Fluocinolone

BRAND NAMES

Fluocinolone is available under several brand names for various formulations, including creams, oils, shampoos, solutions, and intravitreal implants. 

Common brand names include:

• Capex (shampoo)

• Derma-Smoothe/FS (body oil, scalp oil)

• Dermotic (otic oil for the ear canal)

• Flucort (cream, lotion, various combination products)

• Iluvien (intravitreal implant for diabetic macular edema)

• Synalar (cream, ointment, solution)

MECHANISM OF ACTION

Fluocinolone acetonide is a corticosteroid that reduces inflammation by inhibiting edema, fibrin deposition, capillary dilation, leukocyte migration, capillary and fibroblast proliferation, collagen deposition, and scar formation. It has a high binding affinity for the glucocorticoid receptor. Once bound, the receptor-ligand complex moves into the cell nucleus and attaches to glucocorticoid response elements in the promoter regions of target genes. This activates the production of phospholipase A2 inhibitory proteins, known as lipocortins. Specifically, fluocinolone induces annexin 1, a lipocortin that inhibits the release of arachidonic acid, the precursor of inflammatory mediators like prostaglandins and leukotrienes, thereby reducing inflammation.

PHARMACOKINETICS

Absorption

Fluocinolone is primarily administered topically, and only a small portion is absorbed systemically through the skin. The extent of absorption depends on factors such as skin integrity, thickness, and the presence of occlusive dressings.

Distribution

Once absorbed, fluocinolone binds to plasma proteins and distributes throughout the body, though systemic levels are usually low due to its topical use. It can reach target tissues like skin and eyes when applied in appropriate formulations.

Metabolism

Fluocinolone undergoes metabolism mainly in the liver through reduction and hydroxylation reactions. These metabolic processes convert it into inactive metabolites that can no longer exert corticosteroid effects.

Excretion

The drug and its metabolites are primarily excreted via the urine. Small amounts may also be eliminated in feces, depending on the route of administration and systemic absorption.

PHARMACODYNAMICS

Fluocinolone is a synthetic corticosteroid that exerts its pharmacodynamic effects as a corticosteroid hormone receptor agonist, primarily through anti-inflammatory, antipruritic (anti-itching), and vasoconstrictive actions. Its potent effects are mediated via several cellular and molecular mechanisms.

ADMINISTRATION

Fluocinolone is a corticosteroid used topically in multiple formulations—such as cream, ointment, solution, oil, and shampoo—for application on the skin or scalp. It is also available as an intravitreal implant for treating specific eye conditions.

DOSAGE AND STRENGTH

Fluocinolone is available in various topical forms, including creams, ointments, solutions, and oils, typically at concentrations of 0.01% to 0.025%, applied 1–3 times daily depending on the severity of the condition. For scalp disorders, the shampoo formulation (Capex 0.01%) is usually applied 2–3 times per week. For ophthalmic use, the intravitreal implant (Retisert) contains 0.59 mg of fluocinolone acetonide, providing sustained release for up to 36 months to treat chronic non-infectious uveitis. The exact dosage and formulation should always be determined by a healthcare professional based on the patient’s condition.

DRUG INTERACTIONS

Fluocinolone, a topical corticosteroid, primarily has drug interactions when absorbed into the bloodstream, which is typically minimal with proper use. However, systemic absorption can be increased if used over large areas, for prolonged periods, or under occlusive dressings, raising the risk of interactions.

FOOD INTERACTIONS

Fluocinolone, a topical corticosteroid, primarily has drug interactions when absorbed into the bloodstream, which is typically minimal with proper use. However, systemic absorption can be increased if used over large areas, for prolonged periods, or under occlusive dressings, raising the risk of interactions.

CONTRAINDICATIONS

Fluocinolone is contraindicated in patients with a known hypersensitivity to any of its ingredients and should not be applied to areas affected by untreated infections.

SIDE EFFECTS

• Burning, stinging, itching, or dryness of the skin

• Redness or irritation

• Development of acne or pimples

• Changes in skin color, such as lightening or darkening

• Small white or red bumps on the skin

• Rash around the mouth

• Unusual or increased hair growth in the treated area

TOXICITY                                            

Fluocinolone, a potent corticosteroid, can cause toxicity mainly with prolonged use, application over large areas, or use under occlusive dressings, potentially leading to systemic side effects like adrenal suppression and Cushing’s syndrome. Local effects, including skin thinning and irritation, are more commonly observed with topical use.