Quixin

Medical Editor: John P. Cunha, DO, FACOEP Last updated on RxList: 7/21/2022

Drug Summary

What Is Quixin?

Quixin (levofloxacin ophthalmic solution 0.5%) is a fluoroquinolone antibiotic used to treat bacterial infections of the eyes. Quixin is available in generic form.

What Are Side Effects of Quixin?

Common side effects of Quixin include:

  • temporary blurred or decreased vision,
  • temporary stinging/burning/pain/discomfort in the eyes,
  • feeling as if something is in the eye,
  • sensitivity of the eyes to light,
  • dry or itchy eyes,
  • fever,
  • headache, or
  • sore throat

Quixin may cause serious side effects including:

  • hives,
  • difficulty breathing,
  • swelling of your face, lips, tongue, or throat,
  • drainage or crusting of your eye,
  • severe eye irritation after using the eye drops,
  • feeling like there is something in your eye,
  • vision problems,
  • increased sensitivity to light,
  • a skin rash (no matter how mild),
  • fever, and
  • any sign of a new infection

Get medical help right away, if you have any of the symptoms listed above.

Seek medical care or call 911 at once if you have the following serious side effects:

  • Serious eye symptoms such as sudden vision loss, blurred vision, tunnel vision, eye pain or swelling, or seeing halos around lights;
  • Serious heart symptoms such as fast, irregular, or pounding heartbeats; fluttering in your chest; shortness of breath; and sudden dizziness, lightheartedness, or passing out;
  • Severe headache, confusion, slurred speech, arm or leg weakness, trouble walking, loss of coordination, feeling unsteady, very stiff muscles, high fever, profuse sweating, or tremors.

This document does not contain all possible side effects and others may occur. Check with your physician for additional information about side effects.

Dosage for Quixin

The recommended dosing schedule for Quixin is on days 1 and 2, instill one to two drops in the affected eye(s) every 2 hours while awake, up to 8 times per day. On days 3 through 7, instill one to two drops in the affected eye(s) every 4 hours while awake, up to 4 times per day.

What Drugs, Substances, or Supplements Interact with Quixin?

It is not likely other drugs you take orally or inject will have an effect on Quixin ophthalmic. But many drugs can interact with each other.

Quixin During Pregnancy or Breastfeeding

Oral levofloxacin can interact with caffeine, theophylline or blood thinners. Tell your doctor all medications and supplements you use. During pregnancy, Quixin should be used only when prescribed. Based on information from related drugs, this medication may pass into breast milk. Consult your doctor before breastfeeding.

Additional Information

Our Quixin (levofloxacin ophthalmic solution 0.5%) Side Effects Drug Center provides a comprehensive view of available drug information on the potential side effects when taking this medication.

Description for Quixin

QUIXIN® (levofloxacin ophthalmic solution) 0.5% is a sterile topical ophthalmic solution. Levofloxacin is a fluoroquinolone antibacterial active against a broad spectrum of Gram-positive and Gram-negative ocular pathogens. Levofloxacin is a fluorinated 4-quinolone containing a six-member (pyridobenzoxazine) ring from positions 1 to 8 of the basic ring structure. Levofloxacin is the pure (-)-(S)-enantiomer of the racemic drug substance, ofloxacin. It is more soluble in water at neutral pH than ofloxacin.

QUIXIN® (levofloxacin ophthalmic solution) Structural Formula Illustration

C18H20FN3O4 •½H2O      Mol Wt 370.38

Chemical Name: (-)-(S)-9-fluoro-2,3-dihydro-3-methyl-10-(4-methyl-1-piperazinyl)-7-oxo-7H­pyrido[1,2,3-de]-1,4 benzoxazine-6-carboxylic acid hemihydrate. Levofloxacin (hemihydrate) is a yellowish-white crystalline powder.

Each mL of QUIXIN® contains 5.12 mg of levofloxacin hemihydrate equivalent to 5 mg levofloxacin.

Contains: Active: Levofloxacin 0.5% (5 mg/mL); Preservative: benzalkonium chloride 0.005%; Inactives: sodium chloride and water. May also contain hydrochloric acid and/or sodium hydroxide to adjust pH to approximately 6.5. UIXIN® solution is isotonic with an osmolality of approximately 300 mOsm/kg.

Uses for Quixin

QUIXIN® solution is indicated for the treatment of bacterial conjunctivitis caused by susceptible strains of the following organisms:

Gram-positive Bacteria

Corynebacterium species*
Staphylococcus aureus

Staphylococcus epidermidis

Streptococcus pneumonia

Streptococcus
(Groups C/F)
Streptococcus
(Group G)
Viridans group streptococci*

Gram-negative Bacteria

Acinetobacter lwoffii *
Haemophilus influenzae
Serratia marcescens*

*Efficacy for this organism was studied in fewer than 10 infections

Dosage for Quixin

DaysB 1 and 2

Instill one to two drops in the affected eye(s) every 2 hours while awake, up to 8 times per day.

