This paper summarizes the pharmacological properties of
calcium channel blockers (CCBs), their established
therapeutic uses for cardiovascular disorders and the current improvement of their clinical effects through
drug combinations. Their identification resulted from study of small molecules including coronary dilators, which were named
calcium antagonists. Further experiments showed that they reduced contraction of arteries by inhibiting
calcium entry and by interacting with binding sites identified on
voltage-dependent calcium channels. This led to the denomination
calcium channel blockers. In short-term studies, by decreasing total peripheral resistance, CCBs lower arterial pressure. By unloading the heart and increasing coronary blood flow, CCBs improve myocardial oxygenation. In long-term treatment, the decrease in blood pressure is more pronounced in hypertensive than in normotensive patients. A controversy on the safety of CCBs ended after a large
antihypertensive trial (ALLHAT) sponsored by the National Heart, Lung, and Blood Institute. There are two main types of CCBs: dihydopyridine and non-
dihydropyridine; the first type is vascular selective. Dihydropyrines are indicated for
hypertension, chronic, stable and vasospastic angina. Non-
dihydropyridines have the same indications plus antiarrythmic effects in
atrial fibrillation or flutter and
paroxysmal supraventricular tachycardia. In addition, CCBs reduced newly formed coronary lesions in
atherosclerosis. In order to reach recommended blood pressure goals, there is a recent therapeutic move by combination of CCBs with other
antihypertensive agents particularly with inhibitors acting at the level of the renin-angiotensin system. They are also combined with
statins. Prevention of
dementia has been reported in hypertensive patients treated with
nitrendipine, opening a way for further studies on CCBs' beneficial effect in cognitive deterioration associated with aging.