Ofloxacin (ophthalmic)
Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief: Adeel Jamil, M.D. [2]
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Overview
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Adult Indications and Dosage
FDA-Labeled Indications and Dosage (Adult)
- Ofloxacin ophthalmic solution is indicated for the treatment of infections caused by susceptible strains of the following bacteria in the conditions listed below:
Off-Label Use and Dosage (Adult)
Guideline-Supported Use
There is limited information regarding Off-Label Guideline-Supported Use of Ofloxacin (ophthalmic) in adult patients.
Non–Guideline-Supported Use
There is limited information regarding Off-Label Non–Guideline-Supported Use of Ofloxacin (ophthalmic) in adult patients.
Pediatric Indications and Dosage
FDA-Labeled Indications and Dosage (Pediatric)
There is limited information regarding Ofloxacin (ophthalmic) FDA-Labeled Indications and Dosage (Pediatric) in the drug label.
Off-Label Use and Dosage (Pediatric)
Guideline-Supported Use
There is limited information regarding Off-Label Guideline-Supported Use of Ofloxacin (ophthalmic) in pediatric patients.
Non–Guideline-Supported Use
There is limited information regarding Off-Label Non–Guideline-Supported Use of Ofloxacin (ophthalmic) in pediatric patients.
Contraindications
- Ofloxacin Ophthalmic Solution is contraindicated in patients with a history of hypersensitivity to ofloxacin, to other quinolones, or to any of the components in this medication.
Warnings
NOT FOR INJECTION.
- Ofloxacin ophthalmic solution should not be injected subconjunctivally, nor should it be introduced directly into the anterior chamber of the eye.
- Serious and occasionally fatal hypersensitivity (anaphylactic) reactions, some following the first dose, have been reported in patients receiving systemic quinolones, including ofloxacin. Some reactions were accompanied by cardiovascular collapse, loss of consciousness, angioedema (including laryngeal, pharyngeal or facial edema), airway obstruction, dyspnea, urticaria, and itching. A rare occurrence of Stevens-Johnson syndrome, which progressed to toxic epidermal necrolysis, has been reported in a patient who was receiving topical ophthalmic ofloxacin. If an allergic reaction to ofloxacin occurs, discontinue the drug. Serious acute hypersensitivity reactions may require immediate emergency treatment. Oxygen and airway management, including intubation should be administered as clinically indicated.
PRECAUTIONS
General:
- As with other anti-infectives, prolonged use may result in overgrowth of nonsusceptible organisms, including fungi. If superinfection occurs discontinue use and institute alternative therapy. Whenever clinical judgement dictates, the patient should be examined with the aid of magnification, such as slit lamp biomicroscopy and, where appropriate, fluorescein staining. Ofloxacin should be discontinued at the first appearance of a skin rash or any other sign of hypersensitivity reaction.
- The systemic administration of quinolones, including ofloxacin, has led to lesions or erosions of the cartilage in weight-bearing joints and other signs of arthropathy in immature animals of various species. Ofloxacin, administered systemically at 10 mg/kg/day in young dogs (equivalent to 110 times the maximum recommended daily adult ophthalmic dose) has been associated with these types of effects.
Adverse Reactions
Clinical Trials Experience
There is limited information regarding Ofloxacin (ophthalmic) Clinical Trials Experience in the drug label.
Postmarketing Experience
There is limited information regarding Ofloxacin (ophthalmic) Postmarketing Experience in the drug label.
Drug Interactions
- Specific drug interaction studies have not been conducted with ofloxacin ophthalmic solution. However, the systemic administration of some quinolones has been shown to elevate plasma concentrations of theophylline, interfere with the metabolism of caffeine, and enhance the effects of the oral anticoagulant warfarin and its derivatives, and has been associated with transient elevations in serum creatinine in patients receiving cyclosporine concomitantly.
Use in Specific Populations
Pregnancy
Pregnancy Category (FDA):
There is no FDA guidance on usage of Ofloxacin (ophthalmic) in women who are pregnant.
Pregnancy Category (AUS):
There is no Australian Drug Evaluation Committee (ADEC) guidance on usage of Ofloxacin (ophthalmic) in women who are pregnant.
