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Клиническая фармакология сартанов: класс-эффект и фармакодинамические особенности препаратов
Клиническая фармакология сартанов: класс-эффект и фармакодинамические особенности препаратов
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Аннотация
Блокада ренин-ангиотензиновой системы (РАС) является одним из концептуальных решений в лечении пациентов с сердечно-сосудистой патологией. Показания к назначению относительно нового класса препаратов – сартанов, влияющих на функциональную активность РАС, пересматриваются и расширяются. Сартаны являются блокаторами рецепторов к ангиотензину II с выраженным гипотензивным класс-специфическим эффектом, обусловленным наличием имидазоловой группы в структуре соединений. Тем не менее существуют молекулярные различия между препаратами, что влияет не только на фармакокинетические характеристики, но и модулирует фармакодинамику, обеспечивает дополнительные, независимые от уровня снижения артериального давления органопротективные эффекты препаратов.
Ключевые слова: ренин-ангиотензиновая система, сартаны, блокаторы рецепторов к ангиотензину II, лозартан, эпросартан, валсартан, ирбесартан, кандесартан, телмисартан, олмесартан, азилсартан.
Key words: renin-angiotensin system, sartans, angiotensin II receptor blockers, losartan, eprosartan, valsartan, irbesartan, candesartan, telmisartan, olmesartan, azilsartan.
Ключевые слова: ренин-ангиотензиновая система, сартаны, блокаторы рецепторов к ангиотензину II, лозартан, эпросартан, валсартан, ирбесартан, кандесартан, телмисартан, олмесартан, азилсартан.
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Key words: renin-angiotensin system, sartans, angiotensin II receptor blockers, losartan, eprosartan, valsartan, irbesartan, candesartan, telmisartan, olmesartan, azilsartan.
Полный текст
Список литературы
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2. Brunner HR, Gavras H, Laragh JH et al. Angiotensin-II blockade in man by Sar1-Ala8-angiotensin II for understanding and treatment of high blood pressure. Lancet 1973; 2: 1045.
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7. Burnier M. Angiotensin II Type 1 Receptor Blockers. Circulation 2001; 103: 904–12.
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12. Azilsartan medoxomil (Edarbi) the eighth ARB. Med Lett Drugs Ther 2011; 16 (53): 1364.
13. Le MT, De Backer JP, Hunyady L et al. Ligand binding and functional properties of human angiotensin AT1 receptors in transiently and stably expressed CHO-K1 cells. Eur J Pharmacol 2005; 513 (1–2): 35–45.
14. Van Liefde I, Vauquelin G. Sartan-AT1 receptor interactions: in vitro evidence for insurmountable antagonism and inverse agonism. Mol Cell Endocrinol 2009; 302 (2): 237–43.
15. Bhuiyan MA, Ishiguro M, Hossain M et al. Binding sites of valsartan, candesartan and losartan with angiotensin II receptor 1 subtype by molecular modeling. Life Sci 2009; 85 (3, 4): 136.
16. Ojima M, Igata H, Tanaka M et al. In vitro antagonistic properties of a new angiotensin type 1 receptor blocker, azilsartan, in receptor binding and function studies. J Pharmacol Exp Ther 2011; 336 (3): 801–8.
17. Westerink J, Visseren F. Cardiovasc Pharmacological and non-pharmacological interventions to influence adipose tissue function. Cardiovasc Diabetol 2011; 10: 13.
18. Bangalore S. Angiotensin receptor blockers and risk of myocardial infarction: meta-analyses and trial sequential analyses of 147 020 patients from randomised trials. BMJ 2011; 342: d2234.
19. Ishii H, Tsukada T, Yoshida M. Angiotensin II Type-I Receptor Blocker, Candesartan, Improves Brachial-Ankle Pulse Wave Velocity Independent of Its Blood Pressure Lowering Effects in Type 2 Diabetes Patients. J Soc Int Med 2008; 47: 2013–8.
