[Pharma-clinics medication of the month. Nebivolol (Nobiten)].
Nebivolol (Nobiten, Menarini) is a new beta-blocker recommended for the management of essential hypertension, at a dose of 5 mg once daily. It is administered as a racemic mixture of equal proportions of d- and l-enantiomers. As a lipophilic agent, it is metabolised in the liver and transformed in several active metabolites, essentially via the CYP 2D6, an isoform of cytochrome P450 characterized by a genetic polymorphism. Nebivolol is highly specific for beta-1 adrenergic receptors; it is devoid of intrinsic sympathomimetic or membrane stabilising activity. Interestingly enough, it appears to have nitric oxide-mediated vasodilatory effects which might explain its favourable haemodynamic profile. Several comparative trials demonstrated an antihypertensive activity that was similar or slightly superior to that observed with various other reference antihypertensive agents. Nebivolol has an additive antihypertensive effect in combination with hydrochlorothiazide. All studies reported that the drug has a good clinical and biological tolerance profile. Therefore, nebivolol may be recommended as an alternative first-line treatment option for the management of patients with mild to moderate essential hypertension.
Scheen
A J
AJ
Université de Liège.
D000959:Antihypertensive Agents / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000494:pharmacology*; D001578:Benzopyrans / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000494:pharmacology*; D019389:Cytochrome P-450 CYP2D6 / Q000378:metabolism; D004359:Drug Therapy, Combination; D004983:Ethanolamines / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000494:pharmacology*; D006801:Humans; D006973:Hypertension / Q000188:drug therapy*; D008099:Liver / Q000201:enzymology; D000068577:Nebivolol
D000959:Antihypertensive Agents; D001578:Benzopyrans; D004983:Ethanolamines; D000068577:Nebivolol; D019389:Cytochrome P-450 CYP2D6