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Symbicort & COPD - Mechanism of Action - Anti-Inflammatory Action
Symbicort®: Mechanism of action
Symbicort® contains formoterol (a selective long-acting ß2-agonist bronchodilator) and budesonide (a glucocorticosteroid), each of which have a different mechanism of action [1]. Together, they show additive effects [2,3]. The specific properties of budesonide and formoterol allow the combination to be used as a maintenance treatment for COPD. Read about Symbicort in asthma: mechanism of action.
Budesonide: Mechanism of action
Budesonide is a glucocorticosteroid which, when inhaled, has a dose-dependent anti-inflammatory action in the airways. Inhaled budesonide has less severe adverse effects than systemic corticosteroids [4]. Budesonide has been shown to be very effective against the characteristic inflammation of asthma although the exact mechanism responsible for the anti-inflammatory effect of budesonide is unknown. Read more about this on the Symbicort in asthma: mechanism of action page. COPD has a distinctly different pattern of chronic ongoing airway inflammation to asthma and there are conflicting results as to the benefits of inhaled corticosteroid (ICS) therapy when used alone [5-8]. However, budesonide is reported to reduce the risk of COPD exacerbations and slow the rate of decline of health-related quality of life in symptomatic COPD patients [9,10].
Formoterol: Mechanism of action
Formoterol is a selective long-acting ß2-agonist (LABA) bronchodilator that, when inhaled, results in rapid and long-acting relaxation of bronchial smooth muscle in patients with reversible airways obstruction [11]. In patients with COPD, formoterol has been shown to have a fast onset of effect, as rapid as salbutamol [12,13] and faster than salmeterol [14] as well as a long duration (12 hours) [15].
Does Symbicort® Turbuhaler® deliver budesonide and formoterol effectively?
Yes. Symbicort is delivered via Turbuhaler® which is an easy-to-use, inspiratory flow-driven inhaler [16]. The Turbuhaler is designed for optimal delivery of budesonide and formoterol to the airways and plays an essential role in the efficacy of Symbicort Turbuhaler®. The unique Turbuhaler vortex design of the mouth piece ensures that a high fraction of budesonide and formoterol fine particles are deposited into the lungs. Turbuhaler® only requires an inspiratory flow rate of 30 L/min to lift the dose from the dosing disc. Most patients, even those with a limited peak inspiratory flow, such as elderly patients – achieve flow rates well above this value [16].
Compared with other dry powder inhalers such as Diskus™, Turbuhaler delivers a greater proportion of fine particles to the airways, per dose, resulting in greater lung deposition [17-20]. Fine particle dose and lung deposition achieved with Turbuhar are both comparable to that reported with the pressurised metered dose inhaler Modulite® [20, 21]
Turbuhaler delivers a high proportion of fine particles to the airways
Data are not direct treatment comparisons
1. Dhillon S, Keating GM. Drugs 2006;66: 1475–83.
2. Borgstrom L, et al. Int J Clin Pract 2005;59: 1488–95.
Turbuhaler deposits a high proportion of drug in the lungs
Data are not direct treatment comparisons
1. Dhillon S, Keating GM. Drugs 2006;66: 1475–83.
2. Borgstrom L, et al. Int J Clin Pract 2005;59: 1488–95.
References
- Cazzola M,.Hanania NA. The role of combination therapy with corticosteroids and long-acting beta2-agonists in the prevention of exacerbations in COPD. Int J Chron Obstruct Pulmon Dis 2006;1:345-354.
- Calverley PM, Boonsawat W, Cseke Z, et al. Maintenance therapy with budesonide and formoterol in chronic obstructive pulmonary disease. Eur Respir J 2003;22:912-919.
- Szafranski W, Cukier A, Ramirez A, et al. Efficacy and safety of budesonide/formoterol in the management of chronic obstructive pulmonary disease. Eur Respir J 2003;21:74-81.
