Fluocinolone: highly potent topical glucocorticoid

Fluocinolone (more precisely fluocinolone acetonide) is a potent synthetic glucocorticoid with two fluorine atoms, used mainly as a topical anti inflammatory in inflammatory skin disease. By European classification it falls into class 3 (potent). A special form is intravitreal implants (Iluvien, Yutiq), which release fluocinolone acetonide continuously and are used in diabetic macular oedema or chronic non infectious uveitis.

Topical fluocinolone is available as cream, ointment, emulsion and solution. The galenical forms are chosen by skin location and condition: ointment for dry, scaly areas, cream for wet areas, solution for hairy areas.

Mechanism of action

Fluocinolone binds intracellular glucocorticoid receptors and modifies the transcription of numerous genes. Main effects:

• Anti inflammatory through inhibition of phospholipase A2, with reduced synthesis of prostaglandins and leukotrienes
• Immunosuppressive through inhibition of T cell and macrophage function
• Antiproliferative in skin, useful in psoriasis and chronic eczema
• Vasoconstriction in skin microcirculation

Potency is about 100 times that of hydrocortisone. Lipophilicity and good skin penetration make fluocinolone an effective topical steroid; they also raise the risk of systemic absorption with extensive or occluded use.

Indications

• Atopic dermatitis (eczema): acute flares
• Psoriasis vulgaris: particularly chronic plaques on areas with thick stratum corneum
• Lichen planus: cutaneous and mucocutaneous
• Allergic and toxic contact dermatitis
• Discoid lupus erythematosus
• Lichen sclerosus et atrophicus
• Diabetic macular oedema (intravitreal Iluvien): chronic and unresponsive to other therapies
• Chronic non infectious uveitis: intravitreal Yutiq

Dosing and administration

Topical: fluocinolone acetonide 0.025 % (or other strengths) applied thinly once or twice daily to affected skin. Treatment as short as possible, depending on site and condition.

On the face and in skin folds: shorter application due to higher risk of atrophy and perioral dermatitis.

In infants and small children: use only with restraint, prefer less potent steroids.

Intravitreal Iluvien: 190 µg implant releasing drug over about 36 months.

Intravitreal Yutiq: 180 µg implant lasting up to 36 months.

Topical therapy not over large areas or under occlusion without medical instruction. Wash hands thoroughly after use unless treating the hands themselves.

Adverse effects

Topical common: skin atrophy, telangiectasia, striae, hypopigmentation, perioral dermatitis, acne, steroid acne, impaired wound healing, local burning.

Topical rare: steroid rebound after abrupt cessation, secondary fungal infections, allergic contact dermatitis to drug or vehicle.

With extensive or occluded use: systemic steroid effects with adrenal suppression, hyperglycaemia, Cushing like symptoms.

Intravitreal: raised intraocular pressure (steroid glaucoma), cataract, intraocular inflammation, vitreous haemorrhage, endophthalmitis.

Important points:

• Use cautiously on the face and in skin folds
• Keep duration as short as possible; in chronic disease use intermittent therapy
• Intravitreal use only in specialised ophthalmology with close post injection follow up
• Steroid glaucoma can cause irreversible damage; monitor IOP regularly

Interactions

With usual topical doses clinically relevant systemic interactions are unlikely.

• Other topical agents: use with time interval
• Systemic CYP3A4 inhibitors (itraconazole, ritonavir): with extensive use and systemic absorption, enhanced steroid effect
• Live vaccines: contraindicated at systemically active doses

Special considerations

Pregnancy: small area topical use acceptable. Avoid extensive or occluded use if possible.

Breastfeeding: when applied to the breast, not directly before nursing.

Children: use highly potent steroids such as fluocinolone with restraint, prefer lower classes. Particular caution in infants and small children.

Duration: in chronic disease use intermittent therapy (e.g. twice weekly maintenance) or switch to less potent steroids or calcineurin inhibitors.

Stopping therapy: taper after longer use to avoid rebound.

Patient communication: steroid phobia is common. Honest information about correct use, sensible duration and possible adverse events reduces fear and supports adherence. It is also important that patients do not stop therapy on their own too early or too late.

Related substances

• Betamethasone, highly potent glucocorticoid
• Betamethasone valerate, mid potency ester
• Prednisolone acetate, ester prodrug for ophthalmic use
• Aflibercept, intravitreal therapy in AMD and DME
• Fluticasone, highly potent inhaled and topical steroid

Frequently asked questions

Sources

• EMA European Medicines Agency
• BfArM German Federal Institute for Drugs and Medical Devices
• AWMF guidelines atopic dermatitis and psoriasis
• Gelbe Liste fluocinolone monograph