Atorvastatin with St John's Wort 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)
Medical Content Editor Dr. Brian Staiger, PharmD
Last updated
Mar 04, 2024
Interaction Effect
Reduced effectiveness of atorvastatin
Interaction Summary
Concomitant use of atorvastatin with CYP3A4 inducers can lead to variable reductions in plasma concentrations of atorvastatin[1]. In a systematic review of studies, concomitant use resulted in a decrease in atorvastatin AUC of 12% with St. Johns wort products containing hyperforin dosages of 18 to 36 mg/day. The risk of interactions cannot be excluded even for low-dose hyperforin St. John’s wort products, however the use of products that result in a dose of not more than 1 mg hyperforin per day may minimize the risk of interactions [2].
Severity
Moderate
Onset
Delayed
Evidence
Established
How To Manage Interaction
Concomitant use of atorvastatin with CYP3A4 inducers can lead to variable reductions in plasma concentrations of atorvastatin[1]. The risk of interactions cannot be excluded even for low-dose hyperforin St. John’s wort products, however the use of products that result in a dose of not more than 1 mg hyperforin per day may minimize the risk of interactions [2].
Mechanism Of Interaction
Induction of CYP3A4-mediated metabolism of atorvastatin by St John's Wort
Literature Reports
A) In a systematic review of studies of pharmacokinetic interactions involving St John's Wort, concomitant use with atorvastatin in 1 study (n=12) resulted in a 12% decrease in atorvastatin AUC with products containing hyperforin dosages of 18 to 36 mg/day [2].
B) St. John's Wort significantly increased P-glycoprotein expression and associated drug efflux in a randomized, single-blind, placebo-controlled trial of 22 healthy subjects (13 female, 9 male). Subjects received St. John's Wort (Good n' Natural, standardized to 0.15% hypericin) 600 mg (n=15) or placebo (n=7) 3 times daily for 16 days. P-glycoprotein expression in peripheral blood mononuclear cells increased 4.2-fold with St. John's Wort after 16 days (29.5 +/- 14.3 median fluorescence intensity (MFI, a measure of P-glycoprotein expression) versus 7 +/- 1.9 MFI, 95% CI: 13.5, 31.6). Individual variability occurred with a range of 1.09 to 9.06 MFI after St. John's Wort. No change in P-glycoprotein expression occurred in subjects receiving placebo. P-glycoprotein expression returned to baseline 16 days after discontinuing St. John's Wort. Efflux of the known P-glycoprotein substrate rhodamine was increased with St. John's Wort; no change in efflux occurred with placebo. Ritonavir (5 mcmol), known to reverse P-glycoprotein drug efflux, was significantly less effective in reducing rhodamine efflux in subjects treated with St. John's Wort (75.4 +/- 16.4% versus 23.9 +/- 15.3%, 95% CI: 43.7, 70.1). Three subjects receiving St. John's Wort withdrew from the study, one experienced adverse effects (nausea, dry mouth), and two needed potentially interacting medications. Analyses of 2 capsules from 3 batches of St. John's Wort with high performance liquid chromatography verified the hypericin content to be 0.15%, 0.14%, and 0.15% [3].
References
1 ) Product Information: LIPITOR(R) oral tablets, atorvastatin calcium oral tablets. Parke-Davis (per FDA), New York, NY, 2018.
2 ) Chrubasik-Hausmann S, Vlachojannis J, & McLachlan AJ: Understanding drug interactions with St John's wort (Hypericum perforatum L.): impact of hyperforin content. J Pharm Pharmacol 2019; 71(1):129-138.PubMed Abstract: http://www.ncbi.nlm.nih.gov/...
3 ) Hennessy M, Kelleher D, Spiers JP, et al: St. John's Wort increases expression of P-glycoprotein: implications for drug interactions. Br J Clin Pharmacol 2002; 53(1):75-82.
Atorvastatin Overview
-
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.
-
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.
Return To Our Drug Interaction Homepage
Feedback, Question Or Comment About This Information?
Ask Dr. Brian Staiger, PharmD, our medical editor, directly! He's always more than happy to assist.
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.