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Антагонист кальция лерканидипин при артериальной гипертензии
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Ключевые слова: артериальная гипертензия, антигипертензивная терапия, антагонисты кальция, лерканидипин.
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The article presents the results of studies on the effectiveness and safety of a III generation calcium antagonist lercanidipine in the treatment of hypertension. Lercanidipine treatment leads to a marked significant reduction in systolic and diastolic blood pressure without producing a significant effect on heart rate. The drug has organ-protective effect, reduces left ventricular hypertrophy, improves kidney function and has antiproteinuric action. Lercanidipine is well tolerated, less likely to cause peripheral edema compared with other calcium antagonists.
Key words: hypertension, antihypertensive therapy, calcium antagonists, lercanidipine.
2. Mancia G, Fagard R, Narkiewicz K et al. Practice guidelines for the management of arterial hypertension of the European Society of Hypertension (ESH) and the European Society of Cardiology (ESC): ESH/ESC Task Force for the Management of Arterial Hypertension. J Hypertens 2013; 31: 1925–38.
3. James PA, Oparil S, Carter BL et al. Evidence-Based Guideline for the Management of High Blood Pressure in Adults: Report Fr om the Panel Members Appointed to the Eighth Joint National Committee (JNC 8). JAMA 2014; 311: 507–20.
4. Angeli F et al. Calcium channel blockade to prevent stroke in hypertension: a meta-analysis of 13 studies with 103 793 subjects. Am J Hypertens 2004; 17 (9): 817–22.
5. Angelico P, Guarneri L, Leonardi A et al. Vascular-selective effect of lercanidipine and other 1,4-dihydropyridines in isolated rabbit tissues. J Pharmacol 1999; 51: 709–14.
6. Herbette LG, Vecchiarelli M, Sartani A, Leonardi A. Lercanidipine: Short Plasma Half-Life, Long Duration of Action and High Cholesterol Tolerance. Updated Molecular Model to Rationalize its Pharmacokinetic Properties. Blood Pres Suppl 1998; 2: 10–7.
7. 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): 95–100.
8. Fogari R, Mugellini A, Zoppi A et al. Differential effects of lercanidipine and nifedipine GITS on plasma norepinephrine in chronic treatment of hypertension. Am J Hypertens 2003; 16 (7): 596–9.
9. Bang LM, Chapman TM, Goa KL. Lercanidipine: a review of its efficacy in the management of hypertension. Drugs 2003; 63: 2449–72.
10. 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): S31–35.
11. Cavallini A. 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): 477–87.
12. De Giorgio LA, Orlandini F, Malasoma P et al. Double-blind, crossover study of lercanidipine versus amlodipine in the treatment of mild-to-moderate essential hypertension. Curr Ther Res 1999; 60: 511–20.
13. Zanchetti A. Emerging data on calcium-channel blockers: the COHORT study. Clin Cardiol 2003; 26 (Suppl. 2): II 17–20.
14. Sironi G, Colombo D, Greto L et al. Regional vasodilating effects of lercanipine in dogs. ISHR XVI World Congress 1998.
15. Sabbatini M, Tomassoni D, Amenta F. Influence of treatment with Ca2+ antagonistis on cerebral vasculature of spontaneously hypertensive rats. Mechanisms of Ageing and Development 2001; 122: 795–809.
16. Leonetti G. The safety profile of antihypertensive drugs as the key factor for the achievement of blood pressure control: current experience with lercanidipine. High Blood Press 8; р. 92–101.
17. Barrios V, Escobar C, De la Figuera M et al. High doses of lercanidipine are better tolerated than other dihydropyridines in hypertensive patients with metabolic syndrome: results from the TOLERANCE study. Int J Clin Pract 2008; 62 (5): 723–8.
18. 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: 203–12.
19. Marx A, Lichtenthal A, Milbredt C et al. Effect of anthypertensive therapy with a new third generation calcium antagonist lercanidipine on patients with concomitant diseases. J Hypertens 2004; 22 (Suppl. 2): S236.
20. Barrios V, Calderon A, Navarro A et al. Lercanidipine effectiveness and tolerability profile is not influenced by overweight or body fat increase. The LERZAMIG study. J Hypertens 2004; 17 (9): 823–7.
21. Sangiorgi BG, Putignano E, Calcara L, Barbagallo M. Efficacy and tolerability of lercanidipine vs. captopril in patients with mild to moderate hypertension in a double-blind controlled study. J Cardiovasc Pharmacol 1997; 29 (Suppl. 2): S36–S39.
