Expert consensus on the rational use of rifamycins in the treatment of tuberculosis with comorbidities

doi:10.19982/j.issn.1000-6621.20250254

Abstract

Abstract:

Tuberculosis frequently coexists with multiple chronic diseases, necessitating combination pharmacotherapy. Rifamycin-class anti-tuberculosis agents exhibit clinically significant interactions with many drugs used to treat comorbidities, potentially reducing their efficacy, causing treatment failure, or increasing toxicity. However, evidence-based clinical guidance on these interactions is currently lacking. To improve clinicians’ understanding of the interactions between rifamycins and medications for comorbid conditions and to support their rational use, this consensus statement was developed. It was based on a systematic review of domestic and international literature, drug-label information, and appraisal of the best available evidence, and was finalized after three rounds of focused discussion and revision. The document covers an overview of rifamycins agents, their mechanisms of drug-drug interaction, guiding principles for clinical application, and a comprehensive summary of evidence on interactions with commonly prescribed comorbidity medications, together with practical dose-adjustment recommendations. The aim is to provide safe and effective rifamycin-based therapeutic regimens for tuberculosis patients with comorbidities and to offer an actionable reference for clinical practice.

Key words: Rifamycins, Tuberculosis, Comorbidity, Therapeutic uses, Guidebooks

CLC Number:

National Clinical Research Center for Infectious Disease/Shenzhen Third People's Hospital , Tuberculosis and Diabetes Branch of Chinese Antituberculosis Association , Multidisciplinary Diagnosis and Treatment Branch of Chinese Antituberculosis Association . Expert consensus on the rational use of rifamycins in the treatment of tuberculosis with comorbidities[J]. Chinese Journal of Antituberculosis, 2025, 47(11): 1391-1415. doi: 10.19982/j.issn.1000-6621.20250254

Figures/Tables 17

药物	利福平	利福喷丁	利福布汀	推荐意见	证据等级
二甲双胍	降糖作用增强	-	-	监测血糖,必要时减少二甲双胍剂量	1B
沙格列汀	沙格列汀AUC降低73%,峰浓度降低53%,作用不受影响	-	-	监测血糖,与利福平、利福喷丁、利福布汀谨慎合用	1B
利格列汀	利格列汀AUC降低约40%	-	-	监测血糖,必要时增加利格列汀剂量,或将利福平更换为利福喷丁、利福布汀	2B
维格列汀	无报道	-	-	与利福平、利福喷丁、利福布汀谨慎合用	2C
卡格列净	卡格列净AUC降低51%	-	-	监测血糖,必要时增加卡格列净剂量,或将利福平更换为利福喷丁、利福布汀	1B
达格列净	达格列净AUC降低22%,峰浓度降低7%	-	-	与利福平、利福喷丁、利福布汀谨慎合用,不调整剂量	1B
格列齐特	格列齐特AUC降低70%	-	-	监测血糖,必要时增加格列齐特剂量,或将利福平更换为利福喷丁、利福布汀	1B
格列美脲	格列美脲AUC降低34%	-	-	监测血糖,必要时增加格列美脲剂量,或将利福平更换为利福喷丁、利福布汀	1B
那格列奈	那格列奈AUC降低24%	-	-	监测血糖,必要时增加那格列奈剂量,或将利福平更换为利福喷丁、利福布汀	1B
瑞格列奈	瑞格列奈AUC降低57%	-	-	监测血糖,增加瑞格列奈的给药剂量,或将利福平更换为利福喷丁、利福布汀	1B
吡格列酮	吡格列酮AUC降低54%	-	-	监测血糖,增加吡格列酮剂量,最大剂量不超过45mg;当使用45mg吡格列酮,血糖仍控制不理想时,建议考虑将利福平更换为利福喷丁、利福布汀继续监测,或更换其他降糖方案	2B 1B
罗格列酮	罗格列酮AUC降低54%~65%			监测血糖;必要时更换降糖药物;或将利福平更换为利福喷丁、利福布汀	2B
多格列艾汀	多格列艾汀预计AUC降低51%以上			监测血糖;必要时更换降糖药物;或将利福平更换为利福喷丁、利福布汀	2C
利拉鲁肽	相互作用可能性极低	-	-	与利福平、利福喷丁、利福布汀谨慎合用,监测胃肠道不良反应	1C
司美格鲁肽	相互作用可能性极低	-	-	与利福平、利福喷丁、利福布汀谨慎合用,监测胃肠道不良反应	1C

药物	利福平	利福喷丁	利福布汀	推荐意见	证据等级
螺内酯	可能存在潜在的相互作用	-	-	与利福平、利福喷丁、利福布汀谨慎合用,监测治疗反应	1D
硝苯地平	硝苯地平AUC降低60%,高血压恶化增加	-	-	与利福平、利福喷丁、利福布汀避免合用	1C
氨氯地平	氨氯地平血药浓度降低,肾功能损伤者降低81.7%±20.6%	-	-	密切监测血压;与利福平避免合用,尤其是肾功能损伤者。与利福喷丁、利福布汀谨慎合用。确需使用利福平时更换降压药物,或增加氨氯地平剂量	1A
二氢吡啶类钙通道阻滞剂 (尼卡地平、尼莫地平、非洛地平等)	二氢吡啶类血药浓度剧烈降低	-	-	密切监测血压;与利福平避免合用,与利福喷丁、利福布汀谨慎合用。更换降压药物,确需使用利福平时增加本类药物剂量,或将利福平更换为利福喷丁、利福布汀	1A
厄贝沙坦	对厄贝沙坦的影响可能较小	-	-	与利福平、利福喷丁、利福布汀谨慎合用	1C
氯沙坦	氯沙坦AUC降低35%,活性代谢物AUC降低40%	-	-	监测血压;与利福平、利福喷丁、利福布汀谨慎合用,在出现血压升高时,考虑增加氯沙坦的剂量,或将利福平更换为利福喷丁、利福布汀	1B
沙库巴曲缬沙坦	影响较小	-	-	与利福平、利福喷丁、利福布汀谨慎合用	1C
美托洛尔	肾功能不全者美托洛尔药物浓度降低91.9%±16.2%	-	-	监测血压;肾功能不全者,美托洛尔与利福平避免合用。确需与利福平合用时,增加美托洛尔剂量,或将利福平更换为利福喷丁、利福布汀	2B
比索洛尔	比索洛尔AUC降低34%	-	-	监测血压;仅在治疗反应不佳时,考虑增加比索洛尔的剂量,或将利福平更换为利福喷丁、利福布汀	2B
普萘洛尔	普萘洛尔血药浓度降低20%~40%,预计会发生临床疗效减弱	-	-	建议更换为同类药物,或将利福平更换为利福喷丁、利福布汀,并监测治疗反应	2C
特拉唑嗪	可能不存在有意义的药物相互作用	-	-	与利福平、利福喷丁、利福布汀谨慎合用	1C
福辛普利	可能不存在有意义的药物相互作用	-	-	与利福平、利福喷丁、利福布汀谨慎合用	1C
卡托普利	可能不存在有意义的药物相互作用	-	-	与利福平、利福喷丁、利福布汀谨慎合用	1C
贝那普利	可能不存在有意义的药物相互作用	-	-	与利福平、利福喷丁、利福布汀谨慎合用	1C

