药代动力学etravirine和non-antiretroviral药物之间的相互作用。
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Kakuda TN, Scholler-Gyure M, Hoetelmans RM
药代动力学etravirine和non-antiretroviral药物之间的相互作用。
Pharmacokinet。2011年1月;50 (1):25 - 39。doi: 10.2165 / 11534740-000000000-00000。
- PubMed ID
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21142266 (在PubMed]
- 文摘
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Etravirine(以前TMC125)是一种非核苷逆转录酶抑制剂(NNRTI)活动对野生型和NNRTI-resistant hiv - 1菌株。Etravirine已经在几个国家被批准用作treatment-experienced病人高活性抗逆转录病毒疗法的一部分。体内,etravirine衬底,弱的诱导物,肝细胞色素P450 (CYP)同工酶3 a4和衬底和弱CYP2C9抑制剂和CYP2C19。22 Etravirine也是一个薄弱的抑制剂。一个广泛的药物之间相互作用项目在艾滋病毒阴性的受试者进行了评估潜在的药代动力学etravirine和各种non-antiretroviral药物之间的相互作用。阿托伐他汀、克拉霉素、美沙酮、奥美拉唑口服避孕药,帕罗西汀、雷尼替丁、西地那非在药代动力学etravirine处置是没有临床意义的。同样,etravirine没有对氟康唑的药物动力学,临床上重要影响美沙酮、口服避孕药、帕罗西汀、伏立康唑。etravirine之间没有预计临床相关的交互和阿奇霉素或病毒唑,因此,etravirine可以结合这些代理没有剂量调整。氟康唑和伏立康唑etravirine暴露增加1.9和1.4倍,分别在健康受试者中,然而,没有副作用的发生率增加病人接受etravirine和氟康唑在临床试验中观察到,因此,etravirine虽然谨慎是可以结合这些抗真菌治疗建议。地高辛等离子体接触时略有增加与etravirine流行性流感减毒活疫苗。 No dose adjustments of digoxin are needed when used in combination with etravirine, however, it is recommended that digoxin levels should be monitored. Caution should be exercised in combining rifabutin with etravirine in the presence of certain boosted HIV protease inhibitors due to the risk of decreased exposure to etravirine. Although adjustments to the dose of clarithromycin are unnecessary for the treatment of most infections, the use of an alternative macrolide (e.g. azithromycin) is recommended for the treatment of Mycobacterium avium complex infection since the overall activity of clarithromycin against this pathogen may be altered when co-administered with etravirine. Dosage adjustments based on clinical response are recommended for clopidogrel, HMG-CoA reductase inhibitors (e.g. atorvastatin) and for phosphodiesterase type-5 inhibitors (e.g. sildenafil) because changes in the exposure of these medications in the presence of co-administered etravirine may occur. When co-administered with etravirine, a dose reduction or alternative to diazepam is recommended. When combining etravirine with warfarin, the international normalized ratio (INR) should be monitored. Systemic dexamethasone should be co-administered with caution, or an alternative to dexamethasone be found as dexamethasone induces CYP3A4. Caution is also warranted when co-administering etravirine with some antiarrhythmics, calcineurin inhibitors (e.g. ciclosporin) and antidepressants (e.g. citalopram). Co-administration of etravirine with some antiepileptics (e.g. carbamazepine and phenytoin), rifampicin (rifampin), rifapentine or preparations containing St John's wort (Hypericum perforatum) is currently not recommended as these are potent inducers of CYP3A and/or CYP2C and may potentially decrease etravirine exposure. Antiepileptics that are less likely to interact based on their known pharmacological properties include gabapentin, lamotrigine, levetiracetam and pregabalin. Overall, pharmacokinetic and clinical data show etravirine to be well tolerated and generally safe when given in combination with non-antiretroviral agents, with minimal clinically significant drug interactions and no need for dosage adjustments of etravirine in any of the cases, or of the non-antiretroviral agent in the majority of cases studied.
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 Etravirine 细胞色素P450 2 c19 蛋白质 人类 未知的底物抑制剂细节 Etravirine 细胞色素P450 2 c9 蛋白质 人类 未知的底物抑制剂细节 Etravirine 细胞色素P450 3 a4 蛋白质 人类 未知的底物诱导物细节 - 药物转运蛋白
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药物 转运体 类 生物 药理作用 行动 Etravirine 多药耐药性蛋白3 蛋白质 人类 未知的抑制剂细节 Etravirine 22 - 1 蛋白质 人类 未知的抑制剂细节 - 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
在您的软件的交互阿托伐他汀 Etravirine 阿托伐他汀的血清浓度可以结合Etravirine时下降。 安定 Etravirine 时可以减少安定的新陈代谢与Etravirine相结合。 地高辛 Etravirine 血清地高辛浓度时可以增加与Etravirine相结合。 Etravirine 利福 时可以降低血清浓度Etravirine结合利福。
