Ciloxan Information
Ciloxan (Ciprofloxacin) Description
Ciloxan (Ciprofloxacin) ® (ciprofloxacin HCl ophthalmic solution) is a synthetic, sterile, multiple dose, antimicrobial for topical ophthalmic use. Ciprofloxacin is a fluoroquinolone antibacterial active against a broad spectrum of gram-positive and gram-negative ocular pathogens. It is available as the monohydrochloride monohydrate salt of 1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-7-(1-piperazinyl)-3-quinoline-carboxylic acid. It is a faint to light yellow crystalline powder with a molecular weight of 385.8. Its empirical formula is CHFNO•HCl•HO and its chemical structure is as follows:
Ciprofloxacin differs from other quinolones in that it has a fluorine atom at the 6-position, a piperazine moiety at the 7-position, and a cyclopropyl ring at the 1-position.
Each mL of Ciloxan (Ciprofloxacin) Ophthalmic Solution contains: ciprofloxacin HCl 3.5 mg equivalent to 3 mg base. benzalkonium chloride 0.006%. sodium acetate, acetic acid, mannitol 4.6%, edetate disodium 0.05%, hydrochloric acid and/or sodium hydroxide (to adjust pH) and purified water. The pH is approximately 4.5 and the osmolality is approximately 300 mOsm.
Ciloxan (Ciprofloxacin) Clinical Pharmacology
Ciprofloxacin has been shown to be active against most strains of the following organisms both and in clinical infections. (See section).
Ciprofloxacin has been shown to be active against most strains of the following organisms, however, :
Most strains of and some strains of are resistant to ciprofloxacin as are most anaerobic bacteria, including and .
The minimal bactericidal concentration (MBC) generally does not exceed the minimal inhibitory concentration (MIC) by more than a factor of 2. Resistance to ciprofloxacin usually develops slowly (multiple-step mutation).
Ciprofloxacin does not cross-react with other antimicrobial agents such as beta-lactams or aminoglycosides; therefore, organisms resistant to these drugs may be susceptible to ciprofloxacin.
Following therapy with Ciloxan (Ciprofloxacin) Ophthalmic Solution, 76% of the patients with corneal ulcers and positive bacterial cultures were clinically cured and complete re-epithelialization occurred in about 92% of the ulcers.
In 3 and 7 day multicenter clinical trials, 52% of the patients with conjunctivitis and positive conjunctival cultures were clinically cured and 70-80% had all causative pathogens eradicated by the end of treatment.
Ciloxan (Ciprofloxacin) Indications And Usage
Ciloxan (Ciprofloxacin) Ophthalmic Solution is indicated for the treatment of infections caused by susceptible strains of the designated microorganisms in the conditions listed below:
*Efficacy for this organism was studied in fewer than 10 infections.
Ciloxan (Ciprofloxacin) Contraindications
A history of hypersensitivity to ciprofloxacin or any other component of the medication is a contraindication to its use. A history of hypersensitivity to other quinolones may also contraindicate the use of ciprofloxacin.
Ciloxan (Ciprofloxacin) Warnings
NOT FOR INJECTION INTO THE EYE.
Serious and occasionally fatal hypersensitivity (anaphylactic) reactions, some following the first dose, have been reported in patients receiving systemic quinolone therapy. Some reactions were accompanied by cardiovascular collapse, loss of consciousness, tingling, pharyngeal or facial edema, dyspnea, urticaria, and itching. Only a few patients had a history of hypersensitivity reactions. Serious anaphylactic reactions require immediate emergency treatment with epinephrine and other resuscitation measures, including oxygen, intravenous fluids, intravenous antihistamines, corticosteroids, pressor amines and airway management, as clinically indicated.
Remove contact lenses before using.
Ciloxan (Ciprofloxacin) Precautions
As with other antibacterial preparations, prolonged use of ciprofloxacin may result in overgrowth of nonsusceptible organisms, including fungi. If superinfection occurs, appropriate therapy should be initiated. Whenever clinical judgment dictates, the patient should be examined with the aid of magnification, such as slit lamp biomicroscopy and, where appropriate, fluorescein staining.
Ciprofloxacin should be discontinued at the first appearance of a skin rash or any other sign of hypersensitivity reaction.