药物	利福平	利福喷丁	利福布汀	推荐意见	证据等级
奥希替尼	奥希替尼AUC降低约78%	-	-	与利福平、利福喷丁、利福布汀避免合用,或按说明书增加奥希替尼剂量	1B
伏美替尼	伏美替尼AUC降低86%,总活性物质AUC降低62%	-	-	与利福平、利福喷丁、利福布汀避免合用,或按说明书增加伏美替尼剂量	1B
吉非替尼	吉非替尼AUC降低83%	-	-	与利福平、利福喷丁、利福布汀避免合用,或按说明书增加吉非替尼剂量	1B
厄洛替尼	厄洛替尼AUC降低约67%	-	-	与利福平、利福喷丁、利福布汀避免合用,或按说明书增加厄洛替尼剂量	1B
克唑替尼	克唑替尼AUC降低82%,活性代谢物AUC降低94%	-	-	与利福平、利福喷丁、利福布汀避免合用	1B
伊马替尼	伊马替尼峰浓度降低54%,AUC降低74%	-	-	与利福平、利福喷丁、利福布汀避免合用	1B
尼洛替尼	尼洛替尼AUC降低80%	-	-	与利福平、利福喷丁、利福布汀避免合用	1B
瑞戈非尼	瑞戈非尼AUC降低50%,代谢物AUC升高264%	-	-	与利福平、利福喷丁、利福布汀避免合用	1B
阿帕替尼	阿帕替尼AUC降低83%	-	-	与利福平、利福喷丁、利福布汀避免合用	1B
多纳非尼	预计药物相互作用较小	-	-	与利福平、利福喷丁、利福布汀谨慎合用	1C
仑伐替尼	预计仅有轻微影响			与利福平、利福喷丁、利福布汀谨慎合用	1C
培美曲塞	预计影响较小	-	-	与利福平、利福喷丁、利福布汀谨慎合用	1C
铂类	预计影响较小			与利福平、利福喷丁、利福布汀谨慎合用	1C
紫杉醇	紫杉醇的药物暴露可能降低	-	-	与利福平、利福喷丁、利福布汀谨慎合用,关注其疗效下降	1C
多西他赛	多西他赛的药物暴露可能降低	-	-	与利福平、利福喷丁、利福布汀谨慎合用,关注其疗效下降	1C
吉西他滨	-	-	-	与利福平、利福喷丁、利福布汀谨慎合用	1C
氟尿嘧啶	-	-	-	与利福平、利福喷丁、利福布汀谨慎合用	1C
他莫昔芬	他莫昔芬AUC降低86%	-	-	与利福平、利福喷丁、利福布汀避免合用	1B
托瑞米芬	托瑞米芬AUC降低87%	-	-	与利福平、利福喷丁、利福布汀避免合用	1B
伊立替康	伊立替康活性代谢物SN-38的AUC降低20%,SN-38G的AUC降低58.8%	-	-	与利福平、利福喷丁、利福布汀谨慎合用	2C

药物	利福平	利福喷丁	利福布汀	推荐意见	证据等级
多替拉韦	多替拉韦AUC下降54%	多替拉韦谷浓度下降53%	多替拉韦AUC下降5%	与利福平合用时,多替拉韦剂量增加到2次/d。与利福喷丁合用时,如利福喷丁给药频次为1次/d,需增加多替拉韦剂量;如利福喷丁给药频次为1次/周,则无需调整剂量;如利福喷丁给药频次为2次/周,需加强疗效监测。多替拉韦与利福布汀合用无需调整剂量	1B
拉替拉韦	拉替拉韦AUC下降40%	拉替拉韦AUC无明显变化	-	与利福平合用时,拉替拉韦剂量增加到2次/d,与利福喷丁、利福布汀合用无需调整剂量	1B
比克替拉韦	比克替拉韦AUC下降75%	-	比克替拉韦AUC下降38%	与利福平、利福喷丁、利福布汀避免合用	1B
拉米夫定	预计不存在有临床意义的相互作用	预计不存在有临床意义的相互作用	预计不存在有临床意义的相互作用	与利福平、利福喷丁、利福布汀谨慎合用	1B
阿巴卡韦	预计不存在有临床意义的相互作用	预计不存在有临床意义的相互作用	预计不存在有临床意义的相互作用	与利福平、利福喷丁、利福布汀谨慎合用	1B
多拉韦林	多拉韦林AUC下降88%	-	多拉韦林AUC降低50%	与利福平、利福喷丁避免合用,与利福布汀合用,多拉韦林给药增加到2次/d	1B
利匹韦林	利匹韦林AUC下降80%	-	利匹韦林AUC下降43%	与利福平、利福喷丁避免合用,与利福布汀合用,利匹韦林给药量增加到50mg(1次/d)	1B
依非韦伦	依非韦伦AUC降低26%	依非韦伦表观清除率增加4%	利福布汀AUC下降38%	与利福平合用,体质量50kg以上者增加依非韦伦的剂量到800mg(1次/d);与利福布汀合用,利福布汀剂量增加50%;与利福喷丁合用,无需调整剂量	1B
达芦那韦/ 考比司他	预计达芦那韦、考比司他的血药浓度降低	达芦那韦AUC下降71%	预计达芦那韦、考比司他的血药浓度降低,利福布汀的暴露增加	达芦那韦/考比司他与利福平、利福喷丁避免合用,与利福布汀合用时,减少利福布汀的剂量到150mg(1次/2d)	1B

