Abstract:
:The majority of calcium antagonists used clinically belong to three distinct chemical classes: the phenylalkylamines, the dihydropyridines, and the benzothiazepines. In recent years their mode of action has been unravelled, their limitations recognized, and their efficacy and use in the management of patients with a broad spectrum of cardiovascular and other disorders defined. It is clear, however, that these drugs are not all alike, providing an explanation for their differing effects. The final therapeutic effect in humans depends on the mechanisms of action at the molecular level, the tissue selectivity, and the hemodynamic changes of each agent. All these aspects are examined in detail in this article. Concepts that are highlighted are as follows: (a) Molecular biology has allowed recognition of the polypeptide components of the alpha 1 subunit of the L-type Ca2+ channel and the finding of peptide segments covalently labelled by all three classes of drugs. (b) The location of these segments within the peptides is different: Binding sites for dihydropyridines are located externally, whereas those for verapamil and diltiazem are located internally, in the cytosolic part of the membrane. (c) Dihydropyridine binding is voltage dependent. This explains the selectivity of this class of drugs for vascular smooth muscle, which is more depolarized than cardiac muscle. (d) Phenylalkylamines and benzothiazepines reach their receptors at the internal surface of the sarcolemma through the channel lumen. Their binding is facilitated by the repetitive depolarization of atrioventricular and cardiac tissue, a phenomenon described as use dependence. This explains why these drugs are not highly selective, but equipotent for the myocardium, the atrioventricular conducting tissue, and the vasculature. (e) Dihydropyridines act through selective vasodilatation and may increase heart rate and contractility via a reflex mechanism. On the contrary, phenylalkylamines and diltiazem act through a combination of effects, including reduction of afterload, heart rate, and contractility. When taken together, all these differences distinguish the preferential clinical utilization of one of these compounds for a given cardiovascular pathology.
journal_name
Cardiovasc Drugs Therjournal_title
Cardiovascular drugs and therapyauthors
Ferrari R,Cucchini F,Bolognesi R,Bachetti T,Boraso A,Bernocchi P,Gaia G,Visioli Odoi
10.1007/BF00877225subject
Has Abstractpub_date
1994-08-01 00:00:00pages
565-75eissn
0920-3206issn
1573-7241journal_volume
8 Suppl 3pub_type
杂志文章,评审abstract::Thrombolytic therapy has gained widespread acceptance as a means of treating coronary artery thrombosis in patients with acute myocardial infarction. Although experimental data have demonstrated that timely reperfusion limits the extent of infarction caused by regional ischemia, there is growing evidence that reperfus...
journal_title:Cardiovascular drugs and therapy
pub_type: 杂志文章,评审
doi:10.1007/BF00133206
更新日期:1989-01-01 00:00:00
abstract::The combination of aspirin and clopidogrel is the mainstay antiplatelet therapy for acute coronary syndromes (ACS). However, the dosing of aspirin, the dosing of clopidogrel, the timing of clopidogrel initiation as well as the duration of clopidogrel therapy remain controversial matters. Clopidogrel resistance is an e...
journal_title:Cardiovascular drugs and therapy
pub_type: 杂志文章,评审
doi:10.1007/s10557-009-6212-5
更新日期:2010-02-01 00:00:00
abstract::In vitro and in vivo studies have demonstrated many similarities between the three calcium antagonists verapamil, nifedipine, and diltiazem in relation to protection of the myocardium during hypoxia. Important clinical differences exist between the three drugs when they are used during or after an acute myocardial inf...
journal_title:Cardiovascular drugs and therapy
pub_type: 杂志文章,评审
doi:10.1007/BF03029738
更新日期:1991-08-01 00:00:00
abstract:BACKGROUND:Markers of thrombosis, inflammation, endothelial dysfunction and neurohumoral activation such as fibrinogen, D-dimer, C-reactive protein, von Willebrand factor, tumour necrosis factor-alpha and chromogranin-A are reported to be linked to the increase of cardiovascular risk for atherosclerosis progression and...