- Global Initiative for Chronic Obstructive Lung Disease. Global strategy for the diagnosis, management, and prevention of chronic obstructive pulmonary disease. Updated 2009. Available at: http://goldcopd.org/Guidelineitem.asp?l1=2&l2=1&intId=2003. Accessed December 9, 2009.
- Pauwels RA, Lofdahl CG, Laitinen LA, et al. Long-term treatment with inhaled budesonide in persons with mild chronic obstructive pulmonary disease who continue smoking. European Respiratory Society Study on Chronic Obstructive Pulmonary Disease. N Engl J Med 1999;340:1948-1953.
- Vestbo J, Sorensen T, Lange P, et al. Long-term effect of inhaled budesonide in mild and moderate chronic obstructive pulmonary disease: a randomised controlled trial. Lancet 1999;353:1819-1823.
- Burge PS, Calverley PM, Jones PW, et al, for the ISOLDE study investigators. Randomised, double blind, placebo controlled study of fluticasone propionate in patients with moderate to severe chronic obstructive pulmonary disease: the ISOLDE trial. Br Med J 2000;320:1297-1303.
- Spencer S, Calverley PM, Burge PS, et al. Impact of preventing exacerbations on deterioration of health status in COPD. Eur Respir J 2004;23:698-702.
- Sin DD,.Tu JV. Inhaled corticosteroids and the risk of mortality and readmission in elderly patients with chronic obstructive pulmonary disease. Am J Respir Crit Care Med 2001;164:580-584.
- Alsaeedi A, Sin DD, McAlister FA. The effects of inhaled corticosteroids in chronic obstructive pulmonary disease: a systematic review of randomized placebo-controlled trials. Am J Med 2002;113:59-65.
- Seberova E,.Andersson A. Oxis (formoterol given by Turbuhaler) showed as rapid an onset of action as salbutamol given by a pMDI. Respir Med 2000;94:607-611.
- Benhamou D, Cuvelier A, Muir JF, et alI. Rapid onset of bronchodilation in COPD: a placebo-controlled study comparing formoterol (Foradil Aerolizer) with salbutamol (Ventodisk). Respir Med 2001;95:817-821.
- Cazzola M, Centanni S, Regorda C, et al. Onset of action of single doses of formoterol administered via Turbuhaler in patients with stable COPD. Pulm Pharmacol Ther 2001;14:41-45.
- Cote C, Pearle JL, Sharafkhaneh A, et al. Faster onset of action of formoterol versus salmeterol in patients with chronic obstructive pulmonary disease: a multicenter, randomized study. Pulm Pharmacol Ther 2009;22:44-49.
- Ceylan E. Budesonide-formoterol (inhalation powder) in the treatment of COPD. Int J Chron Obstruct Pulmon Dis 2006;1:115-122.
- Selroos O, Borgstrom L, Ingelf J. Performance of Turbuhaler® in Patients with Acute Airway Obstruction and COPD, and in Children with Asthma : Understanding the Clinical Importance of Adequate Peak Inspiratory Flow, High Lung Deposition, and Low In Vivo Dose Variability. Treat Respir Med 2006;5:305-315.
- Agertoft L,.Pedersen S. Lung deposition and systemic availability of fluticasone Diskus and budesonide Turbuhaler in children. Am J Respir Crit Care Med 2003;168:779-782.
- Asking L, Maayan C, Petterson G. Flutide Diskus less consistent than Pulmicort Turbuhaler with respect to in vitro fine particle dose proportionality. Am J Respir Crit Care Med 2009;163:A441.
- Thorsson L, Edsbacker S, Kallen A, et al. Pharmacokinetics and systemic activity of fluticasone via Diskus and pMDI, and of budesonide via Turbuhaler. Br J Clin Pharmacol 2001;52:529-538.
- Borgstrom L, Asking L, Thorsson L. Idealhalers or realhalers? A comparison of Diskus and Turbuhaler. Int J Clin Pract 2005;59:1488-1495.
- Dhillon S,.Keating GM. Beclometasone dipropionate/formoterol: in an HFA-propelled pressurised metered-dose inhaler. Drugs 2006;66:1475-1483.
