Inhaled corticosteroids for adult asthma: Impact of formulation and delivery device on relative pharmacokinetics, efficacy and safety

Respiratory Medicine

Volumn 93, Issue 3, 1999, Pages 149-160

  Shaw, R J ^a,b  

^a NATIONAL HEART AND LUNG INSTITUTE   (United Kingdom)

^b HAMMERSMITH HOSPITAL   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

BECLOMETASONE DIPROPIONATE; BUDESONIDE; CHLOROFLUOROCARBON; CORTICOSTEROID; FLUORINATED HYDROCARBON; FLUTICASONE; PROPELLANT;

ADULT; AEROSOL; ASTHMA; BONE ATROPHY; CLINICAL TRIAL; CONTROLLED CLINICAL TRIAL; CONTROLLED STUDY; DOUBLE BLIND PROCEDURE; DRUG DELIVERY SYSTEM; DRUG EFFICACY; DRUG FORMULATION; DRUG SAFETY; DRUG TOLERABILITY; HUMAN; HYPOTHALAMUS HYPOPHYSIS ADRENAL SYSTEM; INHALATIONAL DRUG ADMINISTRATION; MAJOR CLINICAL STUDY; METERED DOSE INHALER; ORAL DRUG ADMINISTRATION; PARTICLE SIZE; PRIORITY JOURNAL; RANDOMIZED CONTROLLED TRIAL; REVIEW; STEROID THERAPY;

EID: 0033060857     PISSN: 09546111     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0954-6111(99)90000-8     Document Type: Review

References (104)

1. National Heart, Lung, and Blood Institute, National Institutes of Health. Global Initiative for Asthma: Global Strategy for Asthma Management and Prevention. NHLBI/WHO workshop report. NIH publ. no 95-3659; January 1995.
2. British Thoracic Society, British Paediatric Association, Royal College of Physicians of London, The King's Fund Centre, National Asthma Campaign et al. Guidelines on the management of asthma. Thorax 1993; 48: S1-S24.
3. British Asthma Guidelines Coordinating Committee. British guidelines on asthma management: 1995 review and position statement. Thorax 1997; 52: S1-S24.
4. Montreal Protocol on substances that deplete the ozone layer, Final Act (Nairobi: UNEP, 1987). Federal Register 1994; 59: 56276-56298.
5. Azzawi M, Bradley B, JefTery PK, et al. Identification of activated T lymphocytes and eosinophils in bronchial biopsies in stable atopic asthma. Am Rev Respir Dis 1990; 142: 1407-1413.
6. Kay AB. 'Helper' (CD4+) T cells and eosinophils in allergy and asthma. Am Rev Respir Dis 1992; 145: S22-S26.
7. Hamid Q, Song Y, Kotsimbos TC, Minshall E, Bai TR, Hegele RG, Hogg JC. Respiratory pathophysiologic responses. Inflammation of small airways in asthma. J Allergy Clin Immunol 1997; 100: 44-51.
8. Carroll N, Elliot J, Morton A, James A. The structure of large and small airways in nonfatal and fatal asthma. Am Rev Respir Dis 1993; 147: 405-10.
9. Carroll N, Lehmann E, Barret J, Morton A, Cooke C, James A. Variability of airway structure and inflammation in normal subjects and in cases of nonfatal and fatal asthma. Path Res Pract 1996; 192: 238-248.
10. Evans RM. The steroid and thyroid hormone receptor superfamily. Science 1988; 247: 889-895.
11. Barnes PJ, Pedersen S. Efficacy and safety of inhaled corticosteroids in asthma. Am Rev Respir Dis 1993; 148: S1-S26.
12. Brattsand R, Axelsson B. In: Barnes PJ, ed. New Drugs for Asthma. London: IBC Technical Services, 1992: 192-207.
13. Jenner WN, Kirkham DJ. Immunoassay of beclomethasone 17,21-dipropionate and metabolites. In: Reid E, ed. Bioanalysis of Drugs and Metabolites. London: Plenum, 1988: 77-86.