References 198

[1]	胡鑫洋, 高静韬. 世界卫生组织《2024年全球结核病报告》解读. 结核与肺部疾病杂志, 2024, 5 (6): 500-504. doi:10.19983/j.issn.2096-8493.2024164.
[2]	Schünemann H, Brożek J, Guyatt G, et al. GRADE handbook. Hamilton:GRADE Working Group 2013.
[3]	Burman WJ, Gallicano K, Peloquin C. Comparative pharmacokinetics and pharmacodynamics of the rifamycin antibacterials. Clin Pharmacokinet, 2001, 40(5): 327-341. doi:10.2165/00003088-200140050-00002. pmid: 11432536
[4]	Hibma JE, Radtke KK, Dorman SE, et al. Rifapentine Population Pharmacokinetics and Dosing Recommendations for Latent Tuberculosis Infection. Am J Respir Crit Care Med, 2020, 202(6): 866-877. doi:10.1164/rccm.201912-2489OC.
[5]	中华人民共和国国家药典委员会. 中华人民共和国药典临床用药须知(2020年版): 化学药和生物制品卷. 北京: 中国医药科技出版社, 2022: 1055-1059.
[6]	Surette MD, Spanogiannopoulos P, Wright GD. The Enzymes of the Rifamycin Antibiotic Resistome. Acc Chem Res, 2021, 54(9): 2065-2075. doi:10.1021/acs.accounts.1c00048.
[7]	Asif M, Qusty NF, Alghamdi S. An Overview of Various Rifampicin Analogs against Mycobacterium tuberculosis and their Drug Interactions. Med Chem, 2024, 20(3): 268-292. doi:10.2174/0115734064260853230926080134.
[8]	Loos U, Musch E, Jensen JC, et al. Pharmacokinetics of oral and intravenous rifampicin during chronic administration. Klin Wochenschr, 1985, 63(23): 1205-1211. doi:10.1007/BF01733779. pmid: 4087830
[9]	Reinach B, de Sousa G, Dostert P, et al. Comparative effects of rifabutin and rifampicin on cytochromes P450 and UDP-glucuronosyl-transferases expression in fresh and cryopreserved human hepatocytes. Chem Biol Interact, 1999, 121(1): 37-48. doi:10.1016/s0009-2797(99)00089-7.
[10]	利福平胶囊药品说明书. 批准文号: H51022701. 2024-11-13.
[11]	利福喷丁胶囊药品说明书. 批准文号: H10940199. 2024-12-26.
[12]	US Food and Drug Administration. Sanofi Aventis US: PRIFTIN Labeling-Package Insert[DB/OL]. [2025-09-12]. https://www.accessdata.fda.gov/drugsatfda_docs/label/1998/21024lbl.pdf.
[13]	Heifets L, Sanchez T, Vanderkolk J, et al. Development of rifapentine susceptibility tests for Mycobacterium tuberculosis. Antimicrob Agents Chemother, 1999, 43(1): 25-28. doi:10.1128/AAC.43.1.25. pmid: 9869560
[14]	Mor N, Simon B, Mezo N, et al. Comparison of activities of rifapentine and rifampin against Mycobacterium tuberculosis residing in human macrophages. Antimicrob Agents Chemother, 1995, 39(9): 2073-2077. doi:10.1128/AAC.39.9.2073. pmid: 8540718
[15]	Della Bruna C, Schioppacassi G, Ungheri D, et al. LM 427, a new spiropiperidylrifamycin: in vitro and in vivo studies. J Antibiot (Tokyo), 1983, 36(11): 1502-1506. doi:10.7164/antibiotics.36.1502.
[16]	Truffot-Pernot C, Giroir AM, Maury L, et al. Study of the minimal inhibitory concentration of rifabutine (Ansamycin LM 427) for Mycobacterium tuberculosis, Mycobacterium xenopi and Mycobacterium avium-intracellulare. Rev Mal Respir, 1988, 5(4): 401-406. pmid: 2845531
[17]	利福布汀胶囊药品说明书. 批准文号: H20070296. 2022-04-08.
[18]	US Food and Drug Administration. Pfizer: MYCOBUTIN Labeling-Package Insert[DB/OL]. [2025-09-12]. https://www.accessdata.fda.gov/drugsatfda_docs/label/2024/050689s027lbl.pdf.
[19]	Crabol Y, Catherinot E, Veziris N, et al. Rifabutin: where do we stand in 2016?. J Antimicrob Chemother, 2016, 71(7): 1759-1771. doi:10.1093/jac/dkw024. pmid: 27009031
[20]	Mangat R, Brode SK, Mah HK, et al. Characteristics of and treatment outcomes in rifampicin-intolerant patients. IJTLD Open, 2024, 1(4): 160-165. doi:10.5588/ijtldopen.23.0466. pmid: 38988405
[21]	国家药品监督管理局药品审评中心.国家药监局药审中心关于发布《药物相互作用研究技术指导原则(试行)》的通告(2021年第4号). 2021-01-25.
[22]	MacDougall C, Canonica T, Keh C, et al. Systematic review of drug-drug interactions between rifamycins and anticoagulant and antiplatelet agents and considerations for management. Pharmacotherapy, 2022, 42(4): 343-361. doi:10.1002/phar.2672.
[23]	Chen J, Li J, Wu J, et al. An open-label study to explore the optimal design of CYP3A drug-drug interaction clinical trials in healthy Chinese people. Pharmacol Res Perspect, 2024, 12(4): e1252. doi:10.1002/prp2.1252.
[24]	Gallicano KD, Sahai J, Shukla VK, et al. Induction of zidovudine glucuronidation and amination pathways by rifampicin in HIV-infected patients. Br J Clin Pharmacol, 1999, 48(2): 168-179. doi:10.1046/j.1365-2125.1999.00987.x.
[25]	Phondeth L, Kamaraj R, Nilles J, et al. Rifabutin but not rifampicin can partly out-balance P-glycoprotein induction by concurrent P-glycoprotein inhibition through high affinity binding to the inhibitory site. Arch Toxikol, 2024, 98(1): 223-231. doi:10.1007/s00204-023-03618-w.
[26]	Parvez MM, Jung JA, Shin HJ, et al. Characterization of 22 Antituberculosis Drugs for Inhibitory Interaction Potential on Organic Anionic Transporter Polypeptide (OATP)-Mediated Uptake. Antimicrob Agents Chemother, 2016, 60(5): 3096-3105. doi:10.1128/AAC.02765-15. pmid: 26976869
[27]	Cho SK, Yoon JS, Lee MG, et al. Rifampin enhances the glucose-lowering effect of metformin and increases OCT 1 mRNA levels in healthy participants. Clin Pharmacol Ther, 2011, 89(3): 416-421. doi:10.1038/clpt.2010.266. pmid: 21270793
[28]	US Food and Drug Administration. Astrazeneca AB: ONGLYZA Labeling-Package Insert[DB/OL]. [2025-09-12]. https://www.accessdata.fda.gov/drugsatfda_docs/label/2024/022350s026lbl.pdf.
[29]	Upreti VV, Boulton DW, Li L, et al. Effect of rifampicin on the pharmacokinetics and pharmacodynamics of saxagliptin, a dipeptidyl peptidase-4 inhibitor, in healthy subjects. Br J Clin Pharmacol, 2011, 72(1): 92-102. doi:10.1111/j.1365-2125.2011.03937.x.
[30]	US Food and Drug Administration. Boehringer Ingelheim: TRADJENTA Labeling-Package Insert[DB/OL]. [2025-09-12]. https://www.accessdata.fda.gov/drugsatfda_docs/label/2023/201280s027lbl.pdf.
[31]	维格列汀片(佳维乐)说明书. 批准文号: H20170023. 2018-10-15.
[32]	Devineni D, Vaccaro N, Murphy J, et al. Effects of rifampin, cyclosporine A, and probenecid on the pharmacokinetic profile of canagliflozin, a sodium glucose co-transporter 2 inhibitor, in healthy participants. Int J Clin Pharmacol Ther, 2015, 53(2): 115-128. doi:10.5414/CP202158.
[33]	US Food and Drug Administration. Janssen Pharms: INVOKANA Labeling-Package Insert[DB/OL]. [2025-09-12]. https://www.accessdata.fda.gov/drugsatfda_docs/label/2024/204042s043lbl.pdf.
[34]	Kasichayanula S, Liu X, Griffen SC, et al. Effects of rifampin and mefenamic acid on the pharmacokinetics and pharmacodynamics of dapagliflozin. Diabetes Obes Metab, 2013, 15(3): 280-283. doi:10.1111/dom.12024. pmid: 23061428
[35]	US Food and Drug Administration. Astrazeneca AB: FARXIGA Labeling-Package Insert[DB/OL]. [2025-09-12]. https://www.accessdata.fda.gov/drugsatfda_docs/label/2024/202293s031lbl.pdf.
[36]	Park JY, Kim KA, Park PW, et al. Effect of rifampin on the pharmacokinetics and pharmacodynamics of gliclazide. Clin Pharmacol Ther, 2003, 74(4): 334-340. doi:10.1016/S0009-9236(03)00221-2.
