Calcium Channel Blocker Amlodipine Besylate Research Articles

Effect of amlodipine on the circulating renin-angiotensin-aldosterone system in healthy cats.

Systemic hypertension (SH) is a common cardiovascular disease in older cats that is treated primarily with the calcium channel blocker amlodipine besylate (AML). The systemic effect of AML on the classical and alterative arms of the renin-angiotensin-aldosterone system (RAAS) in cats is incompletely characterized. To determine the effect of AML compared to placebo on circulating RAAS biomarkers in healthy cats using RAAS fingerprinting. Twenty healthy client-owned cats. Cats were administered amlodipine besylate (0.625 mg in toto) or placebo by mouth once daily for 14 days in a crossover design with a 4-week washout period. Plasma AML concentrations and RAAS biomarker concentrations were measured at multiple timepoints after the final dose in each treatment period. Time-weighted averages for RAAS biomarkers over 24 hours after dosing were compared between treatment groups using Wilcoxon rank-sum testing. Compared to placebo, AML treatment was associated with increases in markers of plasma renin concentration (median 44% increase; interquartile range [IQR] 19%-86%; P = .009), angiotensin I (59% increase; IQR 27-101%; P = .006), angiotensin II (56% increase; IQR 5-70%; P = .023), angiotensin IV (42% increase; -19% to 89%; P = .013); and angiotensin 1-7 (38% increase; IQR 9-118%; P = .015). In healthy cats, administration of AML resulted in nonspecific activation of both classical and alternative RAAS pathways.

Calcium channel blocker amlodipine besylate therapy is associated with reduced case fatality rate of COVID-19 patients with hypertension

The coronavirus disease (COVID-19) caused by the novel severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) has now spread to >200 countries posing a global public health concern. Patients with comorbidity, such as hypertension suffer more severe infection with elevated mortality. The development of effective antiviral drugs is in urgent need to treat COVID-19 patients. Here, we report that calcium channel blockers (CCBs), a type of antihypertensive drug that is widely used in clinics, inhibited the post-entry replication events of SARS-CoV-2 in vitro, while no in vitro anti-SARS-CoV-2 effect was observed for the two other major types of antihypertensive drugs, namely, angiotensin-converting enzyme inhibitors and angiotensin II receptor blockers. CCB combined with chloroquine showed a significantly enhanced anti-SARS-CoV-2 efficacy. A retrospective clinical investigation on hospitalized COVID-19 patients with hypertension as the only comorbidity revealed that the CCB amlodipine besylate therapy was associated with a decreased case fatality rate. The results from this study suggest that CCB administration to COVID-19 patients with hypertension as the comorbidity might improve the disease outcome.

Chronic Conjunctival Chemosis From Amlodipine Besylate (Norvasc)

To report a case of conjunctival chemosis and bipedal edema associated with amlodipine besylate antihypertensive medication. Case report. A 69-year-old white man presented with a diffuse conjunctival mass on his left eye. Examination revealed extensive bulbar conjunctival dependent chemosis of his left eye without injection, pruritus, discharge, or pain. Bipedal pitting edema was found. History revealed that the features were noted 3 months after starting amlodipine besylate (Norvasc) for essential hypertension. Evaluation was unrevealing for allergic or contact irritants and systemic conditions, and the findings were attributed to the previously described side effects of the calcium channel blocker amlodipine besylate with resolution 6 months after cessation. Patients with conjunctival chemosis and bipedal edema should be evaluated for drug reaction and local or systemic medical problems.

