Calcium channel blockers and treatment of hypertension

Over the past years, research efforts have been focused on the pathophysiologic role of calcium ions, and the implication for the potential role of calcium channel blockers in the management of essential hypertension. Numerous studies have shown that nifedipine and verapamil are effective antihypertensive agents, initial experience with diltiazem is also encouraging. The magnitude of blood pressure reduction with these drugs is related to the pre-treatment blood pressure. In refractory hypertension, combination with other antihypertensive agents provide additive effect. In the elderly population and in patients with ischemic heart disease, supraventricular arrhythmia, bronchospastic disease, peripheral vascular disease or diabetes mellitus, the calcium channel blockers offer potential advantages over other antihypertensive agents. Experimental studies also suggest that these drugs may reverse ventricular hypertrophy. When long-term safety with these drugs is documented from well-controlled clinical trials, the calcium channel blockers may be our first line of therapy for the management of hypertension.     

Calcium Channel Antagonists in the Treatment of Hypertension

Calcium channel antagonists are widely used antihypertensive agents. Their popularity among primary care physicians is not only due to their blood pressure-lowering effects, but also because they appear to be effective regardless of the age or ethnic background of the patients. The first available calcium channel antagonists utilized immediate-release formulations which, although effective in patients with angina pectoris, were not approved by the US FDA for use in hypertension. When long-acting once-daily formulations were approved in this indication, the short-acting preparations — which had by then become generic and inexpensive — retained some residual unapproved use for hypertension. An observational case-controlled trial, based on such usage, noted that these agents were associated with a greater risk of myocardial infarctions than conventional agents such as diuretics and β-adrenoceptor antagonists. Further case-controlled trials showed, in fact, that the dangers of calcium channel antagonists were confined to the short-acting agents and that approved long-acting agents were at least as well tolerated and effective as other antihypertensive drugs. Cardiovascular outcomes during treatment with calcium channel antagonists have been examined in randomized, controlled trials. Compared with placebo, the calcium channel antagonists clearly prevented strokes and other cardiovascular events and reduced mortality. The effects of these agents on survival and clinical outcomes were similar to those with other antihypertensive drugs. There is a slight tendency for the calcium channel antagonists to be more effective than other drug types in preventing stroke, but slightly less effective in preventing coronary events. These observations extend to high-risk patients with hypertension including those with diabetes mellitus. Even so, patients with evidence of nephropathy should not receive monotherapy with calcium channel antagonists. Such patients are optimally treated with angiotensin receptor antagonists or ACE inhibitors, although addition of other drugs, including calcium channel antagonists, is often required to achieve the tight blood pressure control necessary to provide adequate renal protection. Calcium channel antagonists have a highly acceptable tolerability profile and careful reviews of available data have shown that their use is not associated with increased bleeding or promotion of tumor formation. It is now recognized that reduction of blood pressure in patients with hypertension to levels often <130/85mm Hg should be undertaken in presence of other cardiovascular risk factors or evidence of end organ damage. Because of this important concept, calcium channel antagonists, like the other antihypertensive drug classes, are progressively being prescribed less often as monotherapy, but more typically as part of combination regimens.     

Plasma renin activity-guided strategy for the management of hypertension

Despite the wide array of antihypertensive agents and the availability of national guidelines regarding treatment for hypertension, the disease remains uncontrolled in nearly 50% of affected patients. Furthermore, the number of patients with resistant hypertension continues to increase. For patients with resistant hypertension, the American Heart Association has advocated for clinical studies to determine appropriate pharmacologic treatment strategies. One proposed strategy involves ambulatory measurement of plasma renin activity (PRA) to guide the selection of antihypertensive therapy. Patients with low PRA would be prescribed natriuretic volume-mediated therapies (e.g., diuretics and calcium channel blockers), whereas those with high PRA would receive antirenin system therapies (e.g., β-blockers, angiotensin-converting enzyme inhibitors, and angiotensin II receptor blockers). This review focuses on the principles of PRA-guided therapy, its historical development, alternative approaches to classifying patients into categories of response to antihypertensive agents, and recent data supporting the use of plasma renin activity-guided hypertension management.     