journal_title:Cardiovascular drugs and therapy
pub_type: 临床试验,杂志文章,多中心研究,随机对照试验
doi:10.1023/a:1024394610648
更新日期:2003-01-01 00:00:00
abstract:PURPOSE:To assess whether glycoprotein IIb/IIIa inhibition using tirofiban in low risk patients undergoing percutaneous coronary intervention (PCI) may reduce the risk of periprocedural myocardial infarction compared to standard care in poor responders to aspirin and/or clopidogrel. METHODS:We will enroll patients at ...
journal_title:Cardiovascular drugs and therapy
pub_type: 杂志文章,多中心研究,随机对照试验
doi:10.1007/s10557-008-6121-z
更新日期:2008-08-01 00:00:00
abstract::Early reperfusion represents the key strategy in ST elevation myocardial infarction. However, reperfusion may induce myocardial damage due to the reperfusion myocardial injury, compromising the full potential of reperfusion therapy and accounting for unfavourable results in high risk patients. Adenosine seems to atten...
journal_title:Cardiovascular drugs and therapy
pub_type: 杂志文章,评审
doi:10.1007/s10557-015-6606-5
更新日期:2015-01-01 00:00:00
abstract:PURPOSE:Oxidative stress plays an important role in the pathogenesis of cardiovascular diseases. Azelnidipine is a novel dihydropyridine calcium channel blocker. Several studies have demonstrated that some dihydropyridine calcium channel blockers have antioxidant effects. We evaluated the antioxidant effects of azelnid...
journal_title:Cardiovascular drugs and therapy
pub_type: 杂志文章
doi:10.1007/s10557-007-6008-4
更新日期:2007-02-01 00:00:00
abstract:BACKGROUND:High health service expenditure on the one hand, and the politically declared objective of stability of statutory contributions and restriction of public funds on the other hand, have been central points of the political and social discussion for several years. The over-proportional increase in health servic...
journal_title:Cardiovascular drugs and therapy
pub_type: 杂志文章
doi:10.1023/a:1015323700206
更新日期:2002-01-01 00:00:00
abstract::One hundred thirteen patients undergoing cardiopulmonary bypass were randomly assigned to receive either bovine or porcine heparin. Heparin was infused at 4.5 mg/kg during bypass and administered at the lesser of 70 units/kg or 5000 units/dose at 12-hour intervals postoperatively. Platelet counts decreased to 45% of p...
journal_title:Cardiovascular drugs and therapy
pub_type: 临床试验,杂志文章,随机对照试验
doi:10.1007/BF01857644
更新日期:1990-02-01 00:00:00
abstract::Torsades de pointes (TdP) is a life-threatening ventricular tachycardia that occurs in the setting of a prolonged QT interval and is most frequently related to administration of antiarrhythmic drugs. Patients with organic heart disease, with low serum electrolyte levels, with a previous episode of TdP and with bradyca...
journal_title:Cardiovascular drugs and therapy
pub_type: 杂志文章,评审
doi:10.1007/BF03029778
更新日期:1991-04-01 00:00:00
abstract:PURPOSE:The aim of this study was to evaluate the efficacy and safety of intravenous infusion of low-dose flecainide (50 mg) followed by oral pilsicainide (50 mg t.i.d.)in patients with paroxysmal atrial fibrillation (AF). METHODS:Thirty-one patients with symptomatic and hemodynamically stable AF lasting less than 48 ...
journal_title:Cardiovascular drugs and therapy
pub_type: 临床试验,信件
doi:10.1023/a:1024368111557
更新日期:2003-01-01 00:00:00
abstract:OBJECTIVE:Permanent polymer drug-eluting stents (DES) are associated with a higher risk of late and very late stent thrombosis (ST); biodegradable polymer drug-eluting stents (BP-DES) were designed to reduce these risks. However, their benefits are not completely clear. METHOD:We undertook a meta-analysis of randomize...
journal_title:Cardiovascular drugs and therapy
pub_type: 杂志文章,meta分析
doi:10.1007/s10557-014-6528-7
更新日期:2014-08-01 00:00:00
abstract::The present study was performed in order to compare the efficacy, safety, and tolerability of lisinopril, a long-acting angiotensin-converting enzyme (ACE) inhibitor, with captopril, the shorter acting ACE inhibitor available, in the treatment of elderly patients (mean age 70 +/- 0.5 years) with congestive heart failu...
