Imatinib with Amlodipine Interaction Details

Brand Names Associated with Imatinib

Brand Names Associated with Amlodipine

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

Interaction Effect

Increased amlodipine exposure; increased risk of imatinib toxicity

Interaction Summary

Use caution with coadministration of amlodipine (a CYP3A substrate and inhibitor)[1] with imatinib (a CYP3A4 substrate and inhibitor) [2], as increased amlodipine [1] and imatinib exposure may occur [2]. Although not specifically studied with amlodipine, Cmax and AUC of simvastatin (a CYP3A4 substrate) increased by 2- and 3.5-fold, respectively, with concurrent imatinib use [2]. Imatinib toxicity and peripheral neuropathy developed in 1 patient when amlodipine was added to an imatinib regimen [3]. Assess for edema and hypotension if coadministered. Dose adjustment may be warranted if symptoms develop [1].

Severity

Moderate

Onset

Unspecified

Evidence

Theoretical

How To Manage Interaction

Use caution with coadministration of amlodipine (a CYP3A substrate and inhibitor)[1] with imatinib (a CYP3A4 substrate and inhibitor) [2], as increased amlodipine [1] and imatinib exposure may occur [2]. If used concurrently, assess for edema and hypotension. Dose adjustment may be warranted if symptoms develop [1].

Mechanism Of Interaction

Inhibition of CYP3A4-mediated amlodipine metabolism; interference with CYP3A4-mediated imatinib metabolism

Literature Reports

A) Imatinib toxicity and peripheral neuropathy occurred with concurrent use of amlodipine and imatinib in a 74-year-old male with chronic myeloid leukemia. During treatment with imatinib 400 mg twice daily, concomitant perindopril was switched to amlodipine 10 mg daily due to suspected perindopril-induced angioedema. Two weeks after amlodipine initiation, the patient developed nausea and periorbital and ankle edema. Diuretics abated the edema; however, 10 days later, the patient developed bilateral pain and numbness in the soles of his feet, numbness of the chin, and reduced acuity to light touch and vibrations. The edema, pain, and numbness resolved with amlodipine discontinuation and imatinib dose reduction. Despite residual numbness in his feet, the patient tolerated imatinib titration to 600 mg daily. Two months after onset of the neuropathy, nerve conduction testing revealed mild sensorimotor axonal neuropathy. The neuropathy completely resolved 9 months later during treatment with imatinib 600 mg day [3].

References

1 ) Product Information: PRESTALIA(R) oral tablets, perindopril arginine amlodipine oral tablets. SYMPLMED LLC (per FDA), Cincinnati, OH, 2015.

2 ) Product Information: GLEEVEC oral tablets, imatinib mesylate oral tablets. Novartis Pharmaceuticals Corporation (per FDA), East Hanover, NJ, 2014.

3 ) Ross DM: Peripheral neuropathy on imatinib treatment for chronic myeloid leukaemia: suspected adverse drug interaction with amlodipine. Intern Med J 2009; 39(10):708-708.PubMed Abstract: http://www.ncbi.nlm.nih.gov/...

Imatinib Overview

• Imatinib is used to treat certain types of leukemia (cancer that begins in the white blood cells) and other cancers and disorders of the blood cells. Imatinib is also used to treat certain types of gastrointestinal stromal tumors (GIST; a type of tumor that grows in the walls of the digestive passages and may spread to other parts of the body). Imatinib is also used to treat dermatofibrosarcoma protuberans (a tumor that forms under the top layer of skin) when the tumor cannot be removed surgically, has spread to other parts of the body, or has come back after surgery. Imatinib is in a class of medications called kinase inhibitors. It works by blocking the action of the abnormal protein that signals cancer cells to multiply. This helps stop the spread of cancer cells.

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.

Return To Our Drug Interaction Homepage

Feedback, Question Or Comment About This Information?

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.