治疗的儿童和青少年中,尽可能同时测量了刺激唾液样本、未刺激唾液样本和血浆中的拉莫三嗪浓度。在个体中,服药后至少2小时的测量值之间存在密切相关性。刺激唾液和未刺激唾液中的浓度相似;刺激对唾液分泌率影响不大。血浆拉莫三嗪浓度每增加1毫克/升,唾液与血浆浓度比线性增加0.78%,血浆拉莫三嗪浓度为10毫克/升时,平均值为48.8%。在唾液采集时间上采取适当的预防措施,并通过单次血浆拉莫三嗪浓度测量来校准个体的唾液值,唾液拉莫三嗪浓度测量似乎是一种可行的治疗药物监测方法。这对阐明拉莫三嗪在儿科人群中的药代动力学具有重要意义。

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