Days 3 through 7

Instill one to two drops in the affected eye(s) every 4 hours while awake, up to 4 times per day.

HOW SUPPLIED

Dosage Forms And Strengths

5 cc bottle filled with 5 mL sterile ophthalmic solution of levofloxacin, 0.5%.

Storage Handling

QUIXIN® (levofloxacin ophthalmic solution) 0.5% is supplied in a white, low density polyethylene bottle with a controlled dropper tip and a tan, high density polyethylene cap.

5mL fill in a 5cc container ---NDC 68669-135-05

Storage

Store at 15° – 25°C (59° – 77°F)

Manufactured by: Santen Oy, P.O. Box 33, FIN-33721 Tampere, Finland Licensed from: Daiichi Sankyo Co., Ltd., Tokyo, Japan Revised: Nov 2014

Side Effects for Quixin

The most frequently reported adverse reactions in the overall study population were transient decreased vision, fever, foreign body sensation, headache, transient ocular burning, ocular pain or discomfort, pharyngitis and photophobia. These reactions occurred in approximately 1-3% of patients. Other reported reactions occurring in less than 1% of patients included allergic reactions, lid edema, ocular dryness, and ocular itching.

Drug Interactions for Quixin

No information provided.

Warnings for Quixin

Included as part of the PRECAUTIONS section.

Precautions for Quixin

Hypersensitivity Reactions

In patients receiving systemically administered quinolones, including levofloxacin, serious and occasionally fatal hypersensitivity (anaphylactic) reactions have been reported, some following the first dose. Some reactions were accompanied by cardiovascular collapse, loss of consciousness, angioedema, (including laryngeal, pharyngeal or facial edema), airway obstruction, dyspnea, urticaria and itching. If allergic reaction to levofloxacin occurs, discontinue the drug. Serious acute hypersensitivity reactions may require immediate emergency treatment. Oxygen and airway management should be administered as clinically indicated.

Growth Of Resistant Organisms With Prolonged Use

As with other anti-infectives, prolonged use may result in overgrowth of non-susceptible organisms, including fungi. If superinfection occurs, discontinue use and institute alternative therapy. Whenever clinical judgment dictates, the patient should be examined with the aid of magnification, such as slit-lamp biomicroscopy, and where appropriate, fluorescein staining.

Avoidance Of Contact Lens Wear

Patients should be advised not to wear contact lenses if they have signs and symptoms of bacterial conjunctivitis.

Nonclinical Toxicology

Carcinogenesis, Mutagenesis, Impairment Of Fertility

In a long term carcinogenicity study in rats, levofloxacin exhibited no carcinogenic or tumorigenic potential following daily dietary administration for 2 years at doses up to 100 mg/kg/day, corresponding to plasma levels that were 1235 times the maximum clinical exposure, based on Cmax.

Levofloxacin was not mutagenic in the following assays: Ames bacterial mutation assay (S. typhimurium and E. coli), CHO/HGPRT forward mutation assay, mouse micronucleus test, mouse dominant lethal test, rat unscheduled DNA synthesis assay, and the in vivo mouse sister chromatid exchange assay. It was positive in the in vitro chromosomal aberration (CHL cell line) and in vitro sister chromatid exchange (CHL/IU cell line) assays. Levofloxacin caused no impairment of fertility or reproduction in rats at oral doses as high as 360 mg/kg/day, at which systemic exposure was estimated to be 23,000 times that at the maximum recommended human ophthalmic dose.

Use In Specific Populations

Pregnancy

Pregnancy Category C

Teratogenic Effects

Levofloxacin at oral doses of 810 mg/kg/day in rats caused decreased fetal body weight and increased fetal mortality. No teratogenic effect was observed when rabbits were dosed orally as high as 50 mg/kg/day, at which systemic exposure was approximately 2,250 times that observed at the maximum recommended human ophthalmic dose, or when dosed intravenously as high as 25 mg/kg/day, at which systemic exposure was approximately 1000 times that observed at the maximum recommended human ophthalmic dose.

There are, however, no adequate and well-controlled studies in pregnant women. Levofloxacin should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Nursing Mothers

Levofloxacin has not been measured in human milk. Based upon data from ofloxacin, it can be presumed that levofloxacin is excreted in human milk. Caution should be exercised when QUIXIN® is administered to a nursing mother.

Pediatric Use

Safety and effectiveness in children below the age of six years have not been established. Oral administration of systemic quinolones has been shown to cause arthropathy in immature animals. There is no evidence that the ophthalmic administration of levofloxacin has any effect on weight bearing joints.

Geriatric Use

No overall differences in safety or effectiveness have been observed between elderly and other adult patients.

Overdose Information for Quixin

No information provided.

Contraindications for Quixin

QUIXIN® solution is contraindicated in patients with a history of hypersensitivity to levofloxacin, to other quinolones, or to any of the components in this medication.

