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Gatifloxacin

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. More

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Description

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.

Generic Name

Gatifloxacin

Chemical names

Gatifloxacin; Tequin; Zymar; Gatiflo

Brand names

Adgat, Algat, Amgat, Avigat, C-Gat, Dasikon, Diragyl, Ecogat, Ecogat BCD, Engatt, Engatt-DX, Floxigat, Floxigat M, Flurogat, G –Cebran, Gabact, Gabee, Gabir DPS, Gaity, Garnid, Gate Eye DPS, Gate-DX DPS, Gateme, Gatiaid-F, Gatiba, Gatiblu, Gatiblu-D, Gaticin, Gaticin Conc. INJ, Gaticin DPS, Gatifect, Gatiflo, Gatigo, Gatigram, Gatigram Oz, Gatik, Gatikind DPS, Gatilab, Gatilink, Gatilox, Gatilox DPS, Gatilox-DM, Gatimore, Gatin, Gatiquin, Gatiquin DPS, Gatiquin OINT, Gatiquin-OZ, Gatiquin-P, Gatispan

IUPAC name

1-cyclopropyl-6-fluoro-8-methoxy-7-(3-methylpiperazin-1-yl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid

Pharmacokinetics

Oral absorption.

Actions

Gatifloxacin is a synthetic broad-spectrum 8-methoxyfluoroquinolone antibacterial agent active against both Gram-positive and Gram-negative bacteria for oral or intravenous administration. It is bactericidal and its mode of action depends on blocking of bacterial DNA replication by binding itself to an enzyme called DNA gyrase, which allows the untwisting required replicating one DNA double helix into two. 

Dosage/Dosage form

400 mg once daily.

Therapeutic uses

For the treatment of bronchitis, sinusitis, community-acquired pneumonia, and skin infections (abscesses, wounds) caused by S. pneumoniae, H. influenzae, S. aureus, M. pneumoniae, C. pneumoniae, L. pneumophila, S. pyogenes

Adverse effects/Side effects

Rapid heartbeat, mental confusion, hallucinations, agitation, nightmares, depression; photophobia; tendon rupture; headache, dizziness, insomnia, chills, fever; back pain, abdominal pain; constipation, nausea, vomiting, diarrhoea, inflammation of the tongue, mouth sores; abnormal vision, ringing in the ears, vaginitis.

Interaction

  • Increased risk of adverse CV reactions when used with class IA or III antiarrhythmics e.g. disopyramide and amiodarone.
  • Antacids, ferrous salts, bismuth subsalicylate, sucralfate and zinc salts reduce bioavailability of gatifloxacin.
  • NSAIDs may increase the risk of CNS stimulation and convulsions. May increase digoxin plasma levels.
  • Probenecid, cimetidine and loop diuretics increase gatifloxacin levels.
  •  Concurrent use of erythromycin, bepridil, phenothiazines, cisapride, pentamidine, or TCAs may prolong QT interval.
  • Concurrent corticosteroid therapy may increase the risk of tendon rupture.
  •  Increased risk of hypoglycaemia when used with oral antidiabetic agents.
  • May enhance hypoprothrombinaemic effects of oral anticoagulants.

Contraindications

Hypersensitivity; children <18 years; concurrent use of class IA or III antiarrhythmics, QT-prolongation drugs; diabetics; pregnancy, lactation.

Storage

Store at 25°C.

Information

Molecular weight

375.3941

Molecular formula

C19H22FN3O4

CAS number

112811-59-3

Precautions

Elderly. Uncorrected hypokalaemia; renal and hepatic impairment. Known or suspected CNS disorders, May prolong QT interval