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Active ingredient: Fluticasone Propionate - Brands, Medical Use, Clinical Data

Brands, Medical Use, Clinical Data

Drug Category

  • Anti-allergic Agents
  • Dermatologic Agents
  • Bronchodilator Agents
  • Anti-inflammatory Agents
  • Adrenergic Agents

Dosage Forms

  • Metered-dose (aerosol)

Brands / Synonyms

Advair Diskus 100/50; Advair Diskus 250/50; Advair Diskus 500/50; Cutivate; Flixonase; Flixotide; Flonase; Flovent; Flovent Diskus 100; Flovent Diskus 250; Flovent Diskus 50; Flovent HFA; Flunase

Indications

For the maintenance treatment of asthma as prophylactic therapy and for patients requiring oral corticosteroid therapy for asthma.

Pharmacology

Fluticasone propionate, a medium-potency synthetic corticosteroid, is used topically to relieve inflammatory and pruritic symptoms of dermatoses and psoriasis, intranasally to manage symptoms of allergic and non-allergic rhinitis, and orally for the treatment of asthma.

Mechanism of Action

Binds to the glucocorticoid receptor. Unbound corticosteroids cross the membranes of cells such as mast cells and eosinophils, binding with high affinity to glucocorticoid receptors (GR). The results include alteration of transcription and protein synthesis, a decreased release of leukocytic acid hydrolases, reduction in fibroblast proliferation, prevention of macrophage accumulation at inflamed sites, reduction of collagen deposition, interference with leukocyte adhesion to the capillary wall, reduction of capillary membrane permeability and subsequent edema, reduction of complement components, inhibition of histamine and kinin release, and interference with the formation of scar tissue. In the management of asthma, the glucocorticoid receptor complexes down-regulates proinflammatory mediators such as interleukin-(IL)-1, 3, and 5, and up-regulates anti-inflammatory mediators such as IkappaB [inhibitory molecule for nuclear factor kappaB1], IL-10, and IL-12. The antiinflammatory actions of corticosteroids are also thought to involve release of cytosolic phospholipase A2 which controls the biosynthesis of potent mediators of inflammation such as prostaglandins and leukotrienes.

Absorption

The extent of percutaneous absorption of topical corticosteroids is determined by many factors, including the vehicle and the integrity of the epidermal barrier.

Toxicity

Not Available

Biotrnasformation / Drug Metabolism

Fluticasone propionate is metabolized in the liver by cytochrome P450 3A4-mediated hydrolysis of the 5-fluoromethyl carbothioate grouping. This transformation occurs in 1 metabolic step to produce the inactive 17-(beta)-carboxylic acid metabolite, the only known metabolite detected in man.

Contraindications

CUTIVATE Cream is contraindicated in those patients with a history of hypersensitivity to any of the components in the preparation.

Drug Interactions

No Information Provided.

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