药代动力学相互作用etravirine或内/例如在健康志愿者和蒿甲醚/ lumefantrine:两版,双向,两期,随机试验。
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Kakuda TN, DeMasi R,范·代尔夫特Y,穆罕默德P
药代动力学相互作用etravirine或内/例如在健康志愿者和蒿甲醚/ lumefantrine:两版,双向,两期,随机试验。
HIV地中海。2013年8月,14 (7):421 - 9。doi: 10.1111 / hiv.12019。Epub 2013年2月26日。
- PubMed ID
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23441978 (在PubMed]
- 文摘
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目标:Etravirine衬底和诱导细胞色素P450 (CYP) 3和CYP2C9底物和抑制剂和CYPC2C19。内/例如CYP3A的底物和抑制剂。蒿甲醚和lumefantrine主要由CYP3A代谢;蒿甲醚也是代谢CYP2B6程度较轻,CYP2C9和CYP2C19。双氢青蒿素含量测定蒿甲醚有活性代谢物。目的是研究药代动力学相互作用内/例如或etravirine和arthemether / lumefrantrine。方法:这个只有随机、双向、两年期交叉研究包括33名健康志愿者。在面板1中,17名健康志愿者接受两种治疗方法(A和B)以随机的顺序,洗脱期4周的治疗:治疗:蒿甲醚/ lumefantrine 80/480毫克,在为期3天的课程;治疗B: etravirine 200毫克,一天两次(投标)21天蒿甲醚/ lumefantrine 80/480毫克每天8(为期3天的疗程)。在面板2中,另一个16名健康志愿者接受两种治疗方法,类似于那些在面板1而是etravirine darunavir /例如600/100毫克投标。 RESULTS: Overall, 28 of the 33 volunteers completed the study. Co-administration of etravirine reduced the area under the plasma concentration-time curve (AUC) of artemether [by 38%; 90% confidence interval (CI) 0.48-0.80], dihydroartemisinin (by 15%; 90% CI 0.75-0.97) and lumefantrine (by 13%; 90% CI 0.77-0.98) at steady state. Co-administration of darunavir/ritonavir reduced the AUC of artemether (by 16%; 90% CI 0.69-1.02) and dihydroartemisinin (by 18%; 90% CI 0.74-0.91) but increased lumefantrine (2.75-fold; 90% CI 2.46-3.08) at steady state. Co-administration of artemether/lumefantrine had no effect on etravirine, darunavir or ritonavir AUC. No drug-related serious adverse events were reported during the study. CONCLUSIONS: Co-administration of etravirine with artemether/lumefantrine may lower the antimalarial activity of artemether and should therefore be used with caution. Darunavir/ritonavir can be co-administered with artemether/lumefantrine without dose adjustment but should be used with caution.
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 蒿甲醚 细胞色素P450 2 c9 蛋白质 人类 未知的底物细节 - 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
在您的软件的交互蒿甲醚 Etravirine 蒿甲醚的血清浓度的活性代谢物在蒿甲醚结合使用时,可以减少Etravirine导致失去功效。 Lumefantrine 内 的血清浓度Lumefantrine时可以增加结合内。
