Fluorometholone is a topical anti-inflammatory agent for ophthalmic use indicated for the treatment of corticosteroid-responsive inflammation of the palpebral and bulbar conjunctiva, cornea, and anterior segment of the globe. Fluorometholone is a synthetic-fluorinated corticosteroid that is structurally related to progesterone. In clinical studies, fluorometholone demonstrated a significant longer average time to produce a rise in intraocular pressure. Fluorometholone is one of three ophthalmic corticosteroids preferred for long-term treatment because it is less likely to increase intraocular pressure. Fluorometholone was approved by the FDA in July 1982.
General Administration Information
For storage information, see the specific product information within the How Supplied section.
Route-Specific Administration
Ophthalmic Administration
-Administer topically to the eye; do not administer by any other route.
-Wash hands before and after use.
-Tilt head back slightly and pull the lower eyelid down to form a pouch. Try not to touch the tip of the dropper to the eye, fingertips, or any other surface. Squeeze the prescribed number of drops into the pouch. Close the eye gently to spread the drops.
-Administer doses at regular intervals.
-Administer ophthalmic solutions or suspensions prior to applying eye ointments. Allow 5 to 10 minutes between different ocular product applications.
-To prevent infection of the eyes, do not share any eye products or other personal care items with other patients.
Ophthalmic corticosteroids can cause ocular hypertension after 1 to 6 weeks of use. In a small study, the average time to produce an increase in intraocular pressure demonstrated by fluorometholone was significantly longer than dexamethasone; however, the final magnitude of the increase was equivalent for both drugs. Once the medication is discontinued, ocular pressures usually reverse to normal within a few weeks. With long term administration, open-angle glaucoma can occur. Intraocular pressure should be checked frequently during treatment. Other adverse effects include glaucoma with optic nerve damage, visual impairment with acuity and field defects, and posterior subcapsular cataract formation. Following prolonged topical administration (more than two years), other corticosteroids have caused posterior subcapsular cataracts that do not regress when the drug is withdrawn.
Like other corticosteroids, fluorometholone can reduce host resistance to secondary ocular infection (bacterial, fungal and viral); acute purulent infections may be masked or exacerbated. Fungal and viral infections of the cornea are particularly prone to develop coincidentally with long-term applications of steroids. The possibility of fungal invasion should be considered in any persistent corneal ulceration. In diseases that cause thinning of the cornea or sclera, topical steroids have been known to cause perforation. Delayed or impaired wound healing has also been reported.
Ocular irritation, including transient stinging and burning, may occur upon instillation of fluorometholone, especially when using the ointment or the 0.25% suspension. Allergic reactions, ocular inflammation or swelling, rash (unspecified), blurred vision, ocular pain, ocular discharge, increased lacrimation, blepharedema, foreign body sensation, ocular pruritus, conjunctival hyperemia, and blepharitis have all been reported with use.
Corticosteroid-containing preparations have been reported to cause acute anterior uveitis and perforation of the globe. Conjunctivitis, keratoconjunctivitis, corneal ulcers, mydriasis, conjunctival hyperemia, loss of accommodation and ptosis have occasionally been reported following local use of corticosteroids. If any of these reactions occur, ophthalmic fluorometholone should be considered.
Cushing's syndrome and hypothalamic-pituitary-adrenal (HPA) suppression have rarely been reported and may occur after very frequent use of topical ophthalmic steroid use, particularly in very young children. Although systemic effects are uncommon with ophthalmic fluorometholone administration, it should be noted that there have been rare occurrences of systemic hypercorticoidism after use of topical dermatologic steroids applied to the skin. Systemic absorption can be limited by compression of the lacrimal sac on administration of ophthalmic suspensions.
In some instances, given appropriate anti-infective treatment concurrently, ocular corticosteroids can be used to limit serious ocular damage.
Fluorometholone is contraindicated in most viral diseases of the cornea and conjunctiva, including acute superficial herpes simplex virus epithelial keratitis, varicella, and viral infection. Patients with other active herpes infection of the eye (stromal keratitis or uveitis) should not receive fluorometholone unless in conjunction with antiviral therapy. Persons with a history of herpes infections should be prescribed ocular corticosteroids with caution. In addition, the use of ocular corticosteroids may exacerbate the severity of many viral infections of the eye.
Fluorometholone is contraindicated in mycobacterial infection and fungal infection of the eye or ocular structures. Depending on the severity and the use of concurrent anti-infective agents, bacterial infections of the eye may also preclude use of fluorometholone. The use of the ointment may be more prone to retard corneal healing.
Patients who wear contact lenses should be aware that benzalkonium chloride, a preservative in many of the fluorometholone products, can be absorbed by soft contact lenses. Patients wearing soft contact lenses should wait 15 minutes or more before inserting their lenses.
Because fluorometholone has resulted in increased intraocular pressures in some individuals, this drug should be used cautiously in patients with glaucoma. If any patient receives this drug beyond 10 days, intraocular pressure should be monitored. The initial prescription and renewal of the medication order should be made only after examination of the patient with the aid of magnification, such as slit lamp biomicroscopy, and, where appropriate, fluorescein staining. If signs and symptoms fail to improve after 2 days, re-evaluate the patient.
