345
Views
2
CrossRef citations to date
0
Altmetric
Drug profiles

Budesonide/salmeterol in fixed-dose combination for the treatment of asthma

, &
Pages 113-125 | Received 19 Oct 2015, Accepted 15 Dec 2015, Published online: 21 Jan 2016

References

  • Papers of special note have been highlighted as:
  • • of interest
  • •• of considerable interest
  • Barnes PJ. Scientific rationale for combination inhalers with a long-acting b2-agonists and corticosteroids. Eur Respir J. 2002;19:182–191.
  • Barnes PJ. Scientific rationale for using a single inhaler for asthma control. Eur Respir J. 2007;29:587–595.
  • Greening AP, Ind PW, Northfield M, et al. Added salmeterol versus higher dose corticosteroids in asthma patients. Lancet. 1994;344:523–529.
  • Shrewsbury S, Pyke S, Britton M. Meta-analysis of increased dose of inhaled steroid or addition of salmeterol in symptomatic asthma (MIASMA). Bmj. 2000;320:1368–1373.
  • Markham A, Jarvis B. Inhaled salmeterol/fluticasone propionate combination: a review of its use in persistent asthma. Drugs. 2000;60:1207–1233.
  • Shapiro G, Lumry W, Wolfe J, et al. Combined salmeterol 50 mg and fluticasone propionate 250 mg in the Diskus device for the treatment of asthma. Am J Respir Crit Care Med. 2000;161:527–534.
  • McGavin JK, Goa KL, Jarvis B. Inhaled budesonide/formoterol combination. Drugs. 2001;61:71–78.
  • O’Byrne PM, Barnes PJ, Rodriguez-Roisin R. Low dose inhaled budesonide and formoterol in mild persistent asthma. Am J Respir Critical Care Med. 2001;164:1392–1397.
  • Roth M, Rüdiger JJ, Bihl MP, et al. β2-agonist, formoterol activates the glucocorticoid receptor in vivo. Eur Respir J. 2000;16(Suppl 31):437s.
  • Roth M, Johnson Q, Ge M, et al. Budesonide and formoterol inhibits proliferation of human bronchial smooth musle cells (BSMC) via glucocorticoid receptor mediated activation of p21Waf/Cip-1. Am J Respir Crit Care Med. 2001;163(5):A270.
  • Papi A, Paggiaro PL, Nicolini G, et al. Beclomethasone/formoterol vs fluticasone/salmeterol inhaled combination in moderate to severe asthma. Allergy. 2007;62:1182–1188.
  • Papi A, Paggiaro PL, Nicolini G, et al. Beclomethasone/formoterol versus budesonide/formoterol combination therapy in asthma. Eur Respir J. 2007;29:682–689.
  • Dusser, Vicaut E, Lefrançois G, et al. Double-blind, double-dummy, multinational, multicenter, parallel-group design clinical trial of clinical non-inferiority of formoterol 12 microg/unit dose in a b.i.d. regimen administered via an HFA-propellant-pMDI or a dry powder inhaler in a 12-week treatment period of moderate to severe stable persistent asthma in adult patients. Respiration. 2005;72:20–27.
  • Corren J, Korenblat PE, Miller CJ, et al. Twelve-week, randomized, placebo-controlled, multicenter study of the efficacy and tolerability of budesonide and formoterol in one metered-dose inhaler compared with budesonide alone and formoterol alone in adolescents and adults with asthma. Clin Ther. 2007;29(5):823–843.
  • Goldsmith DR, Keating GM. Budesonide/Formoterol : a review of its use in asthma. Drugs. 2004;64(14):1597–1618.
  • Barnes PJ, Nicolini G, Bizzi A, et al. Do inhaled corticosteroid/long-acting beta2-agonist fixed combinations provide superior clinical benefits compared with separate inhalers? A literature reappraisal. Allergy Asthma Proc. 2012;33(2):140–144.

•• A review of the benefits of the fixed-dose combinations of inhaled corticosteroid (ICS) + long-acting β-agonists (LABA) in a single inhaler over the separate components.