Fixed combination therapies based on direct renin inhibition: a commentary to the ACCELERATE trial

Despite the well-established concept that the treatment of high blood pressure (BP) represents a key strategy in reducing the burden of cardiovascular (CV) and renal diseases, arterial hypertension remains poorly controlled worldwide. To improve BP control in the hypertensive population, a more extensive use of combination therapies rather than monotherapies should be adopted, even as a first-line approach, in patients with grade 2–3 hypertension, in high-risk individuals or in those who need more ambitious BP goals (e.g., diabetics). Today, this represents an emerging clinical strategy for the daily clinical practice of hypertension, since recent randomized clinical trials have demonstrated the efficacy, safety and tolerability of such therapeutic approach. Among the potentially effective antihypertensive-combination strategies currently available for the clinical management of hypertension, those based on the combination of drugs inhibiting the renin–angiotensin system (RAS) and calcium-channel blockers (CCBs) appear to ensure effective and extended control of BP levels, as well as CV and renal protection. The recent availability of a novel class of antihypertensive drugs, the direct renin inhibitors (DRI), has prompted studies to further investigate the use of combination strategies to achieve a rapid, persistent and effective BP control. In the present article, we discuss the interesting findings of a recent randomized clin ical trial, the Aliskiren and the Calcium Channel Blocker Amlodipine Combination as an Initial Treatment Strategy for Hypertension (ACCELERATE) trial, which investigated the BP lowering effect and the tolerability of the combination of two long-acting compounds, the calcium-channel blocker amlodipine besylate and the DRI aliskiren. Fixed combination therapy for the clinical management of hypertension Blood pressure elevation is paralleled by a progressive increase in the risk of developing major CV events, including myocardial infarction and stroke, independently of age and gender [1]. The reduction and, most importantly, normalization of BP levels in hypertensive patients is, in turn, associated with significant CV benefits [2]. Achievement of recommended BP targets, however, remains poorly accomplished in both western and developing countries, and recent international surveys demonstrated that almost three quarters of treated hypertensive patients are not normalized under pharmacological treatment [3–5]. Among the potential factors that may contribute to this disappointing observation, frequent presence of comorbidities, doctors’ clinical inertia and the widespread use of monotherapy rather than combination therapy, may all play an important 1

Comparison of Olmesartan Medoxomil Versus Amlodipine Besylate on Regression of Ventricular and Vascular Hypertrophy

Reversal of left ventricular (LV) hypertrophy is an important goal of antihypertensive therapy. This phase 3b study compared the ability of the angiotensin receptor blocker olmesartan medoxomil with the calcium channel blocker amlodipine besylate to induce regression of LV hypertrophy and vascular hypertrophy after achieving blood pressure (BP) goal. After a washout phase, 102 patients with hypertension and LV hypertrophy were randomized to olmesartan medoxomil 20 mg/day, up titrated to 40 mg/day, or amlodipine 5 mg/day, up titrated to 10 mg/day, for up to 4 weeks until a BP goal of <140/90 mm Hg (<130/85 mm Hg for diabetes) was achieved (hydrochlorothiazide 25 mg/day and terazosin 1 to 5 mg/day 2 times/day could be added if needed). Upon achieving the BP goal or by week 8, and again at weeks 26 and 52, assessments of LV mass and compliance and arterial structure and function were performed by echocardiography, Doppler flow, and arterial ultrasonography, respectively. There was no statistically significant percent change in LV mass at 52 weeks in either treatment group (11.6% with olmesartan medoxomil vs 2.9% with amlodipine) and no statistically significant difference between treatment groups. There were no significant changes in LV compliance or carotid or femoral artery wall-to-lumen ratios in either treatment group at 52 weeks. In conclusion, there did not appear to be a clinically significant BP-independent effect with olmesartan medoxomil or amlodipine on LV mass decrease, diastolic function or vascular structure, and compliance in patients with hypertension and LV hypertrophy.

A single-pill combination of amlodipine besylate and atorvastatin calcium (update)

This review describes the clinical profile and rationale for the development of a single-pill formulation of the calcium channel blocker amlodipine besylate, a blood-pressure--lowering agent, and atorvastatin calcium, a statin with lipid-lowering antiatherosclerotic properties. Amlodipine and atorvastatin have been demonstrated in numerous clinical trials to be highly effective in lowering blood pressure and low-density lipoprotein cholesterol. Furthermore, both amlodipine and atorvastatin have been demonstrated to reduce cardiovascular events in a broad range of patients' in hypertensive patients with three concomitant cardiovascular risk factors but normal to mildly elevated cholesterol levels, amlodipine combined with atorvastatin demonstrated a reduction in cardiovascular events. The amlodipine/atorvastatin single pill has been shown to improve patients; achievement of national-guideline-recommended blood pressure and lipid target levels and exhibits a safety profile consistent with its parent compounds. The combination pill is now available in parts of Europe in formulations containing either 5 or 10 mg amlodipine and 10 mg atorvastatin. Amlodipine combined with atorvastatin has been demonstrated to reduce cardiovascular events in hypertensive patients at high cardiovascular risk, and the single-pill formulation has the potential to improve adherence and decrease prescription costs. These potential benefits are associated with important implications because hypertensive patients with additional risk factors represent a large proportion of those at risk for cardiovascular events.

