Products
Nebivolol is commercially available in tablet form as a monopreparation (Nebilet, generic, USA: Bystolic) and in combination with hydrochlorothiazide (Nebilet plus). The active ingredient has been approved in many countries since 1998. A fixed combination with valsartan is also available in some countries (Byvalson).
Structure and properties
Nebivolol (C22H25F2NO4, Mr = 405.4 g/mol) has four chiral centers and consists of two isomers, D- and L-nebivolol. Both agents are involved in the effects (see below). In drugs, it is present as nebivolol hydrochloride, a white powder soluble in methanol.
Effects
Nebivolol (ATC C07AB12) has antihypertensive and mild vasodilatory properties and reduces heart rate. The effects are due, on the one hand, to selective and competitive antagonism at beta-1 receptors (D isomer). On the other hand, the vasodilatation is the result of a release of nitric oxide (NO) from endothelial cells (L-isomer). It is not due to antagonism at alpha receptors as is the case with carvedilol.
Indications
For the treatment of hypertension and stable and chronic heart failure.
Dosage
According to the SmPC. The drug is taken once a day regardless of meals and preferably at the same time of day. The maximum effect is delayed within 1-4 weeks.
Contraindications
- Hypersensitivity
Full details of precautions and interactions can be found in the drug label.
Interactions
There are potentially numerous drug-drug interactions. Nebivolol is metabolized by CYP2D6.
Adverse effects
The most common potential adverse effects include reduced heart rate, low blood pressure, dizziness, difficulty breathing, headache, paresthesias, fatigue, oedema, constipation, nausea, and diarrhea.