22. Morisco C, Trimarco B. Efficacy and tolerability of lercanidipine in comparison and in combination with atenolol in patients with mild to moderate hypertension in double-blind controlled study. J Cardiovasc Pharmacol 1997; 29 (Suppl. 2): S26–S30.
23. Aranda P, Aranda FT, Bianchi JL et al. Therapeutic efficacy and tolerability of lercanidipine versus candesartan, alone or in combination, in mild-moderate essential hypertensives (abstract). J Hypertens 2000; 18 (Suppl. 2): S152.
24. Fogari R, Mugellini A, Corradi L et al. Efficacy of lercanidipinevs losartan on left ventricular hypertrophy in hypertensive type 2 diabetic patients (abstract P1.191). J Hypertens 2000; 18 (Suppl. 2): S65.
25. Sanchez 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 Amsterdam 1999.
26. Dworkin Ld. Effects of calcium channel blockers on experimental glomerular injury. J Am Soc Nephrol 1990; 1: S21–27.
27. Viberti G. Microalbuminuria Reduction With Valsartan in Patients With Type 2 Diabetes Mellitus: A Blood Pressure – Independent Effect. Wheeldon and for the Microalbuminuria Reduction WithVALsartan (MARVAL) Study Investigators. Circulation 2002; 106: 672–8.
28. Kloke HJ et al. Meta-analysis of changes in albuminuria and arterial pressure in hypertensive patients with proteinuria in studies wh ere patients received nifedipine, any other DHP CCB, a non-DHP CCB, or an ACE inhibitor. Kidney Int 1998; 53: 1559–73.
29. Herlitz H, Harris K, Risler T et al. The effects of an ACE inhibitor and a calcium antagonist on the progression of renal disease: the Nephros Study. Nephrol Dial Transplant 2001; 16: 2158–65.
30. DallaVestra M, Pozza G, Mosca A et al. Effect of lercanidipine compared with ramipril on albumin excretion rate in hypertensive Type 2 diabetic patients with microalbuminuria: DIAL study (diabete, ipertensione, albuminuria, lercanidipina). Diabetes Nutr Metab 2004; 17 (5): 259–66.
31. 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.
32. Sabbatini M, Leonardi A, Testa R et al. Effect of calcium antagonists on glomerular arteriolesin spontaneously hypertensive rats. Hypertension 2000; 35 (3): 775–9.
33. Cafiero M, Giasi M. Long-term (12-month) treatment with lercanidipine in patients with mild to moderate hypertension. J Cardiovasc Pharmacol 1997; 29 (Suppl. 2): S45–49.
34. Borghi C, Prandin MG, Dormi A. The use of lercanidipine can improve the individual tolerability to dihydropyridine calcium blockers in hypertensive patients (abstract). J Hypertens 2000; 18 (Suppl. 2): S155.
35. Fogari R, Malamani GD, Zoppi A et al. Comparative effect of lercanidipine and nifedipine gastrointestinal therapeutic system on ankle volume and subcutaneous interstitial pressure in hypertensive patients: a double-blind, randomized, parallel-group study. Curr Ther Res 2000; 61 (12): 850–62.
36. Lund-Johansen P, Stranden E, Helberg S et al. Quantification of leg oedema in postmenopausal hypertensive patients treated with lercanidipine or amlodipine. J Hypertens 2003; 21: 1003–10.
37. Rengo F, Romis L. Activity of lercanidipine in double-blind comparison with nitrendipine in combination treatment of resistant essential hypertension. J Cardiovasc Pharmacol 1997; 29 (Suppl. 2): S54–58.
38. Marx A, Lichtenthal A, Milbredt C et al. Effect of anthypertensive therapy with a new third generation calcium antagonist lercanidipine on patients with concomitant diseases. J Hypertens 2004; 22 (Suppl. 2): S236.
39. Sironi G, Montagna E, Greto L et al. Haemodynamic effects of lercanidipine in anaesthetized open-chest dogs. Arzneim-Forsch Drug Res 1996; 46: 256–61.
40. Specchia G, Saccaggi SP, Ghezzi C. Cardiovascular safety of lercanidipine in patients with angina pectoris: a review of six randomized clinical trials. Curr Ther Res 2001; 62: 3–15.
41. Ortiz M, Calcino G. Inferred mortality differences between dihydropyridine antihypertensives. Hypertension 2009; 53: 1116.
