Antihypertensive Effects of Nifedipine and Changing for Modified-Release Formula

Abstract

Nifedipine was initially developed as an anti-anginal drug, and it was Professor Murakami who first reported its usefulness in the management of hypertension. However, rapid decrease in blood pressure with immediate-release formulations of nifedipine led to simultaneous increases in heart rate, presumably because of reflex sympathetic activation, and a meta-analysis in the mid-1990s suggested an increased incidence of serious adverse events (AEs) with short-acting Ca2+ channel antagonists. Although subsequent reviews of the literature found little scientific basis for increased serious AEs with short-acting Ca2+ channel antagonists, this controversy led to the accelerated development of long-acting preparations. Recent clinical research has found improved outcomes in hypertensive patients receiving long-acting Ca2+ channel antagonist preparations and reconfirmed the role of nifedipine as a first-line agent.