Calcium Channel Blockers and Hypertension

Abstract

Effective treatment of high blood pressure (BP) represents a key strategy for reducing the burden of hypertension-related cardiovascular and renal diseases. In spite of these well-established concepts, hypertension remains poorly controlled worldwide. In order to improve BP control in patients with hypertension, several interventions have been proposed, among which (1) preferred use of more effective, sustained, and well-tolerated antihypertensive drug aimed to ensure adherence to prescribed medications and (2) extensive use of rational, integrated, and synergistic combination therapies, even as first-line strategy, aimed to achieve the recommended BP targets. Within the possible antihypertensive drug classes currently available for the clinical management of hypertension, both in monotherapy and in combination therapy, drugs inhibiting the renin-angiotensin system and calcium channel blockers (CCBs) have demonstrated to be effective and safe in lowering BP levels and achieving the recommended BP targets with a good tolerability profile. In particular, CCBs have been one of the most widely used classes of antihypertensive agents in the last 20 years, based on their effectiveness in reducing BP levels, good tolerability, and abundant evidence on reducing cardiovascular and renal consequences of hypertension. This article provides an updated overview of the evidence supporting the use of CCBs-based antihypertensive regimen, both in monotherapy and in combination therapies with different classes of antihypertensive drugs.

Discovery and Development of Calcium Channel Blockers

“…However, several mechanisms might be involved (Godfraind, 2014). As demonstrated in various clinical trials (Tocci et al, 2015), BP lowering reduces the incidence of stroke and myocardial infarction. Head-to-head comparisons are incomplete but ASCOT trial (Sever et al, 2003) and several meta-analyses indicate that CCBs offer a better protection against stroke and myocardial infarction than angiotensin receptor blockers (Wang et al, 2007).…”

Association between gene polymorphisms of voltage-dependent Ca2+ channels and hypertension in the Dai people of China: a case-control study

“…The relationship between hypertension and intracellular calcium concentration has been confirmed by a large number of experiments [4][5][6][7]. Therefore, changes in the function of calcium channel proteins, which have a regulatory effect on intracellular calcium concentration, may be closely related to the abnormal changes in blood pressure and the development of hypertension.…”

A Study of the Effects of Amlodipine and Cilnidipine on Haemodynamic Parameters and Renoprotection in Hypertensive Subjects With Proteinuria

“…Beyond evidence in favour of cardiovascular and renal protection, clinical trials have also demonstrated a better tolerability profile and favourable metabolic properties by RAS-inhibiting drugs, especially ARBs and by CCBs compared to β-blockers and diuretics, thus promoting the use of these drug classes, both in monotherapy and in combination therapies for hypertension management and control. 12 Diabetic and black hypertensive patients with low renin levels, salt-sensitive and volume-expanded are more often responsive to a CCB than to an ACE inhibitor or a β blocker. Also, the response to increasing the dose of a CCB is generally that of significant additional BP reduction, which separates this drug class from both ACE inhibitors and ARBs.…”

“…13 Indeed, monotherapy based on CCBs has demonstrated to provide sustained antihypertensive efficacy and to reduce cardiovascular and renal complications compared to other antihypertensive drug classes. 12 Calcium channel blockers are effective as single-drug therapy in approximately 60% of patients in all demographic groups and all grades of Hypertension. 2 However, the reduction of blood pressure associated with these agents is associated with reflex sympathetic overactivity, which leads to increased cardiovascular morbidity and mortality.…”