Lercanidipine (Rec 15/2375): A Novel 1,4‐Dihydropyridine Calcium Antagonist for Hypertension
1997; Wiley; Volume: 15; Issue: 3 Linguagem: Italiano
10.1111/j.1527-3466.1997.tb00331.x
ISSN1527-3466
AutoresR. Testa, Amedeo Leonardi, A Tajana, E. Riscassi, R Magliocca, A. Sartani,
Tópico(s)Synthesis and biological activity
ResumoCardiovascular Drug ReviewsVolume 15, Issue 3 p. 187-219 Free Access Lercanidipine (Rec 15/2375): A Novel 1,4-Dihydropyridine Calcium Antagonist for Hypertension R. Testa, Corresponding Author R. Testa Pharmaceutical R&D Division, Recordati S.p.A., Milano, ItalyPlease address correspondence and reprint requests to Dr. R. Testa, Pharmaceutical R&D Division, Recordati S.p.A., Via Civitali 1, 20148 Milano, Italy. Fax: 39-2-48-70-9017.Search for more papers by this authorA. Leonardi, A. Leonardi Pharmaceutical R&D Division, Recordati S.p.A., Milano, ItalySearch for more papers by this authorA. Tajana, A. Tajana Pharmaceutical R&D Division, Recordati S.p.A., Milano, ItalySearch for more papers by this authorE. Riscassi, E. Riscassi Pharmaceutical R&D Division, Recordati S.p.A., Milano, ItalySearch for more papers by this authorR. Magliocca, R. Magliocca Pharmaceutical R&D Division, Recordati S.p.A., Milano, ItalySearch for more papers by this authorA. Sartani, A. Sartani Pharmaceutical R&D Division, Recordati S.p.A., Milano, ItalySearch for more papers by this author R. Testa, Corresponding Author R. Testa Pharmaceutical R&D Division, Recordati S.p.A., Milano, ItalyPlease address correspondence and reprint requests to Dr. R. Testa, Pharmaceutical R&D Division, Recordati S.p.A., Via Civitali 1, 20148 Milano, Italy. Fax: 39-2-48-70-9017.Search for more papers by this authorA. Leonardi, A. Leonardi Pharmaceutical R&D Division, Recordati S.p.A., Milano, ItalySearch for more papers by this authorA. Tajana, A. Tajana Pharmaceutical R&D Division, Recordati S.p.A., Milano, ItalySearch for more papers by this authorE. Riscassi, E. Riscassi Pharmaceutical R&D Division, Recordati S.p.A., Milano, ItalySearch for more papers by this authorR. Magliocca, R. Magliocca Pharmaceutical R&D Division, Recordati S.p.A., Milano, ItalySearch for more papers by this authorA. Sartani, A. Sartani Pharmaceutical R&D Division, Recordati S.p.A., Milano, ItalySearch for more papers by this author First published: 02 April 2007 https://doi.org/10.1111/j.1527-3466.1997.tb00331.xCitations: 38AboutPDF ToolsRequest permissionExport citationAdd to favoritesTrack citation ShareShare Give accessShare full text accessShare full-text accessPlease review our Terms and Conditions of Use and check box below to share full-text version of article.I have read and accept the Wiley Online Library Terms and Conditions of UseShareable LinkUse the link below to share a full-text version of this article with your friends and colleagues. Learn more.Copy URL Share a linkShare onFacebookTwitterLinkedInRedditWechat REFERENCES 1 1993 Joint National Committee. The fifth report of the Joint National Committee on detection, evaluation and treatment of high blood pressure. Arch Intern Med 1993; 153: 154– 183. 2 1993 Guidelines for the Management of Mild Hypertension: Memorandum from a WHO/ISH Meeting. Bulletin of the ISH 1993. 3 Ambrosioni E, Circo A. Activity of lercanidipine administered in single and repeated doses once daily as monitored over 24 hours in patients with mild to moderate essential hypertension. J Cardiovasc Pharmacol 1997; 29 (Suppl. 2): S16– S20. 4 Barbagallo Sangiorgi G, 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): S37– S40. 5 Barchielli M, Dolfini E, Farina P, et al. Clinical pharmacokinetics of lercanidipine. J Cardiovasc Pharmacol 1997; 29 (Suppl. 2): S1– S15. 6 Bean BP. Nitrendipine block of cardiac calcium channels: High-affinity binding to the inactivated state. Proc Natl Acad Sci 1984; 81: 6388– 6392. 7 Bernocchi P, Ceconi C, Pedersini P, Boraso A, Curello S, Ferrari R. Effects of lercanidipine on Fe2+-induced mitochondrial lipid peroxidation. J Cardiovasc Pharmacol 1997; 29 (Suppl. 