Professional Drug Information > Quixin

Levofloxacin (Ophthalmic)

VA CLASSIFICATION
Primary: OP201

Commonly used brand name(s): Quixin.

Note: For a listing of dosage forms and brand names by country availability, see Dosage Forms section(s).



Category:


Antibacterial (ophthalmic) —

Indications

Accepted

Conjunctivitis, bacterial (treatment)—Levofloxacin ophthalmic solution is indicated in the treatment of conjunctivitis caused by susceptible strains of bacteria, includingAcinetobacter lwoffii, Corynebacterium species, Haemophilus influenzae, Serratia marcescens, Staphylococcus aureus (methicillin-susceptible strains only), Staphylococcus epidermidis (methicillin-susceptible strains only), Streptococcus pneumoniae, Streptococcus (groups C/F), Streptococcus (group G), and viridans group Streptococci.^{01}


Pharmacology/Pharmacokinetics

Physicochemical characteristics:

Chemical group—
    Fluoroquinolone^{01}
    Levofloxacin is the pure (-)-(S)– enantiomer of ofloxacin.^{01}
Molecular weight—
    370.38^{01}


pH
    6.5

Mechanism of action/Effect:

Levofloxacin's bactericidal action results from interference with the enzymes topoisomerase IV and DNA gyrase, which are needed for the synthesis of bacterial DNA. ^{01}

Absorption:

Fifteen subjects were treated with varying doses of levofloxacin over a 15 day testing period. The plasma concentration of levofloxacin ranged from 0.86 ng/ml on day 1 to 2.05 ng/ml on day 15. The highest level, 2.25 ng/ml, was recorded on day 4.^{01}


Precautions to Consider

Cross-sensitivity and/or related problems

Patients sensitive to other quinolones, such as cinoxacin, ciprofloxacin, nalidixic acid, norfloxacin, or ofloxacin, may be sensitive to this medication also. ^{01}

Carcinogenicity

Rats and mice administered dietary levofloxacin for up to 2 years did not show carcinogenic effects. The highest dose, 100 mg per kg per day, was 875 times higher than the highest recommended human ophthalmic dose.^{01}

Mutagenicity

Levofloxacin was found to be mutagenic in the in vitro chromosomal aberration (CHL cell line) and in vitro sister chromatid exchange (CHL/IU cell line) assays. It was negative in the Ames bacterial mutation assay (S. typhimurium and E. coli), the CHO/HGPRT forward mutation assay, the mouse micronucleus test, the mouse dominant lethal test, the rat unscheduled DNA synthesis assay, and the in vivo mouse sister chromatid exchange assay^{01}.

Pregnancy/Reproduction
Fertility—
Studies performed in rats administered levofloxacin in oral doses as high as 360 mg per kg per day, (3,150 times higher than the highest recommended human ophthalmic dose), revealed no evidence of impaired fertility. ^{01}

Pregnancy—
Adequate and well-controlled studies in humans have not been done. ^{01}No teratogenic effects were found when rabbits were given 50 mg per kg per day of levofloxacin orally or 25 mg per kg per day intravenously, (400 and 200 times the highest recommended ophthalmic dose, respectively). ^{01} Decreased fetal body weight and increased fetal mortality occurred in rats given oral levofloxacin at doses of 810 mg per kg per day, (7,000 times the highest recommended human ophthalmic dose).^{01}

FDA Pregnancy Category C.^{01}

Breast-feeding

It is not known whether ophthalmic levofloxacin is distributed into breast milk.^{01}However, based upon data from ofloxacin, it can be presumed that levofloxacin is excreted in human milk.^{01}

Pediatrics

The safety of levofloxacin in infants less than one year of age has not been determined. Although oral administration of quinolones have been shown to cause arthropathy in immature animals, there is no evidence that ophthalmic administration of levofloxacin has any negative effect on weight bearing joints.^{01}


Geriatrics


Appropriate studies performed to date have not demonstrated geriatrics-specific problems that would limit the usefulness of levofloxacin in the elderly.^{01}

Medical considerations/Contraindications
The medical considerations/contraindications included have been selected on the basis of their potential clinical significance (reasons given in parentheses where appropriate)— not necessarily inclusive (» = major clinical significance).


