Ticagrelor with Simvastatin Interaction Details

Brand Names Associated with Ticagrelor

Brand Names Associated with Simvastatin

Medical Content Editor Dr. Brian Staiger, PharmD
Last updated Nov 10, 2023

Interaction Effect

Increased simvastatin plasma concentrations

Interaction Summary

In vitro metabolism studies showed that ticagrelor and its major active metabolite are weak inhibitors of CYP3A4; therefore, concomitant administration of simvastatin and ticagrelor will increase simvastatin plasma concentrations. During drug interaction studies (n=20), concomitant use of simvastatin and ticagrelor resulted in increased simvastatin AUC and Cmax. Avoid simvastatin doses greater than 40 mg when administered concomitantly with ticagrelor.

Severity

Moderate

Onset

Unspecified

Evidence

Established

How To Manage Interaction

Concomitant use of simvastatin and ticagrelor may result in higher serum concentrations of simvastatin. Therefore, the dose of simvastatin greater than 40 mg daily should be avoided if given concomitantly with ticagrelor.

Mechanism Of Interaction

Inhibition of CYP3A4-mediated simvastatin metabolism by ticagrelor

Literature Reports

A) In a two-way crossover study of simvastatin and ticagrelor, patients received either ticagrelor loading dose 270 mg followed by 180 mg twice daily for 7 days and simvastatin 80 mg on day 5 or simvastatin 80 mg only administered on day 5. Coadministration of ticagrelor and simvastatin resulted in an increase in simvastatin AUC by 56% (95% confidence interval (CI), 1.3 to 1.87) and Cmax by 81% (95% CI, 1.49 to 2.21) compared with simvastatin alone. AUC and Cmax increases of up to 2.3 fold were reported in some patients. Changes of Cmax and AUC of ticagrelor and its metabolite were not significant. Patients receiving ticagrelor should avoid simvastatin doses greater than 40 mg .

Ticagrelor Overview

• Ticagrelor is used to prevent a serious or life-threatening heart attack or stroke, or death in people who have had a heart attack or who have acute coronary syndrome (ACS; blockage of blood flow to the heart). It is also used to prevent blood clots from forming in people who have received coronary stents (metal tubes surgically placed in clogged blood vessels to improve blood flow) to treat ACS. Ticagrelor is used to decrease the risk of a first-time heart attack or stroke in people at risk with coronary artery disease (CAD; reduced blood flow to the heart). It is also used to decrease the risk of another more serious stroke in people who are having a mild to moderate stroke or a transient ischemic attack (TIA; ministroke). Ticagrelor is in a class of medications called antiplatelet medications. It works by preventing platelets (a type of blood cell) from collecting and forming clots that may cause a heart attack or stroke.

Simvastatin Overview

• Simvastatin 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. Simvastatin 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. Simvastatin 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). Simvastatin 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 simvastatin has been shown to prevent heart disease, angina (chest pain), strokes, and heart attacks.

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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:

• Gold Standard Drug Database
• Micromedex
• Lexicomp
• DrugBank

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.