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
Uses for Levofloxacin
Bacterial Ophthalmic Infections
Treatment of conjunctivitis caused by susceptible Acinetobacter lwoffii, Corynebacterium spp, Haemophilus influenzae, Serratia marcescens, Staphylococcus aureus, S. epidermidis, groups C, F, and G streptococci, viridans streptococci, or Streptococcus pneumoniae.1 8
Role of topical fluoroquinolones in management of uncomplicated bacterial conjunctivitis not fully elucidated; some clinicians suggest that the drugs be reserved principally for severe bacterial conjunctivitis because of potential development of quinolone resistance, and possibly, cost considerations.7 12 13 14
Levofloxacin Dosage and Administration
Apply topically to the eye as an ophthalmic solution.1
Avoid contamination of applicator tip.1
Bacterial Ophthalmic Infections
Children ≥1 year of age: 1 or 2 drops of 0.5% solution in affected eye(s) every 2 hours while awake (up to 8 times daily) for 2 days, then 1 or 2 drops every 4 hours while awake (up to 4 times daily) for the next 5 days.1
Bacterial Ophthalmic Infections
1 or 2 drops of 0.5% solution in affected eye(s) every 2 hours while awake (up to 8 times daily) for 2 days, then 1 or 2 drops every 4 hours while awake (up to 4 times daily) for the next 5 days.1
Cautions for Levofloxacin
Hypersensitivtity to levofloxacin, other quinolones, or any ingredient in the formulation.1
Serious, potentially fatal hypersensitivity reactions reported following systemic administration of fluoroquinolones; has occurred with the initial dose.1
If allergic reaction occurs, discontinue levofloxacin and institute appropriate therapy if indicated.1
Possible overgrowth of nonsusceptible organisms (e.g., fungi) with prolonged use; if superinfection occurs, discontinue levofloxacin and institute other appropriate therapy.1
Careful monitoring, including slit-lamp biomicroscopy and fluorescein staining when appropriate, may be necessary in some patients.1
Safety and efficacy not established in children <1 year of age.1
No substantial 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, headache, fever, pharyngitis, photophobia.1
Maximum mean plasma levofloxacin concentrations after topical application of 0.5% ophthalmic solution to the eye for 15 days were >1000 times lower than those reported after standard oral doses.1
Actions and Spectrum
Spectrum of activity includes gram-positive aerobic bacteria and some gram-negative aerobic bacteria.1
Advice to Patients
Importance of discontinuing drug and informing clinician at first sign of rash or other sign of hypersensitivity.1
Importance of learning and adhering to proper administration techniques to avoid contamination of the product.1
Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs.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.
Quixin (with benzalkonium chloride)
AHFS DI Essentials. © Copyright 2016, Selected Revisions October 30, 2014. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.
1. Santen. Quixin (levofloxacin) ophthalmic solution 0.5% prescribing information. Napa, CA; 2000 Oct.
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. [IDIS 248086] [PubMed 3195996]
5. O’Brien T. Conjunctivitis. In: Mandell GL, Bennett JE, Dolin R eds. Principles and practices of infectious diseases. 5th ed. New York: Churchill Livingstone; 2000:1251-6.
6. Limberg MB. A review of bacterial keratitis and bacterial conjunctivitis. Am J Ophthalmol. 1991; 112:2-9S.
7. Thielen TL, Castle SS, Terry JE. Anterior ocular infections: an overview of pathophysiology and treatment. Ann Pharmacother. 2000; 34:235-46. [IDIS 439875] [PubMed 10676832]
8. Santen. Quixin (levofloxacin ophthalmic solution) 0.5% product monograph. Napa, CA; 2000.
9. Hwang DG, Rotberg MH, Montgomery JE et al. Efficacy and safety of 0.5% levofloxacin ophthalmic solution (LVFX) compared to placebo for the treatment of bacterial conjunctivitis. Poster presented at the Association for Research in Vision and Ophthalmology (ARVO) annual meeting. Fort Lauderdale, FL: 2000 Apr 30-May 5.
10. McCulley JP, Wapner FJ, Graves AL et al. Efficacy and safety of 0.5% levofloxacin ophthalmic solution (LVFX) for the treatment of bacterial conjunctivitis. Poster presented at the Association for Research in Vision and Ophthalmology (ARVO) annual meeting. Fort Lauderdale, FL: 2000 Apr 30-May 5.
11. Graves AL, Lichtenstein SJ, Moran CT et al. Pediatric efficacy and safety of 0.5% levofloxacin ophthalmic solution (LVFX) for the treatment of bacterial conjunctivitis. Poster presented at the Association for Research in Vision and Ophthalmology (ARVO) annual meeting. Fort Lauderdale, FL: 2000 Apr 30-May 5.
12. Yolton DP. New antibacterial drugs for topical ophthalmic use. Optom Clin. 1992; 2:59-72.
13. Gwon A for the Ofloxacin Study Group II. Ofloxacin vs tobramycin for the treatment of external ocular infection. Arch Ophthalmol. 1992; 110:1234-7. [IDIS 301536] [PubMed 1520109]
14. Robert PY, Adenis JP. Comparative review of topical ophthalmic antibacterial preparations. Drugs. 2001; 61:175-85.
15. Santen. Napa, CA: Personal communication.
16. Bearden DT, Danziger LH. Mechanism of action of and resistance to quinolones. Pharmacotherapy. 2001; 21:224S-32S. [IDIS 472236] [PubMed 11642689]