| 词条 | Gatifloxacin |
| 释义 |
| Watchedfields = changed | verifiedrevid = 461119081 | IUPAC_name = 1-Cyclopropyl-6-fluoro-8-methoxy-7-(3-methylpiperazin-1-yl)-4-oxo-quinoline-3-carboxylic acid | image = Gatifloxacin.svg | image2 = Gatifloxacin ball-and-stick.png | tradename = Gatiflo, Tequin, Zymar, others | Drugs.com = {{drugs.com|monograph|gatifloxacin}} | MedlinePlus = a605012 | pregnancy_category = | legal_status = Rx only | routes_of_administration = Oral (discontinued), Intravenous (discontinued) ophthalmic | bioavailability = | protein_bound = 20% | metabolism = | elimination_half-life = 7 to 14 hours | CAS_number_Ref = {{cascite|correct|??}} | CAS_number = 112811-59-3 | ATC_prefix = J01 | ATC_suffix = MA16 | ATC_supplemental = {{ATC|S01|AE06}} | PubChem = 5379 | DrugBank_Ref = {{drugbankcite|correct|drugbank}} | DrugBank = DB01044 | ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}} | ChemSpiderID = 5186 | UNII_Ref = {{fdacite|correct|FDA}} | UNII = 81485Y3A9A | KEGG_Ref = {{keggcite|correct|kegg}} | KEGG = D08011 | ChEBI_Ref = {{ebicite|correct|EBI}} | ChEBI = 5280 | ChEMBL_Ref = {{ebicite|correct|EBI}} | ChEMBL = 31 | NIAID_ChemDB = 044913 | C=19 | H=22 | F=1 | N=3 | O=4 | SMILES = Fc1c(c(OC)c2c(c1)C(=O)C(\\C(=O)O)=C/N2C3CC3)N4CC(NCC4)C | StdInChI_Ref = {{stdinchicite|correct|chemspider}} | StdInChI = 1S/C19H22FN3O4/c1-10-8-22(6-5-21-10)16-14(20)7-12-15(18(16)27-2)23(11-3-4-11)9-13(17(12)24)19(25)26/h7,9-11,21H,3-6,8H2,1-2H3,(H,25,26) | StdInChIKey_Ref = {{stdinchicite|correct|chemspider}} | StdInChIKey = XUBOMFCQGDBHNK-UHFFFAOYSA-N }} Gatifloxacin (brand names Gatiflo, Tequin, and Zymar) is an antibiotic of the fourth-generation fluoroquinolone family,[1] that like other members of that family, inhibits the bacterial enzymes DNA gyrase and topoisomerase IV. It was patented in 1986 and approved for medical use in 1999.[2] Side effectsA Canadian study published in the New England Journal of Medicine in March 2006 claimed that Tequin can have significant side effects including dysglycemia.[3] An editorial by Jerry Gurwitz in the same issue called for the Food and Drug Administration (FDA) to consider giving Tequin a black box warning.[4] This editorial followed distribution of a letter dated February 15 by Bristol-Myers Squibb to health care providers indicating action taken with the FDA to strengthen warnings for the medication.[5] Subsequently, Bristol-Myers Squibb reported it would stop manufacture of Tequin, end sales of the drug after existing stockpiles were exhausted, and return all rights to Kyorin.[6] By contrast, ophthalmic gatifloxacin is generally well tolerated. The observed systemic concentration of the drug following oral administration of 400 mg gatifloxacin is approximately 800 times higher than that of the 0.5% gatifloxacin eye drop. Given as an eye drop, gatifloxacin has very low systemic exposure. Therefore, the systemic exposures resulting from the gatifloxacin ophthalmic solution are not likely to pose any risk for systemic toxicities.{{citation needed|date=March 2017}} ContraindicationsHypersensitivity[7]{{not in source|date=May 2018}} Society and cultureAvailabilityGatifloxacin is currently available in the US and Canada only as an ophthalmic solution. In 2011, the Union Health and Family Welfare Ministry of India banned the manufacture, sale, and distribution of gatifloxacin because of its adverse side effects.