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How CaV1.2-bound verapamil blocks Ca2+ influx into cardiomyocyte: Atomic level views.
Li, W, Shi, G
Pharmacological research. 2019;:153-157
Abstract
The first clinically used antiarrhythmic, antianginal and anti-hypertensive phenylalkylamine, verapamil's cardiovascular activity is inextricably linked to its ability to antagonize Ca2+ overload via blocking CaV1.2, a cardiac L-type Ca2+ channel of undisputed physiological and pharmacological importance in cardiovascular disorders such as myocardial ischemia-reperfusion injury. From a structural point of view, however, the action mechanism of verapamil is still elusive. Therefore, incorporating previous findings for verapamil and CaV1.2, this review article puts forward two experimental data-derived and -supported 3D structure models for CaV1.2's α1 subunit and its verapamil-bound form. Furthermore, this article suggests three biophysical mechanisms, namely competitive binding, steric hindrance and electrostatic repulsion, towards an atomic level understanding of how verapamil blocks the L-type Ca2+ current mediated by CaV1.2 in reality, which can be useful for the design and development of next-generation Ca2+ antagonists to provide safer and more effective treatment of cardiovascular diseases.
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2.
[Use of Verapamil and Dilthiasem in treating patients at high cardiovascular risk (review of literature)].
Baryshnikova, GA, Chorbinskayva, SA, Stepanova, II, Blochina, OE, Zverkov, IV, Maslovskyi, LV, Korchazhkina, NB, Maslennikova, OM
Meditsina truda i promyshlennaia ekologiia. 2016;(2):15-8
Abstract
The article deals with usage of nondihydropiridine calcium antagonists--verapamil and dilthiasem--in treating patients with arterial hypertension, cardiomyopathy and arrhythmia, for secondary prevention of IHD. Data also concern cardio-, angio--and nephroprotective activity of the medications, their ability to prevent left ventricle hypertrophy, possible usage in patients after myocardial infarction. The authors also discuss problems of tolerance and safety of calcium antagonists with prolonged action vs. those with short-term action.
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3.
Brewing the right cocktail for radial intervention.
Vuurmans, T, Hilton, D
Indian heart journal. 2010;(3):221-5
Abstract
Radial access angioplasty has increased in popularity worldwide due to its decrease of access site complications, early patient mobility, patient comfort and lower costs. In a minority of patients, radial artery occlusion and radial artery spasm occurs. Because of the dual blood supply to the hand, radial artery occlusion is not associated with major clinical sequelae but prevention is important. Radial artery spasm rarely leads to serious vascular complications but can cause patient discomfort and can result in prolonging or failure of the procedure. Pharmacological and non-pharmacological strategies have been evaluated to prevent radial artery occlusion and radial artery spasm. A number of pharmacological 'cocktails' have been successfully tested but there is currently no agreement on the optimal combination of agents. In order to evaluate the best strategy to prevent radial artery occlusion and radial artery spasm we reviewed the relevant studies to date. From these studies it is clear that a 'cocktail' of agents should be given before transradial coronary angiography or angioplasty. A combination of heparin, nitroglycerin and verapamil is associated with the best preventive outcome.
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4.
Verapamil for cluster headache. Clinical pharmacology and possible mode of action.
Tfelt-Hansen, P, Tfelt-Hansen, J
Headache. 2009;(1):117-25
Abstract
Verapamil is used mainly in cardiovascular diseases. High-dose verapamil (360-720 mg) is, however, currently the mainstay in the prophylactic treatment of cluster headache. The oral pharmacokinetics are variable. The pharmacodynamic effect of verapamil, the effect on blood pressure, also varies considerably among subjects. The dose of verapamil used for cluster headache is approximately double the dose used in cardiovascular disease, most likely because verapamil is a substrate for the efflux transporter P-glycoprotein in the blood-brain barrier. The access of verapamil to the central nervous system is therefore limited. The clinical use of verapamil in cluster headache is reviewed and several relevant drug interactions are mentioned. Finally, its possible mode of action in cluster headache is discussed. The effect of verapamil in cluster headache most likely takes place in the hypothalamus.Verapamil is an L-type calcium channel blocker but it is also a blocker of other calcium channels (T-, P-, and possibly N- and Q-type Ca(2+) channels) and the human ether-a-go-go-related gene potassium channel. With so many different actions of verapamil, it is impossible at the present time to single out a certain mode of action of the drug in cluster headache.
