硝唑尼特

硝唑尼特
临床资料
商品名（英语：Drug nomenclature）	Alinia, Nizonide, others
AHFS/Drugs.com	Monograph
MedlinePlus	a603017
核准状况	美 DailyMed: Nitazoxanide;
给药途径	By mouth
药物类别（英语：Drug class）	Antiprotozoal; Broad-spectrum antiparasitic; Broad-spectrum antiviral
ATC码	P01AX11 (WHO) ;
法律规范状态
法律规范	美：处方药（℞-only）;
药物动力学数据
血浆蛋白结合率	Nitazoxanide: ?; Tizoxanide: over 99%
药物代谢	Rapidly hydrolyzed to tizoxanide
代谢产物	tizoxanide; tizoxanide glucuronide
生物半衰期	3.5 hours
排泄途径	Kidney, bile duct, and fecal
识别信息
	IUPAC命名法 [2-[(5-Nitro-1,3-thiazol-2-yl)carbamoyl]phenyl]ethanoate; ;
CAS号	55981-09-4
PubChem CID	41684;
DrugBank	DB00507 ;
ChemSpider	38037 ;
UNII	SOA12P041N;
KEGG	D02486 ;
ChEMBL	ChEMBL1401 ;
NIAID ChemDB	057131;
CompTox Dashboard（英语：CompTox Chemicals Dashboard） (EPA)	DTXSID5033757 ;
ECHA InfoCard	100.054.465
化学信息
化学式	C12H9N3O5S
摩尔质量	307.28 g·mol−1
3D模型（JSmol（英语：JSmol））	交互式图像;
	SMILES O=C(Nc1ncc(s1)[N+]([O-])=O)c2ccccc2OC(=O)C;
	InChI InChI=1S/C12H9N3O5S/c1-7(16)20-9-5-3-2-4-8(9)11(17)14-12-13-6-10(21-12)15(18)19/h2-6H,1H3,(H,13,14,17) ; Key:YQNQNVDNTFHQSW-UHFFFAOYSA-N ;

硝唑尼特是一种抗寄生虫药和抗病毒药，用于治疗由寄生虫、原生动物、小隐孢子虫、兰氏贾第鞭毛虫、芽囊原虫属^[4]^[5]、溶组织内阿米巴^[6]、蛔虫^[7]和病毒引起的感染。 ^[8]^[9]^[10] 它还能治疗流行性感冒^[1]^[10]以及慢性乙型肝炎^[11]。

