LAM Extra for General Practicioners

[MODERN BETA-BLOCKER THERAPY FROM THE CARDIOLOGIST’S VIEWPOINT]

ÉDES István

OCTOBER 25, 2010

LAM Extra for General Practicioners - 2010;2(04)

[Following the publication of some large, randomised trials (LIFE, ASCOT), the benefits of the use of beta-blockers in hypertension have been questioned. On the basis of these clinical trials it has been posited that beta-blockers administered for the treatment of hypertonia are less effecient for stroke prevention. It has been suggested that first-generation beta-blockers (atenolol) have adverse metabolic effects (insulin sensitivity, lipid parameteres), which might contribute to the differences observed in clinical outcomes. On the basis of a number of clinical trials and meta-analyses performed in recent years it is now evident that the most important goal is to reach target blood pressure levels, which is usually achieved by combination therapy. Choosing drugs on the basis of strict protocols is less important. In general, beta-blockers remain one of the most important drug class for the treatment of hypertension. The author reviews the pharmacology of the cardioselective, vasodilatory drug nebivolol in detail, as well as clinical trials on nebivolol. Nebivolol has a neutral (or rather beneficial) effect on metabolic parameters (lipid parameters, blood glucose level and insulin sensitivity) as well as on left ventricular function. If hypertension is associated with cardiovascular diseases (left ventricular dysfunction, ischaemic hears disease, atrial fibrillation), nebivolol offers an excellent therapeutic alternative due to its excellent tolerability and side effect profile]

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LAM Extra for General Practicioners

[PAIN AND PAIN CONTROL IN RHEUMATOLOGY]

GAÁL János

[In developed industrial countries the overall population prevalence of chronic rheumatic pain is around 35%. A classification that is useful in everyday practice is based on the origin of musculoskeletal pain and lists pain associated with degenerative joint diseases, pain related to metabolic bone diseases, non-articular and soft tissue rheumatism, and pain due to inflammation. In chronic pain syndrome pain itself has lost its adaptive biological role, and presents as a pathogenetic factor in its own right, accompanied by significant vegetative and psychological symptoms. Therapeutic exercise is of basic importance in the management of rheumatic pain. It is supplemented by various pharmacologic and nonpharmacologic methods. The latter include, among others, fomentations, packs, balneo- and hydrotherapeutic methods, electro-, mechanoand thermotherapeutic approaches. Pharmacological therapy usually means the use of simple analgesics, non-steroidal antiinflammatory drugs, steroids, minor opiates, and, lately, also major opiates, which may be supplemented by adjuvant agents such as tricyclic antidepressants and anticonvulsive drugs. When indicating the most often used non-steroidal antiinflammatory drugs, their potential side effects should carefully be considered. Invasive pain-killing methods on the border area between anaesthesiology and rheumatology (epidural steroid administration, ganglionic blockade, intravenous regional blockade) are applied in cases that do not respond to conventional therapy, and sometimes also as successful first-line intervention.]

LAM Extra for General Practicioners

[CARDIOVASCULAR PREVENTION OPPORTUNITIES OF RISK REDUCTION, 2010]

NAGY András Csaba

[10 years of experience following the millennium has confirmed again that data on long term cardiovascular morbidity and mortality can be influenced by effective prevention most substantially. Growing body of knowledge and experience in the field of modern cardiovascular prevention is available, but novel and novel milestone studies have been published leading to updating of guidelines, however, we cannot be satisfied with the results. Evidence suggest that despite recent efforts, Hungarian cardiovascular morbidity and mortality has not been reduced significantly and except for some success - acute ST elevation myocardial infarction care in accordance with the European standard - we are behind the other EU countries in cardiovascular mortality of the active (age 30-65 years) age group. Recently several interesting contradiction has been published in the field of prevention, like the effectiveness of aspirin as primer prevention, which changes our common prevention conception. Data have to be also addressed, which can explain the controversial results from a different point of view. Now we are talking about the results of REALITY study, which highlight not only the noncompliance of the patient but that of the physician as well.]

