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OverviewMechanism of ActionHow To UseUsesBenfitsIndicationsMethod of AdministrationDosage StrengthsDosage FormsDietary RestrictionsContraindicationsWarnings and Precautions for usingAdverse ReactionsSide EffectsUse of Diflorasone diacetate in Specific PopulationsClinical Pharmacology Clinical StudiesAuthored by Reviewed by References
Diflorasone diacetate

Diflorasone diacetate

Indications, Uses, Dosage, Drugs Interactions, Side effects
Diflorasone diacetate
Medicine Type :
Allopathy
Prescription Type:
Prescription Required
Approval :
DCGI (Drugs Controller General of India)
Schedule
Schedule H
Pharmacological Class:
Corticosteroid,
Therapy Class:
Anti-inflammatory Agent,

Diflorasone diacetate is an Anti-inflammatory belonging to the Corticosteroid class.

Diflorasone is a topical corticosteroid used to treat the symptoms of various inflammatory skin conditions that cause erythema, pruritus, and discomfort.

Around 1% of Diflorasone reaches dermal layers or systemic circulation; occlusive dressings increase absorption percutaneously. Diflorasone undergoes primarily hepatic metabolism. Diflorasone excreted via urine and faeces.

Diflorasone diacetate shows side effects like Burning, itching, irritation, redness, or drying or cracking of the skin, acne, rash, increased hair growth, change in skin color, bruising or shiny skin, tiny red bumps, or rash around the mouth, small white or red bumps on the skin.

Diflorasone diacetate is available in the form of Topical cream and ointment.

Diflorasone diacetate is available in China, India, United States, Italy, Israel, Canada, Croatia, and Malaysia.

Diflorasone diacetate is a Corticosteroid belonging to the class Anti-inflammatory.

Mechanism of the Diflorasone diacetate anti-inflammatory activity of topical steroids in the treatment of steroid-responsive dermatoses, in general, is uncertain. 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.

The Onset of action and duration of action of Diflorasone diacetate is not clinically established.

Diflorasone diacetate is available in the form of Topical cream and ointment.

Diflorasone comes as a cream and an ointment to apply to the skin. It is usually applied to the affected area one to three times a day.

Diflorasone is used to treat the itching, redness, dryness, crusting, scaling, inflammation, and discomfort of various skin conditions, including psoriasis (a skin disease in which red, scaly patches form on some areas of the body and eczema (a skin disease that causes the skin to be dry and itchy and to sometimes develop red, scaly rashes).

Diflorasone diacetate is an Anti-inflammatory belonging to the Corticosteroid class.

Diflorasone diacetate topical corticosteroids have anti-inflammatory, antipruritic, and vasoconstrictive properties. May depress the formation, release, and activity of endogenous chemical mediators of inflammation (kinins, histamine, liposomal enzymes, prostaglandins) through the induction of phospholipase A2 inhibitory proteins (lipocortins) and sequential inhibition of the release of arachidonic acid.

Diflorasone diacetate is approved for use in the following clinical indications

  • Diflorasone is a topical corticosteroid used to treat the symptoms of various inflammatory skin conditions that cause erythema, pruritus, and discomfort.
  • Corticosteroid-responsive dermatosis: Topical: Apply sparingly 1 to 3 times daily.

Diflorasone diacetate is available in various strengths as 0.05%.

Diflorasone diacetate is available in the form of Topical cream and ointment.

Diflorasone diacetate is contraindicated in patients with

  • Topical steroids are contraindicated in those patients with a history of hypersensitivity to any of the components of the preparation.
  • Adrenal suppression

May cause hypercortisolism or suppression of hypothalamic-pituitary-adrenal (HPA) axis, particularly in younger children or in patients receiving high doses for prolonged periods. HPA axis suppression may lead to adrenal crisis.

  • Contact dermatitis

Allergic contact dermatitis can occur, it is usually diagnosed by failure to heal rather than clinical exacerbation.

  • Immunosuppression

Prolonged use may result in fungal or bacterial superinfection; discontinue if dermatological infection persists despite appropriate antimicrobial therapy.

  • Kaposi sarcoma

Prolonged treatment with corticosteroids has been associated with the development of Kaposi sarcoma (case reports); if noted, discontinuation of therapy should be considered.

  • Ocular effects

Subcapsular cataracts, glaucoma (with possible nerve damage), and increased intraocular pressure have been reported with topical use.

  • Skin reactions

Local adverse effects (eg, atrophy, striae, telangiectasias, burning, itching, irritation, dryness, folliculitis, acneiform eruptions, hypopigmentation, perioral dermatitis, allergic contact dermatitis, secondary infection, and miliaria) may occur. Reactions may not be reversible and may be more likely to occur with prolonged use, higher potency corticosteroids, and occlusive dressings.

  • Systemic effects

Topical corticosteroids may be absorbed percutaneously. Absorption of topical corticosteroids may cause manifestations of Cushing's syndrome, hyperglycemia, or glycosuria. Absorption is increased using occlusive dressings, application to denuded skin, or application to large surface areas.

Breast Feeding Warning

It is not known whether topical administration of corticosteroids could result in sufficient systemic absorption to produce detectable quantities in breast milk. Because many drugs are excreted in human milk, caution should be exercised when Diflorasone diacetate Ointment is administered to a nursing woman.

Pregnancy Warning

Corticosteroids are generally teratogenic in laboratory animals when administered systemically at relatively low dosage levels. The more potent corticosteroids have been shown to be teratogenic after dermal application in laboratory animals. There are no adequate and well-controlled studies in pregnant women on teratogenic effects from topically applied corticosteroids. Therefore, topical corticosteroids should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Drugs of this class should not be used extensively on pregnant patients, in large amounts, or for prolonged periods of time.

