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Gatifloxacin

Gatifloxacin

Systematic (IUPAC) name
1-cyclopropyl-6-fluoro- 8-methoxy-7-(3-methylpiperazin-1-yl)- 4-oxo-quinoline-3-carboxylic acid
Identifiers
CAS number	112811-59-3
ATC code	J01MA16 S01AX21
PubChem	CID 5379
DrugBank	APRD00996
ChemSpider	5186
UNII	81485Y3A9A
KEGG	D08011
ChEMBL	CHEMBL31
Chemical data
Formula	C19H22FN3O4
Mol. mass	375.394 g/mol
SMILES	eMolecules & PubChem
Pharmacokinetic data
Protein binding	20%
Half-life	7 to 14 hours
Therapeutic considerations
Pregnancy cat.	?
Legal status	Rx only
Routes	Oral (discontinued), Intravenous (discontinued) ophthalmic
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Gatifloxacin sold under the brand names Gatiflo, Tequin and Zymar, is an antibiotic of the fourth-generation fluoroquinolone family, 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 of Japan. Allergan produces an eye-drop formulation called Zymar. 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 "life threatening" side effects including serious diabetes. 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. 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. 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.

Other serious side effects reported with gatifloxacin include hallucinations, liver damage and purpura. Union Health and Family Welfare Ministry of India on 18 march 2011 banned the manufacture, sale and distribution of Gatifloxacin as it they caused certain adverse side effects

Contraindications

Diabetes

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.

Gatifloxacin was banned in India on the 18th of March along with Tegaserod. A statement from the health ministry said: 'The use of the following drugs is likely to involve certain risks to human beings, whereas safer alternatives to the said drugs are available.' The move comes after international studies revealed that Gatifloxacin posed 17 times higher risk of developing serious hyperglycemia (high blood sugar) than other antibiotics in elderly patients.

gatifloxacin The Ministry of Health and Family Welfare, Govt of India in the Gazette notification dated on 16th March 2011, has prohibited the manufacture, sale and distribution of two drugs; Gatifloxacin for systemic use and Tegaserod. The prohibitory order on Gatifloxacin is applicable only for its systemic use as mentioned in the Gazette notification and does not apply to any topical formulations of Gatifloxacin.

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

Retrieved from : http://en.wikipedia.org/wiki/Gatifloxacin