.png)
.png)
Послать статью по эл. почте 
Клиническая фармакология рофлумиласта
https://doi.org/10.18093/0869-0189-2012-0-2-90-98
Аннотация
Клиническая фармакология рофлумиласта.
Об авторе
В. В. АрхиповРоссия
д. м. н., проф. кафедры клинической фармакологии и пропедевтики внутренних болезней
109249, Москва, ул. Яузская, 11, корп. 5. Тел.: +7-903-966-54-14.
Список литературы
1. Jeon Y., Heo Y., Kim C. et al. Phosphodiesterase: overview of protein structures, potential therapeutic applications and recent progress in drug development. Cell. Mol. Life Sci. 2005; 62 (11): 1198–1220.
2. Boswell*Smith V., Spina D., Page C.P. Phosphodiesterase inhibitors. Br. J. Pharmacol. 2006; 147: S252–S257.
3. Uckert S., Kuthe A., Stief C.G., Jonas U. Phosphodiesterase isoenzymes as pharmacological targets in the treatment of male erectile dysfunction. Wld J. Urol. 2001; 19: 14–22.
4. McIvor R.A. Future options for disease intervention: important advances in phosphodiesterase 4 inhibitors. Eur. Respir. Rev. 2007; 16 (105): 105–112.
5. Wang P., Wu P., Ohleth K.M. et al. Phosphodiesterase 4B2 is the predominant phosphodiesterase species and undergoes differential regulation of gene expression in human monocytes and neutrophils. Mol. Pharmacol. 1999; 56: 170–174.
6. Erdogan S., Houslay M.D. Challenge of human Jurkat T-cells with the adenylate cyclase activator forskolin elicits major changes in cAMP phosphodiesterase (PDE) expression by up-regulating PDE3 and inducing PDE4D1 and PDE4D2 splice variants as well as down-regulating a novel PDE4A splice variant. Biochem. J. 2003; 321 (Pt 1): 165–175.
7. Mehats C., Jin S.L., Wahlstrom J. et al. PDE4D plays a critical role in the control of airway smooth muscle contraction. FASEB J. 2003; 17: 1831–1841.
8. Giembycz M.A. Cilomilast: a second generation phosphodiesterase 4 inhibitor for asthma and chronic obstructive pulmonary disease. Exp. Opin. Invest. Drugs 2001; 10: 1361–1379.
9. Jin S.L., Conti M. Induction of the cyclic nucleotide phosphodiesterase PDE4B is essential for LPS-activated TNF-alpha responses. Proc. Natl Acad. Sci. USA 2002; 99: 7628–7633.
10. Robichaud A., Stamatiou P.B., Jin S.L. et al. Deletion of phosphodiesterase 4D in mice shortens alpha(2)-adrenoceptor- mediated anaesthesia, a behavioural correlate of emesis. J. Clin. Invest. 2002; 110: 1045–1052.
11. Wang D., Cui X. Evaluation of PDE4 inhibition for COPD. Int. J. Chron. Obstruct. Pulm. Dis. 2006; 1 (4): 373–379.
12. LeadDiscovery. 2006. Phosphodiesterase 4 (PDE4) & phosphodiesterase 5 (PDE5) inhibitors [online]. Accessed 16 June 2006. URL: http://www.leaddiscovery.co.uk/reports/Phosphodiesterase*library.html
13. Hatzelmann A., Morcillo E.J., Lungarella G. et. al. The preclinical pharmacology of roflumilast – a selective, oral phosphodiesterase 4 inhibitor in development for chronic obstructive pulmonary disease. Pulm. Pharmacol. Ther. 2010; 23: 235–256.
14. Bethke T.D., Böhmer G.M., Hermann R. et al. Dose-proportional intraindividual single- and repeated-dose pharmacokinetics of roflumilast, an oral, once-daily phosphodiesterase 4 inhibitor. J. Clin. Pharmacol. 2007; 47: 26–36.
15. Lahu G., Hünnemeyer A., Diletti E. et al. Population pharmacokinetic modelling of roflumilast and roflumilast N-Oxide by total phosphodiesterase 4 inhibitory activity and development of a population pharmacodynamicadverse event model. Clin. Pharmacokinet. 2010; 49: 589–606.
16. Nassr N., Lahu G., Hunnemeyer A. et al. Magnesium hydroxide / aluminium hydroxide-containing antacid does not affect the pharmacokinetics of the targeted phosphodiesterase 4 inhibitor roflumilast. J. Clin. Pharmacol. 2007; 47: 660–666.
17. Lahu G., Hunnemeyer A., Herzog R. et al. Effect of repeated dose of erythromycin on the pharmacokinetics of roflumilast and roflumilast N-oxide. Int. J. Clin. Pharmacol. Ther. 2009; 47: 236–245.
18. Lahu G., Hünnemeyer A., von Richter O. et al. Effect of single and repeated doses of ketoconazole on the pharmacokinetics of roflumilast and roflumilast N-oxide. J. Clin. Pharmacol. 2008; 48: 1339–1349.
