Evidence for a vasoconstriction-mediating receptor for UTP, distinct from the P2 purinoceptor, in rabbit ear artery.
Self-identified Hispanics with stage I-II hypertension were randomized to receive a double-blind treatment: placebo (n = 136) or nebivolol (n = 141, starting dose 5 mg/day) for 8 weeks. Nebivolol dosage could be uptitrated at 2-week intervals to 10, 20, or 40 mg/day, as needed to achieve diastolic blood pressure (DBP) control (JNC7 criteria). Efficacy outcome measures were the mean changes from baseline to the end of week 8 in trough-seated DBP (primary) and systolic blood pressure (SBP) (secondary). Safety and tolerability were also assessed.
A MEDLINE literature search (1966-May 2013) was performed using the following key terms: hypertension, β-blockers, atenolol, carvedilol, metoprolol tartrate, metoprolol succinate, nebivolol, pharmacology, pharmacodynamics, pharmacokinetics, blood pressure, metabolic, lipid, central aortic pressure, diabetes, and insulin resistance. References from publications reviewed were included.
The clinical and demographic characteristics were similar in the two groups at baseline. Individualized propranolol dose adjustment ensured a similar degree of beta-blockade, as assessed by resting heart rate and chronotropic reserve. The mean propranolol dose used was 109 +/- 43 mg/day. Only one patient presented with intolerance to propranolol, thus carvedilol was reintroduced. One death was recorded in group propranolol. Ejection fraction significantly increased in the propranolol group. No significant change was observed in the other cardiovascular variables after betablocker replacement.
Erectile dysfunction, which is common in men with hypertension, has been reported as a common adverse effect of many antihypertensive drug classes, including beta-blockers and diuretics. Atenolol and nebivolol are both beta(1)-selective blockers, but nebivolol is a new-generation compound with nitric oxide-mediated vasodilating activity. The aim of the study was to compare the effects of nebivolol and atenolol +/- chlorthalidone on the sexual function of hypertensive men.
Rats were divided into four groups: sham operated (sham-control), MI-induced (MI-control), immediate nebivolol loaded (MI-neb1), orally nebivolol treated (MI-neb2). MI was induced by the ligation of the LAD. Loading dose of nebivolol (0.1 mg/kg) was administrated i.v. during reperfusion and continuation dose was administrated orally (2 mg/kg) by gastric gavages once daily. NOS related mechanisms were assessed either in acute (2nd day) and sub-acute (28th day) period of MI by histologic, hemodynamic and biologic studies.
Nebivolol is a safe and well-tolerated drug that improves NYHA class, systolic and diastolic LV function in NIDC patients, although it is associated with a lower maximal exercise duration at 3 months.
There is limited information about the effects of beta-blockers in heart failure (HF) stratified by blood pressure, especially in the elderly and those with preserved EF. We evaluate the effects of nebivolol on outcomes in elderly patients with HF stratified by baseline systolic blood pressure (SBP) and EF.
A total of 54 patients with postinfarction left ventricular dysfunction and chronic cardiac failure of NYHA functional class II-III were divided into two groups: group 1 (n=24) comprised patients with effort angina FC II-III and impaired glucose tolerance, group 2 (n=30) consisted of anginal patients associated with type 2 diabetes mellitus (DM). Clinical, laboratory and functional indices were registered before therapy with nebivolol and 6 months after it. Immunological control included determination of the subpopulation composition of lymphocytes, immunoglobulins, circulating immune complexes (CIC), antibodies to cardiolipin (CL), proinflammatory cytokines: IL-1alpha, IL-2, IL-6, IL-8, alpha-interferon, tumor necrosis factor alpha (TNFalpha).
Nebivolol showed antiepileptic effects in addition to its reported antihypertensive effect, which could be attributed to action of the two drugs through different mechanisms or due to drug interaction that may be pharmacodynamic or pharmacokinetic needing elucidation.
In a model of acute and normotensive glomerular fibrosis, beta-adrenergic antagonism does not reduce TGF-beta overexpression, suggesting that its pressure-independent antifibrotic action may be limited to chronic renal diseases. The beneficial effect of angiotensin II inhibition even on acute matrix expansion may be a relevant mechanism as to the explanation of its superiority in treating fibrotic renal diseases.
We found that nebivolol reduced the expression of proinflammatory genes in endothelial cells and vascular smooth muscle cells in vitro whereas metoprolol did not. In vivo, nebivolol inhibited neointima formation by reducing SMC proliferation and macrophage accumulation.
Six-week antihypertensive treatment resulted in a DBP reduction of 13.7 mm Hg. The rate of responders, defined as those patients achieving DBP <90 mm Hg, was 70%. SBP was reduced by 26.1 mm Hg. According to the Framingham Risk Model, 313 deaths would be avoided. Coronary heart disease (CHD) could be reduced by 94 cases (from 1339 to 1245 events) and 150 strokes would be avoided (from 518 to 368 events) in a 10-year period. This reduction of 244 cardiovascular events among the 8682 patients investigated corresponded to cost savings of between Euro 250,000 and Euro 2.5 million, depending on the healthcare environment and the intervention applied.