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Amlodipine heart block

Arijit Das, Prakash Kumar, Abha Kumari, Satish Chandra, Manju Gari, Nidhi Singh, Debleena Dey
BACKGROUND: The relation between hypertension and hyperuricemia has been established by epidemiological studies. Calcium channel blockers are one of the first-line drugs for newly diagnosed patients with essential hypertension. Cilnidipine is a new calcium channel blocker acting by blocking both L- and N-type calcium channels. The aim of this study was to compare the effectiveness of amlodipine and cilnidipine in patients with essential hypertension and their effects on heart rate and serum uric acid levels...
October 2016: Cardiology Research
Thomas A Dewland, Elsayed Z Soliman, Barry R Davis, Jared W Magnani, Jose-Miguel Yamal, Linda B Piller, L Julian Haywood, Alvaro Alonso, Christine M Albert, Gregory M Marcus
IMPORTANCE: Cardiac conduction abnormalities are associated with an increased risk for morbidity and mortality, and understanding factors that accelerate or delay conduction system disease could help to identify preventive and therapeutic strategies. Antifibrotic and anti-inflammatory properties of angiotensin-converting enzyme inhibitors and treatment for hyperlipidemia may reduce the risk for incident conduction system disease. OBJECTIVE: To identify the effect of pharmacologic therapy randomization and clinical risk factors on the incidence of conduction system disease...
August 1, 2016: JAMA Internal Medicine
Jasmina Jović-Stosić, Vesna Putić, Dragan Zivanović, Milica Mladenov, Gordana Brajković, Snelana Djordjević
INTRODUCTION: Calcium channel blockers and beta-blockers are among the most frequently ingested cardiovascular drugs in self-poisoning causing significant mortality. Intravenous lipid emulsion (ILE) is reported as a potentially novel antidote for treatment of acute poisoning caused by some of these drugs. CASE REPORT: We presented two cases of poisoning with these drugs. The case 1, a 24-year-old woman ingested amplodipine, metformin and gliclazide for self-poisoning...
January 2016: Vojnosanitetski Pregled. Military-medical and Pharmaceutical Review
Alan H Gradman
LCZ696 is a single molecule which combines the angiotensin receptor blocker valsartan with the neprilysn inhibitor sacubitril (AHU377). In the recently published PARADIGM-HF trial, LCZ696 proved superior to enalapril in reducing overall mortality, heart failure hospitalizations, and other endpoints in patients with systolic dysfunction heart failure. Increases in counter-regulatory natriuretic peptides which oppose sodium retention, vasoconstriction, and the deleterious structural changes which follow neurohormonal activation are thought to account for these improved outcomes...
May 2015: Current Hypertension Reports
Amarah Shakoor, Maaman Zahoor, Alina Sadaf, Najveen Alvi, Zehra Fadoo, Arjumand Rizvi, Farheen Quadri, Fateh Ali Tipoo, Mohammad Khurshid, Zaffar Sajjad, Steven Colan, Babar S Hasan
INTRODUCTION: Sideroblastic cardiomyopathy secondary to repeated blood transfusions is a feared complication in thalassaemia. Control of myocardial iron is thus becoming the cornerstone of thalassaemia management. Recent evidence suggests a role for L-type Ca(2+) channels in mediating iron uptake by the heart. Blocking the cellular iron uptake through these channels may add to the benefit of therapy to standard chelation in reducing myocardial iron. We aim to determine the efficacy of amlodipine (a calcium channel blocker) as an adjunct to standard aggressive chelation in retarding myocardial iron deposition in thalassaemics with or without cardiomyopathy...
December 8, 2014: BMJ Open
Yanlin Zhu, Fen Wang, Quan Li, Mingshe Zhu, Alicia Du, Wei Tang, Weiqing Chen
Amlodipine is a commonly prescribed calcium channel blocker for the treatment of hypertension and ischemic heart disease. The drug is slowly cleared in humans primarily via dehydrogenation of its dihydropyridine moiety to a pyridine derivative (M9). Results from clinical drug-drug interaction studies suggest that CYP3A4/5 mediate metabolism of amlodipine. However, attempts to identify a role of CYP3A5 in amlodipine metabolism in humans based on its pharmacokinetic differences between CYP3A5 expressers and nonexpressers failed...
February 2014: Drug Metabolism and Disposition: the Biological Fate of Chemicals
Bertrand Caillier, Sylvie Pilote, Dany Patoine, Xavier Levac, Christian Couture, Pascal Daleau, Chantale Simard, Benoit Drolet
Type II diabetes was shown to prolong the QT interval on the ECG and to promote cardiac arrhythmias. This is not so clear for metabolic syndrome, a precursor state of type II diabetes. The objectives of the present study were to generate a guinea pig model of metabolic syndrome by long-term exposure to diabetogenic diets, and to evaluate the monophasic action potential duration (MAPD)-modulating effects of drugs in these animals. Male Hartley guinea pigs were fed with either the control, the High Fat High Sucrose (HFHS) or the High Fat High Fructose (HFHF) diet for 150 days...
