Difluprednate

• Approved Indications:
• Treatment of inflammation and pain associated with ocular surgery (e.g., cataract surgery)
• Management of endogenous anterior uveitis (inflammation of the anterior chamber of the eye)
• Treatment of inflammatory ocular conditions responsive to corticosteroids (e.g., conjunctivitis, keratitis)
• Off-label Uses:
• Postoperative control of pain and inflammation following various ocular procedures
• Treatment of allergic conjunctivitis or other inflammatory eye disorders under specialist supervision

• Route: Ophthalmic (eye drops)
• Adults and Pediatrics:
• Typical dosage: 1 drop into the affected eye(s) four times daily (every 6 hours)
• Duration varies depending on condition; generally used for up to 2 weeks or as prescribed
• For postoperative inflammation: begin immediately after surgery
• Elderly:
• No specific dose adjustment necessary, monitor for side effects
• Special Populations:
• Use with caution in patients with glaucoma or ocular hypertension
• Avoid use in viral, fungal, or mycobacterial infections of the eye
• Administration Tips:
• Shake well before use
• Avoid touching the dropper tip to the eye or other surfaces to prevent contamination

Difluprednate is a potent corticosteroid prodrug that, upon topical ocular administration, is rapidly converted to its active metabolite, difluoroprednisolone, in ocular tissues. It binds to glucocorticoid receptors in the cytoplasm, modulating gene expression to suppress the inflammatory response. This results in inhibition of multiple inflammatory mediators, including cytokines, prostaglandins, and leukotrienes, leading to reduced vascular permeability, edema, and leukocyte infiltration, thus alleviating inflammation and associated pain in the eye.

• Absorption: Minimal systemic absorption following ocular administration; primarily localized action
• Distribution: Concentrated in ocular tissues (cornea, aqueous humor); negligible plasma levels
• Metabolism: Rapidly converted to active metabolite in ocular tissues
• Half-life: Not well defined systemically due to minimal absorption; ocular activity sustained due to retention in tissues
• Elimination: Metabolites cleared via ocular aqueous outflow and systemic metabolism when absorbed

• Pregnancy:
• FDA Category C — Use only if clearly needed; potential risks cannot be excluded due to lack of well-controlled studies in pregnant women
• Lactation:
• Unknown if excreted in human milk; caution advised
• Breastfeeding women should avoid direct ocular exposure of infants to the medication

• Primary Class: Corticosteroid
• Subclass: Ophthalmic anti-inflammatory corticosteroid

• Known hypersensitivity to difluprednate or any component of the formulation
• Active ocular infections caused by fungi, bacteria, viruses (e.g., herpes simplex keratitis), or mycobacteria
• Untreated glaucoma or ocular hypertension (risk of intraocular pressure elevation)
• Hypersensitivity to other corticosteroids

• Use with caution in patients with glaucoma or increased intraocular pressure; regular monitoring recommended
• Prolonged use may result in cataract formation or secondary ocular infections
• Discontinue if signs of ocular infection develop or worsen
• Avoid abrupt cessation after prolonged therapy to prevent rebound inflammation
• Use cautiously in patients with corneal epithelial defects or history of herpetic eye disease
• Patients should avoid wearing contact lenses during treatment unless advised by a healthcare professional

• Common:
• Ocular burning or stinging upon instillation
• Blurred vision
• Increased intraocular pressure (ocular hypertension)
• Eye redness or irritation
• Serious/Rare:
• Cataract formation with long-term use
• Secondary ocular infections (fungal, bacterial, viral)
• Hypersensitivity reactions including eyelid edema and conjunctival hyperemia
• Glaucoma due to increased intraocular pressure

• No significant systemic drug interactions reported due to minimal systemic absorption
• Caution when used concurrently with other topical ocular drugs that may increase intraocular pressure
• Avoid concomitant use with ocular live vaccines

• Difluprednate has been increasingly recommended for postoperative ocular inflammation due to its potent anti-inflammatory effects and favorable dosing schedule (four times daily) compared to older corticosteroids
• Recent guidelines emphasize close monitoring of intraocular pressure with all corticosteroid eye drops
• New formulations have improved ocular tissue penetration, enhancing efficacy

• Store at room temperature between 20°C and 25°C (68°F to 77°F)
• Protect from light and excessive heat
• Keep bottle tightly closed when not in use
• Do not freeze
• Keep out of reach of children