Ciloxan (Ciprofloxacin)

CILOXAN®

Alcon

Ciprofloxacin HCl

Antibacterial Agent

Action And Clinical Pharmacology: The bactericidal action of ciprofloxacin results from inhibition of the enzyme, DNA gyrase, which is required for the synthesis of bacterial DNA.

Pharmacokinetics: Topically applied ciprofloxacin ophthalmic solution is absorbed systemically with ciprofloxacin plasma concentrations approaching steady state at the end of dosing each day. Ciprofloxacin plasma concentrations following a routine ophthalmic treatment regimen were in the range of nonquantifiable to 4.7 ng/mL with the majority of levels falling between 1.5 to 2.5 ng/mL. Maximum serum concentration following a single oral administration of a 250 mg ciprofloxacin tablet is about 1 200 ng/mL.

Indications And Clinical Uses: Ointment: For the treatment of the following infections of the eye and its adnexae when caused by susceptible strains of the designated bacteria.

Corneal Ulcers: P. aeruginosa, S. aureus, S. epidermidis.

Conjunctivitis: S. aureus, S. epidermidis, Streptococcus (Viridans group), S. pneumoniae, H. influenzae.

Solution: For the treatment of the following infections of the eye and its adnexae when caused by susceptible strains of the designated bacteria.

Corneal Ulcers: P. aeruginosa, S. aureus, S. epidermidis, S. pneumoniae.

Conjunctivitis: S. aureus, S. epidermidis, Streptococcus (Viridans group), S. pneumoniae, H. influenzae.

Contra-Indications: A history of hypersensitivity to ciprofloxacin, other quinolones including nalidixic acid, or any other component of the medication.

Manufacturers’ Warnings In Clinical States: Not for injection into the eye.

Precautions: General: Prolonged use of ciprofloxacin ophthalmic solution or ointment 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.

Anaphylactic reactions following the first dose, have been reported in patients receiving therapy with quinolones by systemic administration. 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 reaction. Anaphylactic reactions may require epinephrine and other emergency measures. Ciprofloxacin should be discontinued at the first sign of hypersensitivity or allergy and the patient monitored until the risk of anaphylaxis is no longer present. Severe hypersensitivity reactions characterized by rash, fever, eosinophilia, jaundice and hepatic necrosis with fatal outcome have been reported rarely (less than 1 per million prescriptions) in patients receiving systemically administered ciprofloxacin along with other drugs. One report exists of anaphylaxis in a patient treated with topical ciprofloxacin concomitantly with several other antibiotics and medications. The possibility that these reactions were related to ciprofloxacin cannot be excluded. 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 29 (18.8%) out of 154 patients administered ciprofloxacin ophthalmic solution and in 32 (12.6%) of 253 patients administered ciprofloxacin ophthalmic ointment. The onset of the precipitate was within 24 hours to 7 days (solution) and 13 days (ointment) after starting therapy. In 16 patients administered ciprofloxacin ophthalmic solution, resolution of the precipitate was seen in 1 to 8 days (7 within the first 24 to 72 hours), in 4 patients, resolution was noted in 10 to 13 days. In 1 patient, the precipitate was immediately irrigated out upon its appearance.

In 6 patients, exact resolution days were unavailable, however, at follow-up examinations 18 to 44 days after onset of the event, complete resolution of the precipitate was noted. In 2 patients, outcome information was unavailable. The presence of the white precipitate did not preclude continued use of ciprofloxacin ophthalmic solution or ointment, nor did it adversely affect the clinical course of the ulcer or visual outcome. A literature report exists of a single case of ciprofloxacin-associated dense precipitate apparently interfering with re-epithelialization.

Dosage regimens involving both solution and ointment formulations of ciprofloxacin 0.3% have not been studied. A controlled study of the efficacy and safety of ciprofloxacin ointment versus ciprofloxacin solution 0.3% has not been conducted.

In patients with large (>4 mm) and/or deep stromal ulcers, the clinical success rate was lower for both ciprofloxacin and standard (fortified antibiotics) therapy.

Drug Interactions: Specific drug interaction studies have not been conducted with ciprofloxacin ophthalmic solution or ointment. However, the systemic administration of some quinolones has been shown to elevate plasma concentrations of theophylline, interfere with the metabolism of caffeine, enhance the effects of oral coagulant, warfarin and its derivatives, and has been associated with transient elevations in serum creatinine in patients receiving cyclosporine concomitantly.

Pregnancy: There are no adequate and well controlled studies of ciprofloxacin ophthalmic solution or ointment in pregnant women. This drug should be used in pregnant women only if in the physician’s opinion, the benefit clearly outweighs any potential unknown risks.

Reproduction studies have been performed in rats and mice at doses up to 6 times the usual daily human dose and have revealed no evidence of impaired fertility or harm to the fetus due to ciprofloxacin. In rabbits, as with most antimicrobial agents, ciprofloxacin (30 and 100 mg/kg orally) produced gastrointestinal disturbances resulting in maternal weight loss and an increased incidence of abortion. No teratogenicity was observed at either dose. After i.v. administration in rabbits, at doses up to 20 mg/kg, no maternal toxicity was produced and no embryotoxicity or teratogenicity was observed.

Lactation: It is not known whether topically applied ciprofloxacin ophthalmic solution or ointment is excreted in human milk, however, it is known that orally administered ciprofloxacin is excreted in milk of lactating rats and that other drugs of this class are excreted in human milk. For this reason, and because of the potential for serious adverse reactions from ciprofloxacin in nursing infants, a decision should be made to discontinue nursing or to discontinue the drug, taking into consideration the importance of the drug to the mother.