March 2012: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
Qiong Luo, Wan-ling Xuan, Fang Xi, Yu-lin Liao, Masafumi Kitakaze
OBJECTIVE: To compare the effects of amlodipine, benidipine and nifedipine on myocardial hypertrophy and evaluate the underlying mechanism. METHODS: Myocardial hypertrophy model was created by transverse aortic constriction (TAC) in C57 BL/6 mice, and plasma catecholamine concentrations were measured 7 days after surgery to confirm the sympathetic activation. The 3 drugs were administered in TAC mice for 7 days and cardiac hypertrophy was evaluated according to the heart-to-body weight ratio (HW/BW)...
April 2010: Nan Fang Yi Ke da Xue Xue Bao, Journal of Southern Medical University
Yoshitaka Hirooka, Kenji Sunagawa
Calcium channel blockers are widely used for the treatment of hypertension. Although they are effective for their strong vasodilator action, there are concerns regarding related baroreflex-mediated activation of sympathetic nervous system. However, long-acting calcium channel blockers, such as amlodipine, are now known safe for the treatment of hypertension. Furthermore, the new type of calcium channel blockers, such as cilnidipine with N-type calcium channel blocking action, or azelnidipine that has sympatho-inhibitory action with anti-oxidant effect, provide a new insight for the future use of calcium channel blockers...
January 2010: Clinical Calcium
A Grothusen, D Divchev, M Luchtefeld, B Schieffer
Chronic activation of the renin-angiotensin system (RAS) plays a crucial role in the development of various cardiovascular diseases (CVD). Thus, effective RAS inhibition has been a major achievement to improve the treatment of patients at risk for CVDs, such as myocardial infarction, heart failure and stroke. Three substance classes that block RAS-activation are currently available, angiotensin converting enzyme (ACE) inhibitors, angiotensin II type 1 receptor blockade (ARB) and renin inhibitors. Although the overall goal of these drugs remains the blockade of RAS activation, their individual targets in this system vary and may substantially influence the clinical benefit derived from the long term use of these substances...
December 2009: Minerva Cardioangiologica
A Takahara, Y Nakamura, H Wagatsuma, S Aritomi, A Nakayama, Y Satoh, Y Akie, A Sugiyama
BACKGROUND AND PURPOSE: The heart of the canine model of chronic atrioventricular block is known to have a ventricular electrical remodelling, which mimics the pathophysiology of long QT syndrome. Using this model, we explored a new pharmacological therapeutic strategy for the prevention of cardiac sudden death. EXPERIMENTAL APPROACH: The L-type Ca(2+) channel blocker amlodipine (2.5, L/N-type Ca(2+) channel blocker cilnidipine (5, or the angiotensin II receptor blocker candesartan (12 mg...
November 2009: British Journal of Pharmacology
Michio Fujisawa, Ryosuke Yorikane, Shigetoshi Chiba, Hiroyuki Koike
Azelnidipine, a dihydropyridine calcium channel blocker unlike other dihydropyridine calcium channel blockers, does not increase but slightly decreases heart rate (HR) in clinical settings. In the present study, the mechanism for the HR-lowering action characteristic of azelnidipine was investigated in anesthetized dogs. In the in situ perfused sinus node preparation, the negative chronotropic action of azelnidipine was almost 5 times more potent than that of amlodipine. When injected intravenously in intact anesthetized dogs, both drugs produced a long-lasting blood pressure reduction, but the action of azelnidipine developed more slowly than that of amlodipine...
April 2009: Journal of Cardiovascular Pharmacology
J D Thomason, T L Fallaw, K P Carmichael, M A Radlinsky, C A Calvert
BACKGROUND: Calcium channel blocking drugs, usually nifedipine and less often amlodipine, have been reported to cause gingival hyperplasia (GH) in humans. HYPOTHESIS: Amlodipine, a dihydropyridine calcium channel blocking drug, can cause GH when administered chronically to older small dogs with degenerative valvular disease. ANIMALS STUDIED: From January 2004 to May 2008, 82 client-owned dogs with degenerative valvular disease and left atrial dilatation were treated with amlodipine in combination with spironolactone and enalapril and followed for >6 months...
