Drug class: Antibacterials
VA class: OP210
Chemical name: (S)-9-Fluoro-2,3-dihydro-3-methyl-10-(4-methyl-1-piperazinyl)-7-oxo-hydrate-7H-pyrido[1,2,3-de]-1,4-benzoxazine-6-carboxylic acid
Molecular formula: C₁₈H₂₀FN₃O₄•½H₂O
CAS number: 138199-71-0

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

Introduction

Antibacterial; fluoroquinolone; levorotatory isomer of ofloxacin.

Uses for levoFLOXacin (EENT)

Bacterial Ophthalmic Infections

Topical treatment of bacterial conjunctivitis caused by susceptible Staphylococcus aureus, S. epidermidis, Streptococcus pneumoniae, groups C, F, and G streptococci, viridans streptococci, Corynebacterium, Acinetobacter lwoffii, Haemophilus influenzae, or Serratia marcescens.

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

Treatment of acute bacterial conjunctivitis generally is empiric; use of a broad-spectrum topical ophthalmic antibacterial usually recommended. 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.

levoFLOXacin (EENT) Dosage and Administration

Administration

Ophthalmic Administration

Apply 0.5% ophthalmic solution topically to the eye.

For topical ophthalmic use only.

Avoid contaminating applicator tip with material from eye, fingers, or other source.

Dosage

Pediatric Patients

Bacterial Ophthalmic Infections

Conjunctivitis

Ophthalmic

Children ≥6 years of age: Instill 1–2 drops of 0.5% solution in affected eye(s) every 2 hours while awake (up to 8 times daily) on days 1 and 2, then 1–2 drops every 4 hours while awake (up to 4 times daily) on days 3 through 7.

Adults

Bacterial Ophthalmic Infections

Conjunctivitis

Ophthalmic

Instill 1–2 drops of 0.5% solution in affected eye(s) every 2 hours while awake (up to 8 times daily) on days 1 and 2, then 1–2 drops every 4 hours while awake (up to 4 times daily) on days 3 through 7.

Cautions for levoFLOXacin (EENT)

Contraindications

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

Warnings/Precautions

Sensitivity Reactions

Hypersensitivity

Serious and occasionally fatal hypersensitivity and/or anaphylactic reactions reported with systemic fluoroquinolones, including systemic levofloxacin; these reactions may occur with first dose. Some hypersensitivity reactions reported with systemic fluoroquinolones have been accompanied by cardiovascular collapse, hypotension or shock, seizures, loss of consciousness, angioedema (e.g., laryngeal, pharyngeal, facial), airway obstruction, dyspnea, urticaria, and itching.

Immediately discontinue levofloxacin ophthalmic solution at first sign of rash or hypersensitivity reaction.

Superinfection

Prolonged use may result in overgrowth of nonsusceptible organisms, including fungi.

If superinfection occurs, discontinue levofloxacin ophthalmic solution and institute appropriate therapy.

Patient Monitoring

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

Contact Lenses

Do not wear contact lenses if any signs or symptoms of bacterial conjunctivitis are present.

Specific Populations

Pregnancy

Category C.

Data not available regarding use of levofloxacin 0.5% ophthalmic solution in pregnant women; use only if potential benefits to the woman justify potential risks to fetus.

Lactation

Since ofloxacin is distributed into human milk, levofloxacin (levorotatory isomer of ofloxacin) is presumed to be distributed into human milk.

Use with caution in nursing women.

Pediatric Use

Safety and efficacy not established in children <6 years of age.

Geriatric Use

No overall differences in safety and efficacy relative to younger adults.

Common Adverse Effects

Transient decrease in vision, transient ocular burning, ocular pain or discomfort, foreign body sensation, photophobia, headache, fever, pharyngitis.

Interactions for levoFLOXacin (EENT)

No formal drug interaction studies using levofloxacin 0.5% ophthalmic solution.

levoFLOXacin (EENT) Pharmacokinetics

Absorption

Bioavailability

Following topical application of levofloxacin 0.5% ophthalmic solution to the eye, the drug is absorbed systemically and low levofloxacin concentrations are attained in plasma.

In 15 healthy adults who received topical application of levofloxacin ophthalmic solution for 15 days, mean plasma concentrations of levofloxacin 1 hour after dosing was 0.86 ng/mL on day 1 and 2.05 ng/mL on day 15.

After topical application of levofloxacin 0.5% ophthalmic solution to the eye for 15 days, maximum mean plasma concentrations of the drug were >1000 times lower than those reported after usually recommended oral dosages of levofloxacin.

Stability

Storage

Ophthalmic

Solution

20–25°C.

Contains benzalkonium chloride as a preservative.

Actions and Spectrum

• Fluoroquinolone anti-infective.

• Like other fluoroquinolones, inhibits bacterial DNA synthesis in susceptible bacteria via inhibition of type II DNA topoisomerases (DNC gyrase, topoisomerase IV).

• May be bactericidal at concentrations equal to or slightly greater than inhibitory concentrations.

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

• Active in vitro and in vivo in conjunctival infections against Staphylococcus aureus, S. epidermidis, Streptococcus pneumoniae, groups C, F, and G streptococci, viridans streptococci, Corynebacterium, Acinetobacter lwoffii, Haemophilus influenzae, and Serratia marcescens.

• Cross-resistance can occur between levofloxacin and other fluoroquinolones, but some bacteria resistant to other fluoroquinolones may be susceptible to levofloxacin.

Advice to Patients

• Advise patients to avoid contaminating applicator tip with material from the eye, fingers, or other source.

• Advise patients not to wear contact lenses if any signs or symptoms of bacterial conjunctivitis are present.

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

• Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as any concomitant illnesses.

• Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.

• Importance of informing patients of other important precautionary information. (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.

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