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Gatifloxacin


Pronunciation

 (gat i FLOKS a sin)


U.S. Brand Names

 Tequin®; Zymar™


Generic Available

 No


Canadian Brand Names

 Tequin®


Use

Oral, I.V.: Treatment of the following infections when caused by susceptible bacteria: Acute bacterial exacerbation of chronic bronchitis; acute sinusitis; community-acquired pneumonia including pneumonia caused by multidrug-resistant S. pneumoniae (MDRSP); uncomplicated skin and skin structure infection; uncomplicated urinary tract infections (cystitis); complicated urinary tract infections; pyelonephritis; uncomplicated urethral and cervical gonorrhea; acute, uncomplicated rectal infections in women

Ophthalmic: Bacterial conjunctivitis


Pregnancy Risk Factor

 C


Pregnancy Implications

 Reports of arthropathy (observed in immature animals and reported rarely in humans) have limited the use of fluoroquinolones during pregnancy. Gatifloxacin has been show to be fetotoxic in animal studies. There are no adequate and well-controlled studies in pregnant women. Based on limited data, quinolones are not expected to be a major human teratogen. Although quinolone antibiotics should not be used as first-line agents during pregnancy, when considering treatment for life-threatening infection and/or prolonged duration of therapy, the potential risk to the fetus must be balanced against the severity of the potential illness.


Lactation

 Excretion in breast milk unknown/use caution


Contraindications

 Hypersensitivity to gatifloxacin, other quinolone antibiotics, or any component of the formulation


Warnings/Precautions

 Use with caution in patients with significant bradycardia or acute myocardial ischemia. May prolong QT interval (concentration related). Use caution in patients with known prolongation of QT interval, uncorrected hypokalemia, or concurrent administration of other medications known to prolong the QT interval (including Class Ia and Class III antiarrhythmics, cisapride, erythromycin, antipsychotics, and tricyclic antidepressants). May cause increased CNS stimulation, increased intracranial pressure, convulsions, or psychosis. Use with caution in individuals at risk of seizures (CNS disorders or concurrent therapy with medications which may lower seizure threshold). Discontinue in patients who experience significant CNS adverse effects (dizziness, hallucinations, suicidal ideation or actions). Use caution in renal dysfunction (dosage adjustment required) and in severe hepatic insufficiency (no data available). Serious disruptions in glucose regulation (including hyperglycemia and severe hypoglycemia) may occur, generally in patients with diabetes and typically within 1-3 days of initiation. Monitor closely and discontinue if hyper- or hypoglycemia occur. Tendon inflammation and/or rupture has been reported with this and other quinolone antibiotics. Risk may be increased with concurrent corticosteroids, particularly in the elderly. Discontinue at first signs or symptoms of tendon or pain.

Severe hypersensitivity reactions, including anaphylaxis, have occurred with quinolone therapy. If an allergic reaction occurs (itching, urticaria, dyspnea, facial edema, loss of consciousness, tingling, cardiovascular collapse) discontinue drug immediately. Prolonged use may result in superinfection; pseudomembranous colitis may occur and should be considered in all patients who present with diarrhea. Quinolones may exacerbate myasthenia gravis, use with caution (rare, potentially life-threatening weakness of respiratory muscles may occur). May cause peripheral neuropathy (rare); discontinue if symptoms of sensory or sensorimotor neuropathy occur.

Safety and efficacy for ophthalmic use have not been established in children <1 year of age. Safety and efficacy for systemic use have not been established in patients <18 years of age.


Adverse Reactions

Systemic therapy:

3% to 10%:

Central nervous system: Headache (3%), dizziness (3%)

Gastrointestinal: Nausea (8%), diarrhea (4%)

Genitourinary: Vaginitis (6%)

Local: Injection site reactions (5%)

0.1% to 3%: Abdominal pain, abnormal dreams, abnormal vision, agitation, alkaline phosphatase increased, allergic reaction, anorexia, anxiety, arthralgia, back pain, chest pain, chills, confusion, constipation, diaphoresis, dry skin, dyspepsia, dyspnea, dysuria, facial edema, fever, flatulence, gastritis, glossitis, hematuria, hyperglycemia, hypertension, insomnia, leg cramps, mouth ulceration, nervousness, oral candidiasis, palpitation, paresthesia, peripheral edema, pharyngitis, pruritus, rash, serum amylase increased, serum bilirubin increased, serum transaminases increased, somnolence, stomatitis, taste perversion, thirst, tinnitus, tremor, weakness, vasodilation, vertigo, vomiting

