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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2016/02/24 14:19:07」(JST)

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Gatifloxacin sold under the 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. Bristol-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.

Side-effects and removal from the market

A Canadian study published in the New England Journal of Medicine in March 2006 claims Tequin can have significant side effects including dysglycemia.^[2] An editorial by Dr. Jerry Gurwitz in the same issue called for the Food and Drug Administration (FDA) to consider giving Tequin a black box warning.^[3] 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.^[4] Subsequently it was reported on May 1, 2006 that Bristol-Myers Squibb would stop manufacture of Tequin, end sales of the drug after existing stockpiles were exhausted, and return all rights to Kyorin.^[5]

Union Health and Family Welfare Ministry of India on 18 March 2011 banned the manufacture, sale and distribution of Gatifloxacin as it caused certain adverse side effects^[6]

Contraindications

Diabetes^[7]

Availability

Gatifloxacin is currently available only in the US and Canada as an ophthalmic solution.

In China it is sold in tablet as well as in eye drop formulations.

Ophthalmic anti-infectives are generally well tolerated. The concentration of the drug observed following oral administration of 400 mg gatifloxacin systemically is approximately 800 times higher than that of the 0.5% Gatifloxacin eye drop. Given as an eye drop, Gatifloxacin Ophthalmic Solution 0.3% & 0.5% cause very low systemic exposures. Therefore, the systemic exposures resulting from the gatifloxacin ophthalmic solution are not likely to pose any risk for systemic toxicities.

References

^ Burka JM, Bower KS, Vanroekel RC, Stutzman RD, Kuzmowych CP, Howard RS (July 2005). "The effect of fourth-generation fluoroquinolones gatifloxacin and moxifloxacin on epithelial healing following photorefractive keratectomy". Am. J. Ophthalmol. 140 (1): 83–7. doi:10.1016/j.ajo.2005.02.037. PMID 15953577.
^ Park-Wyllie, Laura Y.; David N. Juurlink; Alexander Kopp; Baiju R. Shah; Therese A. Stukel; Carmine Stumpo; Linda Dresser; Donald E. Low; Muhammad M. Mamdani (March 2006). "Outpatient Gatifloxacin Therapy and Dysglycemia in Older Adults". The New England Journal of Medicine 354 (13): 1352–1361. doi:10.1056/NEJMoa055191. PMID 16510739. Retrieved 2006-05-01. Note: publication date 30 March; available on-line 1 March
^ Gurwitz, Jerry H. (March 2006). "Serious Adverse Drug Effects — Seeing the Trees through the Forest". The New England Journal of Medicine 354 (13): 1413–1415. doi:10.1056/NEJMe068051. PMID 16510740. Retrieved 2006-05-01.
^ Lewis-Hall, Freda (February 15, 2006). "Dear Healthcare Provider:" (PDF). Bristol-Myers Squibb. Retrieved May 1, 2006.
^ Schmid, Randolph E. (May 1, 2006). "Drug Company Taking Tequin Off Market". Associated Press. Archived from the original on November 25, 2007. Retrieved 2006-05-01. ^{[dead link]}
^ "Two drugs banned". The Hindu (Chennai, India). 19 March 2011.
^ Peggy Peck (2 May 2006). "Bristol-Myers Squibb Hangs No Sale Sign on Tequin". Med Page Today. Retrieved 24 February 2009.

UpToDate Contents

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1. フルオロキノロン系抗菌薬に対する過敏反応 hypersensitivity reactions to fluoroquinolones antimicrobials
2. フルオロキノロン類 fluoroquinolones
3. コンタクトレンズの合併症 complications of contact lenses
4. セレウス菌およびその他の非炭疽菌バシラス属 bacillus cereus and other non anthracis bacillus species
5. 成人における市中肺炎の治療に関する抗菌薬の研究 antibiotic studies for the treatment of community acquired pneumonia in adults

English Journal

Prevalence and antimicrobial resistance of Mycoplasmas and Chlamydiae in patients with genital tract infections in Shanghai, China.