Labor and Delivery
There is no FDA guidance on use of Ofloxacin (ophthalmic) during labor and delivery.
Nursing Mothers
There is no FDA guidance on the use of Ofloxacin (ophthalmic) in women who are nursing.
Pediatric Use
There is no FDA guidance on the use of Ofloxacin (ophthalmic) in pediatric settings.
Geriatic Use
There is no FDA guidance on the use of Ofloxacin (ophthalmic) in geriatric settings.
Gender
There is no FDA guidance on the use of Ofloxacin (ophthalmic) with respect to specific gender populations.
Race
There is no FDA guidance on the use of Ofloxacin (ophthalmic) with respect to specific racial populations.
Renal Impairment
There is no FDA guidance on the use of Ofloxacin (ophthalmic) in patients with renal impairment.
Hepatic Impairment
There is no FDA guidance on the use of Ofloxacin (ophthalmic) in patients with hepatic impairment.
Females of Reproductive Potential and Males
There is no FDA guidance on the use of Ofloxacin (ophthalmic) in women of reproductive potentials and males.
Immunocompromised Patients
There is no FDA guidance one the use of Ofloxacin (ophthalmic) in patients who are immunocompromised.
Administration and Monitoring
Administration
- Ophthalmic
Monitoring
There is limited information regarding Ofloxacin (ophthalmic) Monitoring in the drug label.
IV Compatibility
There is limited information regarding the compatibility of Ofloxacin (ophthalmic) and IV administrations.
Overdosage
There is limited information regarding Ofloxacin (ophthalmic) overdosage. If you suspect drug poisoning or overdose, please contact the National Poison Help hotline (1-800-222-1222) immediately.
Pharmacology
There is limited information regarding Ofloxacin (ophthalmic) Pharmacology in the drug label.
Mechanism of Action
There is limited information regarding Ofloxacin (ophthalmic) Mechanism of Action in the drug label.
Structure
- Ofloxacin ophthalmic solution 0.3% is a sterile ophthalmic solution. It is a fluorinated carboxyquinolone anti-infective for topical ophthalmic use.
- Chemical Name: (±)-9-Fluoro-2,3-dihydro-3-methyl-10-(4-methyl-1-piperazinyl)-7-oxo-7H pyrido [1,2,3-de]-1,4 benzoxazine-6-carboxylic acid.
- Contains: Active: ofloxacin 0.3% (3 mg/mL)
- Preservative: benzalkonium chloride (0.005%)
- Inactives: sodium chloride and water for injection. May also contain hydrochloric acid and/or sodium hydroxide to adjust pH.
- Ofloxacin ophthalmic solution is unbuffered and formulated with a pH of 6.4 (range 6.0 to 6.8). It has an osmolality of 300 mOsm/kg. Ofloxacin is a fluorinated 4-quinolone which differs from other fluorinated 4-quinolones in that there is a six member (pyridobenzoxazine) ring from positions 1 to 8 of the basic ring structure.
Pharmacodynamics
Microbiology:
- Ofloxacin has in vitro activity against a broad range of gram-positive and gram-negative aerobic and anaerobic bacteria. Ofloxacin is bactericidal at concentrations equal to or slightly greater than inhibitory concentrations. Ofloxacin is thought to exert a bactericidal effect on susceptible bacterial cells by inhibiting DNA gyrase, an essential bacterial enzyme which is a critical catalyst in the duplication, transcription, and repair of bacterial DNA.
- Cross-resistance has been observed between ofloxacin and other fluoroquinolones. There is generally no cross-resistance between ofloxacin and other classes of antibacterial agents such as beta-lactams or aminoglycosides.
- Ofloxacin has been shown to be active against most strains of the following organisms both in vitro and clinically, in conjunctival and/or corneal ulcer infections as described in the INDICATIONS AND USAGE section.
- The safety and effectiveness of ofloxacin ophthalmic solution in treating ophthalmologic infections due to the following organisms have not been established in adequate and well-controlled clinical trials. Ofloxacin ophthalmic solution has been shown to be active in vitro against most strains of these organisms but the clinical significance in ophthalmologic infections is unknown.