19. Nassr N., Huennemeyer A., Herzog R. et al. Effects of rifampicin on the pharmacokinetics of roflumilast and roflumilast N-oxide in healthy subjects. Br. J. Clin. Pharmacol. 2009; 68: 580–587.
20. von Richter O., Lahu G., Hunnemeyer A. et al. Effect of fluvoxamine on the pharmacokinetics of roflumilast and roflumilast N-oxide. Clin. Pharmacokinet. 2007; 46: 613–622.
21. Ram F.S. Use of theophylline in chronic obstructive pulmonary disease: examining the evidence. Curr. Opin. Pulm. Med. 2006;12 (2): 132–139.
22. Bennett J.A., Thompson Coon I., Pavord P. et al. The airway effects of stopping regular oral theophylline in patients with asthma. Br. J. Clin. Pharmacol. 1998; 45: 402–404.
23. Boswell*Smith V., Cazzola M., Page C.P. Are phosphodiesterase 4 inhibitors just more theophylline? J. Allergy Clin. Immunol. 2006; 117 (6):1237–1243.
24. Profita M., Sala A., Bonanno A. et al. Chronic obstructive pulmonary disease and neutrophil infiltration: role of cigarette smoke and cyclooxygenase products. Am. J. Physiol. Lung Cell. Mol. Physiol. 2010; 298 (2): L261–L269.
25. Brightling C.E., Monteiro W., Ward R. et al. Sputum eosinophilia and short–term response to prednisolone in chronic obstructive pulmonary disease: a randomized controlled trial. Lancet 2000; 356: 1480–1485.
26. Tenor H., Hatzelmann A., Church M.K. et al. Effects of theophylline and rolipram on leukotriene C4 (LTC4) synthesis and chemotaxis of human eosinophils from normal and atopic subjects. Br. J. Pharmacol. 1996; 118: 1727–1235.
27. Grootendorst D.C., Gauw S.A., Verhoosel R.M. et al. Reduction in sputum neutrophil and eosinophil numbers by the PDE4 inhibitor roflumilast in patients with COPD. Thorax 2007; 62 (12): 1081–1087.
28. Jones N.A., Boswell*Smith V., Lever R., Page C.P. The eff ect of selective phosphodiesterase isoenzyme inhibition on neutrophil function in vitro. Pulm. Pharmacol. Ther. 2005; 18: 93–101.
29. Hidi R., Timmermans S., Liu E. et al. Phosphodiesterase and cyclic adenosine monophosphate-dependent inhibition of T-lymphocyte chemotaxis. Eur. Respir. J. 2000; 15: 342–349.
30. Au B.T., Teixeira M.M., Collins P.D., Williams T.J. Effect of PDE4 inhibitors on zymosan-induced IL-8 release from human neutrophils: synergism with prostanoids and salbutamol. Br. J. Pharmacol. 1998; 123: 1260–1266.
31. Cortijo J., Villagrasa V., Navarrete C. et al. Effects of SCA40 on human isolated bronchus and human polymorphonuclear leukocytes: comparison with rolipram, SKF94120 and levcromakalim. Br. J. Pharmacol. 1996; 119: 99–106.
32. Nadel J.A. Role of neutrophil elastase in hypersecretion during COPD exacerbations, and proposed therapies. Chest 2000; 117 (5, Suppl. 2): S386–S389.
33. Fitzgerald M.F., Spicer D., McAulay A.E. et al. Roflumilast butnot methylprednisolone inhibited cigarette smokeinduced pulmonary inflammation in guinea pigs. Eur. Respir. J. Suppl. 2006; 663s: P3850.
34. Barnes N.C., Qiu Y.S., Pavord I.D. et al. Antiinflammatory effects of salmeterol / fluticasone propionate in chronic obstructive lung disease. Am. J. Respir. Crit. Care Med. 2006; 173 (7): 736–743.
35. Confalonieri M., Mainardi E., Della Porta R. et al. Inhaled corticosteroids reduce neutrophilic bronchial inflammation in patients with chronic obstructive pulmonary disease. Thorax 1998; 53: 583–585.
36. Keatings V., Jatakanon A., Worsdell Y. et al. Effects of inhaled and oral glucocorticoids on inflammatory indices in asthma and COPD. Am. J. Respir. Crit. Care Med. 1997; 155: 548.
37. Leigh R., Pizzichini M.M., Morris M.M. et al. Stable COPD: predicting benefit from high-dose inhaled corticosteroid treatment. Eur. Respir. J. 2006; 27 (5): 964–971.
38. Barnes P.J., Adcock I.M. Glucocorticoid resistance in inflammatory diseases. Lancet 2009; 373: 1905–1917.
39. Lipworth B.J. Phosphodiesterase-4 inhibitors for asthma and chronic obstructive pulmonary disease. Lancet 2005; 365: 167–175.
40. Boszormenyi*Nagy G., Pieters W.R., Steffen H. et al. The effect of roflumilast treatment and subsequent withdrawal in patients with COPD [abstract]. Proc. Am. Thor. Soc. 2005; 2: A544.
41. Grootendorst D.C., Gauw S.A., Baan R. et al. Does a single dose of the phosphodieasterase 4 inhibitor, cilomilast (15 mg), induce bronchodilatation in patients with chronic obstructive pulmonary disease? Pulm. Pharmacol. Ther. 2003; 16: 115–120.
