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Hypertension and nephrology

FEBRUARY 20, 2019

[Carvedilol in chronic kidney disease]

CSIKY Botond

[Chronic kidney disease (CKD) is endemic affecting 850 million people worldwide. Adequate antihypertensive treatment slows the progression of the kidney disease and also decreases the mortality of this population. Because of the comorbidities and the high cardiovascular risk beta-blockers have to be administered frequently in these patients. Carvedilol is a 3rd generation non-selective beta-blocker with alpha- 1 receptor blocking and antioxidant properties. It is metabolically neutral, it does not increase the risk of new onset diabetes and it does not increase the patients’ body weight. In some animal models of CKD and in several human CKD studies carvedilol has shown to have nephroprotective properties and it also decreased the cardiovascular risk in combination therapies.]

Hypertension and nephrology

APRIL 20, 2018

[Role of β-blockers, especially carvedilol in the treatment of hypertension]

PÁLL Dénes, MARODA László, ZRÍNYI Miklós

[Changes in hypertension guidelines in the past years have affected the clinical thinking about β-blockers. Authors reviewed the development of β-blockers emphasizing the differences across various active pharmaceutical agents. Different hemodynamic and metabolic effects are being discussed in details for the third ge - neration vasodilatator carvedilol. Carvedilol has no effect on cardiac output but decreases peripheral vascular resistance which results in lower blood pressure values. However, carvedilol, opposite to unfavorable effects of traditional β-blockers, has a neutral impact on both carbohydrate and lipid metabolisms. Its more advanced cardiac effects include decreased left ventricular hypertrophy and increased coronary flow reserve. Vasodilatator type β-blockers (carvedilol, nebivolol) are indicated in the combi - nation treatment of hypertension, especially when the patient has heart failure, coronary disease or suffered from a previous heart attack.]

Hypertension and nephrology

MARCH 20, 2018

[Nebivolol’s unique molecule structure and its effect onthe quality of life]

KERKOVITS Gábor

[The β receptor blockers have very different effects depending on their receptor selectivity, ISA effect, which gives a wide opportunity of beneficial therapeutic choice. Resulting from its unique molecule structure nebivolol has its unique effects. It consists two isomers in 1:1 ratio. D-nebivolol is a highly β1 receptor blocker, while l-nebivolol causes NO release resulting vasodilatation. As a result of this dual effect, nebivolol more strongly reduces the blood pressure. The pressure reducing effect of nebivolol is stronger than 25 mg of atenolol, and is equal with the effect of 100 mg of atenolol. Nebivolol has a significantly higher responders’ rate than bisoprolol, and significantly fewer adverse effect. Comparing to losartan nebivolol produces significantly higher reduction in systolic and in diastolic blood pressure as well. Nebivolol has beneficial haemodynamic effects. It raises the stroke volume by 20.6 percent, the cardias output by 7.1 per cent, the ejection fraction by 7.8 per cent while reduces the peripheral resistance by 13.2 per cent. Both at rest and during exercise nebivolol cases significantly higher reduction in pulmonary wedge pressure than atenolol. Nebivolol has a better profile of adverse effects. The following adverse effects were observed: fatigue in 1.3 per cent, cold extremities in 0.8 per cent, impotence in 0.08 per cent and dyspnea in 0.05 per cent. It has also a beneficial effect on erectile dysfunction. It cases a significant elevation in erectile dysfunction score from 17.22 to 22.09. The number of sexual activity also raised from 3.41 to 6.38 during nebivolol treatment. The prevalence of erectile dysfunction is also significantly lower as compared to any β receptor blocker. Nebivolol has a synergic effect on PDE5 blockers, raises the cGMP concentration in the erectile tissue. There is also a significant difference among the β receptor blockers in the reduction of exercise tolerance. The nonselective β receptor blocker cause 40 per cent, carvedilol 35 per cent, the β1 selective receptor blocker 25 per cent while nebivolol 6 per cent reduction in the duration time.]

Hypertension and nephrology

SEPTEMBER 20, 2015

[Carvedilol therapy in hypertension]

KÉKES Ede

[Author analyzed the properties and antihypertensive effect of one of the best beta blockers with vasodilative effects, the carvedilol on the base of the Hungarian and international literature . Author deals with this issue for many years and he presented his own experience. The beta blockers could never be missed on therapy of the endemic hypertension. They are equivalent to other drug family. This played a big role , that the new , strong beta-1 selective and -- especially 3. generation beta blockers (carvedilol and nebivolol) - came to the fore in the therapy of hypertension compared with conventional beta blockers. The carvedilol has many beneficial properties, as vasodilatation, antioxidant effect, beneficial effect on the vascular stiffness, regression of left ventricular hypertrophy, increasing coronary reserve. Carvedilol is able to stable success on the therapy of hypertension as monotherapy or combination with the other drugs. In Hungary the physicians applied beta blockers about 30-35% in the treatment of hypertension.]

