Levofloxacin is a fluoroquinolone anti-infective agent.1, 2, 20
Levofloxacin 0.5% ophthalmic solution is used for the 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 .1
Although many cases of mild, acute bacterial conjunctivitis resolve spontaneously without anti-infective therapy,6, 17, 18, 19 topical ophthalmic anti-infectives may shorten the time to resolution and reduce severity and risk of complications.6, 17, 18, 19 Treatment of acute bacterial conjunctivitis generally is empiric and use of a broad-spectrum topical ophthalmic antibacterial usually is recommended;6, 17, 18 however, indiscriminate use of topical anti-infectives should be avoided.6, 17 In vitro staining and/or cultures of conjunctival material may be indicated in the 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
Efficacy and safety of levofloxacin 0.5% ophthalmic solution for the topical treatment of bacterial conjunctivitis have been evaluated in several randomized, double-masked, vehicle- or active-controlled, multicenter trials.1, 9, 10, 11 In a study that included 117 pediatric and adult patients (range: 2-91 years of age) with a clinical diagnosis of bacterial conjunctivitis and positive conjunctival cultures, patients were randomized to receive a 5-day regimen of levofloxacin 0.5% ophthalmic solution or vehicle control.9 At the final evaluation (6-10 days after initiation of treatment), the clinical cure rate was 78% in patients treated with levofloxacin ophthalmic solution and 61% in those treated with vehicle control;9 the microbiologic eradication rate was 92 and 53%, respectively.9 In 2 studies comparing efficacy of levofloxacin 0.5% ophthalmic solution and ofloxacin 0.3% ophthalmic solution for the topical treatment of bacterial conjunctivitis in adults or pediatric patients, clinical cure rates were similar for the drugs, but the microbiologic eradication rate in those treated with levofloxacin ophthalmic solution was 87-89% compared with 62-80% in patients treated with ofloxacin ophthalmic solution.10, 11
For systemic uses of levofloxacin, see Levofloxacin 8:12.18.
Levofloxacin is applied topically to the eye as a 0.5% ophthalmic solution.1
Levofloxacin ophthalmic solution is for topical ophthalmic use only .1
Care should be taken to avoid contaminating the applicator tip with material from the eye, fingers, or other source.1
For the topical treatment of bacterial conjunctivitis in adults and children 6 years of age and older, 1-2 drops of levofloxacin 0.5% ophthalmic solution should be instilled in the affected eye(s) every 2 hours while awake (up to 8 times daily) on days 1 and 2, then 1-2 drops should be instilled every 4 hours while awake (up to 4 times daily) on days 3 through 7.1
Levofloxacin 0.5% ophthalmic solution is contraindicated in patients with known hypersensitivity to levofloxacin, other quinolones, or any component in the formulation.1
Serious and occasionally fatal hypersensitivity and/or anaphylactic reactions have been reported in patients receiving systemic fluoroquinolones, including systemic levofloxacin.1, 21 These reactions may occur with the first dose.1, 21 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.1, 21
Levofloxacin ophthalmic solution should be discontinued immediately at the first sign of rash or hypersensitivity reaction.1 Serious acute hypersensitivity reactions may require immediate emergency treatment;1 oxygen and airway management should be administered as clinically indicated.1
As with other anti-infectives, prolonged use of levofloxacin ophthalmic solution may result in overgrowth of nonsusceptible organisms, including fungi.1
If superinfection occurs, levofloxacin ophthalmic solution should be discontinued and appropriate therapy instituted.1
Whenever clinical judgment dictates, the patient should be examined with the aid of magnification (e.g., slit lamp biomicroscopy) and, if appropriate, fluorescein staining.1
Contact lenses should not be worn if any signs or symptoms of bacterial conjunctivitis are present.1
Category C.1 (See Users Guide.)
