Nebivolol – a place in the therapy of hypertension in various clinical situations

2021 ◽  
Vol 14 (2) ◽  
pp. 195-200
Author(s):  
Wioletta Wydra ◽  
Marek Kuch
Keyword(s):  
Nitric Oxide ◽  
Cardiovascular Events ◽  
Pleiotropic Effects ◽  
Central Pressure ◽  
Treatment Of Hypertension ◽  
Β Blocker ◽  
Β Blockers ◽  
Long Acting ◽  
Therapy Of Hypertension

Nebivolol is a long-acting, most cardioselective β1-blocker. It stimulates endothelial production of nitric oxide, demonstrating vasodilatory and pleiotropic effects. It has better tolerance compared to classic β-blockers. It lowers the central pressure, reducing the risk of cardiovascular events. It is the preferred β-blocker in the treatment of hypertension in various clinical situations.

scholarly journals β-blockers in hemodialysis: simple questions, complicated answers

2020 ◽  
Author(s):  
Gregory L Hundemer ◽  
Manish M Sood ◽  
Mark Canney
Keyword(s):  
Cardiovascular Events ◽  
Population Based ◽  
Major Adverse Cardiovascular Events ◽  
Maintenance Hemodialysis ◽  
High Risk Population ◽  
Dialysis Patients ◽  
Term Survival ◽  
All Cause Mortality ◽  
Β Blocker ◽  
Β Blockers

Abstract In this issue of the Clinical Kidney Journal, Wu et al. present the results of a nationwide population-based study using Taiwanese administrative data to compare safety and efficacy outcomes with initiation of bisoprolol versus carvedilol among patients receiving maintenance hemodialysis for >90 days. The primary outcomes were all-cause mortality and major adverse cardiovascular events over 2 years of follow-up. The study found that bisoprolol was associated with a lower risk for both major adverse cardiovascular events and all-cause mortality compared with carvedilol. While the bulk of the existing evidence favors a cardioprotective and survival benefit with β-blockers as a medication class among dialysis patients, there is wide heterogeneity among specific β-blockers in regard to pharmacologic properties and dialyzability. While acknowledging the constraints of observational data, these findings may serve to inform clinicians about the preferred β-blocker agent for dialysis patients to help mitigate cardiovascular risk and improve long-term survival for this high-risk population.

scholarly journals The role of nitric oxide in improving endothelial function andcardiovascular health: focus on nebivolol

2011 ◽  
Vol 10 (2) ◽  
pp. 116-121
Author(s):  
G. L. Bakris ◽  
J. N. Basile ◽  
T. D. Giles ◽  
A. A. Taylor
Keyword(s):  
Quality Of Life ◽  
Nitric Oxide ◽  
Antihypertensive Agents ◽  
Clinical Implications ◽  
Cvd Risk ◽  
Patients With Diabetes ◽  
Β Blocker ◽  
Β Blockers

Although β-blockers have been endorsed by guidelines committees for the treatment of patients with hypertension, particularly those with significant CVD and high CVD risk, there are concerns about conventional β-blockers related to poorer clinical outcomes compared with other classes of antihypertensive agents, as well as deleterious effects on quality of life and lipid and carbohydrate metabolism. β-blockers comprise a heterogeneous group of antihypertensive agents, including nonselective agents, cardioselective, nonvasodilating agents, and vasodilating agents that either combine β-nonselectivity with β-blockade or possess cardioselectivity without β-blockade. The pharmacologic, mechanistic, and hemodynamic differences between conventional, nonvasodilating β-blockers and vasodilating β-blockers are discussed in this review, with a focus on the cardioselective vasodilating β-blocker nebivolol. These differences may have important clinical implications, particularly in the treatment of complicated hypertension, such as that associated with patients with diabetes or cardiometabolic syndrome, elderly patients, and African American patients, suggesting that mechanism of action may be an important consideration when choosing a β-blocker.

scholarly journals Beta-blocker could show the prognostic impact in heart failure patients even on the regular hemodialysis

2021 ◽  
Vol 42 (Supplement_1) ◽  
Author(s):  
M Kishihara ◽  
J Kentaro ◽  
T Takuma ◽  
A Takuro ◽  
S Shota ◽  
...  
Keyword(s):  
Heart Failure ◽  
Primary Endpoint ◽  
Cardiovascular Events ◽  
Left Ventricular ◽  
Left Ventricular Ejection ◽  
Prognostic Impact ◽  
Ventricular Ejection Fraction ◽  
Β Blocker ◽  
Β Blockers ◽  
Regular Hemodialysis

