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
Antibacterial; fluoroquinolone; levorotatory isomer of ofloxacin.1 2 20
Uses for Levofloxacin
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.1 9 10 11
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 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
Levofloxacin Dosage and Administration
Apply 0.5% ophthalmic solution topically to the eye.1
For topical ophthalmic use only.1
Avoid contaminating applicator tip with material from eye, fingers, or other source.1
Bacterial Ophthalmic Infections
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 7.1
Bacterial Ophthalmic Infections
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 7.1
Cautions for Levofloxacin
Hypersensitivity to levofloxacin, other quinolones, or any ingredient in the formulation.1
Serious and occasionally fatal hypersensitivity and/or anaphylactic reactions reported with systemic fluoroquinolones, including systemic levofloxacin;1 21 these reactions may occur with 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
Immediately discontinue levofloxacin ophthalmic solution at first sign of rash or hypersensitivity reaction.1
Prolonged use may result in overgrowth of nonsusceptible organisms, including fungi.1
If superinfection occurs, discontinue levofloxacin ophthalmic solution and institute appropriate therapy.1
Whenever clinical judgment dictates, examine patient with the aid of magnification (e.g., slit lamp biomicroscopy) and, if appropriate, fluorescein staining.1
Do not wear contact lenses if any signs or symptoms of bacterial conjunctivitis are present.1
Data not available regarding use of levofloxacin 0.5% ophthalmic solution in pregnant women;1 use only if potential benefits to the woman justify potential risks to fetus.1
Since ofloxacin is distributed into human milk, levofloxacin (levorotatory isomer of ofloxacin) is presumed to be distributed into human milk.1
Use with caution in nursing women.1
Safety and efficacy not established in children <6 years of age.1
No overall differences in safety and efficacy relative to younger adults.1
Common Adverse Effects
Transient decrease in vision, transient ocular burning, ocular pain or discomfort, foreign body sensation, photophobia, headache, fever, pharyngitis.1
Interactions for Levofloxacin
No formal drug interaction studies using levofloxacin 0.5% ophthalmic solution.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 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 15.1
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.1
Contains benzalkonium chloride as a preservative.1
Actions and Spectrum
Fluoroquinolone anti-infective.1 2 20
Like other fluoroquinolones, inhibits bacterial DNA synthesis in susceptible bacteria via inhibition of type II DNA topoisomerases (DNC gyrase, topoisomerase IV).1 16 20
May be bactericidal at concentrations equal to or slightly greater than inhibitory concentrations.1 4
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, Streptococcus pneumoniae, groups C, F, and G streptococci, viridans streptococci, Corynebacterium, 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
Advice to Patients
Advise patients to avoid contaminating applicator tip with material from the eye, fingers, or other source.1
Advise patients 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 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.)
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.
levoFLOXacin Ophthalmic Solution
AHFS DI Essentials. © Copyright 2018, Selected Revisions May 22, 2017. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.
1. Akorn. Levofloxacin ophthalmic solution 0.5% prescribing information. Lake Forest, IL; 2016 May.
2. Davis R, Bryson HM. Levofloxacin: a review of its antibacterial activity, pharmacokinetics and therapeutic efficacy. Drugs. 1994; 47:677-700. [PubMed 7516863]
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. [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. [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.
18. Azari AA, Barney NP. Conjunctivitis: a systematic review of diagnosis and treatment. JAMA. 2013; 310:1721-9. [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.
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