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Author: Admin | 2025-04-28
The pharmacokinetics of nebivolol. Under fed conditions, nebivolol glucuronides are slightly reduced. Nebivolol tablets may be administeredwithout regard to meals.DistributionThe in vitro human plasma protein binding of nebivolol is approximately 98%, mostly to albumin, and is independent of nebivolol concentrations.MetabolismNebivolol is predominantly metabolized via direct glucuronidation of parent and to a lesser extent via N-dealkylation and oxidation via cytochrome P450 2D6. Itsstereospecific metabolites contribute to the pharmacologic activity [see DRUG INTERACTIONS].EliminationAfter a single oral administration of 14C-nebivolol, 38% of the dose was recovered in urine and 44% in feces for EMs and 67% in urine and 13% in feces for PMs.Essentially all nebivolol was excreted as multiple oxidative metabolites or their corresponding glucuronide conjugates.Pharmacokinetics In Special PopulationsHepatic Diseased-Nebivolol peak plasma concentration increased 3-fold, exposure (AUC) increased 10-fold, and the apparent clearance decreased by 86% in patients with moderatehepatic impairment (Child-Pugh Class B). No formal studies have been performed in patients with severe hepatic impairment and nebivolol should be contraindicatedfor these patients [see DOSAGE AND ADMINISTRATION].Renal DiseaseThe apparent clearance of nebivolol was unchanged following a single 5 mg dose of nebivolol tablets in patients with mild renal impairment (ClCr 50 to 80 mL/min,n=7), and it was reduced negligibly in patients with moderate (ClCr 30 to 50 mL/min, n=9), but clearance was reduced by 53% in patients with severe renal impairment(ClCr DOSAGE AND ADMINISTRATION].Drug-Drug InteractionsDrugs that inhibit CYP2D6 can be expected to increase plasma levels of nebivolol. When nebivolol tablet is co-administered with an inhibitor or an inducer of thisenzyme, monitor patients
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