Fluticasone furoate nasal spray: Profile of an enhanced-affinity corticosteroid in treatment of seasonal allergic rhinitis

Abstract

Of the classes of pharmacotherapy for seasonal allergic rhinitis, intranasal corticosteroids are the preferred treatment and are recommended in practice guidelines as first-line pharmacotherapy for rhinitis with prominent nasal congestion. The enhanced-affinity intranasal corticosteroid fluticasone furoate nasal spray (GW685698X), is one of the newest additions to the armamentarium for allergic rhinitis. This review summarizes the preclinical and clinical data on fluticasone furoate nasal spray and discusses its place in pharmacotherapy for seasonal allergic rhinitis. Important attributes of fluticasone furoate in seasonal allergic rhinitis include low systemic bioavailability (<0.5%), onset of symptom relief as early as eight hours after initiation of treatment, 24-hour symptom relief with once-daily dosing, comprehensive coverage of both nasal and ocular symptoms, safety and tolerability with daily use, and availability in a side-actuated device that makes medication delivery simple and consistent. With these attributes, fluticasone furoate nasal spray has the potential to enhance patient satisfaction and compliance and reduce the need for polypharmacy in the management of seasonal allergic rhinitis.

The Pharmacokinetics of Fluticasone Furoate Given Intranasally in Healthy Subjects Using an Ultra-Sensitive Analytical Assay

“…different INCS are characterized by different pharmacological and pharmacokinetic properties [8]. It is reported that fluticasone furoate has the highest relative glucocorticoid receptor affinity and lipophilicity, an extensive hepatic first-pass metabolism, and with one of the lowest systemic exposures and potential risks among INCS used for AR [3,8].…”

“…It exhibits its antiinflammatory effect as an entire molecule and is therefore not a prodrug or a salt [2]. The exact mechanism of action of fluticasone furoate in treating AR is not full known, and may affect the early and late phase inflammatory response [3]. It is suggested that being a corticosteroid, it exhibits its anti-inflammatory effect on multiple inflammatory cells (such as, mast cells, eosinophils, neutrophils, macrophages, and lymphocytes) and mediators (such as, histamine, eicosanoids, leukotrienes, and cytokines) [1,3].…”

“…The exact mechanism of action of fluticasone furoate in treating AR is not full known, and may affect the early and late phase inflammatory response [3]. It is suggested that being a corticosteroid, it exhibits its anti-inflammatory effect on multiple inflammatory cells (such as, mast cells, eosinophils, neutrophils, macrophages, and lymphocytes) and mediators (such as, histamine, eicosanoids, leukotrienes, and cytokines) [1,3]. Other theories suggest that fluticasone furoate can suppress inflammatory gene activation through multiple mechanisms, such as inhibition of pro-inflammatory transcription factors like the NFκB [2,4].…”

“…Other theories suggest that fluticasone furoate can suppress inflammatory gene activation through multiple mechanisms, such as inhibition of pro-inflammatory transcription factors like the NFκB [2,4]. Symptom relief can be achieved approximately 8 h after starting treatment and can last for up to 24 h [3].…”

Perbandingan terapi radiofrekuensi disertai steroid topikal dan steroid topikal saja pada rinitis alergi persisten

“…2 Efektivitas terapi steroid topikal ini adalah 67% dibandingkan dengan terapi plasebo 39%. 5 Terapi operatif sendiri menurut WHO ARIA dilakukan setelah terapi medikamentosa gagal, 2 namun terjadinya kongesti hidung, baik karena proses remodelling yang bersifat ireversibel atau proses inflamasi yang menimbulkan edema, dapat membatasi penetrasi steroid topikal ke mukosa rongga hidung. 6,7 Terapi reduksi konka merupakan salah satu operasi pada RA.…”