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Tiotropium Bromide

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Abstract

  • ▴ Tiotropium bromide is an anticholinergic bronchodilator that antagonises muscarinic M1, M2 and M3 receptors. It dissociates more slowly from M1 receptors and, importantly, from M3 receptors (which are located in bronchial smooth muscle) than from M2 receptors and subsequently has a long duration of action permitting once-daily administration.

  • ▴ In patients with chronic obstructive pulmonary disease (COPD), tiotropium 18μg once daily significantly improved lung function compared with placebo and ipratropium 40μg four times daily in 1-year trials or salmeterol 50μg twice daily in a 6-month study.

  • ▴ The incidence of COPD exacerbations decreased and use of rescue medication was lower with tiotropium compared with placebo or ipratropium. There was no evidence of tachyphylaxis during 1-year treatment with tiotropium.

  • ▴ Compared with placebo, salmeterol and ipratropium, tiotropium produced significant improvements in patients’ perception of dyspnoea and health-related quality of life.

  • ▴ Tiotropium is generally well tolerated; dry mouth is the most common drug-related adverse event, occurring in about 10 to 16% of patients in clinical trials.

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References

  1. The COPD Guidelines Group of the Standards of Care Committee of the BTS. BTS guidelines for the management of chronic obstructive pulmonary disease. Thorax 1997 Dec; 52 Suppl. 5: S1–S28

    Google Scholar 

  2. American Thoracic Society. Standards for the diagnosis and care of patients with chronic obstructive pulmonary disease. Am J Respir Crit Care Med 1995; 152: S77–120

    Google Scholar 

  3. Pauwels RA, Buist AS, Calverley PMA, et al. Global strategy for the diagnosis, management, and prevention of chronic obstructive pulmonary disease: NHLBI/WHO Global initiative for chronic Obstructive Lung Disease (GOLD) workshop summary. Am J Respir Crit Care Med 2001; 163: 1256–76

    PubMed  CAS  Google Scholar 

  4. Eglen RM, Hegde SS, Watson N. Muscarinic receptor subtypes and smooth muscle function. Pharmacol Rev 1996; 48(4): 531–65

    PubMed  CAS  Google Scholar 

  5. Haddad E-B, Mak JCW, Barnes PJ. Characterization of [3H]Ba 679 BR, a slowly dissociating muscarinic antagonist, in human lung: radioligand binding and autoradiographic mapping. Mol Pharmacol 1994 May; 45: 899–907

    PubMed  CAS  Google Scholar 

  6. Disse B, Reichl R, Speck G, et al. Ba 679 BR, a novel long-acting anticholinergic bronchodilator. Life Sci 1993; 52: 537–44

    Article  PubMed  CAS  Google Scholar 

  7. Takahashi T, Belvisi MG, Patel H, et al. Effect of Ba 679 BR, a novel long-acting anticholinergic agent, on cholinergic neurotransmission in guinea pig and human airways. Am J Respir Crit Care Med 1994 Dec; 150 (6 Pt 1): 1640–5

    PubMed  CAS  Google Scholar 

  8. Maesen FPV, Smeets JJ, Sledsens TJH, et al. Tiotropium bromide, a new long-acting antimuscarinic bronchodilator: a pharmacodynamic study in patients with chronic obstructive pulmonary disease (COPD). Eur Respir J 1995; 8: 1506–13

    PubMed  CAS  Google Scholar 

  9. Calverley PMA, Towse LJ, Lee A. The timing of dose and pattern of bronchodilatation of tiotropium (TIO) in stable COPD [abstract no. P523]. Eur Respir J 2000; 16 Suppl. 31: 56s

    Google Scholar 

  10. Hasani A, Agnew JE, Dilworth JP, et al. Effect of tiotropium on distribution pattern of aerosol particles deposited in the lung [abstract no. A98]. Am J Respir Crit Care Med 2001 Apr; 163 Suppl. Pt 2: A277

    Google Scholar 

  11. Hasani A, Agnew JE, Dilworth JP, et al. Effect of tiotropium on lung ventilatory distribution in COPD patients [abstract]. Am J Respir Crit Care Med 2001 Apr; 163 Suppl. Pt 2: 282

    Google Scholar 

  12. McNicholas WT, Calverley PMA, Edwards C, et al. Effects of anticholinergic therapy (tiotropium) on REM-related desaturation (SaO2) and sleep quality in patients with COPD [abstract]. Am J Respir Crit Care Med 2001 Apr; 163 Suppl. Pt 2: 280

    Google Scholar 

  13. Disse B, Speck GA, Rominger KL, et al. Tiotropium (Spiriva): mechanistical considerations and clinical profile in obstructive lung disease. Life Sci 1999; 64: 457–64

    Article  PubMed  CAS  Google Scholar 

  14. Disse B, Rominger K, Serby CW, et al. The pharmacokinetic (PK) profile of tiotropium during long-term treatment in stable COPD [abstract]. Am J Respir Crit Care Med 1999 Mar; 159 Suppl. Pt 2: A524

    Google Scholar 

  15. Vincken W, van Noord JA, Greefhorst APM, et al. Improved health outcomes in patients with COPD during 1 yr’s treatment with tiotropium. Eur Respir J 2002 Feb; 19(2): 200–16

