Pharmacological and Hemodynamic Profile of Nebivolol,* a Chemically Novel, Potent, and Selective β1-Adrenergic Antagonist

Water, A. Van De; Janssens, W. J.; Neuten, J. Van; Xhonneux, R.; Cree, J. De; Verhaegen, H.; Reneman, Robert S.; Janßen, Paul

doi:10.1097/00005344-198805000-00007

Cited by 195 publications

(138 citation statements)

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“…[6][7][8] Consequently, currently available b-blockers represent a highly heterogeneous class, differentiated by their pharmacologic effects on b 1 -specificity, peripheral vascular resistance, cardiac output, metabolic profile and overall tolerability. [6][7][8] Nebivolol is a selective b 1 -adrenoreceptor blocker 9 that possesses vasodilatory properties. [10][11][12][13] Nebivolol possesses a distinct hemodynamic profile, including reduced peripheral vascular resistance and neutral impact on cardiac output.…”

Section: Introductionmentioning

confidence: 99%

Adding nebivolol to ongoing antihypertensive therapy improves blood pressure and response rates in patients with uncontrolled stage I–II hypertension

2009

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This study assessed blood pressure (BP) reductions and response rates following addition of nebivolol to ongoing antihypertensive therapy in patients with uncontrolled stage I-II hypertension despite antihypertensive treatment. Patients with an average sitting diastolic BP (SiDBP) X90 and p109 mm Hg while taking an antihypertensive regimen were included in this double-blind, placebo-controlled, parallel-group study. The primary efficacy end point was reduction from baseline to week 12 in mean trough SiDBP. In total, 669 patients were randomized to once-daily nebivolol 5, 10 or 20 mg or placebo. Addition of nebivolol 5, 10 and 20 mg significantly reduced BP; placebo-subtracted least squares mean reductions in trough SiDBP were À3.3, À3.5 and À4.6 mm Hg, respectively (Po0.001) and À5.7, À3.7 and À6.2 mm Hg in trough sitting systolic BP (SiSBP), respectively (Pp0.015). Adding nebivolol 5-20 mg resulted in significantly more responders (SiDBP o90 or X10 mm Hg reduction; range: 53.0-65.1 vs 41.3% with placebo; Pp0.028) and significantly better control rates (SiSBP/ SiDBP o140/90 mm Hg; range: 41.3-52.7 vs 29.3% with placebo; Pp0.029). Nebivolol was well tolerated; the incidence of adverse events with nebivolol was similar to that with placebo (40.2 vs 38.9%, respectively; P ¼ 0.763). Addition of once-daily nebivolol to ongoing antihypertensive therapy provided significant additional BP reductions and better response rates in patients with uncontrolled hypertension and was well tolerated.

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Section: Introductionmentioning

confidence: 99%

Adding nebivolol to ongoing antihypertensive therapy improves blood pressure and response rates in patients with uncontrolled stage I–II hypertension

2009

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“…Exclusion metic activity. 1,2 It has been shown to control blood criteria are listed in Table 1. pressure (BP) over 24 h with dosage once daily.…”

Section: Introductionmentioning

confidence: 99%

A dose-response trial of nebivolol in essential hypertension

et al. 1997

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A double-blind placebo-controlled dose-response trial clear inferiority of efficacy in black patients. A single of nebivolol, a cardioselective beta-blocking drug which daily dose of 5 mg was appropriate, with no evident also induces endothelium-dependent dilatation via nitric advantage at 10 mg. The drug was well tolerated, even oxide, has been performed. Nebivolol reduced blood at 10 mg daily. BP control was achieved largely in the pressure (BP) in a dose dependent way, and was shown absence of typical side effects of beta-blockade. The to be effective given once daily, without appreciable difcombination of properties of nebivolol renders it an ferences between peak and trough drug levels. There attractive addition to the antihypertensive repertoire. was no postural component to the BP fall. There was no

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“…23,24 It lowers blood pressure by reducing peripheral vascular resistance, and significantly increases stroke volume with preservation of cardiac output. [16][17][18] The net hemodynamic effect of nebivolol is the result of a balance between the depressant effects of beta blockade and an action that maintains cardiac output. It is thought that the anti-oxidative and nitric oxide-mediated mechanisms of action observed in nebivolol may be beneficial in reducing the progression of insulin resistance, diabetes mellitus and cardiovascular diseases.…”

Section: Discussionmentioning

confidence: 99%

“…Nebivolol is a highly cardioselective vasodilatory beta 1 receptor blocker that lowers blood pressure (BP) by reducing peripheral vascular resistance, and significantly increases stroke volume with preservation of cardiac output when compared with atenolol, another beta 1 receptor blocker. [16][17][18] Methods Subjects Obese African-American men and women between the ages of 18 and 75 years (mean age 50 years) with recently diagnosed Stage 1 hypertension were enrolled in the study. Obesity was defined as body mass index 430.…”

Section: Introductionmentioning

confidence: 99%

Effects of nebivolol in obese African Americans with hypertension (NOAAH): markers of inflammation and obesity in response to exercise-induced stress

Merchant

Rahman²,

Ferdinand

et al. 2010

J Hum Hypertens

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We sought to determine whether the antihypertensive drug nebivolol has beneficial effects on vascular markers of inflammation and oxidation in obese African-American patients with hypertension when exposed to exercise-induced stress. Forty-three obese, AfricanAmerican subjects with hypertension were treated with nebivolol (5-10 mg/day) for 8 weeks. Before treatment the subjects underwent an exercise treadmill study to a level of eight metabolic equivalents. Circulating levels of soluble interleukin-6 (sIL-6), vascular cell adhesion molecule (VCAM-1), adiponectin and leptin were measured at pre-treadmill, and 1 min, 30 min, 60 min and 24 h after treadmill. After the 8-week treatment period, exercise treadmill study and the measurement of markers were repeated. Treatment with nebivolol reduced levels of sVCAM-1 at pre-exercise by 21% and at 1 and 30 min by 12.5 and 20%, respectively (Po0.005 from corresponding time point). In nebivolol-treated patients there was a reduction in sIL-6 levels by 20% and preexercise and at 1 and 60 min by 19.7 and 33.5%, respectively (Po0.005 from corresponding time point). Treatment with nebivolol increased levels of serum adiponectin by 28% (P ¼ 0.012) and decreased levels of leptin by 32% (Po0.005 from pre-treatment). Treatment with nebivolol improves markers of inflammation and obesity in a high-risk African-American population. Moreover, this effect is potentiated in response to exercise-induced stress. These results suggest that nebivolol differentially regulates markers of inflammation and obesity, thereby providing vascular protection.

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Pharmacological and Hemodynamic Profile of Nebivolol,* a Chemically Novel, Potent, and Selective β1-Adrenergic Antagonist

Cited by 195 publications

References 0 publications

Adding nebivolol to ongoing antihypertensive therapy improves blood pressure and response rates in patients with uncontrolled stage I–II hypertension

Adding nebivolol to ongoing antihypertensive therapy improves blood pressure and response rates in patients with uncontrolled stage I–II hypertension

A dose-response trial of nebivolol in essential hypertension

Effects of nebivolol in obese African Americans with hypertension (NOAAH): markers of inflammation and obesity in response to exercise-induced stress

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