Fluticasone furoate nasal spray in the treatment of allergic rhinitis

Abstract

Allergic rhinitis (AR) is a prevalent disease with great morbidity and signifi cant societal and economic burden. Intranasal corticosteroids are recommended as fi rst-line therapy for patients with moderate-to-severe disease, especially when nasal congestion is a major component of symptoms. To compare the effi cacy and safety profi le of different available intranasal corticosteroids for the treatment of AR, it is important to understand their different structures and pharmacokinetic and pharmacodynamic properties. Knowledge of these drugs has increased tremendously over the last decade. Studies have elucidated mechanisms of action, pharmacologic properties, and the clinical impact of these drugs in allergic respiratory diseases. Although the existing intranasal corticosteroids are already highly effi cient, the introduction of further improved formulations with a better effi cacy/ safety profi le is always desired. Fluticasone furoate nasal spray is a new topical corticosteroid, with enhanced-affi nity and a unique side-actuated delivery device. As it has high topical potency and low potential for systemic effects, it is a good candidate for rhinitis treatment.

The association of absolute eosinophil count, serum immunoglobulin E and spirometry with co-morbid bronchial asthma in patients with allergic rhinitis

“…This spray was given for 6 months and, at the end of these 6 months, all subjects were symptomatically better. Pedro Giavina-Bianchi et al states that fluticasone furoate nasal spray "has a high topical potency and low potential for systemic effects" and is proved to be a good treatment for rhinitis 8 , which is in accordance with our findings.…”

Icon

“…111,115 The intranasal steroid (INS) used in recommended doses are generally considered safe and are not associated with long-term, clinically significant or irreversible side effects. 116,117 However, in a retrospective chart review of 12 glaucoma patients using nasal corticosteroids, changes in intraocular pressure have been reported. 118 Although the assessment of the quality of the evidence (AMSTAR2) from 5 systemic reviews evaluating INS for ocular symptoms associated with allergic rhinitis was recently reviewed, 119 the effect of "long-term" chronic use of INS on the eye has not been well studied.…”

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

“…Fluticasone furoate is a synthetic fluorinated corticosteroid (Figure 1) with anti-inflammatory effects arising from its interaction with intracellular glucocorticoid receptors 13. An enhanced-affinity corticosteroid, fluticasone furoate has greater relative receptor affinity in vitro for the human glucocorticoid receptor than other corticosteroids including dexamethasone, mometasone furoate, fluticasone propionate, ciclesonide active principle, and budesonide (Figure 2).…”

“…Fluticasone furoate administered intranasally to 16 healthy volunteers at supratherapeutic dosages of 880 μg at eight-hour intervals for 10 doses, or 2640 μg /day, had a geometric mean absolute bioavailability of 0.50% (90% confidence interval [CI] 0.34%–0.74%) 19. Except in isolated cases, fluticasone furoate is not quantifiable in plasma following intranasal dosing of 110 μg once daily 13,15. Even after administration of a 2 mg oral dose in a study in healthy volunteers, bioavailability was low (1.6%) because of extensive first-pass metabolism 20…”