Lege Artis Medicinae

[Carvedilol and its antioxidant effect]

KOVÁCS Imre

OCTOBER 20, 2010

Lege Artis Medicinae - 2010;20(10)

[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.]

COMMENTS

0 comments

Further articles in this publication

Lege Artis Medicinae

[Disorders of despair]

BÁNFALVI Attila

Lege Artis Medicinae

[Connection between fetal development and adult diseases - Long acting effects of stress affecting the mother and the fetus]

MOLNÁR Ildikó

[The stress responses affecting the mother and the fetus have a life-long consequence in the manifestation of adult metabolic disorders. The perinatal stress inducing fetal adaptation contributes to alterations in tissue structures and hormone regulations as well as could lead to intrauterine growth retardation. The newborns with low birth weight are associated with the glucocorticoid, adrenaline and insulin resistance making them postnatal susceptible to obesity, diabetes type 2 and hypertonia. The number of newborns with low birth weight increase, therefore the prevention of adult diseases originating from perinatal misprogramming represents a frequent challenge for health services and society.]

Lege Artis Medicinae

[Successful localization of an insulinoma with angiography]

BAKÓ Barnabás, LÁZÁR István, TARKÓ Erzsébet, OROSZ Péter

Lege Artis Medicinae

[A new DPP-IV inhibitor: saxagliptin]

KIS János Tibor, MÉSZÁROS Gabriella

[Saxagliptin is a selective, potent inhibitor of dipeptidyl peptidase-IV (DPP-IV). By inhibiting DPP-IV, saxagliptin reduces the degradation of endogenous incretin hormones, resulting in increased glucose-dependent insulin and decreased glucagon secretion from the pancreas islets. Clinical trials of saxagliptin as monotherapy and as combination therapy with other oral antidiabetic medications including metformin, glibenclamide, glipizide, pioglitazone and rosiglitazone have demonstrated clinical benefits in different glycaemic endpoints. Due to its glucose- dependent mechanism of action, saxagliptin as monotherapy or in combination with metformin results in a very low risk for hypoglycemia. It has also been shown to be generally well-tolerated, with not having any relevant effect on weight. The authors summarize the most important saxagliptin trials.]

Lege Artis Medicinae

[International trials of immunogenicity of H1N1 vaccines]

CSÁSZÁR Albert

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]

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

[Experience with coenzyme Q10 in heart failure]

KOHUT László

[INTRODUCTION - The protein complex coenzyme Q10 (CoQ10) has a role in ATP production as a mitochondrial electron transport molecule, and it also has a strong antioxidant effect. Several studies have proved the correlation between the decrease in CoQ10 level and the severity of heart failure. Heart failure is a multifactorial syndrome, the development of which is greatly influenced by an abnormal energy metabolism. CASE REPORT - The 61-year-old woman developed heart failure after a myocardial infarction. She complained of fatigue, dyspnoea and reduced physical endurance even with optimal treatment. When her therapy was completed by CoQ10, her endurance and life quality significantly improved and her symptoms ameliorated. CONCLUSIONS - Medical treatment of chronic heart failure is an evidence-based, complex therapy. Despite the complex management, morbidity and mortality of this condition remain high. A number of studies have shown that CoQ10 substitution can improve the clinical and haemodynamical parameters of patients with heart failure. On the basis of these results, the use of CoQ10 as an adjuvant therapy to complex treatment has an increasing role.]

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.]