General

Pronunciation:
rol-ap-i-tant


Trade Name(s)

  • Varubi

Ther. Class.
antiemetics

Pharm. Class.
neurokinin antagonists

Indications

With other antiemetic agents in adults to prevent delayed nausea and vomiting associated with initial/repeat courses of emetogenic cancer chemotherapy.

Action

Acts as a selective antagonist at substance P/neurokinin 1 (NK1 ) receptors in the brain.

Therapeutic Effect(s):

  • Decreased nausea and vomiting associated with chemotherapy.
  • Augments the antiemetic effects of dexamethasone and 5-HT3 antagonists.

Pharmacokinetics

Absorption: Well absorbed following oral administration.

Distribution: Unk

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)

ROUTEONSETPEAKDURATION
POwithin 30 min4 hr7 days

Contraindication/Precautions

Contraindicated in:

  • 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)

Hemat: neutropenia

* CAPITALS indicate life-threatening.
Underline indicate most frequent.

Interactions

Drug-Drug

  • ↑ 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.

Route/Dosage

PO: (Adults) 180 mg 1–2 hr prior to start of chemotherapy; with dexamethasone and a 5-HT3 antagonist.

Availability

Tablets: 90 mg

Assessment

  • Assess nausea, vomiting, appetite, bowel sounds, and abdominal pain prior to and following administration.

Lab Test Considerations:

May cause ↓ WBC.

Potential Diagnoses

Implementation

  • 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.

Patient/Family Teaching

  • 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.

Evaluation/Desired Outcomes

Decreased delayed nausea and vomiting associated with emetogenic chemotherapy.

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Citation

* When formatting your citation, note that all book, journal, and database titles should be italicized* Article titles in AMA citation format should be in sentence-case
TY - ELEC T1 - rolapitant ID - 110374 A1 - Quiring,Courtney, AU - Sanoski,Cynthia A, AU - Vallerand,April Hazard, BT - Davis's Drug Guide UR - https://peds.unboundmedicine.com/pedscentral/view/Davis-Drug-Guide/110374/all/rolapitant PB - F.A. Davis Company ET - 16 DB - Pediatrics Central DP - Unbound Medicine ER -