Calcium channel blockers as the treatment of choice for hypertension in renal transplant recipients: fact or fiction

Posttransplantation hypertension has been identified as an independent risk factor for chronic allograft dysfunction and loss. Based on available morbidity and mortality data, posttransplantation hypertension must be identified and managed appropriately. During the past decade, calcium channel blockers have been recommended by some as the antihypertensive agents of choice in this population, because it was theorized that their vasodilatory effects would counteract the vasoconstrictive effects of the calcineurin inhibitors. With increasing data becoming available, reexamining the use of traditional antihypertensive agents, including diuretics and beta-blockers, or the newer agents, angiotensin-converting enzyme (ACE) inhibitors and angiotensin II receptor blockers, may be beneficial. Transplant clinicians must choose antihypertensive agents that will provide their patients with maximum benefit, from both a renal and a cardiovascular perspective. Beta-blockers, diuretics, and ACE inhibitors have all demonstrated significant benefit on morbidity and mortality in patients with cardiovascular disease. Calcium channel blockers have been shown to possess the ability to counteract cyclosporine-induced nephrotoxicity. When compared with beta-blockers, diuretics, and ACE inhibitors, however, the relative risk of cardiovascular events is increased with calcium channel blockers. With the long-term benefits of calcium channel blockers on the kidney unknown and a negative cardiovascular profile, these agents are best reserved as adjunctive therapy to beta-blockers, diuretics, and ACE inhibitors.     

Azelnidipine

Azelnidipine is a new dihydropyridine calcium channel antagonist with selectivity for L-type calcium channels that has recently been approved in Japan for the treatment of patients with hypertension. Results from clinical trials showed that, in 95 patients with mild-to-moderate hypertension, long-term treatment with azelnidipine effectively controls blood pressure (BP). The mean reduction from baseline in sitting systolic/diastolic BP after 1 year of treatment was 27.8/16.6 mm Hg. Among 172 patients with uncontrolled hypertension receiving non-calcium channel antagonist antihypertensive agents, the addition of azelnidipine therapy significantly reduced mean BP in a noncomparative, 1-year study (a reduction from 165.7/95.4 mm Hg at baseline to 138.2/79.9 mm Hg at study end). The antihypertensive efficacy of azelnidipine in patients with mild-to-moderate hypertension was shown to be similar to that of amlodipine or nitrendipine in randomised, double-blind studies. Azelnidipine and amlodipine controlled 24-hour BP to a similar extent. Azelnidipine is generally well tolerated; vasodilator adverse events such as as headache and hot facial flushes account for most of the adverse events. Its use is not associated with reflex tachycardia.     

Hemodynamic Effects of Calcium Channel Blockers in Essential Hypertension

Abstract: Calcium channel blockers decrease blood pressure in essential hypertension due to a marked reduction of systemic vascular resistance (arteriolar tone). They also dilate conducting arteries but have no venodilatory effect in antihypertensive doses. With the dihydropyridines (e.g. nifedipine) and diltiazem there is a transient increase in heart rate and cardiac output but this is not observed with verapamil. The vasodilatory responsiveness in the resistance vessels to calcium channel blockers is selectively enhanced in patients with established essential hypertension but not in the early borderline phase of hypertension. During treatment with chlorthalidone, atenolol, acebutolol or nitrendipine for four to six weeks the reduction of blood pressure is accompanied by a selective decrease in the vasodilatory responsiveness to calcium channel blockers.     

Antihypertensive therapy: special focus on drug interactions

Today, the lifetime risk of patients aged 55 – 65 years to receive antihypertensive drugs approaches 60%. Yet, recent trials suggest that hypertension is not adequately controlled in the majority of patients. The prevalence of hypertension increases with advancing age, as does the prevalence of comorbid conditions and the total number of medications taken. Multi-drug therapy, advancing age and comorbid conditions are also key risk factors for adverse drug reactions and drug interactions. In this review, the authors evaluate the most frequently used antihypertensive drugs (diuretics, β-adrenergic blockers, angiotensin-converting enzyme inhibitors, calcium channel blockers, angiotensin II receptor Type 1 blockers and α-adrenergic blockers) with special reference to pharmacodynamic and pharmacokinetic drug interactions. As the spectrum of drugs prescribed is constantly changing, safety yesterday does not imply safety today and safety today does not imply safety tomorrow. Furthermore, therapeutic efficacy should not be neglected over concerns regarding drug interactions. Many patients are at risk of clinically relevant drug interactions involving antihypertensive drugs but, presently, even more patients may be at risk of suffering from the consequences of their inadequately treated hypertension. In this respect, the authors discuss controversial viewpoints on the overall clinical relevance of drug interactions occurring at the level of cytochrome P450 metabolism.     

