Lercanidipine – noteworthy calcium antagonist Review article
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Published:
Jun 30, 2023
Keywords:
calcium antagonists, lercanidipine, hypertension, therapy
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Abstract
Hypertension remains globally one of the key clinical problem associated with elevated risk of cardiovascular morbidity and mortality. The effective therapy has been still a challenge in contemporary medicine. Several strategies as well as new drugs with improved tolerance are proposed in order to increase patients compliance and endurance on hypotensive therapy. Lercanidipine is one of a newer calcium antagonists with potent antihypertensive activity and a good safety profile on long-term use. The paper focuses no most important clinical features specifically on high effectiveness of lercanidipine in longer term therapy of patients with hypertension. Some important pleiotropic effects of lercanidipine are pointed out that makes the drug particularly recommended in therapy of patients with chronic kidney disease. Finally, the paper summarizes available research documenting outstanding tolerance of lercanidipine that enables the widespread use of the drug in therapy of hypertensive patients.
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How to Cite
Rozentryt, P. (2023). Lercanidipine – noteworthy calcium antagonist. Medycyna Faktow (J EBM), 16(2(59), 183-194. https://doi.org/10.24292/01.MF.0223.09
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References
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10. Hsu PF, Cheng HM, Wu CH et al. High Short-Term Blood Pressure Variability Predicts Long-Term Cardiovascular Mortality in Untreated Hypertensives But Not in Normotensives. Am J Hypertens. 2016; 29(7): 806-13.
11. Del Pinto R, Pietropaoli D, Dobre M et al. Prognostic importance of long-term SBP variability in high-risk hypertension. J Hypertens. 2020; 38(11): 2237-44.
12. Colbourne L, Harrison PJ. Brain-penetrant calcium channel blockers are associated with a reduced incidence of neuropsychiatric disorders. Mol Psychiatry. 2022; 27(9): 3904-12.
13. Grassi G, Robles NR, Seravalle G et al. Lercanidipine in the Management of Hypertension: An Update. J Pharmacol Pharmacother. 2017; 8(4): 155-65.
14. Leonetti G, Magnani B, Pessina AC et al. Tolerability of long-term treatment with lercanidipine versus amlodipine and lacidipine in elderly hypertensives. Am J Hypertens. 2002; 15(11): 932-40.
15. 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): 236-53.
16. Barrios V, Navarro A, Esteras A et al. Antihypertensive efficacy and tolerability of lercanidipine in daily clinical practice. The ELYPSE Study. Eficacia de Lercanidipino y su Perfil de Seguridad. Blood Press. 2002; 11(2): 95-100.
17. Hart P, Bakris GL. Calcium antagonists: Do they equally protect against kidney injury? Kidney Int. 2008; 73(7): 795-6.
18. Taddei S, Virdis A, Ghiadoni L et al. Calcium antagonist treatment by lercanidipine prevents hyperpolarization in essential hypertension. Hypertension (Dallas, Tex : 1979). 2003; 41(4): 950-5.
19. Menne J, Park JK, Agrawal R et al. Cellular and molecular mechanisms of tissue protection by lipophilic calcium channel blockers. Faseb J. 2006; 20(7): 994-6.
20. 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(3): 565-74.
21. Canavesi M, Baldini N, Leonardi A et al. In vitro inhibitory effect of lercanidipine on cholesterol accumulation and matrix metalloproteinases secretion by macrophages. J Cardiovasc Pharmacol. 2004; 44(4): 416-22.
22. Farah R, Khamisy-Farah R, Shurtz-Swirski R. Calcium channel blocker effect on insulin resistance and inflammatory markers in essential hypertension patients. Int Angiol. 2013; 32(1): 85-93.
23. Wu JR, Liou SF, Lin SW et al. Lercanidipine inhibits vascular smooth muscle cell proliferation and neointimal formation via reducing intracellular reactive oxygen species and inactivating Ras-ERK1/2 signaling. Pharmacol Res. 2009; 59(1): 48-56.
24. Notarbartolo A, Rengo F, Scafidi V et al. Long-term effects of lercanidipine on the lipoprotein and apolipoprotein profile of patients with mild-to-moderate essential hypertension. Curr Ther Res. 1999; 60(4): 228-36.
