PHARMACOKINETICS AND PHARMACODYNAMICS OF NEBIVOLOL- A THIRD GENERATION β-BLOCKER

Abstract

Nebivolol is a newer third generation β-blocker, which is highly selective for the β1-adrenoceptor. Nebivolol differs chemically from all other β-blockers with a hydroxypropanolamine substructure in that its cardiac antihypertensive activity resides in the R-enantiomer at the hydroxy group, whereas all other β-blockers have antihypertensive activity in the S-enantiomer and is marketed as d-nebivolol (+SRRR nebivolol) and l-nebivolol (–RSSS nebivolol). The d-enantiomer is responsible for the betablocking properties whereas the l-enantiomer induces a vasodilation via a nitric oxide (NO) mechanism. Nebivolol is a unique agent for the management of patients with hypertension, coronary heart disease or congestive heart failure. This paper reviews the Pharmacokinetics, Pharmacodynamics and additional pharmacologic actions of nebivolol.