20. Izuhara Y, Sada T, Yanagisawa H et al. A novel Sartan derivative with very low angiotensin II type 1 receptor affinity protects the kidney in type 2 diabetic rats. Arterioscler Thromb Vasc Biol 2008; 28 (10): 1767–73.
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23. Matchar DB, McCrory DC, Orlando LA et al. Systematic review: comparative effectiveness of angiotensin-converting enzyme inhibitors and angiotensin II receptor blockers for treating essential hypertension. Ann Intern Med 2008; 148: 16.
24. Granger CB, McMurray JJ, Yusuf S et al. Effects of candesartan in patients with chronic heart failure and reduced left-ventricular systolic function intolerant to angiotensin-converting-enzyme inhibitors: the CHARM-Alternative trial. Lancet 2003; 362: 772.
25. Lee VC, Rhew DC, Dylan M et al. Meta-analysis: angiotensin-receptor blockers in chronic heart failure and high-risk acute myocardial infarction. Ann Intern Med 2004; 141: 693.
26. Eklind-Cervenka M, Benson L, Dahlström U et al. Association of candesartan vs losartan with all-cause mortality in patients with heart failure. JAMA 2011; 305: 175.
27. Weir RA, McMurray JJ, Puu M et al. Efficacy and tolerability of adding an angiotensin receptor blocker in patients with heart failure already receiving an angiotensin-converting inhibitor plus aldosterone antagonist, with or without a beta blocker. Findings from the Candesartan in Heart failure: Assessment of Reduction in Mortality and morbidity (CHARM)-Added trial. Eur J Heart Fail 2008; 10 (2): 157–63.
28. Drazner MH, Rame JE, Marino EK et al. Increased left ventricular mass is a risk factor for the development of a depressed left ventricular ejection fraction within five years: the Cardiovascular Health Study. J Am Coll Cardiol 2004; 43: 2207.
29. Klingbeil AU, Schneider M, Martus P et al. A meta-analysis of the effects of treatment on left ventricular mass in essential hypertension. Am J Med 2003; 115: 41.
30. Os I, Franco V, Kjeldsen SE et al. Effects of losartan in women with hypertension and left ventricular hypertrophy: results from the Losartan Intervention for Endpoint Reduction in Hypertension Study. Hypertension 2008; 51: 1103.
31. Cuspidi C, Negri F, Zanchetti A. Angiotensin II receptor blockers and cardiovascular protection: focus on left ventricular hypertrophy regression and atrial fibrillation prevention. Vasc Health Risk Manag 2008; 4: 67.
32. Yusuf S, Pfeffer MA, Swedberg K et al. Effects of candesartan in patients with chronic heart failure and preserved left-ventricular ejection fraction: the CHARM-Preserved Trial. Lancet 2003; 362: 777.
33. Yamashita T, Inoue H, Okumura K et al. Randomized trial of angiotensin II-receptor blocker vs. dihydropiridine calcium channel blocker in the treatment of paroxysmal atrial fibrillation with hypertension (J-RHYTHM II study). Europace 2011; 13 (4): 473–9.
34. Tissot AC, Maurer P, Nussberger J et al. Effect of immunisation against angiotensin II with CYT006-AngQb on ambulatory blood pressure: a double-blind, randomised, placebo-controlled phase IIa study. Lancet 2008; 371: 821.
2. Brunner HR, Gavras H, Laragh JH et al. Angiotensin-II blockade in man by Sar1-Ala8-angiotensin II for understanding and treatment of high blood pressure. Lancet 1973; 2: 1045.
3. Bergsma DJ, Ellis C, Kumar C et al. Cloning and characterization of a human angiotensin II type 1 receptor. Biochem Biophys Res Commun 1992; 183: 989–95.
4. Леонова М.В., Белоусов Ю.Б., Штейнберг Л.Л. и др. Фармакоэпидемиология артериальной гипертонии в России (по результатам фармакоэпидемиологического исследования ПИФАГОР III. Рос. кардиол. журн. 2011; 2: 9–17.