There are no adequate and well-controlled studies of fluorometholone in pregnant women, and it is not known whether fluorometholone can cause fetal harm when administered to a pregnant woman. Fluorometholone should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
It is not known whether topical ophthalmic administration of corticosteroids, including fluorometholone could result in sufficient systemic absorption to produce detectable quantities in breast milk. Systemically-administered corticosteroids appear in breast milk and could suppress growth, interfere with endogenous corticosteroid production, or cause other untoward effects. Because of the potential for serious adverse reactions in breast-fed infants from fluorometholone, a decision should be made whether to discontinue breast-feeding or to discontinue the fluorometholone, taking into account the importance of the drug to the mother. When use of fluorometholone ophthalmic suspension is necessary during breast-feeding, proper lacrimal occlusion after dosage will help limit the risk of maternal systemic absorption.
For the treatment of corticosteroid-responsive ocular inflammation of the palpebral and bulbar conjunctiva, cornea, and anterior segment inflammation of the globe, such as allergic conjunctivitis, dry eye disease*, eyelid acne rosacea, superficial punctate keratitis, iritis, cyclitis, and uveitis:
-for the treatment of corticosteroid-responsive inflammatory ocular conditions of the palpebral and bulbar conjunctiva, cornea, and anterior segment of the globe:
Ophthalmic dosage (Flarex 0.1% ophthalmic suspension):
Adults: 1 to 2 drops in the affected eye(s) 4 times daily; may increase dose to 2 drops in the affected eye(s) every 2 hours for the first 24 to 48 hours. Reevaluate if no improvement after 2 weeks.
Ophthalmic dosage (FML Liquifilm 0.1% or 0.25% ophthalmic suspension):
Adults: 1 drop in the affected eye(s) 2 to 4 times daily; may increase dose to 1 drop in the affected eyes every 4 hours for the first 24 to 48 hours. Reevaluate if no improvement after 2 days. Withdraw treatment by gradually decreasing dose in chronic conditions.
Children and Adolescents 2 to 17 years: 1 drop in the affected eye(s) 2 to 4 times daily; may increase dose to 1 drop in the affected eyes every 4 hours for the first 24 to 48 hours. Reevaluate if no improvement after 2 days. Withdraw treatment by gradually decreasing dose in chronic conditions.
Ophthalmic dosage (0.1% ointment):
Adults: 0.5 inch ribbon in the affected eye(s) 1 to 3 times daily; may increase dose to 0.5 inch ribbon in the affected eye(s) every 4 hours for the first 24 to 48 hours. Reevaluate if no improvement after 2 days. Withdraw treatment by gradually decreasing dose in chronic conditions.
Children and Adolescents 2 to 17 years: 0.5 inch ribbon in the affected eye(s) 1 to 3 times daily; may increase dose to 0.5 inch ribbon in the affected eye(s) every 4 hours for the first 24 to 48 hours. Reevaluate if no improvement after 2 days. Withdraw treatment by gradually decreasing dose in chronic conditions.
-for the treatment of dry eye disease*:
Ophthalmic dosage (0.1% ophthalmic suspension):
Adults: 1 to 2 drops in each eye 4 times daily, initially. Reduce dose to 1 to 2 drops in each eye twice daily after 1 to 2 weeks if positive response in signs and/or symptoms and start cyclosporine, then taper or discontinue steroid therapy after 2 to 4 weeks. Consider extending duration to 4 weeks if no response at 2 weeks, especially in patients with moderate to severe disease.
Maximum Dosage Limits:
Corticosteroid dosage must be individualized and is highly variable depending on the nature and severity of the disease and on patient response. Renewal of fluorometholone prescriptions beyond 20 mL of ophthalmic suspension or 8 grams of ophthalmic ointment should be made by only after re-examination with the aid of magnification.
Patients with Hepatic Impairment Dosing
Specific guidelines for dosage adjustments in hepatic impairment are not available; it appears that no dosage adjustments are needed.
Patients with Renal Impairment Dosing
Specific guidelines for dosage adjustments in renal impairment are not available; it appears that no dosage adjustments are needed.
*non-FDA-approved indication
There are no drug interactions associated with Fluorometholone products.
Ocular topical corticosteroids exert anti-inflammatory activity against inciting agents of mechanical, chemical or immunological nature. There is no generally accepted explanation for the mechanism of action of ocular corticosteroids. However, corticosteroids are thought to act by the induction of phospholipase A2 inhibitory proteins, collectively called lipocortins. These lipocortins are postulated to control the biosynthesis of mediators of inflammation, especially prostaglandins and leukotrienes, by inhibiting the release of the precursor molecule arachidonic acid from membrane phospholipids by phospholipase A2. In ocular medicine, these actions inhibit edema, capillary dilatation, migration of leukocytes, fibrin and collagen deposition, and scar formation associated with inflammation. Ocular application of corticosteroids also results in potentiation of epinephrine vasoconstriction, decreased macrophage movement, and stabilization of lysosomal membranes. Corticosteroids are able to increase intraocular pressures, the degree of which is related to relative potency, concentration, and dosage form pharmacokinetics. Decreases in vascularization and scarring make these agents useful in limiting tissue damage in chemical and thermal exposures.
Fluorometholone is administered topically to the eye. Like most ophthalmic corticosteroids, fluorometholone is absorbed through the aqueous humor, and distributes into the local tissues. Minimal systemic absorption occurs. Fluorometholone has lower systemic penetration activity than other ocular steroids, such as dexamethasone. The low overall doses used in ophthalmic administration usually circumvent the appearance of clinical evidence of systemic absorption. Metabolism of the ocular corticosteroids occurs locally. Ophthalmic ointments will have a lower metabolic clearance rate than solutions or suspensions due to product formulation and contact times.
Affected cytochrome P450 isoenzymes: None