1. Clinical Overview
Fluorometholone is a synthetic, medium-potency corticosteroid for ophthalmic use. It is a fluorinated derivative of prednisolone, designed to provide potent anti-inflammatory and immunosuppressive effects on the eye while minimizing systemic absorption and side effects. It is particularly valued for its lower propensity to raise intraocular pressure (IOP) compared to other potent steroids like dexamethasone, making it a preferred choice for treating inflammatory conditions in patients with a known or suspected risk of steroid-induced glaucoma. Its 0.1% w/v concentration is the standard strength for topical ocular application.
| Onset | Duration | Bioavailability |
|---|---|---|
| Therapeutic anti-inflammatory effects typically begin within 24 to 48 hours of initiation. | Effects are sustained for the duration of dosing; the drug requires regular application (e.g., 2-4 times daily) to maintain therapeutic levels in the eye. | Negligible systemic bioavailability (<1%) following topical ocular administration due to minimal absorption into the systemic circulation. |
2. Mechanism of Action
Fluorometholone binds to cytoplasmic glucocorticoid receptors, forming a complex that translocates to the nucleus. This complex modulates gene transcription, leading to the synthesis of anti-inflammatory proteins (lipocortins) and inhibition of the production of pro-inflammatory mediators such as prostaglandins, leukotrienes, histamine, and cytokines (IL-1, IL-2, TNF-α). It also stabilizes lysosomal membranes and inhibits the migration of polymorphonuclear leukocytes and macrophages to the site of inflammation.
3. Indications & Uses
- Treatment of steroid-responsive inflammatory conditions of the palpebral and bulbar conjunctiva, cornea, and anterior segment of the globe (e.g., allergic conjunctivitis, vernal keratoconjunctivitis, episcleritis, non-infectious anterior uveitis).
- Post-operative inflammation following ophthalmic surgery (e.g., cataract surgery).
4. Dosage & Administration
Adult Dosage: Instill 1 to 2 drops into the conjunctival sac of the affected eye(s) every 4 to 6 hours (typically 2 to 4 times daily). In severe inflammation, dosing may be initiated every 1 to 2 hours during the first 24-48 hours, then tapered.
Administration: 1. Wash hands. 2. Tilt head back. 3. Gently pull lower eyelid down to form a pouch. 4. Instill prescribed drops without touching the dropper tip to eye, eyelid, or any surface. 5. Close eyes gently for 1-2 minutes and apply gentle pressure to the nasolacrimal duct (inner corner of eye) to minimize systemic absorption. 6. Wait at least 5-10 minutes before instilling any other eye drops.
5. Side Effects
Common side effects may include:
- Transient burning or stinging upon instillation.
- Blurred vision temporarily after application.
- Mild ocular irritation or itching.
- Watery eyes (epiphora).
6. Drug Interactions
| Drug | Effect | Severity |
|---|---|---|
| Other Ocular Corticosteroids | Additive risk of IOP elevation, cataract, and infection. | Major |
| Ocular NSAIDs (e.g., Ketorolac, Nepafenac) | May increase risk of corneal healing complications. Use combination with caution post-surgery. | Moderate |
| Ocular Cholinergic Agents (e.g., Pilocarpine) | Theoretical increased inflammation; clinical significance is low. | Minor |
| Systemic CYP3A4 Inducers (e.g., Rifampicin, Phenytoin, Carbamazepine) | May theoretically increase metabolism if systemically absorbed, reducing efficacy. Not clinically significant for topical use. | Minor |
7. Patient Counselling
- DO wash hands before use.
- DO apply gentle pressure on the inner corner of the eye for 1 minute after instillation.
- DO wait at least 5-10 minutes before using other eye drops.
- DO NOT touch the dropper tip to any surface to avoid contamination.
- DO NOT wear contact lenses while using this medication or if you have an active eye infection/inflammation.
- DO NOT discontinue abruptly if used for more than 10 days; taper as directed by your doctor.
- DO NOT share your eye drops with others.
8. Toxicology & Storage
Overdose: Topical ocular overdose is unlikely to cause acute systemic toxicity. Symptoms would be local: severe ocular irritation, pain, increased IOP, corneal edema. Accidental oral ingestion may cause systemic corticosteroid effects (hyperglycemia, fluid retention).
Storage: Store at controlled room temperature (15°C to 25°C). Protect from light. Keep the bottle tightly closed when not in use. Do not freeze. Keep out of reach of children. Discard the bottle 4 weeks after opening to prevent microbial contamination. Do not use if the solution is discolored or contains particles.