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PHARMACOLOGY: Pharmacodynamics: Nebivolol is a cardioselective beta blocker. It has vasodilating activity, which appears to be due to a direct action on the endothelium, possibly involving nitric oxide release.
It is reported to lack intrinsic sympathomimetic and membrane-stabilising activity.
Pharmacokinetics: Nebivolol is rapidly absorbed after oral doses. It is extensively metabolised in the liver by alicyclic and aromatic hydroxylation, N-dealkylation, and glucuronidation; the hydroxy metabolites are reported to be active. The rate of aromatic hydroxylation by cytochrome P450 isoenzyme CYP2D6 is subject to genetic polymorphism, and bioavailability and half-life vary widely. In fast metabolisers the elimination half-life of nebivolol is about 10 hours and that of the hydroxy metabolites is about 24 hours. Peak plasma concentrations of unchanged drug plus active metabolites are 1.3 to 1.4 times higher in slow metabolisers and the half-lives of nebivolol and its hydroxy metabolites are prolonged.
Nebivolol is about 98% bound to plasma proteins. It has high lipid solubility. It is excreted in the urine and faeces, almost entirely as metabolites. Nebivolol is distributed into breast milk in animals.