journal_title:Cardiovascular drugs and therapy
pub_type: 临床试验,杂志文章,多中心研究,随机对照试验
doi:10.1023/a:1007704024393
更新日期:1997-03-01 00:00:00
abstract::Inhibition of the renin-angiotensin system has been a highly successful therapeutic approach for the prevention of hypertension-related end organ damage. Angiotensin converting enzyme inhibitors and angiotensin II receptor blockers lower blood pressure and reduce morbidity and mortality in patients with cardiovascular...
journal_title:Cardiovascular drugs and therapy
pub_type: 杂志文章,评审
doi:10.1007/s10557-010-6278-0
更新日期:2011-02-01 00:00:00
abstract::Early reperfusion after an organ ischemia is essential to salvage tissue from eventual death. However, abundant evidence suggests that reperfusion also elicits pathophysiological changes responsible for additional tissue injury after restoration of blood flow. Postconditioning (Postcon) defined as rapid sequential int...
journal_title:Cardiovascular drugs and therapy
pub_type: 杂志文章,评审
doi:10.1007/s10557-010-6240-1
更新日期:2010-06-01 00:00:00
abstract::Eighteen hypertensive patients (13 males, 5 females; age 48 +/- 13; diastolic blood pressure greater than 95 mmHg), either previously untreated or who had been off treatment for more than 3 months, underwent M-mode echocardiography before (DO) and after (D90) 3 months of nicardipine therapy (60-90 mg/day). All echocar...
journal_title:Cardiovascular drugs and therapy
pub_type: 临床试验,杂志文章
doi:10.1007/BF01865511
更新日期:1989-08-01 00:00:00
abstract::Excess activity of the sympathetic nervous system (SNS) is linked to human obese hypertension and to salt-sensitive hypertension. Paradoxically, reduced SNS activity has been implicated as a contributor to obesity, particularly in animal models, and salt loading usually inhibits SNS activity. We have investigated the ...
journal_title:Cardiovascular drugs and therapy
pub_type: 杂志文章
doi:10.1007/BF00120497
更新日期:1996-06-01 00:00:00
abstract::The DAVIT-II trial has shown that the verapamil type of calcium antagonist can beneficially be used in post-infarct patients. A recent re-analysis suggests that verapamil may also prevent post-infarct sudden death. There are good theoretical reasons to suppose that calcium antagonists should help prevent ventricular f...
journal_title:Cardiovascular drugs and therapy
pub_type: 临床试验,社论,评审
doi:10.1007/BF03029739
更新日期:1991-08-01 00:00:00
abstract::The present study was undertaken on 10 patients with angina undergoing percutaneous transluminal coronary angioplasty. The angioplasty procedure consisted of two successive 30-second balloon inflations at 5 minute intervals. After the first inflation, nicorandil (0.1 mg/kg) was given intravenously over a 2-minute peri...
journal_title:Cardiovascular drugs and therapy
pub_type: 临床试验,杂志文章
doi:10.1007/BF00878473
更新日期:1995-03-01 00:00:00
abstract::Diabetic cardiomyopathy as a distinct entity was first recognized by Rubler et al. in diabetics with congestive heart failure (CHF), who had no evidence of coronary atherosclerosis. The Framingham study showed a 2.4-fold increased incidence of CHF in diabetic men and a 5.1-fold increase in diabetic women over 18 years...
journal_title:Cardiovascular drugs and therapy
pub_type: 杂志文章,评审
doi:10.1007/BF00877091
更新日期:1994-02-01 00:00:00
abstract::This article considers the dominant role of trials involving thousands of patients--the mega-trials--in cardiovascular disease. Problems with large trials mean that alternative strategies must be developed to aid the introduction of new drugs. The limitations of meta-analysis, and of trials with combined and surrogate...
journal_title:Cardiovascular drugs and therapy
pub_type: 杂志文章,评审
doi:10.1007/BF00053034
更新日期:1997-01-01 00:00:00
abstract::This review will present a summary of a description of apoptotic pathways in the heart, followed by ways to measure it and the experimental and clinical evidence for the role of apoptosis in cardiac disease. An evaluation of the effectiveness of pharmacological and other therapeutic interventions in the prevention of ...
