The calcium antagonist controversy: the emerging importance of drug formulation as a determinant of risk

The American Journal of Cardiology
M Epstein

Abstract

Calcium antagonists are one of the widely available classes of antihypertensive agents. Their broad appeal is attributable to several features, including their efficacy, their beneficial characteristics such as metabolic neutrality, and the occurrence of relatively few nuisance-type side effects. Despite these attributes, a number of retrospective analyses have suggested that calcium antagonists may be detrimental and may both promote adverse cardiovascular events and increase the risk of cancer by interfering with cellular apoptosis. On the basis of this and other retrospective analyses, Furberg and Psaty (Am J Hypertens 1996; 9: 122-125) have proposed that the use of calcium antagonists as first-line antihypertensive agents should be discontinued. I have previously countered these allegations and have suggested that they are not relevant to the newer calcium antagonist formulations in current use. It is not widely appreciated that different formulations of the same chemical moiety can produce markedly different hemodynamic and neurohormonal effects, due to differences in the rate of drug delivery into the systemic circulation. During chronic treatment with dihydropyridine calcium antagonists, major fluctuations in blood press...Continue Reading

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Citations

Jun 21, 2001·The American Journal of Geriatric Cardiology·Murray Epstein
Nov 5, 1999·The New England Journal of Medicine·D R Abernethy, J B Schwartz
Dec 9, 1998·Kidney International·M Epstein
Apr 21, 2004·Journal of Hypertension·Guido Grassi
Nov 8, 2018·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Su-Jin BaekChul Kim
Jun 26, 1998·The Annals of Pharmacotherapy·S J Billups, B L Carter

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