He M1, Xie Y2, Zhang R2, Gao S1, Xu G1, Zhang L1, Liu P1, Li Y1, Wu S3.
Journal of infection and chemotherapy : official journal of the Japan Society of Chemotherapy.J Infect Chemother.2016 Jun 17. pii: S1341-321X(16)30081-2. doi: 10.1016/j.jiac.2016.05.007. [Epub ahead of print]
The infections of Mycoplasmas and Chlamydiae are still severe in patients with genital tract diseases and antimicrobial resistance for these organisms has been changing in recent years. In this study, we reported the prevalence status of Ureaplasma urealyticum, Mycoplasma hominis and Chlamydia trach
PMID 27324895

Gyrase Mutations in Pre-extensively and Extensively Drug-resistant Tuberculosis in Thai Clinical Isolates: Insights into the Role of gyrB Mutations in Quinolone Resistance.

Disratthakit A1, Prammananan T2, Tribuddharat C1, Thaipisuttikul I1, Doi N3, Leechawengwongs M4, Chaiprasert A5.
Antimicrobial agents and chemotherapy.Antimicrob Agents Chemother.2016 Jun 13. pii: AAC.00539-16. [Epub ahead of print]
DNA gyrase mutations are a major cause of quinolone resistance in Mycobacterium tuberculosis We therefore conducted the first comprehensive study to determine the diversity of gyrase mutations in pre-extensively (pre-XDR; n=71) and extensively drug-resistant (XDR; n=30) tuberculosis Thai clinical is
PMID 27297489

In Vitro Resistance Development to Nemonoxacin in Streptococcus pneumoniae: A Unique Profile for a Novel Nonfluorinated Quinolone.

Roychoudhury S1, Makin K1, Twinem T1, Leunk R1, Hsu MC2.
Microbial drug resistance (Larchmont, N.Y.).Microb Drug Resist.2016 Jun 7. [Epub ahead of print]
Selection of resistant strains in Streptococcus pneumoniae was studied in vitro with nemonoxacin, a novel nonfluorinated quinolone (NFQ), in comparison with quinolone benchmarks, ciprofloxacin, garenoxacin, and gatifloxacin. In stepwise resistance selection studies, a 256-fold loss of potency was ob
PMID 27267788

Japanese Journal

1.5%レボフロキサシン点眼液と0.3%ガチフロキサシン点眼液の白内障手術当日点眼における結膜囊減菌化試験

藤紀彦,近藤寛之,田原昭彦 [他]
あたらしい眼科 32(9), 1339-1343, 2015-09
NAID 40020609709

ガチフロ点眼液0.3%の細菌学的効果に関する特定使用成績調査

末信敏秀,川口えり子,星最智
あたらしい眼科 31(11), 1674-1682, 2014-11
NAID 40020281956

The Mechanisms of Insulin Secretion and Calcium Signaling in Pancreatic β-Cells Exposed to Fluoroquinolones

Bito Motoki,Tomita Takashi,Komori Mika [他],Taogoshi Takanori,Kimura Yasuhiro,Kihira Kenji
Biological and Pharmaceutical Bulletin 36(1), 31-35, 2013
… Even where the absence of supplemental extracellular Ca2+, insulin secretion and [Ca2+]c were increased by gatifloxacin, levofloxacin or tolbutamide. …
NAID 130003361342

Related Pictures

★リンクテーブル★

リンク元	「ガチフロキサシン」
拡張検索	「gatifloxacin hydrate」

「ガチフロキサシン」

Gatifloxacin
Systematic (IUPAC) name
	1-cyclopropyl-6-fluoro- 8-methoxy-7-(3-methylpiperazin-1-yl)- 4-oxo-quinoline-3-carboxylic acid
Clinical data
Trade names	Zymar
AHFS/Drugs.com	monograph
MedlinePlus	a605012
Legal status	℞ (Prescription only);
Routes of; administration	Oral (discontinued),; Intravenous (discontinued); ophthalmic
Pharmacokinetic data
Protein binding	20%
Biological half-life	7 to 14 hours
Identifiers
CAS Number	112811-59-3
ATC code	J01MA16 S01AE06
PubChem	CID 5379
DrugBank	DB01044
ChemSpider	5186
UNII	81485Y3A9A
KEGG	D08011
ChEBI	CHEBI:5280
ChEMBL	CHEMBL31
NIAID ChemDB	044913
Chemical data
Formula	C19H22FN3O4
Molar mass	375.394 g/mol
	SMILES Fc1c(c(OC)c2c(c1)C(=O)C(\C(=O)O)=C/N2C3CC3)N4CC(NCC4)C ;
	InChI InChI=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) ; Key:XUBOMFCQGDBHNK-UHFFFAOYSA-N ;
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