flumetasone

Action and Spectrum

Actions and Spectrum: 

flumetasone is a synthetic corticosteroid that is used topically for its anti-inflammatory and immunosuppressive effects. As a corticosteroid, it exerts its actions by interacting with glucocorticoid receptors. flumetasone has anti-inflammatory, antipruritic, and vasoconstrictive properties.  

• Glucocorticoid Receptor Binding: flumetasone binds to glucocorticoid receptors present in the cytoplasm of target cells. 
• Receptor Activation: Upon binding, flumetasone causes a conformational change in the glucocorticoid receptor. 
• Translocation to Nucleus: The activated glucocorticoid receptor complex translocates into the cell nucleus. 
• Gene Transcription Regulation: In the nucleus, the glucocorticoid receptor complex modulates the transcription of specific genes by interacting with glucocorticoid response elements (GREs) on the DNA. 
• Anti-Inflammatory Effects: flumetasone suppresses the transcription of pro-inflammatory genes, such as those encoding cytokines and enzymes involved in the inflammatory response. This leads to a reduction in the synthesis of inflammatory mediators. 

Drug Interaction

Adverse Reaction

Frequency not defined 

Hypersensitivity reactions 

Black Box Warning

Black box warning: 

None 

Contraindication / Caution

Contraindications/caution: 

Contraindications: 

• Hypersensitivity: Individuals who have a known hypersensitivity or allergy to flumetasone or any of the components in the formulation should avoid its use. 
• Perioral Dermatitis: flumetasone and other topical corticosteroids are generally contraindicated in cases of perioral dermatitis, a facial rash that tends to spare the area around the eyes. 
• Acne Vulgaris: The use of flumetasone may be contraindicated in the presence of acne vulgaris due to the potential for exacerbation of the condition. 
• Skin Infections: Topical corticosteroids should not be used in the presence of untreated bacterial, viral, or fungal skin infections. If a skin infection is present, appropriate antimicrobial therapy may be necessary before initiating corticosteroid treatment. 
• Rosacea: flumetasone and other topical corticosteroids are generally contraindicated in rosacea, a chronic skin condition characterized by facial redness and sometimes pimples. 

Caution: 

Tapering: 

• Systemic Absorption: Even when used topically, some corticosteroids can be absorbed systemically. Prolonged use of high-potency corticosteroids or application over large areas of the body increases the risk of systemic absorption. 
• Adrenal Suppression: Prolonged use, especially in large areas of the body, may lead to adrenal suppression. Gradual tapering may be necessary to avoid adrenal insufficiency, particularly if the treatment is stopped abruptly. 
• Skin Folds: Care should be taken when applying flumetasone to intertriginous areas (areas where skin surfaces come into contact, such as under the breasts or in the groin), as these areas are more prone to skin thinning and other adverse effects. 
• Perioral Dermatitis: Topical corticosteroids, including flumetasone, should be used cautiously on the face and are generally contraindicated in perioral dermatitis. 
• Infection Risk: Topical corticosteroids can mask or exacerbate infections. If an infection is present, appropriate antimicrobial therapy should be initiated before starting corticosteroid treatment. 

Pregnancy / Lactation

Pregnancy consideration: Insufficient data available 

Lactation: Excretion of the drug in human breast milk is unknown 

Pregnancy category: 

Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester. 

Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.    

Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.    

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.    

Category N: There is no data available for the drug under this category 

Pharmacology

Pharmacology: 

flumetasone is a synthetic corticosteroid with anti-inflammatory, immunosuppressive, and vasoconstrictive properties. It is primarily used in topical formulations for the treatment of various dermatological conditions. 

• Glucocorticoid Receptor Agonist: flumetasone binds to intracellular glucocorticoid receptors in target cells, forming a receptor-ligand complex. 
• Translocation to Nucleus: The receptor-ligand complex translocates into the nucleus of the cell. 