  • Esmailpour N, Hogger P, Rohdewald P. Binding kinetics of budesonide to the human glucocorticoid receptor. Eur J Pharm Sci. 1998;6:219–223.
  • Miller-Larsson A, Jansson P, Runström A, et al. Prolonged airway activity and improved selectivity of budesonide possibly due to esterification. Am J Respir Crit Care Med. 2000;162(4 Pt 1):1455–1461.
  • Ryrfeldt A, Andersson P, Edsbäcker S, et al. Pharmacokinetics and metabolism of budesonide, a selective glucocorticoid. Eur J Respir Dis Suppl. 1982;122:86–95.
  • Szefler SJ. Pharmacodynamics and pharmacokinetics of budesonide: a new nebulized corticosteroid. J Allergy Clin Immunol. 1999;104(4 Pt 2):175–183.
  • Brogden RN, Faulds D. Salmeterol xinafoate. A review of its pharmacological properties and therapeutic potential in reversible obstructive airways disease. Drugs. 1991;42:895–912. Review.
  • Johnson M, Butchers PR, Coleman RA, et al. The pharmacology of salmeterol. Life Sci. 1993;52(26):2131–2143.
  • Murnane D, Martin GP, Marriott C. Validation of a reverse-phase high performance liquid chromatographic method for concurrent assay of a weak base (salmeterol xinafoate) and a pharmacologically active steroid (fluticasone propionate). J Pharm Biomed Anal. 2006;40(5):1149–1154.
  • Lötvall J. Pharmacological similarities and differences between β2-agonist. Respir Med. 2001;95(supplement B):S7–S11.
  • Palmqvist M, Persson G, Lazer L, et al. Inhaled dry-powder formoterol and salmeterol in asthmatic patients: onset of action, duration of effect and potency. Eur Respir J. 1997Nov;10(11):2484–2489.
  • Van Noord JA, Smeets JJ, Raaijmakers JAM, et al. Salmeterol versus formoterol in patients with moderately severe asthma: onset and duration of action. Eur Respir J. 1996;9:1684–1688.
  • Baker JG, Proudman RG, Hill SJ. Salmeterol’s extreme beta2 selectivity is due to residues in both extracellular loops and transmembrane domains. Mol Pharmacol. 2015 Jan;87(1):103–120.
  • Szczuka A, Wennerberg M, Packeu A, et al. Molecular mechanisms for the persistent bronchodilatory effect of the beta 2-adrenoceptor agonist salmeterol. Br J Pharmacol. 2009 Sep;158(1):183–194.
  • Green SA, Rathz DA, Schuster AJ, et al. The Ile164 beta(2)-adrenoceptor polymorphism alters salmeterol exosite binding and conventional agonist coupling to G(s). Eur J Pharmacol. 2001;421(3):141–147.
  • Rong Y, Arbabian M, Thiriot DS, et al. Probing the salmeterol binding site on the beta 2-adrenergic receptor using a novel photoaffinity ligand, [(125)I]iodoazidosalmeterol. Biochemistry. 1999;38(35):11278–11286.
  • Nelson HS, Weiss ST, Bleecker ER, et al. The salmeterol multicenter asthma research trial: a comparison of usual pharmacotherapy for asthma or usual pharmacotherapy plus salmeterol. Chest. 2006;129:15–26.
  • Mcivor RA, Pizzichini E, Turner MO, et al. Potential masking effects of salmeterol on airway inflammation in asthma. Am J Respir Crit Care Med. 1998;158:924–930.
  • Usmani OS, Biddiscombe MF, Barnes PJ. Regional lung deposition and bronchodilator response as a function of beta2-agonist particle size. Am J Respir Crit Care Med. 2005;172:1497–1504.
  • Bronsky E, Grossman J, Henis MJ, et al. Inspiratory flow rates and volumes with the Aerolizer dry powder inhaler in asthmatic children and adults. Curr Med Res Opin. 2004;20(2):131–137.
  • Ball D, Hirst P, Newman S, et al. Deposition and pharmacokinetics of budesonide from the Miat Monodose inhaler, a simple dry powder device. Int J Pharm. 2002;245:123–132.
  • The Global Strategy for Asthma Management and Prevention, Global Initiative for Asthma (GINA); 2015 [cited 2015 Sep 23]. Available from: http://www.ginasthma.org/
  • Guideline on clinical development of fixed combination medicinal products; EMA/CHMP/281825/2015 [cited 2015 Sep 23]. Available from:http://www.ema.europa.eu/ema/index.jsp?curl=pages/regulation/general/general_content_000366.jsp
  • Adams NP, Jones PW. The dose-response characteristics of inhaled corticosteroids when used to treat asthma: an overview of Cochrane systematic reviews. Respir Med. 2006;100:1297–1306.
  • Adams NP, Bestall JC, Jones P. Budesonide at different doses for chronic asthma (Cochrane Review). Cochrane Database Syst Rev. 2000;2(reprinted 2008, 4):CD003271.
  • Boe J, Rosenhall L, Alton M, et al. Comparison of dose-response effects of inhaled beclomethasone dipropionate and budesonide in the management of asthma. Allergy. 1989;44(5):349–355.
  • Bousquet J, Ben-Joseph R, Messonnier M, et al. A meta-analysis of the dose-response relationship of inhaled corticosteroids in adolescents and adults with mild to moderate persistent asthma. Clin Ther. 2002;24:1–20.
  • O’Connell EJ. Efficacy of budesonide in moderate to severe asthma. Clin Ther. 2002;24:887–904.
  • Kemp JP, Bierman CW, Cocchetto DM. Dose-response study of inhaled salmeterol in asthmatic patients with 24-hour spirometry and Holter monitoring. Ann Allergy. 1993;70:316–322.
  • Masoli M, Holt S, Weatherall M, et al. Dose-response relationship of inhaled budesonide in adult asthma : a meta-analysis. Eur Respir J. 2004;23:552–558.

