Abstract:
:Ca2+ channel antagonists are agents that interact with the voltage-dependent Ca2+ channel in a highly specific way. The prototype agents of cardiovascular importance are verapamil, nifedipine, and diltiazem, in historical order of appearance. These agents all have different molecular structures and bind separately with receptor sites located in or near the calcium channel, at molecular sites still to be fully identified. There are probably three distinct receptor sites (V, N, D) which stand in relation to the "gate" of the long-acting "L" calcium channel. There is probably overlap among the receptor sites, especially between the V and D sites to explain their common properties. All three agents inhibit the voltage-dependent calcium channel in vascular smooth muscle and also myocardial slow calcium channels. The ratio of the arterial to the myocardial effect is an index of the arterial selectivity, generally held to be a desirable property because the negative inotropic effect is usually a liability. The general clinical impression that nifedipine is the agent most active in vascular tissue in relation to the myocardial effect is supported by data on the relative potencies of these three agents on blood perfused dog preparations and by a comparison of the potency on rat vascular (portal vein) versus myocardial effects. Nonetheless all three agents are highly active in the inhibition of K(+)-induced vascular contractions (nifedipine 10(-9) M to 10(-8) M; verapamil 10(-7) M to 10(-6) M; and diltiazem 5 x 10(-7) M to 10(-6) M; concentrations for 50% inhibition of K(+)-induced vascular contractions in rat or rabbit aorta; comparative data for resistance vessels not available). The clinical impression that verapamil and diltiazem are more active on nodal tissue is also supported by a comparison of potencies on blood perfused dog nodal preparations in comparison with effects on coronary flow, with verapamil and diltiazem being approximately 10x more potent on the AV node than increasing coronary blood flow, so that the nodal effect is first detected. These basic pharmacological properties explain why all these three agents have clinical effects relevant to inhibition of vascular contraction (antihypertensive and antianginal effects) and only verapamil and diltiazem have clinically relevant inhibitory effects on the AV node (inhibition of supraventricular tachycardias). The comparative potencies of verapamil, diltiazem, and nifedipine in angina and hypertension will be examined in Parts II and III of this review.
journal_name
Cardiovasc Drugs Therjournal_title
Cardiovascular drugs and therapyauthors
Opie LHdoi
10.1007/BF02209083subject
Has Abstractpub_date
1987-12-01 00:00:00pages
411-30issue
4eissn
0920-3206issn
1573-7241journal_volume
1pub_type
杂志文章,评审abstract:BACKGROUND:Acute ST-elevation myocardial infarction (STEMI) is associated with a high incidence of complications as well as a considerable hospitalization rate and economic burden. Preliminary evidence suggests that remote ischemic conditioning (RIC) is a promising non-invasive intervention that may effectively and saf...
journal_title:Cardiovascular drugs and therapy
pub_type: 杂志文章
doi:10.1007/s10557-020-07022-9
更新日期:2020-06-30 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::People who consume a diet rich in fruit and vegetables have lower risks of cancer, cardiovascular disease and all-cause mortality. Many prospective cohort studies have reported inverse associations between dietary intake or blood levels of beta-carotene and risks of cancer. Several large-scale trials were set up to as...
journal_title:Cardiovascular drugs and therapy
pub_type: 杂志文章,评审
doi:10.1023/a:1022134418372
更新日期:2002-09-01 00:00:00
abstract::The place of digoxin in the pediatric cardiologist's armamentarium remains uncertain. As an antiarrhythmic, its use in the Wolff-Parkinson-White syndrome is obsolete, but it remains useful in the treatment of the chronic atrial fibrillation seen in some patients postoperatively and in children with dilated cardiomyopa...
journal_title:Cardiovascular drugs and therapy
pub_type: 杂志文章,评审
doi:10.1007/BF01881525
更新日期:1989-03-01 00:00:00
abstract::Elgodipine is a new second-generation dihydropyridine calcium antagonist. Its hemodynamic and antiischemic properties were evaluated in a single-blind, placebo-controlled trial in 22 males with chronic stable angina. Coronary artery disease was angiographically confirmed. Measurements were performed with a Swan-Ganz t...
journal_title:Cardiovascular drugs and therapy
pub_type: 临床试验,杂志文章
doi:10.1007/BF00878092
更新日期:1995-08-01 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::Free radical injury may contribute to the delayed postoperative recovery of myocardial metabolism and ventricular function after elective coronary artery revascularization. This clinical study was designed to evaluate, in stable angina patients having aortocoronary bypass surgery, whether orally administered alpha-toc...