LAM Extra for General Practicioners

[CARVEDILOL AND ITS ANTIOXIDANT EFFECT]

KOVÁCS Imre

[Carvedilol, the typical basic variant of the third generation beta blocker drugs is a complex adrenergic blocker that also has Ca channel blocking effects. It has no effect of the metabolism and has a pregnant antioxidant effect that is significant for cardiac and hypertension target organ protection. Its beneficial effect on cardiac decompensation, on target organ protection in patients with hypertension and on primary and secondary prevention of ischemic heart disease is proven by clinical studies. The effect of free radicals trapping - not shown by the majority of beta blockers - plays a major role in these beneficial effects. Inflammatory factors and free radicals (ROS) play a central role in cardiovascular diseases and can be regarded as prognostic markers of vascular damage. Elevated levels of glucose, lipids, or elevated intraluminal pressure triggers the production of various free radicals. The anti-inflammatory effect of carvedilol results out of its antioxidant (scavenger) and ROS suppressive effects. Besides its complex adrenergic blocking effect, this ability of carvedilol gives a molecular explanation for its efficiency proven by clinical trials.]

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

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[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.]

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[Nebivolol: the long-acting, vasodilatator beta-blocker]

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[Nebivolol is a third-generation, long-acting, vasodilator beta-adrenoceptor-blocker with very high selectivity to beta-1 receptor. In addition to its efficient blood pressure lowering effect, results of previous trials have shown that nebivolol, which has a vasodilator effect and improves endothelial dysfunction, offers a safe, well-tolerable therapeutic option for elderly patients with heart failure, chronic pulmonary disease, diabetes, hyperlipidaemia and hypertension. It does not affect or improves lipid and carbohydrate metabolism, moreover, it can improve patients’ quality of life in multiple ways.]

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[Epidemiology, comorbidity, etiology of depression and cardiovascular diseases]

PÉTER László, RIHMER Zoltán

[Psychiatric problems are a common comorbid condition in patients with cardiovascular disease. Depression is a well-known risk factor for the development of cardiovascular disease and mortality too. Psychiatric and cardiovascular diseases are prevalent public health problems in the western world. Depression is associated with endo­thelial dysfunction and increased platelet aggregation, which may explain the consequent cardiovascular complications. Specific affective temperaments may be associated with special cardiovascular diseases. Antidepressant therapy does not only reduce depression but also cardiac mortality.]

Hypertension and nephrology

[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

[Focus on central arterial pressure. Beta blockers - one group of agents with different efficacy]

BARNA István

[Not only have beta blockers excellent antihypertensive effect but both in monotherapy and in combination they exert antiarrhythmic and antiischemic efficacy, as well. They are recommended on A level of evidence in the treatment of patients with primary hypertension. Certain beta blockers differ from each other considering their lipid solubility, membrane stabilizing effect and in many other characteristics which difference can be exploited in the treatment. Nebivolol increases the release of nitrogen oxide, it is metabolically neutral and has vasodilating and antioxidant effect. The consequence of the stiffness of the arterial wall is the rise of systolic blood pressure, the diminshed diastolic circulation in the coronary vessels, the increase of the central pulse pressure and the frequent occurrence of cardiovascular diseases. Various antihypertensive agents have different mode of action on central blood pressure and arterial stiffness. Comparing nebivolol/atenolol and nebivolol/bisoprolol, respectively, nebivolol decreased aortic pulse pressure with greater efficacy than other beta blockers. The extent of the reduction of blood pressure was the same in the nebivolol and atenolol group while the augmentation index decreased significantly among the patients receiving nebivolol. In addition to the well known beneficial effects of nebivolol recent studies proved another, yet still unknown and unique characteristic of this agent, i.e. favourable influence on arterial stiffness. It not only improves endothelial dysfunction which has emphasized role on development of atherosclerosis but - independently of its antihypertensive effect - it has favourable action on arterial stiffness, too. These features guarantee a decisive position in the treatment of arterial hypertension.]