Выбор блокаторов кальциевых каналов при артериальной гипертензии. Фармакокинетические и фармакодинамические механизмы высокой селективности и сверхдлительности действия лерканидипина
Выбор блокаторов кальциевых каналов при артериальной гипертензии. Фармакокинетические и фармакодинамические механизмы высокой селективности и сверхдлительности действия лерканидипина
Морозова Т.Е., Вартанова О.А. Выбор блокаторов кальциевых каналов при артериальной гипертензии. Фармакокинетические и фармакодинамические механизмы высокой селективности и сверхдлительности действия лерканидипина. Consilium Medicum. 2017; 19 (12): 59–65. DOI: 10.26442/2075-1753_19.12.59-65
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Morozova T.E., Vartanova O.A. Choice of calcium channel blockers in arterial hypertension. Pharmacokinetic and pharmacodynamic mechanisms of high selectivity and superlative action of lercanidipine.. Consilium Medicum. 2017; 19 (12): 59–65. DOI: 10.26442/2075-1753_19.12.59-65
Выбор блокаторов кальциевых каналов при артериальной гипертензии. Фармакокинетические и фармакодинамические механизмы высокой селективности и сверхдлительности действия лерканидипина
Морозова Т.Е., Вартанова О.А. Выбор блокаторов кальциевых каналов при артериальной гипертензии. Фармакокинетические и фармакодинамические механизмы высокой селективности и сверхдлительности действия лерканидипина. Consilium Medicum. 2017; 19 (12): 59–65. DOI: 10.26442/2075-1753_19.12.59-65
________________________________________________
Morozova T.E., Vartanova O.A. Choice of calcium channel blockers in arterial hypertension. Pharmacokinetic and pharmacodynamic mechanisms of high selectivity and superlative action of lercanidipine.. Consilium Medicum. 2017; 19 (12): 59–65. DOI: 10.26442/2075-1753_19.12.59-65
В обзоре представлены данные об эффективности, плейотропных эффектах и безопасности нового блокатора кальциевых каналов лерканидипина в лечении артериальной гипертензии. Препарат является высокоселективным липофильным блокатором L-каналов, длительность действия обеспечивается его медленным накоплением в билипидных мембранах клеток, что не вызывает активации симпатоадреналовой системы. Лерканидипин обладает органопротективным действием, уменьшает гипертрофию левого желудочка, улучшает функцию почек и оказывает антипротеинурическое действие, имеет хороший профиль безопасности, реже вызывает периферические отеки по сравнению с другими дигидропиридинами, хорошо сочетается с приемом других препаратов.
The review presents data on the efficacy, pleiotropic effects and safety of a new lercanidipine calcium channel blocker in the treatment of hypertension. This medicine is the high-selective lipophilic blocker of L-channels, duration of action is provided by its slow accumulation in the bilipid cell membranes, that does not cause activating of the sympathoadrenal system. Lercanidipine possesses an organoprotective effect, diminishes the hypertrophy of the left ventricle, improves the kidney function, has anantiproteinuric effect, has a good profile of safety, rarely causes peripheral edema as compared to other dihydropyridines, and is well combined with the intake of other medicines.
1. 2013 ESH/ESC Guidelines for the management of arterial hypertension. J Hypertension 2013; 1281–13.
2. Toyo-Oka T, Nayler WG. Third generation calcium entry blockers. Blood Press 1996; 5: S206–8.
3. Epstein M. Role of a third generation calcium antagonists in the management of hypertension. Drugs 1999; 57 (Suppl. 1): S1–10.
4. Morisco C, Trimarco B. Efficacy and tolerability of lercanidipine in comparison to and in combination with atenolol in patients with mild to moderate hypertension in a double blind controlled study. J Cardiovasc Pharmacol 1997; 29 (Suppl. 2): S26–30.
5. Barchielli M, Dolfini E, Farina P et al. Clinical pharmacokinetics of lercanidipine. J Cardiovascul Pharmacol 1997; 29 (Suppl. 2): S1–S15.
6. Fogari R, Mugellini A, Corradi L et al. Efficacy of lercanidipine vs losartan on left ventricular hypertrophy in hypertensive type 2 diabetic patients [abstract no. P1.191]. J Hypertens 2000; 18 (Suppl. 2): S65.
7. Macchiarulo C, Pieri R, Mitolo DC et al. Antihypertensive effects of six calcium antagonists: evidence from Fourier analysis of 24-hour ambulatory blood pressure recordings. Curr Ther Res 2001; 62 (4): S236–253.
8. McClellan KJ, Jarvis B. Lercanidipine. A review of its use in hypertension. Drugs 2000; 60 (5): 1123–40.
9. Licher ThF, Cosebtino F. The classification of calcium antagonists and their selection in the treatment of hypertension. Drugs 1998; 55 (4): S309–17.