<0.1%: Abnormal thinking, arthritis, asthenia, ataxia, bone pain, bradycardia, breast pain, bronchospasm, cheilitis, colitis, cyanosis, depersonalization, depression, diabetes mellitus, dysphagia, ear pain, ecchymosis, edema, epistaxis, ethanol intolerance, euphoria, eye pain, gastrointestinal hemorrhage, gingivitis, halitosis, hallucination, hematemesis, hematuria, hostility, hyperesthesia, hypertonia, hyperventilation, hypoglycemia, lymphadenopathy, maculopapular rash, metrorrhagia, migraine, myalgia, myasthenia, neck pain, panic attacks, paranoia, parosmia, photophobia, pseudomembranous colitis, psychosis, ptosis, rectal hemorrhage, seizure, stress, tachycardia, taste disturbance, tongue edema, vesiculobullous rash

Postmarketing and/or case reports: Acute renal failure, anaphylactic reaction, angioneurotic edema, hepatitis, INR increased, prothrombin time increased, severe hyper-/hypoglycemia, nonketotic hyperglycemia, pancreatitis, peripheral neuropathy, Stevens-Johnson syndrome, syncope, tendon rupture, thrombocytopenia, torsade de pointes

Ophthalmic therapy:

5% to 10%: Ocular: Conjunctival irritation, keratitis, lacrimation increased, papillary conjunctivitis

1% to 4%:

Central nervous system: Headache

Gastrointestinal: Taste disturbance

Ocular: Chemosis, conjunctival hemorrhage, discharge, dry eye, edema, irritation, pain, visual acuity decreased


Overdosage/Toxicology

 Potential symptoms of overdose may include CNS excitation, seizures, QT prolongation, and arrhythmias (including torsade de pointes). Patients should be monitored by continuous ECG in the event of an overdose. Management is supportive and symptomatic. Not removed by dialysis.


Drug Interactions

Corticosteroids: Concurrent use may increase the risk of tendon rupture, particularly in elderly patients (overall incidence rare).

Hypoglycemic agents: Gatifloxacin may alter glucose control in patients receiving hypoglycemic agents with or without insulin. Cases of severe disturbances (including symptomatic hypoglycemia) have been reported, typically within 1-3 days of gatifloxacin initiation.

Metal cations (aluminum, calcium, iron, magnesium, and zinc) bind quinolones in the gastrointestinal tract and inhibit absorption. Concurrent administration of most antacids (not calcium carbonate), oral electrolyte supplements, quinapril, sucralfate, and some didanosine formulations (chewable/buffered tablets and pediatric powder for oral suspension) should be avoided. Gatifloxacin should be administered 4 hours before these agents.

Probenecid: May decrease renal secretion of quinolones.

QTc-prolonging agents: Effects may be additive with gatifloxacin. Use caution with Class Ia and Class III antiarrhythmics, erythromycin, cisapride, antipsychotics, and cyclic antidepressants.

Warfarin: The hypoprothrombinemic effect of warfarin may be enhanced by some quinolone antibiotics; monitor INR.


Ethanol/Nutrition/Herb Interactions

 Herb/Nutraceutical: Avoid dong quai, St John's wort (may also cause photosensitization).


Stability

Ophthalmic solution: Store between 15°C to 25°C (59°F to 77°F). Do not freeze.

Powder for oral suspension: Prior to reconstitution, store at 25°C (77°F); do not freeze. Reconstitute with appropriate amount of water as specified on bottle. Shake vigorously until suspended. Following reconstitution, store under refrigeration at 2°C to 8°C (36°F to 46°F); do not freeze. Discard any unused portion after 14 days.

Solution for injection: Store at 25°C (77°F). Do not freeze. Single-use vials must be diluted to a concentration of 2 mg/mL prior to administration; do not dilute with SWFI (a hypertonic solution results). Following dilution, stable for 14 days.

Tablet: Store at 25°C (77°F).


