FLUOROMETHOLONE
Clinical safety rating: safe
Animal studies have demonstrated safety
Corticosteroid that binds to glucocorticoid receptors, modulating gene expression to induce phospholipase A2 inhibitory proteins, thereby reducing prostaglandin and leukotriene synthesis. Exhibits anti-inflammatory, antipruritic, and vasoconstrictive effects.
| Metabolism | Primarily hepatic; undergoes reduction via 11β-hydroxysteroid dehydrogenase and conjugation. Key enzyme: CYP3A4 (minor). |
| Excretion | Renal (primarily as metabolites): ~70%; Fecal: ~20%; Unchanged in urine: <5% |
| Half-life | Terminal elimination half-life: 1.3–2.2 hours; However, the pharmacodynamic half-life (duration of adrenal suppression) is longer (~24–36 hours) due to receptor-mediated effects. |
| Protein binding | Plasma protein binding: ~90–95% (primarily to albumin and corticosteroid-binding globulin). |
| Volume of Distribution | Apparent volume of distribution: 0.2–0.4 L/kg (low, indicating limited extravascular distribution). |
| Bioavailability | Ophthalmic: Not applicable (local administration); Topical: Minimal systemic absorption (~1–3% through intact skin; higher if damaged). |
| Onset of Action | Ophthalmic: Within 30 minutes; Topical (dermatologic): Within 1–2 hours; Oral: Not applicable (not available orally); Intramuscular: Not applicable. |
| Duration of Action | Ophthalmic: 4–8 hours (single dose); Topical: 6–12 hours; Adrenal suppression can persist for 24–36 hours after single dose. |
1-2 drops of 0.1% suspension in conjunctival sac 2-4 times daily; severe cases: every 4 hours initially, then taper. Ointment: 0.5 inch ribbon 1-3 times daily.
| Dosage form | SUSPENSION/DROPS |
| Renal impairment | No dosage adjustment required for renal impairment. |
| Liver impairment | No dosage adjustment required for hepatic impairment. |
| Pediatric use | Safety and efficacy not established; use same as adult dose per ophthalmologist discretion, caution with extended use. |
| Geriatric use | No specific adjustment; monitor intraocular pressure closely due to increased risk of steroid-induced glaucoma. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
No significant drug interactions May increase intraocular pressure and cause cataract formation with prolonged use.
| Breastfeeding | No data on M/P ratio. Topical use likely low systemic absorption, but systemic corticosteroids appear in milk; caution with prolonged use. |
| Teratogenic Risk | Pregnancy category C. Insufficient human data; corticosteroid studies in animals show increased incidence of cleft palate at high systemic doses. Risk likely low with ophthalmic use due to minimal systemic absorption, but avoid as first-line in first trimester. |
| Fetal Monitoring |
■ FDA Black Box Warning
None.
| Common Effects | Increased intraocular pressure |
| Serious Effects |
["Hypersensitivity to fluorometholone or any component of the formulation","Active epithelial herpes simplex keratitis (dendritic keratitis)","Vaccinia, varicella, and other viral diseases of the cornea and conjunctiva","Fungal diseases of ocular structures","Mycobacterial infections of the eye"]
| Precautions | ["Prolonged use may lead to glaucoma, optic nerve damage, and posterior subcapsular cataract formation","May suppress host immune response, increasing susceptibility to secondary ocular infections","Prolonged use may result in steroid-induced ocular hypertension","Caution in patients with herpes simplex keratitis (risk of corneal perforation)","May mask or exacerbate fungal or viral infections"] |
| Food/Dietary |
Loading safety data…
| No specific monitoring required for short-term ophthalmic use; monitor IOP with prolonged therapy. |
| Fertility Effects | No known effects on fertility from ophthalmic use; animal studies with systemic corticosteroids show impaired fertility at high doses. |
| No known food interactions with ophthalmic fluorometholone. |
| Clinical Pearls | Fluorometholone is a corticosteroid with lower intraocular pressure (IOP) elevation risk compared to dexamethasone or prednisolone. Use with caution in patients with corneal thinning or herpes simplex keratitis. Monitor IOP in long-term therapy. Avoid in epithelial herpes simplex keratitis, vaccinia, varicella, and fungal infections. Shake suspension well before use. |
| Patient Advice | Shake the bottle well before each use. · Do not touch the dropper tip to any surface to avoid contamination. · Remove contact lenses before instillation and wait at least 15 minutes before reinserting. · Do not drive immediately after use if vision is blurred. · Report any vision changes, eye pain, or worsening redness to your doctor. · Use exactly as prescribed; do not stop abruptly. |