42. Mackenzie IS, Carmel M, McEniery CM et al. Comparison of the Effects of Antihypertension Agents on Central Blood pressure and Arterial Stiffness in Isolated Systolic Hypertension. Hypertension 2009; 54: 409–13.
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1. Рекомендации РМОАГ/ВНОК по диагностике и лечению артериальной гипертонии (четвертый пересмотр). 2010.
2. Mancia G, Fagard R, Narkiewicz K et al. Practice guidelines for the management of arterial hypertension of the European Society of Hypertension (ESH) and the European Society of Cardiology (ESC): ESH/ESC Task Force for the Management of Arterial Hypertension. J Hypertens 2013; 31: 1925–38.
3. James PA, Oparil S, Carter BL et al. Evidence-Based Guideline for the Management of High Blood Pressure in Adults: Report Fr om the Panel Members Appointed to the Eighth Joint National Committee (JNC 8). JAMA 2014; 311: 507–20.
4. Angeli F et al. Calcium channel blockade to prevent stroke in hypertension: a meta-analysis of 13 studies with 103 793 subjects. Am J Hypertens 2004; 17 (9): 817–22.
5. Angelico P, Guarneri L, Leonardi A et al. Vascular-selective effect of lercanidipine and other 1,4-dihydropyridines in isolated rabbit tissues. J Pharmacol 1999; 51: 709–14.
6. Herbette LG, Vecchiarelli M, Sartani A, Leonardi A. Lercanidipine: Short Plasma Half-Life, Long Duration of Action and High Cholesterol Tolerance. Updated Molecular Model to Rationalize its Pharmacokinetic Properties. Blood Pres Suppl 1998; 2: 10–7.
7. 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): 95–100.
8. Fogari R, Mugellini A, Zoppi A et al. Differential effects of lercanidipine and nifedipine GITS on plasma norepinephrine in chronic treatment of hypertension. Am J Hypertens 2003; 16 (7): 596–9.
9. Bang LM, Chapman TM, Goa KL. Lercanidipine: a review of its efficacy in the management of hypertension. Drugs 2003; 63: 2449–72.
10. 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): S31–35.
11. Cavallini A. 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): 477–87.
12. De Giorgio LA, Orlandini F, Malasoma P et al. Double-blind, crossover study of lercanidipine versus amlodipine in the treatment of mild-to-moderate essential hypertension. Curr Ther Res 1999; 60: 511–20.
13. Zanchetti A. Emerging data on calcium-channel blockers: the COHORT study. Clin Cardiol 2003; 26 (Suppl. 2): II 17–20.
14. Sironi G, Colombo D, Greto L et al. Regional vasodilating effects of lercanipine in dogs. ISHR XVI World Congress 1998.
15. Sabbatini M, Tomassoni D, Amenta F. Influence of treatment with Ca2+ antagonistis on cerebral vasculature of spontaneously hypertensive rats. Mechanisms of Ageing and Development 2001; 122: 795–809.
16. Leonetti G. The safety profile of antihypertensive drugs as the key factor for the achievement of blood pressure control: current experience with lercanidipine. High Blood Press 8; р. 92–101.
17. Barrios V, Escobar C, De la Figuera M et al. High doses of lercanidipine are better tolerated than other dihydropyridines in hypertensive patients with metabolic syndrome: results from the TOLERANCE study. Int J Clin Pract 2008; 62 (5): 723–8.
18. 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: 203–12.
19. Marx A, Lichtenthal A, Milbredt C et al. Effect of anthypertensive therapy with a new third generation calcium antagonist lercanidipine on patients with concomitant diseases. J Hypertens 2004; 22 (Suppl. 2): S236.
20. Barrios V, Calderon A, Navarro A et al. Lercanidipine effectiveness and tolerability profile is not influenced by overweight or body fat increase. The LERZAMIG study. J Hypertens 2004; 17 (9): 823–7.
21. Sangiorgi BG, Putignano E, Calcara L, Barbagallo M. Efficacy and tolerability of lercanidipine vs. captopril in patients with mild to moderate hypertension in a double-blind controlled study. J Cardiovasc Pharmacol 1997; 29 (Suppl. 2): S36–S39.
22. Morisco C, Trimarco B. Efficacy and tolerability of lercanidipine in comparison and in combination with atenolol in patients with mild to moderate hypertension in double-blind controlled study. J Cardiovasc Pharmacol 1997; 29 (Suppl. 2): S26–S30.