journal_title:Cardiovascular drugs and therapy
pub_type: 临床试验,杂志文章
doi:10.1007/BF00054753
更新日期:1991-03-01 00:00:00
abstract::Recent surveys in the U.S. have reported, for the first time, that a significant number of patients with hypertension are finding that the cost of medication and treatment in general is an obstacle to treatment. The cost of management of hypertension can be contained if: a) the diagnostic workup is kept simple (this d...
journal_title:Cardiovascular drugs and therapy
pub_type: 杂志文章
doi:10.1007/BF01857624
更新日期:1989-10-01 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::The effects of administration of guava and papaya fruit (100 g/day), vegetables, and mustard oil (5 g/day) (group A); antioxidant vitamins C (50 mg/day) and E (30 mg/day), plus betacarotene (10 mg/day) (group B); a high-fat (5-10 g/day) (group C); or a low-fat (4-5 g/day) diet (group D) were compared over 24 diet week...
journal_title:Cardiovascular drugs and therapy
pub_type: 杂志文章
doi:10.1007/BF00879869
更新日期:1995-12-01 00:00:00
abstract::Thiazide diuretics are particularly efficacious in the treatment of hypertension in blacks. A number of observations suggest that many hypertensive blacks have features consistent with a status of "corrected" volume expansion. Our studies, as well as those of other investigators, show that the Na,K pump is inhibited i...
journal_title:Cardiovascular drugs and therapy
pub_type: 杂志文章,评审
doi:10.1007/BF02603181
更新日期:1990-03-01 00:00:00
abstract::In order to compare and clarify the effects of various antiarrhythmic drugs when given as monotherapy, we reevaluated our previous data on antiarrhythmic drugs and recalculated antiarrhythmic plasma concentrations of drugs for several canine arrhythmia models. We used three spontaneously occurring arrhythmias: a) digi...
journal_title:Cardiovascular drugs and therapy
pub_type: 杂志文章
doi:10.1007/BF00120829
更新日期:1991-08-01 00:00:00
abstract::Cardiovascular disease is the leading cause of death in men and women in the USA. Once a patient experiences an acute coronary syndrome (ACS), they are at increased risk for hospital readmission within 30 days and 6 months after discharge and more importantly, they have worse survival. Hospital readmissions lead to po...
journal_title:Cardiovascular drugs and therapy
pub_type: 杂志文章
doi:10.1007/s10557-018-6798-6
更新日期:2018-12-01 00:00:00
abstract::Heart rate variability is a noninvasive indicator of autonomic nervous system activity. The role of the autonomic nervous system in the genesis of atrial or ventricular arrhythmias is now well established. Little is known about the effects of flecainide on heart rate variability in patients with normal heart structure...
journal_title:Cardiovascular drugs and therapy
pub_type: 杂志文章
doi:10.1023/a:1007710301259
更新日期:1998-10-01 00:00:00
abstract::Based on a retrospective analysis of the DAVIT II database, we attempted to propose subgroups of post-infarction patients with heart failure, who might benefit or not benefit from antiischemic medical intervention. In DAVIT II, patients were randomized in a double-blind fashion to either verapamil 360 mg/day or placeb...
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:10.1007/BF00877400
更新日期:1994-12-01 00:00:00
abstract::The following discourse addresses the pharmacologic profile of KT-362, its clinical potential as an anti-arrhythmic agent with associated hypotensive effects, as well as its additional related potential in myocardial ischemia and related sequellae, and the specific cellular actions that may be responsible for these po...
journal_title:Cardiovascular drugs and therapy
pub_type: 杂志文章,评审
doi:10.1007/BF02018262
更新日期:1990-10-01 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::To compare the antiischemic effects of intracoronary administration of a beta blocker, atenolol, and of a calcium antagonist, nifedipine, on the clinical and electrocardiographic signs of myocardial ischemia induced by balloon occlusion of the coronary artery, we studied 32 consecutive patients undergoing routine PTCA...
journal_title:Cardiovascular drugs and therapy
pub_type: 杂志文章
doi:10.1007/BF00051147
更新日期:1992-06-01 00:00:00
abstract::Understanding and controlling the consequences of myocardial ischemia requires us to acknowledge that we are dealing with a complex, dynamic, and highly variable process. The severity and progression of ischemic injury is not solely determined by the extent of oxygen deprivation, but by many other factors, including t...
