共同伏立康唑和苯妥英:药代动力学相互作用,安全,和宽容。
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Purkins L,木头N, Ghahramani P,爱呃,夏娃MD,菲尔丁
共同伏立康唑和苯妥英:药代动力学相互作用,安全,和宽容。
Br中国新药杂志。2003;12月56 1:37-44。doi: 10.1046 / j.1365-2125.2003.01997.x。
- PubMed ID
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14616412 (在PubMed]
- 文摘
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目的:伏立康唑是一种新型三唑抗真菌剂,和代谢的细胞色素P450同功酶CYP2C9, CYP2C19, CYP3A4的较小程度上。苯妥英是CYP3A4活性的诱导物和基质和CYP2C9和CYP2C19的诱导物。目前的研究调查当coadministered伏立康唑和苯妥英的药代动力学的相互作用。方法:两个安慰剂对照与这些相应平行的组织在健康男性志愿者进行了研究。学习是一个开放的研究和调查的影响苯妥英(300毫克每日一次)的稳态药物动力学伏立康唑(200毫克和400毫克每日两次)。研究B是一个双盲随机研究探讨伏立康唑的影响(400毫克每日两次)的稳态药物动力学苯妥英(300毫克每日一次)。Cmax和AUCtau在7天相比,21日和28日(研究),在天7和17(研究B)。所有不良事件都记录下来。结果:研究一:21个受试者可评价的(10伏立康唑+苯妥英11伏立康唑+安慰剂)。受试者接受伏立康唑(200毫克每日两次)+苯妥英,伏立康唑的第21天/ 7天比率Cmax AUCtau和60.7%(90%可信区间(CI) 50.1, 73.6)和35.9% (90% CI 29.7, 43.3),分别。调整的伏立康唑+安慰剂,意味着之间的比率为50.7% (90% CI 38.8, 66.1)和30.6% (90% CI 23.5, 39.7),分别。 When the dose of voriconazole was increased to 400 mg twice daily, the day 28/day 7 ratios for voriconazole Cmax and AUCtau were 134% (90% CI 89.2, 200) and 139% (90% CI 97.3, 199), respectively. Study B: 15 subjects were evaluable for pharmacokinetic assessments (six phenytoin + voriconazole, nine phenytoin + placebo). The ratios between the means for phenytoin + voriconazole/phenytoin + placebo on day 17 vs. day 7 were: phenytoin Cmax 167% (90% CI 144, 193) and phenytoin AUCtau 181% (90% CI 156, 210). All treatments were well tolerated: most adverse events were mild/moderate and transient. CONCLUSIONS: Repeat dose administration of phenytoin decreased the mean steady-state Cmax and AUCtau of voriconazole by approximately 50% and 70%, respectively. Increasing the dose of voriconazole from 200 mg to 400 mg b.d. compensated for this effect. Repeat dose administration of 400 mg b.d. voriconazole increased the mean steady-state Cmax and AUCtau of phenytoin by approximately 70% and 80%, respectively. It is therefore recommended that plasma phenytoin concentrations are monitored and the dose adjusted as appropriate when phenytoin is coadministered with voriconazole.
beplay体育安全吗DrugBank数据引用了这篇文章
- 药物酶
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药物 酶 类 生物 药理作用 行动 苯妥英 细胞色素P450 3 a4 蛋白质 人类 没有底物诱导物细节 - 药物的相互作用Learn More" title="" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
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药物 交互 整合药物之间
在您的软件的交互伏立康唑 Fosphenytoin 伏立康唑的血清浓度可以结合Fosphenytoin时下降。 伏立康唑 苯妥英 伏立康唑的血清浓度时可以减少与苯妥英相结合。