14. Högger P, Röhdewald P. Binding kinetics of fluticasone propionate to the human glucocorticoid receptor. Steroids 1994; 59: 597-602.
15. Ryrfeldt T, Andersson P, Edsbäcker S, Tönnesson M, Davies D, Pauwels R. Pharmacokinetics and metabolism of budesonide, a selective glucocorticoid. Eur J Respir Dis 1982; 63 (Suppl. 122): 86-95.
16. Wurthwein G, Rehder S, Röhdewald P. Lipophilicity and receptor affinity of glucocorticosteroids. Pharm Ztg Wiss 1992; 4: 161-167.
17. Mackie AE, Ventresca GP, Fuller RW, Bye A. Pharmacokinetics of intravenous fluticasone propionate in healthy subjects. Br J Clin Pharmacol 1996; 41: 539-542.
18. Pedersen S, O'Byrne P. A comparison of the efficacy and safety of inhaled corticosteroids in asthma. Eur J Allergy Clin Immunol 1997; 52 (Suppl. 39): 1-34.
19. Scale JP, Harrison L. Effect of changing the fine particle mass of inhaled beclomethasone dipropionate on intrapulmonary deposition and pharmacokinetic absorption. Respir Med 1998; 92 (Suppl. A): 9-15.
20. Andersson P, Ryrfeldt A. Biotransformation of the topical glucocorticoids budesonide and beclomethasone 17a,21-dipropionate in human liver and lung homogenate. J Pharm Pharmacol 1984; 36: 763-765.
21. Harding SM. The human pharmacology of fluticasone propionate. Respir Med 1990; 84 (Suppl. A): 25-29.
22. Harrison L, Leach CL, Scale P. Improvement in topical lung versus systemic availability of beclomethasone dipropionate (BDP) from an extrafine aerosol formulation. Eur Respir J 1997; 10 (Suppl. 25): 349S.
23. Task Group on Lung Dynamics. Deposition and retention models for internal dosimetry of the human respiratory tract. Health Phys 1966; 12: 173-208.
24. Rees PJ, Clark TJH, Morén F. The importance of particle size in response to inhaled bronchodilators. Eur J Respir Dis 1982; 63 (Suppl. 199): 72-78.
25. Lipworth BJ. New perspectives on inhaled drug delivery and systemic bioactivity. Thorax 1995; 50: 105-110.
26. Borgström L. Methodological studies on lung deposition. Evaluation of inhaler devices and absorption mechanisms. In: Act Univ Upps. Comprehensive Summaries from the Uppsala Faculty of Pharmacy. Uppsala: University of Uppsala, 1993: 105.
27. Melchor R, Biddiscombe MF, Mak VHP, Short MD, Spiro SG. Lung deposition patterns of directly labelled salbutamol in normal subjects and in patients with reversible outflow limitation. Thorax 1993; 48: 506-511.
28. Newman SP, Wiesz AW, Talaee N, Clarke SW. Improvement of drug delivery with a breath-actuated pressurized aerosol for patients with poor inhaler technique. Thorax 1991; 46: 712-716.
29. Newman SP. A comparison of lung deposition patterns between different asthma inhalers. J Aerosol Med 1995; 8 (Suppl. 3): S21-S27.
30. King D, Earnshaw SM, Delaney JC. Pressurised aerosol inhalers: the cost of misuse. Br J Clin Pract 1991; 45: 48-49.
31. Manzella BA, Brooks CM, Richards JM, Windsor RA, Soong S-J, Bailey WC. Assessing the use of metered dose inhalers by adults with asthma. J Asthma 1989; 26: 223-230.
32. Taylor D, Tunstell P. Metered dose inhalers: a system for assessing technique in patients and health professionals. Pharmacol J 1991; 239: 626-627.