5. Dzau VJ, Sasamura H, Hein L. Heterogeneity of angiotensin synthetic pathways and receptor subtypes: physiological and pharmacological implications. J Hypertens 1993; 11 (Suppl. 3): S13–S22.
6. Urata K, Kinoshita A, Misono K et al. Identification of a highly specific chymase as the major angiotensin-forming enzyme in the human heart. J Biol Chem 1990; 265: 22348–82.
7. Burnier M. Angiotensin II Type 1 Receptor Blockers. Circulation 2001; 103: 904–12.
8. Ohkubo N, Matsubara H, Nozawa Y et al. Angiotensin type 2 receptors are re-expressed by cardiac fibroblasts from failing myopathic hamster hearts and inhibit cell growth and fibrillar collagen metabolism. Circulation 1997; 96: 3954–62.
9. Ritter JM. Angiotensin converting enzyme inhibitors and angiotensin receptor blockers in hypertension. BMJ 2011; 342: d1673 doi: 10.1136/bmj.d1673.
10. Miura S, Karnik S and Saku K. Review: Angiotensin II type 1 receptor blockers: class effects versus molecular effects. J Renin-Angiotensin-Aldosterone Syst 2011; 12: 1.
11. Doulton T, He F and MacGregor G. MacGregor Angiotensin Receptor Blockade in Hypertension. Systematic Review of Combined Angiotensin-Converting Enzyme Inhibition and Angiotensin Receptor Blockade in Hypertension. Hypertension 2005; 45: 880–6.
12. Azilsartan medoxomil (Edarbi) the eighth ARB. Med Lett Drugs Ther 2011; 16 (53): 1364.
13. Le MT, De Backer JP, Hunyady L et al. Ligand binding and functional properties of human angiotensin AT1 receptors in transiently and stably expressed CHO-K1 cells. Eur J Pharmacol 2005; 513 (1–2): 35–45.
14. Van Liefde I, Vauquelin G. Sartan-AT1 receptor interactions: in vitro evidence for insurmountable antagonism and inverse agonism. Mol Cell Endocrinol 2009; 302 (2): 237–43.
15. Bhuiyan MA, Ishiguro M, Hossain M et al. Binding sites of valsartan, candesartan and losartan with angiotensin II receptor 1 subtype by molecular modeling. Life Sci 2009; 85 (3, 4): 136.
16. Ojima M, Igata H, Tanaka M et al. In vitro antagonistic properties of a new angiotensin type 1 receptor blocker, azilsartan, in receptor binding and function studies. J Pharmacol Exp Ther 2011; 336 (3): 801–8.
17. Westerink J, Visseren F. Cardiovasc Pharmacological and non-pharmacological interventions to influence adipose tissue function. Cardiovasc Diabetol 2011; 10: 13.
18. Bangalore S. Angiotensin receptor blockers and risk of myocardial infarction: meta-analyses and trial sequential analyses of 147 020 patients from randomised trials. BMJ 2011; 342: d2234.
19. Ishii H, Tsukada T, Yoshida M. Angiotensin II Type-I Receptor Blocker, Candesartan, Improves Brachial-Ankle Pulse Wave Velocity Independent of Its Blood Pressure Lowering Effects in Type 2 Diabetes Patients. J Soc Int Med 2008; 47: 2013–8.
20. Izuhara Y, Sada T, Yanagisawa H et al. A novel Sartan derivative with very low angiotensin II type 1 receptor affinity protects the kidney in type 2 diabetic rats. Arterioscler Thromb Vasc Biol 2008; 28 (10): 1767–73.
21. Mancia G, De Backer G, Dominiczak A et al. 2007 ESH-ESC Practice Guidelines for the Management of Arterial Hypertension: ESH-ESC Task Force on the Management of Arterial Hypertension. J Hypertens.
22. Чазова И.Е., Ратова Л.Г., Бойцов С.А., Небиеридзе Д.В. (рабочая группа). Диагностика и лечение артериальной гипертензии (Рекомендации Российского медицинского общества по артериальной гипертонии и Всероссийского научного общества кардиологов). Системные гипертензии. 2010; 3: 5–27.
