Drug Interactions between berotralstat and ketoconazole
This report displays the potential drug interactions for the following 2 drugs:
- berotralstat
- ketoconazole
Interactions between your drugs
ketoconazole berotralstat
Applies to: ketoconazole and berotralstat
Consumer information for this interaction is not currently available.
MONITOR: Coadministration of berotralstat with drugs that are both substrates of the isoenzyme CYP450 3A4 as well as inhibitors of the efflux transporters P-glycoprotein (P-gp) and/or breast cancer resistance protein (BCRP) may lead to an increase in the plasma concentrations and effects of both drugs. Berotralstat is considered a moderate CYP450 3A4 inhibitor and has been reported in drug interaction studies to increase the peak plasma concentration (Cmax) and systemic exposure (AUC) of the sensitive CYP450 3A4 substrate midazolam by approximately 1.5-fold and 2.25-fold, respectively. In addition, berotralstat is a substrate of both P-gp and BCRP. Coadministration with the potent P-gp and BCRP inhibitor cyclosporine increased berotralstat peak plasma concentration (Cmax) and total systemic drug exposure (AUC 0-inf) by 25% and 69%, respectively. Increased plasma concentrations of berotralstat may increase the risk of adverse effects, including the potential for QT prolongation. Berotralstat may cause concentration-dependent prolongation of the Fridericia-corrected QT interval (QTcF). A mean increase in the QTcF interval of 15.9 milliseconds has been reported at three times the recommended dose of berotralstat; however, berotralstat has not been shown to prolong the QT interval to any clinically relevant extent when administered at the recommended daily dose of 150 mg.
MANAGEMENT: During concomitant use of berotralstat with drugs that are substrates of CYP450 3A4, particularly those with a narrow therapeutic index, clinical and laboratory monitoring for patient response and tolerance and individual dose adjustments as needed are recommended. Conversely, while no dose adjustments of berotralstat are recommended, monitoring for adverse events may be advisable during concomitant use of berotralstat with drugs that are also P-gp and/or BCRP inhibitors. Patients should be advised to contact their physician if they experience any undue adverse effects from their medications. Patients should seek prompt medical attention if they experience symptoms that could indicate the occurrence of torsade de pointes such as dizziness, lightheadedness, fainting, palpitations, irregular heartbeat, shortness of breath, or syncope. In addition, the prescribing information for concomitant medications should be consulted and dosages adjusted as needed.
Drug and food interactions
ketoconazole food
Applies to: ketoconazole
You should avoid the use of alcohol while being treated with ketoconazole. Ketoconazole may cause liver damage and using it with alcohol or products containing alcohol may increase that risk. In addition, consumption of alcoholic beverages or products containing alcohol during treatment with ketoconazole may trigger a disulfiram-like reaction in some patients, with unpleasant symptoms such as flushing, palpitations, and nausea. Ketoconazole may be taken with or without food. You should avoid consumption of grapefruit, grapefruit juice, or any supplements that contain grapefruit extract during treatment with ketoconazole unless directed otherwise by your doctor. Grapefruit juice may increase the blood levels of ketoconazole. This may increase the risk and/or severity of side effects and liver problems. You should seek immediate medical attention if you develop signs and symptoms of liver damage during treatment with ketoconazole, such as joint pain or swelling, unusual bleeding or bruising, skin rash, itching, loss of appetite, fatigue, nausea, vomiting, dark colored urine, light colored stools, and yellowing of the skin or eyes. Talk to your doctor if you have any questions or concerns. It is important to tell your doctor about all other medications you use, including vitamins and herbs. Do not stop using any medications without first talking to your doctor.
Therapeutic duplication warnings
No warnings were found for your selected drugs.
Therapeutic duplication warnings are only returned when drugs within the same group exceed the recommended therapeutic duplication maximum.
See also
Drug Interaction Classification
Highly clinically significant. Avoid combinations; the risk of the interaction outweighs the benefit. | |
Moderately clinically significant. Usually avoid combinations; use it only under special circumstances. | |
Minimally clinically significant. Minimize risk; assess risk and consider an alternative drug, take steps to circumvent the interaction risk and/or institute a monitoring plan. | |
No interaction information available. |
Further information
Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.
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