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5.
[Clinical application of verapamil in patients with supraventricular cardiac rhythm disturbances and arterial hypertension].
Volkov, VE, Babaev, FZ, Pshenitsin, AI, Zhezheva, FM, Mazur, NA
Kardiologiia. 2008;(7):30-4
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6.
Adenosine vs. calcium channel blockers for supraventricular tachycardia.
Anugwom, C, Sulangi, S, Dachs, R
American family physician. 2007;(11):1653-4
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7.
Trandolapril/verapamil combination in hypertensive diabetic patients.
García Donaire, JA, Ruilope, LM
Vascular health and risk management. 2007;(1):77-82
Abstract
Cardiovascular diseases are directly affected by arterial hypertension. When associated with diabetes mellitus, the potential deleterious effects are well amplified. Both conditions play a central role in the pathogenesis of coronary artery disease, heart failure, stroke, and renal insufficiency. Prevalence of hypertension is much higher among diabetic than non-diabetic patients, and the hypertensive patient is more likely to develop type 2 diabetes. Current international guidelines recommend aggressive reductions in blood pressure (BP) in hypertensive patients with additional risk factors, including cardiovascular risk factors, and emphasize the relevance of intensive reduction in patients with diabetes mellitus; a goal of 130/80 mm Hg is required. To achieve BP target a combination of antihypertensives will be needed, and the use of long-acting drugs that are able to provide 24-hour efficacy with a once-daily dosing confers the noteworthy advantages of compliance improvement and BP variation lessening. Lower dosages of the individual treatments of the combination therapy can be administered for the same antihypertensive efficiency as that attained with high dosages of monotherapy. Angiotensin-converting enzyme inhibitors and calcium-channel blockers as a combination have theoretically compelling advantages for vessel homeostasis. Trandolapril/verapamil sustained release combination has showed beneficial effects on cardiac and renal systems as well as its antihypertensive efficacy, with no metabolic disturbances. This combination can be considered as an effective therapy for the diabetic hypertensive population.
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8.
Managing hypertension in diabetic patients--focus on trandolapril/verapamil combination.
Sharma, SK, Ruggenenti, P, Remuzzi, G
Vascular health and risk management. 2007;(4):453-65
Abstract
Hypertensive diabetes individuals are at higher risk for cardiovascular events and progression to end stage renal disease. Several well conducted clinical trials indicate that aggressive treatment of hypertension in individual with diabetes reduces these complications. Combinations of two or more antihypertensive drugs are frequently required to reach the target blood pressure and to improve the cardiovascular and renal outcomes in these patients. There are physiological and clinical rationales for renin-angiotensin system blockade in hypertensive diabetics. Trandolapril/verapamil sustained released (SR) is a fixed-dose combination of trandolapril and a sustained release formulation of verapamil and indicated in treatment of hypertension in patients who require more than one drug to reach target blood pressure. The antihypertensive efficacy of trandolapril/verapamil SR has been evaluated extensively in large trials. In the INVEST trial, a verapamil SR-based treatment strategy that included trandolapril in most patients was effective in reducing the primary outcome in hypertensive patients with coronary artery disease. The new onset of diabetes was also significantly lower in the verapamil SR/trandolapril treatment group in comparison with those on the atenolol/hydroclorothiazide treatment group. The BErgamo NEphrologic Diabetes Complications Trial (BENEDICT) documented that in hypertensive diabetes and normoalbuminuria, trandolapril plus verapamil or trandolapril alone delayed the onset of microalbuminuria independent of their blood pressure-reducing effect. Thus, trandolapril/verapamil is an effective option for treatment of hypertensive diabetes patients requiring more than one agent to achieve target blood pressure.