January 2009: Journal of Veterinary Internal Medicine
Ru-xing Wang, Jian-ping Song, Xiang-jun Yang, Zhi-hua Liu, Ting-bo Jiang, Hong-xia Li, Lin Zhou, Xiao-rong Li, Wen-ping Jiang
OBJECTIVE: To investigate the effects of different amlodipine isomers on L-type calcium current (ICa-L) and kinetics of rat ventricular myocytes. METHODS: Rat ventricular myocytes were isolated by enzyme digestion. ICa-L, peak currents, I-V curves, steady state activation curves, steady state inactivation curves and recovery curves from inactivation with S-amlodipine, R-amlodipine and R, S-amlodipine at concentrations of 0.1, 0.5, 1, 5, and 10 micromol/L were recorded by whole-cell patch clamp configuration...
May 2008: Zhonghua Xin Xue Guan Bing za Zhi
Ru-Xing Wang, Wen-Ping Jiang
To investigate the effects of S- and R-amlodipine (Aml) on action potential (AP) and L-type calcium channel current (ICa-L), the whole-cell patch-clamp technique was used on rat ventricular myocytes to record AP, ICa-L, peak currents, steady-state activation currents, steady-state inactivation currents, and recovery currents from inactivation with S-Aml and R-Aml at various concentrations. Increasing concentrations of S-Aml gradually shortened AP durations (APDs). At concentrations of 0.1, 0.5, 1, 5, and 10 micromol/L, S-Aml blocked 1...
September 2008: Canadian Journal of Physiology and Pharmacology
Bernard R Chaitman, Junko Sano
Pharmacologic therapy to alleviate symptoms in chronic angina has been enhanced by the recent approval of several novel compounds that complement the traditional approach using beta-adrenergic blocking drugs, calcium antagonists, and long-acting nitrates. In the United States, ranolazine, a drug that inhibits late I(Na), was approved for patients with chronic angina that remain symptomatic on beta-blockers, calcium antagonists, or long-acting nitrates, on the basis of an acceptable safety profile and efficacy in several randomized placebo controlled studies...
February 2007: Clinical Cardiology
Jessica D Dietz, Sarah Du, Charles W Bolten, Maria A Payne, Chunsheng Xia, James R Blinn, John W Funder, Xiao Hu
Calcium channel blockers are widely used antihypertensives. Mineralocorticoid receptor antagonists are also used to treat hypertension and heart failure. We report here that a number of widely used dihydropyridine class calcium channel blockers are able to inhibit aldosterone-induced activation of mineralocorticoid receptor. These dihydropyridines varied in the extent of their effect on mineralocorticoid receptor, with nimodipine and felodipine the most potent and amlodipine the least. In contrast, both diltiazem and verapamil, nondihydropyridine calcium channel blockers, had no effect on mineralocorticoid receptor...
March 2008: Hypertension
Heinz Rupp
Angiotensin (AT) II and noradrenaline play major roles in hypertension, stroke and coronary heart disease, which are themselves interlinked. Harmful effects of AT II are not blocked solely by angiotensin-converting enzyme inhibitors, as it is now evident that AT II is generated by other enzymes such as chymase. Angiotensin II also stimulates noradrenaline release modulated by presynaptic receptors on sympathetic nerves. Numerous studies have defined the action of the AT II type 1 receptor blocker (ARB) eprosartan as controlling noradrenergic and adrenergic effects, resulting from actions on the renin-angiotensin-aldosterone system and the sympathetic nervous system...
November 2007: Current Medical Research and Opinion
Ji-Young Park, Kyoung-Ah Kim, Pil-Whan Park, Ock-Je Lee, Jong Hyeon Ryu, Geun Hyeog Lee, Mun Choun Ha, Jin Sun Kim, Seoung Woo Kang, Kyung Ryul Lee
BACKGROUND: Amlodipine, a dihydropyridine calcium channel antagonist, is prescribed for the management of angina and hypertension. It is used therapeutically as a racemic mixture, composed of S- and R-enantiomers, but its calcium channel-blocking effect is confined to S-amlodipine; R-amlodipine has 1000-fold less activity than its S-enantiomer. OBJECTIVE: The objective of this study was to compare the pharmacokinetic and pharmacodynamic properties and safety profiles of a newly developed amlodipine formulation, composed wholly of S-amlodipine, with those of the conventionally prescribed racemic formulation...
November 2006: Clinical Therapeutics
David Putnam, Deborah Griffis, Trent P McLaughlin, Raul Arocho, Simon Tang
The relative efficacy of long-acting calcium channel antagonists and angiotensin II receptor blocking agents has been described in clinical trials; however, their effectiveness in an actual practice setting has not been well studied. This study assessed the effectiveness of 2 commonly prescribed antihypertensives, amlodipine and losartan, either as monotherapy or as add-on for patients insufficiently controlled on beta-blocker or diuretic therapy. This was a retrospective, observational study that utilized electronic medical records...
March 2006: American Journal of Therapeutics
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