Increased vascular selectivity and prolonged pharmacological efficacy of the L-type Ca2+ channel antagonist lercanidipine in human cardiovascular tissue

Clinical and Experimental Pharmacology and Physiology

Volumn 32, Issue 9, 2005, Pages 708-713

  Brixius, Klara ^a   Gross, Thomas ^a   Tossios, Paschalios ^a   Geissler, Hans Joachim ^a   Mehlhorn, Uwe ^a   Schwinger, Robert H G ^a   Hekmat, Khosro ^a  

^a UNIVERSITY OF COLOGNE   (Germany)

Author keywords

Amlodipine; Lercanidipine; Nifedipine vasoselectivity

Indexed keywords

1,4 DIHYDROPYRIDINE; AMLODIPINE; CALCIUM CHANNEL BLOCKING AGENT; CALCIUM CHANNEL L TYPE; LERCANIDIPINE; NIFEDIPINE; DIHYDROPYRIDINE DERIVATIVE;

ADULT; AGED; ARTICLE; CLINICAL ARTICLE; CONGESTIVE CARDIOMYOPATHY; CONTROLLED STUDY; CORONARY ARTERY BYPASS GRAFT; DRUG EFFICACY; FEMALE; HEART; HEART GRAFT; HEART MUSCLE; HEART TRANSPLANTATION; HUMAN; HUMAN TISSUE; HYPERTENSION; IC 50; INOTROPISM; MALE; MAMMARY ARTERY; RADIOASSAY; VASODILATATION; ADOLESCENT; BINDING COMPETITION; DRUG EFFECT; HEART CONTRACTION; IN VITRO STUDY; MIDDLE AGED; PROTEIN BINDING; STIMULATION;

ADOLESCENT; ADULT; AGED; AMLODIPINE; BINDING, COMPETITIVE; CALCIUM CHANNEL BLOCKERS; CALCIUM CHANNELS, L-TYPE; DIHYDROPYRIDINES; FEMALE; HUMANS; MALE; MAMMARY ARTERIES; MIDDLE AGED; MYOCARDIAL CONTRACTION; NIFEDIPINE; PROTEIN BINDING; STIMULATION, CHEMICAL; VASODILATION;

EID: 26944439119     PISSN: 03051870     EISSN: None     Source Type: Journal    
DOI: 10.1111/j.1440-1681.2005.04265.x     Document Type: Article

References (36)