Hypertension and nephrology

JUNE 25, 2015

[The use of beta-blockers in Hungary 2007-2014 based on data from National Health Insurance]

BARNA István, GYURCSÁNYI András

[disease, various rhythm disturbances, migraine, essential tremor case, addition to the treatment of endocrine disorders caused tachycardia and also may be used in the treatment of systolic and diastolic heart failure. Using the National Health Insurance Fund (NHIF) database, we analyzed changes in the turnover of beta-blockers used domestically between 2007 and 2014. At the beginning of the period more than 50% was metoprolol as the used active ingredient, the end of the period, nebivolol became the most frequently assigned active agent betablocker (29%). Besides nebivolol the use of bisoprolol and carvedilol increased, among the “old” beta-blockers the use of pindolol, bopindolol continuously decreases, propranolol and sotalolol consumption stagnant after the initial small decrease. Metabolic syndrome, disorders of carbohydrate metabolism, in case of sleep apnea the advantage of nebivolol is accompanied by the status of enhanced sympathetic activity and consequent reduction of RAS activation. Vasodilation, inhibition of plaque formation, reduction of platelet aggregation and anti-proliferative effects of nebivolol are its unique characteristics in the beta-blocker group. Improves insulin sensitivity, thus it is not characterized by a long-term side effects that cause diabetes. Effective reduction in the central blood pressure with nebivolol is likely to reduce the risk of complications in stroke and other related central blood pressure. Therefore, if the recommendations of the international and domestic support for considering it is not surprising that the use of metoprolol reduced such a large extent and how nebivolol covered the significant majority of the entire domestic beta-blockers market. Carvedilol was before the second and currently has become the 3rd or 4th most frequently used beta blocker. The decrease in the use of metoprolol undoubtedly caused by change in the recommendations, getting out of the subsidized products, and the appearance of the above known, new effective drugs.]

Lege Artis Medicinae

SEPTEMBER 20, 2011

[The use of carvedilol following invasive interventions]

KOVÁCS Imre

[The primary goals of the treatment of AMI are to rapidly open - either mechanically or by thrombolysis - the blocked blood vessel and to keep it open. Restarting of the blood flow in blocked vessels results in an increased load in volume, pressure and metabolism in the blood vessel's supply area, which triggers the activation of a pathophysiological cascade. Pathophysiological processes accompanying the opening of the blood vessel include activation of catecholamines, RAS and neutrophils and subsequent free radical production, and increases in the levels of proinflammatory citokines and intracellular CA levels, that is, the so called oxygen paradox. The above mentioned processes can be blocked by beta receptor blockers (BRB) as demonstrated by class I, type A evidence. A number of clinical studies have shown their clinical efficiency following PCI. The PAMI, StentPAMI, AirPAMI and CADILLAC studies have proved that BRBs decrease mortality and morbidity after the intervention. The third-generation BRB carvedilol, which acts as a beta and alpha blocker in patients with STEMI successfully treated with PCI, and is also a Ca-channel blocker and a free radical trap, is the firstchoice agent for both theoretical and clinical reasons. Animal studies have shown that carvedilol results in greater reductions in the levels of markers indicating postinfarction reperfusion and ventricular remodeling (MCP1, MMP2, TIMP2) compared with metoprolol. Animal studies have also showed that carvedilol is the most efficient BRB for preventing the damaging of gap junction structure in reperfusion, and for inhibiting the ventricular arrhythmias induced by reperfusion, through restoring connexin 43. The beneficial effect of this drug on the cardiovascular events and mortality following myocardial infarction have been demonstrated in a number of human studies with hard endpoints. The unique efficiency of carvedilol in vascular prevention following PCI has been demonstrated by the short-term and longterm efficiency of carvedilol-filled stents, compared with BMSE-filled stents. Information on the postintervention, long-term (3-year) efficiency of carvedilol in a large (N :7500) patient group is expected to be published in 2015 in the CAPITAL-RCT study coordinated by the University of Kyoto. In summary, the results of experimental and clinical studies on carvedilol have shown that within the BRB group, carvedilol is highly recommended for the prevention of oxygen paradox following successful PCI and preserving the myocardium.]

Lege Artis Medicinae

JULY 14, 2007

[THE USE OF BETA RECEPTOR BLOCKERS IN CHRONIC HEART FAILURE]

CZURIGA István

[The beneficial effects of treatment with betablockers in patients with chronic heart failure have been demonstrated in several large, prospective, randomised, placebo-controlled clinical trials. In large trials with mortality as the endpoint, the long-term use of bisoprolol, carvedilol, nevibolol and metoprolol succinate have been associated with a reduction in total mortality, cardiovascular mortality, sudden cardiac death and death due to progression of heart failure in patients of functional classes II-IV. These favorable clinical experiences warrant a recommendation that beta-blockers should be used in all haemodynamically stable heart failure patients with reduced left ventricular systolic function who are on standard treatment, unless contraindicated. In this review, the most important data of clinical trials and practical considerations of therapy with beta-blockers in heart failure are summarized.]