Diltiazem with Sirolimus Interaction Details
Brand Names Associated with Diltiazem
- Cardizem®
- Cardizem® CD
- Cardizem® LA
- Cardizem® SR
- Cartia® XT
- Dilacor® XR
- Dilt-CD®
- Diltiazem
- Diltzac®
- Taztia® XT
- Teczem® (as a combination product containing Diltiazem, Enalapril)
- Tiamate®
- Tiazac®
Brand Names Associated with Sirolimus
- Rapamune®
- Rapamycin
- Sirolimus
Medical Content Editor Dr. Brian Staiger, PharmD
Last updated
Nov 13, 2023
Interaction Effect
An increased risk of sirolimus toxicity (anemia, leukopenia, thrombocytopenia, hypokalemia, diarrhea)
Interaction Summary
The concurrent administration of sirolimus 10 mg oral solution and diltiazem 120 mg to 18 healthy volunteers resulted in an increased sirolimus maximum concentration (Cmax), time to Cmax (tmax), and area under the concentration-time curve (AUC) of 1.4-fold, 1.3-fold, and 1.6-fold, respectively. Sirolimus had no effect on the pharmacokinetics of diltiazem or its metabolites.
Severity
Moderate
Onset
Delayed
Evidence
Probable
How To Manage Interaction
Monitor sirolimus levels and adjust sirolimus dosage as necessary. Also, monitor the patient for increased sirolimus toxicity.
Mechanism Of Interaction
Inhibition of cytochrome P450 3A4-mediated sirolimus metabolism
Literature Reports
A) Single-dose diltiazem coadministration leads to higher sirolimus exposure. An open single-dose, randomized, three-period, crossover study was conducted in 18 healthy subjects to study the interaction between a single oral dose of sirolimus 10 mg and a single oral dose of diltiazem 120 mg. The mean whole blood sirolimus concentrations were greater after 2 hours with diltiazem coadministration at all times compared with sirolimus monotherapy (p less than 0.05). Sirolimus area under the concentration-time curve (AUC) varied between 317 and 1487 ng h/mL; the sirolimus AUC in combination with diltiazem, varied between 777 and 2786 ng h/mL (p less than 0.001). The geometric mean values of the maximum serum concentration (Cmax) increased 43% (14-81%) and the AUC increased 60% (35-90%). The time to peak sirolimus concentration was prolonged by an average of 14 minutes with diltiazem coadministration. There was no statistically significant effects on exposure to diltiazem or its metabolite. No significant pharmacodynamic interactions were observed. Further clinical studies are needed to evaluate the effect of repeated doses of diltiazem .
Diltiazem Overview
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Diltiazem is used to treat high blood pressure and to control angina (chest pain). Diltiazem is in a class of medications called calcium-channel blockers. It works by relaxing the blood vessels so the heart does not have to pump as hard. It also increases the supply of blood and oxygen to the heart.
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High blood pressure is a common condition, and when not treated it 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.
Sirolimus Overview
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Sirolimus is used in combination with other medications to prevent rejection of kidney transplants. Sirolimus is in a class of medications called immunosuppressants. It works by suppressing the body's immune system.
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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:
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.