Data are not available regarding use of levofloxacin 0.5% ophthalmic solution in pregnant women, and the drug should be used during pregnancy only if potential benefits to the woman justify potential risks to the fetus.1
In animal studies using oral levofloxacin, reduced fetal weight and increased fetal mortality were reported.1
Since ofloxacin is distributed into human milk, levofloxacin (the levorotatory isomer of ofloxacin) is presumed to be distributed into human milk.1
Caution is advised if levofloxacin ophthalmic solution is used in nursing women.1
Safety and efficacy of levofloxacin 0.5% ophthalmic solution have not been established in children younger than 6 years of age.1
Although systemic quinolones have been associated with arthropathy in immature animals, there is no evidence that administration of levofloxacin ophthalmic solution has any effect on weight bearing joints.1
No overall differences in safety and efficacy of levofloxacin 0.5% ophthalmic solution have been observed between geriatric and younger adults.1
Adverse effects reported in 1-3% of patients treated with levofloxacin 0.5% ophthalmic solution include transient decrease in vision, transient ocular burning, ocular pain or discomfort, foreign body sensation, photophobia, headache, fever, and pharyngitis.1 Allergic reactions, lid edema, ocular dryness, and ocular itching occur in less than 1% of patients receiving levofloxacin 0.5% ophthalmic solution.1
No formal drug interaction studies have been performed using levofloxacin 0.5% ophthalmic solution.1
Levofloxacin is a fluoroquinolone anti-infective agent.1, 2, 20 Like other commercially available fluoroquinolones, levofloxacin contains a fluorine at the C-6 position of the quinolone nucleus.1, 2, 4 Levofloxacin is the levorotatory isomer of ofloxacin1, 3, 4 and is 8-128 times as active against susceptible gram-positive and gram-negative bacteria as the dextrorotatory isomer of ofloxacin and twice as active as racemic ofloxacin.3, 4
Levofloxacin may be bactericidal in action at concentrations equal to or slightly greater than inhibitory concentrations.1, 4 Like other fluoroquinolones, levofloxacin inhibits DNA synthesis in susceptible organisms via inhibition of type II DNA topoisomerases (DNA gyrase, topoisomerase IV).1, 16, 20
Levofloxacin is active in vitro and in vivo in conjunctival infections against some aerobic gram-positive bacteria, including Staphylococcus aureus , S. epidermidis , Streptococcus pneumoniae , groups C, F, and G streptococci, viridans streptococci, and Corynebacterium , and some aerobic gram-negative bacteria, including Acinetobacter lwoffii , Haemophilus influenzae , and Serratia marcescens .1
Cross-resistance can occur between levofloxacin and other fluoroquinolones,21 but some bacteria resistant to other fluoroquinolones may be susceptible to levofloxacin.21
For the topical treatment of conjunctivitis caused by susceptible bacteria, levofloxacin is commercially available as an aqueous ophthalmic solution containing 5 mg of levofloxacin per mL.1 Levofloxacin 0.5% ophthalmic solution is isotonic (osmolality of 300 mOsm/kg), has a pH of approximately 6.5, and contains benzalkonium chloride as a preservative.1
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.1 In a study in 15 healthy adults who received topical application of levofloxacin ophthalmic solution for 15 days, mean plasma concentrations of levofloxacin at 1 hour after dosing ranged from 0.86 ng/mL on day 1 to 2.05 ng/mL on day 15.1 Maximum mean plasma levofloxacin concentrations reported following topical application of 0.5% ophthalmic solution to the eye were more than 1000 times lower than plasma concentrations reported in patients receiving usually recommended dosages of oral levofloxacin.1
Patients should be advised to avoid contaminating the applicator tip with material from the eye, fingers, or other source.1
Patients should be advised not to wear contact lenses if any signs or symptoms of bacterial conjunctivitis are present.1
Advise patients to immediately discontinue levofloxacin ophthalmic solution and contact a clinician at the first sign of rash or hypersensitivity reaction.1
Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as any concomitant illnesses.1
Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.1
Importance of informing patients of other important precautionary information.1 (See Cautions.)
Additional Information
The American Society of Health-System Pharmacists, Inc. represents that the information provided in the accompanying monograph was formulated with a reasonable standard of care, and in conformity with professional standards in the field. Readers are advised that decisions regarding use of drugs are complex medical decisions requiring the independent, informed decision of an appropriate health care professional, and that the information contained in the monograph is provided for informational purposes only. The manufacturer's labeling should be consulted for more detailed information. The American Society of Health-System Pharmacists, Inc. does not endorse or recommend the use of any drug. The information contained in the monograph is not a substitute for medical care.