journal_title:Cardiovascular drugs and therapy
pub_type: 杂志文章,评审
doi:10.1023/a:1013715704835
更新日期:2001-11-01 00:00:00
abstract::The aim of the present study was to investigate the effects of almokalant on sustained reentrant supraventricular tachycardias. Reentrant tachycardias were induced, using transesophageal atrial stimulation, in 82 patients with atrioventricular reentrant tachycardia (n = 54) or AV nodal reentrant tachycardia (n = 28). ...
journal_title:Cardiovascular drugs and therapy
pub_type: 临床试验,杂志文章
doi:10.1023/a:1007761825414
更新日期:1997-07-01 00:00:00
abstract:PURPOSE:The mitogen-activated protein kinase phosphatases (MKPs) are a family of dual-specificity phosphatases that inactivate MAPKs by dephosphorylation. Impairment of MKP-1 expression in insulin resistance has been suggested to affect the cardioprotective properties of insulin. We hypothesized that manipulation of it...
journal_title:Cardiovascular drugs and therapy
pub_type: 杂志文章
doi:10.1007/s10557-017-6731-4
更新日期:2017-06-01 00:00:00
abstract:PURPOSE:Single- and multiple-dose studies were conducted to assess the pharmacokinetics, pharmacodynamics and safety of tolvaptan in healthy Japanese subjects. METHODS:All studies were single-center, randomized, placebo-controlled, single-blind or double-blind. In an ascending single-dose study, subjects were given a ...
journal_title:Cardiovascular drugs and therapy
pub_type: 临床试验,杂志文章,随机对照试验
doi:10.1007/s10557-011-6299-3
更新日期:2011-12-01 00:00:00
abstract::The direct myocardial protective effects of intracoronary infusions of cromakalim and pinacidil were determined in an anesthetized canine model of coronary occlusion and reperfusion. The left circumflex coronary artery was occluded for 90 minutes and reperfused for 5 hours, at which time the infarct size was determine...
journal_title:Cardiovascular drugs and therapy
pub_type: 杂志文章
doi:10.1007/BF01857755
更新日期:1990-04-01 00:00:00
abstract:RATIONALE:Pulmonary hypertension (PH) represents a serious health complication accompanied with hypoxic conditions, elevated levels of asymmetric dimethylarginine (ADMA), and overall dysfunction of pulmonary vascular endothelium. Since the prevention strategies for treatment of PH remain largely unknown, our study aime...
journal_title:Cardiovascular drugs and therapy
pub_type: 杂志文章
doi:10.1007/s10557-016-6700-3
更新日期:2016-12-01 00:00:00
abstract::Cilazapril, an angiotensin-converting enzyme inhibitor, and mibefradil, a selective T-type voltage-operated calcium channel blocker, have been shown to prevent neointima formation after vascular injury. The goal of the present study was to evaluate the mechanism of action of both drugs. For this purpose, the influence...
journal_title:Cardiovascular drugs and therapy
pub_type: 杂志文章
doi:10.1007/BF00823586
更新日期:1996-05-01 00:00:00
abstract::During acute myocardial ischemia, passage of potassium ions across the sarcolemma to the extracellular space is a well-established phenomenon. A recent hypothesis is that the ATP-dependent potassium channel plays a role in contributing to the potassium loss. As the potassium loss starts while the overall level of ATP ...
journal_title:Cardiovascular drugs and therapy
pub_type: 杂志文章,评审
doi:10.1007/BF00877615
更新日期:1993-08-01 00:00:00
abstract:PURPOSE:In addition to lowering hemoglobin A1C, colesevelam has been shown to improve the atherogenic lipoprotein profile of subjects with type 2 diabetes mellitus (T2DM) when used in combination with metformin and/or sulfonylureas. A recent study evaluated the effects of colesevelam as antidiabetes monotherapy in adul...
journal_title:Cardiovascular drugs and therapy
pub_type: 杂志文章,多中心研究,随机对照试验
doi:10.1007/s10557-014-6516-y
更新日期:2014-06-01 00:00:00