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ALIMENTARY TRACT AND METABOLISM › ANTIEMETICS AND ANTINAUSEANTS › ANTIEMETICS AND ANTINAUSEANTS › Other antiemetics
rolapitant
A04AD14
Adult Dosing
- Prevention of chemotherapy-induced nausea and vomiting (CINV): 180 mg (two 90 mg tablets) administered orally approximately 1 hour prior to the start of each chemotherapy cycle
- Administered in combination with a 5-HT3 receptor antagonist and dexamethasone
- Maximum frequency: No more than once every 2 weeks
Pediatric Dosing
- Safety and effectiveness in pediatric patients have not been established
Indications
- Prevention of delayed nausea and vomiting associated with initial and repeat courses of emetogenic cancer chemotherapy, including highly emetogenic chemotherapy
Mechanism of Action
- Selective and long-acting antagonist of human substance P/neurokinin 1 (NK1) receptors
- Crosses the blood-brain barrier and occupies brain NK1 receptors, preventing substance P-mediated emetic signaling
Contraindications
- Known hypersensitivity to rolapitant or any components of the product
- Concomitant use with thioridazine (due to risk of QTc prolongation and severe arrhythmias)
Adverse Reactions
- Hiccups
- Neutropenia
- Decreased appetite
- Dizziness
Drug Interactions
- Inhibits breast cancer resistance protein (BCRP); may increase exposure of BCRP substrates (e.g., methotrexate, rosuvastatin, topotecan)
- Substrate of CYP3A4; strong CYP3A4 inducers (e.g., rifampin) significantly decrease rolapitant plasma concentrations
- Thioridazine: Concomitant use is contraindicated due to potential for CYP2D6 inhibition leading to increased thioridazine concentrations and QTc prolongation
Curated Content: Needs Vetting Before Put to Clinical Use