Abstract Background β-blockers are recommended as standard medications for patients with heart failure (HF) and reduced left ventricular ejection fraction (LVEF). However, this favorable prognostic effect of β-blockers has not been fully validated in patients receiving regular hemodialysis. Indeed, prior clinical trials have generally excluded such very high-risk population for adverse cardiovascular events. Main reasons for that are the limited number of regular hemodialysis patients in the Western nations, and too high rates of clinical events. Purpose This study aimed to clarify the prognostic benefit of β-blocker in patients on regular hemodialysis who were hospitalized due to HF. Methods This observational study included 1,930 consecutive patients who were hospitalized for worsening of HF and discharged alive from 2013 to 2019. Of them, 151 patients who underwent regular hemodialysis were ultimately analyzed. They were divided into 2 groups depending on the prescription of β-blocker at the discharge; β-blocker group (n=115) and No-β-blocker group (n=36). The primary endpoint of this study was a composite of death from any cause and rehospitalization due to HF. Results During the observation period with 501 days of median follow-up (IQR: 197–954 days), the primary endpoint was occurred in 45 patients (39%) who were receiving β-blockers, while in 24 patients (67%) who were not. Kaplan-Meier analysis showed a significantly lower rate of the primary endpoint in patients in the β-blocker group (Log-rank, p<0.001, Figure). After the adjustment for age, sex, LVEF, systolic blood pressure, heart rate and atrial fibrillation, the administration of β-blocker was still an independent predictor for the primary endpoint in patients who underwent regular hemodialysis (hazard ratio; 0.46, 95% confidence interval; 0.26–0.82). Further analysis each for the population with reduced LVEF (<45%) and preserved LVEF (>45%) showed that the main result of the current study was consistent with that in the reduced LVEF group (Log-rank, p=0.005), but was diminished in the preserved LVEF group (p=0.13). Conclusion The prescription of β-blocker at discharge in HF patients with regular hemodialysis was associated with lower risk of adverse cardiovascular events, mainly in the patients with reduced LVEF. From the findings of our study, we should consider the administration of β-blockers in HF patients, even they are on the regular hemodialysis. FUNDunding Acknowledgement Type of funding sources: None. Figure 1

Effects of an Antihypertensive Combination in Japanese Hypertensive Outpatients Based on the Long-Acting Calcium Channel Blocker Benidipine on Vascular and Renal Events: A Sub-Analysis of the COPE Trial

2020 ◽  
Vol 16 ◽  
Author(s):  
Seiji Umemoto ◽  
Toshio Ogihara ◽  
Masunori Matsuzaki ◽  
Hiromi Rakugi ◽  
Kazuyuki Shimada ◽  
...  
Keyword(s):  
Blood Pressure ◽  
Calcium Channel ◽  
Calcium Channel Blocker ◽  
Channel Blocker ◽  
Rank Test ◽  
Vascular Events ◽  
Treatment Groups ◽  
Β Blocker ◽  
The Difference ◽  
Long Acting

Background: In the trial known as COPE (Combination Therapy of Hypertension to Prevent Cardiovascular Events) three benidipine (a calcium channel blocker; CCB) regimens were compared. Hypertensive Japanese outpatients aged 40–85 years (n=3,293) who did not achieve the target blood pressure of <140/90 mmHg with benidipine 4 mg/day were treated with the diuretic thiazide (n=1,094) or a β-blocker (n=1,089) or an additional angiotensin receptor blocker (ARB; n=1,110). A significantly higher incidence of hard cardiovascular composite endpoints and of fatal or non-fatal strokes was observed in the benidipine-β-blocker group compared to the benidipine-thiazide group. Objective and Methods: We further evaluated the treatment effects of the three benidipine-based regimens on vascular and renal events in a sub-analysis of the COPE patients. Results: A total of 10 vascular events (0.8 per 1,000 person-years) including one aortic dissection (0.1 per 1,000 person-years) and nine cases of peripheral artery disease (0.8 per 1,000 person-years) were documented, as was a total of seven renal events (0.6 per 1,000 person-years). No significant differences in vascular and renal events were revealed among the three treatment groups: vascular events p=0.92 renal events p=0.16 log-rank test. Conclusions: Blood pressure-lowering therapy with benidipine combined with an ARB, β-blocker, or thiazide was similarly effective in the prevention of vascular and renal events in hypertensive outpatients, although there is no enough these events to compare the difference in the three treatment groups.

scholarly journals Lipase Catalyzed Synthesis of Enantiopure Precursors and Derivatives for β-Blockers Practolol, Pindolol and Carteolol

