FLAREX OPHTHALMIC SUSPENSION

Indications

• Local treatment of inflammatory eye conditions
• Short-term management of eye inflammation

Dosage

Children: For children aged 2–17 years, apply every 1 hour for 24–48 hours, then reduce to 2–4 times a day as needed.

Adults: Apply every 1 hour for 24–48 hours, then reduce to 2–4 times a day as needed.

Mechanism of action

Fluorometholone acts by inducing phospholipase A2 inhibitory proteins known as lipocortins, which control the biosynthesis of inflammatory mediators like prostaglandins and leukotrienes. These proteins inhibit the release of arachidonic acid from membrane phospholipids. The drug binds to cytosolic glucocorticoid receptors, forming a receptor-ligand complex that translocates into the nucleus to bind glucocorticoid response elements in target genes, leading to modulation of gene expression related to inflammation.

Pharmacodynamics

Fluorometholone inhibits the inflammatory response, affecting various processes such as edema, fibrin deposition, capillary dilation, leukocyte migration, capillary proliferation, fibroblast proliferation, collagen deposition, and scar formation. This broad anti-inflammatory action helps in managing symptoms associated with ocular inflammation.

Pharmacokinetics

Fluorometholone is primarily administered topically as eye drops, which allows for localized action with limited systemic absorption. The pharmacokinetics of the drug in the eye involve rapid penetration into ocular tissues, with peak concentrations occurring shortly after administration. Due to its formulation, it is designed to minimize systemic exposure and side effects.

Adverse effects

• Eye discomfort
• Stinging
• Altered taste
• Visual impairment
• Cataract
• Eye disorders

Precautions

• Risk of central serous chorioretinopathy with local and systemic administration
• Consider the potential for increased intraocular pressure with prolonged use

Pregnancy

Fluorometholone should be used in pregnancy only if the potential benefit justifies the potential risk to the fetus. Consultation with a healthcare provider is recommended.

Breast-feeding

There is no specific information on the excretion of fluorometholone in human milk. Caution should be exercised when administering to breastfeeding women.

Storage

Store in a cool, dry place, away from light. Keep out of reach of children.

Formulations

• Fluorometholone 0.1% eye drops (FML Liquifilm) - 5 ml or 10 ml bottles

Mechanism of action

There is no generally accepted explanation for the mechanism of action of ocular corticosteroids. However, corticosteroids are thought to act by the induction of phospholipase A2 inhibitory proteins, collectively called lipocortins. It is postulated that these proteins control the biosynthesis of potent mediators of inflammation such as prostaglandins and leukotrienes by inhibiting the release of their common precursor, arachidonic acid. Arachidonic acid is released from membrane phospholipids by phospholipase A2. Their primary target is the cytosolic glucocorticoid receptor. After binding the receptor the newly formed receptor-ligand complex translocates itself into the cell nucleus, where it binds to many glucocorticoid response elements (GRE) in the promoter region of the target genes. The DNA bound receptor then interacts with basic transcription factors, causing the increase in expression of specific target genes.

Pharmacodynamics

Corticosteroids such as fluorometholone inhibit the inflammatory response to a variety of inciting agents and probably delay or slow healing. They inhibit the edema, fibrin deposition, capillary dilation, leukocyte migration, capillary proliferation, fibroblast proliferation, deposition of collagen, and scar formation associated with inflammation.