Imatinib with Midazolam Interaction Details
Brand Names Associated with Imatinib
- Gleevec®
- Imatinib
Brand Names Associated with Midazolam
- Midazolam
- Versed®
Medical Content Editor Dr. Brian Staiger, PharmD
Last updated
Nov 07, 2023
Interaction Effect
Increased midazolam exposure and increased risk for prolonged sedation
Interaction Summary
Concomitant use of midazolam (CYP3A4 substrate) with this drug (moderate CYP3A4 inhibitor) may result in prolonged sedation because of a decrease in plasma clearance of midazolam and should be avoided. Concomitant use of midazolam with moderate CYP3A4 inhibitors has reduced midazolam clearance and increased its half-life in pharmacokinetic studies.
Severity
Major
Onset
Unspecified
Evidence
Probable
How To Manage Interaction
Concomitant use of midazolam (CYP3A4 substrate) with this drug (moderate CYP3A4 inhibitor) may result in prolonged sedation because of a decrease in plasma clearance of midazolam and should be avoided.
Mechanism Of Interaction
Inhibition of CYP3A4-mediated midazolam metabolism
Literature Reports
A) Concomitant administration of a single dose of midazolam 0.5 mg/kg IV (CYP3A4 substrate) and erythromycin 500 mg 3 times a day (moderate CYP3A4 inhibitor), for 1 week (n=6), reduced the clearance of midazolam and doubled the half-life .
B) In a 3-way crossover study (n=9) concomitant administration of midazolam (CYP3A4 substrate), diltiazem 60 mg 3 times a day, and verapamil 80 mg 3 times a day (moderate CYP3A4 inhibitors) increased the half-life of midazolam from 5 to 7 hours. No interaction was observed in healthy subjects between midazolam and nifedipine .
C) In a clinical study, the concurrent administration of letermovir and oral midazolam in healthy women (n=16) increased midazolam mean Cmax by 172.4% and mean AUC(0 to last measurable concentration) by 225.3%. Similarly, the concurrent administration of letermovir and IV midazolam led to increases in midazolam mean Cmax by 105.2% and mean AUC(0 to last measurable concentration) by 146.6%. Participants received oral letermovir 240 mg on days 1 to 6. A single bolus of IV midazolam 1 mg/mL was administered on day 4 alone and immediately after letermovir on day 4. Oral midazolam 1 mL was administered on the morning of day 2 alone and immediately after letermovir on day 6. Letermovir is an inhibitor of CYP3A, while midazolam is a substrate of CYP3A. Clearance for midazolam was decreased in the presence of letermovir compared with midazolam alone. If letermovir and midazolam are coadministered, frequent monitoring and possible dose adjustments may be needed during and after discontinuation of letermovir .
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.
Midazolam Overview
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Midazolam is given to children before medical procedures or before anesthesia for surgery to cause drowsiness, relieve anxiety, and prevent any memory of the event. Midazolam is in a class of medications called benzodiazepines. It works by slowing activity in the brain to allow relaxation and sleep.
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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.