Catalysts ◽  
2021 ◽  
Vol 11 (4) ◽  
pp. 503
Author(s):  
Morten Gundersen ◽  
Guro Austli ◽  
Sigrid Løvland ◽  
Mari Hansen ◽  
Mari Rødseth ◽  
...  
Keyword(s):  
Building Block ◽  
Kinetic Resolution ◽  
Enantiomeric Excess ◽  
Catalytic Amount ◽  
Building Blocks ◽  
Β Blocker ◽  
Β Blockers ◽  
Optical Rotations ◽  
Reported Data ◽  
By Products

Sustainable methods for producing enantiopure drugs have been developed. Chlorohydrins as building blocks for several β-blockers have been synthesized in high enantiomeric purity by chemo-enzymatic methods. The yield of the chlorohydrins increased by the use of catalytic amount of base. The reason for this was found to be the reduced formation of the dimeric by-products compared to the use of higher concentration of the base. An overall reduction of reagents and reaction time was also obtained compared to our previously reported data of similar compounds. The enantiomers of the chlorohydrin building blocks were obtained by kinetic resolution of the racemate in transesterification reactions catalyzed by Candida antarctica Lipase B (CALB). Optical rotations confirmed the absolute configuration of the enantiopure drugs. The β-blocker (S)-practolol ((S)-N-(4-(2-hydroxy-3-(isopropylamino)propoxy)phenyl)acetamide) was synthesized with 96% enantiomeric excess (ee) from the chlorohydrin (R)-N-(4-(3-chloro-2 hydroxypropoxy)phenyl)acetamide, which was produced in 97% ee and with 27% yield. Racemic building block 1-((1H-indol-4-yl)oxy)-3-chloropropan-2-ol for the β-blocker pindolol was produced in 53% yield and (R)-1-((1H-indol-4-yl)oxy)-3-chloropropan-2-ol was produced in 92% ee. The chlorohydrin 7-(3-chloro-2-hydroxypropoxy)-3,4-dihydroquinolin-2(1H)-one, a building block for a derivative of carteolol was produced in 77% yield. (R)-7-(3-Chloro-2-hydroxypropoxy)-3,4-dihydroquinolin-2(1H)-one was obtained in 96% ee. The S-enantiomer of this carteolol derivative was produced in 97% ee in 87% yield. Racemic building block 5-(3-chloro-2-hydroxypropoxy)-3,4-dihydroquinolin-2(1H)-one, building block for the drug carteolol, was also produced in 53% yield, with 96% ee of the R-chlorohydrin (R)-5-(3-chloro-2-hydroxypropoxy)-3,4-dihydroquinolin-2(1H)-one. (S)-Carteolol was produced in 96% ee with low yield, which easily can be improved.

Metabolic responses of the whole body, portal-drained viscera and hindquarter to adrenaline infusion: Effects of nonselective and selective β-adrenoceptor blockade

1997 ◽  
Vol 77 (2) ◽  
pp. 307-316 ◽  
Author(s):  
J. O. O. Miaron ◽  
R. J. Christopherson
Keyword(s):  
Blood Flow ◽  
Oxygen Consumption ◽  
Portal Vein ◽  
Influencing Factor ◽  
External Iliac Artery ◽  
Open Circuit ◽  
Whole Body ◽  
Organ Blood Flow ◽  
Β Blocker ◽  
Β Blockers

Propranolol, a nonselective β-blocker and selective β-blockers (metoprolol a β1-blocker and ICI 118551 a β2-blocker) were used to investigate the β-adrenoceptor-mediated adrenaline-induced increase in whole-body and organ VO2 in five whether sheep. Transit time blood flow probes were chronically implanted on the portal vein and the external iliac artery and sampling catheters were placed in the mesenteric artery, iliac vein and portal vein. Oxygen consumption by the whole body was measured by open circuit calorimetry, and oxygen consumption by the portal-drained viscera and the hindquarter was determined from A-VO2 differences and organ blood flow. Absolute pre-infusion VO2 values for the whole body, portal-drained viscera and hindquarters were 236 ± 7.4, 61 ± 6.0 and 13 ± 3.1 mL min−1 respectively. The mean changes in VO2 in response to infusion were 74 vs. 11, 26, 10 and 12 mL min−1 (SE = 9.1) for whole body; 31 vs. −2, −15, 13 and −4 mL min−1 (SE = 7.3) for portal-drained viscera and 8 vs. −0.4, 2.1, 1.0 and −2.7 mL min−1; SE = 4.3) for hindquarters during adrenaline, control, propranolol, metoprolol and ICI 118551 treatments, respectively. Adrenaline increased VO2 (P < 0.05) in the whole body and portal-drained viscera, but not hindquarters relative to controls. All β-blockers suppressed (P < 0.05) the adrenaline-induced increase in VO2 except for the portal-drained viscera where metoprolol was less effective and the hindquarters where β-blockers had no effect. The blood flow pattern was similar to VO2 responses for the portal-drained viscera. The nonselective β1 and β2 blockers were effective in reducing the adrenaline-induced increases in blood flow from the portal-drained viscera and to the hindquarters, with more pronounced β-adrenoceptor-mediated haemodynamic effects. The results indicate that the β-adrenoceptor system modulates whole body VO2, clearly establishes that adrenaline induces an increased VO2 in portal-drained viscera which can be reversed by a β2 or nonselective β blocker and implicates β adrenoceptors as an influencing factor in the maintenance energy requirements of ruminants. Key words: Calorimetry, adrenaline, β blockers, blood flow, sheep

