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This study was designed as prospective single-arm controlled study. We prospectively studied 35 Behçet's patients who were diagnosed according to the International Study Group criteria. Patients received 5 mg nebivolol per day for 3 months. Endothelial dysfunction was evaluated by brachial artery flow-mediated dilatation (FMD) method using high-resolution vascular ultrasound device at baseline and after for 3-month therapy. The paired samples t test, Wilcoxon test, Pearson, Spearman correlation analyses were used for statistical analysis.
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The effect of pretreatment with selective beta 1-adrenoceptor blockers (dl-nebivolol or atenolol) on myocardial mechanical activity, mitochondrial function, morphology, and calcium cytochemistry was studied during normothermic ischemic arrest and reperfusion of isolated working rabbit hearts. The hearts subjected to 25 min of ischemia followed by 30 min of post-ischemic reperfusion showed typical signs of severe myocardial ischemic damage. The ultrastructural changes showed a good relation with the changes in mechanical activity and mitochondrial function. To determine whether these changes could be prevented or reduced by beta 1-adrenoceptor blockade, dl-nebivolol or atenolol (0.62 mg/liter) was added to the perfusate 30 min before the induction of ischemia. The results showed that dl-nebivolol exerted a protective effect on recovery of mechanical activity, on mitochondrial function during reperfusion as well as on the ultrastructure as examined at the end of the reperfusion period. On the other hand, atenolol failed to protect the myocardium against ischemia-reperfusion damage in the isolated working rabbit heart.
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Twenty-four-hour ambulatory blood pressure (ABP) monitoring was used as a measure of drug efficacy and criterion for inclusion of 29 patients with primary hypertension in a double-blind crossover comparison of the novel cardioselective beta-blocker nebivolol (2.5--10 mg) with lisinopril (10--40 mg) once daily. After 8 weeks of therapy, both regimens reduced clinic BP to a similar and significant extent. Similar and significant reductions in systolic and diastolic ABP in every one of the 24-h periods were observed with both treatments. Moreover, the percentages of "BP loads" were lowered similarly from 64% to 31% and 30% with nebivolol and lisinopril, respectively. Furthermore, a comparable trough:peak ratio of 70% was obtained with both therapies. These data demonstrate that both once daily nebivolol and lisinopril given as monotherapies in patients with ambulatory hypertension provide adequate and similar clinic and ambulatory BP control. In addition, our findings indicate that ABP monitoring may improve the clinical evaluation of new antihypertensive agents.
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Chronic salt administration increased systolic blood pressure by 38 +/- 5 mmHg in salt-treated rats as compared with that in control rats. Both nebivolol and atenolol prevented a salt-induced increase in pressure. cNOS activity was significantly decreased by a high-salt diet. The impairment of endothelium-dependent relaxations in response to acetylcholine in salt-treated rats was prevented only by nebivolol, in both large and small arteries. In contrast, the reduced endothelium-independent relaxations and contractions in response to sodium nitroprusside and endothelin-1, respectively, were restored by both drugs. Nebivolol, but not atenolol, restored cNOS activity.
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Therefore, we performed a randomized, double-blind, placebo-controlled, cross-over trial in 16 healthy males. Subjects received 10 mg bisoprolol, 50 mg carvedilol, 10 mg nebivolol and placebo on the first morning followed by 5 mg bisoprolol once daily, 25 mg carvedilol twice daily, 5 mg nebivolol once daily and placebo for 1 week. Heart rate and blood pressure were measured at rest and exercise 3 and 24 h following intake of the first dose, and immediately before and 3 hours following intake of the last dose of each drug. In addition, effects of the drugs on nocturnal melatonin release were determined, and quality of life (QOL) was evaluated.
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A total of 152 UK general practices.
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In rats with relatively mild chronic heart failure (CHF) there was an increase in plasma LDL levels. In turn, in severe CHF it was revealed a significant decrease in total cholesterol concentration due to LDL levels decline. ACE inhibitors (captopril, enalapril and lisinopril) and the most selective beta1-adrenoblockers (metoprolol, nebivolol) had not any significant influence on plasma lipids. Less selective and especially nonselective beta-adrenoblockers pindolol and propranolol brought up the atherogenic potential of plasma because of HDL levels reduction in mild CHF whereas in case of severe model--due to the trends toward decrease in HDL concentration and toward increase in LDL levels. Lipophilic ACE-inhibitors and beta-adrenoblockers without intrinsic sympathomimetic activity improved survival in rats with mild CHF to the equal extent. On the contrary in severe CHF beta-adrenoblockers, especially non-selective, had an advantage over ACE inhibitors on the survival effect.
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Nebivolol is a highly cardioselective long-acting beta-blocker with vasodilating properties, which acts in part via the endothelial L-arginine/nitric oxide pathway. As an antihypertensive drug it is effective in once-daily dosage. Nebivolol has previously been shown to improve left ventricular function in patients with cardiac impairment.
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In elderly patients with mild hypertension, a depressor trend of pulse pressure while standing can be turned into a significant pressor response by treatment with a beta-blocker.