Atorvastatin with Rifampin Interaction Details
Brand Names Associated with Atorvastatin
- Atorvastatin
- Caduet® (as a combination product containing Amlodipine, Atorvastatin)
- Lipitor®
- Liptruzet® (as a combination product containing Atorvastatin, Ezetimibe)
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
Mar 04, 2024
Interaction Effect
Reduced atorvastatin concentration when administered separately after rifampin or increased atorvastatin exposure when administered simultaneously with rifampin
Interaction Summary
Coadministration of rifampin and atorvastatin may change atorvastatin exposure, varying with the timing of administration, due to multiple effects of rifampin upon the distribution and metabolism of atorvastatin. Simultaneous coadministration may lead to increased atorvastatin AUC and Cmax[1]. When administered at separate times, however, the atorvastatin AUC and Cmax were decreased [2]. If concurrent therapy is needed, simultaneous coadministration of the two drugs is recommended to avoid significantly decreased atorvastatin exposure [3][4].
Severity
Moderate
Onset
Unspecified
Evidence
Probable
How To Manage Interaction
If concurrent therapy of atorvastatin and rifampin is needed, simultaneous coadministration of the two drugs is recommended; when atorvastatin administration is delayed after rifampin administration, a significant decrease in atorvastatin exposure may occur[3][4].
Mechanism Of Interaction
Induction of CYP3A4-mediated metabolism of atorvastatin by rifampin; inhibition of OATP1B1-mediated efflux transport of atorvastatin by rifampin
Literature Reports
A) Subjects receiving rifampin 600 mg once daily for 7 days, who were administered a single dose of atorvastatin 40 mg at separate times after rifampin, had an 80% decrease in the atorvastatin AUC and a 40% reduction in the atorvastatin Cmax. When doses were administered simultaneously, a 30% increase in atorvastatin AUC and a 2.7-fold increase in atorvastatin Cmax were noted. Therefore, when used concurrently, administration of atorvastatin and rifampin simultaneously is recommended [3].
B) In 11 healthy volunteers, coadministration of a single IV rifampin 600 mg dose with a single oral atorvastatin 40 mg dose increased the atorvastatin acid AUC by 6.8-fold, and significantly increased the exposure to 2 active metabolites, 2-hydroxyatorvastatin acid and 4-hydroxyatorvastatin acid. Changes were attributed to the ability of rifampin to block organic anion-transporting polypeptide (OATP)1B1-mediated uptake of atorvastatin by hepatic cells; it is not known if these effects persist with daily dosing [1].
C) A study involving 10 healthy volunteers found rifampin 600 mg once daily for 5 days when given concurrently with a single atorvastatin 40 mg dose decreased the atorvastatin exposure. Rifampin decreased the AUC and Cmax of atorvastatin by 80% and 40% respectively. Rifampin also decreased the AUC of 2-hydroxyatorvastatin acid and 4-hydroxyatorvastatin acid by 43% and 81% respectively. This was attributed to the rifampin induction of CYP3A4-mediated atorvastatin metabolism [2].
D) Coadministration of rifampin 600 mg once daily for 5 days with a single dose of atorvastatin 40 mg at separate times after rifampin, increased the atorvastatin AUC by 0.2-fold and Cmax by 0.6-fold. When the same doses were administered simultaneously for 7 days, a 1.12-fold increase in atorvastatin AUC and a 2.9-fold increase in atorvastatin Cmax were noted [3].
References
1 ) Lau YY , Huang Y , Frassetto L , et al: effect of OATP1B transporter inhibition on the pharmacokinetics of atorvastatin in healthy volunteers. Clin Pharmacol Ther 2007; 81(2):194-204.PubMed Abstract: http://www.ncbi.nlm.nih.gov/...
2 ) Backman J, Luurila H, Neuvonen M, et al: Rifampin markedly decreases and gemfibrozil increases the plasma concentrations of atorvastatin and its metabolites. Clin Pharmacol Ther 2005; 78:154-167.
3 ) Product Information: LIPITOR(R) oral tablets, atorvastatin calcium oral tablets. Pfizer (Per FDA), New York, NY, 2012.
4 ) Product Information: ATORVALIQ(R) oral suspension, atorvastatin calcium oral suspension. CMP Pharma Inc (per FDA), Farmville, NC, 2023.
Atorvastatin Overview
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Atorvastatin is used together with diet, weight loss, and exercise to reduce the risk of heart attack and stroke and to decrease the chance that heart surgery will be needed in people who have heart disease or who are at risk of developing heart disease. Atorvastatin is also used to decrease the amount of fatty substances such as low-density lipoprotein (LDL) cholesterol ('bad cholesterol') and triglycerides in the blood and to increase the amount of high-density lipoprotein (HDL) cholesterol ('good cholesterol') in the blood. Atorvastatin may also be used to decrease the amount of cholesterol and other fatty substances in the blood in children and teenagers 10 to 17 years of age who have familial heterozygous hypercholesterolemia (an inherited condition in which cholesterol cannot be removed from the body normally). Atorvastatin is in a class of medications called HMG-CoA reductase inhibitors (statins). It works by slowing the production of cholesterol in the body to decrease the amount of cholesterol that may build up on the walls of the arteries and block blood flow to the heart, brain, and other parts of the body.
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Accumulation of cholesterol and fats along the walls of your arteries (a process known as atherosclerosis) decreases blood flow and, therefore, the oxygen supply to your heart, brain, and other parts of your body. Lowering your blood level of cholesterol and fats with atorvastatin has been shown to prevent heart disease, angina (chest pain), strokes, and heart attacks.
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.