Cardiac autonomic associations on exercise and ambulatory capacity in individuals with lower-extremity artery disease

2021 ◽  
Vol 28 (Supplement_1) ◽  
Author(s):  
I Roque Marcal ◽  
N Cornelis ◽  
R Buys ◽  
I Fourneau ◽  
EG Ciolac ◽  
...  
Keyword(s):  
Heart Rate ◽  
Autonomic Function ◽  
Cardiopulmonary Exercise Test ◽  
Treadmill Test ◽  
Cardiopulmonary Exercise ◽  
Sympathetic Modulation ◽  
Β Blocker ◽  
Β Blockers ◽  
Artery Disease ◽  
Lower Extremity Artery Disease

Abstract Funding Acknowledgements Type of funding sources: Foundation. Main funding source(s): This work was in part supported by Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP #2019/19596-7), and Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq #303399/2018-0). OnBehalf Exercise and Chronic Disease Research Laboratory - Bauru, Brazil; Research Group for Cardiovascular Rehabilitation - Leuven, Belgium. INTRODUCTION Lower-extremity artery disease (LEAD) characterized by progressive atherosclerotic build-up in leg arteries is becoming increasingly prevalent, affecting more than 200 million people worldwide. In line with other atherosclerotic disorders, LEAD is often associated with autonomic dysfunction as evidenced by a reduced heart rate variability (HRV). To date, little is known on the impact of cardiac autonomic function on exercise and ambulatory capacity. PURPOSE We aimed to investigate whether autonomic function is associated with ambulatory capacity and exercise capacity in patients with LEAD. METHODS Thirty-four patients (age≥17 years) diagnosed with LEAD (ankle brachial index: ABI ≤ 0.9 and/or 20% decrease after a maximal treadmill test) suffering from intermittent claudication (Rutherford I-III) were recruited in the PROSECO-IC trial. Patients were grouped based on beta-blocker medication (β-blocker and non β-blocker). Intervals between R waves (i-RR) obtained by heart rate (HR) signal were acquired beat-to-beat via a digital telemetry system (Polar®️ H10) during 15 min of supine rest and were used for 5-minute HRV analysis. Time domain indexes (mean i-RR, SNDD, pNN50%), and frequency domains (high frequency band (HF), low frequency (LF, very LF (VLF)) and the ratio (LF/HF). HRV was analyzed in absolute (abs), normalized (nu) and log units (log). Ambulatory capacity was assessed by means of a submaximal treadmill test, graded maximal treadmill test using Gardner protocol (GTM) and 6 minutes walking test (6MWT); exercise capacity was assessed by means of a graded maximal cardiopulmonary exercise test (HR, blood pressure (BP) and peak oxygen uptake (VO2peak)) at resting, 2 minutes, and peak of exercise. RESULTS Pearson test showed that sympathetic modulation indexes were moderate associated with pain free distance in GTM (LF/HF: r = 0.52, p = 0.04), and pain free time in 6MWT (LFlog: r=-0.62, p = 0.01; VLF: r=-0.52, p = 0.04), respectively, in patients without β-blocker. Similar HR associations with HRV (time and frequency domain) were observed during submaximal treadmill test and cardiopulmonary exercise test (p ≤ 0.05). Test-t demonstrated a significantly increased response intra-groups in HR and BP during both tests (p ≤ 0.05). Average BP were positive associated with the earlier stages of the cardiopulmonary test (resting to 2 min) with LFlog (r = 0.70, p= &lt;0.001) in β-blocker while non-β-blocker were associated from 2 min to peak with LFabs (r = 0.67, p= &lt;0.001) and LF/HF (r = 0.52, p = 0.03).  CONCLUSION Sympathetic modulation was correlated with a longer pain free walking capacity in non-β-blockers. Yet, individuals treated by -β-blockers showed an earlier sympathetic modulation through exercise pressor response during the first stages of cardiopulmonary exercise compared to non-β-blockers with LEAD.

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