Trade Name(s)

  • Varubi

Ther. Class.

Pharm. Class.
neurokinin antagonists


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.

Therapeutic Effect(s):

  • 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)

POwithin 30 min4 hrunknown


Contraindicated in:

  • 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

CV: dizziness

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.

Potential Diagnoses


  • 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.

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.

rolapitant is a sample topic from the Davis's Drug Guide.

To view other topics, please or .

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. .