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QuickView for Fluticasone Propionate (compound)

Name: fluticasone propionate
Name (isomeric): DB00588
Drug Type: small molecule
Brand: Cutivate, Flovent Diskus 100, Flovent Diskus 50, Flovent Diskus 250, Advair Diskus, Flovent HFA, Flixotide, Advair Diskus 250/50, Flixonase, Flovent, Flonase, Flunase, Advair Diskus 500/50, Advair Diskus 100/50
Category: Adrenergic Agents, Anti-Allergic Agents, Bronchodilator Agents, Dermatologic Agents, Anti-inflammatory Agents
CAS number: 80474-14-2
Indication: 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, p...
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Absorption: The extent of percutaneous absorption of topical corticosteroids is determined by many factors, including the vehicle and the integrity of the epidermal barrier.
Protein binding: 91%
Biotransformation: 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.
Half Life: 10 hours
Clearance: 1093 mL/min
Affected organisms: Humans and other mammals
Drug interaction:
ConivaptanCYP3A4 Inhibitors (Strong) may increase the serum concentration of Fluticasone (Oral Inhalation). Concurrent use of orally inhaled fluticasone with strong CYP3A4 inhibitors is not recommended.
VoriconazoleVoriconazole, a strong CYP3A4 inhibitor, may increase the serum concentration of fluticasone by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects of fluticasone if voriconazole is initiated, discontinued or dose changed.
TipranavirTipranavir, co-administered with Ritonavir, may increase the plasma concentration of Fluticasone propionate. Concomitant therapy should be avoided if possible.
TelithromycinTelithromycin may reduce clearance of Fluticasone. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Fluticasone if Telithromycin is initiated, discontinued or dose changed.