Apalutamide
Severe
Database
Drug interaction classified as: metabolism
Source: DDInter
Drug reference
Rolapitant
Antiemetic
AntiemeticATC A04AD14
CDSCO approvedSchedule HATC A04AD14
EXCRETION
—
not curated
INTERACTIONS
12 major
SEVERE in our sources
PREGNANCY
Nausea in the first trimester of pregnancy is generally mild
FDA category + note
Top interactionssee all 12 →
- ApalutamideSevereDatabaseDDInter
- BerotralstatSevereDatabaseDDInter
- BetrixabanSevereDatabaseDDInter
- CarbamazepineSevereDatabaseDDInter
Mechanism
Neurokinin 1 (NK1)-receptor antagonists have antiemetic properties that are mediated through central blockade in the area postrema. Rolapitant is a highly selective NK1-receptor antagonist that crosses the blood-brain barrier and occupies brain NK1 receptors. It has no affinity for serotonin, dopamine, or corticosteroid receptors.
Indications
Prevention of delayed nausea and vomiting associated with highly and moderately emetogenic chemotherapy.Used in combination with 5-HT3-receptor antagonists and corticosteroids for the prevention of acute and delayed nausea and vomiting from highly emetogenic chemotherapeutic regimens.antiemeticPrevention of chemotherapy-induced delayed emesis
Dosing
- Adult
- ▶ BY RECTUM ▶ Antiemetics should be given to prevent motion sickness rather than after nausea or vomiting develop. The most effective drug for the prevention of motion sickness is hyoscine hydrobromide p. 458. The sedating antihistamines are slightly less effective against motion sickness, but are generally better tolerated than hyoscine.…
Pharmacokinetics
Peak effect
4 h
Half-life
180 hours
Metabolism
Metabolized by the liver, primarily by the CYP3A4 pathway
Excretion
Mainly via hepatic/biliary route
Contraindications
- Patients receiving drugs that are CYP2D6 substrates (e.g., thioridazine, pimozide)
Side effects
Common
NeutropeniaHiccupsDecreased appetiteDizziness
Serious
- QT prolongation and torsades de pointes (with CYP2D6 substrates like thioridazine or pimozide due to increased plasma concentrations)
Pregnancy & lactation
Pregnancy
Nausea in the first trimester of pregnancy is generally mild
Drug interactions
Berotralstat
Severe
Database
Drug interaction classified as: absorption
Source: DDInter
Betrixaban
Severe
Database
Drug interaction classified as: others
Source: DDInter
Carbamazepine
Severe
Database
Drug interaction classified as: metabolism
Source: DDInter
Colchicine
Severe
Database
Drug interaction classified as: excretion
Source: DDInter
Edoxaban
Severe
Database
Clinical effect not specified
Source: DDInter
Eliglustat
Severe
Database
Clinical effect not specified
Source: DDInter
Enzalutamide
Severe
Database
Drug interaction classified as: metabolism
Source: DDInter
Fosphenytoin
Severe
Database
Clinical effect not specified
Source: DDInter
Lumacaftor
Severe
Database
Clinical effect not specified
Source: DDInter
Mitotane
Severe
Database
Clinical effect not specified
Source: DDInter
Oliceridine
Severe
Database
Clinical effect not specified
Source: DDInter
Related guidelines
Other Antiemetic drugs
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Sources: Goodman & Gilman 14e, BNF·Verified: 2026-05-13 · House clinical team