25. Rachmani R, Levi Z, Zadok BS et al. Losartan and lercanidipine attenuate low-density lipoprotein oxidation in patients with hypertension and type 2 diabetes mellitus: a randomized, prospective crossover study. Clin Pharmacol Ther. 2002; 72(3): 302-7.
26. van Zwieten PA, Pfaffendorf M, Mancia G. Attempts to improve the selectivity of calcium antagonistic drugs. Blood Press Suppl. 1996; 5: 7-9.
27. Sabbatini M, Vitaioli L, Baldoni E et al. Nephroprotective effect of treatment with calcium channel blockers in spontaneously hypertensive rats. J Pharmacol Exp Ther. 2000; 294(3): 948-54.
28. Sabbatini M, Leonardi A, Testa R, Vitaioli L, Amenta F. Effect of Calcium Antagonists on Glomerular Arterioles in Spontaneously Hypertensive Rats. Hypertension (Dallas, Tex: 1979). 2000; 35(3): 775-9.
29. Cherubini A, Fabris F, Ferrari E et al. Comparative effects of lercanidipine, lacidipine, and nifedipine gastrointestinal therapeutic system on blood pressure and heart rate in elderly hypertensive patients: the ELderly and LErcanidipine (ELLE) study. Arch Gerontol Geriatr. 2003; 37(3): 203-12.
30. Barrios V, Escobar C, Calderón A et al. The effectiveness and tolerability of lercanidipine is independent of body mass index or body fat percent. The LERZAMIG study. Br J Cardiol. 2006; 13: 434-40.
31. Barrios V, Escobar C, Navarro A et al. Lercanidipine is an effective and well tolerated antihypertensive drug regardless the cardiovascular risk profile: The LAURA study. Int J Clin Pract. 2006; 60(11): 1364-70.
32. Klag MJ, Whelton PK, Randall BL et al. Blood Pressure and End-Stage Renal Disease in Men. N Engl J Med. 1996; 334(1): 13-8.
33. Yan P, Zhu X, Li H et al. Association of High Blood Pressure with Renal Insufficiency: Role of Albuminuria, from NHANES, 1999–2006. PLOS ONE. 2012; 7(7): e37837.
34. Dalla Vestra 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.
35. 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.
36. Robles NR, Calvo C, Sobrino J et al. Lercanidipine valuable effect on urine protein losses: the RED LEVEL study. Curr Med Res Opin. 2016; 32(sup2): 29-34.
37. Fici F, Ari Bakir E, Ilkay Yüce E et al. PAIT-Survey Follow-Up: Changes in Albuminuria in Hypertensive Diabetic Patients with Mild-Moderate Chronic Kidney Disease. High Blood Press Cardiovasc Prev. 2020; 27(1): 43-9.
38. Viazzi F, Muiesan ML, Schillaci G et al. Changes in albuminuria and cardiovascular risk under antihypertensive treatment: a systematic review and meta-regression analysis. J Hypertens. 2016; 34(9) 1689-97.
39. Makani H, Bangalore S, Romero J et al. Peripheral edema associated with calcium channel blockers: incidence and withdrawal rate – a meta- analysis of randomized trials. J Hypertens. 2011; 29(7): 1270-80.
40. Makarounas-Kirchmann K, Glover-Koudounas S, Ferrari P. Results of a meta-analysis comparing the tolerability of lercanidipine and other dihydropyridine calcium channel blockers. Clin Ther. 2009; 31(8): 1652-63.
41. Borghi C, Prandin MG, Dormi A et al. Improved tolerability of the dihydropyridine calcium-channel antagonist lercanidipine: the lercanidipine challenge trial. Blood Press Suppl. 2003; 1: 14-21.
42. Burnier M, Gasser UE. Efficacy and tolerability of lercanidipine in patients with hypertension: results of a Phase IV study in general practice. Expert Opin Pharmacother. 2007; 8(14): 2215-23.
2. Zamponi GW, Striessnig J, Koschak A et al. The Physiology, Pathology, and Pharmacology of Voltage-Gated Calcium Channels and Their Future Therapeutic Potential. Pharmacol Rev. 2015; 67(4): 821-70.
