Atorvastatin with Telaprevir Interaction Details

Brand Names Associated with Atorvastatin

Brand Names Associated with Telaprevir

Medical Content Editor Dr. Brian Staiger, PharmD
Last updated Mar 04, 2024

Interaction Effect

Increased atorvastatin concentrations

Interaction Summary

Telaprevir is a potent inhibitor of CYP3A isozymes[1]. In a pharmacokinetic study in healthy volunteers (n=21), coadministration of atorvastatin (a CYP3A4 substrate; given as a coformulation with amlodipine) with telaprevir increased the mean AUC and Cmax of atorvastatin by 10.6-fold and 7.88-fold, respectively [2]. Due to the potential for increased atorvastatin plasma concentrations and risk of serious side effects, such as myopathy and rhabdomyolysis, coadministration of atorvastatin and telaprevir should be avoided [1].

Severity

Major

Onset

Unspecified

Evidence

Established

How To Manage Interaction

Avoid the concomitant use of atorvastatin and telaprevir due to the potential for significant increases in atorvastatin concentration, which may lead to serious side effects such as myopathy, including rhabdomyolysis[1].

Mechanism Of Interaction

Inhibition of CYP3A-mediated atorvastatin metabolism

Literature Reports

A) In an pharmacokinetic study in healthy volunteers (n=21), telaprevir, when given concomitantly with a coformulation of amlodipine/atorvastatin, resulted in a significant increase in both amlodipine and atorvastatin exposure. Study participants were given a single dose of amlodipine 5 mg/atorvastatin 20 mg on day 1, telaprevir (750 mg every 8 hours) starting day 11 and continued through day 26, and a second dose of amlodipine/atorvastatin on day 17. There was a 10.6-fold increase (90% confidence interval (CI), 8.74 to 12.85) in mean Cmax and a 7.88-fold increase (90% CI, 6.84 to 9.07) in mean AUC of atorvastatin on day 11 compared to day 1. Atorvastatin mean apparent clearance decreased from 685 L/hr to 83.8 L/hr. For amlodipine, there was 1.27-fold increase (90% CI, 1.21 to 1.33) in Cmax and a 2.79-fold increase (90% CI, 2.58 to 3.01) in AUC on day 11 compared with day 1. The steady-state pharmacokinetic parameters of telaprevir were not significantly effected by the coadministration of amlodipine/atorvastatin [2].

References

1 ) Product Information: INCIVEK(TM) oral film coated tablets, telaprevir oral film coated tablets. Vertex Pharmaceuticals Incorporated (per manufacturer), Cambridge, MA, 2012.

2 ) Lee JE, van Heeswijk R, Alves K, et al: Effect of the hepatitis C virus protease inhibitor telaprevir on the pharmacokinetics of amlodipine and atorvastatin. Antimicrob Agents Chemother 2011; 55(10):4569-4574.PubMed Abstract: http://www.ncbi.nlm.nih.gov/...

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.

Telaprevir Overview

• Telaprevir is used along with two other medications (ribavirin [Copegus, Rebetol] and peginterferon alfa [Pegasys]) to treat chronic hepatitis C (an ongoing viral infection that damages the liver) in people who have not yet been treated for this condition or whose condition could not successfully be treated with ribavirin and peginterferon alfa alone. Telaprevir is in a class of medications called protease inhibitors. It works by decreasing the amount of hepatitis C virus (HCV) in the body. Telaprevir may not prevent the spread of hepatitis C to other people.

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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.