33. Thorsson L, Edsbäcker S, Conradson TB. Lung deposition of budesonide from Turbuhaler is twice that from a pressurised metered dose inhaler p-MDI. Eut Respir J 1994; 7: 1839-1844.
34. Thorsson L. Influence of inhaler systems on availability, with focus on inhaled corticosteroids. J Aerosol Med 1995; 8 (Suppl. 3): S29-S37.
35. Leach CH. Enhanced drug delivery through reformulating MDIs with HFA propellants - drug deposition and its effect on preclinical and clinical programs. Respir Drug Delivery V 1996; 133-144.
36. Leach CL, Davidson P, Boudreau R. Improved targeting of the airways with CFC-free HFAbeclomethasone metered dose inhaler compared with CFC-beclomethasone. Respir Med 1998; 92 (Suppl. A): 3-8.
37. Killer FC, Mazumder MK, Wilson JD, Bone RC. Aerodynamic size distribution, hygroscopicity and deposition estimation of beclomethasone dipropionate aerosol. J Pharm Pharmacol 1980; 32: 605-609.
38. Ross DL, Schulz RK. Effect of inhalation flow rate on the dosing characteristics of dry powder inhaler (DPI) and metered dose inhaler (MDI) products. J Aerosol Med 1996; 9: 215-226.
39. Leach C. Relevance of radiolabeled steroid inhalation studies to clinical outcomes. J Aerosol Med 1998; 11 (Suppl. 1): S29-S34.
40. June DS, Schulz D W. Improved performance characteristics of CFC-free aerosol MDIs. J Aerosol Med 1995; 8: 91.
41. Donnell D, Harrison LI, Ward S, et al. Acute safety of the CFC-free propellant HFA-134a from a pressurized metered dose inhaler. Eur J Clin Res 1995; 48: 473-77.
42. Alexander DJ. Safety of propellants. J Aerosol Med 1995; 8 (Suppl. 1): S41-S47.
43. Leach CL, Davidson P, Boudreau R. HFAbeclomethasone dipropionate (BDP) provides equivalent lung deposition with or without add-on spacers. Eur Respir J 1997; 10 (Suppl. 25): 236S.
44. Bedazone (bedomethasone dipropionate BP) CFCfree inhaler. Summary of Product Characteristics. Waterford, Eire: Norton (Waterford) Ltd.
45. Ashurst LC, Cripps AL, Munro AJ, et al. Pharmaceutical evaluation of the Volumatic and Babyhaler spacer devices with a new range of HFA-based metered dose inhalers. Eur Respir J 1997; 10 (Suppl. 25): P0346.
46. Ariyananda PL, Agnew JE, Clarke SW. Aerosol delivery systems for bronchial asthma. Postgrad Med J 1996; 72: 151-156.
47. O'Callaghan C, Cant M, Robertson C. Delivery of bedomethasone dipropionate from a spacer device: what dose is available for inhalation? Thorax 1994; 49: 961-964.
48. Barry PW, O'Callaghan C. The effect of delay, multiple actuations and spacer static charge on the in-vitro delivery of budesonide from the Nebuhaler. Br J Clin Pharmacol 1995; 40: 76-78.
49. Leach CL, Davidson P, Boudreau R. Comparison of a breath-activated MDI to coordinated and discoordinated technique with press & breathe HFAbeclomethasone MDIs. Eur Respir J 1997; 10 (Suppl. 25): 236S.
50. Marchik PL. A novel breath actuated device (Autohaler®) consistently actuates during the early phase of inspiration. J Aerosol Med 1995; 8: 187-195.
51. Hindle H, Byron R. Dose emissions from marketed dry powder inhalers. Int J Pharmacol 1995; 116: 169-177.
52. Borgström L, Bondesson E, Moren F, Trofast E, Newman SP. Lung deposition of budesonide inhaled via Turbuhaler: a comparison with terbutaline in normal subjects. Eur Respir J 1994; 7: 69-73.