[37]	Kang P, Cho CK, Jang CG, et al. Effects of CYP2C9 and CYP2C 19 genetic polymorphisms on the pharmacokinetics and pharmacodynamics of gliclazide in healthy subjects. Arch Pharm Res, 2023, 46(5): 438-447. doi:10.1007/s12272-023-01448-z.
[38]	Niemi M, Kivistö KT, Backman JT, et al. Effect of rifampicin on the pharmacokinetics and pharmacodynamics of glimepiride. Br J Clin Pharmacol, 2000, 50(6): 591-595. doi:10.1046/j.1365-2125.2000.00295.x.
[39]	US Food and Drug Administration. Sanofi Aventis US: AMARYL Labeling-Package Insert[DB/OL]. [2025-09-12]. https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/020496s029lbl.pdf.
[40]	那格列奈片(唐力)药品说明书. 批准文号: H20030503. 2018-03-06.
[41]	Niemi M, Backman JT, Neuvonen M, et al. Effect of rifam-picin on the pharmacokinetics and pharmacodynamics of nateglinide in healthy subjects. Br J Clin Pharmacol, 2003, 56(4): 427-432. doi:10.1046/j.1365-2125.2003.01884.x.
[42]	Niemi M, Backman JT, Neuvonen M, et al. Rifampin decreases the plasma concentrations and effects of repaglinide. Clin Pharmacol Ther, 2000, 68(5): 495-500. doi:10.1067/mcp.2000.111183. pmid: 11103752
[43]	Bidstrup TB, Stilling N, Damkier P, et al. Rifampicin seems to act as both an inducer and an inhibitor of the metabolism of repaglinide. Eur J Clin Pharmacol, 2004, 60(2): 109-114. doi:10.1007/s00228-004-0746-z. pmid: 15034704
[44]	US Food and Drug Administration. Gemini Labs: PRANDIN Labeling-Package Insert[DB/OL]. [2025-09-12]. https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/020741s044lbl.pdf.
[45]	US Food and Drug Administration. Takeda Pharms Usa: ACTOS Labeling-Package Insert[DB/OL]. [2025-09-12]. https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021073s049lbl.pdf.
[46]	Jaakkola T, Backman JT, Neuvonen M, et al. Effect of rifampicin on the pharmacokinetics of pioglitazone. Br J Clin Pharmacol, 2006, 61(1): 70-78. doi:10.1111/j.1365-2125.2005.02515.x.
[47]	Park JY, Kim KA, Kang MH, et al. Effect of rifampin on the pharmacokinetics of rosiglitazone in healthy subjects. Clin Pharmacol Ther, 2004, 75(3): 157-162. doi:10.1016/j.clpt.2003.10.003.
[48]	多格列艾汀片药品说明书. 批准文号: H20220024. 2024-07-23.
[49]	Xie P, Abildlund MT, Bækdal TA, et al. A phase 1, randomized, double-blind, placebo-controlled trial investigating the pharmacokinetics, pharmacodynamics, safety and tolerability of oral semaglutide in healthy Chinese subjects. Diabetes Obes Metab, 2024, 26(8): 3068-3077. doi:10.1111/dom.15624.
[50]	Hall S, Isaacs D, Clements JN. Pharmacokinetics and Clinical Implications of Semaglutide: A New Glucagon-Like Peptide (GLP)-1 Receptor Agonist. Clin Pharmacokinet, 2018, 57(12): 1529-1538. doi:10.1007/s40262-018-0668-z. pmid: 29915923
[51]	Jiang J, Zhang J, Jacobsen LV, et al. The pharmacokinetics, pharmacodynamics, and tolerability of liraglutide, a once-daily human GLP-1 analogue, after multiple subcutaneous administration in healthy Chinese male subjects. J Clin Pharmacol, 2011, 51(12): 1620-1627. doi:10.1177/0091270010389468.
[52]	Malm-Erjefält M, Bjørnsdottir I, Vanggaard J, et al. Metabolism and excretion of the once-daily human glucagon-like peptide-1 analog liraglutide in healthy male subjects and its in vitro degradation by dipeptidyl peptidase IV and neutral endopeptidase. Drug Metab Dispos, 2010, 38(11): 1944-1953. doi:10.1124/dmd.110.034066. pmid: 20709939
[53]	US Food and Drug Administration. Pfizer: ALDACTONE Labeling-Package Insert[DB/OL]. [2025-09-12]. https://www.accessdata.fda.gov/drugsatfda_docs/label/2022/012151s079lbl.pdf.
[54]	US Food and Drug Administration. Viatris: NORVASC Labeling-Package Insert[DB/OL]. [2025-09-12]. https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/019787s062lbl.pdf.
[55]	盐酸尼卡地平缓释胶囊(佩尔)药品说明书. 批准文号: H20030233. 2015-12-16.
[56]	尼莫地平片(尼膜同)药品说明书. 批准文号: H20003010. 2024-10-18.
[57]	盐酸乐卡地平片(再宁平)药品说明书. 批准文号: HJ20160258. 2022-04-25.
[58]	US Food and Drug Administration. Bayer Pharms: ADALAT Labeling-Package Insert[DB/OL]. [2025-09-12]. https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/020198s023lbl.pdf.
[59]	Ndanusa BU, Mustapha A, Abdu-Aguye I. The effect of single does of rifampicin on the pharmacokinetics of oral nifedipine. J Pharm Biomed Anal, 1997, 15(9-10): 1571-1575. doi:10.1016/s0731-7085(97)00044-7. pmid: 9226591
[60]	非洛地平缓释片(波依定)药品说明书. 批准文号: H20030414. 2020-04-17.
[61]	氯沙坦钾片(科素亚)药品说明书. 批准文号: HJ20171245. 2022-07-12.
[62]	Williamson KM, Patterson JH, McQueen RH, et al. Effects of erythromycin or rifampin on losartan pharmacokinetics in healthy volunteers. Clin Pharmacol Ther, 1998, 63(3): 316-323. doi:10.1016/S0009-9236(98)90163-1. pmid: 9542475
[63]	厄贝沙坦片(安博维)药品说明书. 批准文号: HJ 20171182. 2024-07-03.
[64]	缬沙坦胶囊(代文)药品说明书. 批准文号: H20040217. 2020-08-28.
[65]	美托洛尔片(倍他乐克)药品说明书. 批准文号: H32025390. 2025-01-22.
[66]	Bennett PN, John VA, Whitmarsh VB. Effect of rifampicin on metoprolol and antipyrine kinetics. Br J Clin Pharmacol, 1982, 13(3): 387-391. doi:10.1111/j.1365-2125.1982.tb01390.x.
[67]	Kirch W, Rose I, Klingmann I, et al. Interaction of bisoprolol with cimetidine and rifampicin. Eur J Clin Pharmacol, 1986, 31(1): 59-62. doi:10.1007/BF00870987. pmid: 2877885
[68]	Herman RJ, Nakamura K, Wilkinson GR, et al. Induction of propranolol metabolism by rifampicin. Br J Clin Pharmacol, 1983, 16(5): 565-569. doi:10.1111/j.1365-2125.1983.tb02218.x.
[69]	Liu W, Yan T, Chen K, et al. Predicting Interactions between Rifampin and Antihypertensive Drugs Using the Biopharmaceutics Drug Disposition Classification System. Pharmacotherapy, 2020, 40(4): 274-290. doi:10.1002/phar.2380.
[70]	Flarakos J, Du Y, Bedman T, et al. Disposition and metabolism of [¹⁴C] Sacubitril/Valsartan (formerly LCZ696) an angiotensin receptor neprilysin inhibitor, in healthy subjects. Xenobiotica, 2016, 46(11): 986-1000. doi:10.3109/00498254.2015.1014944. pmid: 26931777
[71]	Oude Munnink TH, Demmer A, Slenter RHJ, et al. Amiodarone Rifampicin Drug-Drug Interaction Management With Therapeutic Drug Monitoring. Ther Drug Monit, 2018, 40(2): 159-161. doi:10.1097/FTD.0000000000000487. pmid: 29470228
[72]	Zarembski DG, Fischer SA, Santucci PA, et al. Impact of rifampin on serum amiodarone concentrations in a patient with congenital heart disease. Pharmacotherapy, 1999, 19(2): 249-251. doi:10.1592/phco.19.3.249.30929. pmid: 10030779
[73]	盐酸索他洛尔片(伟特)药品说明书. 批准文号: H20000238. 2022-10-20.
[74]	盐酸维拉帕米片说明书. 批准文号: H12020051. 2020-07-20.
[75]	Barbarash RA. Verapamil-rifampin interaction. Drug Intell Clin Pharm, 1985, 19(7-8):559-560. doi:10.1177/106002808501900712. pmid: 4028962
[76]	Dilger K, Greiner B, Fromm MF, et al. Consequences of rifampicin treatment on propafenone disposition in extensive and poor metabolizers of CYP2D6. Pharmacogenetics, 1999, 9(5): 551-559. pmid: 10591535