1): S63– S68. 8 Bianchi G, Leonardi A. Rec 15/2375. Drugs Future 1987; 12: 1113– 1116. 9 Bianchi G, Passoni A, Griffini PL. Effects of a new calcium antagonist, Rec 15/2375, on cardiac contractility of conscious rabbits. Pharmacol Res 1989; 21: 193– 200. 10 Boraso A, Bernocchi P, Benigno M, et al. Time-dependence of the cardioprotective effects of lercanidipine. J Cardiovasc Pharmacol 1997; 29 (Suppl. 1): S69– S77. 11 Cafiero M, Giasi M. Long-term (12 month) treatment with lercanidipine in patients with mild to moderate hypertension. J Cardiovasc Pharmacol 1987; 9 (Suppl. 2): S46– S50. 12 Cargnoni A, Benigno M, Ferrari F, et al. Effects of lercanidipine and its enantiomers on ischemia and reperfusion. J Cardiovasc Pharmacol 1997; 29 (Suppl. 1): S48– S62. 13 Cerbai E, Barbieri M, Mugelli A. Electrophysiological study on lercanidipine and its enantiomers. J Cardiovasc Pharmacol 1997; 29 (Suppl. 1): S1– S9. 14 Circo A. Active dose findings for lercanidipine in a double-blind, placebo-controlled design in patients with mild to moderate hypertension. J Cardiovasc Pharmacol 1997; 29 (Suppl. 2): S22– S26. 15 Corsini A, Bonfatti M, Quarato P, et al. Effect of the new calcium antagonist lercanidipine and its enantiomers on the migration and proliferation of arterial myocytes. J Cardiovasc Pharmacol 1996; 28: 687– 694. 16 Farina P, Targa G, Leoni B, Tajana A. Pharmacokinetics of lercanidipine in animals. I. Absorption, plasma concentrations, and excretion after administration of [14C]lercanidipine to rats, mice, rabbits and dogs. J Cardiovasc Pharmacol 1997; 29 (Suppl. 1): S86– S96. 17 Farina P, Targa G, Leoni B, Tajana A. Pharmacokinetics of lercanidipine in animals. II. Distribution to and elimination from organs and tissues after administration of [14C]lercanidipine to rats and dogs. Whole-body autoradiography, biliary excretion and enterohepatic circulation and biotransformation in rats. J Cardiovasc Pharmacol 1997; 29 (Suppl. 1): S97– S108. 18 Ferreira-Filho SR, Saragoça MA, Oliveira PC, et al. Use of nitrendipine in the treatment of systolic hypertension in elderly patients. J Cardiovasc Pharmacol 1987; 9 (Suppl. 4): S218– S220. 19 Floras JS. Antihypertensive treatment, myocardial infarction and nocturnal myocardial ischaemia. Lancet 1988; 2: 994– 996. 20 Freedam D, Waters D. Second generation dihydropyridine calcium antagonists. Drugs 1987; 34: 578– 599. 21 Furberg CD, Patsy BM and Meyer JV. Niiedipine, dose-related increase in mortality in patients with coronary heart disease. Circulation 1995; 92: 1326– 1331. 22 Ganten D. Role of animal models in hypertension research. Hypertension 1987; 9: 12– 14. 23 Godfraind T. Classification of calcium antagonists. Am J Cardiol 1987; 59: 11B– 23B. 24 Godfraind T. Cardioselectivity of calcium antagonists. Cardiovasc Drugs Ther 1994; 8: 353– 364. 25 Greene MA, Friedlander R, Boltax AJ, Hadjigeorge CC, Lustic GA. Distensibility of arteries in human hypertension. Proc R Soc Exp Biol 1966; 121: 580– 585. 26 Guarneri L, Angelico P, Ibba M, et al. Pharmacological in vitro studies of the new 1,4-dihydropyridine calcium antagonist lercanidipine. Arzneim Forsch/Drug Res 1996; 46: 15– 24. 27 Guarneri L, Sironi G, Angelico P, et al. In vitro and in vivo vascular selectivity of lercanidipine and its enantiomers. J Cardiovasc Pharmacol 1997; 29 (Suppl. 1): S25– S32. 28 Herbette LG, Vant Erve YMH, Rhodes DG. Interaction of 1,4-dihydropyridine calcium antagonists with biological membranes: Lipid bilayer partitioning could occur before drug binding to receptor. J Mol Cell Cardiol 1989; 21: 187– 201. 29 Herbette LG, Vecchiarelli M, Leonardi A. Lercanidipine: Short plasma half-life, long duration of action "A molecular model to rationalize its pharmacokinetic properties". J Cardiovasc Pharmacol 1997; 29 (Suppl. 1): S19– S24. 