53. Prime D, Parkes PA, Petchey L, et al. Evaluation of the pharmaceutical performance of two dry powder inhalers: comparison of Diskus® and Turbohaler® inhalers. Am J Respir Crit Care Med 1996; 153: A46.
54. Ryan G, Dolovich MB, Obminski G, Cockcroft DW, Juniper E, Hargreave FE, Newhouse MT. Standardisation of inhalation provocation tests. J Allergy Clin Immunol 1981; 67: 156-161.
55. The Nebuliser Project Group of the British Thoracic Society Standards of Care Committee. Current best practices for nebuliser treatment. Thorax 1997; 52 (Suppl. 2): S1-S106.
56. Lipworth BJ. Clinical pharmacology of corticosteroids in bronchial asthma. Pharmacol Ther 1993; 58: 173-209.
57. Geddes DN. Inhaled corticosteroid: benefits and risks. Thorax 1992; 47: 404-407.
58. Davies B. A comparison of bedomethasone dipropionate and budesonide in the treatment of asthma. Br J Clin Pract 1993; 47: 87-93.
59. Tjwa MK. Budesonide inhaled via Turbuhaler: a more effective treatment for asthma than bedomethasone dipropionate via Rotahaler. Ann Allergy Asthma Immunol 1995; 75: 107-111.
60. Selroos O, Backman R, Forsén K-O, Löfroos AB, Niemistö, Pietinalho A, Riska H. Clinical efficacy of budesonide Turbuhaler® compared with that of beclomethasone pMDI with volumatic spacer. A 2-year randomized study in 102 asthma patients. Allergy 1994; 49: 833-836.
61. Brambilla C, Godard P, Lacronique J, Allaert FA, Duroux P and the French Budesonide Trial Group. A 3-month comparative dose-reduction study with inhaled beclomethasone dipropionate and budesonide in the management of moderate to severe adult asthma. Drug Invest 1994; 8: 49-56.
62. Piquet J, Zuck P, Dennewald G, et al. Equally efficacious asthma management with budesonide 800 fig administered by Turbuhaler® or with beclomethasone dipropionate 1500 fig given through a pressurised metered dose inhaler with a spacer. Adv Therapy 1996; 13: 39-50.
63. Boe J, Rosenhall L, Alton M, et al. Comparison of dose-response effects of inhaled beclomethasone dipropionate and BUD in the management of asthma. Allergy 1989; 44: 349-355.
64. Holliday SM, Faulds D, Sorkin EM. Inhaled fluticasone propionate. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic use in asthma. Drugs 1994; 47: 318-331.
65. Fuller R, Johnson M, Bye A. Fluticasone propionate - an update on preclinical and clinical experience. Respir Med 1995; 89 (Suppl. A): 3-18.
66. Clark DJ, Lipworth BJ. Dose-response of inhaled drugs in asthma: an update. Clin Pharmacokinet 1997; 32: 58-74.
67. -1 administered by pressurized inhaler. Respir Med 1993; 87: 609-620.
68. Conolly A, on behalf of a UK Study Group. A comparison of fluticasone propionate 100 μg twice daily with budesonide 200μg twice daily via their respective powder devices in the treatment of asthma. Eur J Clin Res 1996; 7: 15-29.
69. Barnes NC, Marone G, DiMaria GU, Visser S, Utama I, Payne SL on behalf of an International Study Group. A comparison of fluticasone propionate, 1 mg daily, with beclomethasone dipropionate, 2 mg daily, in the treatment of severe asthma. Eur Respir J 1993; 6: 877-885.
70. Langdon CG, Thompson J, on behalf of a UK Study Group. A multicentre study to compare the efficacy and safety of inhaled fluticasone propionate and budesonide via metered-dose inhalers in adults with mild-to-moderate asthma. Br J Clin Res 1994; 5: 73-84.
