LAM Extra for General Practicioners

[CARVEDILOL AND ITS ANTIOXIDANT EFFECT]

KOVÁCS Imre

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.]

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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

[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

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

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]

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Lege Artis Medicinae

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[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.]

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