Clinical Pharmacology for Quixin

Mechanism Of Action

Levofloxacin is a member of the fluoroquinolone class of anti-infective drugs. (See Microbiology)

Pharmacokinetics

Levofloxacin concentration in plasma was measured in 15 healthy adult volunteers at various time points during a 15-day course of treatment with QUIXIN® solution. The mean levofloxacin concentration in plasma 1 hour postdose, ranged from 0.86 ng/mL on Day 1 to 2.05 ng/mL on Day 15. The highest maximum mean levofloxacin concentration of 2.25 ng/mL was measured on Day 4 following 2 days of dosing every 2 hours for a total of 8 doses per day. Maximum mean levofloxacin concentrations increased from 0.94 ng/mL on Day 1 to 2.15 ng/mL on Day 15, which is more than 1,000 times lower than those reported after standard oral doses of levofloxacin.

Levofloxacin concentration in tears was measured in 30 healthy adult volunteers at various time points following instillation of a single drop of QUIXIN® solution. Mean levofloxacin concentrations in tears ranged from 34.9 to 221.1 mcg/mL during the 60-minute period following the single dose. The mean tear concentrations measured 4 and 6 hours postdose were 17.0 and 6.6 mcg/mL. The clinical significance of these concentrations is unknown.

Microbiology

Levofloxacin is the L-isomer of the racemate, ofloxacin, a quinolone antimicrobial agent. The antibacterial activity of ofloxacin resides primarily in the L-isomer. The mechanism of action of levofloxacin and other fluoroquinolone antimicrobials involves the inhibition of bacterial topoisomerase IV and DNA gyrase (both of which are type II topoisomerases), enzymes required for DNA replication, transcription, repair, and recombination.

Levofloxacin has in vitro activity against a wide range of Gram-negative and Gram-positive microorganisms and is often bactericidal at concentrations equal to or slightly greater than inhibitory concentrations.

Fluoroquinolones, including levofloxacin, differ in chemical structure and mode of action from β-lactam antibiotics and aminoglycosides, and therefore may be active against bacteria resistant to β-lactam antibiotics and aminoglycosides. Additionally, β-lactam antibiotics and aminoglycosides may be active against bacteria resistant to levofloxacin. Resistance to levofloxacin due to spontaneous mutation in vitro is a rare occurrence (range: 10-9 to 10-10)

Levofloxacin has been shown to be active against most strains of the following microorganisms, both in vitro and in clinical infections as described in the INDICATIONS AND USAGE section:

Aerobic Gram-positive Microorganisms

Corynebacterium species*
Staphylococcus aureus

Staphylococcus epidermidis

Streptococcus pneumonia

Streptococcus
(Groups C/F)
Streptococcus
(Group G)
Viridans group streptococci*

Aerobic Gram-negative Microorganisms

Acinetobacter lwoffii*
Haemophilus influenzae

Serratia marcescens*

*Efficacy for this organism was studied in fewer than 10 infections.

The following in vitro data are also available, but their clinical significance in ophthalmic infections is unknown. The safety and effectiveness of levofloxacin in treating ophthalmological infections due to these microorganisms have not been established in adequate and well-controlled trials.

These organisms are considered susceptible when evaluated using systemic breakpoints. However, a correlation between the in vitro systemic breakpoint and ophthalmological efficacy has not been established. The list of organisms is provided as guidance only in assessing the potential treatment of conjunctival infections. Levofloxacin exhibits in vitro minimal inhibitory concentrations (MICs) of 2 mcg/mL or less (systemic susceptible breakpoint) against most ( ≥ 90%) strains of the following ocular pathogens:

Aerobic Gram-positive Microorganisms

Enterococcus faecalis
Staphylococcus saprophyticus

Streptococcus agalactiae

Streptococcus pyogenes

Aerobic Gram-negative Microorganisms

Acinetobacter anitratus
Acinetobacter baumannii

Citrobacter koseri

Citrobacter freundii

Enterobacter aerogenes

Enterobacter agglomerans

Enterobacter cloacae

Escherichia coli

Haemophilus parainfluenzae

Klebsiella oxytoca

Klebsiella pneumonia

Legionella pneumophila

Moraxella catarrhalis

Morganella morganii

Neisseria gonorrhoeae

Proteus mirabilis

Proteus vulgaris

Providencia rettgeri

Providencia stuartii

Pseudomonas aeruginosa

Pseudomonas fluorescens

Clinical Studies

In randomized, double-masked, multicenter controlled clinical trials where patients were dosed for 5 days, QUIXIN® demonstrated clinical cures in 79% of patients treated for bacterial conjunctivitis on the final study visit day (day 6-10). Microbial outcomes for the same clinical trials demonstrated an eradication rate for presumed pathogens of 90%.

Patient Information for Quixin

Avoid Contamination Of The Product

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

Avoid Contact Lens Wear

Advise patients not to wear contact lenses if they have signs and symptoms of bacterial conjunctivitis.

Hypersensitivity Reactions

Systemically administered quinolones, including levofloxacin, have been associated with hypersensitivity reactions, even following a single dose. Advise patients to discontinue use immediately and contact their physician at the first sign of a rash or allergic reaction.

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Report Problems to the Food and Drug Administration

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