Antihypertensive therapy: special focus on drug interactions

Today, the lifetime risk of patients aged 55-65 years to receive antihypertensive drugs approaches 60%. Yet, recent trials suggest that hypertension is not adequately controlled in the majority of patients. The prevalence of hypertension increases with advancing age, as does the prevalence of comorbid conditions and the total number of medications taken. Multi-drug therapy, advancing age and comorbid conditions are also key risk factors for adverse drug reactions and drug interactions. In this review, the authors evaluate the most frequently used antihypertensive drugs (diuretics, beta-adrenergic blockers, angiotensin-converting enzyme inhibitors, calcium channel blockers, angiotensin II receptor Type 1 blockers and alpha-adrenergic blockers) with special reference to pharmacodynamic and pharmacokinetic drug interactions. As the spectrum of drugs prescribed is constantly changing, safety yesterday does not imply safety today and safety today does not imply safety tomorrow. Furthermore, therapeutic efficacy should not be neglected over concerns regarding drug interactions. Many patients are at risk of clinically relevant drug interactions involving antihypertensive drugs but, presently, even more patients may be at risk of suffering from the consequences of their inadequately treated hypertension. In this respect, the authors discuss controversial viewpoints on the overall clinical relevance of drug interactions occurring at the level of cytochrome P450 metabolism.     

门诊抗高血压药物使用情况分析

目的分析我院目前抗高血压药物的使用情况,为临床更好地应用抗高血压药物提供参考。方法抽取门诊2006年4月-2009年4月132 588份处方,取出其中含抗高血压药物的处方36 756张进行分析。结果含抗高血压药物处方占总抽取处方的27.72%,钙离子拮抗剂的使用频率最高,其次是β受体阻滞剂。单联用药占总处方的49.17%,二联用药占总处方的26.93%,三联以上用药占总处方的23.90%。结论我院门诊抗高血压药的使用基本合理,药物合用总体符合阶梯式治疗原则。     

Fixed-dose combination enalapril/nitrendipine: a review of its use in mild-to-moderate hypertension

The fixed-dose combination of enalapril 10mg with nitrendipine 20mg combines an ACE inhibitor with a calcium channel antagonist (CCA) and is indicated for the treatment of patients with mild-to-moderate hypertension whose blood pressure (BP) is inadequately controlled with enalapril or nitrendipine monotherapy. In randomised, double-blind clinical trials, enalapril/nitrendipine 10/20 mg/day was significantly more effective than its individual components in reducing diastolic BP (DBP) in patients with mild-to-moderate hypertension inadequately controlled with enalapril 10 mg/day or nitrendipine 20 mg/day. The fixed-dose combination was similar in efficacy at reducing DBP to amlodipine 10 mg/day in patients who failed to achieve BP control with amlodipine 5 mg/day, and to losartan/hydrochlorothiazide 50/12.5 mg/day in patients who received the combinations as first-line therapy. Enalapril/nitrendipine 10/20 mg produced a consistent antihypertensive effect that persisted for the entire 24-hour dosage interval as shown by ambulatory BP monitoring. Enalapril/nitrendipine 10/20 mg was well tolerated in clinical trials where it was administered to patients with mild-to-moderate hypertension for up to 12 weeks. The adverse events were those expected of ACE inhibitors and CCAs and included cough, headache and flushing. Evidence from clinical trials, including a pooled analysis, suggests that the incidence of oedema may be significantly lower with the fixed-dose combination than with CCA monotherapy.In conclusion, enalapril/nitrendipine 10/20 mg is a well tolerated fixed-dose combination of two established antihypertensive agents administered once daily that effectively lowers BP throughout the 24-hour dosage interval. Importantly, the fixed-dose combination may have a lower incidence of oedema than CCA monotherapy. Enalapril/nitrendipine 10/20 mg provides an additional treatment option for patients with mild-to-moderate hypertension for whom combination therapy is appropriate.     

Hypertension control in the elderly with amlodipine

Treatment of hypertension in the elderly reduces the incidence of cardiovascular events. Some classes of antihypertensive drugs, including long-acting dihydropyridine calcium channel blockers such as amlodipine, can be prescribed in the presence of comorbid conditions. The results of clinical trials support the use of long-acting dihydropyridine calcium channel blockers in the elderly; amlodipine has been shown to be effective and well tolerated in the elderly population.     