    Article  Google Scholar 

  16. Littner MR, Ilowite JS, Tashkin DP, et al. Long-acting bronchodilation with once-daily dosing of tiotropium (Spiriva) in stable chronic obstructive pulmonary disease. Am J Respir Crit Care Med 2000 Apr; 161: 1136–42

    PubMed  CAS  Google Scholar 

  17. Casaburi R, Mahler DA, Jones PW, et al. A long-term evaluation of once-daily inhaled tiotropium in chronic obstructive pulmonary disease. Eur Respir J 2002 Feb; 19(2): 217–24

    Article  PubMed  CAS  Google Scholar 

  18. Donohue JF, van Noord JA, Bateman ED, et al. A 6-month placebo-controlled study comparing lung function and health status changes in COPD patients treated with tiotropium or salmeterol. Chest. In press

  19. San Pedro G, Elias DJ, Serby CW, et al. Tiotropium (Spiriva): one year bronchodilator efficacy established with once daily dosing in COPD patients [abstract]. Am J Respir Crit Care Med 2000 Mar; 161 Suppl. Part 2: 749

    Google Scholar 

  20. Zu Wallack R, Jones PW, Kotch A, et al. Tiotropium (Spiriva) improves health status in patients with COPD [abstract]. Am J Respir Crit Care Med 2000 Mar; 161 Suppl. Part 2: 892

    Google Scholar 

  21. Mahler DA, Montner P, Brazinsky SA, et al. Tiotropium (Spiriva), a new long-acting anticholinergic bronchodilator, improves dyspnea in patients with COPD [abstract]. Am J Respir Crit Care Med 2000 Mar; 161 Suppl. Part 2: 892

    Google Scholar 

  22. Casaburi R, Briggs Jr DD, Donohue JF, et al. The spirometric efficacy of once-daily dosing with tiotropium in stable COPD. Chest 2000; 118: 1294–302

    Article  PubMed  CAS  Google Scholar 

  23. Wanner A, ZuWallack R, Elias D, et al. Efficacy of once daily tiotropium (TIO) in stable COPD [abstract no. P3406]. Eur Respir Soc 1999 Oct 9

  24. van Noord JA, Bantje TA, Eland ME, et al. A randomised controlled comparison of tiotropium nd ipratropium in the treatment of chronic obstructive pulmonary disease. Dutch Tiotropium Study Group. Thorax 2000 Apr; 55: 289–94

    Article  PubMed  Google Scholar 

  25. Vincken W, Greefhorst APM, Westbroek J, et al. Once-daily tiotropium (TIO) is more efficacious than q.i.d. ipratropium (IB) as maintenance treatment of COPD [abstract no. P3407]. Eur Respir Soc 1999 Oct 9

  26. Vincken WG, Vermiere P, Menjoge SS, et al. Maintenance of bronchodilation following tiotropium in patients with mild, moderate and severe COPD in one year clinical trials [abstract no. P2202]. Eur Respir J Suppl 2001 Sep; 18 Suppl. 33: 331s

    Google Scholar 

  27. Kesten S, Flanders J, Menjoge SS, et al. Improvements in COPD following treatment with tiotropium in elderly patients [abstract]. Am J Respir Crit Care Med 2001 Apr; 163 (5) Suppl. Pt 2

  28. Weisman I, Menjoge SS, Serby CW, et al. Influence of gender on outcomes in large COPD clinical trials [abstract]. Am J Respir Crit Care Med 2001 Apr; 163(5) Suppl. Pt 2: A281

    Google Scholar 

  29. Vincken W, van Noord JA, Greefhorst APM, et al. Superior bronchodilator effects of tiotropium (TIO) vs. ipratropium (IB) in COPD over a one year clinical trial [abstract no. P516]. Eur Respir J 2000; 16 Suppl. 31: 55s

    Google Scholar 

  30. Kesten S, Flanders J, Serby CW, et al. Compliance with tiotropium, a once daily dry powder inhaled bronchodilator, in one year COPD trials. Chest 2000 Oct; 118 Suppl.: 191S–2S

    Google Scholar 

  31. Chodosh S, Flanders J, Serby CW, et al. Effective use of HandiHaler dry powder inhalation system over a range of COPD disease severity [abstract]. Am J Respir Crit Care Med 1999; 159 Suppl: A524

    Google Scholar 

  32. Jones PW, Quirk FH, Baveystock CM, et al. A self-complete measure of health status for chronic airflow limitation. The St. George’s Respiratory Questionnaire. Am Rev Respir Dis 1992; 145: 1321–7

    PubMed  CAS  Google Scholar 

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  1. Adis International Limited, 41 Centorian Drive, Private Bag 65901, Mairangi Bay, Auckland 10, New Zealand

    Karen M. Hvizdos & Karen L. Goa

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  1. Karen M. Hvizdos
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  2. Karen L. Goa
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Correspondence to Karen L. Goa.

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Hvizdos, K.M., Goa, K.L. Tiotropium Bromide. Drugs 62, 1195–1203 (2002). https://doi.org/10.2165/00003495-200262080-00008

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