LAM Extra for General Practicioners



OCTOBER 25, 2010

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

[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.]



Further articles in this publication

LAM Extra for General Practicioners


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


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


ÉDES István

[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]

All articles in the issue

Related contents

Clinical Neuroscience

[Vinpocetin in neurological diseases]

SZAPÁRY László, KÉSMÁRKY Gábor, TÓTH Kálmán, MISNYOVSZKY Melinda, TÓTH Tímea, BALOGH Ágnes, NAGY Krisztián, NÉMETH György, FEHÉR Gergely

[Introduction - Stroke is the third leading cause of death worldwide (following cardiovascular and cancer mortality) and associated with serious disability for the vast majority of patients. There is no salvage therapy for irreversibly damaged brain areas, improving the circulation of the surrounding hypoperfused territories may be associated with benefitial clinical states. Cerebral hypoperfusion may play a role in the pathogenesis of other kind of neurological diseases, improvement of global circulation may have a preventive effect on these conditions. Aims - The aim of our study was to review the experimental and clinical articles focusing on the role of vinpocetin in different neurological conditions. Results - Vinpocetin appears to have several different mechanisms of action that allow for its antiinflammatory, antioxidant, vasodilating, antiepileptic and neuroprotective activities in experimental conditions. On the other hand, several meta-analysis of the existing studies in acute stroke examining short and long term fatality rates with vinpocetin was unable to assess efficacy. In chronic cerebrovascular patients, vinpocetin improves impaired hemorheological variables, has significant vasodilating properties, improves endothelial dysfunction, neuroimaging studies showed selective increase in cerebral blood flow and cerebral metabolic rate, all of which are potentially beneficial in cerebrovascular disease and may improve cognitive functions. Summary - Based on the above mentioned results vinpocetin plays an important role both in basic research and in clinical management of different neurological diseases.]

Hypertension and nephrology

[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.]

Lege Artis Medicinae

[The use of carvedilol following invasive interventions]


[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

[Experience with coenzyme Q10 in heart failure]

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Lege Artis Medicinae

[Pycnogenol in the clinical practice of French maritime pine bark extractum]

KISS István, TAVASZY Mariann, FARSANG Csaba

[Polyphenols, which belong to the group of flavonoids, can be found in a number of plants, and are present in a high concentration in the French maritime pine bark. The authors summarise results of large-scale experimental and clinical studies on pycnogenol, the standardised extract of French maritime pine bark. Pycnogenol decreases production and effects of free radicals (antioxidant effect). It has antiinflammatory properties, and, by the stimulation of eNOSsynthesis, it increases the production of vasodilatory compounds (e.g. NO, prostacyclin) and decreases that of vascoconstrictor compounds (endothelin-1, thromboxane) materials. These changes lead to vasodilation, which results in increased tissue perfusion and decreased blood pressure. Pycnogenol also decreases platelet aggregation and LDL-cholesterol level and increases HDL-cholesterol level. Its antidiabetic effect has also been shown. Consequently, it may substantially decrease cardiovascular risk. In addition to these results, pycnogenol has been also found to have antibacterial and antiviral effects. It has been successfully used in children with attention deficit hyperactivity disorder, as well as in adults with dysmenorrhea, climacterial disturbances, glaucoma or asthma bronchiale.]