10. Triggle DJ. Mechanisms of action of calcium channel antagonists. In: Calcium antagonists in clinical medicine. Ed. by M.Epstein. Philadelphia 1998; S1–26.
11. Herbette LG, Vecchiarelli M, Leonardi A. Lercanidipine: Short plasma half-life, long duration of action. J Cardiovascul Pharmacol 1997; 29 (Suppl. 1): S19–S24.
12. Van Zweiten PA, Pfaffendorf M. Pharmacology of dihydropyridine calcium antagonists; Relatiomship between lipophilicity and pharmacodynamic response. J Hypertension 1993; 11 (Suppl. 6): S3–S11.
13. S’anchez A, Sayans R, Alvarez JL et al. Left ventricular hypertrophy regression after a short antihypertensive treatment with lercanidipine vs. enalapril [abstract №12]. Fourth European Meeting on Calcium Antagonists; 1999 Oct 27–29; Amsterdam.
14. Bang LM, Chapman TM, Goa KL. (New Zealand.) Лерканидипин: обзор эффективности в терапии артериальной терапии. Drugs 2003; 63 (22): 2449–72. / Bang LM, Chapman TM, Goa KL. (New Zealand.) Lerkanidipin: obzor effektivnosti v terapii arterial'noi terapii. Drugs 2003; 63 (22): 2449–72. [in Russian]
15. Barrios V, Navarro A, Esteras A et al. Antihypertensive efficacy and tolerability of lercanidipine in daily clinical practice. The ELYPSE study. Blood Press 2002; 11 (2): S95–100.
16. Policicchio D, Magliocca R, Malliani A. Efficacy and tolerability of lercanidipine in patients with mild to moderate essential hypertension: a comparative study with slow-release nifedipine. J Cardiovasc Pharmacol 1997; 29 (Suppl. 2): S31–5.
17. Romito R, Pansini MI, Perticone F et al. Comparative effect of oflercandipine, felodipine and nifedipine GITS on blood pressure and heart rate in patients with mild to moderate arterial hypertension: the Lercandipine in Adults (LEAD) study. J Clin Hypertens 2003; 5 (4): S249–53.
18. Paterna S, Licata A, Arnone S et al. Lercanidipine in two different dosage regimens as a sole treatment for severe essential hypertension. J Cardiovasc Pharmacol 1997; 29 (Suppl. 2): S50–3.
19. James IGV, Jones A, Davies P. A randomised, double-blind, double-dummy comparison of the efficacy and tolerability of lercanidipine tablets and losartan tablets in patients with mild to moderate essential hypertension. J Hum Hypertens 2002; 16 (8): S605–10.
20. Barrios V, Escobar C, de la Figuera M et al. High doses of lercanidipineare better tolerated than other dihydropyridines in hypertensivepatients with metabolic syndrome: results from the TOLERANCE study. Int J Clin Pract 2008; 62 (5): 723–8.
21. Barbagallo M, Sangiorgi GB. Efficacy and tolerability of lercanidipine in monotherapy in elderly patients with isolated systolic hypertension. Aging Clin Exp Res 2000; 12 (5): 375–9.
22. Nayler WG. Amlodipine. Berlin, 1995; p. 1–273.
23. Robles NR, Ocon J, Gomez CF et al. Lercanidipine in patients with chronic renal failure: the ZAFRA study. Ren Fail 2005; 27 (1): 73–80.
24. Robles NR, Romero B et al. Treatment of Proteinuria with Lercanidipine Associated with Renin-Angiotensin Axis-Blocking Drugs. Ren Fail 2010; 32 (2): 192–7.
25. Acanfora D, Trojano L, Gheorghiade M et al. A randomized, double-blind comparison of 10 and 20 mg lercanidipine in patients with stable effort angina: effects on myocardial ischemia and heart rate variability. Am J Ther 2002; 9 (5): S444–53.
26. Cherubini A, Fabris F, Ferrari E et al. Comparative effects of lercanidipine, lacidipine and nifidepine GITS on blood pressure and heart rate in elderly hypertensive patients: the ELderly and LErcanidipine (ELLE) study. Arch Gerontol Geriatr 2003; 3: S203–12.
27. Martinez ML, Castro MM, Rizzi E et al. Lercanidipine reduces matrix metalloproteinase-2 activity and reverses vascular dysfunction in renovascular hypertensive rate. Int J Clin Pract 2008: 65 (2): 723–8.