Genomic Effects: 

• Gene Transcription Regulation: In the nucleus, the glucocorticoid receptor complex binds to glucocorticoid response elements (GREs) on the DNA, modulating the transcription of specific genes. 
• Anti-Inflammatory Effects: flumetasone suppresses the transcription of genes involved in the inflammatory response, leading to a reduction in the synthesis of inflammatory mediators such as prostaglandins and leukotrienes. 
• Immunosuppressive Effects: flumetasone inhibits the function of immune cells, particularly T-lymphocytes, leading to a dampened immune response. 

Non-Genomic Effects: 

• Membrane Stabilization: flumetasone may exert rapid, non-genomic effects by stabilizing cell membranes, leading to decreased release of inflammatory mediators. 

Pharmacodynamics:  

• Glucocorticoid Receptor Binding: flumetasone binds to intracellular glucocorticoid receptors (GR) present in the cytoplasm of target cells. 
• Receptor Activation: Upon binding, flumetasone induces a conformational change in the glucocorticoid receptor. 
• Translocation to Nucleus: The activated glucocorticoid receptor complex translocates from the cytoplasm to the cell nucleus. 
• Gene Transcription Modulation: In the nucleus, the glucocorticoid receptor complex interacts with specific DNA sequences known as glucocorticoid response elements (GREs). This interaction results in the modulation of gene transcription, either enhancing or suppressing the expression of specific genes. 
• Anti-Inflammatory Effects: flumetasone suppresses the transcription of pro-inflammatory genes, including those encoding cytokines (e.g., interleukins), enzymes involved in the inflammatory process (e.g., cyclooxygenase-2), and other mediators. The overall effect is a reduction in the synthesis of inflammatory proteins, leading to anti-inflammatory actions. 
• Immunosuppressive Effects: flumetasone inhibits the function of immune cells, particularly T-lymphocytes. This immunosuppressive effect is due to the modulation of genes involved in the immune response, leading to a decreased production of inflammatory cytokines. 

Pharmacokinetics: 

Absorption 

flumetasone is primarily administered topically in the form of creams, ointments, or lotions for dermatological conditions. When applied to the skin, flumetasone is absorbed through the epidermis into the systemic circulation. 

Distribution 

Corticosteroids, including flumetasone, are highly bound to plasma proteins, mainly albumin. flumetasone is distributed to various tissues, including the skin and underlying tissues, after systemic absorption. 

Metabolism 

flumetasone undergoes metabolism primarily in the liver. The cytochrome P450 enzyme system, particularly CYP3A4, is involved in the metabolism of flumetasone. 

flumetasone is metabolized into various metabolites during hepatic metabolism. The metabolites formed are generally inactive and are excreted from the body. 

Elimination and Excretion 

Metabolites of flumetasone are excreted in the urine. Some portion of the drug and its metabolites may be excreted in the feces. flumetasone and its metabolites have a relatively short elimination half-life. Despite the short half-life, the effects of flumetasone may persist due to its impact on gene transcription and protein synthesis. 

Adminstartion

Administration: 

Topical administration 

flumetasone is a corticosteroid that is commonly administered topically for dermatological conditions. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: flumetasone 

Why do we use flumetasone? 

flumetasone is a synthetic corticosteroid that is primarily used for its anti-inflammatory and immunosuppressive properties. It is commonly employed in dermatology for the treatment of various skin conditions.  

• Atopic Dermatitis (Eczema): flumetasone is used topically to manage the symptoms of atopic dermatitis. 
• Contact Dermatitis: It is used to alleviate inflammation and itching associated with allergic contact dermatitis and irritant contact dermatitis, which are skin reactions caused by exposure to allergens or irritants. 
• Psoriasis: flumetasone is prescribed for the treatment of psoriasis, a chronic autoimmune skin disorder. 
• Seborrheic Dermatitis: This corticosteroid is used to manage seborrheic dermatitis. 
• Allergic Reactions: flumetasone may be employed to relieve inflammation and itching associated with various allergic skin reactions.