[77]	Backman JT, Luurila H, Neuvonen M, et al. Rifampin markedly decreases and gemfibrozil increases the plasma concentrations of atorvastatin and its metabolites. Clin Pharmacol Ther, 2005, 78(2): 154-167. doi:10.1016/j.clpt.2005.04.007. pmid: 16084850
[78]	瑞舒伐他汀钙片(可定)药品说明书. 批准文号: HJ20160546. 2024-03-18.
[79]	Oswald S, Giessmann T, Luetjohann D, et al. Disposition and sterol-lowering effect of ezetimibe are influenced by single-dose coadministration of rifampin, an inhibitor of multidrug transport proteins. Clin Pharmacol Ther, 2006, 80(5): 477-485. doi:10.1016/j.clpt.2006.07.006. pmid: 17112804
[80]	阿司匹林肠溶片(拜阿司匹灵)说明书. 批准文号: H20130339. 2021-02-06.
[81]	Lau WC, Gurbel PA, Watkins PB, et al. Contribution of hepatic cytochrome P 450 3A4 metabolic activity to the phenomenon of clopidogrel resistance. Circulation, 2004, 109(2): 166-171. doi:10.1161/01.CIR.0000112378.09325.F9.
[82]	Judge HM, Patil SB, Buckland RJ, et al. Potentiation of clopidogrel active metabolite formation by rifampicin leads to greater P2Y 12 receptor blockade and inhibition of platelet aggregation after clopidogrel. J Thromb Haemost, 2010, 8(8): 1820-1827. doi:10.1111/j.1538-7836.2010.03925.x.
[83]	US Food and Drug Administration. Astrazeneca: BRILINTA Labeling-Package Insert[DB/OL]. [2025-09-12]. https://www.accessdata.fda.gov/drugsatfda_docs/label/2024/022433s037lbl.pdf.
[84]	Teng R, Mitchell P, Butler K. Effect of rifampicin on the pharmacokinetics and pharmacodynamics of ticagrelor in healthy subjects. Eur J Clin Pharmacol, 2013, 69(4): 877-883. doi:10.1007/s00228-012-1436-x. pmid: 23093043
[85]	盐酸伊伐布雷定片(可兰特)药品说明书. 批准文号: H20160102. 2020-12-09.
[86]	地高辛片(可力)药品说明书. 批准文号: H33021738. 2023-11-14.
[87]	Bussey HI, Merritt GJ, Hill EG. The influence of rifampin on quinidine and digoxin. Arch Intern Med, 1984, 144(5): 1021-1023. doi:10.1001/archinte.1984.00350170183029. pmid: 6712395
[88]	Oh J, Kim B, Lee S. Effects of rifampin coadministration on the pharmacokinetics of digoxin: a real-world data approach. Transl Clin Pharmacol, 2023, 31(3): 148-153. doi:10.12793/tcp.2023.31.e13. pmid: 37810625
[89]	Boettcher M, Gerisch M, Lobmeyer M, et al. Metabolism and Pharmacokinetic Drug-Drug Interaction Profile of Vericiguat, A Soluble Guanylate Cyclase Stimulator: Results From Preclinical and Phase I Healthy Volunteer Studies. Clin Pharmacokinet, 2020, 59(11): 1407-1418. doi:10.1007/s40262-020-00895-x.
[90]	O’Reilly RA. Interaction of chronic daily warfarin therapy and rifampin. Ann Intern Med, 1975, 83(4): 506-508. doi:10.7326/0003-4819-83-4-506. pmid: 1166982
[91]	Center for Drug Evaluation and Research. Clinical pharmacology and biopharmaceutics reviews. Application number: 022406 Orig1s000[EB/OL]. (2013-09-05) [2025-05-20]. https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022406Orig1s000ClinPharmR.pdf.
[92]	Mendell J, Chen S, He L, et al. The effect of rifampin on the pharmacokinetics of edoxaban in healthy adults. Clin Drug Investig, 2015, 35(7): 447-453. doi:10.1007/s40261-015-0298-2.
[93]	Lutz JD, Kirby BJ, Wang L, et al. Cytochrome P450 3A Induction Predicts P-glycoprotein Induction; Part 1: Establi-shing Induction Relationships Using Ascending Dose Rifampin. Clin Pharmacol Ther, 2018, 104(6): 1182-1190. doi:10.1002/cpt.1073.
[94]	Härtter S, Koenen-Bergmann M, Sharma A, et al. Decrease in the oral bioavailability of dabigatran etexilate after co-medication with rifampicin. Br J Clin Pharmacol, 2012, 74(3): 490-500. doi:10.1111/j.1365-2125.2012.04218.x.
[95]	Lutz JD, Kirby BJ, Wang L, et al. Cytochrome P450 3A Induction Predicts P-glycoprotein Induction; Part 2: Prediction of Decreased Substrate Exposure After Rifabutin or Carbama-zepine. Clin Pharmacol Ther, 2018, 104(6): 1191-1198. doi:10.1002/cpt.1072.
[96]	US Food and Drug Administration. Horizon: RAYOS Labeling-Package Insert[DB/OL]. [2025-09-12]. https://www.accessdata.fda.gov/drugsatfda_docs/label/2024/202020s013lbl.pdf.
[97]	McAllister WA, Thompson PJ, Al-Habet SM, et al. Rifam-picin reduces effectiveness and bioavailability of prednisolone. Br Med J (Clin Res Ed), 1983, 286(6369): 923-925. doi:10.1136/bmj.286.6369.923. pmid: 6403136
[98]	Baciewicz AM, Self TH. Rifampin drug interactions. Arch Intern Med, 1984, 144(8): 1667-1671. doi:10.1001/archinte.144.8.1667. pmid: 6380442
[99]	Pozniak AL, Coyne KM, Miller RF, et al. British HIV Association guidelines for the treatment of TB/HIV coinfection 2011. HIV Med, 2011, 12(9): 517-524. doi:10.1111/j.1468-1293.2011.00954.x.
[100]	中华医学会器官移植学分会. 中国肾移植受者结核病临床诊疗指南(2023版). 器官移植, 2024, 15(3): 323-332. doi:10.3969/j.issn.1674-7445.2024098.
[101]	Yee GC, McGuire TR. Pharmacokinetic drug interactions with cyclosporin (Part II). Clin Pharmacokinet, 1990, 19(5): 400-415. doi:10.2165/00003088-199019050-00004. pmid: 2268987
[102]	他克莫司胶囊(普乐可复)药品说明书. 批准文号: J20150101. 2023-06-08.
[103]	Hebert MF, Fisher RM, Marsh CL, et al. Effects of rifampin on tacrolimus pharmacokinetics in healthy volunteers. J Clin Pharmacol, 1999, 39(1): 91-96. doi:10.1177/00912709922007499. pmid: 9987705
[104]	Kim OH, Shim TS, Jo KW. Drug-level change and optimal dose adjustment of tacrolimus with the use of rifabutin for treating mycobacterial disease in solid organ transplant recipients. Transpl Infect Dis, 2022, 24(4): e13893. doi:10.1111/tid.13893.
[105]	西罗莫司片(雷帕鸣)药品说明书. 批准文号: H20120482. 2013-08-01.
[106]	Tortorici MA, Matschke K, Korth-Bradley JM, et al. The effect of rifampin on the pharmacokinetics of sirolimus in healthy volunteers. Clin Pharmacol Drug Dev, 2014, 3(1): 51-56. doi:10.1002/cpdd.40.
[107]	Lefeuvre S, Rebaudet S, Billaud EM, et al. Management of rifamycins-everolimus drug-drug interactions in a liver-transplant patient with pulmonary tuberculosis. Transpl Int, 2012, 25(11): e120-e123. doi:10.1111/j.1432-2277.2012.01561.x.
[108]	吗替麦考酚酯片(骁悉)药品说明书. 批准文号: 20031240. 2024-05-07.
[109]	US Food and Drug Administration. Novartis: MYFORTIC Labeling-Package Insert[DB/OL]. [2025-09-12]. https://www.accessdata.fda.gov/drugsatfda_docs/label/2022/050791s035lbl.pdf.
[110]	Naesens M, Kuypers DR, Streit F, et al. Rifampin induces alterations in mycophenolic acid glucuronidation and elimination: implications for drug exposure in renal allograft recipients. Clin Pharmacol Ther, 2006, 80(5): 509-521. doi:10.1016/j.clpt.2006.08.002. pmid: 17112807
[111]	Hwang S, Lee Y, Jang Y, et al. Comprehensive Evaluation of OATP- and BCRP-Mediated Drug-Drug Interactions of Methotrexate Using Physiologically-Based Pharmacokinetic Modeling. Clin Pharmacol Ther, 2024, 116(4): 1013-1022. doi:10.1002/cpt.3329. pmid: 38860384
[112]	Shaffer JL, Hughes S, Linaker BD, et al. Controlled trial of rifampicin and ethambutol in Crohn’s disease. Gut, 1984, 25(2): 203-205. doi:10.1136/gut.25.2.203. pmid: 6363219