Compatibility

Y-site administration: Compatible: Acyclovir, alfentanil, amikacin, aminophylline, ampicillin, ampicillin/sulbactam, aztreonam, bretylium, buprenorphine, butorphanol, calcium chloride, calcium gluconate, carboplatin, cefazolin, cefotetan, ceftazidime, ceftizoxime, ceftriaxone, chlorpromazine, cimetidine, cisatracurium, cisplatin, clindamycin, cyclophosphamide, cyclosporine, cytarabine, dexamethasone sodium phosphate, digoxin, diphenhydramine, dobutamine, dopamine, doxorubicin, droperidol, enalaprilat, esmolol, etoposide, famotidine, fentanyl, fluconazole, fluorouracil, ganciclovir, gemcitabine, gentamicin, granisetron, haloperidol, hydrocortisone sodium succinate, hydromorphone, hydroxyzine, ifosfamide, imipenem/cilastatin, labetalol, leucovorin, lidocaine, lorazepam, magnesium sulfate, mannitol, meperidine, mesna, methotrexate, methylprednisolone sodium succinate, metoclopramide, metronidazole, midazolam, mitoxantrone, morphine, nalbuphine, naloxone, nicardipine, nitroglycerin, ondansetron, paclitaxel, pentamidine, pentobarbital, phenobarbital, potassium chloride, prochlorperazine edisylate, promethazine, propranolol, ranitidine, remifentanil, sodium bicarbonate, sodium phosphates, sufentanil, theophylline, ticarcillin, ticarcillin/clavulanate potassium, tobramycin, trimethoprim/sulfamethoxazole, vecuronium, verapamil, vinblastine, vincristine, vinorelbine, zidovudine. Incompatible: Amphotericin B, amphotericin B cholesteryl sulfate complex, cefoperazone, cefoxitin, diazepam, furosemide, heparin, phenytoin, piperacillin, piperacillin/tazobactam, potassium phosphates, vancomycin


Mechanism of Action

 Gatifloxacin is a DNA gyrase inhibitor, and also inhibits topoisomerase IV. DNA gyrase (topoisomerase II) is an essential bacterial enzyme that maintains the superhelical structure of DNA. DNA gyrase is required for DNA replication and transcription, DNA repair, recombination, and transposition; inhibition is bactericidal.


Pharmacodynamics/Kinetics

Absorption: Oral: Well absorbed; Ophthalmic: Not measurable

Distribution: Vd: 1.5-2.0 L/kg; concentrates in alveolar macrophages and lung parenchyma

Protein binding: 20%

Metabolism: Only 1%; no interaction with CYP

Bioavailability: 96%

Half-life elimination: 7.1-13.9 hours; ESRD/CAPD: 30-40 hours

Time to peak: Oral: 1 hour

Excretion: Urine (70% as unchanged drug, <1% as metabolites); feces (5%)


Dosage

Children 1 year and Adults: Ophthalmic: Bacterial conjunctivitis:

Days 1 and 2: Instill 1 drop into affected eye(s) every 2 hours while awake (maximum: 8 times/day)

Days 3-7: Instill 1 drop into affected eye(s) up to 4 times/day while awake

Adults: Oral, I.V.:

Acute bacterial exacerbation of chronic bronchitis: 400 mg every 24 hours for 5 days

Acute sinusitis: 400 mg every 24 hours for 10 days

Community-acquired pneumonia: 400 mg every 24 hours for 7-14 days

Uncomplicated skin/skin structure infections: 400 mg every 24 hours for 7-10 days

Uncomplicated urinary tract infections (cystitis): 400 mg single dose or 200 mg every 24 hours for 3 days

Complicated urinary tract infections: 400 mg every 24 hours for 7-10 days

Acute pyelonephritis: 400 mg every 24 hours for 7-10 days

Uncomplicated urethral gonorrhea in men, cervical or rectal gonorrhea in women: 400 mg single dose

Elderly: No dosage adjustment is required based on age, however, assessment of renal function is particularly important in this population.

Dosage adjustment in renal impairment: Creatinine clearance <40 mL/minute (or patients on hemodialysis/CAPD) should receive an initial dose of 400 mg, followed by a subsequent dose of 200 mg every 24 hours. Patients receiving single-dose or 3-day therapy for appropriate indications do not require dosage adjustment. Administer after hemodialysis.

Dosage adjustment in hepatic impairment: No dosage adjustment is required in mild-moderate hepatic disease. No data are available in severe hepatic impairment (Child-Pugh Class C).


Administration

Oral: May be administered with or without food, milk, or calcium supplements. Gatifloxacin should be taken 4 hours before supplements (including multivitamins) containing iron, zinc, or magnesium. Suspension may be administered through a gastric feeding tube.

I.V.: For I.V. infusion only. Concentrated injection (10 mg/mL) must be diluted to 2 mg/mL prior to administration. No further dilution is required for premixed 100 mL and 200 mL solutions. Infuse over 60 minutes. Avoid rapid or bolus infusions.


Monitoring Parameters

 WBC, signs of infection


Dietary Considerations

 May take tablets with or without food, milk, or calcium supplements. Gatifloxacin should be taken 4 hours before supplements (including multivitamins) containing iron, zinc, or magnesium. Oral suspension contains phenylalanine 168 mg/5 mL.


