Nebivolol

Nebivolol is a highly selective third-generation beta-1 blocker with a unique additional property: it releases nitric oxide (NO) and thereby dilates the blood vessels. This combination of beta blockade and vasodilation makes nebivolol particularly well tolerated.

Nebivolol is used to treat high blood pressure and as an add-on therapy for chronic heart failure. Well-known products include Nebilet® and various generics.

Nebivolol has a dual mechanism of action:

Beta-1 blockade:

• Highest beta-1 selectivity of all beta blockers
• Lowers heart rate and blood pressure
• Reduces the heart's oxygen consumption
• Inhibits renin release

NO release (nitric oxide):

• Activates endothelial NO synthase (eNOS)
• Nitric oxide dilates the blood vessels
• Improves endothelial function
• Lowers peripheral vascular resistance

Metabolism:

• No worsening of glucose metabolism
• No negative effect on blood lipids

Onset of action: Maximum blood pressure reduction after 1-2 weeks of regular use. Stable control after 4 weeks.

Nebivolol is suitable for:

• Adults with high blood pressure
• Chronic stable heart failure (as add-on therapy, aged 70 and over)

Particularly recommended for:

• Patients with erectile dysfunction on other beta blockers
• Metabolic syndrome / diabetes (metabolically neutral)
• Younger patients who value good tolerability

Not suitable:

• History of bronchial asthma or bronchospasm
• Second- or third-degree AV block
• Bradycardia (heart rate below 60/min before starting treatment)
• Decompensated heart failure
• Hepatic insufficiency or impaired liver function
• Cardiogenic shock

High blood pressure:

• Starting dose: 5 mg once daily
• Usual maintenance dose: 5 mg once daily
• Maximum dose: 5 mg daily
• Patients over 65: starting dose 2.5 mg once daily, increase to 5 mg if needed

Heart failure (aged 70 and over):

• Starting dose: 1.25 mg once daily
• Slow increase every 1-2 weeks
• Target dose: 10 mg once daily

In renal insufficiency:

• Starting dose: 2.5 mg once daily
• Maximum dose: 5 mg daily

Available strengths:

• 5 mg tablets (can be split)

How to take:

• Once daily, preferably at the same time of day
• With or without meals
• With enough water
• The tablet can be split

Dose adjustment:

• For high blood pressure: assess the effect after 1-2 weeks
• For heart failure: very slow increase
• Regular pulse and blood pressure checks

Important notes:

• Do not stop abruptly – taper off over at least 1-2 weeks
• Inform the anesthesiologist before surgery
• In people with diabetes, monitor blood sugar

Nebivolol must not be taken in case of:

• Hypersensitivity to nebivolol
• Hepatic insufficiency or impaired liver function
• Acute heart failure or cardiogenic shock
• Second- or third-degree AV block (without a pacemaker)
• Sick sinus syndrome
• Bradycardia (heart rate below 60/min before starting treatment)
• Hypotension (systolic blood pressure below 90 mmHg)
• History of bronchospasm or bronchial asthma
• Untreated pheochromocytoma
• Metabolic acidosis
• Severe peripheral circulatory disorders

Caution with:

• COPD (narrowing of the airways may increase)
• Diabetes mellitus (metabolically neutral, but caution)
• Psoriasis (may be worsened)
• Peripheral circulatory disorders (may be worsened)

Pregnancy: Only if strictly indicated. May cause fetal bradycardia.

Common (1-10%):

• Headache
• Dizziness
• Tiredness
• Gastrointestinal complaints
• Tingling in the extremities
• Constipation, nausea
• Shortness of breath
• Edema

Uncommon (0.1-1%):

• Bradycardia
• Sleep disturbances
• Depressed mood
• Bronchospasm
• Skin rash

Very rare:

• Syncope (fainting)

Contraindicated with:

• Verapamil or diltiazem IV
• Floctafenine
• Sultopride

Caution with:

• Oral verapamil/diltiazem → increased effect on the heart
• Antiarrhythmics (class I) → additive cardiodepressant effect
• Clonidine → when stopping clonidine, taper off the beta blocker first
• Insulin and oral antidiabetics → masking of hypoglycemia
• Anesthetics → increased myocardial depression
• CYP2D6 inhibitors (paroxetine, fluoxetine) → increased nebivolol levels

Note: Nebivolol is mainly metabolized via CYP2D6. In poor metabolizers (approx. 7% of the population), bioavailability is higher.