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Drug Interactions between efavirenz and Nubeqa

This report displays the potential drug interactions for the following 2 drugs:

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Interactions between your drugs

Moderate

efavirenz darolutamide

Applies to: efavirenz and Nubeqa (darolutamide)

MONITOR: Coadministration with inducers of CYP450 3A4 and/or P-glycoprotein (P-gp) may decrease the plasma concentrations of darolutamide, which is a substrate of both the isoenzyme and the efflux transporter. When darolutamide was coadministered with rifampin, a dual P-gp and potent CYP450 3A4 inducer, mean darolutamide peak plasma concentration (Cmax) and systemic exposure (AUC) decreased by 52% and 72%, respectively, compared to administration of darolutamide alone. The decrease in darolutamide exposure by dual P-gp and moderate CYP450 3A4 inducers is expected to be in the range of 36% to 58% according to the prescribing information. The interaction has not been studied with lone inducers of CYP450 3A4 or P-gp. In addition, when two or more medications with similar adverse effect profiles are given concurrently, the likelihood of experiencing these adverse reactions may be increased. For example, coadministration with other agents that can prolong the QT interval (e.g., apalutamide, encorafenib, enzalutamide) may result in additive effects and an increased risk of ventricular arrhythmias like torsade de pointes.

MANAGEMENT: The potential for diminished pharmacologic effects of darolutamide should be considered during coadministration with CYP450 3A4 and/or P-gp inducers. Alternative treatments may be required if an interaction is suspected. If the CYP450 3A4 inducer also carries a risk of prolonging the QT interval, then obtaining more frequent electrocardiograms (ECGs) to monitor the QT interval may be advisable. Patients should be counseled to seek immediate medical attention if they experience symptoms that could indicate the occurrence of torsade de pointes such as dizziness, lightheadedness, syncope, palpitations, irregular heartbeat, and/or shortness of breath. The prescribing information for the concomitant CYP450 3A4 inducers should be consulted for specific recommendations.

References (1)
  1. (2019) "Product Information. Nubeqa (darolutamide)." Bayer HealthCare Pharmaceuticals Inc.

Drug and food interactions

Moderate

efavirenz food

Applies to: efavirenz

ADJUST DOSING INTERVAL: Administration with food increases the plasma concentrations of efavirenz and may increase the frequency of adverse reactions. According to the product labeling, administration of efavirenz capsules (600 mg single dose) with a high-fat/high-caloric meal (894 kcal, 54 g fat, 54% calories from fat) or a reduced-fat/normal-caloric meal (440 kcal, 2 g fat, 4% calories from fat) was associated with mean increases of 39% and 51% in efavirenz peak plasma concentration (Cmax) and 22% and 17% in systemic exposure (AUC), respectively, compared to administration under fasted conditions. For efavirenz tablets, administration of a single 600 mg dose with a high-fat/high-caloric meal (approximately 1000 kcal, 500-600 kcal from fat) resulted in a 79% increase in mean Cmax and a 28% increase in mean AUC of efavirenz relative to administration under fasted conditions.

GENERALLY AVOID: Alcohol may potentiate the central nervous system (CNS) depressant effects of efavirenz. Concomitant use may result in additive CNS depression and impairment of judgment, thinking, and psychomotor skills. In more severe cases, hypotension, respiratory depression, profound sedation, coma, or even death may occur.

MANAGEMENT: Efavirenz should be taken on an empty stomach, preferably at bedtime. Dosing at bedtime may improve the tolerability of nervous system symptoms such as dizziness, insomnia, impaired concentration, somnolence, abnormal dreams and hallucinations, although they often resolve on their own after the first 2 to 4 weeks of therapy . Patients should be advised of the potential for additive central nervous system effects when efavirenz is used concomitantly with alcohol or psychoactive drugs, and to avoid driving or operating hazardous machinery until they know how the medication affects them.

References (4)
  1. (2001) "Product Information. Sustiva (efavirenz)." DuPont Pharmaceuticals
  2. (2023) "Product Information. Sustiva (efavirenz)." Bristol-Myers Squibb, SUPPL-59/47
  3. (2024) "Product Information. Stocrin (efavirenz)." Merck Sharp & Dohme (Australia) Pty Ltd
  4. (2024) "Product Information. Efavirenz (efavirenz)." Viatris UK Healthcare Ltd
Moderate

darolutamide food

Applies to: Nubeqa (darolutamide)

ADJUST DOSING INTERVAL: Food enhances the oral absorption of darolutamide. According to the prescribing information, bioavailability of darolutamide increased by 2.0 to 2.5-fold when administered with food. A similar increase in exposure was observed for the active metabolite keto-darolutamide.

MANAGEMENT: Darolutamide should be administered with food.

References (1)
  1. (2019) "Product Information. Nubeqa (darolutamide)." Bayer HealthCare Pharmaceuticals Inc.

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.


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Drug Interaction Classification

These classifications are only a guideline. The relevance of a particular drug interaction to a specific individual is difficult to determine. Always consult your healthcare provider before starting or stopping any medication.
Major Highly clinically significant. Avoid combinations; the risk of the interaction outweighs the benefit.
Moderate Moderately clinically significant. Usually avoid combinations; use it only under special circumstances.
Minor 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.
Unknown No interaction information available.

Further information

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.