Isradipine. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic use in cardiovascular disease

Isradipine, a dihydropyridine derivative, inhibits the inward calcium flux through 'slow' channels of cardiac and vascular tissue, thereby eliciting potent coronary, cerebral and peripheral vasodilatation. In comparison with other calcium channel blockers the drug offers the advantages of minimal cardiodepressant activity, a selective action on the coronary and skeletal muscle vasculature, and a prolonged vasodilatory action. Clinical trials indicate that isradipine is an effective antihypertensive agent, suitable as monotherapy or in combination with beta-blockers, diuretics or ACE inhibitors, for long term treatment of mild to moderate hypertension. Preliminary findings suggest that the drug has a potential role in the treatment of chronic stable angina and, possibly, congestive heart failure. Adverse effects associated with the vasodilatory action of isradipine are generally mild, transient and well-tolerated, and are similar to those encountered with other calcium channel blockers. Thus, isradipine appears to offer a useful alternative to other dihydropyridine derivatives currently employed for the treatment of mild to moderate hypertension and, to a lesser extent, chronic stable angina. While its relative freedom from serious adverse effects may prove of value, its place in therapy vis-à-vis the established calcium channel blockers requires further clarification.     

Drug treatment for hypertension in Finnish primary health care

Objective: To analyse the prescribing patterns of antihypertensive drugs in Finnish primary health care and to describe the profiles of monotherapy and combination therapy in relation to the duration of high blood pressure. Methods: Thirty out of 250 primary health care centres were randomly selected for the study. All doctors (n?=?337) from the participating health centres recorded all hypertensive patients (n?=?4405) during a 2-week period in May 1995. Adequate information was obtained concerning 4294 hypertensives, of whom 65% were women with a mean age for the total study population of 64 years. 85% of the patients (n= 3638) had antihypertensive medication which was classified into five main categories: diuretics, beta blocking agents, calcium channel blockers, ACE inhibitors and hypotensives. Results: Of the patients using antihypertensive medication, 48% were undergoing monotherapy and 52% combination therapy. Beta blocking agents were the most frequently prescribed drugs for hypertension, being used by half of the patients. ACE inhibitors and diuretics were prescribed in a different manner for male and female hypertensives, with men receiving more ACE inhibitors and women more diuretics. The number of antihypertensive drugs increased with the duration of hypertension, though 38% of the patients having hypertension for over 10 years were still undergoing monotherapy. Among patients undergoing combination therapy, 75% received two different agents, most often a diuretic with a beta blocking agent. Conclusions: With increasing duration of hypertension, the number of antihypertensive drugs also increased. Beta blocking agents were the drug of choice for all patients. For women, combination therapy more frequently included diuretics, whereas ACE inhibitors were favoured for men.     

Use of Calcium Channel Blockers in Cardiovascular Risk Reduction

Cardiovascular disease (CVD) is a continuum that begins with the presence of several risk factors for CVD, including smoking, hypertension, obesity, diabetes mellitus, and high levels of cholesterol, and if unaddressed can result in premature death, ischemic heart disease, stroke, congestive heart failure, and end-stage renal disease. Hypertension is associated with a significant increase in cardiovascular (CV) morbidity and mortality, raising the risk of stroke, myocardial infarction, heart failure, kidney disease, and peripheral arterial disease. In Latin America, the prevalence of hypertension and other CV risk factors has become similar to that seen in more developed countries, increasing the proportion of the population at high risk for CVD and congestive heart failure; however, it is hypertension that is a key driving force behind CV risk in Latin America. Despite the existence of a wide range of antihypertensive agents, BP control and reductions in CV risk remain poor in Latin America and in Hispanics living in the US. Ethnic differences in treatment rates and disease awareness have been well documented. Studies have shown that calcium channel blockers (CCBs; calcium channel antagonists) are at least as effective in reducing BP and improving the CV risk profile as other classes of antihypertensive agents when administered as monotherapy. CCBs have also been shown to be effective when administered as part of combination therapy in both low- and high-risk hypertensive patients, suggesting that CCBs can easily be combined with other antihypertensive classes in order to achieve BP control and CV risk reduction. In patients with hypertension, coronary artery disease, and high cholesterol, CCBs have been associated with beneficial effects on a range of other aspects of the CV continuum, including the vasculature, coronary calcification, and progression of atherosclerosis. CCBs have also been shown to preserve renal function. Unlike diuretics and β-adrenoreceptor antagonists, CCBs are metabolically neutral, inducing minimal changes in serum lipids and decreasing the incidence of new-onset diabetes compared with other antihypertensive agents. CCBs are well tolerated when administered as monotherapy or combination therapy, with long-acting formulations minimizing adverse events even further compared with short-acting formulations. These characteristics make CCBs an attractive option for the treatment of hypertension and CV risk in Latin America, which remain significant health issues in this region.     