71. Langdon CG, Capsey LJ, UK Study Group. Fluticasone propionate and budesonide in adult asthmatics: a comparison using dry-powder inhaler devices. Br J Clin Res 1994; 5: 85-99.
72. Lorentzen KA, Van Helmond JL, Bauer K, Langaker KE, Bonifazi F, Harris TA. Fluticasone propionate 1 mg daily and beclomethasone dipropionate 2 mg daily: a comparison over 1 year. Respir Med 1996; 90: 609-617.
73. Barnes NC, Hallett C, Harris TAJ. An overview of morning peak expiratory flow rate (PEFR) for clinical trials comparing fluticasone propionate (FP) with budesonide (BUD). Eur Respir J 1996; 9 (Suppl. 23): 52S-53S.
74. Dahl R, Lundbäck B, Malo JM, Mazza JA, Nieminen MM, Saarelainen P, Barnacle H on behalf of an International Study Group. A dose-ranging study of fluticasone propionate in adult patients with moderate asthma. Chest 1993; 104: 1352-1358.
75. Ayres JG, Bateman ED, Lundbäck B, Harris TAJ, on behalf of an International Study Group. High dose fluticasone propionate 1 mg daily, versus fluticasone propionate 2mg daily or budesonide 1.6mg daily in patients with severe chronic asthma. Eur Respir J 1995; 8: 579-586.
76. Dahl R, Ringdal N, Ward SM, Stampone P, Donnell D. Equivalence of asthma control with new CFC-free formulation HFA-134a beclomethasone dipropionate and CFC-beclomethasone dipropionate. Br J Clin Pract 1997; 51: 11-15.
77. Vanden Bürgt J, Donnell D, Stampone P, Dockhorn R. Efficacy of HFA-134a beclomethasone dipropionate (BDP), a new CFC-free formulation. Am J Respir Crit Care Med 1995; 151: A60.
78. Busse W. Improving steroid dose response: is respired dose the key? Presented at the European Respiratory Society, Berlin, 1997.
79. Busse W, Colice G, Hannon S, Madison WI. CFCBDP requires 2.6 times the dose to achieve equivalent improvement in FEV1 as HFA-BDP. Am J Respir Crit Care Med 1998; 157: A405.
80. Busse W, Schmitt K, Colice G. Improved asthma symptom control with 100 meg/day HFA-BDP but not with 100 meg/day CFC-BDP. Am J Respir Crit Care Med 1998; 157: A405.
81. Busse W, Colice G, Donnell D, Hannon S. A doseresponse dose-comparison of HFA-BDP and CFCBDP based on FEV, and FEF25_75/o. Presented at the European Respiratory Society, Geneva, 1998.
82. Davies RJ, Stampone P, O'Connor BJ. HFA-134a beclomethasone dipropionate extrafine aerosol provides equivalent asthma control to CFC beclomethasone dipropionate at approximately half the total daily dose. Respir Med 1998; 92 (Suppl. A): 23-31.
83. Gross G, Thompson P, Chervinsky P, Vanden Bürgt J, the Study Group. HFA-134a BDP 400 fig as effective as CFC-BDP 800 fig for the treatment of moderate asthma. Chest 1998; (in press).
84. Magnussen H for the Comparative Inhaled Steroid Investigation Group. In moderate stable asthma 400 meg/day beclomethasone dipropionate delivered by metered dose inhaler (MDI) with HFA-134a propellant is as effective as 1000 meg/day BDP inhaled from MDI containing CFC. Presented at European Respiratory Society Meeting, Geneva, September, 1998.
85. Hampel F, Vanden Bürgt J, Stampone P. HFAbeclomethasone dipropionate (HFA-BDP) is effective at improving asthma at doses as low as 50 meg twice daily. J Allergy Clin Immunol 1998; 101: Abs 274.