  • Common

Burning sensation, Acneiform eruption, allergic contact dermatitis, atrophic striae, folliculitis, hypertrichosis, hypopigmentation, maceration of the skin, miliaria, perioral dermatitis, pruritus, skin atrophy, skin irritation, xeroderma, HPA-axis suppression (children at greater risk), Secondary infection.

  • Rare

Acne rosacea, aggravation reaction, cataract, dermal ulcer, glaucoma, hirsutism, hyperpigmentation, Kaposi's sarcoma (reactivation), nonthrombocytopenic purpura, ocular hypertension, psoriasis flare (rebound), purpura, skin photosensitivity, spontaneous star-shaped scar-like lesions, telangiectasia, tinea (tinea incognito).

  • Aldesleukin: Diflorasone diacetate corticosteroids may diminish the antineoplastic effect of Aldesleukin.

The common side effects of diflorasone diacetate include the following

  • Common side effects

Burning, itching, irritation, redness, or drying or cracking of the skin, acne, rash, increased hair growth, change in skin color, bruising or shiny skin, tiny red bumps, or rash around the mouth, small white or red bumps on the skin.

  • Rare side effects

Redness, swelling, oozing pus or other signs of skin infection in the place where you applied diflorasone, changes in the way fat is spread around the body, sudden weight gain, unusual tiredness, muscle weakness, depression, and irritability.

  • Pregnancy

Pregnancy Category C

Corticosteroids are generally teratogenic in laboratory animals when administered systemically at relatively low dosage levels. The more potent corticosteroids have been shown to be teratogenic after dermal application in laboratory animals. There are no adequate and well-controlled studies in pregnant women on teratogenic effects from topically applied corticosteroids. Therefore, topical corticosteroids should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Drugs of this class should not be used extensively on pregnant patients, in large amounts, or for prolonged periods of time.

  • Nursing Mothers

It is not known whether topical administration of corticosteroids could result in sufficient systemic absorption to produce detectable quantities in breast milk. Because many drugs are excreted in human milk, caution should be exercised when diflorasone Ointment is administered to a nursing woman.

  • Pediatric Use

Safety and effectiveness of diflorasone diacetate ointment) in pediatric patients have not been established. Because of a higher ratio of skin surface area to body mass, pediatric patients are at a greater risk than adults of HPA axis suppression when they are treated with topical corticosteroids. They are, therefore, also at greater risk of glucocorticosteroid insufficiency after withdrawal of treatment and of Cushing’s syndrome while on treatment. Adverse effects including striae have been reported with inappropriate use of topical corticosteroids in pediatric patients.

  • Geriatric Use

Clinical studies of diflorasone diacetate topical formulations did not include enough subjects aged 65 and over to determine whether they respond differently from younger subjects.

  • Pharmacodynamic

Diflorasone has anti-inflammatory, antipruritic, and vasoconstrictive properties. Once absorbed through the skin, topical corticosteroids are handled through pharmacokinetic pathways like systemically administered corticosteroids. Diflorasone is a potent topical corticosteroid that should not be used with occlusive dressings. It is recommended that treatment should be limited to 2 consecutive weeks and therapy should be discontinued when adequate results have been achieved.

  • Pharmacokinetics

Absorption

Around 1% of Diflorasone reaches dermal layers or systemic circulation; occlusive dressings increase absorption percutaneously.

Distribution

Information is not available.

Metabolism and Excretion

Diflorasone undergoes primarily hepatic metabolism. Diflorasone excreted via urine and faeces.

There are some clinical studies of the drug Diflorasone diacetate mentioned below:
  1. Shupack JL, Jondreau L, Kenny C, Stiller MJ. Diflorasone diacetate ointment 0.05% versus betamethasone dipropionate ointment 0.05% in moderate-severe plaque-type psoriasis. Dermatology. 1993 Oct 8;186(2):129-32.
  2. Krueger GG, O'Reilly MA, Weidner M, Dromgoole SH, Killey FP. Comparative efficacy of once-daily flurandrenolide tape versus twice-daily diflorasone diacetate ointment in the treatment of psoriasis. Journal of the American Academy of Dermatology. 1998 Feb 1;38(2):186-90.
  3. Kaidbey K, Kopper SC, Sefton J, Gibson JR. A pilot study to determine the effect of tazarotene gel 0.1% on steroid‐induced epidermal atrophy. International journal of dermatology. 2001 Jul;40(7):468-71.
  • https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/019260s009lbl.pdf
  • https://www.uptodate.com/contents/diflorasone-drug-information?search=diflorasone&source=panel_search_result&selectedTitle=1~2&usage_type=panel&kp_tab=drug_general&display_rank=1
  • https://medlineplus.gov/druginfo/meds/a602019.html#:~:text=Diflorasone is used to treat,and itchy and to sometimes
  • https://www.drugs.com/pro/diflorasone.html
  • https://go.drugbank.com/drugs/DB00223
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Jyoti Suthar
Jyoti is a Post graduate in Pharmaceutics ( M Pharm) She did her graduation ( B Pharm) From SSR COLLEGE OF PHARMACY And thereafter did her M Pharm specialized in Pharmaceutics from SSR COLLEGE OF PHARMACY
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Dr JUHI SINGLA
Dr JUHI SINGLA has completed her MBBS from Era’s Lucknow Medical college and done MD pharmacology from SGT UNIVERSITY Gurgaon. She can be contacted at editorial@medicaldialogues.in. Contact no. 011-43720751
Published on: 3 Aug 2023 5:26 PM GMT
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