Formoterol fumarate

Formoterol fumarate (Foradil Aerolizer) is administered only by oral inhalation using the Aerolizer Inhaler. 

Formoterol Fumarate + Fluticasone Propionate dry powder inhaler... 

Charge 4.5 g of micronized oxitropium bromide and 0.675 g of micronized formoterol fumarate into a pressure-addition vessel. After sealing and evacuation thereof, 10.5 kg of HFA 227, which has previously been aerated with carbon dioxide and adjusted to a pressure of 6.25 bar (20°C)... 

Synonym Formoterol fumarate Trade name Oxeze Indications Asthma, bronchospasm Category Adrenergic beta2-receptor agonist Half-life 10-14 hours... 

In the processing of formoterol fumarate by means of the SEDS technique (31), totally amorphous material was obtained when dry carbon dioxide was used as the antisolvent, while the use of water-saturated carbon dioxide afforded a mixture of amorphous formoterol fumarate and crystalline dihydrate form. 

D.C. Apperley, A.F. MarkweU, 1. Frantsuzov, A.J. llott, R.K. Harris, P. Hodgkinson, NMR characterisation of dynamics in solvates and desolvates of formoterol fumarate, Phys. Chem. Chem. Phys. 15 (17) (2013) 6422-6430. 

Nix et al. (1990) found the protective effect of formoterol against methacholine-induced broncho-constriction in 12 asthmatic patients lasting for at least 5 h. The rapid pulmonary absorption of inhaled formoterol and its slow elimination from plasma are in agreement with the fast onset and the long duration, respectively, of bronchodilation of inhaled formoterol fumarate in clinical trials (Le-CAiLLON et al. 1997). There was no indication that formoterol produced a more pronounced tachyphylaxis to P2-adrenoceptor stimulation in the bronchial muscle of asthmatics than the P2-adrenoceptor agonists normally used, e.g. salbutamol (Larsson et al. 1988, Arvidsson et al. 1989). Formoterol powder is as potent as solution (Clauzel et al. 1991). 

In vitro, formoterol fumarate has been found to be about 50 times more potent than salbutamol on bronchial smooth muscle (Ida 1976, Decker et al. 1982) and at least as Pj-selective as salbutamol and terbutaline (Decker et al. 1982). 

Gross NJ, Kerwin E, Levine B, Kim KT, Denis-Mize K, Hamzavi M, et al. Nebulized formoterol fumarate dose selection and pharmacokinetics. Pulm Pharmacol Ther 2008 21(5) 818-23. 

Tashkin DP, Doherty DE, Kerwin E, Matiz-Bueno CE, Knorr B, Shekar T, et al. Efficacy and safety of a fixed-dose combination of mometasone furcate and formoterol fumarate in subjects with moderate to very severe COPD results from a 52-week phase III trial. Int J Chron Obstruct Pulmon Dis 2012 7 43-55. 

Formoterol fumarate formulated for dry powder inhaler. Adult dose 0.012-0.024 mg twice a day from 0.012 mg dose unit. 

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