Nebivolol !
A β1-selective beta blocker that also promotes nitric oxide release from vessel walls, adding vasodilation. Used for high blood pressure.
Updated 2026-11-01
The figure shows the turkey β1 receptor with cyanopindolol, another beta blocker in the same binding site where nebivolol acts; no structure with nebivolol bound is available.
Mechanism of action
Nebivolol blocks β1 receptors with high selectivity, slowing the heart and lowering renin. It also promotes endothelium-dependent vasodilation through nitric oxide, so resistance falls as well. At higher exposure, or in people who metabolise it slowly by CYP2D6, it loses part of its β1 selectivity.
- Nebivolol selectively blocks β1 receptors
- Heart rate and renin release fall
- Nitric oxide from the endothelium dilates vessels
Pharmacokinetics
- Metabolism
- Liver, mainly by CYP2D6; slow metabolisers have much higher exposure
- Half-life
- About 12 hours for the active form, longer in CYP2D6 poor metabolisers
Indications
- High blood pressure Arterial hypertension →
Adverse effects
Common
- Headache
- Fatigue
- Dizziness
- Bradycardia
Contraindications
- Severe bradycardia or heart block greater than first degree
- Cardiogenic shock or decompensated heart failure
- Sick sinus syndrome without a pacemaker
- Severe liver impairment
Key interactions
- CYP2D6 inhibitors (fluoxetine, paroxetine, quinidine, propafenone)
- Higher nebivolol levels
- Verapamil or diltiazem
- Added bradycardia and AV block
- Clonidine
- Excessive fall in sympathetic activity
What is monitored
- Heart rate and blood pressure
- Signs of heart failure
Administration and safety
- Given by mouth once a day, with or without food
- Withdrawn gradually, never stopped suddenly
- Many «-olol» names look alike: the name is checked on every order
Nursing care
- Check pulse and blood pressure before doses
- Review other drugs for CYP2D6 inhibitors
- Teach the patient not to stop it abruptly and to report wheezing or fainting
Pregnancy and breastfeeding
Human data are limited; beta blockers can slow fetal growth and cause bradycardia and hypoglycaemia in the newborn.
Test yourself
Think of the answer, then tap the question to see it.
What extra vasodilating action does nebivolol have?
It promotes nitric oxide-mediated, endothelium-dependent vasodilation.
Which enzyme metabolises nebivolol, and why does it matter?
CYP2D6: poor metabolisers and patients on CYP2D6 inhibitors reach much higher levels.
Which liver condition is a contraindication to nebivolol?
Severe hepatic impairment.
Related drugs
Related conditions
← Back to the class: Beta blockers
Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.
Sources: DailyMed - NEBIVOLOL tablet (DailyMed (U.S. National Library of Medicine), 2026); ATCDDD - ATC/DDD Index (WHO Collaborating Centre for Drug Statistics Methodology, 2026); Goodman & Gilman's The Pharmacological Basis of Therapeutics, 14th ed., ch. 14 (McGraw Hill, 2023).
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Representative model, for educational purposes only.