Except under special circumstances, this medication should not be used when the following medical problem exists
Hypersensitivity to levofloxacin or other quinolones^{01}


Side/Adverse Effects
The following side/adverse effects have been selected on the basis of their potential clinical significance (possible signs and symptoms in parentheses where appropriate)—not necessarily inclusive:

Those indicating need for medical attention only if they continue or are bothersome
Incidence less frequent or rare
    
Allergic reactions^{01} (itching, pain, redness, or swelling of eye or eyelid; watering of eyes)
    
fever ^{01}
    
foreign body sensation ^{01}( feeling of having something in the eye)
    
headache
    
ocular problems,^{01} such as,
decreased vision^{01}
lid edema^{01} (swelling of eyelid ), burning, dryness, itching, or pain^{01}
photophobia,^{01} (increased sensitivity of eyes to light)
    
pharyngitis.^{01} (body aches or pain; congestion; dryness or soreness of throat; fever; hoarseness ; runny nose; tender, swollen glands in neck; trouble in swallowing; voice changes )





Overdose
For more information on the management of overdose or unintentional ingestion, contact a poison control center (see Poison Control Center Listing).

Treatment of overdose


Specific treatment:
There is no known specific antidote to levofloxacin. Treatment is generally symptomatic and supportive.^{01}

Patients in whom intentional overdose is confirmed or suspected should be referred for psychiatric consultation.^{01}



Patient Consultation
As an aid to patient consultation, refer to Advice for the Patient, Levofloxacin (Ophthalmic).

In providing consultation, consider emphasizing the following selected information (» = major clinical significance):

Before using this medication
»   Conditions affecting use, especially:
Sensitivity to levofloxacin or other quinolones





Breast-feeding—Based on data from ofloxacin, it can be presumed that levofloxacin is distributed in human milk. However, levofloxacin has not been measured in human milk.




Use in children——Safety and efficacy have not been established in children below the age of one year.


Proper use of this medication
Proper administration technique

» Compliance with full course of therapy

» Proper dosing
Using as soon as possible; not using if almost time for next scheduled dose; not doubling doses

Proper storage

Precautions while using this medication
Checking with physician if no improvement within a few days, or if infection gets worse

Possible photophobic reactions; wearing sunglasses and avoiding prolonged exposure to bright light


General Dosing Information
Levofloxacin ophthalmic solution is not for injection into the eye, nor should it be introduced directly into the anterior chamber of the eye. ^{01}

If hypersensitivity develops, therapy with ophthalmic levofloxacin should be discontinued. ^{01}

Patients should be advised not be wear contacts if they have signs and symptoms of bacterial conjunctivitis.^{01}

As with other antiinfectives, prolonged use may result in overgrowth of non-susceptible organisms. Should superinfection occur, discontinue use and consider alternative therapy.^{01}

For treatment of adverse effects
Recommended treatment includes

   • Discontinue levofloxacin treatments if an allergic reaction occurs.^{01}
   • Serious hypersensitivity reactions should receive emergency medical treatment including administration of oxygen and airway management.^{01}


Ophthalmic Dosage Forms

Note: The dosing and strengths of the dosage forms available are expressed in terms of levofloxacin base.


LEVOFLOXACIN OPHTHALMIC SOLUTION

Usual adult and adolescent dose
Bacterial conjunctivitis
Topical, to the conjunctiva, Day 1 and 2: one to two drops in the affected eye(s) every 2 hours while awake, up to 8 times per day. Days 3–7: one to two drops in the affected eye(s) every 4 hours while awake, up to 4 times per day.^{01}


Usual pediatric dose
Bacterial conjunctivitis
Infants up to 1 year of age: Safety and efficacy have not been established. ^{01}

Children over 1 year of age: See Usual adult and adolescent dose. ^{01}


Strength(s) usually available
U.S.—


5.12 mg (5 mg base) per mL (Rx) [Quixin^{01} (benzalkonium chloride 0.005%) (sodium chloride) (hydrochloric acid and/or) (sodium hydroxide)]

Packaging and storage:
Store between 15 –25 °C (59 and 77 °F) in a tight container.^{01}

Auxiliary labeling:
   • For the eye.
   • Continue medicine for full time of treatment.

Developed: 10/20/2000

References

1. Product Information: Quixin™, levofloxacin. Santen, Napa, CA, (PI revised 8/2000) reviewed 10/2000.
   

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