28. 31 Wu JR, Liou SF, Lin SW et al. Lercanidipine inhibits vascular smooth muscle cell proliferation and neointimal formation via reducing intracellurlar reactive oxygen species and inactivating Ras-ERK1/2 signaling. Pharmacol Res 2009; 59 (1): 48–56.
29. Sironi G, Colombo D, Greto L et al. Regional vasodilating effect of lercanidipine in dogs. ISHR XVI World Congress, 1998.
30. Sabbatini M, Tomassoni D, Amenta P. Influence of effect of treatment with Ca2+ antagonists on cerebral vasculature of spontaneously hypertensive rats. Mech Ageing Dev 2001; 122 (8): 795–809.
31. De Ciuceis C, Salvetti M, Rossini C et al. Effect of antihypertensive treatment on microvascular structure, central blood pressure and oxidative stress in patients with mild essential hypertension. J Hypertens 2014; 32 (2): 565–74.
32. Macchiarulo C, Pieri R, Mitolo DC et al. Antihypertensive effects of six calcium antagonists: evidence from Fourier analysis of 24-hour ambulatory blood pressure recordings. Curr Ther Res 2001; 62 (4): S236–53.
33. Cavallini A, Terzi G. Effects of antihypertensive therapy with lercanidipine and verapamil on cardiac electrical activity in patients with hypertension: a randomized, double-blind pilot study. Curr Ther Res 2000; 61 (7): S477–87.
________________________________________________
1. 2013 ESH/ESC Guidelines for the management of arterial hypertension. J Hypertension 2013; 1281–13.
2. Toyo-Oka T, Nayler WG. Third generation calcium entry blockers. Blood Press 1996; 5: S206–8.
3. Epstein M. Role of a third generation calcium antagonists in the management of hypertension. Drugs 1999; 57 (Suppl. 1): S1–10.
4. Morisco C, Trimarco B. Efficacy and tolerability of lercanidipine in comparison to and in combination with atenolol in patients with mild to moderate hypertension in a double blind controlled study. J Cardiovasc Pharmacol 1997; 29 (Suppl. 2): S26–30.
5. Barchielli M, Dolfini E, Farina P et al. Clinical pharmacokinetics of lercanidipine. J Cardiovascul Pharmacol 1997; 29 (Suppl. 2): S1–S15.
6. Fogari R, Mugellini A, Corradi L et al. Efficacy of lercanidipine vs losartan on left ventricular hypertrophy in hypertensive type 2 diabetic patients [abstract no. P1.191]. J Hypertens 2000; 18 (Suppl. 2): S65.
7. Macchiarulo C, Pieri R, Mitolo DC et al. Antihypertensive effects of six calcium antagonists: evidence from Fourier analysis of 24-hour ambulatory blood pressure recordings. Curr Ther Res 2001; 62 (4): S236–253.
8. McClellan KJ, Jarvis B. Lercanidipine. A review of its use in hypertension. Drugs 2000; 60 (5): 1123–40.
9. Licher ThF, Cosebtino F. The classification of calcium antagonists and their selection in the treatment of hypertension. Drugs 1998; 55 (4): S309–17.
10. Triggle DJ. Mechanisms of action of calcium channel antagonists. In: Calcium antagonists in clinical medicine. Ed. by M.Epstein. Philadelphia 1998; S1–26.
11. Herbette LG, Vecchiarelli M, Leonardi A. Lercanidipine: Short plasma half-life, long duration of action. J Cardiovascul Pharmacol 1997; 29 (Suppl. 1): S19–S24.
12. Van Zweiten PA, Pfaffendorf M. Pharmacology of dihydropyridine calcium antagonists; Relatiomship between lipophilicity and pharmacodynamic response. J Hypertension 1993; 11 (Suppl. 6): S3–S11.
13. S’anchez A, Sayans R, Alvarez JL et al. Left ventricular hypertrophy regression after a short antihypertensive treatment with lercanidipine vs. enalapril [abstract №12]. Fourth European Meeting on Calcium Antagonists; 1999 Oct 27–29; Amsterdam.
14. Bang LM, Chapman TM, Goa KL. (New Zealand.) Лерканидипин: обзор эффективности в терапии артериальной терапии. Drugs 2003; 63 (22): 2449–72. / Bang LM, Chapman TM, Goa KL. (New Zealand.) Lerkanidipin: obzor effektivnosti v terapii arterial'noi terapii. Drugs 2003; 63 (22): 2449–72. [in Russian]
15. Barrios V, Navarro A, Esteras A et al. Antihypertensive efficacy and tolerability of lercanidipine in daily clinical practice. The ELYPSE study. Blood Press 2002; 11 (2): S95–100.
16. Policicchio D, Magliocca R, Malliani A. Efficacy and tolerability of lercanidipine in patients with mild to moderate essential hypertension: a comparative study with slow-release nifedipine. J Cardiovasc Pharmacol 1997; 29 (Suppl. 2): S31–5.
