Seasonal allergic rhinitis: fluticasone propionate and fluticasone furoate therapy evaluated

Abstract

Seasonal allergic rhinitis (SAR) is increasing in prevalence such that 1 in 4 persons is affected in the UK. It represents a considerable burden of disease since in a significant proportion of individuals the severity of nasal-ocular symptoms has an important effect on daily activity, performance and quality of life. Intranasal steroids (INS) form the mainstay of treatment, having been shown in meta-analyses to be superior to oral antihistamines, intranasal antihistamines and anti-leukotrienes. Fluticasone propionate is an established INS for the treatment of rhinitis, including SAR. Its favorable pharmacological profile combining high local efficacy with low systemic bioavailability has established fluticasone propionate as an effective intervention. The more recent introduction of structurally related fluticasone furoate with similar but enhanced pharmacological characteristics with a novel delivery device may confer further therapeutic advantages.

Rapid Measurement of Heteronuclear Coupling Constants in Complex NMR Spectra

“…The structural analysis of a crude extract of fluticasone propionate, a pharmaceutical known for its anti-inflammatory properties, was facilitated by IPAP-FESTA. 36,37 The extraction process (detailed in the SI) resulted in a dilute mixture (Figure 2a) in which fluticasone propionate is present at approximately 4%, determined by 1 H NMR, of the concentration of the major component of the extracted formulation, the excipient 2-phenylethan-1-ol. The presence of fluticasone propionate (Scheme 1) was confirmed by the appearance of three distinct signals in the 19 F NMR, corresponding to F6, F9, and F21 (Figure S2c).…”

“…The structural analysis of a crude extract of fluticasone propionate, a pharmaceutical known for its anti-inflammatory properties, was facilitated by IPAP-FESTA. , …”

“…The new IPAP-FESTA method (Figure ) allows the extraction of both the signs and magnitudes of J HF couplings as small as 0.1 Hz in as little as 3 min, much more rapidly than HD-HAPPY-FESTA or alternative 2D experiments. Its usefulness is demonstrated in the structural analysis of a crude mixture of fluticasone propionate, extracted from a nasal formulation used to treat asthma and allergic rhinitis. , IPAP-FESTA suppresses the signals of the major excipient in the mixture, and aids structure determination, by revealing the signs and magnitudes of all the J HF couplings of weakly coupled 1 H signals within the selected spin system (Figure ). The chemical utility of the method is also illustrated by experimentally measuring J HF values (Figure ) to investigate solvent effects in a physically inseparable fluorohydrin mixture of two isomers, each with two main conformers in rapid equilibrium.…”

The Role of Small Molecules Containing Fluorine Atoms in Medicine and Imaging Applications

“…Fluticasone 4 is used for relieving nasal symptoms such as sneezing, itching, and runny nose provoked by allergies; recent studies use this compound in combination with other medications to improve its effects against allergic rhinitis [ 38 , 39 , 40 ]. Also, fluticasone is combined with salmeterol and prescribed under the medication named Advair for the treatment of asthma as well as other obstructive airway diseases [ 41 , 42 ].…”

“…The study determined that derivatives of escitalopram containing aromatic fluorine and the presence of the cyano group were significant for a twofold decrease in dissociation rate and had a high contribution to allosteric potency. Fluticasone 4 is used for relieving nasal symptoms such as sneezing, itching, and runny nose provoked by allergies; recent studies use this compound in combination with other medications to improve its effects against allergic rhinitis [38][39][40]. Also, fluticasone is combined with salmeterol and prescribed under the medication named Advair for the treatment of asthma as well as other obstructive airway diseases [41,42].…”