1. Brown MJ, Palmer CR, Castaigne A et al. Morbidity and mortality in patients randomised to double-blind treatment with a long-acting calcium-channel blocker or diuretic in the International Nifedipine GITS study: Intervention as a Goal in Hypertension Treatment (INSIGHT). Lancet 2000; 356: 366-72.
2. Hansson L, Hedner T, Lund-Johansen P et al. Randomised trial of effects of calcium antagonists compared with diuretics and beta-blockers on cardiovascular morbidity and mortality in hypertension: The Nordic Diltiazem (NORDIL) study. Lancet 2000; 356: 359-65.
3. Messerli FH. Evolution of calcium antagonists: Past, present, and future. Clin. Cardiol. 2003; 26 (Suppl.): II12-16.
4. White WB. Clinical trial experience around the globe: Focus on calcium-channel blockers. Clin. Cardiol. 2003; 26 (Suppl.): II7-11.
5. Sorkin EM, Clissold 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.
6. Soward AL, Vanhaleweyk GL, Serruys PW. The haemodynamic effects of nifedipine, verapamil and diltiazem in patients with coronary artery disease. A review. Drugs 1986; 32: 66-101.
7. Reicher-Reiss H, Barasch E. Calcium antagonists in patients with heart failure. A review. Drugs 1991; 42: 343-64.
8. Opie LH. Choosing the correct drug for the individual hypertensive patient. Drugs 1992; 44 (Suppl. 1): 147-55.
9. 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: 596-9.
10. Furberg CD, Psaty BM, Meyer JV. Nifedipine. Dose-related increase in mortality in patients with coronary heart disease. Circulation 1995; 92: 1326-31.
11. Ljung B. Vascular selectivity of felodipine. Drugs 1985; 29 (Suppl. 2): 46-58.
12. Packer M, O'Connor CM, Ghali JK et al. Effect of amlodipine on morbidity and mortality in severe chronic heart failure. Prospective Randomized Amlodipine Survival Evaluation Study Group. N. Engl. J. Med. 1996; 335: 1107-14.
13. Kiowski W, Bertel O, Erne P et al. Hemodynamic and reflex responses to acute and chronic antihypertensive therapy with the calcium entry channel blocker nifedipine. Hypertension 1983; 5: 170-4.
14. Guarneri L, Angelico P, Ibba M et al. Pharmacological in vitro studies of the new 1,4-dihydropyridine calcium antagonist lercanidipine. Arzneimittelforschung 1996; 46: 15-24.
15. Angelico P, Guarneri L, Leonardi A, Testa R. Vascular-selective effect of lercanidipine and other 1,4-dihydropyridines in isolated rabbit tissues. J. Pharm. Pharmacol. 1999; 51: 709-14.
16. Mecca TE, Love SD. Comparative cardiovascular actions of clentiazem, diltiazem, verapamil, nifedipine, and nimodipine in isolated rabbit tissues. J. Cardiovasc. Pharmacol. 1992; 20: 678-82.
17. Magnon M, Gallix P, Cavero I. Intervessel (arteries and veins) and heart/vessel selectivities of therapeutically used calcium entry blockers: Variable, vessel-dependent indexes. J. Pharmacol. Exp. Ther. 1995; 275: 1157-66.
18. Videbaek LM, Kvist S, Mulvany MJ. Time course of action of amlodipine and felodipine in the rat is most rapid in small arteries. Eur. J. Pharmacol. 1995; 274: 109-15.
19. +-channel activators BDF 9148, BDF 9196 and BDF 9167 in human failing and nonfailing myocardium. J. Pharmacol. Exp. Ther. 1996; 276: 1180-8.
20. Brixius K, Mohr V, Muller-Ehmsen J, Hoischen S, Munch G, Schwinger RHG. Potent vasodilatory with minor cardiodepressant actions of mibefradil in human cardiac tissue. Br. J. Pharmacol. 1998; 125: 41-8.
21. van der Lee R, Kam KL, Pfaffendorf M, van Zwieten PA. Differential time course of the vasodilator action of various calcium antagonists. Fundam. Clin. Pharmacol. 1998; 12: 607-12.
22. 2+-antagonists in human myocardial tissue. Klin. Wochenschr. 1990; 68: 797-805.
23. 2+-channel in myocardium from patients with end-stage heart failure and in non-failing human hearts. J. Mol. Cell. Cardiol. 1999; 31: 283-96.
24. 3H](+)PN 200-110 binding to dihydropyridine receptors associated with calcium channels in rat cerebral cortex and heart. Life Sci. 1984; 35: 721-32.
25. Brixius K, Bundkirchen A, Bolck B, Mehlhorn U, Schwinger RHG. Nebivolol, bucindolol, metoprolol and carvedilol are devoid of intrinsic sympathomimetic activity in human myocardium. Br. J. Pharmacol. 2001; 133: 1330-8.
26. Bean BP. Nitrendipine block of cardiac calcium channels: High affinity binding to the inactivated state. Proc. Natl Acad. Sci. USA 1984; 81: 6388-92.
27. Noble D. The Initiation of the Heart Beat. Oxford University Press, Oxford. 1979.
28. Sperelakis N (ed.). Physiology and Pathophysiology of the Heart. Kluwer Academic, Boston. 1995.
29. Sun J, Triggle DJ. Calcium channel antagonists. Cardiovascular selectivity of action. J. Pharmacol. Exp. Ther. 1995; 274: 419-26.
30. Leonardi A, Poggesi E, Taddei C et al. In vitro calcium antagonist activity of lercaidipine and its enantiomers. J. Cardiovasc. Pharmacol. 1997; 29 (Suppl. 1): S10-18.
31. Herbette L, Gaviraghi G, Tulenko T, Mason RP. Molecular interactions between lacidipine and biological membranes. J. Hypertens. Suppl. 1993; 11: S13-19.
32. 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): S16-21.
33. Kleinbloesem CH, van Harten J, Wilson JP, Danhof M, van Brummer P, Breimer DD. Nifedipine: Kinetics and hemodynamic effects in patients with liver cirrhosis after intravenous and oral adiistration. Clin. Pharmacol. Ther. 1986; 40: 21-8.
34. Herbette LG, Vecchiarelli M, Leonardi A. Lercanidipine: Short plasma half-life, long duration of action. J. Cardiovasc. Pharmacol. 1997; 29 (Suppl. I): S19-24.
35. Burges R, Moisey D. Unique pharmacologic properties of amlodipine. Am. J. Cardiol. 1994; 73 (Suppl.): A2-9.
36. Garcha RS, Sever PS, Hughes AD. The action of amlodipine on human subcutaneous resistance arteries studied in vitro. J. Pharmacol. Exp. Ther. 1993; 265: 860-5.