Gatifloxacin (EENT) (Monograph)

Brand name: Zymar
Drug class: Antibacterials
VA class: OP210
Chemical name: (±-1-Cyclopropyl-6-fluoro-1,4-dihydro-8-methoxy-7-(3-methyl-1-piperazinyl)-4-oxo-3-quinoline- carboxylic acid sesquihydrate
Molecular formula: C₁₉H₂₂FN₃O₄
CAS number: 112811-59-3

Medically reviewed by Drugs.com on May 12, 2023. Written by ASHP.

Introduction

Antibacterial; 8-methoxy fluoroquinolone.^{1 2 4 5 20}

Uses for Gatifloxacin (EENT)

Bacterial Ophthalmic Infections

Topical treatment of bacterial conjunctivitis caused by susceptible Staphylococcus aureus, S. epidermidis, Streptococcus mitis group, S. oralis, S. pneumoniae, or Haemophilus influenzae.^{1 2 3}

Many cases of mild, acute bacterial conjunctivitis resolve spontaneously without anti-infective therapy.^{6 17 18 19} Although topical ophthalmic anti-infectives may shorten time to resolution and reduce severity and risk of complications,^{6 8 17 18 19} avoid indiscriminate use of topical anti-infectives.^{6 17}

Treatment of acute bacterial conjunctivitis generally is empiric;^{6 17 18} use of a broad-spectrum topical ophthalmic antibacterial usually recommended.^{6 17 18} In vitro staining and/or cultures of conjunctival material may be indicated in diagnosis and management of recurrent, severe, or chronic purulent conjunctivitis or when acute conjunctivitis does not respond to initial empiric topical treatment.^{6 17 18}

Gatifloxacin (EENT) Dosage and Administration

Administration

Ophthalmic Administration

Apply 0.5% ophthalmic solution topically to the eye.^{1 2}

For topical ophthalmic use only;^{1 2} do not inject directly into anterior chamber of the eye.^{1 2} (See Administration Precautions under Cautions.)

Avoid contaminating applicator tip with material from eye, fingers, or other source.^{1 2}

Dosage

Pediatric Patients

Bacterial Ophthalmic Infections

Conjunctivitis

Ophthalmic

Children ≥1 year of age: Instill 1 drop of 0.5% solution in the affected eye(s) every 2 hours while awake (up to 8 times daily) on day 1, then 1 drop 2–4 times daily while awake on days 2 through 7.^{1 2}

Adults

Bacterial Ophthalmic Infections

Conjunctivitis

Ophthalmic

Instill 1 drop of 0.5% solution in the affected eye(s) every 2 hours while awake (up to 8 times daily) on day 1, then 1 drop 2–4 times daily while awake on days 2 through 7.^{1 2}

Cautions for Gatifloxacin (EENT)

Contraindications

• Hypersensitivity to gatifloxacin, other quinolones, or any ingredient in the formulation.¹

Warnings/Precautions

Sensitivity Reactions

Hypersensitivity

Hypersensitivity reactions, including anaphylactic reactions, angioedema (e.g., pharyngeal, laryngeal, or facial edema), dyspnea, urticaria, and itching, reported in patients receiving gatifloxacin ophthalmic solution.¹ Stevens-Johnson syndrome reported rarely.¹

Hypersensitivity reactions have occurred following a single dose.¹

Immediately discontinue at first sign of rash or hypersensitivity reaction.¹

Administration Precautions

For topical ophthalmic use only.^{1 2}

Corneal endothelial cell injury may occur if gatifloxacin ophthalmic solution is introduced directly into anterior chamber of the eye.¹

Superinfection

Prolonged use may result in overgrowth of nonsusceptible organisms, including fungi.^{1 2}

If superinfection occurs, discontinue gatifloxacin ophthalmic solution and institute appropriate therapy.^{1 2}

Patient Monitoring

Whenever clinical judgment dictates, examine patient with the aid of magnification (e.g., slit lamp biomicroscopy) and, if appropriate, fluorescein staining.^{1 2}

Contact Lenses

Do not wear contact lenses during treatment with gatifloxacin ophthalmic solution or if any signs or symptoms of bacterial conjunctivitis are present.²

Specific Populations

Pregnancy

Data not available regarding use of gatifloxacin 0.5% ophthalmic solution in pregnant women.^{1 2}

Lactation

Distributed into milk in rats after oral administration;^{1 2} not known whether distributed into human milk following topical application to the eye.^{1 2}

Consider benefits of breast-feeding and importance of the drug to the woman;¹ also consider potential adverse effects on the breast-fed child from the drug or underlying maternal condition.¹

Pediatric Use

Safety and efficacy not established in children <1 year of age.^{1 2}

Geriatric Use

No overall differences in safety and efficacy relative to younger adults.^{1 2}

Common Adverse Effects

Worsening of conjunctivitis, eye irritation, dysgeusia, eye pain.^{1 2}

No formal drug interaction studies using gatifloxacin 0.5% ophthalmic solution.²

Gatifloxacin (EENT) Pharmacokinetics

Absorption

Bioavailability

Serum concentrations of gatifloxacin were undetectable (<5 ng/mL) after topical application to one eye of gatifloxacin 0.5% ophthalmic solution in an escalated dosage regimen (2 drops initially, then 2 drops 4 times daily for 7 days, and then 2 drops 8 times daily for 3 days).^{1 2}

Stability

Storage

Ophthalmic

Solution

15–25°C (may be exposed to 15–30°C).^{1 2} Protect from freezing.^{1 2}

Contains benzalkonium chloride as a preservative.^{1 2}

Actions and Spectrum

• Fluoroquinolone anti-infective.^{1 2 4 5 20}

• Like other fluoroquinolones, inhibits DNA synthesis in susceptible bacteria via inhibition of type II DNA topoisomerases (DNA gyrase, topoisomerase IV).^{1 2 4 6 9 20}

• Spectrum of activity includes gram-positive aerobic bacteria and some gram-negative aerobic bacteria.¹

• Active in vitro and in vivo in conjunctival infections against Staphylococcus aureus, S. epidermidis, S. mitis group, S. oralis, Streptococcus pneumoniae, and Haemophilus influenzae.^{1 2}

• Cross-resistance between gatifloxacin and some other fluoroquinolones reported.^{1 2}

Advice to Patients

• Advise patients to avoid contaminating applicator tip with material from the eye, fingers, or other source.^{1 2}

• Advise patients not to wear contact lenses during treatment with gatifloxacin ophthalmic solution or if any signs or symptoms of bacterial conjunctivitis are present.²

• Advise patients to immediately discontinue gatifloxacin ophthalmic solution and contact a clinician at first sign of rash or hypersensitivity reaction.¹

• Importance of informing clinicians of existing or contemplated therapy, including prescription and OTC drugs, as well as other concomitant illnesses.^{1 2}

• Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.^{1 2}

• Importance of informing patients of other important precautionary information.^{1 2} (See Cautions.)

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name

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