Nebivolol a Novel Somewhat Different Βeta Adrenergic Receptor Blocker

Kumar, Dharmendra; Loc, Bhulan Prasad

doi:10.22270/jddt.v3i6.695

Cited by 2 publications

(2 citation statements)

References 62 publications

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“…However, some important aspects regarding the pharmacodynamic effects of nebivolol have to be acknowledged if a conclusive decision regarding the absence or presence of any clinical consequences associated with this drug combination is to be made. For example, nebivolol has a maximal antihypertensive effect after 2 to 8 weeks of therapy (42). As for the heart rate, pronounced reductions were also evident only after weeks of continued therapy with this beta-blocker (43).…”

Section: Discussionmentioning

confidence: 99%

Investigation of a Potential Pharmacokinetic Interaction Between Nebivolol and Fluvoxamine in Healthy Volunteers

et al. 2017

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-PURPOSE:To investigate whether fluvoxamine coadministration can influence the pharmacokinetic properties of nebivolol and its active hydroxylated metabolite (4-OH-nebivolol) and to assess the consequences of this potential pharmacokinetic interaction upon nebivolol pharmacodynamics. METHODS:This open-label, non-randomized, sequential clinical trial consisted of two periods: Period 1 (Reference), during which each volunteer received a single dose of 5 mg nebivolol and Period 2 (Test), when a combination of 5 mg nebivolol and 100 mg fluvoxamine was given to all subjects, after a 6-days pretreatment regimen with fluvoxamine (50-100 mg/day). Non-compartmental analysis was used to determine the pharmacokinetic parameters of nebivolol and its active metabolite. The pharmacodynamic parameters (blood pressure and heart rate) were assessed at rest after each nebivolol intake, during both study periods. RESULTS: Fluvoxamine pretreatment increased C max and AUC 0-∞ of nebivolol (C max : 1.67 ± 0.690 vs 2.20 ± 0.970 ng/mL; AUC 0-∞ : 12.1 ± 11.0 vs 19.3 ± 19.5 ng*h/mL ) and of its active metabolite (C max : 0.680 ± 0.220 vs 0.960 ± 0.290 ng/mL; AUC 0-∞ : 17.6 ±20.1 vs 25.5 ± 29.9 ng*h/mL). Apart from C max , AUC 0-t and AUC 0-∞ , the other pharmacokinetic parameters (t max , k el and t ½ ) were not significantly different between study periods. As for the pharmacodynamic analysis, decreases in blood pressure and heart rate after nebivolol administration were similar with and without fluvoxamine concomitant intake. CONCLUSIONS: Due to enzymatic inhibition, fluvoxamine increases the exposure to nebivolol and its active hydroxylated metabolite in healthy volunteers. This did not influence the blood pressure and heart-rate lowering effects of the beta-blocker administered as single-dose. However, more detail studies involving actual patients are required to further investigate the clinical relevance of this drug interaction.

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Section: Discussionmentioning

confidence: 99%

Investigation of a Potential Pharmacokinetic Interaction Between Nebivolol and Fluvoxamine in Healthy Volunteers

et al. 2017

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“…As a newer beta blocker, nebivolol has improved tolerability without any loss of efficacy compared with older beta blockers [38][39][40][41] . Patients using nebivolol compared with patients using other beta blockers are reported to have a lower incidence of side effects, such as fatigue, depression, bradycardia and impotence 42 . Such benefits may help patients achieve better persistence with nebivolol 27 .…”

Section: Discussionmentioning

confidence: 99%