Ciprofloxacin
ciprofloxacin 0.3% · ophthalmic solution
Antibiotic
Approved uses
Bacterial corneal ulcer
2 drops q15min x 6 hours, then q30min for the rest of day 1; 2 drops hourly on day 2; 2 drops q4h on days 3 to 14, extended past day 14 if not re-epithelialized.
Cures as often as fortified tobramycin-cefazolin, with significantly less discomfort.
Bacterial conjunctivitis
1 or 2 drops in the conjunctival sac q2h while awake x 2 days, then 1 or 2 drops q4h while awake x 5 days.
Eradicated bacteria in 90% of children by day 7, on par with tobramycin.
Contraindications
- Hypersensitivity to ciprofloxacin or any other component of this product.
- A history of hypersensitivity to other quinolones may also contraindicate use.
Available FormsOphthalmic solution, 2.5 mL, 5 mL, 10 mL bottles, 0.3% (3 mg ciprofloxacin base per mL)
Mechanism of ActionFluoroquinolone; bactericidal through interference with DNA gyrase, the enzyme needed for synthesis of bacterial DNA, with additional inhibition of topoisomerase IV, the primary quinolone target in susceptible Staphylococcus aureus. Broad gram-negative and gram-positive ocular coverage including Pseudomonas aeruginosa, with peak plasma concentrations under 5 ng/mL on the labeled conjunctivitis schedule.
Warnings & Precautions
- White corneal precipitate: In corneal ulcer studies a white crystalline precipitate formed in the superficial portion of the corneal defect in 35 of 210 patients (16.6%), with onset 24 hours to 7 days after starting therapy; it did not preclude continued use and did not adversely affect the clinical course of the ulcer or the visual outcome.
- Precipitate and re-epithelialization: A prospective multicenter cohort of 624 keratitis patients treated with the 0.3% solution or ointment found precipitate in 15.2%, no significant effect on time to therapeutic improvement (P = 0.09), but a 55% slowing of re-epithelialization (95% confidence limits 32% to 70%), with 3.7 times the risk of deposition at age 70 and older versus under 40 (95% confidence limits 2.6 to 5.0).
- Intraocular injection: Not for injection into the eye.
- Systemic quinolone anaphylaxis: Serious and occasionally fatal hypersensitivity reactions, some after the first dose, have been reported in patients on systemic quinolone therapy, with cardiovascular collapse, loss of consciousness, pharyngeal or facial edema, dyspnea, urticaria and itching; only a few of those patients had any prior history of hypersensitivity reactions.
- Nonsusceptible organism overgrowth: Prolonged use may allow overgrowth of nonsusceptible organisms including fungi; start appropriate therapy if superinfection occurs.
- Hypersensitivity rash: Discontinue at the first appearance of a skin rash or any other sign of hypersensitivity reaction.
- Contact lens wear: Remove lenses before instillation.
Common Side Effects
- Ocular, most frequent: Local burning or discomfort.
- Ocular, about 17% in ulcer studies: White crystalline corneal precipitate under the frequent administration used for corneal ulcers.
- Ocular, under 10%: Lid margin crusting, crystals or scales, foreign body sensation, itching, conjunctival hyperemia.
- Ocular, under 1%: Corneal staining, keratopathy or keratitis, corneal infiltrates, decreased vision, lid edema, tearing, photophobia, allergic reactions.
- Systemic, under 10%: Bad taste following instillation.
- Systemic, under 1%: Nausea.
Pregnancy & LactationPregnancy: Category C. Oral reproduction studies in rats and mice at up to 6 times the usual daily human oral dose showed no impaired fertility and no fetal harm; oral dosing in rabbits at 30 and 100 mg/kg caused gastrointestinal disturbance, maternal weight loss and increased abortion without teratogenicity, and intravenous dosing up to 20 mg/kg produced no maternal toxicity, embryotoxicity or teratogenicity. No adequate and well controlled studies in pregnant women; use only if the potential benefit justifies the potential fetal risk.
Lactation: Excretion of topically applied drug in human milk is unknown; oral dosing is excreted in the milk of lactating rats and has been reported in human breast milk after a single 500 mg dose.
Pediatric UseSafety and effectiveness established in all ages, including neonates.