journal_title:Cardiovascular drugs and therapy
pub_type: 杂志文章,评审
doi:10.1007/BF00054247
更新日期:1988-05-01 00:00:00
abstract::Cholesterol plays an essential role in cell membrane synthesis and in cell growth and differentiation. In mammalian cells, cholesterol can be synthesized from acetate precursors or taken up from dietary or exogenous sources. The major catabolic route for disposal of cholesterol involves conversion into excretable bile...
journal_title:Cardiovascular drugs and therapy
pub_type: 社论,评审
doi:10.1007/BF00054556
更新日期:1992-04-01 00:00:00
abstract::When choosing antihypertensive agents for the treatment of hypertension, it is necessary to consider the predisposition of individuals to renal damage, which may be associated with the long-term effect of such agents. In this respect, this study examined the effect of two commonly used antihypertensive drugs (Brinerdi...
journal_title:Cardiovascular drugs and therapy
pub_type: 杂志文章
doi:10.1007/BF00879029
更新日期:1995-06-01 00:00:00
abstract:OBJECTIVE:The aim was to study the pharmacodynamic interactions and safety of the co-administration of the calcium sensitizer levosimendan and the calcium antagonist felodipine in patients with coronary heart disease (CHD) and with normal ejection fraction (EF). METHODS:The study was a randomized, double blind, placeb...
journal_title:Cardiovascular drugs and therapy
pub_type: 临床试验,杂志文章,随机对照试验
doi:10.1023/b:card.0000015860.08185.6d
更新日期:2003-09-01 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::Intravenous amiodarone has been found useful in the emergent management of life-threatening arrhythmias. Experimental studies have shown that its electrophysiologic effects are proportional to its myocardial concentration. However, early after its intravenous administration, the extent of the concentration of amiodaro...
journal_title:Cardiovascular drugs and therapy
pub_type: 杂志文章
doi:10.1023/a:1007756411790
更新日期:1999-05-01 00:00:00
abstract::Male Japanese white rabbits were fed a restricted amount (100 g/head/day) of an atherogenic diet containing 0.2% cholesterol and 6% peanut oil during an 8-week experimental period. Atherosclerotic lesions, characterized by intimal thickening with lipid deposition, were produced by de-endothelialization of the rabbit a...
journal_title:Cardiovascular drugs and therapy
pub_type: 杂志文章
doi:10.1007/BF00878516
更新日期:1993-04-01 00:00:00
abstract:BACKGROUND:The use of sodium-glucose co-transporter 2 inhibitors (SGLT2i) is currently expanding to cardiovascular risk reduction in non-diabetic subjects, but renal (side-)effects are less well studied in this setting. METHODS:Male non-diabetic Sprague Dawley rats underwent permanent coronary artery ligation to induc...
journal_title:Cardiovascular drugs and therapy
pub_type: 杂志文章
doi:10.1007/s10557-020-06954-6
更新日期:2020-06-01 00:00:00
abstract:AIMS:Rapid restoration of sinus rhythm using pharmacological cardioversion is commonly indicated in patients with symptomatic recent-onset atrial fibrillation (AF). The objectives of this large, international, multicenter observational study were to determine the safety and effectiveness of intravenous (IV) vernakalant...
journal_title:Cardiovascular drugs and therapy
pub_type: 杂志文章
doi:10.1007/s10557-020-07103-9
更新日期:2020-11-18 00:00:00
abstract::Unselective and beta 1-selective beta-blockers may induce vasoconstriction of normal and stenotic epicardial coronary arteries. To analyze the influence of the "vasodilatory" beta-blocker celiprolol on coronary vasomotility, 0.4 mg celiprolol/kg were intravenously infused over 4 minutes in 13 patients with coronary ar...
journal_title:Cardiovascular drugs and therapy
pub_type: 临床试验,杂志文章
doi:10.1023/a:1007780713915
更新日期:1997-04-01 00:00:00
abstract:PURPOSE:The glucagon-like peptide-1 (GLP-1) has been shown to exert cardioprotective effects in animals and patients. This study tests the hypothesis that preservation of GLP-1 by the GLP-1 receptor agonist liraglutide or the dipeptidyl peptidase-4 (DPP-4) inhibitor linagliptin is associated with a reduction of angiote...
journal_title:Cardiovascular drugs and therapy
pub_type: 杂志文章
doi:10.1007/s10557-015-6592-7
更新日期:2015-06-01 00:00:00
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 b...
journal_title:Cardiovascular drugs and therapy
pub_type: 杂志文章,评审
doi:10.1007/BF00877225
更新日期:1994-08-01 00:00:00