利福昔明

Rifaximin
临床资料
商品名（英语：Drug nomenclature）	Xifaxan, Zaxine, Xifaxanta, Normix, others
AHFS/Drugs.com	Monograph
MedlinePlus	a604027
怀孕分级	澳: B1 ; ;
给药途径	口服
ATC码	A07AA11 (WHO) D06AX11, QG51AA06, QJ51XX01;
法律规范状态
法律规范	美：处方药（℞-only）; 处方药（℞-only）;
药物动力学数据
生物利用度	< 0.4%
药物代谢	肝脏
生物半衰期	6小时
排泄途径	粪便（97%）
识别信息
	IUPAC命名法 (2S,16Z,18E,20S,21S,22R,23R,24R,25S,26S,27S,28E)-5,6,21,23,25-pentahydroxy-27-methoxy-2,4,11,16,20,22,24,26-octamethyl-2,7-(epoxypentadeca-[1,11,13]trienimino)benzofuro; [4,5-e]pyrido[1,2-a]-benzimida-zole-1,15(2H)-dione,25-acetate; ;
CAS号	80621-81-4
PubChem CID	6436173;
DrugBank	DB01220 ;
ChemSpider	10482302 ;
UNII	L36O5T016N;
KEGG	D02554 ;
ChEBI	CHEBI:75246 ;
ChEMBL	ChEMBL1617 ;
CompTox Dashboard（英语：CompTox Chemicals Dashboard） (EPA)	DTXSID7045998 ;
ECHA InfoCard	100.111.624
化学信息
化学式	C43H51N3O11
摩尔质量	785.89 g·mol−1
3D模型（JSmol（英语：JSmol））	交互式图像;
熔点	200至205 °C（392至401 °F）（分解）
	SMILES CC(=O)O[C@H]3[C@H](C)[C@H](O)[C@H](C)[C@@H](O)[C@@H](C)\C=C\C=C(\C)C(=O)Nc6c2c(nc1cc(C)ccn12)c5c4C(=O)[C@@](C)(O/C=C/[C@H](OC)[C@H]3C)Oc4c(C)c(O)c5c6O;
	InChI InChI=1S/C43H51N3O11/c1-19-14-16-46-28(18-19)44-32-29-30-37(50)25(7)40-31(29)41(52)43(9,57-40)55-17-15-27(54-10)22(4)39(56-26(8)47)24(6)36(49)23(5)35(48)20(2)12-11-13-21(3)42(53)45-33(34(32)46)38(30)51/h11-18,20,22-24,27,35-36,39,48-51H,1-10H3,(H,45,53)/b12-11+,17-15+,21-13-/t20-,22+,23+,24+,27-,35-,36+,39+,43-/m0/s1 ; Key:NZCRJKRKKOLAOJ-XRCRFVBUSA-N ;

利福昔明（Rifaximin），商品名Xifaxan，是一种用于治疗旅行者腹泻，肠躁症和肝性脑病的抗生素。 ^[3] 由于利福昔明的口服吸收率相当低，只有0.4%会吸收到血流中^[4]，因此可以在肠道达到相当高的药物浓度。

医疗用途

肠躁症

利福昔明在美国核准用于治疗肠躁症。 ^[5] 它具有抗发炎和抗菌效果，且难被肠道吸收入身体循环，因而能在肠道发挥局部作用，有效缓解非便秘型肠躁症（IBS）的慢性功能症状。即使反复使用似乎仍能保持效果。 ^[6] ^[7] 利福昔明特别适用于怀疑肠躁症与小肠细菌过度生长有关的病人。

困难梭菌感染

利福昔明可能可以与万古霉素并用以治疗复发性困难梭菌感染。 ^[8] ^[9] 不过这些研究的证据等级不高。^[10]

肝性脑病

虽然缺乏良好证据，但利福昔明似乎与其他现有的肝性脑病治疗方法（如乳果糖）一样有效，耐受性更好，并且可能更快发生效果。它可减少肠道中产生氨的细菌，而能减轻肝性脑病的症状，降低了死亡率。 ^[11] 利福昔明的缺点是比较昂贵，且目前对于肝性脑病患者，缺乏未并用乳果糖治疗的临床试验。

特别注意

对于Child-Pugh评分为C级严重程度的肝硬化患者，必须谨慎使用。 ^[11]

副作用

由于本药由肠胃道吸收程度不高，全身性副作用不多，副作用一般而言轻微并不常见 ^[6] 除非存在诸如免疫抑制和住院等危险因素，否则艰难梭菌感染通常不是由利福昔明疗法引起的。利福昔明对艰难梭菌具有活性。