参考文献

^ ^1.0 ^1.1 ^1.2 ^1.3 ^1.4 ^1.5 ^1.6 Alinia- nitazoxanide tablet Alinia- nitazoxanide powder, for suspension. DailyMed. [13 February 2021]. （原始内容存档于2021-03-20）.
^ ^2.0 ^2.1 ^2.2 Stockis A, Allemon AM, De Bruyn S, Gengler C. Nitazoxanide pharmacokinetics and tolerability in man using single ascending oral doses. International Journal of Clinical Pharmacology and Therapeutics. May 2002, 40 (5): 213–220. PMID 12051573. doi:10.5414/cpp40213.
^ Nitazoxanide. PubChem. National Center for Biotechnology Information, U.S. National Library of Medicine. [3 January 2016]. （原始内容存档于2016-03-06）.
^ Blastocystis: Resources for Health Professionals. United States Centers for Disease Control and Prevention. 2017-05-02 [4 January 2016]. （原始内容存档于2015-11-08）.
^ Roberts T, Stark D, Harkness J, Ellis J. Update on the pathogenic potential and treatment options for Blastocystis sp. Gut Pathogens. May 2014, 6: 17 [2023-11-18]. PMC 4039988  . PMID 24883113. doi:10.1186/1757-4749-6-17  . （原始内容存档于2022-11-11）. Blastocystis is one of the most common intestinal protists of humans. ... A recent study showed that 100% of people from low socio-economic villages in Senegal were infected with Blastocystis sp. suggesting that transmission was increased due to poor hygiene sanitation, close contact with domestic animals and livestock, and water supply directly from well and river [10]. ...
^ Muñoz P, Valerio M, Eworo A, Bouza E. Parasitic infections in solid-organ transplant recipients. Current Opinion in Organ Transplantation. December 2011, 16 (6): 565–575. PMID 22027588. S2CID 23861504. doi:10.1097/MOT.0b013e32834cdbb0. Nitazoxanide: intestinal amoebiasis: 500 mg po bid x 3 days
^ Hagel I, Giusti T. Ascaris lumbricoides: an overview of therapeutic targets. Infectious Disorders Drug Targets. October 2010, 10 (5): 349–367. PMID 20701574. S2CID 15403331. doi:10.2174/187152610793180876. new anthelmintic alternatives such as tribendimidine and Nitazoxanide have proved to be safe and effective against A. lumbricoides and other soil-transmitted helminthiases in human trials.
^ Di Santo N, Ehrisman J. Research perspective: potential role of nitazoxanide in ovarian cancer treatment. Old drug, new purpose?. Cancers. September 2013, 5 (3): 1163–1176. PMC 3795384  . PMID 24202339. doi:10.3390/cancers5031163  . Nitazoxanide [NTZ: 2-acetyloxy-N-(5-nitro-2-thiazolyl)benzamide] is a thiazolide antiparasitic agent with excellent activity against a wide variety of protozoa and helminths. ... Nitazoxanide (NTZ) is a main compound of a class of broad-spectrum anti-parasitic compounds named thiazolides. It is composed of a nitrothiazole-ring and a salicylic acid moiety which are linked together by an amide bond ... NTZ is generally well tolerated, and no significant adverse events have been noted in human trials [13]. ... In vitro, NTZ and tizoxanide function against a wide range of organisms, including the protozoal species Blastocystis hominis, C. parvum, Entamoeba histolytica, G. lamblia and Trichomonas vaginalis [13]
^ White CA. Nitazoxanide: a new broad spectrum antiparasitic agent. Expert Review of Anti-Infective Therapy. February 2004, 2 (1): 43–49. PMID 15482170. S2CID 219184877. doi:10.1586/14787210.2.1.43.
^ ^10.0 ^10.1 Rossignol JF. Nitazoxanide: a first-in-class broad-spectrum antiviral agent. Antiviral Research. October 2014, 110: 94–103. PMC 7113776  . PMID 25108173. doi:10.1016/j.antiviral.2014.07.014  . Originally developed and commercialized as an antiprotozoal agent, nitazoxanide was later identified as a first-in-class broad-spectrum antiviral drug and has been repurposed for the treatment of influenza. ... From a chemical perspective, nitazoxanide is the scaffold for a new class of drugs called thiazolides. These small-molecule drugs target host-regulated processes involved in viral replication. ... A new dosage formulation of nitazoxanide is presently undergoing global Phase 3 clinical development for the treatment of influenza. Nitazoxanide inhibits a broad range of influenza A and B viruses including influenza A(pH1N1) and the avian A(H7N9) as well as viruses that are resistant to neuraminidase inhibitors. ... Nitazoxanide also inhibits the replication of a broad range of other RNA and DNA viruses including respiratory syncytial virus, parainfluenza, coronavirus, rotavirus, norovirus, hepatitis B, hepatitis C, dengue, yellow fever, Japanese encephalitis virus and human immunodeficiency virus in cell culture assays. Clinical trials have indicated a potential role for thiazolides in treating rotavirus and norovirus gastroenteritis and chronic hepatitis B and chronic hepatitis C. Ongoing and future clinical development is focused on viral respiratory infections, viral gastroenteritis and emerging infections such as dengue fever.
^ Teran CG, Teran-Escalera CN, Villarroel P. Nitazoxanide vs. probiotics for the treatment of acute rotavirus diarrhea in children: a randomized, single-blind, controlled trial in Bolivian children. International Journal of Infectious Diseases. July 2009, 13 (4): 518–523. PMID 19070525. doi:10.1016/j.ijid.2008.09.014  .

[Alinia_FDA_label-1] 1.0 ^1.1 ^1.2 ^1.3 ^1.4 ^1.5 ^1.6 Alinia- nitazoxanide tablet Alinia- nitazoxanide powder, for suspension. DailyMed. [13 February 2021]. （原始内容存档于2021-03-20）.

[Primary:_Kinetics_and_OD-2] 2.0 ^2.1 ^2.2 Stockis A, Allemon AM, De Bruyn S, Gengler C. Nitazoxanide pharmacokinetics and tolerability in man using single ascending oral doses. International Journal of Clinical Pharmacology and Therapeutics. May 2002, 40 (5): 213–220. PMID 12051573. doi:10.5414/cpp40213.

[PubChem-3] Nitazoxanide. PubChem. National Center for Biotechnology Information, U.S. National Library of Medicine. [3 January 2016]. （原始内容存档于2016-03-06）.

[CDC_blastocystosis-4] Blastocystis: Resources for Health Professionals. United States Centers for Disease Control and Prevention. 2017-05-02 [4 January 2016]. （原始内容存档于2015-11-08）.