[113]	Shaffer JL, Houston JB. The effect of rifampicin on sulphapyridine plasma concentrations following sulphasalazine administration. Br J Clin Pharmacol, 1985, 19(4): 526-528. doi:10.1111/j.1365-2125.1985.tb02682.x.
[114]	柳氮磺吡啶肠溶片药品说明书. 批准文号: H31020450. 2013-09-23.
[115]	US Food and Drug Administration. Sanofi Aventis US: ARAVA Labeling-Package Insert[DB/OL]. [2025-09-12]. https://www.accessdata.fda.gov/drugsatfda_docs/label/2024/020905s033lbl.pdf.
[116]	Lemaitre F, Solas C, Grégoire M, et al. Potential drug-drug interactions associated with drugs currently proposed for COVID-19 treatment in patients receiving other treatments. Fundam Clin Pharmacol, 2020, 34(5): 530-547. doi:10.1111/fcp.12586.
[117]	Ducharme J, Farinotti R. Clinical pharmacokinetics and metabolism of chloroquine. Focus on recent advancements. Clin Pharmacokinet, 1996, 31(4): 257-274. doi:10.2165/00003088-199631040-00003. pmid: 8896943
[118]	注射用利福平(天再欣)药品说明书. 批准文号: H20153165. 2020-06-22.
[119]	Jayasagar G, Krishna Kumar M, Chandrasekhar K, et al. Influence of rifampicin pretreatment on the pharmacokinetics of celecoxib in healthy male volunteers. Drug Metabol Drug Interact, 2003, 19(4): 287-296. doi:10.1515/dmdi.2003.19.4.287. pmid: 14768975
[120]	Nam SH, Oh JS, Hong S, et al. Early discontinuation of tofacitinib in patients with rheumatoid arthritis co-treated with rifampin for latent tuberculosis. Joint Bone Spine, 2020, 87(5): 475-479. doi:10.1016/j.jbspin.2020.04.010. pmid: 32387584
[121]	枸橼酸托法替布片(尚杰)药品说明书. 批准文号: HJ20181078. 2022-10-11.
[122]	巴瑞替尼片(艾乐明)药品说明书. 批准文号: HJ20190039. 2024-04-29.
[123]	Mohamed MF, Jungerwirth S, Asatryan A, et al. Assessment of effect of CYP3A inhibition, CYP induction, OATP1B inhibition, and high-fat meal on pharmacokinetics of the JAK1 inhibitor upadacitinib. Br J Clin Pharmacol, 2017, 83(10): 2242-2248. doi:10.1111/bcp.13329. pmid: 28503781
[124]	乌帕替尼缓释片(瑞福)药品说明书. 批准文号: HJ20220010. 2023-10-24.
[125]	US Food and Drug Administration. Sanofi Aventis US: RIFADIN Labeling-Package Insert[DB/OL]. [2025-09-12]. https://www.accessdata.fda.gov/drugsatfda_docs/label/2024/050420s092,050627s037lbl.pdf.
[126]	Apseloff G, Hilligoss DM, Gardner MJ, et al. Induction of fluconazole metabolism by rifampin: in vivo study in humans. J Clin Pharmacol, 1991, 31(4): 358-361. doi:10.1002/j.1552-4604.1991.tb03718.x.
[127]	Jaruratanasirikul S, Sriwiriyajan S. Effect of rifampicin on the pharmacokinetics of itraconazole in normal volunteers and AIDS patients. Eur J Clin Pharmacol, 1998, 54(2): 155-158. doi:10.1007/s002280050437. pmid: 9626920
[128]	Moon SM, Jhun BW, Lee H, et al. Effect of a 150 mg dose of rifabutin on serum itraconazole levels in patients with coexisting chronic pulmonary aspergillosis and Mycobacterium avium complex lung disease. J Infect Chemother, 2017, 23(9): 658-660. doi:10.1016/j.jiac.2017.02.004.
[129]	US Food and Drug Administration. PF Prism CV: VFEND Labeling-Package Insert[DB/OL]. [2025-09-12]. https://www.accessdata.fda.gov/drugsatfda_docs/label/2022/021266s053,021267s063,021630s042lbl.pdf.
[130]	伏立康唑片(威凡)药品说明书. 批准文号: HJ20150051. 2024-06-03.
[131]	Krieter P, Flannery B, Musick T, et al. Disposition of posaconazole following single-dose oral administration in healthy subjects. Antimicrob Agents Chemother, 2004, 48(9): 3543-3551. doi:10.1128/AAC.48.9.3543-3551.2004.
[132]	Wang EJ, Lew K, Casciano CN, et al. Interaction of common azole antifungals with P glycoprotein. Antimicrob Agents Chemother, 2002, 46(1): 160-165. doi:10.1128/AAC.46.1.160-165.2002.
[133]	Power N, Lynch F, Denning DW, et al. Attainment of thera-peutic posaconazole serum levels during co-administration with rifampicin. J Glob Antimicrob Resist, 2020, 23: 284-285. doi:10.1016/j.jgar.2020.09.029.
[134]	Krishna G, Parsons A, Kantesaria B, et al. Evaluation of the pharmacokinetics of posaconazole and rifabutin following co-administration to healthy men. Curr Med Res Opin, 2007, 23(3): 545-552. doi:10.1185/030079906X167507. pmid: 17355736
[135]	Townsend R, Dietz A, Hale C, et al. Pharmacokinetic Evaluation of CYP3A4-Mediated Drug-Drug Interactions of Isavuconazole With Rifampin, Ketoconazole, Midazolam, and Ethinyl Estradiol/Norethindrone in Healthy Adults. Clin Pharmacol Drug Dev, 2017, 6(1): 44-53. doi:10.1002/cpdd.285.
[136]	艾沙康唑胶囊(康新博)药品说明书. 批准文号: HJ20210079. 2023-02-03.
[137]	US Food and Drug Administration. Astellas: CRESEMBA Labeling-Package Insert[DB/OL]. [2025-09-12]. https://www.accessdata.fda.gov/drugsatfda_docs/label/2023/207500s015,207501s013lbl.pdf.
[138]	国家卫生健康委员会办公厅.新型抗肿瘤药物临床应用指导原则(2024年版). 2024-12-30.
[139]	Vishwanathan K, Dickinson PA, So K, et al. The effect of itraconazole and rifampicin on the pharmacokinetics of osimer-tinib. Br J Clin Pharmacol, 2018, 84(6): 1156-1169. doi:10.1111/bcp.13534. pmid: 29381826
[140]	Zhu YT, Zhang YF, Jiang JF, et al. Effects of rifampicin on the pharmacokinetics of alflutinib, a selective third-generation EGFR kinase inhibitor, and its metabolite AST 5902 in healthy volunteers. Invest New Drugs, 2021, 39(4): 1011-1018. doi:10.1007/s10637-021-01071-z.
[141]	Swaisland HC, Ranson M, Smith RP, et al. Pharmacokinetic drug interactions of gefitinib with rifampicin, itraconazole and metoprolol. Clin Pharmacokinet, 2005, 44(10): 1067-1081. doi:10.2165/00003088-200544100-00005. pmid: 16176119
[142]	Hamilton M, Wolf JL, Drolet DW, et al. The effect of rifampicin, a prototypical CYP3A 4 inducer, on erlotinib pharmacokinetics in healthy subjects. Cancer Chemother Pharmacol, 2014, 73(3): 613-621. doi:10.1007/s00280-014-2390-3.
[143]	Xu H, O’Gorman M, Tan W, et al. The effects of ketocona-zole and rifampin on the single-dose pharmacokinetics of crizotinib in healthy subjects. Eur J Clin Pharmacol, 2015, 71(12): 1441-1449. doi:10.1007/s00228-015-1945-5.
[144]	Bolton AE, Peng B, Hubert M, et al. Effect of rifampicin on the pharmacokinetics of imatinib mesylate (Gleevec, STI571) in healthy subjects. Cancer Chemother Pharmacol, 2004, 53(2): 102-106. doi:10.1007/s00280-003-0722-9.
[145]	Tanaka C, Yin OQ, Smith T, et al. Effects of rifampin and ketoconazole on the pharmacokinetics of nilotinib in healthy participants. J Clin Pharmacol, 2011, 51(1): 75-83. doi:10.1177/0091270010367428.
[146]	US Food and Drug Administration. Bayer Hlthcare: STIVARGA Labeling-Package Insert[DB/OL]. [2025-09-12]. https://www.accessdata.fda.gov/drugsatfda_docs/label/2025/203085s016lbl.pdf.
[147]	Liu X, Zhang Y, Chen Q, et al. Pharmacokinetic Drug Intera-ctions of Apatinib With Rifampin and Itraconazole. J Clin Pharmacol, 2018, 58(3): 347-356. doi:10.1002/jcph.1016.
[148]	甲苯磺酸多纳非尼片药品说明书. 批准文号: H20210020. 2022-08-10.
[149]	甲磺酸仑伐替尼胶囊药品说明书. 批准文号: HJ20200044. 2020-11-04.
[150]	注射用培美曲塞二钠(力比泰)药品说明书. 批准文号: H20140662. 2024-06-04.
[151]	注射用奥沙利铂(乐沙定)药品说明书. 批准文号: HJ20171064. 2022-01-21.