3. Tamargo J, Ruilope LM. Investigational calcium channel blockers for the treatment of hypertension. Expert Opin Investig Drugs. 2016; 25(11): 1295-309.
4. Greenberg RN. Overview of patient compliance with medication dosing: a literature review. Clin Ther. 1984; 6(5): 592-9.
5. Gupta P, Patel P, Štrauch B et al. Risk Factors for Nonadherence to Antihypertensive Treatment. Hypertension (Dallas, Tex : 1979). 2017; 69(6): 1113-20.
6. Tykarski A, Filipiak KJ, Januszewicz A et al. Zasady postępowania w nadciśnieniu tętniczym – 2019 rok. Wytyczne Polskiego Towarzystwa Nadciśnienia Tętniczego. Arterial Hypertension. 2019; 5(1): 1-88.
7. Tykarski A, Filipiak K, Januszewicz A et al. 2019 Guidelines for the Management of Hypertension – Part 1–7. Arterial Hypertension. 2019; 23(2): 41-87.
8. Barchielli M, Dolfini E, Farina P et al. Clinical Pharmacokinetics of Lercanidipine. J Cardiovasc Pharmacol. 1997; 29: S1-S15.
9. Cerbai E, Mugelli A. Lercanidipine and T-type calcium current. Eur Rev Med Pharmacol Sci. 2018; 22(12): 4025-31.
10. Hsu PF, Cheng HM, Wu CH et al. High Short-Term Blood Pressure Variability Predicts Long-Term Cardiovascular Mortality in Untreated Hypertensives But Not in Normotensives. Am J Hypertens. 2016; 29(7): 806-13.
11. Del Pinto R, Pietropaoli D, Dobre M et al. Prognostic importance of long-term SBP variability in high-risk hypertension. J Hypertens. 2020; 38(11): 2237-44.
12. Colbourne L, Harrison PJ. Brain-penetrant calcium channel blockers are associated with a reduced incidence of neuropsychiatric disorders. Mol Psychiatry. 2022; 27(9): 3904-12.
13. Grassi G, Robles NR, Seravalle G et al. Lercanidipine in the Management of Hypertension: An Update. J Pharmacol Pharmacother. 2017; 8(4): 155-65.
14. Leonetti G, Magnani B, Pessina AC et al. Tolerability of long-term treatment with lercanidipine versus amlodipine and lacidipine in elderly hypertensives. Am J Hypertens. 2002; 15(11): 932-40.
15. 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): 236-53.
16. Barrios V, Navarro A, Esteras A et al. Antihypertensive efficacy and tolerability of lercanidipine in daily clinical practice. The ELYPSE Study. Eficacia de Lercanidipino y su Perfil de Seguridad. Blood Press. 2002; 11(2): 95-100.
17. Hart P, Bakris GL. Calcium antagonists: Do they equally protect against kidney injury? Kidney Int. 2008; 73(7): 795-6.
18. Taddei S, Virdis A, Ghiadoni L et al. Calcium antagonist treatment by lercanidipine prevents hyperpolarization in essential hypertension. Hypertension (Dallas, Tex : 1979). 2003; 41(4): 950-5.
19. Menne J, Park JK, Agrawal R et al. Cellular and molecular mechanisms of tissue protection by lipophilic calcium channel blockers. Faseb J. 2006; 20(7): 994-6.
20. 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(3): 565-74.
21. Canavesi M, Baldini N, Leonardi A et al. In vitro inhibitory effect of lercanidipine on cholesterol accumulation and matrix metalloproteinases secretion by macrophages. J Cardiovasc Pharmacol. 2004; 44(4): 416-22.
22. Farah R, Khamisy-Farah R, Shurtz-Swirski R. Calcium channel blocker effect on insulin resistance and inflammatory markers in essential hypertension patients. Int Angiol. 2013; 32(1): 85-93.
23. Wu JR, Liou SF, Lin SW et al. Lercanidipine inhibits vascular smooth muscle cell proliferation and neointimal formation via reducing intracellular reactive oxygen species and inactivating Ras-ERK1/2 signaling. Pharmacol Res. 2009; 59(1): 48-56.