17. Romito R, Pansini MI, Perticone F et al. Comparative effect of oflercandipine, felodipine and nifedipine GITS on blood pressure and heart rate in patients with mild to moderate arterial hypertension: the Lercandipine in Adults (LEAD) study. J Clin Hypertens 2003; 5 (4): S249–53.
18. Paterna S, Licata A, Arnone S et al. Lercanidipine in two different dosage regimens as a sole treatment for severe essential hypertension. J Cardiovasc Pharmacol 1997; 29 (Suppl. 2): S50–3.
19. James IGV, Jones A, Davies P. A randomised, double-blind, double-dummy comparison of the efficacy and tolerability of lercanidipine tablets and losartan tablets in patients with mild to moderate essential hypertension. J Hum Hypertens 2002; 16 (8): S605–10.
20. Barrios V, Escobar C, de la Figuera M et al. High doses of lercanidipineare better tolerated than other dihydropyridines in hypertensivepatients with metabolic syndrome: results from the TOLERANCE study. Int J Clin Pract 2008; 62 (5): 723–8.
21. Barbagallo M, Sangiorgi GB. Efficacy and tolerability of lercanidipine in monotherapy in elderly patients with isolated systolic hypertension. Aging Clin Exp Res 2000; 12 (5): 375–9.
22. Nayler WG. Amlodipine. Berlin, 1995; p. 1–273.
23. Robles NR, Ocon J, Gomez CF et al. Lercanidipine in patients with chronic renal failure: the ZAFRA study. Ren Fail 2005; 27 (1): 73–80.
24. Robles NR, Romero B et al. Treatment of Proteinuria with Lercanidipine Associated with Renin-Angiotensin Axis-Blocking Drugs. Ren Fail 2010; 32 (2): 192–7.
25. Acanfora D, Trojano L, Gheorghiade M et al. A randomized, double-blind comparison of 10 and 20 mg lercanidipine in patients with stable effort angina: effects on myocardial ischemia and heart rate variability. Am J Ther 2002; 9 (5): S444–53.
26. Cherubini A, Fabris F, Ferrari E et al. Comparative effects of lercanidipine, lacidipine and nifidepine GITS on blood pressure and heart rate in elderly hypertensive patients: the ELderly and LErcanidipine (ELLE) study. Arch Gerontol Geriatr 2003; 3: S203–12.
27. Martinez ML, Castro MM, Rizzi E et al. Lercanidipine reduces matrix metalloproteinase-2 activity and reverses vascular dysfunction in renovascular hypertensive rate. Int J Clin Pract 2008: 65 (2): 723–8.
28. 31 Wu JR, Liou SF, Lin SW et al. Lercanidipine inhibits vascular smooth muscle cell proliferation and neointimal formation via reducing intracellurlar reactive oxygen species and inactivating Ras-ERK1/2 signaling. Pharmacol Res 2009; 59 (1): 48–56.
29. Sironi G, Colombo D, Greto L et al. Regional vasodilating effect of lercanidipine in dogs. ISHR XVI World Congress, 1998.
30. Sabbatini M, Tomassoni D, Amenta P. Influence of effect of treatment with Ca2+ antagonists on cerebral vasculature of spontaneously hypertensive rats. Mech Ageing Dev 2001; 122 (8): 795–809.
31. De Ciuceis C, Salvetti M, Rossini C et al. Effect of antihypertensive treatment on microvascular structure, central blood pressure and oxidative stress in patients with mild essential hypertension. J Hypertens 2014; 32 (2): 565–74.
32. Macchiarulo C, Pieri R, Mitolo DC et al. Antihypertensive effects of six calcium antagonists: evidence from Fourier analysis of 24-hour ambulatory blood pressure recordings. Curr Ther Res 2001; 62 (4): S236–53.
33. Cavallini A, Terzi G. Effects of antihypertensive therapy with lercanidipine and verapamil on cardiac electrical activity in patients with hypertension: a randomized, double-blind pilot study. Curr Ther Res 2000; 61 (7): S477–87.
Авторы
Т.Е.Морозова*, О.А.Вартанова
ФГАОУ ВО «Первый Московский государственный медицинский университет им. И.М.Сеченова» Минздрава России. 119991, Россия, Москва, ул. Трубецкая, д. 8, стр. 2 *temorozova@gmail.com
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T.E.Morozova*, O.A.Vartanova
I.M.Sechenov First Moscow State Medical University of the Ministry of Health of the Russian Federation. 119991, Russian Federation, Moscow, ul. Trubetskaia, d. 8, str. 2 *temorozova@gmail.com