Cardiovascular drugs nifedipine

Frishman WH, Sherman D, Feinfeld DA. Innovative drug delivery systems in cardiovascular medicine nifedipine-GITS and clonidine-TTS. Cardiol Clin 1987 Nov 5(4) 703-716. 

The Ca +-channel antagonists, the 1,4-dihydropyridines (DHPs), represent a remarkably successful group of cardiovascular drugs that have antihypertensive, antiangi-nal, and antiarrhythmic properties (167). Nifedipine (Fig. 10.8) was the first member of the DHP family a structure that embraces both Ca -channel antagonists and activators (168), which was followed by the synthesis of a number of analogs with a prolonged duration cf action and enhanced vascular selectivity (167). 

The so-called calcium channel blockers constitute a class of cardiovascular agents that have gained prominence in the past few years. These drugs, which obtund contraction of arterial vessels by preventing the movement of calcium ions needed for those contractions, have proved especially useful in the treatment of angina and hypertension. Dihydropyridines such as nifedipine (30) are par-... 

The effects of the prototypical calcium channel blockers are seen most prominently in the cardiovascular system (Table 19.1), although calcium channels are widely distributed among excitable cells. The following calcium channel-blocking drugs are clinically the most widely used compounds in this very extensive class of pharmacological agents amlodipine, diltiazem, isradipine, nifedipine, nicardipine, nimodipine, and verapamil. 

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(3) 182-274. 

In clinical practice, there Is further selectivity of drug action at the L-channels, in part originating from the fact that there seem to be separate, but adjacent, binding sites for different chemical classes of calcium antagonists. Of the L-channel blockers, some chemical families are more active on the smooth muscle of the cardiovascular system (e.g. nifedipine and most other DHPs), whereas others are more cardioactive (e.g. verapamii). Some further details of these... 

Dihydropyridine (DHP) drugs such as nifedipine, nicardipine, amlodipine, and others are effective cardiovascular agents for the treatment of hypertension [63], DHPs have been explored for their calcium charmel activity and are foimd as a constituent in a variety of bioactive compounds which show many biological activities such as vasodilator, bronchodilator, antiatherosclerotic, antitumor, antidiabetic, geroprotec-tive, heptaprotective [64], etc. 

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