24. Notarbartolo A, Rengo F, Scafidi V et al. Long-term effects of lercanidipine on the lipoprotein and apolipoprotein profile of patients with mild-to-moderate essential hypertension. Curr Ther Res. 1999; 60(4): 228-36.
25. Rachmani R, Levi Z, Zadok BS et al. Losartan and lercanidipine attenuate low-density lipoprotein oxidation in patients with hypertension and type 2 diabetes mellitus: a randomized, prospective crossover study. Clin Pharmacol Ther. 2002; 72(3): 302-7.
26. van Zwieten PA, Pfaffendorf M, Mancia G. Attempts to improve the selectivity of calcium antagonistic drugs. Blood Press Suppl. 1996; 5: 7-9.
27. Sabbatini M, Vitaioli L, Baldoni E et al. Nephroprotective effect of treatment with calcium channel blockers in spontaneously hypertensive rats. J Pharmacol Exp Ther. 2000; 294(3): 948-54.
28. Sabbatini M, Leonardi A, Testa R, Vitaioli L, Amenta F. Effect of Calcium Antagonists on Glomerular Arterioles in Spontaneously Hypertensive Rats. Hypertension (Dallas, Tex: 1979). 2000; 35(3): 775-9.
29. Cherubini A, Fabris F, Ferrari E et al. Comparative effects of lercanidipine, lacidipine, and nifedipine gastrointestinal therapeutic system on blood pressure and heart rate in elderly hypertensive patients: the ELderly and LErcanidipine (ELLE) study. Arch Gerontol Geriatr. 2003; 37(3): 203-12.
30. Barrios V, Escobar C, Calderón A et al. The effectiveness and tolerability of lercanidipine is independent of body mass index or body fat percent. The LERZAMIG study. Br J Cardiol. 2006; 13: 434-40.
31. Barrios V, Escobar C, Navarro A et al. Lercanidipine is an effective and well tolerated antihypertensive drug regardless the cardiovascular risk profile: The LAURA study. Int J Clin Pract. 2006; 60(11): 1364-70.
32. Klag MJ, Whelton PK, Randall BL et al. Blood Pressure and End-Stage Renal Disease in Men. N Engl J Med. 1996; 334(1): 13-8.
33. Yan P, Zhu X, Li H et al. Association of High Blood Pressure with Renal Insufficiency: Role of Albuminuria, from NHANES, 1999–2006. PLOS ONE. 2012; 7(7): e37837.
34. Dalla Vestra 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.
35. 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.
36. Robles NR, Calvo C, Sobrino J et al. Lercanidipine valuable effect on urine protein losses: the RED LEVEL study. Curr Med Res Opin. 2016; 32(sup2): 29-34.
37. Fici F, Ari Bakir E, Ilkay Yüce E et al. PAIT-Survey Follow-Up: Changes in Albuminuria in Hypertensive Diabetic Patients with Mild-Moderate Chronic Kidney Disease. High Blood Press Cardiovasc Prev. 2020; 27(1): 43-9.
38. Viazzi F, Muiesan ML, Schillaci G et al. Changes in albuminuria and cardiovascular risk under antihypertensive treatment: a systematic review and meta-regression analysis. J Hypertens. 2016; 34(9) 1689-97.
39. Makani H, Bangalore S, Romero J et al. Peripheral edema associated with calcium channel blockers: incidence and withdrawal rate – a meta- analysis of randomized trials. J Hypertens. 2011; 29(7): 1270-80.
40. Makarounas-Kirchmann K, Glover-Koudounas S, Ferrari P. Results of a meta-analysis comparing the tolerability of lercanidipine and other dihydropyridine calcium channel blockers. Clin Ther. 2009; 31(8): 1652-63.
41. Borghi C, Prandin MG, Dormi A et al. Improved tolerability of the dihydropyridine calcium-channel antagonist lercanidipine: the lercanidipine challenge trial. Blood Press Suppl. 2003; 1: 14-21.
42. Burnier M, Gasser UE. Efficacy and tolerability of lercanidipine in patients with hypertension: results of a Phase IV study in general practice. Expert Opin Pharmacother. 2007; 8(14): 2215-23.