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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

DECEMBER 20, 2016

[Deeper analysis of nebivolol effects]

KÉKES Ede

[Author presents the formation of nitric oxide as a largest vasodilator of human endothelium as well as the endothelial dysfunction a result of formation at adrenergic stimulus. He demonstrates in detail the benefits of selective β-1 blocker and β-3 adrenergic agonist nebivolol in the vascular system. This drug has also receptor independent effects. Complex effects of nebivolol causes vasodilation, inhibits oxidative stress and it is capable to neutralize the effects of free oxygen radicals and as a result the endothelial function will be better. Its clinical effects and the less wellknown beneficial properties are listed. The use of drug is discussed especially in hypertensives with smoking, COPD or PAD. The β-3 agonist effect provides positive reactions not only in the adipocytes and the myocardial tissue. but in the skeletal muscle as well: Increase in energy expenditure - as a compensatory mechanism - is increased in obesity and the glucose uptake + storage on skeletal muscle cells are increased in hyperglycemia. The insulin sensitivity will be better, leptin level is decreased, adiponectin level is increased by nebivolol. It is assumed this drug has antidiabetic and anti-obesity effects.]

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.]

Hypertension and nephrology

MARCH 20, 2015

[Effects of peripheral resistance lowering and elevating beta-blockers on central blood pressure - nebivolol in focus]

BENCZÚR Béla

[Central blood pressure, that is, blood pressure (BP) in the ascending aorta, is considered an important physiologic parameter as it reflects the hemodynamic relationship between the heart and the aorta, both in systole and in diastole. In the systolic phase, central BP represents the pressure against which the left ventricle has to eject blood during systolic contraction. Thus, central arterial pressure reflects both left ventricular stroke volume and afterload, defines cardiac work, and contributes to the development of left ventricular hypertrophy in hypertensive individuals. In the diastolic phase, central BP is a key determinant of the blood flow delivery to the myocardium. Despite the increasing knowledge regarding the importance of central blood pressure and the availability of non-invasive measurement technics it couldn’t spread in everyday clinical practice and rarely or not mentioned in the therapeutic guidelines. The different antihypertensiv drugs significantly differs based on their effects on central blood pressure particularly β-blockers. The so-called ’classical’ β-blockers have un - favourable effect on central blood pressure due to increasing peripherial vascular resistance. In the opposit the vasodilating β-blockers including nebivolol markedly decrease central blood pressure which could explain their beneficial effects.]

Clinical Neuroscience

JULY 30, 2013

[Nebivolol in treatment of multiplex aneurysms]

OLÁH Csaba, DEMETER Béla, SZÓLICS Alex, LÁZÁR István

[Introduction - We examined the effect of nebivolol on blood pressure control after subarachnoidal hemorrhage in three patients with multiple aneurysms. Patients and methods - Endovascular intervention was applied to treat the bleeding aneurysms of all patients, and the silent aneurysms were followed-up. In all patients nebivolol was used as long-term anti-hypertensive medication. Results - With nebivolol treatment the blood pressure in our patients was maintained in the normal range with no unexpected shoot-ups. The size of the silent aneurysms did not increase and the endovascularly treated aneurysms demonstrated acceptable morphology on follow-up catheterangiography. Discussion - After endovascular treatment of the bleeding aneurysm, strict blood pressure control is essential in those with multiple aneurysms to prevent the rupture of silent aneurysms. Antihypertensive medications with a 24-hour effect are preferable. Nebivolol seemed to be an appropriate medication for this purpose in all of our patients.]

LAM Extra for General Practicioners

DECEMBER 15, 2011

[ANTIHYPERTENSIVE THERAPY IN PATIENTS WITH COPD - THE SIGNIFICANCE OF NEBIVOLOL]

FARSANG Csaba

[The occurrence of hypertension associated with chronic obstructive pulmonary disease (COPD) is increasing. Recognising COPD is important in order to choose the appropriate antihypertensive drugs. Antihypertensive drugs that can be used to treat patients with hypertension and COPD include diuretics, ACE-inhibitors, angiotensine receptor blockers (AT1 receptor antagonists) and calcium antagonists, as well as cardioselective beta blockers, as these drugs decrease total and cardiovascular mortality. Of these agents, the importance of the most cardioselective one, nebivolol should be stressed, as this drug has no clinically significant effect on parameters of respiratory function, and, through its additional effects (namely by increasing the synthesis of NO), it has a beneficial effect on COPD-related deterioration of respiratory functions, haemodynamic alterations (cor pulmonale) and local factors that participate in the respiratory inflammation and endothelial dysfunction.]

Hypertension and nephrology

DECEMBER 20, 2011

[Antihypertensive therapy in patients with COPD - the significance of nebivolol]

FARSANG Csaba

[The occurrence of hypertension associated with chronic obstructive pulmonary disease (COPD) is increasing. Recognising COPD is important in order to choose the appropriate antihypertensive drugs. Anti-hypertensive drugs that can be used to treat patients with hypertension and COPD include diuretics, ACE-inhibitors, angioten-sine receptor blockers (AT1 receptor antagonists) and calcium antagonists, as well as cardioselective beta blockers, as these drugs decrease total and cardiovascular mortality. Of these agents, the importance of the most cardioselective one, nebivolol should be stressed, as this drug has no clinically significant effect on parameters of respiratory function, and, through its additional effects (namely by increasing the synthesis of NO), it has a beneficial effect on COPD-related deterioration of respiratory functions, haemodynamic alterations (cor pulmonale) and local factors that participate in the respiratory inflammation and endothelial dysfunction.]