Fluocinolone Acetonide/Fluocinolone is a synthetic glucocorticoid with anti-inflammatory and antipruritic activities. Fluocinolone binds the glucocorticoid receptor, followed by translocation of the ligand-receptor complex to the nucleus and transcription activation of genes containing glucocorticoid-responsive elements. Lipocortin-1 is one factor induced by fluocinolone that interacts with and inhibits cytosolic phospholipase 2 alpha, thereby preventing phospholipase translocation to the perinuclear membrane and subsequent release and conversion of arachidonic acid to inflammatory prostaglandins. In addition, MAPK phosphatase 1 is induced, thereby preventing the triggering of the MAPK cascade resulting in pro-inflammatory effects via Jun N-terminal kinase and c-Jun. Finally, fluocinolone binds to and inhibits nuclear factor.
Fluocinolone Acetonide is the acetonide salt form of fluocinolone, a synthetic fluorinated corticosteroid with anti-inflammatory, antipruritic and vasoconstrictive properties. Fluocinolone is a glucocorticoid receptor agonist that binds to cytoplasmic glucocorticoid receptors and subsequently translocates to the nucleus where it initiates the transcription of glucocorticoid-responsive genes such as lipocortins. Lipocortins inhibit phospholipase A2, thereby blocking the release of arachidonic acid from membrane phospholipids and preventing the synthesis of prostaglandins and leukotrienes, both are potent mediators of inflammation. Fluocinolone exerts its vasoconstrictive effect through inhibition of nitric oxide synthase, thereby blocking nitric oxide production and effectively diminishing the effect of nitric oxide on vascular smooth muscles leading to reduced blood flow.
Mechanism of Action of Fluocinolone
Fluocinolone acetonide is a corticosteroid and thus, it can be inferred that it acts by inhibiting the edema, fibrin deposition, capillary dilation, leukocyte migration, capillary proliferation, fibroblast proliferation, collagen deposition, and scar formation. Some reports have indicated that fluocinolone acetonide presents a high binding affinity for the 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 in the promoter region of the target genes. This effect promotes the induction of phospholipase A2 inhibitory proteins (lipocortins). Through this mechanism of action, it is thought that fluocinolone induces mainly one of the lipocortins, annexin 1, which will later mediate the synthesis of inflammatory mediators such as prostaglandins and leukotrienes by inhibiting the release of arachidonic acid which is the precursor of all these inflammatory mediators. Hence, the induction of these proteins will prevent the release of arachidonic acid by phospholipase A2.
Indications of Fluocinolone
A glucocorticoid derivative used topically in the treatment of various skin disorders. It is usually employed as a cream, gel, lotion, or ointment. It has also been used topically in the treatment of inflammatory eye, ear, and nose disorders.
- Fluocinolone acetonide has been used extensively in different medical areas. -In dermatology, it is extensively used for the relief of inflammatory dermatosis, dermatitis, psoriasis, hypertrophic tissues, keloid tissues, and atopic dermatitis.
- It has been used in shampoo products as a low to medium potency corticosteroid for the treatment of seborrheic dermatitis of the scalp. In-ear drops, it is used as a low to medium potency corticosteroid for the treatment of chronic eczematous external otitis in adults and pediatric patients 2 years and older.
- As an intravitreal implant, it is indicated for the treatment of diabetic macular edema with patients that have been previously treated with a course of corticosteroids and no clinically significant rise in intraocular pressure.
- Fluocinolone acetonide was announced on October 15, 2018, to be FDA approved for the treatment of chronic non-infectious uveitis affecting the posterior segment of the eye. Some reports have indicated the use of fluocinolone acetonide as a vasoprotective agent and for its use in the treatment of first-degree hemorrhoids.
- Treatment of non-infectious uveitis
- Fluocinolone has been used in trials studying the treatment and prevention of Candida Infection, Oral Lichen Planus, Macular Degeneration, and Choroidal Neovascularization.
- Diabetic Macular Edema (DME)
- Non-infectious Posterior Uveitis Chronic Uveitis
- Psoriasis of the scalp
- Seborrheic dermatitis of the scalp
- Uveitis
- Chronic eczematous otitis externa
- Eczema
- Seborrheic Dermatitis
- Atopic Dermatitis
- Dermatitis
- Lichen Sclerosus
- Psoriasis
Contraindications of Fluocinolone
- untreated tuberculosis
- inactive tuberculosis
- herpes simplex infection of the eye
- a herpes simplex infection
- intestinal infection caused by the roundworm Strongyloides
- a condition with low thyroid hormone levels
- diabetes
- insufficiency of the hypothalamus and pituitary gland
- high cholesterol
- low amount of potassium in the blood
- a reduction in the body’s resistance to infection
- psychotic disorder
- brain injury
- a disease with shrinking and weaker muscles called myopathy
- increased pressure in the eye
- wide-angle glaucoma
- clouding of the lens of the eye called cataracts
- sudden blindness and pain upon moving the eye
- high blood pressure
- chronic heart failure
- an ulcer from too much stomach acid
- a type of stomach irritation called gastritis
- diverticulitis
- the surgical joining of two parts of the intestine
- hardening of the liver
- rupture of a tendon
- osteoporosis
- a condition of weak bones
- decreased calcification or density of bone
- seizures
- visible water retention
- Inherited Deficiency of Arginosuccinate Lyase
- inherited carbamoyl phosphate synthetase deficiency
- Citrullinemia
- Infection caused by the Varicella Zoster Virus
- Measles
- Ornithine Carbamoyltransferase Deficiency
- Arginase Deficiency
- Exposure to the Measles
- Exposure to the Chickenpox
- muscle pain or tenderness with increase creatine kinase
- broken bone due to disease or illness
- osteonecrosis
- the death of bone tissue due to a lack of blood supply
- Malaria Affecting the Brain
- Muscle Wasting
- hyperammonemia associated with N-acetyl glutamate synthase deficiency
- Untreated Systemic Fungal Infection
Do not use fluocinolone acetonide if you
- are allergic fluocinolone acetonide or any ingredients of this medication
- are allergic to peanuts
- have skin infections caused by viruses, including herpes simplex, vaccinia, and varicella (chickenpox)
- have tuberculous skin lesions
- have untreated infected skin lesions caused by an infection with fungi or bacteria
Dosage of Fluocinolone
Strengths: 0.01%; 0.025%; 0.2%
Seborrheic Dermatitis
- No more than one ounce of the shampoo should be applied to the scalp area once a day, worked into a lather and allowed to remain on the scalp for approximately 5 minutes
Psoriasis
- Apply a thin film on the scalp, massage well and cover scalp with the supplied shower cap.
