Fluticasone propionate/formoterol fumarate in fixed-dose combination for the treatment of asthma

Abstract

A new combination inhaler containing fluticasone, a potent inhaled corticosteroid (ICS), and formoterol, a long-acting β-agonist (LABA) with rapid onset and sustained bronchodilator effect, has been approved for treatment of persistent asthma in patients ≥12 years of age requiring combination ICS-LABA therapy. The fluticasone/formoterol combination, delivered via pressurized metered-dose inhaler and available in three dose strengths, has demonstrated a good safety and tolerability profile in trials of up to 1 year. The efficacy of fluticasone/formoterol is greater than that of fluticasone or formoterol alone and noninferior to that of fluticasone/salmeterol and budesonide/formoterol in tightly controlled 8-12-week clinical trials. Advantages of the fluticasone/formoterol combination aerosol include rapid onset of bronchodilation, an attribute preferred by patients, and emission of a high fine-particle fraction that is consistent at different flow rates, which may aid consistency of delivery (given patient variability in inhalation maneuvers) and provide real-life benefits.

Co-inhalation of roflumilast, rather than formoterol, with fluticasone more effectively improves asthma in asthmatic mice

“…71 The fixed-dose fluticasone/formoterol inhaler (available in low, medium and high doses) used for treatment of persistent asthma shows an efficacy which is greater than that of either agent alone in addition to good safety. 42 In human, addition of low doses of inhaled b 2 agonists to low doses of ICS produced more inhibition of cellular proliferation and cytokines production in lung because b 2 agonists causes more activation of the corticosteroid receptors 72 and corticosteroids increase the b 2 receptor transcription. 73 Investigating the effects of a triple therapy of roflumilast, formoterol, and fluticasone is an interesting point for a further research to detect whether superior to the two-drug regimens.…”

“…8,36 The drugs given included roflumilast (R, 500 µg/kg), 26,39 formoterol (Fo, 50 µg/kg), 36 fluticasone (F, 1000 µg/kg), 40,41 roflumilast + fluticasone (R + F, 500 + 1000 µg/kg), and formoterol + fluticasone (Fo + F 50 + 1000 µg/kg). 42,40…”

“…8,36 The drugs given included roflumilast (R, 500 mg/kg), 26,39 formoterol (Fo, 50 mg/kg), 36 fluticasone (F, 1000 mg/kg), 40,41 roflumilast þ fluticasone (R þ F, 500 þ 1000 mg/kg), and formoterol þ fluticasone (Fo þ F 50 þ 1000 mg/kg). 42,40 Measurement of airway hyperreactivity to methacholine (MCh) AHR was measured in the conscious unrestrained mice using the single chamber whole body plethysmography (Buxco Electronics, Wilmington, NC, USA) (WBP) and analyzed using Buxco software. Mice were acclimatized to the plethysmograph before experiments.…”

Therapeutic effects of co-inhaled roflumilast or formoterol and fluticasone on asthma-induced ultrastructural changes in murine airways

“…Drugs were given by inhalation for 15 min once/day for seven doses with the last dose given 5 -6 h before the final OVA challenge. The drugs given included roflumilast (R, 500 µg/kg) [12], formoterol (Fo, 50 µg/kg) [10], fluticasone (F, 1000 µg/kg) [13,14], roflumilast + fluticasone (R + F, 500+1000 µg/kg) and formoterol + fluticasone (Fo + F, 50 + 1000 µg/kg) [13,15]. Dimethyl sulfoxide (DMSO) was used as a vehicle for the drugs.…”