30 Híramatsu K, Yamagishi F, Kubota T and Yamada T. Acute effects of the calcium antagonist nifedipine on blood pressure, pulse rate, and renin-angiotensin-aldosterone system in patients with essential hypertension. Am Heart J 1982; 104: 1346– 1350. 31 Ishii A, Nishida K, Nakamizo N. Slow dissociation of the new slow-onset and long-acting calcium antagonist benidipine hydrochloride from [3H]nitrendipine binding sites. Arzneim Forsch/Drug Res 1988; 38: 1681. 32 Kaplan NM. Calcium and blood pressure. Cardiovasc Drugs Therapy 1988; 2: 269– 274. 33 Kauder WF, Watts JA. Antioxidant properties of dihydropyridines in isolated rat hearts. Comparison of nisoldipine, nisoldipine enantiomers, and nifedipine. Biochem Pharmacol 1996; 51: 811– 819. 34 Kelly JG, O'Malley K. Clinical pharmacokinetics of calcium antagonists. An update. Clin Pharmacokinet 1992; 22: 416– 433. 35 Kloner RA. Nifedipine in ischemic heart disease. Circulation 1995; 92: 1074– 1078. 36 Leonardi A, Nardi D, Pennini R, et al. New 1,4-dihydropyridines with antihypertensive activity. IX International Symposium on Medicinal Chemistry, Berlin , September 1418 1986. 37 Leonardi A, Poggesi E, Taddei C, et al. In vitro calcium-antagonistic activity of lercanidipine and its enantiomers. J Cardiovasc Pharmacol 1997; 29 (Suppl. 1): S10– S18. 38 Paterna S, Licata A, Arnone S, Cottone C, Corrao S, Licata G. Lercanidipine in two different dosage regimens as a sole treatment for severe essential hypertension. J Cardiovasc Pharmacol 1997; 29 (Suppl. 2): S51– S54. 39 Lichtlen PR, Hugenholtz PG, Rafflenbleu W, Hecker H, Jost S, Deckers JW. Retardation of angiographie progression of coronary artery disease by nifedipine. Results on the International Trial on Antiatherosclerotic Therapy (INTACT). Lancet 1990; 335: 1109– 1113. 40 Ljung B. Vascular selectivity of felodipine. Drugs 1985; 29: 46– 58. 41 Ljung B, Kjellshed A, Oreback B. Vascular versus myocardial selectivity of calcium antagonists studied by concentration-time-effect relations. J Cardiovasc Pharmacol 1997; 10: S34– S39. 42 Ljung B. Vascular selectivity of felodipine: Experimental pharmacology. J Cardiovasc Pharmacol 1990; 15: S11– S16. 43 Ninci MA, Magliocca R, Malliani A. Efficacy and tolerability of lercanidipine in elderly patients with mild to moderate hypertension in a placebo-controlled, double-blind study. J Cardiovasc Pharmacol 1997; 29 (Suppl. 2): S41– S45. 44 Morel N, Godfraind T. Prolonged depolarization increases the pharmacological effect of dihydropyridines and their binding affinity for calcium channels of vascular smooth muscle. J Pharmacol Exp Ther 1987; 243: 711– 715. 45 Nardi D, Leonardi A, Cerri A, et al. Asymmetric N-(3,3-diphenylpropyl)aminoalkyl esters of 4-aryl-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylic acids with antihypertensive activity. J Mol Cell Cardiol 1995; 27: A385. 46 Omtsuka M, Yokota M, Kodama I, Yamada K. New generation dihydropyridine calcium entry blockers in search of greater selectivity for one tissue subtype. Gen Pharmacol 1989; 20: 539– 556. 47 Opie LH. Should calcium antagonists be used after myocardial infarction? Ischemia selectivity versus vascular selectivity. Cardiovasc Drugs Ther 1992; 6: 19– 24. 48 Packer M. Second generation calcium channel blockers in the treatment of chronic heart failure: Are they any better than their predecessors Am J Cardiol 1992; 14: 1339– 1341. 49 Perez-Vizcaino F, Tamargo J, Hof RP, Ruegg UT. Vascular selectivity of seven prototype calcium antagonists: A study at the single cell level. J Cardiovasc Pharmacol 1993; 22: 768– 775. 50 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): S32– S36. 51 Reicher-Reiss H, Barasch E. Calcium antagonists in patients with heart failure. A Review. Drugs 1991; 42: 343– 364. 52 Rengo F, Romis L. Activity of lercanidipine in double-blind comparison with nitrendipine in combination treatment of patients with resistant essential hypertension. J Cardiovasc Pharmacol 1997; 29 (Suppl. 2): S55– S59. 53 Richard MO. Pharmacocinétique des antagonistes calciaques. Therapie 1993; 48: 651– 657. 