86. Thompson P, Davies RJ, Young WF, Grossman AB, Donnell D. Safety of HFA-134a beclomethasone dipropionate extrafine aerosol. Respir Med 1998; 92 (Suppl. A): 33-39.
87. Brown PH, Matusiewicz SP, Shearing C, Tibi L, Greening AP, Crompton GK. Systemic effects of high dose inhaled steroids: comparison of beclomethasone dipropionate and budesonide in healthy subjects. Thorax 1993; 48: 967-973.
88. Grove A, McFarlane LC, Jackson CM, Lipworth BJ. Effects of short term exposure to inhaled corticosteroids on novel biochemical markers of bone metabolism. Eur J Clin Pharmacol 1996; 50: 275-277.
89. Hanania NA, Chapman KR, Sturtridge WC, Szalai JP, Kesten S. Dose-related decrease in bone density among asthmatic patients treated with inhaled corticosteroids. J Allergy Clin Immunol 1995; 96: 571-579.
90. Boulet LP, Giguere MC, Milot J, Brown J. Effects of long-term use of high-dose inhaled steroids on bone density and calcium metabolism. J Allergy Clin Immunol 1994; 94: 796-803.
91. Toogood JH, Sorva R, Puolijoki H. Review of the effects of inhaled steroid therapy on bone. Int J Risk Safety Med 1994; 5: 1-14.
92. Toogood JH, Hodsman A, Baskerville J, Markov A. Vertebral bone mineral density (VBMD) among .elderly men and women receiving long-term inhaled (I-S) or oral steroids (O-S) for asthma. J Allergy Clin Immunol 1995; 95: 310.
93. Hanania NA, Chapman KR, Kesten S. Adverse effects of inhaled corticosteroids. Am J Med 1995; 98: 196-208.
94. Capewell S, Reynold S, Shuttleworth D, Edwards C, Finlay AY. Purpura and dermal thinning associated with high dose inhaled corticosteroids. Br MedJ 1990; 300: 1548-1551.
95. Mak VHP, Melchor R, Spiro SG. Easy bruising as a side-effect of inhaled corticosteroids. Eur Respir J 1992; 5: 1068-1074.
96. Blaiss MS, Herrod HG, Crawford LV, Lieberman PL. Beclomethasone dipropionate aerosol: hématologie and immunologie effects. Ann Allergy 1982; 48: 210-214.
97. Evans PM, O'Connor BJ, Fuller RW, Barnes PJ, Fan Chung K. Effects of inhaled corticosteroids on peripheral eosinophil counts and density profiles in asthma. J Allergy Clin Immunol 1993; 91: 643-650.
98. Zeitlin SR, Crowley S, Hindmarsh PC, Brook CGD. Inhaled corticosteroids and growth. Eur Respir Rev 1993; 3: 333-337.
99. Allen DB, Müllen M, Müllen B. A meta-analysis of the effect of oral and inhaled corticosteroids on growth. J Allergy Clin Immunol 1994; 93: 967-976.
100. Neville RG, McCowan C, Thomas G, Crombie IK. Asthma and growth-cause for concern? Asthma & growth in Tayside children. Ann Hum Biol 1996; 23: 323-331.
101. Rand CS, Wise RA, Nides M, et al. Metered-dose inhaler adherence in a clinical trial. Am Rev Respir Dis 1992; 146: 1559-1564.
102. Mawhinney H, Spector SL, Kinsman RA, Siegel SC, Rachelefsky GS, Katz RM, Rohr AS. Compliance in clinical trials of two nonbronchodilator, antiasthma medications. Ann Allergy 1991; 66: 294-299.
103. Duncan C (ed.) MIMS Monthly Index of Medical Specialties. Asthma preparations and breath-actuated inhalers. London: Haymarket Publishing Services, 1998.
104. Chief Medical Officer. Propellant changes in metereddose inhalers. CMO's Update 17. London, Department of Health, February 1998.