Use of 24-h ambulatory blood pressure monitoring to assess blood pressure control: a comparison of olmesartan medoxomil and amlodipine besylate

Olmesartan medoxomil is an angiotensin II receptor blocker with similar antihypertensive efficacy as the calcium channel blocker amlodipine besylate in patients with mild-to-moderate hypertension. In addition to a drug's ability to lower blood pressure, the effectiveness of the agent in enabling patients to achieve specific blood pressure targets is an important clinical consideration. This secondary analysis of a randomized, double-blind study compared the efficacy of olmesartan medoxomil with that of amlodipine besylate in achieving ambulatory blood pressure goals among patients with mild-to-moderate hypertension. Following a 4-week placebo run-in, 440 study participants aged >or=18 years were randomized to olmesartan medoxomil (20 mg/day), amlodipine besylate (5 mg/day), or placebo for 8 weeks. The proportion of participants achieving specific systolic and diastolic ambulatory blood pressure goal levels was calculated by dividing the number of participants who had achieved a particular blood pressure goal by the total number of patients in the intent-to-treat population. After 8 weeks of treatment, a mean 24-h ambulatory blood pressure of <130/80 or <130/85 mmHg was achieved by significantly more participants in the olmesartan medoxomil group (18.1 and 30.4%, respectively) than in the amlodipine besylate (7.0 and 14.0%, respectively) or placebo (1.9% for both) groups. The target daytime ambulatory blood pressure of <135/85 mmHg was achieved by more participants in the olmesartan medoxomil group than in the amlodipine besylate group (15.8 vs. 5.8%, respectively; P<0.01). In a previous publication of the same study, we demonstrated that starting doses of olmesartan medoxomil and amlodipine besylate produced similar mean reductions in blood pressure. In this subanalysis of the blood pressure data from that primary publication, however, olmesartan medoxomil therapy was shown to result in a greater proportion of patients achieving specific ambulatory blood pressure goals than therapy with amlodipine besylate. As blood pressure goal attainment may be of more direct clinical relevance than numerical blood pressure lowering, the achievement of blood pressure goals should be a key efficacy parameter assessed in clinical trials of antihypertensive medications.

A single-pill combination of amlodipine besylate and atorvastatin calcium

This review describes the clinical profile and rationale for the development of a single-pill formulation of the calcium channel blocker amlodipine besylate, a blood pressure-lowering agent with pleiotropic effects, and atorvastatin calcium, a statin with lipid-lowering as well as pleiotropic anti-atherosclerotic properties. Amlodipine and atorvastatin have been demonstrated in numerous clinical trials to be highly effective in lowering blood pressure and low-density lipoprotein cholesterol (LDL-C). Furthermore, both amlodipine and atorvastatin have been demonstrated to reduce cardiovascular events in a broad range of patients. The amlodipine/atorvastatin single pill has been shown to improve patients' achievement of national guideline-recommended blood pressure and lipid target levels and exhibits a safety profile consistent with its parent compounds. The combination pill is available in formulations appropriate for administration across therapeutic dose ranges targeted to a wide variety of hypertensive patients with additional risk factors and differing degrees of cardiovascular risk, or with manifest cardiovascular disease. Single-pill amlodipine/atorvastatin has the potential to improve the management of hypertensive patients with additional cardiovascular risk factors, especially dyslipidemia, by reducing pill burden and prescription costs. This potential has important implications because hypertensive patients with additional risk factors represent a large proportion of those at risk for cardiovascular events.