Amlodipine with Telaprevir Interaction Details

Brand Names Associated with Amlodipine

Brand Names Associated with Telaprevir

Medical Content Editor Dr. Brian Staiger, PharmD
Last updated Mar 03, 2024

Interaction Effect

Increased amlodipine plasma concentrations

Interaction Summary

Telaprevir is an inhibitor of CYP3A isozymes[1]. In a pharmacokinetic study in healthy volunteers (n=21), telaprevir was shown to increase the AUC and Cmax of amlodipine by 2.79-fold and 1.27-fold, respectively, when given concomitantly [2]. If coadministration of amlodipine and telaprevir is necessary, clinical monitoring is recommended and dose reductions for amlodipine should be considered. If dose adjustments are required, return to normal amlodipine dosing after therapy with telaprevir has been completed [1].

Severity

Major

Onset

Rapid

Evidence

Established

How To Manage Interaction

Concomitant use of amlodipine and telaprevir may lead to increased amlodipine plasma concentrations. If coadministration of amlodipine and telaprevir is necessary, clinical monitoring is recommended and dose reductions for amlodipine should be considered. If dose adjustments are required, return to normal amlodipine dosing after therapy with telaprevir has been completed[1].

Mechanism Of Interaction

Inhibition of CYP3A4-mediated amlodipine 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 1.27-fold increase (90% confidence interval (CI), 1.21 to 1.33) in Cmax and a 2.79-fold increase (90% CI, 2.58 to 3.01) in AUC of amlodipine on day 11 compared with day 1. Amlodipine mean apparent clearance decreased from 38 L/hr to 12.3 L/hr. For atorvastatin, there was a 10.6-fold increase (90% 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 on day 11 compared to 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) film coated oral tablets, telaprevir film coated oral tablets. Vertex Pharmaceuticals Incorporated, Cambridge, MA, 2011.

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/...

Amlodipine Overview

• Amlodipine is used alone or in combination with other medications to treat high blood pressure in adults and children 6 years and older. It is also used to treat certain types of angina (chest pain) and coronary artery disease (narrowing of the blood vessels that supply blood to the heart). Amlodipine is in a class of medications called calcium channel blockers. It lowers blood pressure by relaxing the blood vessels so the heart does not have to pump as hard. It controls chest pain by increasing the supply of blood to the heart. If taken regularly, amlodipine controls chest pain, but it does not stop chest pain once it starts. Your doctor may prescribe a different medication to take when you have chest pain.

• High blood pressure is a common condition and when not treated, can cause damage to the brain, heart, blood vessels, kidneys and other parts of the body. Damage to these organs may cause heart disease, a heart attack, heart failure, stroke, kidney failure, loss of vision, and other problems. In addition to taking medication, making lifestyle changes will also help to control your blood pressure. These changes include eating a diet that is low in fat and salt, maintaining a healthy weight, exercising at least 30 minutes most days, not smoking, and using alcohol in moderation.

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.