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Nebivolol is a β-adrenergic receptor blocking agent. Nebivolol is a racemate of two enantiomers, d-Nebivolol and l-Nebivolol. Nebivolol has unique pharmacologic properties, including very high selectivity for β-1 receptor and nitric oxide-mediated vasodilatory effect. Mechanism of action may be involved with:
- Decreased heart rate
- Decreased myocardial contractility
- Diminution of tonic sympathetic outflow to the periphery from cerebral vasomotor centers
- Suppression of renin activity and
- Vasodilation and decreased peripheral vascular resistance.
- Absorption: Absorption of Nebivolol is similar to an oral solution. The absolute bioavailability has not been determined. Mean peak plasma nebivolol concentrations occur approximately 1.5 to 4 hours. Food does not alter the pharmacokinetics of nebivolol.
- Distribution: The in vitro human plasma protein binding of nebivolol is approximately 98%, mostly to albumin.
- Metabolism: Nebivolol is predominantly metabolized via direct glucoronidation of parent and to a lesser extent via N-dealkylation and oxidation via cytochrome P450 2D6. Its stereospecific metabolites contribute to the pharmacologic activity.
- Elmination: After a single oral administration of 14C-nebivolol, 38% of the dose was recovered in urine and 44% in feces for extensive metaboliser and 67% in urine and 13% in feces for poor metabolizer. Essentially all Nebivolol was excreted as multiple oxidative metabolites or their corresponding glucuronide conjugates.