NEBIVOLOL Drug Interactions
Also known as: Nebivolol
Nebivolol is a beta-blocker medication used to treat high blood pressure (hypertension). By helping to relax blood vessels and slow the heart rate, it lowers blood pressure, which in turn reduces the risk of serious heart problems like strokes and heart attacks.NEBIVOLOL has 7 documented drug interactions in our database, including 0 contraindicated, 3 major, 2 moderate, and 2 minor interactions.
0
Contraindicated
3
Major
2
Moderate
2
Minor
Concomitant use of nebivolol and fluoxetine can significantly increase nebivolol plasma concentrations, leading to enhanced beta-blockade effects. This can manifest as severe bradycardia, hypotension, and potentially heart block, increasing the risk of cardiovascular adverse events.
Mechanism
Fluoxetine is a potent inhibitor of the cytochrome P450 2D6 (CYP2D6) enzyme. Nebivolol is primarily metabolized by CYP2D6, so fluoxetine inhibits its metabolism, leading to elevated systemic exposure to nebivolol.
Clinical Management
Avoid concomitant use if possible. If co-administration is necessary, closely monitor the patient for signs and symptoms of excessive beta-blockade (e.g., bradycardia, hypotension). A significant dose reduction of nebivolol may be required, or consider an alternative beta-blocker that is not primarily metabolized by CYP2D6 (e.g., atenolol, bisoprolol, nadolol) or an antidepressant with minimal CYP2D6 inhibition (e.g., sertraline, escitalopram).
The co-administration of nebivolol and fluoxetine can lead to significantly increased plasma concentrations of nebivolol. This interaction can result in enhanced beta-adrenergic blockade, potentially causing severe bradycardia, hypotension, or heart block.
Mechanism
Fluoxetine is a potent inhibitor of the cytochrome P450 2D6 (CYP2D6) enzyme. Nebivolol is metabolized by CYP2D6, and its metabolism is inhibited by fluoxetine, leading to reduced clearance and elevated systemic exposure of nebivolol.
Clinical Management
Close monitoring for signs and symptoms of excessive beta-blockade (e.g., bradycardia, hypotension, dizziness) is essential. A reduction in the nebivolol dose may be necessary, or an alternative beta-blocker not primarily metabolized by CYP2D6 (e.g., atenolol, bisoprolol, nadolol) should be considered if the combination cannot be avoided. If an alternative SSRI is needed, sertraline or escitalopram, which have minimal CYP2D6 inhibition, could be considered.
The co-administration of nebivolol and paroxetine can lead to significantly increased plasma concentrations of nebivolol. This can result in enhanced beta-blockade effects, including severe bradycardia, hypotension, and potential heart block, requiring close monitoring.
Mechanism
Paroxetine is a potent inhibitor of the cytochrome P450 2D6 (CYP2D6) enzyme. Nebivolol is primarily metabolized by CYP2D6, so paroxetine inhibits its metabolism, leading to reduced clearance and elevated systemic exposure.
Clinical Management
Avoid concurrent use if possible. If co-administration is necessary, a significant reduction in the nebivolol dose should be considered, along with frequent and close monitoring for signs of bradycardia, hypotension, and other symptoms of excessive beta-blockade. Consider alternative beta-blockers not metabolized by CYP2D6 (e.g., atenolol, bisoprolol, nadolol) or antidepressants with minimal CYP2D6 inhibition (e.g., sertraline, escitalopram).
Citalopram is a weak inhibitor of CYP2D6, which is the primary enzyme responsible for nebivolol's metabolism. This interaction can lead to increased plasma concentrations of nebivolol, potentially enhancing its beta-blocking effects such as bradycardia, hypotension, and heart block.
Mechanism
Citalopram weakly inhibits cytochrome P450 2D6 (CYP2D6). Nebivolol is primarily metabolized by CYP2D6, so inhibition of this enzyme can reduce nebivolol clearance, increasing its systemic exposure.
Clinical Management
Monitor patients for signs and symptoms of increased beta-blockade, including bradycardia, hypotension, and dizziness, especially when initiating or adjusting citalopram or nebivolol. Consider using the lowest effective dose of nebivolol or selecting an alternative antidepressant with minimal CYP2D6 inhibition if close monitoring is not feasible.
Coadministration of nebivolol with fluvoxamine may increase nebivolol plasma concentrations, potentially leading to enhanced beta-blockade effects such as bradycardia and hypotension. This interaction is due to fluvoxamine's inhibition of CYP2D6, the primary enzyme responsible for nebivolol's metabolism.
Mechanism
Nebivolol is primarily metabolized by CYP2D6. Fluvoxamine is a known inhibitor of CYP2D6, though not as potent as fluoxetine or paroxetine. Inhibition of nebivolol's metabolism by fluvoxamine can lead to increased systemic exposure and accumulation of nebivolol.
Clinical Management
Monitor patients closely for signs and symptoms of excessive beta-blockade, including bradycardia, hypotension, and dizziness, especially when initiating fluvoxamine or increasing its dose. A lower starting dose of nebivolol or dose reduction may be necessary if coadministration cannot be avoided. Consider alternative antidepressants with minimal CYP2D6 inhibition if significant adverse effects occur.
The interaction between nebivolol and sertraline is generally considered to be of minor clinical significance. While both drugs can independently cause bradycardia, sertraline has minimal CYP2D6 inhibitory effects, thus unlikely to significantly alter nebivolol's plasma concentrations.
Mechanism
Nebivolol is metabolized by CYP2D6. Sertraline is a weak inhibitor of CYP2D6. Although both drugs can cause bradycardia, the pharmacokinetic interaction is minimal, and additive pharmacodynamic effects are generally not clinically significant.
Clinical Management
Routine monitoring for vital signs, including heart rate, is advisable, especially when initiating or adjusting either medication. No specific dose adjustments are typically required for either drug due to this interaction. Patients should be advised to report symptoms of excessive bradycardia or hypotension.
The interaction between nebivolol and escitalopram is generally considered minor. While both drugs can independently cause bradycardia, escitalopram has minimal CYP2D6 inhibitory activity, suggesting a low risk of significantly increased nebivolol plasma levels.
Mechanism
Nebivolol is metabolized by CYP2D6. Escitalopram is a weak inhibitor of CYP2D6, so it is unlikely to cause a clinically significant increase in nebivolol concentrations. Both drugs can cause bradycardia through different pharmacodynamic mechanisms (beta-blockade for nebivolol, serotonergic effects for escitalopram, though direct bradycardic effect of escitalopram is less common).
Clinical Management
Routine monitoring for additive pharmacodynamic effects like bradycardia and hypotension is advisable, especially when initiating or adjusting doses of either medication. No specific dose adjustments are typically required for either drug due to this interaction, but individual patient response should guide therapy. If bradycardia or hypotension occurs, consider dose reduction or alternative agents.
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