Patient Education

 Inform prescriber of all prescriptions, OTC medications, or herbal products you are taking, and any allergies you have. Do not take any new medication during therapy without consulting prescriber. Pregnancy/breast-feeding precautions: Inform prescriber if you are or intend to be pregnant. Do not breast-feed while taking this medication.

I.V.: Report any redness, pain, itching, burning, or signs of irritation at infusion site; swelling of mouth, lips, or tongue, back pain, tendon pain; dizziness, abnormal thinking, or anxiety

Ophthalmic: Tilt head back and instill drops in affected eye at often as directed for length of time prescribed. Do not allow touch dropper to any surface, including the eyes or hands. Apply light pressure to the inside corner of the eye (near the nose) after each drop. Do not wear contact lenses if being treated for a bacterial eye infection. May cause some temporary stinging, burning, itching, redness or tearing; eyelid swelling or itching, or a bad taste in you mouth after instillation. Report persistent pain, burning, swelling, or visual disturbances.

Oral: Take exactly as directed with or without food. Avoid alcohol. Take 4 hours before antacids or mineral supplements (iron, magnesium, or zinc). Do not miss a dose (take a missed dose as soon as possible unless it is almost time for next dose). Take entire prescription even if feeling better. Maintain adequate hydration (2-3 L/day of fluids, unless instructed to restrict fluids). May cause nausea, vomiting, taste perversion (small, frequent meals, good mouth care, chewing gum, or sucking hard candy may help); headache, dizziness, insomnia, anxiety (use caution when driving or engaging in tasks requiring alertness until response is known). Report immediately any CNS changes (dizziness, insomnia, hallucinations, suicidal ideation or actions); rash or itching; respiratory difficulty or swallowing; tendon pain; swelling of mouth, lips, tongue, or throat; chest pain or tightness; or back pain. Report changes in voiding pattern, vaginal itching, burning, or discharge; vision changes or hearing; abnormal bruising or bleeding or blood in urine; or other adverse reactions.


Anesthesia and Critical Care Concerns/Other Considerations

 Gatifloxacin causes a dose-dependent QT prolongation. Coadministration of gatifloxacin with other drugs that also prolong the QT interval or induce bradycardia (eg, beta-blockers, amiodarone) should be done cautiously. Careful consideration should be given in the use of gatifloxacin in patients with cardiovascular disease, particularly in those with conduction abnormalities.


Cardiovascular Considerations

 Gatifloxacin causes a dose-dependent QT prolongation. Coadministration of gatifloxacin with other drugs that also prolong the QT interval or induce bradycardia (eg, beta-blockers, amiodarone) should be avoided. Careful consideration should be given in the use of gatifloxacin in patients with cardiovascular disease, particularly in those with conduction abnormalities.


Dental Health: Effects on Dental Treatment

 Key adverse event(s) related to dental treatment: Taste disturbance.


Dental Health: Vasoconstrictor/Local Anesthetic Precautions

 No information available to require special precautions


Mental Health: Effects on Mental Status

 Gatifloxacin may cause dizziness, insomnia; may rarely produce abnormal thinking, agitation, anorexia, anxiety, asthenia, ataxia, confusion, depersonalization, depression, euphoria, hallucination, hostility, nervousness, panic attacks, paranoia, psychosis, somnolence, or stress


Mental Health: Effects on Psychiatric Treatment

 May have potential to prolong QT interval; should avoid in patients with uncorrected hypokalemia, or concurrent administration of other medications known to prolong the QT interval (antipsychotics, tricyclic antidepressants, ziprasidone)


Dosage Forms

Injection, infusion [premixed in D5W] (Tequin®): 200 mg (100 mL); 400 mg (200 mL)

Injection, solution [preservative free] (Tequin®): 10 mg/mL (40 mL)

Powder for oral suspension (Tequin®): 200 mg/5 mL (25 mL, 50 mL, 75 mL, 100 mL) [contains phenylalanine 168 mg/5 mL; fruit flavor]

Solution, ophthalmic (Zymar™): 0.3% (5 mL) [contains benzalkonium chloride]

Tablet (Tequin®): 200 mg, 400 mg


References

Blondeau JM, "Expanded Activity and Utility of the New Fluoroquinolones: A Review," Clinical Therapeutics , 1999, 21(1):3-40.

"Gatifloxacin and Moxifloxacin: Two New Fluoroquinolones," The Medical Letter , 2000, Vol 42, 1072:15.

Perry CM, Barman Balfour JA, Lamb HM, "Gatifloxacin," Drugs , 1999, 58(4):683-96.


International Brand Names

 Bonoq® (DE); Gatiflo® (JP); Tequin® (AR, BR, CA, ID, NZ, SG, TH, ZA); Zyquin® (IN)


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