23. Matchar DB, McCrory DC, Orlando LA et al. Systematic review: comparative effectiveness of angiotensin-converting enzyme inhibitors and angiotensin II receptor blockers for treating essential hypertension. Ann Intern Med 2008; 148: 16.
24. Granger CB, McMurray JJ, Yusuf S et al. Effects of candesartan in patients with chronic heart failure and reduced left-ventricular systolic function intolerant to angiotensin-converting-enzyme inhibitors: the CHARM-Alternative trial. Lancet 2003; 362: 772.
25. Lee VC, Rhew DC, Dylan M et al. Meta-analysis: angiotensin-receptor blockers in chronic heart failure and high-risk acute myocardial infarction. Ann Intern Med 2004; 141: 693.
26. Eklind-Cervenka M, Benson L, Dahlström U et al. Association of candesartan vs losartan with all-cause mortality in patients with heart failure. JAMA 2011; 305: 175.
27. Weir RA, McMurray JJ, Puu M et al. Efficacy and tolerability of adding an angiotensin receptor blocker in patients with heart failure already receiving an angiotensin-converting inhibitor plus aldosterone antagonist, with or without a beta blocker. Findings from the Candesartan in Heart failure: Assessment of Reduction in Mortality and morbidity (CHARM)-Added trial. Eur J Heart Fail 2008; 10 (2): 157–63.
28. Drazner MH, Rame JE, Marino EK et al. Increased left ventricular mass is a risk factor for the development of a depressed left ventricular ejection fraction within five years: the Cardiovascular Health Study. J Am Coll Cardiol 2004; 43: 2207.
29. Klingbeil AU, Schneider M, Martus P et al. A meta-analysis of the effects of treatment on left ventricular mass in essential hypertension. Am J Med 2003; 115: 41.
30. Os I, Franco V, Kjeldsen SE et al. Effects of losartan in women with hypertension and left ventricular hypertrophy: results from the Losartan Intervention for Endpoint Reduction in Hypertension Study. Hypertension 2008; 51: 1103.
31. Cuspidi C, Negri F, Zanchetti A. Angiotensin II receptor blockers and cardiovascular protection: focus on left ventricular hypertrophy regression and atrial fibrillation prevention. Vasc Health Risk Manag 2008; 4: 67.
32. Yusuf S, Pfeffer MA, Swedberg K et al. Effects of candesartan in patients with chronic heart failure and preserved left-ventricular ejection fraction: the CHARM-Preserved Trial. Lancet 2003; 362: 777.
33. Yamashita T, Inoue H, Okumura K et al. Randomized trial of angiotensin II-receptor blocker vs. dihydropiridine calcium channel blocker in the treatment of paroxysmal atrial fibrillation with hypertension (J-RHYTHM II study). Europace 2011; 13 (4): 473–9.
34. Tissot AC, Maurer P, Nussberger J et al. Effect of immunisation against angiotensin II with CYT006-AngQb on ambulatory blood pressure: a double-blind, randomised, placebo-controlled phase IIa study. Lancet 2008; 371: 821.
Авторы
Н.В.Захарова1, С.Р.Кузьмина-Крутецкая2
1 Кафедра терапии и клинической фармакологии Санкт-Петербургской медицинской академии последипломного образования;
2 Кафедра сердечно-сосудистой хирургии Санкт-Петербургской медицинской академии последипломного образования
1 Department of Therapy and Clinical Pharmacology, Saint Petersburg Medical Academy of Postgraduate Education;
2 Department of Cardiovascular Surgery, Saint Petersburg Medical Academy of Postgraduate Education
1 Кафедра терапии и клинической фармакологии Санкт-Петербургской медицинской академии последипломного образования;
2 Кафедра сердечно-сосудистой хирургии Санкт-Петербургской медицинской академии последипломного образования
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1 Department of Therapy and Clinical Pharmacology, Saint Petersburg Medical Academy of Postgraduate Education;
2 Department of Cardiovascular Surgery, Saint Petersburg Medical Academy of Postgraduate Education
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