Dermatitis
- Apply a thin film to the affected area two to four times a day
Eczema
- Apply a thin film to the affected area two to four times a day
Atopic Dermatitis
- Topical (body) oil: Apply a thin film to the affected areas three times a day
Pediatric Dose
Atopic Dermatitis
3 months and older
- Topical (scalp and body) oil: Apply to the affected area twice a day for up to 4 weeks
Seborrheic Dermatitis
- No more than one ounce of the shampoo should be applied to the scalp area once a day, worked into a lather and allowed to remain on the scalp for approximately 5 minutes
Dermatitis
- Apply a thin film to the affected area two to four times a day
Eczema
- Apply a thin film to the affected area two to four times a day
Side Effects of Fluocinolone
Most Common
- burning, dryness, irritation, itching, or redness of the skin (usually mild and temporary)
- increased redness or scaling of skin sores (usually mild and temporary)
- skin rash (usually mild and temporary)
- Body aches or pain
- congestion
- cough
- dryness or soreness of the throat
- fever
- headache
- lightening of normal skin color
- lightening of treated areas of dark skin
- sore throat
- stuffy or runny nose
- tender, swollen glands in the neck
- trouble swallowing
- unusual tiredness or weakness
- voice changes
Common
- symptoms of a serious allergic reaction (e.g., difficulty breathing, dizziness, itching, rash, swelling)
- symptoms of high levels of corticosteroids in the bloodstream (e.g., fatigue, increased thirst, and urination, irritability, muscle weakness)
- blood-containing blisters on the skin
- burning and itching of the skin
- lack of healing or worsening of the skin condition
- numbness in the fingers
- painful, red or itchy, pus-containing blisters in hair follicles
- raised, dark red, wart-like spots on the skin, especially when used on the face
- skin infection
- thinning of the skin with easy bruising
Rare
- Acne or pimples
- accumulation of pus
- blistering, crusting, irritation, itching, or reddening of the skin
- burning, itching, and pain in hairy areas, or pus at the root of the hair
- burning and itching of the skin with pinhead-sized red blisters
- change in hearing
- cracked, dry, scaly skin
- diarrhea
- dry skin
- earache or pain in the ear
- ear drainage
- flushing or redness of the skin
- darkening of the skin
- itching, scaling, severe redness, soreness, or swelling of the skin
- itchy, raised, round, smooth, skin-colored bumps found on just one area of the body
- ooze thick white fluid
- raised, dark red, wart-like spots on the skin, especially when used on the face
- redness or swelling in the ear
- skin irritation
- skin rash, encrusted, scaly and oozing
- spots on your skin resembling a blister or pimple
- swelling
- swollen, red, tender area of infection
Drug Interactions of Fluocinolone
Fluocinolone may interact with following drugs, supplements & may change the efficacy of drugs
- amphetamine
- dextroamphetamine
- aspirin
- lorazepam
- diphenhydramine
- duloxetine
- omega-3 polyunsaturated fatty acids
- fluticasone nasal
- pregabalin
- polyethylene glycol
- albuterol
- Probiotic Formula bifidobacterium infantis
- lactobacillus acidophilus
- montelukast
- acetaminophen
- Vitamin B12 (cyanocobalamin)
- Vitamin C (ascorbic acid)
- Vitamin D2 (ergocalciferol)
- Vitamin D3 (cholecalciferol)
- alprazolam
- sertraline
- cetirizine
Pregnancy Category of Fluocinolone
FDA Pregnancy Category – C
Pregnancy
Fluocinolone has not been studied during breastfeeding. Since the only extensive application of the most potent corticosteroids may cause systemic effects in the mother, it is unlikely that short-term application of topical corticosteroids would pose a risk to the breastfed infant by passage into breastmilk. However, it would be prudent to use the least potent drug on the smallest area of skin possible. It is particularly important to ensure that the infant’s skin does not come into direct contact with the areas of skin that have been treated. Only the lower potency corticosteroids should be used on the nipple or areola where the infant could directly ingest the drugs from the skin. Only water-miscible cream or gel products should be applied to the breast because ointments may expose the infant to high levels of mineral paraffin via licking. Any topical corticosteroid should be wiped off thoroughly prior to nursing if it is being applied to the breast or nipple area.
Breast-feeding
This medication may pass into breast milk. If you are a breast-feeding mother and are taking fluocinolone acetonide, it may affect your baby. Talk to your doctor about whether you should continue breast-feeding. The safety and effectiveness of using certain formulations of fluocinolone acetonide have not been established for children. Check with your doctor or pharmacist before using this medication on a child.
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