With other antiemetic agents in adults to prevent delayed nausea and vomiting associated with initial/repeat courses of emetogenic cancer chemotherapy.
Acts as a selective antagonist at substance P/neurokinin 1 (NK1 ) receptors in the brain.
Decreased nausea and vomiting associated with chemotherapy.
Augments the antiemetic effects of dexamethasone and 5-HT3 antagonists.
Absorption: Well absorbed following oral administration.
Protein Binding: 99.8%
Metabolism and Excretion: Mostly metabolized, primarily by CYP3A4; one metabolite, C4–pyrrolidine-hydroxylated rolapitant (M19) has antiemetic activity. Excretion is mainly via hepato/biliary elimination. 14% excreted in urine (8% as metabolites), 73% in feces (38% as unchanged drug).
Half-life: Rolapitant– 7 days; M19– 7 days.
TIME/ACTION PROFILE (blood levels)
within 30 min
Concurrent use of thioridazine or pimozide.
Use Cautiously in:
Concurrent use of other substrates of CYP2D6 with narrow therapeutic indeces (avoid concurrent use if possible, if necessary monitor carefully);
Severe hepatic impairment (avoid if possible, if unavoidable monitor carefully);
Severe renal impairment (effect on pharmacokinetics not known;
Geri: Elderly patients may be more sensitive to drug effects;
OB: Effects in pregnancy are unknown;
Lactation: Weigh maternal benefits against risks to the infant;
Pedi: Safe and effective use in children has not been established.
Adverse Reactions/Side Effects
CV: dizziness (↑ with anthracycline/cyclophosphamide regimens)
GI: ↓ appetite (↑ with anthracycline/cyclophosphamide regimens), hiccups (↑ with cisplatin regimens)
* CAPITALS indicate life-threatening. Underline indicate most frequent.
↑ levels and risk of serious cardiac toxicity with thioridazine and pimozide; thioridazine is contraindicated, pimozide should be avoided.
↑ levels effects and risk of toxicity from irinotecan, methotrexate, rosuvastatin and topotecan, may have a similar effect on other drugs that are handled by Breast-Cancer-Resistance protein (BCRP) transporter; dose reduction may be necessary.
↑ levels, effects and risk of toxicity from digoxin and other drugs that are metabolized by P-glycoprotein (P-gp) transporter, especially those with narrow therapeutic indeces, careful monitoring is recommended.
Strong CYP3A4 inducers including rifampin ↓ blood levels and effectiveness.
PO: (Adults) 180 mg 1–2 hr prior to start of chemotherapy; with dexamethasone and a 5-HT3 antagonist.
Tablets: 90 mg
Assess nausea, vomiting, appetite, bowel sounds, and abdominal pain prior to and following administration.
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