舒马曲坦皮下药物动力学:限定单胺氧化酶抑制剂的效果。

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舒马曲坦皮下药物动力学:限定单胺氧化酶抑制剂的效果。

头痛。2010年2月;50 (2):249 - 55。doi: 10.1111 / j.1526-4610.2009.01568.x。Epub 2009年11月17日。

PubMed ID

19925626 (在PubMed

]

文摘

背景:皮下(南)舒马曲坦的绝对生物利用度为96 - 100%。血浆浓度的衰减曲线6毫克南卡罗来纳州舒马曲坦后(即在T (max) = 0.2小时)包括一个大型分布组件。由单胺代谢oxidase-A(是)导致约40%的南卡罗莱纳州剂量出现尿液中不活跃的吲哚乙酸。产品标签州合并施打抑制剂的是(MAOI-A)导致舒马曲坦等离子体浓度,增加2倍,消除半衰期增加40%。目的:本研究的目的是确定MAOI-A疗法是否应该阻止使用6毫克南卡罗来纳州舒马曲坦在药代动力学。方法:总结药代动力学数据被从文学和葛兰素史克(GSK)研究c92 - 050。半场被转换成速率常数,然后用于吝啬的区划的模型(只需要3微分方程组)。验收标准为模型中观察到等离子体舒马曲坦浓度在T (max), 1、2和10小时post-dose。一组1000浓度测量的分辨率生成36秒。然后模型摄动与消除常量观察相伴moclobemide执政期间,创建第二个组浓度测量。 The 2 sets were then plotted, examined for their differences, and integrated for a second time to obtain and compare areas under the curve (AUCs). RESULTS: The greatest absolute difference between the 2 sets of measurements was 2.85 ng/mL at t = 2.95 hours. A 2-fold difference between the 2 sets occurred only after t = 5.96 hours, when the concentration in the presence of the MAOI-A was 3.72 ng/mL (or <4% of C(max)). At t = 10 hours, the concentrations in both sets were <1 ng/mL (ie, below the lower limit of assay quantitation), and AUC(0-10h) was 97.4 and 117 ng.hour/mL in the absence and presence of the MAOI-A. CONCLUSIONS: There are no pharmacokinetic grounds to deter co-administration of an MAOI-A and subcutaneous sumatriptan. The dominance of the distribution phase and completeness of absorption of a 6 mg dose of s.c. sumatriptan explains the trivial effect size of the MAOI-A on plasma sumatriptan concentrations. Importantly, these findings should not be extrapolated to other routes of administration for sumatriptan.

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药物酶

药物	酶	类	生物	药理作用	行动
舒马曲坦	胺氧化酶(flavin-containing)	蛋白质	人类	未知的	底物	细节