aprepitant: prescribing and clinical use
Focused clinical detail for use alongside current product information, local policy and patient-specific assessment.
aprepitant: clinical details
Prescribing considerations
- Use only as part of an appropriate combination antiemetic strategy for the licensed chemotherapy context.
- Complete a thorough interaction review covering CYP3A4 and CYP2C9 substrates, inhibitors and inducers.
- Use caution in moderate hepatic impairment; evidence is absent in severe hepatic impairment.
- Account for sucrose in capsules and sucrose plus lactose in the selected oral suspension.
- Hormonal contraception may be less effective during exposure and afterwards; counsel about non-hormonal backup.
Contraindications and cautions
- Hypersensitivity to aprepitant or formulation excipients.
- Concurrent pimozide, terfenadine, astemizole or cisapride.
- Relevant rare hereditary sugar-intolerance disorders, according to the excipients in the selected formulation.
Monitoring
- INR in patients receiving chronic warfarin, during and after aprepitant exposure.
- Clinical or concentration monitoring for narrow-therapeutic-range CYP3A4 substrates where applicable.
- Liver status where hepatic disease or abnormal liver tests are clinically relevant.
- Suspected serious or unusual adverse reactions can be reported through the MHRA Yellow Card Scheme.
Clinical pharmacology
Aprepitant is a selective substance P/neurokinin-1 receptor antagonist. It is highly protein-bound, extensively metabolised mainly through CYP3A4 and has non-linear pharmacokinetics. During treatment it moderately inhibits CYP3A4; afterwards it transiently induces CYP2C9, CYP3A4 and glucuronidation.
Formulation and product differences
- Hard capsules are swallowed whole and are licensed by the selected capsule product for adults and adolescents from 12 years.
- The selected powder forms an oral suspension intended for children aged 6 months to under 12 years who weigh at least 6 kg; preparation and measurement are restricted to healthcare professionals.
- The selected suspension contains sucrose and lactose, whereas the selected capsule contains sucrose.
- The selected oral-suspension product is currently listed as discontinued on eMC, although its product information remains available.
aprepitant preparations and strengths
Capsule
Route: Oral
Strengths: 80 mg, 125 mg, 125 mg + 80 mg
aprepitant interactions
Aprepitant both affects and is affected by liver enzymes, so the complete prescription, non-prescription and herbal medicine list should be checked.
Pimozide, terfenadine, astemizole or cisapride
Co-administration is contraindicated because aprepitant may greatly increase concentrations and cause serious reactions.
Dexamethasone or methylprednisolone
Aprepitant increases corticosteroid exposure, so the oncology regimen must account for the interaction.
Warfarin
The anticoagulant effect may change after aprepitant; INR requires close monitoring during and after treatment.
Sources
These sources were used to prepare and review this medicine page.
Prepared and reviewed by the iatroX editorial team.