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Ciprofloxacin (Ophthalmic)


VA CLASSIFICATION
Primary: OP201

Commonly used brand name(s): Ciloxan.

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



Category:


Antibacterial (ophthalmic)—

Indications

Accepted

Corneal ulcers, bacterial (treatment)—Ophthalmic ciprofloxacin solution {07} and [ophthalmic ciprofloxacin ointment{08}] are indicated in the treatment of corneal ulcers caused by susceptible strains of bacteria, including {04} Pseudomonas aeruginosa , Serratia marcescens , Staphylococcus aureus , Staphylococcus epidermidis , Streptococcus pneumoniae , and Streptococcus (Viridans Group) . {01} {06} {07} {08}

Conjunctivitis, bacterial (treatment)—Ophthalmic ciprofloxacin ointment and solution are {07} indicated in the treatment of conjunctivitis caused by Haeomophilus influenzae , Staphylococcus aureus , Staphylococcus epidermidis , Streptococcus pneumoniae , and Streptococcus (Viridans Group) . {01} {06} {07} {08}

Note: Not all species or strains of a particular organism may be susceptible to ciprofloxacin. {01} Streptococcal species are often less susceptible. {04}



Pharmacology/Pharmacokinetics

Physicochemical characteristics:

Chemical group—
    Fluoroquinolone. {01}
Molecular weight—
    385.82 {02}

Mechanism of action/Effect:

Ciprofloxacin's bactericidal action results from interference with the enzyme DNA gyrase, which is needed for the synthesis of bacterial DNA. {01}

Absorption:

During the patient's waking hours, ciprofloxacin was administered in each eye every 2 hours for 2 days followed by every 4 hours for an additional 5 days. The maximum reported plasma concentration of ciprofloxacin was less than 5 nanograms per mL. The mean concentration was usually less than 2.5 nanograms per mL. {01}


Precautions to Consider

Cross-sensitivity and/or related problems

Patients sensitive to other quinolones, such as cinoxacin, nalidixic acid, norfloxacin, or ofloxacin, may be sensitive to this medication also. {01} {07}

Carcinogenicity

Rats and mice administered ciprofloxacin orally for up to 2 years did not show carcinogenic effects. {01} {07}

Mutagenicity

Ciprofloxacin was not found to be mutagenic in the following in vitro tests: Salmonella /Microsome test, E. coli DNA Repair assay, Chinese Hamster V 7 9 Cell HGPRT test, Syrian Hamster Embryo Cell Transformation assay, Saccharomyces cerevisiae Point Mutation assay, and Saccharomyces cerevisiae Mitotic Crossover and Gene Conversion assay. In addition, ciprofloxacin was not found to be mutagenic in the following in vivo tests: Rat Hepatocyte DNA Repair assay, Micronucleus test (mice), and Dominant Lethal test (mice). However, ciprofloxacin was found to be mutagenic in the in vitro Mouse Lymphoma Cell Forward Mutation assay and the in vitro Rat Hepatocyte DNA Repair assay. {01} {07}

Pregnancy/Reproduction
Fertility—
Studies performed in rats and mice administered ciprofloxacin in oral doses up to 6 times the usual daily human oral dose revealed no evidence of impaired fertility. {07}

Pregnancy—
Adequate and well-controlled studies in humans have not been done. {01} {07} However, problems in humans have not been documented.

Reproduction studies performed in rats and mice administered ciprofloxacin in oral doses up to 6 times the usual daily human oral dose revealed no evidence of harm to the fetus. In rabbits, ciprofloxacin, like most antimicrobial agents, when administered in oral doses of 30 and 100 mg per kg of body weight (mg/kg) per day produced gastrointestinal disturbances resulting in maternal weight loss and an increased incidence of abortion. However, no teratogenicity was observed at either dose. Ciprofloxacin administered intravenously in doses of up to 20 mg/kg, produced no maternal toxicity, embryotoxicity, or teratogenicity. {01} {07}

FDA Pregnancy Category C. {01} {07}

Breast-feeding

It is not known whether ophthalmic ciprofloxacin is distributed into breast milk. {07} However, oral ciprofloxacin was shown to be distributed into breast milk after a single 500 mg dose. {01} {07}

