Beta-Blocker Interactions and CYP Enzymes – Free Table

Beta-blockers are a class of medication that is frequently used for cardiac and cardiovascular purposes. Selectivity and evidence of benefit often guide selection, but one thing that may get overlooked is beta-blocker interactions in relation to CYP enzymes. Not all beta-blockers interact with CYP enzymes and those that don’t always follow a pattern.

We wanted to create this table of beta-blocker interactions and CYP enzymes to demonstrate which medications in this class may be affected by commonly used medications that can inhibit or induce certain CYP450 enzymes and how they may impact each individual beta-blocker. These are definitely differences that may show up on a pharmacist board exam!

Drug NameMetabolism and EliminationCYP Drug InteractionsResults of Interaction
Atenolol (Tenormin)Eliminated by the kidneysAvoids CYP Drug InteractionsDose adjustments with declining renal function
Bisoprolol (Zebeta)50% by CYP3A450% renal excretionCYP3A4 inhibitors CYP3A4 InducersClarithromycin, Erythromycin, Diltiazem, Itraconazole, Ketoconazole, Ritonavir, Verapamil, and Grapefruit (CYP3A4 Inhibitors)- increases concentrations of Bisoprolol

Glucocorticoids, Rifampin, Carbamazepine, phenobarbital, and phenytoin (CYP3A4 inducers)– increased metabolism of Bisoprolol and reduced concentrations
Carvedilol (Coreg)Aromatic ring oxidation and glucuronidation
Metabolized by CYP2D6 and 2C9
CYP2D6 Inhibitors CYP2C9 InhibitorsFluoxetine, Paroxetine, Bupropion, antipsychotics antiretrovirals (CYP2D6 inhibitors)– increases levels of Carvedilol
Esmolol (Brevibloc)Metabolized by esterases in red blood cellsAvoids CYP Drug InteractionsN/A
Labetalol (Normodyne, Trandate)Metabolized by UGT2B7 and UGT1A1Avoids CYP Drug interactionsN/A
Metoprolol (Lopressor, Toprol-XL)Metabolized by CYP2D6CYP2D6 inhibitorsFluoxetine, Paroxetine, Bupropion, sertraline, antipsychotics antiretroviral (CYP2D6 inhibitors)-increases concentrations of Metoprolol
Nadolol (Corgard)Eliminated by the kidneysAvoids CYP Dose InteractionsDose adjustments with declining renal impairment
Nebivolol (Bystolic)Metabolized by CYP2D6 and glucuronidation CYP2D6 inhibitors Fluoxetine, Paroxetine, Bupropion, antipsychotics antiretrovirals – increases concentrations of Nebivolol
Pindolol (Visken)Undergoes glucuronidation or sulfate conjugation.Avoids CYP drug interactions.N/A
Propranolol (Inderan)Aromatic ring oxidation and glucuronidation CYP2D6, 1A2, 2C19 involvementCYP2D6 inhibitors 
CYP1A2 inhibitors 
CYP2C19 inhibitors 
Fluoxetine, Paroxetine, Bupropion, antipsychotics antiretrovirals – increases levels of propranolol

Cimetidine, Ciprofloxacin, Fluvoxamine, Isoniazid, Ritonavir (CYP1A2 inhibitors)-  increases levels of propranolol

Fluconazole, Cimetidine, Fluoxetine, Fluvoxamine, Tenioposide (CYP2C19 inhibitors)- increases levels of propranolol
Sotalol (Betapace)Primarily eliminated by the kidneysAvoids CYP drug interactionsDose adjustments with declining renal impairment
Timolol (Blocadren)Metabolized by CYP2D6 and little involvement with 2C19CYP2D6 inhibitorsFluoxetine, Paroxetine, Bupropion, antipsychotics antiretroviral (CYP2D6 inhibitors)- increases concentration of Timolol
Beta Blocker Interactions and CYP Enzymes

Bisoprolol has a compelling indication for heart failure and in my experience is seldom used compared to carvedilol and metoprolol (podcast). It can significantly interact with medications that affect CYP3A4.

CYP2D6 is a critical enzyme for many of the most commonly used beta-blockers. Metoprolol and carvedilol are the two frequently used agents that may be impacted by our patients taking a CYP2D6 inhibitor or inducer.

Propranolol is probably the most complicated beta-blocker when it comes to CYP drug interactions. This medication is broken down by three CYP enzymes. While this does make it more complex, it can also blunt the overall effect of the interaction if there are other pathways for breakdown. I think it is important to emphasize close monitoring when new drugs are started with propranolol because there is a significant potential for many drugs to interact with it.

Note that we have a few beta-blockers that are primarily eliminated via the kidney. Atenolol, sotalol, and nadolol avoid CYP enzymes altogether. A few others are metabolized by non-CYP mechanisms. Esmolol, labetalol, and pindolol are metabolized by alternative methods as you can see in the beta-blocker CYP enzyme table above.

Looking for more on beta-blocker drug interactions? In this previous post, I discuss some options to address the beta-blocker albuterol interaction.

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1 Comment

  1. Dr. Faith IRIFERI

    This is super-helpful; a great reminder for closer prescription audits for those with compelling indications as Cardiovascular diseases. Thanks


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Written By Eric Christianson

April 19, 2023

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