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)
|PO||within 30 min||4 hr||7 days|
- 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.
Lab Test Considerations:
May cause ↓ WBC.
- PO: Administer 1–2 hr before chemotherapy without regard to food. Due to long action, administered no more frequently than onceevery 14 days. Given with dexamethasone and a 5-HT3 antagonist.
- Instruct patient to take rolapitant as directed. Direct patient to read the Patient Package Insert before starting therapy and each time Rx renewed in case of changes.
- Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and consult health care professional before taking any new medications.
- Advise patient and family to use general measures to decrease nausea (begin with sips of liquids and small, nongreasy meals; provide oral hygiene; remove noxious stimuli from environment).
- Advise patient to notify health care professional if pregnancy is planned or suspected or if breast feeding.
Decreased delayed nausea and vomiting associated with emetogenic chemotherapy.
Anesthesia Central is an all-in-one web and mobile solution for treating patients before, during, and after surgery. This collection of drug, procedures and test information is derived from Davis’s Drug, MGH Clinical Anesthesia Procedures, Pocket Guide to Diagnostic Tests, and MEDLINE Journals. Learn more.