Calcium metabolism, calcium-channel blocking agents, and hypertension management

Increasing evidence has suggested that a disturbance of cellular calcium metabolism may have a role in initiating and maintaining elevated systemic vascular resistance in essential hypertension. Controversy exists over whether calcium can alleviate or exacerbate the hypertensive process, and diversity of calcium metabolism in hypertensive patients has been proposed. Calcium-channel blocking agents are potent vasodilators capable of correcting the elevated systemic vascular resistance. Clinical studies have shown that these drugs have antihypertensive efficacy comparable to established agents. The elderly, blacks, and patients with low renin activity respond well to calcium-channel blockers. These drugs may also offer potential advantages over established antihypertensive agents in patients with other coexisting diseases. Sustained release formulations have been developed, and initial experience with long-term efficacy and tolerability is encouraging. The calcium-channel blockers may become first-line therapy for treatment of hypertension in selected patients.     

The Role of Angiotensin Receptor Blocker and Calcium Channel Blocker Combination Therapy in Treating Hypertension

Hypertension remains a significant health problem, affecting approximately 30% of the US population. Of these, only 36.8% have BP controlled to recommended levels of <140/90mmHg for uncomplicated hypertension and <130/80 mmHg for patients with diabetes mellitus or renal disease. For those with uncontrolled hypertension, the risk of diabetes, renal disease, stroke, and cardiovascular disease is increased. Therapeutic options for the treatment of hypertension include several major classes of drugs: diuretics, ß-adrenoceptor antagonists (ß-blockers), ACE inhibitors, angiotensin II type 1 receptor antagonists (angiotensin receptor blockers [ARBs]), renin inhibitors, calcium channel blockers, and central sympatholytics, alone or in combination. Guidelines recommend thiazide diuretics as preferred first-line monotherapy. However, only 50% of patients will respond adequately to this therapy and the rest will require two or more antihypertensive agents to achieve BP goals. Clinical evidence demonstrates that some drugs have advantages when used in combination rather than as monotherapy. Drugs that block the renin-angiotensin-aldosterone system not only provide BP control but may also provide vascular protection and are metabolically neutral. This is a concise review of the safety and efficacy of ARBs in combination with amlodipine for the treatment of hypertension, with focus on the telmisartan-amlodipine combination. A MEDLINE search of the English literature from 2006 to 2009 of amlodipine in combination with ARBs revealed six publications, which are included in this review.     

Lercanidipine: a review of its use in hypertension

Lercanidipine is a vasoselective dihydropyridine calcium antagonist which causes systemic vasodilation by blocking the influx of calcium ions through L-type calcium channels in cell membranes. It is a highly lipophilic drug and as such has a slower onset and longer duration of action than a number of other calcium antagonists. Preclinical evidence suggests that lercanidipine has antiatherogenic potential and it may also protect against end-organ damage. In well controlled clinical studies, once daily administration of lercanidipine 10 or 20mg effectively reduced blood pressure (BP) compared with placebo in patients with mild to moderate hypertension without affecting heart rate. Response rate (percentage of patients with diastolic BP < or =90mm Hg or reduced by > or =10mm Hg from baseline) ranged from 50 to 66% with lercanidipine 10 mg/day and up to 86% with lercanidipine 20 mg/day. The drug had a long duration of action: clinical measurements for diastolic BP yielded a trough/peak ratio of >0.8 for both lercanidipine dosages in 1 study. Comparative trials, either published in full or as abstracts, found lercanidipine 10mg once daily for > or =4 weeks to be at least as effective as atenolol 50mg once daily, candesartan cilexetil 16 mg/day, captopril 25mg twice daily, enalapril 20 mg/day, hydrochlorothiazide 12.5mg once daily, irbesartan 150 mg/day and slow release nifedipine 20mg twice daily in patients with mild to moderate hypertension. In addition, lercanidipine 20 mg/day was as effective as amlodipine 10 mg/day. Lercanidipine is effective in the treatment of elderly patients (aged 60 to 85 years) with mild to moderate essential hypertension and in those with isolated systolic hypertension. In addition, monotherapy with lercanidipine 20 or 40 mg/day has shown efficacy in patients with severe hypertension, and add-on therapy helped control BP in a large proportion of patients with severe hypertension not responding sufficiently to beta-blockers, diuretics or ACE inhibitors. Unpublished data indicate that the drug reduces blood pressure in patients with type 2 (non-insulin-dependent) diabetes mellitus, without adversely affecting glucose homeostasis. Lercanidipine was well tolerated in clinical trials, with most treatment-related adverse events typical of dihydropyridine calcium antagonists, namely headache, flushing, dizziness and ankle oedema. CONCLUSIONS: Lercanidipine is an effective and well tolerated once daily antihypertensive agent in patients with mild to moderate hypertension. In addition, the drug may reduce BP when used as monotherapy in patients with severe hypertension or when used adjunctively in patients with resistant hypertension. Importantly, lercanidipine appears to be at least as effective and well tolerated as other commonly used antihypertensive agents. The drug therefore represents a useful therapeutic option in the management of patients with hypertension and will be particularly useful in patients not responding to, or intolerant of, antihypertensive agents from other drug classes.     

