Abstract
Calcium antagonists have been available for study and clinical use since the 1960s. As a class of antihypertensive agents, they are the most heterogeneous in their chemical structure, modes of action, and clinical indications. However, they all share a common physiologic action: decreasing the intracellular availability of calcium ions in cardiac and vascular smooth muscle cells, thereby directly inhibiting their contractility. At least four different receptors, with varying affinities to calcium antagonists, regulate calcium ion movement across the cell membrane (1). In addition, some of the diversity of this class of drugs may be explained by the difference in intracellular calcium ion release from the sarcoplasmic reticulum and the mitochondria as well as binding to specific intracellular proteins (e.g., calmodulin)
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References
Catterall WA, Stiessnig J (1992) Receptor sites for Ca++ channel antagonists. Trends Pharmacol Sci 13: 256–262.
Guengerich FP, Brian WR, Iwasaki M, Sari M-A, Baarnhielm C, Bretsson P (1991) Oxidation of dihydropyridine calcium channel blockers and analogues by human liver cytochrome P-450 IIIA4. J Med Chem 34: 1838–1844.
Albernethy DR (1997) Pharmacological properties of combination therapies for hypertension. Am J Hypertens 10:13S–16S.
Messerli FH, Oparil S, Feng Z (2000) Comparison of effectiveness and side effects of combined calcium antagonist (nifedipine or amlodipine) and angiotensinconverting enzyme inhibitor (benazepril) versus high-dose calcium antagonist monotherapy for systemic hypertension. Am J Cardiol,in press.
Grossman E, Messerli FH (1997) Effect of calcium antagonists on plasma norepinephrine levels, heart rate, and blood pressure. Am J Cardiol 80: 1453–1458.
Zuanetti G, Mantini L, Hernandez-Bernal F, Barlera S, di Gregorio D, Latini R, Maggioni AP (1998) Relevance of heart rate as a prognostic factor in patients with acute myocardial infarction: insights from the GISSI-2 study. Eur Heart J 19: F19 — F26.
Alderman MH, Cohen H, Roqué R, Madhavan S (1997) Effect of long-acting and short-acting calcium antagonists on cardiovascular outcomes in hypertensive patients. Lancet 349 (9052): 594–598.
Singh BN, Nademanee K (1987) Use of calcium antagonists for cardiac arrhythmias. Am J Cardiol 59: 153B - 162B.
Messerli FH, Ventura HO, Elizardi DJ, Dunn FG, Frohlich ED (1984) Hypertension and sudden death: increased ventricular ectopy activity in left ventricular hypertrophy. Am J Med 77: 18–22.
Schmieder RE, Martus P, Klingbeil A (1996) Reversal of left ventricular hypertrophy in essential hypertension: a meta-analysis of randomized double-blind studies. JAMA 275: 1507–1513.
Schmieder RE, Schlaich MP, Klingbeil AU, Martus P (1998) Update on reversal of left ventricular hypertrophy in essential hypertension (a meta-analysis of all randomized double-blind studies until December 1996). Nephrol Dial Transplant 13: 564–569.
Cruickshank JM, Lewis J, Moore V, Dodd C (1992) Reversibility of left ventricular hypertrophy by differing types of antihypertensive therapy. J Hum Hypertens 6: 85–90.
Wilson DJ, Schwarts GL, Textor SC, Zachariah PK, Sheps SG (1991) Precipitous fall in blood pressure in the treatment of chronic hypertension. Paper presented at the 5th International Symposium on Calcium Antagonists: Pharmacology and Clinical Research, Houston, TX.
Messerli FH, Grossman E (1998) Antihypertensive agents and the risk of cancer. JAMA 280: 600.
The Sixth Report of the Joint National Committee on Prevention, Detection, Evaluation, and Treatment of High Blood Pressure (1997) Arch Intern Med 157: 2413–2446.
Laragh JH, Held C, Messerli F, Pepine C, Sleight P (1996) Calcium antagonists and cardiovascular prognosis: a homogenous group? Am J Hypertens 9: 99–109.