[152]	Komoroski BJ, Parise RA, Egorin MJ, et al. Effect of the St. John’s wort constituent hyperforin on docetaxel metabolism by human hepatocyte cultures. Clin Cancer Res, 2005, 11(19 1): 6972-6979. doi:10.1158/1078-0432.CCR-04-2488.
[153]	Nagashima A, Matsumoto Y, Ohsawa M, et al. Treatment of advanced ovarian carcinoma coexistent with peritoneal tuberculosis. Mol Clin Oncol, 2013, 1(6): 1084-1086. doi:10.3892/mco.2013.183. pmid: 24649297
[154]	注射用吉西他滨(健择)药品说明书. 批准文号: HJ20160224. 2022-12-28.
[155]	Kivistö KT, Villikka K, Nyman L, et al. Tamoxifen and toremifene concentrations in plasma are greatly decreased by rifampin. Clin Pharmacol Ther, 1998, 64(6): 648-654. doi:10.1016/S0009-9236(98)90055-8. pmid: 9871429
[156]	Medina PJ, Adams VR. PD-1 Pathway Inhibitors: Immuno-Oncology Agents for Restoring Antitumor Immune Responses. Pharmacotherapy, 2016, 36(3): 317-334. doi:10.1002/phar.1714.
[157]	艾司唑仑片药品说明书. 批准文号: H32020699. 2020-07-22.
[158]	Gashaw I, Kirchheiner J, Goldammer M, et al. Cytochrome P450 3A4 messenger ribonucleic acid induction by rifampin in human peripheral blood mononuclear cells: correlation with alprazolam pharmacokinetics. Clin Pharmacol Ther, 2003, 74(5): 448-457. doi:10.1016/S0009-9236(03)00237-6. pmid: 14586385
[159]	奥沙西泮片药品说明书. 批准文号: H11020894. 2025-03-26.
[160]	Villikka K, Kivistö KT, Lamberg TS, et al. Concentrations and effects of zopiclone are greatly reduced by rifampicin. Br J Clin Pharmacol, 1997, 43(5): 471-474. doi:10.1046/j.1365-2125.1997.00579.x.
[161]	Villikka K, Kivistö KT, Luurila H, et al. Rifampin reduces plasma concentrations and effects of zolpidem. Clin Pharmacol Ther, 1997, 62(6): 629-634. doi:10.1016/S0009-9236(97)90082-5. pmid: 9433391
[162]	Lamberg TS, Kivistö KT, Neuvonen PJ. Concentrations and effects of buspirone are considerably reduced by rifampicin. Br J Clin Pharmacol, 1998, 45(4): 381-385. doi:10.1046/j.1365-2125.1998.t01-1-00698.x.
[163]	Kivistö KT, Lamberg TS, Neuvonen PJ. Interactions of buspirone with itraconazole and rifampicin: effects on the pharmacokinetics of the active 1-(2-pyrimidinyl)-piperazine metabolite of buspirone. Pharmacol Toxicol, 1999, 84(2): 94-97. doi:10.1111/j.1600-0773.1999.tb00880.x.
[164]	Mahatthanatrakul W, Nontaput T, Ridtitid W, et al. Rifampin, a cytochrome P 450 3A inducer, decreases plasma concentrations of antipsychotic risperidone in healthy volunteers. J Clin Pharm Ther, 2007, 32(2): 161-167. doi:10.1111/j.1365-2710.2007.00811.x.
[165]	Ryom L, Cotter A, De Miguel R, et al. 2019 update of the European AIDS Clinical Society Guidelines for treatment of people living with HIV version 10.0. HIV Med, 2020, 21(10): 617-624. doi:10.1111/hiv.12878.
[166]	The University of Liverpool. HIV drug interactions[EB/OL]. [2025-05-20]. https://www.hiv-druginteractions.org/.
[167]	US Food and Drug Administration. VIIV Hlthcare: Tivicay Prescribing Information[DB/OL]. [2025-09-12]. https://www.accessdata.fda.gov/drugsatfda_docs/label/2024/204790s031,213983s004lbl.pdf.
[168]	多替拉韦钠片(特威凯)说明书. 批准文号: HJ20150683. 2020-12-03.
[169]	Chen JH, Lin YC, Chen CP, et al. Drug monitoring was conducted for rifapentine among people with HIV receiving dolutegravir containing antiretroviral therapy and latent tuberculosis treatment. J Microbiol Immunol Infect, 2025, 58(2): 276-279. doi:10.1016/j.jmii.2024.11.002.
[170]	Podany AT, Cramer Y, Imperial M, et al. Twice-Daily Dolutegravir-Based Antiretroviral Therapy With 1 Month of Daily Rifapentine and Isoniazid for Tuberculosis Prevention. Clin Infect Dis, 2024, 79(4): 983-989. doi:10.1093/cid/ciae183.
[171]	拉替拉韦钾片(艾生特)药品说明书. 批准文号: HJ20171172. 2024-01-08.
[172]	Weiner M, Egelund EF, Engle M, et al. Pharmacokinetic interaction of rifapentine and raltegravir in healthy volunteers. J Antimicrob Chemother, 2014, 69(4): 1079-1085. doi:10.1093/jac/dkt483. pmid: 24343893
[173]	比克恩丙诺片(必妥维)药品说明书. 批准文号: H20190047. 2020-01-20.
[174]	拉米夫定片(贺普丁)药品说明书. 批准文号: H20030581. 2020-03-05.
[175]	硫酸阿巴卡韦片(赛进)药品说明书. 批准文号: H20150352. 2017-03-10.
[176]	多拉韦林片(沛卓)药品说明书. 批准文号: HJ20200050. 2023-10-23.
[177]	利匹韦林片(恩林)药品说明书. 批准文号: HJ20171075. 2022-04-29.
[178]	依非韦伦片(施多宁)药品说明书. 批准文号: H20130135. 2013-03-29.
[179]	Podany AT, Bao Y, Swindells S, et al. Efavirenz Pharmacokinetics and Pharmacodynamics in HIV-Infected Persons Receiving Rifapentine and Isoniazid for Tuberculosis Prevention. Clin Infect Dis, 2015, 61(8): 1322-1327. doi:10.1093/cid/civ464. pmid: 26082504
[180]	达芦那韦考比司他片(普泽力)药品说明书. 批准文号: HJ20180030. 2023-06-14.
[181]	Brooks KM, Pau AK, Swaim D, et al. Pharmacokinetics, Safety, and Tolerability of Once-Daily Darunavir With Cobicistat and Weekly Isoniazid/Rifapentine. J Acquir Immune Defic Syndr, 2023, 94(5): 468-473. doi:10.1097/QAI.0000000000003301. pmid: 37955446
[182]	Droste JA, Verweij-van Wissen CP, Kearney BP, et al. Pharmacokinetic study of tenofovir disoproxil fumarate combined with rifampin in healthy volunteers. Antimicrob Agents Chemother, 2005, 49(2): 680-684. doi:10.1128/AAC.49.2.680-684.2005.
[183]	Cerrone M, Alfarisi O, Neary M, et al. Rifampicin effect on intracellular and plasma pharmacokinetics of tenofovir alafenamide. J Antimicrob Chemother, 2019, 74(6): 1670-1678. doi:10.1093/jac/dkz068. pmid: 30815689
[184]	富马酸丙酚替诺福韦片药品说明书. 批准文号: H20180060. 2020-07-22.
[185]	恩替卡韦片(博路定)药品说明书. 批准文号: H20052237. 2025-02-19.
[186]	Kirby BJ, Symonds WT, Kearney BP, et al. Pharmacokinetic, Pharmacodynamic, and Drug-Interaction Profile of the Hepatitis C Virus NS5B Polymerase Inhibitor Sofosbuvir. Clin Pharmacokinet, 2015, 54(7): 677-690. doi:10.1007/s40262-015-0261-7. pmid: 25822283
[187]	索磷布韦片(索华迪)药品说明书. 批准文号: H20170365. 2020-07-01.
[188]	German P, Mathias A, Brainard DM, et al. Drug-Drug Interaction Profile of the Fixed-Dose Combination Tablet Regimen Ledipasvir/Sofosbuvir. Clin Pharmacokinet, 2018, 57(11): 1369-1383. doi:10.1007/s40262-018-0654-5. pmid: 29644537
[189]	盐酸可洛派韦胶囊药品说明书. 批准文号: H20200001. 2024-11-26.
[190]	盐酸拉维达韦片药品说明书. 批准文号: H20200008. 2025-03-25.
[191]	达诺瑞韦钠片(戈诺卫)药品说明书. 批准文号: H20180008. 2023-01-18.
[192]	磷酸依米他韦胶囊说明书. 批准文号: H20200015. 2020-12-21.
[193]	Nolan SR, Self TH, Norwood JM. Interaction between rifampin and levothyroxine. South Med J, 1999, 92(5): 529-531. doi:10.1097/00007611-199905000-00018. pmid: 10342905
[194]	Hamada Y, Sato A, Motojima S. Pulmonary Tuberculosis and Tuberculous Pleurisy Complicated with Rifampicin-Induced Hypothyroidism: A Case Report. Kekkaku, 2017, 92(1): 41-45.
[195]	秋水仙碱片药品说明书. 批准文号: H20113208. 2020-12-30.
[196]	非布司他片药品说明书. 批准文号:HJ20180051. 2023-07-03.
[197]	Parashar A, Gade SK, Potnuru M, et al. The curious case of benzbromarone: insight into super-inhibition of cytochrome P450. PLoS One, 2014, 9(3): e89967. doi:10.1371/journal.pone.0089967.
[198]	Lin Y, Gu X, Liu J, et al. Effects of different doses glimepiride intake on the pharmacokinetics of benzbromarone in rats. Pak J Pharm Sci, 2023, 36(1): 191-197. pmid: 36967511