Discordant effects of beta-blockade on central aortic systolic and brachial systolic blood pressure: considerations beyond the cuff

The role of beta-blockers in uncomplicated hypertension has been challenged recently. Compared with other antihypertensives, beta-blockers are less effective for preventing cardiovascular events in patients with uncomplicated hypertension. Moreover, a recent meta-analysis of placebo-controlled clinical trials concluded that atenolol is not more efficacious than placebo for preventing cardiovascular events in patients with hypertension. Although these agents lower blood pressure measured conventionally over the brachial artery with a blood pressure cuff, they do not exert a commensurate effect on blood pressure in the central aorta. Central aortic blood pressure and aortic augmentation index are strong predictors of left ventricular hypertrophy, an independent risk factor for cardiovascular events. Emerging data are illuminating the antihypertensive paradox whereby antihypertensive agents may elicit discordant effects on central and peripheral blood pressure and hemodynamics. Vasodilatory antihypertensives, such as renin-angiotensin-aldosterone system inhibitors and calcium channel blockers, elicit reductions in central aortic blood pressure equal to or greater than that in the brachial artery. Conversely, beta-blockers lower central aortic blood pressure to a lesser degree even when blood pressure measured by sphygmomanometry is reduced substantially. Given the strong relationship between central aortic blood pressure and target organ damage, the effectiveness of beta-blockers may be overestimated in practice on the basis of conventional blood pressure measurements alone. Differences in central and peripheral blood pressure may account for the lack of cardiovascular protection afforded by beta-blockers in clinical trials and could account for a portion of the apparent "benefit beyond blood pressure" reduction with other classes of antihypertensive agents. Future studies should aim to better clarify the role of central aortic blood pressure in the treatment of hypertension. In the meantime, the effects of antihypertensive drugs on blood pressure "beyond the brachial blood pressure cuff" should be considered when prescribing antihypertensive agents for a patient.     

Effects of Antihypertensive Agents on the Left Ventricle

Hypertensive heart disease (HHD) is characterized by left ventricular hypertrophy (LVH), alterations of cardiac function, and coronary flow abnormalities. LVH is an independent cardiovascular risk factor related to cardiovascular complications in patients with hypertension. Therefore, a decrease in left ventricular mass is a therapeutic goal in these patients. The effect of the different antihypertensive agents on LVH regression has been studied in nearly 500 clinical trials. Most studies conclude that there is regression of LVH after significant decrease in blood pressure with most commonly prescribed antihypertensive agents. However, the ability to regress LVH is different between antihypertensive drug classes. ACE inhibitors and calcium channel antagonists are more potent in reducing left ventricular mass than β-blockers, with diuretics falling in the intermediate group. Recent data suggest that angiotensin AT₁ receptor antagonists reduce left ventricular mass to a similar extent as ACE inibitors or calcium channel antagonists. Although a large number of studies have established that reversal of LVH decreases the occurrence of adverse cardiovascular events in patients with hypertension, the hypothesis that LVH regression is beneficial has not yet been conclusively proven. On the other hand, the time has come to revisit the current management of HHD simply focused on controlling blood pressure and reducing left ventricular mass. In fact, it is necessary to develop new approaches aimed to repair myocardial structure and protect myocardial perfusion and function and, in doing so, to reduce in a more effective manner, adverse risk associated with HHD. The identification of genes involved in both the process of HHD and the response to therapy may be critical for the development of these new approaches. This article will review briefly the available data on the effects of antihypertensive agents on HHD. In addition, the emerging new concepts on the pharmacology of hypertensive myocardial remodeling and the pharmacogenetic basis of the treatment of HHD will be also considered.