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600毫克依非韦伦与利福平联合用药在中国HIV/TB合并感染患者中的药代动力学

Pharmacokinetics of Efavirenz 600mg in Combination with Rifampicin in Chinese HIV/TB Co-Infection Patients.

作者信息

Wang Tongtong, Liu Yingchu, Zhu Chunyu, Yang Siyuan, Yang Di, Xiao Jiang, Gao Guiju

机构信息

Beijing Ditan Hospital, Capital Medical University, Beijing, People's Republic of China.

School of General Practice and Continuing Education, Capital Medical University, Beijing, People's Republic of China.

出版信息

Infect Drug Resist. 2023 Jul 17;16:4659-4666. doi: 10.2147/IDR.S415749. eCollection 2023.

DOI:10.2147/IDR.S415749
PMID:37484907
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC10361278/
Abstract

BACKGROUND

Rifampicin is a known inducer of the cytochrome P450 (CYP2B6) enzyme, which can lead to a decrease in the concentration of efavirenz. Therefore, we conducted a study to evaluate the effect of daily rifampicin intake on efavirenz 600mg pharmacokinetics and HIV-1 virological suppression.

METHODS

Patients receiving antiretroviral therapy containing efavirenz (600mg daily), and we collected efavirenz concentration at four visit points: ART day 14 (PK1), ART day 42 (PK2), ART day 140 (PK3), and ART day 336 (PK4), and performed pharmacokinetics analysis.

RESULTS

From February 2017 to November 2020, 29 HIV/TB co-infection patients were included. Ninety percent of patients had a concentration of ≥1000ng/mL of efavirenz during the study. All patients had efavirenz C ≥1000ng/mL, 86% patients showed good virology response.

CONCLUSION

Our study shows that the use of rifampicin in HIV/TB co-infection patients does not affect efavirenz drug concentrations, that virological suppression is good and that no efavirenz dose adjustment is required.

摘要

背景

利福平是一种已知的细胞色素P450(CYP2B6)酶诱导剂,可导致依非韦伦浓度降低。因此,我们开展了一项研究,以评估每日服用利福平对600mg依非韦伦药代动力学及HIV-1病毒学抑制的影响。

方法

患者接受含依非韦伦(每日600mg)的抗逆转录病毒治疗,我们在四个访视点收集依非韦伦浓度:抗病毒治疗第14天(PK1)、抗病毒治疗第42天(PK2)、抗病毒治疗第140天(PK3)和抗病毒治疗第336天(PK4),并进行药代动力学分析。

结果

2017年2月至2020年11月,纳入29例HIV/TB合并感染患者。90%的患者在研究期间依非韦伦浓度≥1000ng/mL。所有患者依非韦伦C≥1000ng/mL,86%的患者显示出良好的病毒学反应。

结论

我们的研究表明,在HIV/TB合并感染患者中使用利福平不影响依非韦伦药物浓度,病毒学抑制良好,且无需调整依非韦伦剂量。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8b69/10361278/d98416c80b2d/IDR-16-4659-g0003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8b69/10361278/bf0536fc096f/IDR-16-4659-g0001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8b69/10361278/ccf1b37052e4/IDR-16-4659-g0002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8b69/10361278/d98416c80b2d/IDR-16-4659-g0003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8b69/10361278/bf0536fc096f/IDR-16-4659-g0001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8b69/10361278/ccf1b37052e4/IDR-16-4659-g0002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8b69/10361278/d98416c80b2d/IDR-16-4659-g0003.jpg

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本文引用的文献

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The Potential for Treatment Shortening With Higher Rifampicin Doses: Relating Drug Exposure to Treatment Response in Patients With Pulmonary Tuberculosis.高剂量利福平治疗缩短的潜力:肺结核患者药物暴露与治疗反应的关系。
Clin Infect Dis. 2018 Jun 18;67(1):34-41. doi: 10.1093/cid/ciy026.
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Pharmacokinetics of rifampicin in adult TB patients and healthy volunteers: a systematic review and meta-analysis.利福平在成人结核病患者和健康志愿者中的药代动力学:系统评价和荟萃分析。
J Antimicrob Chemother. 2018 Sep 1;73(9):2305-2313. doi: 10.1093/jac/dky152.
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Is there a need to increase the dose of efavirenz during concomitant rifampicin-based antituberculosis therapy in sub-Saharan Africa? The HIV-TB pharmagene study.
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Pharmacogenomics. 2015;16(10):1047-64. doi: 10.2217/pgs.15.35. Epub 2015 Apr 1.
4
Population pharmacokinetics of dolutegravir in HIV-infected treatment-naive patients.多替拉韦在初治HIV感染患者中的群体药代动力学
Br J Clin Pharmacol. 2015 Sep;80(3):502-14. doi: 10.1111/bcp.12639. Epub 2015 Jul 14.
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Pharmacokinetics of efavirenz and treatment of HIV-1 among pregnant women with and without tuberculosis coinfection.依法韦仑的药代动力学以及合并或未合并结核感染的孕妇中HIV-1的治疗
J Infect Dis. 2015 Jan 15;211(2):197-205. doi: 10.1093/infdis/jiu429. Epub 2014 Jul 31.
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Trends in AIDS-defining opportunistic illnesses incidence over 25 years in Rio de Janeiro, Brazil.巴西里约热内卢25年间艾滋病界定机会性感染发病率的趋势。
PLoS One. 2014 Jun 5;9(6):e98666. doi: 10.1371/journal.pone.0098666. eCollection 2014.
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Why did the FDA approve efavirenz 800 mg when co-administered with rifampin?为什么美国食品药品监督管理局(FDA)批准了依法韦仑800毫克与利福平联合使用?
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