[Efficacy_against_Blastocystis-5] Roberts T, Stark D, Harkness J, Ellis J. Update on the pathogenic potential and treatment options for Blastocystis sp. Gut Pathogens. May 2014, 6: 17 [2023-11-18]. PMC 4039988  . PMID 24883113. doi:10.1186/1757-4749-6-17  . （原始内容存档于2022-11-11）. Blastocystis is one of the most common intestinal protists of humans. ... A recent study showed that 100% of people from low socio-economic villages in Senegal were infected with Blastocystis sp. suggesting that transmission was increased due to poor hygiene sanitation, close contact with domestic animals and livestock, and water supply directly from well and river [10]. ...

[Entamoeba-6] Muñoz P, Valerio M, Eworo A, Bouza E. Parasitic infections in solid-organ transplant recipients. Current Opinion in Organ Transplantation. December 2011, 16 (6): 565–575. PMID 22027588. S2CID 23861504. doi:10.1097/MOT.0b013e32834cdbb0. Nitazoxanide: intestinal amoebiasis: 500 mg po bid x 3 days

[A._lumbricoides-7] Hagel I, Giusti T. Ascaris lumbricoides: an overview of therapeutic targets. Infectious Disorders Drug Targets. October 2010, 10 (5): 349–367. PMID 20701574. S2CID 15403331. doi:10.2174/187152610793180876. new anthelmintic alternatives such as tribendimidine and Nitazoxanide have proved to be safe and effective against A. lumbricoides and other soil-transmitted helminthiases in human trials.

[Thiazolides-8] Di Santo N, Ehrisman J. Research perspective: potential role of nitazoxanide in ovarian cancer treatment. Old drug, new purpose?. Cancers. September 2013, 5 (3): 1163–1176. PMC 3795384  . PMID 24202339. doi:10.3390/cancers5031163  . Nitazoxanide [NTZ: 2-acetyloxy-N-(5-nitro-2-thiazolyl)benzamide] is a thiazolide antiparasitic agent with excellent activity against a wide variety of protozoa and helminths. ... Nitazoxanide (NTZ) is a main compound of a class of broad-spectrum anti-parasitic compounds named thiazolides. It is composed of a nitrothiazole-ring and a salicylic acid moiety which are linked together by an amide bond ... NTZ is generally well tolerated, and no significant adverse events have been noted in human trials [13]. ... In vitro, NTZ and tizoxanide function against a wide range of organisms, including the protozoal species Blastocystis hominis, C. parvum, Entamoeba histolytica, G. lamblia and Trichomonas vaginalis [13]

[Nitazoxanide:_Broad-spectrum_antiparasitic-9] White CA. Nitazoxanide: a new broad spectrum antiparasitic agent. Expert Review of Anti-Infective Therapy. February 2004, 2 (1): 43–49. PMID 15482170. S2CID 219184877. doi:10.1586/14787210.2.1.43.

[Broad-spectrum_antiviral_review-10] 10.0 ^10.1 Rossignol JF. Nitazoxanide: a first-in-class broad-spectrum antiviral agent. Antiviral Research. October 2014, 110: 94–103. PMC 7113776  . PMID 25108173. doi:10.1016/j.antiviral.2014.07.014  . Originally developed and commercialized as an antiprotozoal agent, nitazoxanide was later identified as a first-in-class broad-spectrum antiviral drug and has been repurposed for the treatment of influenza. ... From a chemical perspective, nitazoxanide is the scaffold for a new class of drugs called thiazolides. These small-molecule drugs target host-regulated processes involved in viral replication. ... A new dosage formulation of nitazoxanide is presently undergoing global Phase 3 clinical development for the treatment of influenza. Nitazoxanide inhibits a broad range of influenza A and B viruses including influenza A(pH1N1) and the avian A(H7N9) as well as viruses that are resistant to neuraminidase inhibitors. ... Nitazoxanide also inhibits the replication of a broad range of other RNA and DNA viruses including respiratory syncytial virus, parainfluenza, coronavirus, rotavirus, norovirus, hepatitis B, hepatitis C, dengue, yellow fever, Japanese encephalitis virus and human immunodeficiency virus in cell culture assays. Clinical trials have indicated a potential role for thiazolides in treating rotavirus and norovirus gastroenteritis and chronic hepatitis B and chronic hepatitis C. Ongoing and future clinical development is focused on viral respiratory infections, viral gastroenteritis and emerging infections such as dengue fever.

[Infectious_Diseases_2009-11] Teran CG, Teran-Escalera CN, Villarroel P. Nitazoxanide vs. probiotics for the treatment of acute rotavirus diarrhea in children: a randomized, single-blind, controlled trial in Bolivian children. International Journal of Infectious Diseases. July 2009, 13 (4): 518–523. PMID 19070525. doi:10.1016/j.ijid.2008.09.014  .

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