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Nebivolol: Uses, Dosage & Side Effects
Nebivolol is a selective beta-blocker used to treat high blood pressure and chronic heart failure. It lowers blood pressure and reduces the workload on the heart.
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Nebivolol is a selective beta-blocker used to treat high blood pressure and chronic heart failure. It lowers blood pressure and reduces the workload on the heart.
What is Nebivolol?
Nebivolol is a prescription medication belonging to the class of selective beta-1 adrenoceptor blockers (commonly known as beta-blockers). It is primarily used to treat arterial hypertension (high blood pressure) and chronic heart failure. Nebivolol is distinguished from older beta-blockers by its high selectivity for the beta-1 receptor and its additional vasodilatory effect, which is mediated through the release of nitric oxide (NO).
Indications
Nebivolol is indicated for:
- Arterial hypertension (high blood pressure)
- Stable chronic heart failure in elderly patients (aged 70 and above)
- Supportive treatment in coronary artery disease and certain cardiac arrhythmias
Mechanism of Action
Nebivolol selectively blocks beta-1 adrenoceptors in the heart muscle, producing the following effects:
- Reduction of heart rate (negative chronotropic effect)
- Decrease in myocardial contractility (negative inotropic effect)
- Lowering of blood pressure through reduced cardiac output
Additionally, nebivolol stimulates endothelial nitric oxide synthase (eNOS), leading to relaxation and widening of blood vessels (vasodilation), which further reduces blood pressure. This dual mechanism sets nebivolol apart from conventional beta-blockers.
Dosage and Administration
Nebivolol is typically taken once daily as a tablet, with or without food. Standard dosing is as follows:
- Hypertension: 5 mg once daily
- Heart failure: Starting at 1.25 mg once daily, gradually titrated up to a target dose of 10 mg once daily
Dose adjustments are required in patients with impaired kidney or liver function. Treatment should never be stopped abruptly -- it must be tapered gradually to avoid rebound effects such as a sudden increase in blood pressure or worsening angina.
Side Effects
Like all beta-blockers, nebivolol may cause side effects. Common side effects include:
- Fatigue and tiredness
- Headache
- Dizziness
- Bradycardia (slow heart rate)
- Cold hands and feet
- Gastrointestinal complaints (nausea, diarrhea)
Less common side effects may include sleep disturbances, erectile dysfunction, and -- in predisposed individuals -- worsening of respiratory conditions such as asthma.
Contraindications
Nebivolol must not be used in patients with:
- Severe bradycardia (heart rate below 60 beats per minute)
- AV block of the second or third degree
- Severe bronchial asthma or chronic obstructive pulmonary disease (COPD)
- Cardiogenic shock or decompensated heart failure
- Severe hepatic (liver) impairment
- Pheochromocytoma (without concurrent alpha-blocker therapy)
Drug Interactions
Nebivolol may interact with several other medications:
- Calcium channel blockers (e.g., verapamil, diltiazem): Enhanced blood pressure-lowering and heart rate-reducing effects
- Antiarrhythmic drugs (e.g., amiodarone): Increased risk of bradycardia and AV block
- Antidiabetic agents: Risk of masking symptoms of hypoglycemia
- CYP2D6 inhibitors (e.g., fluoxetine, paroxetine): Increased plasma levels of nebivolol
References
- European Medicines Agency (EMA): Nebivolol - Summary of Product Characteristics. EMA, 2023.
- Wojciechowski D, Papademetriou V: Beta-blockers in the management of hypertension. Expert Review of Cardiovascular Therapy, 2008.
- Flather MD et al.: Randomized trial to determine the effect of nebivolol on mortality and cardiovascular hospital admission in elderly patients with heart failure (SENIORS). European Heart Journal, 2005.
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