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.
Routes | Dosage Forms | Strengths | Brand Names | Manufacturer |
|---|---|---|---|---|
Ophthalmic | Solution | 0.5% | LevoFLOXacin Ophthalmic Solution |
AHFS® Drug Information. © Copyright, 1959-2025, Selected Revisions May 18, 2017. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, MD 20814.
Only references cited for selected revisions after 1984 are available electronically.
1. Akorn. Levofloxacin ophthalmic solution 0.5% prescribing information. Lake Forest, IL; 2016 May.
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3. Fish DN, Chow AT. The clinical pharmacokinetics of levofloxacin. Clin Pharmacokinet . 1997; 32:101-19. [PubMed 9068926]
4. Une T, Fujimoto T, Sato K et al. In vitro activity of DR-3355, an optically active ofloxacin. Antimicrob Agents Chemother . 1988; 32:1336-40. [PubMedCentral][PubMed 3195996]
5. Limberg MB. A review of bacterial keratitis and bacterial conjunctivitis. Am J Ophthalmol . 1991; 112:2-9S.
6. Barnes SD, Kumar NM, Pavin-Langston D et al. Microbial Conjunctivitis. In: Bennett JE, Dolin R, and Blaser MJ, eds. Mandell, Douglas, and Bennett's principles and practices of infectious diseases. 8th ed. Philadelphia, PA: Elsevier Saunders; 2015:1392-1401.
7. Thielen TL, Castle SS, Terry JE. Anterior ocular infections: an overview of pathophysiology and treatment. Ann Pharmacother . 2000; 34:235-46. [PubMed 10676832]
9. Hwang DG, Schanzlin DJ, Rotberg MH et al. A phase III, placebo controlled clinical trial of 0.5% levofloxacin ophthalmic solution for the treatment of bacterial conjunctivitis. Br J Ophthalmol . 2003; 87:1004-9. [PubMedCentral][PubMed 12881345]
10. Schwab IR, Friedlaender M, McCulley J et al. A phase III clinical trial of 0.5% levofloxacin ophthalmic solution versus 0.3% ofloxacin ophthalmic solution for the treatment of bacterial conjunctivitis. Ophthalmology . 2003; 110:457-65. [PubMed 12623805]
11. Lichtenstein SJ, Rinehart M, Levofloxacin Bacterial Conjunctivitis Study Group. Efficacy and safety of 0.5% levofloxacin ophthalmic solution for the treatment of bacterial conjunctivitis in pediatric patients. J AAPOS . 2003; 7:317-24. [PubMed 14566313]
16. Bearden DT, Danziger LH. Mechanism of action of and resistance to quinolones. Pharmacotherapy . 2001; 21:224S-32S. [PubMed 11642689]
17. American Academy of Ophthalmology. Preferred practice pattern (PPP) guidelines: conjunctivitis PPP - 2013. From American Academy of Ophthalmology website. Accessed 17 Oct 2016. [Web]
18. Azari AA, Barney NP. Conjunctivitis: a systematic review of diagnosis and treatment. JAMA . 2013; 310:1721-9. [PubMedCentral][PubMed 24150468]
19. Sheikh A, Hurwitz B, van Schayck CP et al. Antibiotics versus placebo for acute bacterial conjunctivitis. Cochrane Database Syst Rev . 2012; :CD001211.
20. Hooper DC, Strahilevitz J. Quinolones. In: Bennett JE, Dolin R, and Blaser MJ, eds. Mandell, Douglas, and Bennett's principles and practices of infectious diseases. 8th ed. Philadelphia, PA: Elsevier Saunders; 2015:419-39.
21. Janssen Pharmaceuticals Inc. Levaquin® (levofloxacin) tablets, film coated for oral use, solution for oral use, and solution in 5% dextrose for IV use prescribing information. Titusville, NJ; 2016 Jul.