参考文献

^ Rifaximin international. Drugs.com. 2 November 2020 [11 November 2020]. （原始内容存档于2023-07-14）.
^ Xifaxan- rifaximin tablet. DailyMed. 1 October 2019 [11 November 2020]. （原始内容存档于2023-03-22）.
^ Rifaximin. The American Society of Health-System Pharmacists. [8 January 2017]. （原始内容存档于2020-03-01）.
^ Adachi, J. A., & DuPont, H. L. (2006). Rifaximin: a novel nonabsorbed rifamycin for gastrointestinal disorders. Clinical infectious diseases, 42(4), 541-547.
^ Rifaximin for the treatment of diarrhea-predominant irritable bowel syndrome. Expert Rev Gastroenterol Hepatol. 2016, 10 (4): 431–42. PMID 26753693. doi:10.1586/17474124.2016.1140571.
^ ^6.0 ^6.1 Rifaximin for the treatment of irritable bowel syndrome - a drug safety evaluation. Expert Opinion on Drug Safety. July 2016, 15 (7): 983–91. PMID 27149541. doi:10.1080/14740338.2016.1186639.
^ Clinical Practice Guidelines for Irritable Bowel Syndrome in Korea, 2017 Revised Edition. Journal of Neurogastroenterology and Motility. April 2018, 24 (2): 197–215. PMC 5885719  . PMID 29605976. doi:10.5056/jnm17145.
^ Interruption of recurrent Clostridium difficile-associated diarrhea episodes by serial therapy with vancomycin and rifaximin. Clinical Infectious Diseases. March 2007, 44 (6): 846–8. PMID 17304459. doi:10.1086/511870.
^ A randomized, double-blind, placebo-controlled pilot study to assess the ability of rifaximin to prevent recurrent diarrhoea in patients with Clostridium difficile infection. The Journal of Antimicrobial Chemotherapy. December 2011, 66 (12): 2850–5. PMID 21948965. doi:10.1093/jac/dkr377.
^ Antibiotic treatment for Clostridium difficile-associated diarrhoea in adults. The Cochrane Database of Systematic Reviews. March 2017, 3: CD004610. PMC 6464548  . PMID 28257555. doi:10.1002/14651858.CD004610.pub5.
^ ^11.0 ^11.1 Profile of rifaximin and its potential in the treatment of irritable bowel syndrome. Clin Exp Gastroenterol. 2015, 8: 159–67. PMC 4467648  . PMID 26089696. doi:10.2147/CEG.S67231.

[1] Rifaximin international. Drugs.com. 2 November 2020 [11 November 2020]. （原始内容存档于2023-07-14）.

[Xifaxan_FDA_label-2] Xifaxan- rifaximin tablet. DailyMed. 1 October 2019 [11 November 2020]. （原始内容存档于2023-03-22）.

[AHFS2017-3] Rifaximin. The American Society of Health-System Pharmacists. [8 January 2017]. （原始内容存档于2020-03-01）.

[4] Adachi, J. A., & DuPont, H. L. (2006). Rifaximin: a novel nonabsorbed rifamycin for gastrointestinal disorders. Clinical infectious diseases, 42(4), 541-547.

[pmid26753693-5] Rifaximin for the treatment of diarrhea-predominant irritable bowel syndrome. Expert Rev Gastroenterol Hepatol. 2016, 10 (4): 431–42. PMID 26753693. doi:10.1586/17474124.2016.1140571.

[pmid27149541-6] 6.0 ^6.1 Rifaximin for the treatment of irritable bowel syndrome - a drug safety evaluation. Expert Opinion on Drug Safety. July 2016, 15 (7): 983–91. PMID 27149541. doi:10.1080/14740338.2016.1186639.

[pmid29605976-7] Clinical Practice Guidelines for Irritable Bowel Syndrome in Korea, 2017 Revised Edition. Journal of Neurogastroenterology and Motility. April 2018, 24 (2): 197–215. PMC 5885719  . PMID 29605976. doi:10.5056/jnm17145.

[pmid17304459-8] Interruption of recurrent Clostridium difficile-associated diarrhea episodes by serial therapy with vancomycin and rifaximin. Clinical Infectious Diseases. March 2007, 44 (6): 846–8. PMID 17304459. doi:10.1086/511870.

[pmid21948965-9] A randomized, double-blind, placebo-controlled pilot study to assess the ability of rifaximin to prevent recurrent diarrhoea in patients with Clostridium difficile infection. The Journal of Antimicrobial Chemotherapy. December 2011, 66 (12): 2850–5. PMID 21948965. doi:10.1093/jac/dkr377.

[pmid28257555-10] Antibiotic treatment for Clostridium difficile-associated diarrhoea in adults. The Cochrane Database of Systematic Reviews. March 2017, 3: CD004610. PMC 6464548  . PMID 28257555. doi:10.1002/14651858.CD004610.pub5.

[pmid26089696-11] 11.0 ^11.1 Profile of rifaximin and its potential in the treatment of irritable bowel syndrome. Clin Exp Gastroenterol. 2015, 8: 159–67. PMC 4467648  . PMID 26089696. doi:10.2147/CEG.S67231.

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