In clinical studies of patients with bacterial corneal ulcer, a white crystalline precipitate located in the superficial portion of the corneal defect was observed in 35 (16.6%) of 210 patients. The onset of the precipitate was within 24 hours to 7 days after starting therapy. In one patient, the precipitate was immediately irrigated out upon its appearance. In 17 patients, resolution of the precipitate was seen in 1 to 8 days (seven within the first 24-72 hours), in five patients, resolution was noted in 10-13 days. In nine patients, exact resolution days were unavailable; however, at follow-up examinations, 18-44 days after onset of the event, complete resolution of the precipitate was noted. In three patients, outcome information was unavailable. The precipitate did not preclude continued use of ciprofloxacin, nor did it adversely affect the clinical course of the ulcer or visual outcome. (SEE ).
Eight mutagenicity tests have been conducted with ciprofloxacin and the test results are listed below:
Salmonella
E. coli
Mouse Lymphoma Cell Forward Mutation Assay (Positive)
Chinese Hamster V Cell HGPRT Test (Negative)
Syrian Hamster Embryo Cell Transformation Assay (Negative)
Saccharomyces cerevisiae
Saccharomyces cerevisiae
Rat Hepatocyte DNA Repair Assay (Positive)
Thus, two of the eight tests were positive, but the results of the following three test systems gave negative results:
Rat Hepatocyte DNA Repair Assay
Micronucleus Test (Mice)
Dominant Lethal Test (Mice)
Long term carcinogenicity studies in mice and rats have been completed. After daily oral dosing for up to two years, there is no evidence that ciprofloxacin had any carcinogenic or tumorigenic effects in these species.
Ciloxan (Ciprofloxacin) Nursing Mothers:
It is not known whether topically applied ciprofloxacin is excreted in human milk; however, it is known that orally administered ciprofloxacin is excreted in the milk of lactating rats and oral ciprofloxacin has been reported in human breast milk after a single 500 mg dose. Caution should be exercised when Ciloxan (Ciprofloxacin) Ophthalmic Solution is administered to a nursing mother.
Ciloxan (Ciprofloxacin) Pediatric Use:
Safety and effectiveness in pediatric patients below the age of 1 year have not been established.
Although ciprofloxacin and other quinolones cause arthropathy in immature animals after oral administration, topical ocular administration of ciprofloxacin to immature animals did not cause any arthropathy and there is no evidence that the ophthalmic dosage form has any effect on the weight bearing joints.
Ciloxan (Ciprofloxacin) Geriatric Use:
No overall differences in safety or effectiveness have been observed between elderly and younger patients.
Ciloxan (Ciprofloxacin) Adverse Reactions
The most frequently reported drug related adverse reaction was local burning or discomfort. In corneal ulcer studies with frequent administration of the drug, white crystalline precipitates were seen in approximately 17% of patients (SEE ). Other reactions occurring in less than 10% of patients included lid margin crusting, crystals/scales, foreign body sensation, itching, conjunctival hyperemia and a bad taste following instillation. Additional events occurring in less than 1% of patients included corneal staining, keratopathy/keratitis, allergic reactions, lid edema, tearing, photophobia, corneal infiltrates, nausea and decreased vision.
Ciloxan (Ciprofloxacin) Overdosage
A topical overdose of Ciloxan (Ciprofloxacin) Ophthalmic Solution may be flushed from the eye(s) with warm tap water.
Ciloxan (Ciprofloxacin) How Supplied
As a sterile ophthalmic solution in Alcon's DROP-TAINER® dispensing system consisting of a natural low density polyethylene bottle and dispensing plug and tan polypropylene closure. Tamper evidence is provided with a shrink band around the closure and neck area of the package.
2.5 mL in 8 mL bottle - 0065-0656-25
5 mL in 8 mL bottle - 0065-0656-05
10 mL in 10 mL bottle - 0065-0656-10
Ciloxan (Ciprofloxacin) Animal Pharmacology
Ciprofloxacin and related drugs have been shown to cause arthropathy in immature animals of most species tested following oral administration. However, a one-month topical ocular study using immature Beagle dogs did not demonstrate any articular lesions.
Revised: March 2006
©2003, 2004, 2006 Alcon, Inc.
Printed in USA
Ciloxan (Ciprofloxacin) Principal Display Panel
NDC 0065-0656-05
(ciprofloxacin HCl
ophthalmic solution)
0.3% as base
