To prevent delayed nausea and vomiting associated with initial/repeat courses of emetogenic cancer chemotherapy (to be used with dexamethasone and a 5–HT3 antagonist).
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.
Distribution: Extensively distributed to tissues.
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||unknown|
- Concurrent use of CYP2D6 substrates with a narrow therapeutic index.
Use Cautiously in:
- Concurrent use of other CYP2D6 substrates;
- Severe hepatic impairment (avoid if possible; if unavoidable, monitor carefully);
- OB: Safety not established;
- Lactation: Weigh maternal benefits against risks to the infant;
- Pedi: Safety and effectiveness not established;
- Geri: May be more sensitive to drug effects.
Adverse Reactions/Side Effects
GI: abdominal pain, ↓ appetite, dyspepsia, hiccups, stomatitis
GU: ↓ fertility (females)
Hemat: anemia, neutropenia
Misc: infusion reactions
* CAPITALS indicate life-threatening.
Underline indicate most frequent.
- ↑ levels and risk of serious cardiac toxicity with CYP2D6 substrates with a narrow therapeutic index, including thioridazine and pimozide ; concurrent use contraindicated.
- May ↑ levels and risk of toxicity of other CYP2D6 substrates for an extended period of time (≥28 days).
- May ↑ levels and risk of toxicity of Breast-Cancer-Resistance Protein (BCRP) substrates, including irinotecan, methotrexate, rosuvastatin and topotecan ; dose reduction may be necessary.
- May ↑ levels and risk of toxicity of P-glycoprotein substrates, including digoxin ; avoid concurrent use with P-gp substrates with a narrow therapeutic index.
- Strong CYP3A4 inducers, including rifampin , ↓ levels and effectiveness; avoid concurrent use.
PO (Adults): 180 mg within 2 hr prior to start of chemotherapy.
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 2 hr before starting chemotherapy without regard to food. Due to long action, administer no more frequently than once every 14 days. Given with dexamethasone and a 5-HT3 antagonist.
- Intermittent Infusion: Administer 2 hr before starting chemotherapy. Solution is translucent white and does not need to be shaken; do not inject solutions that are discolored or contain particulate matter. Insert a vented IV set through septum of vial and use immediately; do not dilute. Infuse through a Y-site of 0.9% NaCl. D5W, D5/LR, or LR.
- Rate: Infuse over 30 min.
- 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.
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