Venetoclax with Rifampin Interaction Details
Brand Names Associated with Venetoclax
- Venclexta®
- Venetoclax
Brand Names Associated with Rifampin
- Rifadin®
- Rifamate® (as a combination product containing Isoniazid, Rifampin)
- Rifampin
- Rifater® (as a combination product containing Isoniazid, Pyrazinamide, Rifampin)
- Rimactane®
Medical Content Editor Dr. Brian Staiger, PharmD
Last updated
Dec 20, 2023
Interaction Effect
Altered exposure of venetoclax
Interaction Summary
Avoid concomitant use of venetoclax (a CYP3A and P-gp substrate) and rifampin (a strong CYP3A inducer and a P-gp inhibitor) due to the potential for altered venetoclax exposure. Consider using drugs with less CYP3A induction. Coadministration has resulted in decreased venetoclax exposure with multiple doses of rifampin and increased exposure with a single rifampin dose. When venetoclax is coadministered with P-gp inhibitors, reduce the venetoclax dosage by at least 50% and closely monitor patients for venetoclax toxicity. Upon discontinuation of the P-gp inhibitor, wait 2 to 3 days before resuming the venetoclax dosage used prior to initiation of the inhibitor.
Severity
Major
Onset
Unspecified
Evidence
Theoretical
How To Manage Interaction
Avoid concomitant use of venetoclax (a CYP3A and P-gp substrate) and rifampin (a strong CYP3A inducer and a P-gp inhibitor) due to the potential for altered venetoclax exposure. Consider using drugs with less CYP3A induction. Coadministration has resulted in decreased venetoclax exposure with multiple doses of rifampin and increased exposure with a single rifampin dose. When venetoclax is coadministered with P-gp inhibitors, reduce the venetoclax dosage by at least 50% and closely monitor patients for venetoclax toxicity. Upon discontinuation of the P-gp inhibitor, wait 2 to 3 days before resuming the venetoclax dosage used prior to initiation of the inhibitor.
Mechanism Of Interaction
Inhibition of P-gp-mediated transport of venetoclax; induction of CYP3A-mediated venetoclax metabolism
Literature Reports
A) Rifampin is both a strong CYP3A inducer and a P-gp inhibitor. In 2 pharmacokinetic studies, the administration of venetoclax with rifampin 600 mg once daily for 13 days (n=10) decreased the venetoclax Cmax by 42% and the AUC by 71%, while a single dose of rifampin 500 mg (n=11) increased venetoclax Cmax by 106% and AUC by 78% .
Venetoclax Overview
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Venetoclax is used alone or in combination with obinutuzumab (Gazyva) or rituximab (Rituxan) to treat certain types of chronic lymphocytic leukemia (CLL; a type of cancer that begins in the white blood cells) or certain types of small lymphocytic lymphoma (SLL; a type of cancer that begins mostly in the lymph nodes). It is also used in combination with either azacitidine (Vidaza), decitabine (Dacogen), or cytarabine as a first treatment for acute myeloid leukemia (AML; a type of cancer that begins in the white blood cells) in people 75 years of age or older, or in adults who have medical conditions that prevents them from being treated with other chemotherapy medications. Venetoclax is in a class of medications called B-cell lymphoma-2 (BCL-2) inhibitors. It works by blocking the action of a certain protein in the body that helps cancer cells survive. This helps to kill cancer cells.
Rifampin Overview
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Rifampin is used with other medications to treat tuberculosis (TB; a serious infection that affects the lungs and sometimes other parts of the body). Rifampin is also used to treat some people who have Neisseria meningitidis (a type of bacteria that can cause a serious infection called meningitis) infections in their noses or throats. These people have not developed symptoms of the disease, and this treatment is used to prevent them from infecting other people. Rifampin should not be used to treat people who have developed symptoms of meningitis. Rifampin is in a class of medications called antimycobacterials. It works by killing the bacteria that cause infection.
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Antibiotics such as rifampin will not work for colds, flu, or other viral infections. Using antibiotics when they are not needed increases your risk of getting an infection later that resists antibiotic treatment.
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Definitions
Severity Categories
Contraindicated
These drugs, generally, should not be used together simultaneously due to the high risk of severe adverse effects. Combining these medications can lead to dangerous health outcomes and should be strictly avoided unless otherwise instructed by your provider.
Major
This interaction could result in very serious and potentially life-threatening consequences. If you are taking this drug combination, it is very important to be under close medical supervision to minimize severe side effects and ensure your safety. It may be necessary to change a medication or dosage to prevent harm.
Moderate
This interaction has the potential to worsen your medical condition or alter the effectiveness of your treatment. It's important that you are monitored closely and you potentially may need to make adjustments in your treatment plan or drug dosage to maintain optimal health.
Minor
While this interaction is unlikely to cause significant problems, it could intensify side effects or reduce the effectiveness of one or both medications. Monitoring for changes in symptoms and your condition is recommended, and adjustments may be made if needed to manage any increased or more pronounced side effects.
Onset
Rapid: Onset of drug interaction typically occurs within 24 hours of co-administration.
Delayed: Onset of drug interaction typically occurs more than 24 hours after co-administration.
Evidence
Level of documentation of the interaction.
Established: The interaction is documented and substantiated in peer-reviewed medical literature.
Theoretical: This interaction is not fully supported by current medical evidence or well-documented sources, but it is based on known drug mechanisms, drug effects, and other relevant information.
How To Manage The Interaction
Provides a detailed discussion on how patients and clinicians can approach the identified drug interaction as well as offers guidance on what to expect and strategies to potentially mitigate the effects of the interaction. This may include recommendations on adjusting medication dosages, altering the timing of drug administration, or closely monitoring for specific symptoms.
It's important to note that all medical situations are unique, and management approaches should be tailored to individual circumstances. Patients should always consult their healthcare provider for personalized advice and guidance on managing drug interactions effectively.
Mechanism Of Interaction
The theorized or clinically determined reason (i.e., mechanism) why the drug-drug interaction occurs.
Disclaimer: The information provided on this page is for informational purposes only and should not be considered medical advice. Always consult with a qualified healthcare professional regarding your specific circumstances and medical conditions.
Where Does Our Information Come From?
Information for our drug interactions is compiled from several drug compendia, including:
The prescribing information for each drug, as published on DailyMED, is also used.
Individual drug-drug interaction detail pages contain references specific to that interaction. You can click on the reference number within brackets '[]' to see what reference was utilized.
The information posted is fact-checked by HelloPharmacist clinicians and reviewed quarterly.