Drug Interactions between efavirenz and rolapitant
This report displays the potential drug interactions for the following 2 drugs:
- efavirenz
- rolapitant
Interactions between your drugs
efavirenz rolapitant
Applies to: efavirenz and rolapitant
MONITOR: Coadministration with moderate inducers of CYP450 3A4 may decrease the plasma concentrations of rolapitant, which is primarily metabolized by the isoenzyme. When the potent CYP450 3A4 inducer rifampin was administered at 600 mg once daily for 7 days before and 7 days after a single 180 mg dose of rolapitant, mean rolapitant peak plasma concentration (Cmax) and systemic exposure decreased by 30% and 85%, respectively, compared to administration of rolapitant alone. Mean half-life of rolapitant decreased from 176 hours to 41 hours with rifampin. No data are available for other, less potent CYP450 3A4 inducers.
MANAGEMENT: The potential for diminished pharmacologic effects of rolapitant should be considered during coadministration with CYP450 3A4 inducers. Alternative treatments may be required if an interaction is suspected.
References
- Cerner Multum, Inc. "UK Summary of Product Characteristics." O 0
- "Product Information. Varubi (rolapitant)." Tesaro Inc. (2015):
Drug and food interactions
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.
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
- "Product Information. Sustiva (efavirenz)." DuPont Pharmaceuticals PROD (2001):
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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