证据级别	具体描述	研究类型	表达字母
高级证据	非常有信心;真实效应接近评估的结果	随机对照试验;质量升高二级的观察性研究	A
中级证据	对效应估计有中等信心;真实效应可能接近评估的结果,但也可能存在差异	质量降低一级的随机对照试验;质量升高一级的观察性研究	B
低级证据	对效应的评估确信度较低;真实效应可能与评估的结果不同,进一步研究可能对现有评估产生重要影响	质量降低二级的随机对照试验;观察性研究	C
极低证据	对效应的估计几乎没有信心;真实效应可能与评估结果大不相同	病例系列和病例报告;基于机制的药理作用推测	D

推荐强度	具体描述	表达数字
支持使用某项干预措施的强推荐	评价者确信干预措施利大于弊	1
支持使用某项干预措施的弱推荐	利弊不确定或无论高低质量的证据均显示利弊相当	2

代谢特征	利福平	利福喷丁	利福布汀
成人常用量	10~20mg/kg,1次/d, 不超过600mg	600mg,一周1~2次, 体质量<55kg者酌情减量	0.15~0.3g,1次/d
口服生物利用度(%)	68	未知	20
达峰时间(h)	1.5~2.0	5~6	2.5~4.0
峰浓度(mg/L)	8~20	8~30	0.2~0.6
食物的影响	AUC降低6%, 峰浓度降低36%	AUC升高40%~50%, 峰浓度升高44%	AUC、峰浓度不变, 达峰时间增加
抑酸剂的影响	无影响	未知	无影响
主要代谢途径	去乙酰化、水解	去乙酰化、水解	羟基化、去乙酰化
血清半衰期(h)	2~5	14~18	32~67
对细胞色素P450酶的诱导作用	显著	中等	弱
自身诱导作用	有	有	有
给予细胞色素P450酶抑制剂时AUC的变化	无影响	无影响	升高293%

药物	利福平	利福喷丁	利福布汀	推荐意见	证据等级
华法林	华法林AUC降低15%~74%	-	-	与利福平避免合用,与利福喷丁、利福布汀合用时监测国际标准化比值,增加华法林的剂量	1A
利伐沙班	利伐沙班AUC降低49%	-	-	与利福平避免合用。在有条件进行利伐沙班血药浓度检测时,考虑增加利伐沙班的剂量。与利福喷丁、利福布汀谨慎合用	1B
艾多沙班	艾多沙班AUC降低34%	-	-	与利福平避免合用。在有条件进行艾多沙班血药浓度检测时,建议考虑增加艾多沙班的剂量。与利福喷丁、利福布汀谨慎合用	2C
达比加群酯	达比加群AUC降低67%;C_max降低65%~70%	-	达比加群 AUC降低 20%	与利福平避免合用,与利福布汀谨慎合用。在可以选择利福布汀时,避免使用利福喷丁	1C

药物	利福平	利福喷丁	利福布汀	推荐意见	证据等级
泼尼松龙	泼尼松龙AUC降低50%~66%	-	泼尼松龙 AUC降低 33%	增加糖皮质激素的剂量。合用利福平时,糖皮质激素剂量增加50%;合用利福布汀时,糖皮质激素剂量增加33%	2B
环孢素	环孢素血药浓度降低	环孢素暴露降低	-	与利福平、利福喷丁避免合用,与利福布汀谨慎合用,无论使用何种利福霉素,都需监测环孢素的血药浓度,调整剂量	1B
他克莫司	他克莫司血药浓度降低约80%	-	他克莫司血药浓度降低	与利福平避免合用,与利福喷丁、利福布汀谨慎合用,无论使用何种利福霉素,都需密切监测他克莫司谷浓度,根据血药浓度增加他克莫司剂量,都需密切监测移植物功能	1B
西罗莫司	西罗莫司AUC降低82%	-	-	与利福平、利福喷丁避免合用,与利福布汀谨慎合用	1B
依维莫司	谷浓度/剂量比例降低87%~97%	-	-	与利福平、利福喷丁、利福布汀避免合用。确有必要合用时,根据血药浓度增加依维莫司的剂量	1C
吗替麦考酚酯、麦考酚钠	吗替麦考酚酯活性代谢产物霉酚酸AUC降低70%	-	-	与利福平避免合用,与利福喷丁、利福布汀谨慎合用,无论使用何种利福霉素,都需监测暴露水平,调整剂量	1B