Nebivolol: a review of its clinical and pharmacological characteristics.

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Gielen W, Cleophas TJ, Agrawal R

Nebivolol: a review of its clinical and pharmacological characteristics.

Int J Clin Pharmacol Ther. 2006 Aug;44(8):344-57.

PubMed ID

16961165 [ View in PubMed

]

Abstract

Nebivolol is a cardioselective lipophilic beta-blocker devoid of intrinsic sympathomimetic and membrane-stabilizing actions. The pharmacological profile differs from that of conventional cardioselective beta3-blockers in that it displays nitric oxide- (NO) mediated vasodilator activity. The net hemodynamic effect of nebivolol is the result of a balance between the depressant effects of beta3-blockade and an action that tends to maintain cardiac output, presumably connected with its afterload reducing vasodilator effect. Recent studies suggest that nebivolol may also restore endothelial dysfunction. Long-term follow-up studies indicate that the compound is efficacious and safe both in patients with mild hypertension and those with stable angina. An interesting effect of chronic nebivolol therapy in elderly patients with mild hypertension is the reversal of a depressor effect into a pressor effect on standing. This action indicates that nebivolol has advantages over other antihypertensive drugs and that it may protect elderly hypertensive patients from orthostatic complaints. The observation that nebivolol improves exercise capacity in non-claudicant hypertensives is also of clinical interest. Nebivolol resembles serotonin reuptake inhibitors in that it is metabolized by CYP450 2D6 and, therefore, concomitant treatment with serotonin uptake inhibitors may lead to overdosing. Nebivolol compared to placebo does not significantly reduce the mortality risk in elderly subjects. The effects of biological age and comorbidities may be responsible for this finding. In conclusion, clinical studies suggest that nebivolol is effective and safe in patients with hypertension, angina pectoris and heart failure. The beneficial effects on endothelial function, autonomic control and exercise capacity are of considerable clinical interest.

DrugBank Data that Cites this Article

Drugs

Nebivolol

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Nebivolol	Beta-1 adrenergic receptor	Protein	Humans	Yes	Antagonist	Details
Nebivolol	Beta-3 adrenergic receptor	Protein	Humans	Unknown	Agonist	Details

Drug Enzymes

Drug	Enzyme	Kind	Organism	Pharmacological Action	Actions
Nebivolol	Cytochrome P450 2D6	Protein	Humans	Unknown	Substrate	Details