Messerli FH, Boden WE, Fischer Hansen J, Schechtman KB (1996) Heart rate lowering calcium antagonists (HRL-CA) in hypertensive post MI patients. Am Coll Cardiol 27: 178A (abstract).
Messerli FH (1996) What, if anything, is controversial about calcium antagonists? Am J Hypertens (12 pt. 2 ): 177S - 181S.
Rehnqvist N, Hjemdahl P, Björkander I, et al. (1985) Primary prevention in patients with coronary heart disease: the APSIS study. Cardiovasc Drugs Ther 9 (Suppl. 3): 493.
Parker JD (1998) Clinical outcome studies of anti-anginal drug therapy for patients with stable coronary disease: an indication for clinical trials. Eur Heart J 19(Suppl. I):I 15-I 19.
Erne P, Bolli P, Bertel O, et al. (1983) Factors influencing the hypertensive effects of calcium antagonists. Hypertension 5:II97–1I102.
Staessen JA, Fagard R, Thijs L, et al. (1997) Randomised double-blind comparison of placebo and active treatment for older patients with isolated systolic hypertension. The Systolic Hypertension in Europe (Syst-Eur) Trial Investigators. Lancet 350: 757–764.
Liu L, Wang JG, Gong L, Liu G, Staessen JA (1998) Comparison of active treatment and placebo in older Chinese patients with isolated systolic hypertension. Systolic Hypertension in China (Syst-China) Collaborative Group. J Hypertens 16 (12, Pt. 1): 1823–1829.
Tuomilehto J, Rastenyte D, Birkenhager WH, et al. (1999) Effects of calcium-channel blockade in older patients with diabetes and systolic hypertension: Systolic Hypertension in Europe Trial Investigators. N Engl J Med 340: 677–684.
Wang JG, Staessen JA, Gong L, Liu L (2000) Chinese trial on isolated systolic hypertension in the elderly. Systolic Hypertension in China (Syst-China) Collaborative Group. Arch Intern Med 160: 211–220.
Hansson L, Zanchetti A, Carruthers SG et al. (1998) Effects of intensive blood-pressure lowering and low-dose aspirin in patients with hypertension: principal results of the Hypertension Optimal Treatment (HOT) randomised trial. Lancet 351: 1755–1762.
National High Blood Pressure Education Program Working Group report on hypertension in diabetes (1994) Hypertension 23: 145–158.
Messerli FH, Grossman E, Goldbourt U (1998) Are (3-blockers efficacious as first-line therapy for hypertension in the elderly? A systematic review. JAMA 279: 19031907.
Gong L, Zhang W, Zhu Y, Zhu J, 11 collaborating centres in the Shanghai area, Kong D, Pagé V, Ghadirian P, LeLorier J, Hamet P (1996): Shanghai trial of nifedipine in the elderly (STONE). J Hypertens 14: 1237–1245.
Hansson L, Lindholm LH, Ekbom T, Dahlöf B, Lanke J, Scherstén B, Wester P-O, Hedner T, de Faire U, for the STOP-Hypertension-2 study group (1999). Randomised trial of old and new antihypertensive drugs in elderly patients: cardiovascular mortality and morbidity the Swedish Trial in Old Patients with Hypertension-2 study. Lancet 354: 1751–1756.
The Nordic Diltiazem Study (NORDIL) (2000). Lancet,to be published.
International Nifedipine GITS Study Intervention as a goal in Hypertension Treatment (INSIGHT) (2000). Lancet,to be published.
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Messerli, F.H., Dey, J., Feng, Z. (2001). Calcium Antagonists. In: Weber, M.A. (eds) Hypertension Medicine. Current Clinical Practice. Humana Press, Totowa, NJ. https://doi.org/10.1007/978-1-59259-008-7_27
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DOI: https://doi.org/10.1007/978-1-59259-008-7_27
Publisher Name: Humana Press, Totowa, NJ
Print ISBN: 978-1-4757-5446-9
Online ISBN: 978-1-59259-008-7
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