•• The study emphasizes the difficulty/impossibility to demonstrate any dose–response with ICS, even more so with ICS/LABA fixed-dosed combination.

  • Demoly P, Hagedoorn P, De Boer AH, et al. The clinical relevance of dry powder inhaler performance for drug delivery. Respir Med. 2014;108:1195–1203.
  • Renard D, Looby M, Kramer B, et al. Characterization of the bronchodilatory dose response to indacaterol in patients with chronic obstructive pulmonary disease using model-based approaches. Respir Res. 2011;12:54.
  • Bronsky EA, Kemp JP, Orgel HA, et al. A 1-week dose-ranging study of inhaled salmeterol in patients with asthma. Chest. 1994;105:1032–1037.
  • Derom E, Van De Velde V, Marissens S, et al. Effects of inhaled ciclesonide and fluticasone propionate on cortisol secretion and airway responsiveness to adenosine 5’monophosphate in asthmatic patients. Pulm Pharmacol Ther. 2005;18:328–336.
  • Toogood JH, Baskerville J, Jennings B, et al. Bioequivalent doses of budesonide and prednisone in moderate and severe asthma. J Allergy Clin Immunol. 1989;84:688–700.
  • Ayres JG, Bateman ED, Lundbäck B, et al. High dose fluticasone propionate, 1 mg daily, versus fluticasone propionate, 2 mg daily, or budesonide, 1.6 mg daily, in patients with chronic severe asthma. International Study Group. Eur Respir J. 1995;8:579–586.
  • Ebden P, Jenkins A, Houston G, et al. Comparison of two high dose corticosteroid aerosol treatments, beclomethasone dipropionate (1500 micrograms/day) and budesonide (1600 micrograms/day), for chronic asthma. Thorax. 1986;41:869–874.
  • Clark DJ, Grove A, Cargill RI, et al. Comparative adrenal suppression with inhaled budesonide and fluticasone propionate in adult asthmatic patients. Thorax. 1996;51:262–266.
  • Derom E, Van Schoor J, Verhaeghe W, et al. Systemic effects of inhaled fluticasone propionate and budesonide in adult patients with asthma. Am J Respir Crit Care Med. 1999;160:157–161.
  • Clark DJ, Lipworth BJ. Adrenal suppression with chronic dosing of fluticasone propionate compared with budesonide in adult asthmatic patients. Thorax. 1997;52:55–58.
  • Martin RJ, Szefler SJ, Chinchilli VM, et al. Systemic effect comparisons of six inhaled corticosteroid preparations. Am J Respir Crit Care Med. 2002;165:1377–1383.

• The measurement of plasma and urinary cortisol to evaluate the effect of ICS on hypothalamic pituitary adrenocortical axis method in a crossover study is confirmed to be a sensitive method of assessing safety of ICS.

  • Szefler S, Rohatagi S, Williams J, et al. Ciclesonide, a novel inhaled steroid, does not affect hypothalamic-pituitary-adrenal axis function in patients with moderate-to-severe persistent asthma. Chest. 2005;128:1104–1114.
  • Tamm M, Richards DH, Beghe B, et al. Inhaled corticosteroid and long-acting β2 -agonist pharmacological profiles: effective asthma therapy in practice. Respir Med. 2012;106(Suppl 1):S9–S19.
  • Coutts JAP, Gibson NA, Paton JY. Measuring compliance with inhaled medication in asthma. Arch Dis Child. 1992;67:332–333.
  • Horn CR, Clark TJH, Cochrane GM. Compliance with inhaled therapy and morbidity from asthma. Respir Med. 1990;84:67–70.
  • O’Byrne PM, Bisgaard H, Godard PP, et al. Budesonide/formoterol combination therapy as both maintenance and reliever medication in asthma. Am J Respir Crit Care Med. 2005;171:129–136.
  • Aalbers R. Single inhaler as maintenance and reliever therapy–is it SMART? Lancet Respir Med. 2013;1:2–3.

• An interesting comment on the diversity of option to apply ICSs and LABAs.

  • Ehrick JD, Wylie J, Goodey AP, et al. Orally inhaled fixed-dose combination products for the treatment of asthma and chronic obstructive pulmonary disease: not simple math. Ther Deliv. 2014;5:297–317.

•• A valuable analysis on the complexity of factors determining the effects of ICS + LABA fixed-dose combinations.

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.