Pediatrics

Appropriate studies on the relationship of age to the effects of ciprofloxacin have not been performed in children up to 2 years of age for the ophthalmic ointment dosage form and 1 year of age for the ophthalmic solution dosage form. {07} Safety and efficacy have not been established. {01} {07}

Although ciprofloxacin and other quinolones cause arthropathy in immature Beagle dogs after oral administration, ophthalmic ciprofloxacin administered to immature animals did not cause any arthropathy. In addition, there is no evidence that the ophthalmic dosage form has any effect on the weight bearing joints. {01} {07}


Geriatrics


No information is available on the relationship of age to the effects of ciprofloxacin in geriatric patients.

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).


Risk-benefit should be considered when the following medical problem exists
Sensitivity to ciprofloxacin{01}


Side/Adverse Effects

Note: In corneal ulcer studies, frequent administration of ophthalmic ciprofloxacin resulted in white crystalline precipitates in the eyes of 17% of patients using the ophthalmic solution and 13% of patients using the ophthalmic ointment. {01} {07} This precipitate did not prevent the continued use of the medication and did not adversely affect treatment outcome. {01} {04}

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
Incidence rare
    
Allergic reaction,{07} such as skin rash, hives, or itching
    
blurred vision{07}
    
corneal infiltrates{01}{07}
corneal staining{01}{07}
decreased vision{01}{07}
epitheliopathy{07}
or keratopathy{01}{07} (blurred vision or other change in vision)
    
dermatitis{07} (skin rash)
    
eye pain or irritation{07}
    
keratitis{01}{07} (severe irritation or redness of eye)
    
nausea{01}{07}



Those indicating need for medical attention only if they continue or are bothersome
Incidence more frequent
    
Burning or other discomfort of the eye{01}{07}
    
crusting or crystals in corner of eye{01}{07}

Incidence less frequent
    
Bad taste following instillation{01}{07}
    
foreign body sensation{01}{07} (feeling of something in eye)
    
hyperemia, conjunctival{01}{07} (redness of the lining of the eyelids)
    
itching of eye{01}{07}

Rare
    
Dryness of eye{07}
    
lid edema{01}{07} (swelling of eyelid)
    
photophobia{01}{07} (increased sensitivity of eyes to light)
    
tearing of eye{01}{07}





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
A topical overdose of ciprofloxacin ophthalmic solution may be flushed from the eye(s) with warm tap water. {07}


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

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

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





Breast-feeding—Oral ciprofloxacin is distributed into breast milk; it is not known whether ophthalmic ciprofloxacin is distributed into breast milk





Use in children—Safety and efficacy have not been established in children up to 2 years of age for the ophthalmic ointment and 1 year of age for the ophthalmic solution


Proper use of this medication
Proper administration technique

» Compliance with full course of therapy

» Proper dosing
Missed dose: Applying as soon as possible; not applying if almost time for next dose

» Proper storage

Precautions while using this medication
Checking with physician if no improvement within a few days

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


Side/adverse effects
Signs of potential side effects, especially allergic reaction, blurred vision, corneal infiltrates, corneal staining, decreased vision, epitheliopathy, keratopathy, dermatitis, eye pain or irritation, keratitis, or nausea


General Dosing Information
Ciprofloxacin ophthalmic solution is not for injection into the eye. {01}

Although some manufacturers recommend doses of 2 drops of ophthalmic solutions at appropriate intervals, the conjunctival sac usually holds less than 1 drop.

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

For treatment of adverse effects
Recommended treatment includes

   • For mild hypersensitivity reaction—Administering antihistamines and, if necessary, glucocorticoids.
   • For severe hypersensitivity or anaphylactic reaction—Administering epinephrine. Antihistamines and/or glucocorticoids may also be administered as required.


