皮下舒马匹坦药代动力学:划定单胺氧化酶抑制剂的作用。
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皮下舒马匹坦药代动力学:划定单胺氧化酶抑制剂的作用。
头痛。2010年2月;50(2):249-55。doi: 10.1111 / j.1526-4610.2009.01568.x。2009年11月17日。
- PubMed ID
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19925626 (PubMed视图]
- 摘要
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背景:皮下注射舒马曲坦的绝对生物利用度为96-100%。6 mg s.c.舒马匹坦后(即T(max) =约0.2小时后)血浆浓度的衰减曲线包含一个较大的分布成分。beplayappbeplayapp目的:本研究的目的是确定mao - a治疗是否应该根据药代动力学的理由阻止使用6mg s.c.舒马匹坦。方法:从文献和葛兰素史克(GSK)研究C92-050中获取药代动力学数据。将一半时间转换为速率常数，然后将其用于简化的隔室模型(只需要3个联立微分方程)。模型的接受标准包括在给药后T(max)、1、2和10小时观察到的血浆舒马匹坦浓度。生成了一组1000个浓度测量值，分辨率为36秒。然后用伴随使用莫氯比胺时观察到的消除常数扰动模型，产生第二组浓度测量。 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.