54 Ross R. The pathogenesis of atherosclerosis: A perspective for the 1990s. Nature 1993; 362: 801– 809. 55 Rossoni G, Bernareggi M, De Gennaro Colonna, V, Poivani G, Berti F. Lercanidipine protects the heart from low-flow ischaemia damage and antagonizes the vasopressor activity of endothelin-1. J Cardiovasc Pharmacol 1997; 29 (Suppl. 1): S41– S47. 56 Ruzicka M, and Leenen FHH. Relevance of 24 h blood pressure profile and simpathetic activity for outcome on short vs. long-acting diydropyridines. Ann J Hypertens 1996; 9: 86– 94. 57 Saini RK. Calcium antagonists. In: MJ Antonaccio, ed. Cardiovascular Pharmacology, New York : Raven Press, 1984: 415– 452. 58 Simon A, O'Rourke M, Levenson J. Arterial distensibility and its effects on wave reflection and cardiac loading in cardiovascular disease. Coron Artery Dis 1991; 2: 1111– 1120. 59 Sironi G, Greto L, Montagna E, Castiello P, Testa R. Coronaric and antianginal activity of Rec 15/2375 in anaesthetized dogs and rats. Pharmacol Res 1990; 22: 461. 60 Sironi G, Montagna E, Greto L, Bianchi G, Leonardi A, Testa R. Antihypertensive effects of lercanidipine in experimental hypertensive rats and dogs. Arzneim Forsch/Drug Res 1996; 46: 145– 152. 61 Sironi G, Montagna E, Greto L, Leonardi A, Testa R. Hemodynamic effects of lercanidipine in anaesthetized open-chest dogs. Arzneim Forsch/Drug Res 1996; 46: 256– 261. 62 Sironi G, Colombo D, Greto L, Testa R, Leonardi A. Antihypertensive activity of lercanidipine and its enantiomers in animal models. J Cardiovasc Pharmacol 1997; 29 (Suppl. 1): S33– S40. 63 Sorkin EM, Clissod SP, Brogden RN. Nifedipine. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy, in ischaemic heart disease, hypertension and related cardiovascular disorders. Drugs 1985; 30: 182– 274. 64 Sorkin EM, Clissold SP. Nicardipine: A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy, in the treatment of angina pectoris, hypertension and related cardiovascular disorders. Drugs 1987; 33: 296– 345. 65 Soward AL, Vanhaleweyk GLJ, Serruys PW. The haemodynamic effects of nifedipine, verapamil and diltiazem in patients with coronary artery disease. A review. Drugs 1986; 32: 66– 101. 66 Sowers JR. Calcium channel blockers and atherosclerosis. Am J Kid Dis 1990; 16: 3– 9. 67 Tam YK. Individual variation in first-pass metabolism. Clin Pharmacokin 1993; 25: 300– 328. 68 Testa R, Rimoldi O, Sironi G, Leonardi A, Malliani A. Hemodynamic effects and power spectral analysis of heart rate and arterial pressure variabilities induced by lercanidipine and its enantiomers in conscious dogs. J Cardiovasc Pharmacol 1997; 29 (Suppl. 1): S78– S85. 69 Triggle DJ. Calcium channel antagonists: Mechanism of action, vascular selectivities, and clinical relevance. Clev Clin J Med 1992; 59: 617– 627. 70 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): S27– S31. 71 Unterberg C, Buchwald AB, Mindel L, Kreuzer H. Oxygen free radical damage of isolated cardiomyocytes: Comparative protective effect of radical scavengers and calcium antagonists. Basic Res Cardiol 1992; 87: 148– 160. 72 van Zwieten PA, Pfaffendorf M. Pharmacology of the dihydropyridine calcium antagonists: Relationship between lipophilicity and pharmacodynamic responses. J Hyperten 1993; 11: S3– S8. 73 Zimmerman BG. Peripheral neurogenic factors in acute and chronic alterations of arterial pressure. Circ Res 1983; 53: 121– 130. 74 Weinstein DB, Heider JG. Antiatherogenic properties of calcium-antagonists. Am J Cardiol 1987; 59: 163B– 272B. 75 Wibo M. Mode of action of calcium antagonists: Voltage-dependence and kinetics of drug-receptor interaction. Pharmacol Toxicol 1989; 65: 1– 8. 76 Welling PG. Necessity of food studies: Implications of food effects in Bioavailability, Bioeqivalence and Pharmacokinetics. KK Midha and HH Blume, Eds. p. 211– 221— Medpharm—Scientific Publishers, Stuttgart —1993. Citing Literature Volume15, Issue3September 1997Pages 187-219 ReferencesRelatedInformation
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