Description
Nebilet was launched in Germany and the Netherlands as an
antihypertensive agent. It is prepared by a five step route starting with 6-fluoro-4-
oxobenzopyran-2-carboxylic acid. It is a selective β
1-adrenergic receptor antagonist
and is 50 times less potent at β
2-receptors. Vasodialating properties occur via the
nitric oxide pathway. While the L-isomer is more potent than the D-isomer, the
racemic mixture is necessary for optimal activity. Upon administration, an immediate
fall in blood pressure occurs, it improves both left ventricular systolic and diastolic
function, and lowers peripheral blood resistance. Nebilet does not influence insulin
sensitivity nor lipid profile comparible to atenolol. Doses of 50 mg of atenolol and 10
mg of Nebilet are equipotent but Nebilet has a longer duration of action due to an
accumulation of the drug and increasing plasma levels of active metabolites.
