A Comprehensive Pharmacological and Clinical Monograph of Fluorometholone (DB00324)

I. Executive Summary

Fluorometholone is a potent, synthetic, fluorinated corticosteroid primarily utilized in ophthalmology for its robust anti-inflammatory properties. Classified as a small molecule drug, it functions as a high-affinity agonist for the glucocorticoid receptor (GR). Its mechanism of action involves the modulation of gene expression, leading to the synthesis of anti-inflammatory proteins that inhibit the upstream release of arachidonic acid, thereby blocking the production of key inflammatory mediators such as prostaglandins and leukotrienes. This broad-spectrum activity makes it highly effective for treating a wide array of corticosteroid-responsive inflammatory conditions of the anterior segment of the eye, including allergic conjunctivitis, uveitis, keratitis, and post-operative inflammation.

Fluorometholone is available in various topical ophthalmic formulations, including suspensions (0.1% and 0.25%) and an ointment (0.1%), marketed under brand names such as FML®, FML Forte®, and Flarex®. The acetate ester form, fluorometholone acetate, is a more lipophilic prodrug designed for enhanced corneal penetration. Clinically, Fluorometholone is often favored over more potent corticosteroids like dexamethasone due to a comparatively lower propensity to cause a significant elevation in intraocular pressure (IOP). However, its therapeutic efficacy must be carefully balanced against a significant safety profile inherent to all corticosteroids. Prolonged use (10 days or longer) carries a well-documented risk of inducing or exacerbating glaucoma, posterior subcapsular cataract formation, delayed wound healing, and an increased susceptibility to secondary ocular infections. Consequently, its use requires strict medical supervision, including routine monitoring of IOP, and is contraindicated in patients with most viral, fungal, or mycobacterial infections of