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Pharmacokinetics
- Serum, urine and tear concentrations of ofloxacin were measured in 30 healthy women at various time points during a ten-day course of treatment with ofloxacin ophthalmic solution. The mean serum ofloxacin concentration ranged from 0.4 ng/mL to 1.9 ng/mL. Maximum ofloxacin concentration increased from 1.1 ng/mL on day one to 1.9 ng/mL on day 11 after QID dosing for 10 1/2 days. Maximum serum ofloxacin concentrations after ten days of topical ophthalmic dosing were more than 1000 times lower than those reported after standard oral doses of ofloxacin.
- Tear ofloxacin concentrations ranged from 5.7 to 31 mcg/g during the 40 minute period following the last dose on day 11. Mean tear concentration measured four hours after topical ophthalmic dosing was 9.2 mcg/g.
- Corneal tissue concentrations of 4.4 mcg/mL were observed four hours after beginning topical ocular application of two drops of ofloxacin ophthalmic solution every 30 minutes. Ofloxacin was excreted in the urine primarily unmodified.
Nonclinical Toxicology
Carcinogenesis, Mutagenesis, Impairment of Fertility:
- Long term studies to determine the carcinogenic potential of ofloxacin have not been conducted.
- Ofloxacin was not mutagenic in the Ames test, in vitro and in vivo cytogenic assay, sister chromatid exchange assay (Chinese hamster and human cell lines), unscheduled DNA synthesis (UDS) assay using human fibroblasts, the dominant lethal assay, or mouse micronucleus assay. Ofloxacin was positive in the UDS test using rat hepatocyte, and in the mouse lymphoma assay.
- In fertility studies in rats, ofloxacin did not affect male or female fertility or morphological or reproductive performance at oral dosing up to 360 mg/kg/day (equivalent to 4000 times the maximum recommended daily ophthalmic dose).
Clinical Studies
Conjunctivitis:
- In a randomized, double-masked, multicenter clinical trial, ofloxacin ophthalmic solution was superior to its vehicle after 2 days of treatment in patients with conjunctivitis and positive conjunctival cultures. Clinical outcomes for the trial demonstrated a clinical improvement rate of 86% (54/63) for the ofloxacin treated group versus 72% (48/67) for the placebo treated group after 2 days of therapy. Microbiological outcomes for the same clinical trial demonstrated an eradication rate for causative pathogens of 65% (41/63) for the ofloxacin treated group versus 25% (17/67) for the vehicle treated group after 2 days of therapy. Please note that microbiologic eradication does not always correlate with clinical outcome in anti-infective trials.
- Corneal Ulcers: In a randomized, double-masked, multi-center clinical trial of 140 subjects with positive cultures, ofloxacin ophthalmic solution treated subjects had an overall clinical success rate (complete reepithelialization and no progression of the infiltrate for two consecutive visits) of 82% (61/74) compared to 80% (53/66) for the fortified antibiotic group, consisting of 1.5% tobramycin and 10% cefazolin solutions. The median time to clinical success was 11 days for the ofloxacin treated group and 10 days for the fortified treatment group.
How Supplied
There is limited information regarding Ofloxacin (ophthalmic) How Supplied in the drug label.
Storage
There is limited information regarding Ofloxacin (ophthalmic) Storage in the drug label.
Images
Drug Images
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Package and Label Display Panel
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Patient Counseling Information
- Avoid contaminating the applicator tip with material from the eye, fingers or other source.
- Systemic quinolones, including ofloxacin, have been associated with hypersensitivity reactions, even following a single dose. Discontinue use immediately and contact your physician at the first sign of a rash or allergic reaction.
Precautions with Alcohol
Alcohol-Ofloxacin (ophthalmic) interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.
Brand Names
There is limited information regarding Ofloxacin (ophthalmic) Brand Names in the drug label.
Look-Alike Drug Names
There is limited information regarding Ofloxacin (ophthalmic) Look-Alike Drug Names in the drug label.
Drug Shortage Status
Price
References
The contents of this FDA label are provided by the National Library of Medicine.