Ophthalmic Dosage Forms

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


CIPROFLOXACIN HYDROCHLORIDE OPHTHALMIC OINTMENT

Usual adult and adolescent dose
Bacterial conjunctivitis
Topical, to the conjunctiva, 1/2-inch (1.25 cm) strip of ointment in each eye three times a day for two days, then two times a day for the next five days. {07} {08}

[Corneal ulcers]
Topical, to the conjunctiva, 1/2-inch (1.25 cm) strip of ointment in the affected eye every 1 or 2 hours around the clock for the first two days, then every 4 hours for up to twelve days. If corneal re-epithelialization has not occurred after twelve days of treatment, treatment may be continued. {08}


Usual pediatric dose
Bacterial conjunctivitis
Infants and children up to 2 years of age: Safety and efficacy have not been established. {07}

Children over 2 years of age: See Usual adult and adolescent dose. {07}

[Corneal ulcers]
Infants and children up to 12 years of age: Safety and efficacy have not been established. {08}

Children over 12 years of age: See Usual adult and adolescent dose. {08}


Strength(s) usually available
U.S.—


3.33 mg (3 mg base) per gram (Rx) [Ciloxan{07}]

Canada—


3.5 mg (3 mg base) per gram (Rx) [Ciloxan{08}]

Packaging and storage:
Store between 2 and 25 °C (36 and 77 °F), unless otherwise specified by manufacturer. {07}

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


CIPROFLOXACIN HYDROCHLORIDE OPHTHALMIC SOLUTION USP

Usual adult and adolescent dose
Bacterial conjunctivitis
Topical, to the conjunctiva, 1 drop in each eye every two hours, while patient is awake, for two days, then 1 drop every four hours, while patient is awake, for the next five days. {01} {07} {08}

Corneal ulcers
Topical, to the conjunctiva, 2 drops in the affected eye every fifteen minutes for six hours, then 2 drops every thirty minutes, while patient is awake, for the rest of day one; 2 drops every hour, while patient is awake, on day two; and 2 drops every four hours, while patient is awake, on days three through fourteen. If corneal re-epithelialization has not occurred after fourteen days of treatment, treatment may be continued. {01} {07} {08}

Note: During the initial 24 to 48 hours, additional doses may be necessary during the night in some cases. {04}



Usual pediatric dose
Bacterial conjunctivitis
Infants and children up to 1 year of age: Safety and efficacy have not been established. {01} {07}

Children over 1 year of age: See Usual adult and adolescent dose. {01} {07} {08}

Corneal ulcers


In the U.S.:
Infants and children up to 1 year of age: Safety and efficacy have not been established. {07}

Children over 1 year of age: See Usual adult and adolescent dose. {07}



In Canada:
Infants and children up to 12 years of age: Safety and efficacy have not been established. {08}

Children over 12 years of age: See Usual adult and adolescent dose. {08}



Strength(s) usually available
U.S.—


3.5 mg (3 mg base) per mL (Rx) [Ciloxan{01}{07} (benzalkonium chloride 0.006%)]

Canada—


3.5 mg (3 mg base) per mL (Rx) [Ciloxan{05}{08} (benzalkonium chloride 0.006%)]

Packaging and storage:
Store below 40 °C (104 °F), preferably between 15 and 30 °C (59 and 86 °F), unless otherwise specified by manufacturer. {03} Store in a tight container. {03} Protect from light. {03} {07}

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



Revised: 06/14/1999



References
  1. Ciloxan package insert (Alcon—US), PDR Ophthalmology 1993: 211.
  1. Fleeger CA, editor. USAN 1993. USAN and the USP dictionary of drug names. Rockville, MD: The United States Pharmacopeial Convention, Inc., 1992.
  1. The United States pharmacopeia. The national formulary. USP 22nd revision (January 1, 1990). NF 17th ed (January 1, 1990). Rockville, MD: The United States Pharmacopeial Convention, Inc., 1990: 3031.
  1. Panel comments, 4/93.
  1. Ciloxan product monograph (Alcon—Canada), Rev 3/92, Rec 4/93.
  1. Yolton DP. New antibacterial drugs for topical ophthalmic use. Optom Clin 1992; 2(4): 59-72.
  1. Ciloxan (Alcon). In: PDR Physicians' desk reference. 53rd ed. 1999. Montvale, NJ: Medical Economics Company Inc; 1999. p. 490-1.
  1. Ciloxan (Alcon). In: Gillis MC, editor. CPS Compendium of pharmaceuticals and specialties. 34th ed. Ottawa: Canadian Pharmacists Association; 1999. p. 347-8.
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