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Clinical Pharmacokinetics of Nebivolol

A Review

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Nebivolol is the racemic mixture of 2 isomers with 4 asymmetric centres. The d-isomer has the SRRR configuration, and the l-isomer is RSSS. Animal and human pharmacological experiments demonstrated that the antihypertensive and haemodynamic action of the racemic mixture was superior to that of the isomers alone. Many aspects affect the pharmacokinetics of the parent drug without making a firm impact on the clinical outcome. The absolute oral bioavailability of nebivolol varies from 12 to 96% in subjects characterised as extensive and poor debrisoquine hydroxylators. It is likely that active hydroxymetabolites compensate for the difference in both phenotype subjects. Active drug concentrations reflecting β-blockade by d-nebivolol and its hydroxymetabolites can be determined by a radioimmunoassay procedure using enantioselective antibodies. By the use of this method, comparable active drug concentrations were found in extensive and poor metabolisers, which explains why the clinical outcome is the same for both groups.

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Van Peer, A., Snoeck, E., Woestenborghs, R. et al. Clinical Pharmacokinetics of Nebivolol. Drug Invest 3 (Suppl 1), 25–30 (1991).

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