Fluorometholone Acetate

Approved Indications:

• Ocular Inflammation: Treatment of inflammation of the palpebral and bulbar conjunctiva, cornea, and anterior segment of the globe due to infection, trauma, allergy, or surgery, where corticosteroid use is appropriate.
• Postoperative Ocular Inflammation: Control of inflammation and pain following ocular surgeries such as cataract extraction, LASIK, or glaucoma filtering procedures.
• Allergic Conjunctivitis (Severe): Used when standard antihistamines or mast cell stabilizers are insufficient to control severe symptoms.
• Anterior Uveitis (Mild to Moderate): As adjunct therapy to control inflammation.

Clinically Accepted Off-label Uses:

• Keratitis (Non-infectious): Used in specific non-infectious keratitis cases under ophthalmologist supervision.
• Episcleritis: Used occasionally in refractory cases not responding to NSAIDs.

Adults:

• Initial Dose: 1 drop in the affected eye(s) 2 to 4 times daily.
• In severe inflammation: Up to 1 drop every 2 hours, tapering once response is observed.
• Tapering: Reduce frequency gradually to prevent rebound inflammation.

Pediatrics (≥2 years):

• Use is generally considered safe for short durations (typically 1 drop 2–3 times daily). Must be supervised by an ophthalmologist.

Elderly:

• Same dosing as adults. Monitor closely for intraocular pressure elevation and cataract formation.

Renal/Hepatic Impairment:

• No specific adjustments needed due to minimal systemic absorption. Use caution in patients with impaired clearance.

Route of Administration:

• Ophthalmic (topical instillation) only.

Duration:

• Short-term use only, typically not exceeding 2 weeks unless under close monitoring. Prolonged use increases risk of ocular complications.

Special Instructions:

• Shake well before each use.
• Contact lenses should be removed before instillation and reinserted after 15 minutes.
• Avoid touching dropper tip to any surface.

Fluorometholone Acetate is a synthetic corticosteroid that penetrates ocular tissues to bind intracellular glucocorticoid receptors. This binding modifies gene expression, leading to inhibition of pro-inflammatory cytokines, prostaglandins, leukotrienes, and other mediators involved in the inflammatory cascade. It reduces edema, fibrin deposition, capillary dilation, leukocyte migration, and fibroblast proliferation. Compared to fluorometholone alcohol, the acetate form has improved lipophilicity, resulting in enhanced intraocular penetration and stronger anti-inflammatory activity, especially in the anterior chamber.

• Absorption: Minimal systemic absorption after topical application; localized absorption into the cornea, aqueous humor, and conjunctiva.
• Distribution: Primarily distributed in ocular tissues. Plasma concentrations are negligible with standard dosing.
• Metabolism: Metabolized locally within ocular tissues; minimal hepatic metabolism if absorbed systemically.
• Bioavailability: Enhanced intraocular bioavailability due to the acetate ester form.
• Half-life: Not systemically defined; intraocular duration approximately 4–6 hours.
• Elimination: Metabolites excreted primarily in bile and urine.

Pregnancy:

• FDA Category: Category C (use only if clearly needed).
• Risk Summary: Animal studies show potential fetal harm; no adequate human studies. Use only if potential benefit outweighs fetal risks.

Lactation:

• Unknown if excreted in breast milk after ophthalmic use.
• Systemic absorption is minimal, but caution is advised during breastfeeding.
• Recommendation: Apply nasolacrimal occlusion for 1–2 minutes to minimize systemic exposure if used during lactation.

• Primary Class: Ophthalmic Corticosteroid
• Subclass: Low-to-Moderate Potency Glucocorticoid
• Form: Fluorinated acetate ester for enhanced ocular penetration

• Known hypersensitivity to fluorometholone acetate or any component of the formulation.
• Active or suspected ocular viral infections, especially herpes simplex keratitis (dendritic).
• Fungal eye infections.
• Acute purulent untreated bacterial eye infections.
• Mycobacterial ocular infections (e.g., tuberculosis of the eye).
• Use in patients with untreated glaucoma or elevated intraocular pressure without proper monitoring.

• Elevated Intraocular Pressure: Prolonged use may cause steroid-induced glaucoma and optic nerve damage. Monitor IOP frequently.
• Cataract Formation: Risk of posterior subcapsular cataract increases with extended therapy.
• Infections: May mask signs of ocular infection or worsen pre-existing infections.
• Delayed Wound Healing: May slow corneal epithelial regeneration after surgery or injury.
• Herpes Simplex History: Use with extreme caution due to risk of corneal perforation.
• Use in Children: May cause systemic corticosteroid effects such as growth suppression if absorbed; monitor closely.

Common Side Effects (Ocular):

• Transient burning or stinging upon instillation
• Blurred vision
• Eye irritation or foreign body sensation
• Increased tearing

Less Common:

• Eyelid swelling
• Conjunctival hyperemia
• Dry eyes

Serious Adverse Effects:

• Elevated intraocular pressure → potential glaucoma
• Posterior subcapsular cataract
• Secondary ocular infections (e.g., fungal keratitis, bacterial superinfection)
• Corneal thinning or perforation with prolonged use

Timing & Dose Dependence:

• Mild side effects occur immediately post-instillation.
• Serious side effects generally arise with long-term (>2 weeks) or frequent dosing.

• NSAIDs (topical): May delay corneal healing when combined with corticosteroids.
• Ocular Antivirals or Antibacterials: Use in conjunction may be necessary to prevent masking of infection.
• Systemic Steroids: Combined systemic and topical steroid use increases the risk of systemic and ocular side effects.
• CYP450 Enzymes: Not significantly involved due to minimal systemic absorption.

Food & Alcohol Interactions: Not applicable for ophthalmic use.

• Labeling Update: Revised warnings now emphasize the need for frequent intraocular pressure monitoring for all patients using beyond 10 days.
• Formulary Changes: Some regional formularies have listed Fluorometholone Acetate as a preferred corticosteroid for anterior uveitis due to higher ocular penetration compared to the alcohol form.
• Guidance on Duration: Ophthalmology associations recommend use for ≤2 weeks unless monitored, due to risks of IOP elevation and secondary infection.

• Temperature: Store at 15°C to 25°C (59°F to 77°F).
• Light Sensitivity: Protect from direct sunlight.
• Humidity: Keep the container tightly closed to avoid moisture contamination.
• Freezing: Do not freeze.
• Shake Well before each use to ensure uniform suspension.
• Discard after 28 days of opening the bottle, even if product remains.