Nebivolol: Difference between revisions
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| legal = Rx-only in US | | legal = Rx-only in US | ||
| mechanism = The d-enantiomer is a highly β1-selective antagonist; the l-enantiomer triggers endothelial nitric-oxide–mediated vasodilation. Unique among beta blockers for this NO mechanism. | | mechanism = The d-enantiomer is a highly β1-selective antagonist; the l-enantiomer triggers endothelial nitric-oxide–mediated vasodilation. Unique among beta blockers for this NO mechanism. | ||
| intro = Nebivolol is a third-generation beta blocker with two stereoisomers: d-nebivolol provides highly β1-selective blockade, while l-nebivolol releases endothelial NO and produces direct vasodilation. The result is a favorable side-effect profile relative to older beta blockers | | intro = Nebivolol is a third-generation beta blocker with two stereoisomers: d-nebivolol provides highly β1-selective blockade, while l-nebivolol releases endothelial NO and produces direct vasodilation. The result is a favorable side-effect profile relative to older beta blockers, less fatigue, less sexual dysfunction, and even some evidence of improved erectile function. FDA-approved only for hypertension in the US. | ||
| indications = | | indications = | ||
| dosing = | | dosing = | ||
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| pregnancy_details = | | pregnancy_details = | ||
| monitoring = Heart rate, blood pressure | | monitoring = Heart rate, blood pressure | ||
| counseling = Do not stop abruptly. Tolerated well by many patients who can't tolerate other beta blockers, but the FDA problem is HTN only | | counseling = Do not stop abruptly. Tolerated well by many patients who can't tolerate other beta blockers, but the FDA problem is HTN only, off-label use in HF lacks the trial evidence of metoprolol succinate / bisoprolol / carvedilol. | ||
| anecdotes = | | anecdotes = | ||
| seealso = [[Metoprolol]], [[Bisoprolol]], [[Propranolol]] | | seealso = [[Metoprolol]], [[Bisoprolol]], [[Propranolol]] | ||
Latest revision as of 03:16, 19 May 2026
Beta Blocker, Cardioselective (β1) + vasodilator
Nebivolol
Bystolic
Nebivolol is a third-generation beta blocker with two stereoisomers: d-nebivolol provides highly β1-selective blockade, while l-nebivolol releases endothelial NO and produces direct vasodilation. The result is a favorable side-effect profile relative to older beta blockers, less fatigue, less sexual dysfunction, and even some evidence of improved erectile function. FDA-approved only for hypertension in the US.
Heart rate, blood pressure
Do not stop abruptly. Tolerated well by many patients who can't tolerate other beta blockers, but the FDA problem is HTN only, off-label use in HF lacks the trial evidence of metoprolol succinate / bisoprolol / carvedilol.
Metoprolol, Bisoprolol, Propranolol
Experience
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Problems
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+ Add a problemTitration strategies
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Effects
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Pharmacokinetics
Absorption
Highly dependent on CYP2D6 phenotype: ~12% in extensive metabolizers, up to ~96% in poor metabolizers.Distribution
Plasma protein binding ~98%.Metabolism
Hepatic via CYP2D6 (extensive first-pass in EMs).Elimination
Renal (38%) and fecal (44%) excretion of metabolites.Interactions
Pharmacogenomic + mechanism interactions
Pharmacokinetic mechanismSubstrate / metabolism relationships from primary literature
FDA Drug Interactions Table: sensitive index substrate of CYP2D6.
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Clinical relevance: does this interaction matter in practice?trivialcritical
Mechanism description, if it needs work:
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Your own experience with this combination:
Experience (1 a little, 5 a lot)
Outcome (-100 worst, +100 best)
Inferred from pharmacokinetic dataMaterialised by the inference engine; provenance shown per row
Quinidine inhibits CYP2D6 (inhibitor_strong, intensity 95); Nebivolol is a substrate_major of CYP2D6 (intensity 80). Derived: Nebivolol exposure raised.