Children: Safety and efficacy of ciprofloxacin ophthalmic solution or ointment in children less than 1 year of age have not been demonstrated. Ciprofloxacin ophthalmic solution has been used in 123 children between the ages of 1 and 12 years and ciprofloxacin ophthalmic ointment has been used in 182 children between the ages of 1 and 12 years. No serious adverse event was reported in these patients.

Ciprofloxacin and quinolone-related drugs have been shown to cause arthropathy in immature animals of most species tested following oral administration. Topical ocular administration of ciprofloxacin to immature animals (Beagle dogs) did not cause arthropathy or demonstrate any articular lesions and there is no evidence that the ophthalmic dosage form has any effect on the weight bearing joints.

In 634 children treated orally with ciprofloxacin, clinical and radiologic monitoring did not reveal any skeletal toxicity felt to be quinolone-related. However, there are a small number of reports of arthralgia in children, associated with oral ciprofloxacin therapy. This arthralgia has been shown to be reversible on discontinuation of the systemic medication.

Adverse Reactions: During clinical studies, treatment related adverse events to ciprofloxacin ophthalmic solution and ointment were mild, infrequent in occurrence and nonserious in nature, and did not lead to premature discontinuation of therapy. The most frequently reported adverse events that were considered related or possibly related to ciprofloxacin ophthalmic solution were: transient discomfort, i.e., stinging, burning, irritation (8.6%), noticeable taste (4.5%), foreign body sensation (1.8%), and itching (1.2%). Treatment-related or possibly related medical events occurring between 0.5 and 1% incidence were: lid margin crusting, crystals/scales, erythema/redness, dryness, discharge, corneal staining, keratopathy/keratitis, hyperemia/congestion and tearing.

In clinical trials in which 154 patients were treated for bacterial corneal ulcers, the most frequently reported adverse event related or possibly related to therapy was a white crystalline precipitate seen in 29 (18.8%) patients. The precipitate required no adjunctive therapy and resolved spontaneously with continued ciprofloxacin use.

Other rarely reported events related or possibly related to ciprofloxacin ophthalmic solution included: ocular congestion, photophobia, pain, vision decrease, chemosis, corneal infiltrate, inflammation, blurred vision, corneal toxicity, allergy, intolerance, lid edema, heavy sensation, swelling, conjunctival reaction, numbing sensation, conjunctivitis, punctate epithelial erosion, and worsened infiltrate and headache.

The most commonly reported drug adverse reactions in patients with conjunctivitis treated with ciprofloxacin ophthalmic ointment were discomfort (1.3%), pruritus (1.3%), and hyperemia (1.3%), and in patients with corneal ulcers were white precipitate (12.6%), discomfort (2.0%), and blurred vision (1.2%). Other reactions associated with ciprofloxacin ophthalmic ointment occurring in less than 1.0% of patients included hyperemia, pruritus, eye pain, tearing, photophobia, allergic reactions, dry eye, decreased visual acuity, lid erythema, corneal staining, keratoconjunctivitis, keratopathy, corneal lesion, epitheliopathy, ocular edema, irritation, foreign body sensation, nausea, dermatitis and metallic taste.

Symptoms And Treatment Of Overdose: Symptoms and Treatment: A topical overdosage of ciprofloxacin is considered to be a remote possibility. Discontinue medication when heavy or protracted use is suspected. A topical overdosage may be flushed from the eye(s) with warm tap water.

Dosage And Administration: Ointment: Conjunctivitis: Adults and Children (above the age of 1 year): Apply a 1.25 cm ribbon of ophthalmic ointment into the conjunctival sac 3 times a day on the first 2 days and then apply a 1.25 cm ribbon 2 times a day for the next 5 days.

Corneal ulcer: Adults and Children (above the age of 12 years): Apply a 1.25 cm ribbon of ophthalmic ointment into the conjunctival sac every 1 to 2 hours around the clock on the first 2 days, then apply a 1.25 cm ribbon every 4 hours for up to 12 days. If corneal re-epithelialization has not occurred after 12 days, the continuation of the dosing regimen is at the discretion of the attending physician.

Special Instructions: Patients should be advised to avoid contamination of the dispensing tip. As with other ophthalmic ointments, transient blurred vision may be experienced with the use of ciprofloxacin ointment.

Solution: Conjunctivitis: Adults and Children (above the age of 1 year): Instill 1 or 2 drops of ophthalmic solution into the conjunctival sac(s) every 2 hours while awake for 2 days and then 2 drops every 4 hours while awake for 5 days.

Corneal Ulcer: Adults and Children (above the age of 12 years): Instill 2 drops of ophthalmic solution into the affected eye every 15 minutes for the first 6 hours and then 2 drops into the affected eye every 30 minutes for the remainder of the first day. On the second day, instill 2 drops in the affected eye hourly. On the third through the fourteenth day, place 2 drops in the affected eye every 4 hours. If corneal re-epithelialization has not occurred after 14 days, the continuation of the dosing regimen is at the discretion of the attending physician.

Special Instructions: Patients should be advised to avoid contamination of the dispensing tip.

Availability And Storage: Ointment: Each g of ophthalmic ointment contains: ciprofloxacin HCl 3.5 mg equivalent to 3 mg base. Nonmedicinal ingredients: mineral oil and white petrolatum. Metal ophthalmic ointment tubes of 3.5 g.

Solution: Each mL of ophthalmic solution contains: ciprofloxacin HCl 3.5 mg equivalent to ciprofloxacin base 3 mg. Also contains benzalkonium chloride 0.006% as preservative. Nonmedicinal ingredients: acetic acid, edetate disodium, hydrochloric acid and/or sodium hydroxide, mannitol, purified water, and sodium acetate. Plastic Drop-Tainer dispensers of 5 and 10 mL.

Store in the carton at room temperature (2 to 30°C).

CILOXAN® Alcon Ciprofloxacin HCl Antibacterial Agent

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