42. Calverley P., Pauwels R., Vestbo J. et al. Combined salmeterol and fluticasone in the treatment of chronic obstructive pulmonary disease: a randomised controlled trial. Lancet 2003; 361 (9356): 449–456.
43. Rabe K.F., Bateman E.D., O'Donnell D. et al. Roflumilast – an oral anti-inflammatory treatment for chronic obstructive pulmonary disease: a randomized controlled trial. Lancet 2005; 366: 563–571.
44. Nycomed data on file.
45. Calverley P.M., Sanchez*Toril F., McIvor A. et al. Effect of 1-year treatment with roflumilast in severe chronic obstructive pulmonary disease. Am. J. Respir. Crit. Care Med. 2007; 176: 154–161.
46. Calverley P.M., Rabe K.F., Goehring U.M. et al. Roflumilast in symptomatic chronic obstructive pulmonary disease: two randomised clinical trials. Lancet 2009; 374: 685–694.
47. Fabbri L.M., Calverley P.M.A., Izquierdo*Alonso J.L. et al. Roflumilast in moderate-to-severe chronic obstructive pulmonary disease treated with longacting bronchodilators: two randomised clinical trials. Lancet 2009; 374 (9691): 695–703.
48. Aaron S.D., Vandemheen K.L., Fergusson D. et al. Tiotropium in combination with placebo, salmeterol, or fluticasone-salmeterol for treatment of chronic obstructive pulmonary disease. Ann. Intern. Med. 2007; 146 (8): 545–555.
49. Casaburi R., Mahler D.A., Jones P.W. et al. A long-term evaluation of once-daily inhaled tiotropium in chronic obstructive pulmonary disease. Eur. Respir. J. 2002; 19: 217–224.
50. Burge P.S., Calverley P.M., Jones P.W. et al. Randomised, double blind, placebo controlled study of fluticasone propionate in patients with moderate to severe chronic obstructive pulmonary disease: the ISOLDE trial. Bг. Med. J. (Clin. Res. Ed.) 2000; 320 (7245): 1297–1303.
51. Vogelmeier C., Hederer B., Glaab T. et al. Tiotropium versus salmeterol for the prevention of exacerbations of COPD. N. Engl. J. Med. 2011; 364 (12): 1093–1103.
52. Chapman K.R., Rabe K.F. Efficacy and safety of roflumilast in patients with chronic obstructive pulmonary disease (COPD) concomitantly treated with tiotropium or salmeterol. Prim. Care Respir. J. 2010; 19: A12.
53. Rennard S.I., Calverley P.M., Goehring U.M. et al. Reduction of exacerbations by the PDE4 inhibitor roflumilast the importance of defining different subsets of patients with COPD. Respir. Res. 2011; 12: 18.
54. Bateman E.D., Rabe K.F., Calverley P.M. et al. Roflumilast with long-acting β2-agonists for COPD: influence of exacerbation history. Eur. Respir. J. 2011; 38 (3): 553–560.
55. Global Initiative for Chronic Obstructive Lung Disease. Global Strategy for the Diagnosis, Management and Prevention of Chronic Obstructive Pulmonary Disease (updated 2011). http://www.goldcopd.org
56. Mahler D., Wells C. Evaluation of clinical methods for rating dyspnea. Chest 1988; 93: 580–586.
57. Jones P.W., Harding G., Berry P. et al. Development and first validation of the COPD Assessment Test. Eur. Respir. J. 2009; 34 (3): 648–654.
58. Calverley P.M.A., Fabbri L.M., Rabe K.F., Mosberg H. Roflumilast in the treatment of COPD: a pooled safety analysis. In: Presented at the European Respiratory Society annual congress, Barcelona, Spain 18–22 Sept., 2010: Barcelona; 2010. Poster 4732.
59. Boswell*Smith V., Spina D. PDE4 inhibitors as potential therapeutic agents in the treatment of COPD-focus on roflumilast. Int. J. Chron. Obstruct. Pulm. Dis. 2007; 2: 121–129.
60. Rabe K.F. Update on roflumilast, a phosphodiesterase 4 inhibitor for the treatment of chronic obstructive pulmonary disease. Br. J. Pharmacol. 2011; 163 (1): 53–67.
61. Wouters E.F.M., Teichmann P., Brose M. et al. Effects of roflumilast, a phosphodiesterase 4 inhibitor, on body composition in chronic obstructive pulmonary disease. Am. J. Respir. Crit. Care Med. 2010; 181: A4473.
Дополнительные файлы
Для цитирования: Архипов В.В. Клиническая фармакология рофлумиласта. Пульмонология. 2012;(2):90-98. https://doi.org/10.18093/0869-0189-2012-0-2-90-98
For citation: Arkhipov V.V. Clinical pharmacology of roflumilast. Russian Pulmonology. 2012;(2):90-98. (In Russ.) https://doi.org/10.18093/0869-0189-2012-0-2-90-98
Обратные ссылки
- Обратные ссылки не определены.