⏱ reversible competitive, effect resolves over ~5 inhibitor half-livesInferred via Enzyme:CYP2D6 (exposure raised)
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Clinical relevance: does this interaction matter in practice?trivialcritical
Confidence in this inference: is the inferred magnitude sound?overstatedsound
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Kinetics annotation:
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Your own experience with this combination:
Experience (1 a little, 5 a lot)
Outcome (-100 worst, +100 best)
Paroxetine inhibits CYP2D6 (inhibitor_strong, intensity 90); Nebivolol is a substrate_major of CYP2D6 (intensity 80). Derived: Nebivolol exposure raised.
⏱ mechanism-based, interaction persists ~4-6 weeks after stopping the inhibitorInferred via Enzyme:CYP2D6 (exposure raised)
Rate this interaction. Reports are anonymous and help curate the page.
Clinical relevance: does this interaction matter in practice?trivialcritical
Confidence in this inference: is the inferred magnitude sound?overstatedsound
Mechanism description, if it needs work:
Kinetics annotation:
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Your own experience with this combination:
Experience (1 a little, 5 a lot)
Outcome (-100 worst, +100 best)
Fluoxetine inhibits CYP2D6 (inhibitor_strong, intensity 90); Nebivolol is a substrate_major of CYP2D6 (intensity 80). Derived: Nebivolol exposure raised.
⏱ mechanism-based, interaction persists ~4-6 weeks after stopping the inhibitorInferred via Enzyme:CYP2D6 (exposure raised)
Rate this interaction. Reports are anonymous and help curate the page.
Clinical relevance: does this interaction matter in practice?trivialcritical
Confidence in this inference: is the inferred magnitude sound?overstatedsound
Mechanism description, if it needs work:
Kinetics annotation:
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Your own experience with this combination:
Experience (1 a little, 5 a lot)
Outcome (-100 worst, +100 best)
Bupropion inhibits CYP2D6 (inhibitor_strong, intensity 85); Nebivolol is a substrate_major of CYP2D6 (intensity 80). Derived: Nebivolol exposure raised.
⏱ reversible competitive, effect resolves over ~5 inhibitor half-livesInferred via Enzyme:CYP2D6 (exposure raised)
Rate this interaction. Reports are anonymous and help curate the page.
Clinical relevance: does this interaction matter in practice?trivialcritical
Confidence in this inference: is the inferred magnitude sound?overstatedsound
Mechanism description, if it needs work:
Kinetics annotation:
Is this row worth surfacing?
Your own experience with this combination:
Experience (1 a little, 5 a lot)
Outcome (-100 worst, +100 best)
Mirabegron inhibits CYP2D6 (inhibitor_moderate, intensity 55); Nebivolol is a substrate_major of CYP2D6 (intensity 80). Derived: Nebivolol exposure raised.
Inferred via Enzyme:CYP2D6 (exposure raised)
Rate this interaction. Reports are anonymous and help curate the page.
Clinical relevance: does this interaction matter in practice?trivialcritical
Confidence in this inference: is the inferred magnitude sound?overstatedsound
Mechanism description, if it needs work:
Is this row worth surfacing?
Your own experience with this combination:
Experience (1 a little, 5 a lot)
Outcome (-100 worst, +100 best)
Patient experience
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Monitoring
Patient counseling
Relevant anecdote
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Relevant Literature
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See also
References
Summary
Classes
Beta Blocker, Cardioselective (β1) + vasodilator
Common uses
Hypertension0
Pharmacy
Starting dose
5 mg daily
Preparations
2.5, 5, 10, 20 mg tabs
US FDA Max
40 mg/d
Pharmacology
Routes
Oral
Onset
1–2 h
Duration
24 h
Half-life
~10 h (CYP2D6 extensive metabolizers); up to 31 h (poor metabolizers)
Bioavailability
~12% (extensive metabolizers); ~96% (poor metabolizers)
Pregnancy
Category C
Legal status
Rx-only in US
Purported mechanism
The d-enantiomer is a highly β1-selective antagonist; the l-enantiomer triggers endothelial nitric-oxide–mediated vasodilation. Unique among beta blockers for this NO mechanism.