[8] In China, gatifloxacin is sold in tablet as well as in eye drop formulations. Brand namesBristol-Myers Squibb introduced gatifloxacin in 1999 under the proprietary name Tequin for the treatment of respiratory tract infections, having licensed the medication from Kyorin Pharmaceutical Company of Japan. Allergan produces it in eye-drop formulation under the names Zymar and Zymaxid. In many countries, gatifloxacin is also available as tablets and in various aqueous solutions for intravenous therapy. References1. ^{{cite journal |vauthors=Burka JM, Bower KS, Vanroekel RC, Stutzman RD, Kuzmowych CP, Howard RS |title=The effect of fourth-generation fluoroquinolones gatifloxacin and moxifloxacin on epithelial healing following photorefractive keratectomy |journal=Am. J. Ophthalmol. |volume=140 |issue=1 |pages=83–7 |date=July 2005 |pmid=15953577 |doi=10.1016/j.ajo.2005.02.037 |url=http://linkinghub.elsevier.com/retrieve/pii/S0002-9394(05)00260-6}} {{QuinoloneAntiBiotics}}2. ^{{cite book |last1=Fischer |first1=Jnos |last2=Ganellin |first2=C. Robin |title=Analogue-based Drug Discovery |date=2006 |publisher=John Wiley & Sons |isbn=9783527607495 |page=501 |url=https://books.google.ca/books?id=FjKfqkaKkAAC&pg=PA501 |language=en}} 3. ^{{cite journal| last = Park-Wyllie| first = Laura Y.| authorlink = | author2=David N. Juurlink |author3=Alexander Kopp |author4=Baiju R. Shah |author5=Thérèse A. Stukel|author5-link=Thérèse Stukel |author6=Carmine Stumpo |author7=Linda Dresser |author8=Donald E. Low |author9=Muhammad M. Mamdani| date=March 2006| title = Outpatient Gatifloxacin Therapy and Dysglycemia in Older Adults| journal = The New England Journal of Medicine| volume = 354| issue = 13| pages = 1352–1361| pmid = 16510739| url = http://content.nejm.org/cgi/content/abstract/354/13/1352| accessdate = 2006-05-01| doi = 10.1056/NEJMoa055191}} Note: publication date 30 March; available on-line 1 March 4. ^{{cite journal| last = Gurwitz| first = Jerry H.| date=March 2006| title = Serious Adverse Drug Effects — Seeing the Trees through the Forest| journal = The New England Journal of Medicine| volume = 354| issue = 13| pages = 1413–1415| pmid = 16510740| url = http://content.nejm.org/cgi/content/extract/354/13/1413| accessdate = 2006-05-01| doi = 10.1056/NEJMe068051}} 5. ^{{cite web| last = Lewis-Hall| first = Freda| date = February 15, 2006| url = http://www.fda.gov/medwatch/safety/2006/tequin_DHCP.pdf| title = Dear Healthcare Provider:| format = PDF| publisher = Bristol-Myers Squibb| accessdate = May 1, 2006}} 6. ^{{cite news |first = Randolph E. |last = Schmid |url = http://www.sfgate.com/cgi-bin/article.cgi?file=/news/archive/2006/05/01/national/w120748D88.DTL&type=health |title = Drug Company Taking Tequin Off Market |publisher = Associated Press |date = May 1, 2006 |accessdate = 2006-05-01 |archiveurl = https://web.archive.org/web/20071125104959/http://www.sfgate.com/cgi-bin/article.cgi?file=%2Fnews%2Farchive%2F2006%2F05%2F01%2Fnational%2Fw120748D88.DTL&type=health |archivedate = November 25, 2007 |deadurl = yes |df = }} 7. ^{{cite web| url = http://www.medpagetoday.com/PrimaryCare/PreventiveCare/3212| title = Bristol-Myers Squibb Hangs No Sale Sign on Tequin| accessdate = 24 February 2009| author = Peggy Peck| date = 2 May 2006| publisher = Med Page Today}} 8. ^{{cite news| url=http://www.thehindu.com/news/national/article1551233.ece | location=Chennai, India | work=The Hindu | title=Two drugs banned | date=19 March 2011}} 6 : Fluoroquinolone antibiotics|Withdrawn drugs|Piperazines|Phenol ethers|Cyclopropanes|Anti-tuberculosis drugs |
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