23. Aranda P, Aranda FT, Bianchi JL et al. Therapeutic efficacy and tolerability of lercanidipine versus candesartan, alone or in combination, in mild-moderate essential hypertensives (abstract). J Hypertens 2000; 18 (Suppl. 2): S152.
24. Fogari R, Mugellini A, Corradi L et al. Efficacy of lercanidipinevs losartan on left ventricular hypertrophy in hypertensive type 2 diabetic patients (abstract P1.191). J Hypertens 2000; 18 (Suppl. 2): S65.
25. Sanchez 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 Amsterdam 1999.
26. Dworkin Ld. Effects of calcium channel blockers on experimental glomerular injury. J Am Soc Nephrol 1990; 1: S21–27.
27. Viberti G. Microalbuminuria Reduction With Valsartan in Patients With Type 2 Diabetes Mellitus: A Blood Pressure – Independent Effect. Wheeldon and for the Microalbuminuria Reduction WithVALsartan (MARVAL) Study Investigators. Circulation 2002; 106: 672–8.
28. Kloke HJ et al. Meta-analysis of changes in albuminuria and arterial pressure in hypertensive patients with proteinuria in studies wh ere patients received nifedipine, any other DHP CCB, a non-DHP CCB, or an ACE inhibitor. Kidney Int 1998; 53: 1559–73.
29. Herlitz H, Harris K, Risler T et al. The effects of an ACE inhibitor and a calcium antagonist on the progression of renal disease: the Nephros Study. Nephrol Dial Transplant 2001; 16: 2158–65.
30. DallaVestra M, Pozza G, Mosca A et al. Effect of lercanidipine compared with ramipril on albumin excretion rate in hypertensive Type 2 diabetic patients with microalbuminuria: DIAL study (diabete, ipertensione, albuminuria, lercanidipina). Diabetes Nutr Metab 2004; 17 (5): 259–66.
31. 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.
32. Sabbatini M, Leonardi A, Testa R et al. Effect of calcium antagonists on glomerular arteriolesin spontaneously hypertensive rats. Hypertension 2000; 35 (3): 775–9.
33. Cafiero M, Giasi M. Long-term (12-month) treatment with lercanidipine in patients with mild to moderate hypertension. J Cardiovasc Pharmacol 1997; 29 (Suppl. 2): S45–49.
34. Borghi C, Prandin MG, Dormi A. The use of lercanidipine can improve the individual tolerability to dihydropyridine calcium blockers in hypertensive patients (abstract). J Hypertens 2000; 18 (Suppl. 2): S155.
35. Fogari R, Malamani GD, Zoppi A et al. Comparative effect of lercanidipine and nifedipine gastrointestinal therapeutic system on ankle volume and subcutaneous interstitial pressure in hypertensive patients: a double-blind, randomized, parallel-group study. Curr Ther Res 2000; 61 (12): 850–62.
36. Lund-Johansen P, Stranden E, Helberg S et al. Quantification of leg oedema in postmenopausal hypertensive patients treated with lercanidipine or amlodipine. J Hypertens 2003; 21: 1003–10.
37. Rengo F, Romis L. Activity of lercanidipine in double-blind comparison with nitrendipine in combination treatment of resistant essential hypertension. J Cardiovasc Pharmacol 1997; 29 (Suppl. 2): S54–58.
38. Marx A, Lichtenthal A, Milbredt C et al. Effect of anthypertensive therapy with a new third generation calcium antagonist lercanidipine on patients with concomitant diseases. J Hypertens 2004; 22 (Suppl. 2): S236.
39. Sironi G, Montagna E, Greto L et al. Haemodynamic effects of lercanidipine in anaesthetized open-chest dogs. Arzneim-Forsch Drug Res 1996; 46: 256–61.
40. Specchia G, Saccaggi SP, Ghezzi C. Cardiovascular safety of lercanidipine in patients with angina pectoris: a review of six randomized clinical trials. Curr Ther Res 2001; 62: 3–15.
41. Ortiz M, Calcino G. Inferred mortality differences between dihydropyridine antihypertensives. Hypertension 2009; 53: 1116.
42. Mackenzie IS, Carmel M, McEniery CM et al. Comparison of the Effects of Antihypertension Agents on Central Blood pressure and Arterial Stiffness in Isolated Systolic Hypertension. Hypertension 2009; 54: 409–13.
ФГБУ Учебно-научный медицинский центр Управления делами Президента Российской Федерации
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G.A.Baryshnikova, S.A.Chorbinskaya, I.I.Stepanova
Educational Research Medical Center, Office of the President of the Russian Federation