Fluticasone propionate, asthma

Chervinsky P, van As A, Bronsky EA, et al. Fluticasone propionate aerosol for the treatment of adults with mild to moderate asthma. The Fluticasone Propionate Asthma Study Group. J Allergy Clin Immunol 1994 94(4) 676—83. 

Cater, J.I., Vare, M., Peters, W.J., Olsson, B., and Gomez, E., Comparison of the efficacy of fluticasone propionate given twice daily via the Diskus /Accuhaler and the Diskhaler in patients with asthma, Eur. Resp. J., 8 427S (1995). 

Recommended Starting Doses of Fluticasone Propionate/Salmeterol for Asthma Patients (Age 12) Taking Inhaled Corticosteroids ... 

Drake AJ, Howells RJ, Shield JPH, PrendiviUe A, Ward PS, Crowne EC. Symptomatic adrenal insufficiency presenting with hypoglycaemia in asthmatic children with asthma receiving high dose inhaled fluticasone propionate. BMJ 2002 324 1081-2. 

Bateman ED, Jacques L, Goldfrad C, Atienza T, Mi-haescu T, Duggan M. Asthma control can be maintained when fluticasone propionate/sahneterol in a single inhaler is stepped down. J AUergy Clin Immunol 2006 117(3) 563-70. 

Woodcock AA, Bag donas A, Boonsawat W, Gibbs MR, Bousquet J, Bateman ED. GOAL Steering Committee and Investigators. Improvement in asthma endpoints when aiming for total control sahneterol/fluticasone propionate versus fluticasone propionate alone. Prim Care Respir J 2007 16(3) 155-61. 

The first inhaled glucocorticoid, beclomethasone dipropionate, revolutionized asthma therapy, when it was found that topical delivery to the lung resulted in reduced systemic side-effects (adrenal suppression, oseteoporosis and growth inhibition) typically seen with oral steroid treatments. Interestingly, a further reduction in systemic exposure was achieved with the introduction of fluticasone propionate (1). The evolution of this drug stemmed from observations with the steroid 17-carboxylates that showed that these esters were active topically when esterified, while the parent acids were inactive. Thus it was realized that enzymatic hydrolysis of the ester would lead to systemic deactivation. SAR studies led to a series of carbothioates, which were very active in vivo when topically applied to rodents, but were inactive after oral administration. It was shown that fluticasone propionate (1) underwent first pass metabolism in the liver to the corresponding inactive 173-carboxylic acid (la) (Scheme 1). This observation was... 

A 23-year-old man, with a history of asthma, house dust mite allergy, and rhinoconjunctivitis, presented with acute respiratory symptoms. He was given oral cetirizine, inhaled salmeterol, and fluticasone propionate, and oral prednisone 40 mg/day for 1 week and 20 mg/day for 1 week. His asthma recurred when prednisone was withdrawn and he took oral prednisone 60 mg/day for 1 week and 40 mg/day for 1 week. He also took montelukast 10 mg/day. He then developed severe peripheral edema with a gain in weight of 13 kg. Prednisone was withdrawn and his edema resolved. Montelukast was continued. 

The effect of increasing doses of mometasone furoate and fluticasone propionate by dry powder inhaler on adrenal function was studied by using overnight urinary cortisol in 21 patients with asthma (55). Patients were randomized in a crossover fashion to receive 2-weekly consecutive doubling doses of either fluticasone propionate (500, 1000, and 2000 micrograms/day) or mometasone furoate (400, 800, and 1600 micrograms/day). Both treatments were... 

A 32-year-old woman s asthma regimen was changed from budesonide to fluticasone propionate 500 micrograms/day and salmeterol (44). Eight months later, she was evaluated because of excessive bodyweight gain her serum cortisol concentration was 16 nmol/1. Fluticasone propionate was replaced with nedocromil and 1 month later her serum cortisol concentration had normalized. 

Brutsche MH, Brutsche IC, Munawar M, Langley SJ, Masterson CM, Daley-Yates PT, Brown R, Custovic A, Woodcock A. Comparison of pharmacokinetics and systemic effects of inhaled fluticasone propionate in patients with asthma and healthy volunteers a randomised crossover study. Lancet 2000 356(9229) 556-61. 

Berend N, Kellett B, Kent N, Sly PD, Bowler S, Burdon J, Dennis C, Gibson P, James A, Jenkins C. Collaborative Study Group of the Australian Lung Foundation. Improved safety with equivalent asthma control in adults with chronic severe asthma on high-dose fluticasone propionate. Respirology 2001 6(3) 237-46. 

Eid N, Morton R, Olds B, Clark P, Sheikh S, Looney S. Decreased morning serum cortisol levels in children with asthma treated with inhaled fluticasone propionate. Pediatrics 2002 109(2) 217-21. 

Li JT, Ford LB, Chervinsky P, Weisberg SC, Kellerman DJ, Faulkner KG, Herje NE, Hamedani A, Harding SM, Shah T. Fluticasone propionate powder and lack of clinically significant effects on hypothalamic-pituitary-adrenal axis and bone mineral density over 2 years in adults with mild asthma. J Allergy Clin Immunol 1999 103(6) 1062-8. 

Casale TB, Nelson HS, Strieker WE, Raff H, Newman KB. Suppression of hypothalamic-pituitary-adrenal axis activity with inhaled flunisolide and fluticasone propionate in adult asthma patients. Ann Allergy Asthma Immunol 2001 87(5) 379-85. 

Niitsuma T, Okita M, Sakurai K, Morita S, Tsuyuguchi M, Matsumura Y, Hayashi T, Koshishi T, Oka K, Homma M. Adrenal function as assessed by low-dose adrenocortico-tropin hormone test before and after switching from inhaled beclomethasone dipropionate to inhaled fluticasone propionate. J Asthma 2003 40 515-22. 

Nguyen KL, Lauver D, Kim I, Aresery M. The effect of a steroid burst and long-term, inhaled fluticasone propionate on adrenal reserve. Ann Allergy Asthma Immunol 2003 91 38-43. 

Zimmerman B, Gold M, Wherrett D, Hanna AK. Adrenal suppression in two patients with asthma treated with low doses of the inhaled steroid fluticasone propionate. J Allergy Clin Immunol 1998 101(3) 425-6. 

Sim D, Griffiths A, Armstrong D, Clarke C, Rodda C, Freezer N. Adrenal suppression from high-dose inhaled fluticasone propionate in children with asthma. Eur Respir J 2003 21 633-6. 

Gregson RK, Rao R, Murrills AJ, Taylor PA, Warner JO. Effect of inhaled corticosteroids on bone mineral density in childhood asthma comparison of fluticasone propionate with beclomethasone dipropionate. Osteoporos Int 1998 8(5) 418-22. 

Fitzgerald D, Van Asperen P, Mellis C, Honner M, Smith L, Ambler G. Fluticasone propionate 750 micro-grams/day versus beclomethasone dipropionate 1500 micrograms/day comparison of efficacy and adrenal function in paediatric asthma. Thorax 1998 53(8) 656-61. 

Price JF, Russell G, Hindmarsh PC, Weller P, Heaf DP, Williams J. Growth during one year of treatment with fluticasone propionate or sodium cromoglycate in children with asthma. Pediatr Pulmonol 1997 24(3) 178-86. 

Ferguson AC, Spier S, Manjra A, Versteegh FG, Mark S, Zhang P. Efficacy and safety of high-dose inhaled steroids in children with asthma a comparison of fluticasone propionate with budesonide. J Pediatr 1999 134(4) 422-7. 

S. M. Holliday, D. Faulds, and E. M. Sorkin, Inhaled fluticasone propionate. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic use in asthma, Drugs 47 318 (1994). 

Seretide is a combination therapy consisting of fluticasone propionate and salmeterol. It is marketed by GSK for the treatment of asthma. Fluticasone is the chiral component and a steroid derivative. 

Oral glucocorticoids such as dexamethasone and prednisolone are still used in patients with severe asthma, though these agents are associated with adverse systemic effects. Inhaled glucocorticoid therapy was introduced in 1972 with beclomethasone dipropionate, which dramatically reduced systemic effects. Fluticasone propionate (launched in 1993) is very efficiently inactivated in the liver, and exhibits low oral bioavailability, which in turn leads to a further reduction in systemic exposure. 

Fluticasone propionate 400 micrograms/day or budesonide 800 micrograms/day were administered for 20 weeks to children with moderate to severe asthma aged 4—12 years. Fluticasone propionate was superior to... 

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