Rolapitant (Oral Route)

Rolapitant (Varubi) is a prescription medicine classed as a substance P/neurokinin 1 (NK-1) receptor antagonist and is used to prevent nausea and vomiting in adults undergoing chemotherapy.

Overview

Rolapitant is a preventative care anti-nausea medication. It is used together with other medicines to prevent “delayed phase” nausea and vomiting in patients receiving initial and repeat emetogenic cancer chemotherapy.

Nausea and vomiting are side effects that commonly affect patients undergoing this type of cancer treatment. The effects usually occur between 24 hours and 5 days after a chemotherapy session.

The medicine is normally taken about 1 to 2 hours on day 1 of each chemotherapy treatment cycle, and no more than once in every 14 days. It works by blocking NK-1 receptors which are proteins in the brainstem that trigger nausea and vomiting.

Rolapitant is sold in the US under the brand name Varubi. It is supplied as a tablet by doctor’s prescription only and is not recommended for treating nausea or vomiting that has already occurred.

There are not many known side effects caused by the medicine. Some of them may require medical attention when they occur.

Before using Rolapitant

Before using any medicine, including Rolapitant, patients should consider the benefits and the risks of taking it.

Tell your doctor of all prescription medications you are taking, especially if you are taking Thioridazine or Pimozide. These two medicines may not be safe to use while taking Rolapitant as they may cause adverse interaction.

Also tell your doctor about all over-the-counter medicines (OTCs) you are using or plan to use, vitamins, herbal products, and nutritional supplements. They may have active and inactive ingredients that may interact with this tablet and cause unwanted side effects.

You should disclose any other medical condition you have, especially if you have liver disease. This condition may affect the way the drug works.

Allergies:

You should not use this medication if you are allergic to it. Tell your doctor if you have had an allergic reaction to it. Inactive ingredients may also trigger an allergy.

Pediatrics:

This drug is not indicated for use in children.

Geriatrics:

There is no specific problem found that limits the use of this tablet in treating elderly patients.

Pregnancy:

It is not known whether this medication can harm an unborn baby. Tell your doctor if you are pregnant.

Breastfeeding women:

There is no known clinical proof that the medicine can pass through breast milk and affect a breastfeeding infant.

Because of possible health risks, use and dose of Rolapitant in pregnant or breastfeeding women must be determined by a doctor.

Condition treated:

  • Delayed phase nausea and vomiting

Type of medicine:

  • Substance P/neurokinin 1 (NK-1) receptor antagonist

Side Effects

Side effects tend to vary based on the type of chemotherapy a patient is receiving. In treating delayed phase nausea and vomiting in adults receiving emetogenic cancer chemotherapy, the following common side effects may occur. Call your doctor immediately if you experience any of them.

More commonly occur

  • chills
  • soreness in the throat
  • fever
  • unusual weakness or tiredness
  • pale skin
  • cough
  • shortness of breath
  • anemia (decrease in red blood cells)
  • stool that is black or tarry
  • difficulty or pain while urinating
  • urinary tract infection
  • white spots, sores or ulcers in the mouth
  • unusual bleeding or bruising
  • pain in the side or lower back

Less commonly occur

  • urine that is cloudy or bloody
  • difficulty urinating
  • burning or pain during urination
  • pain in the bladder
  • frequent urge to urinate
  • trouble breathing when energy is exerted

Some side effects that may occur usually go away on their own as your body gets used to the medicine. They generally do not require medical attention. You may not need to call your doctor if you experience any of the following side effects unless they become bothersome or do not go away.

More commonly occur

  • loss of desire to eat
  • feeling dizzy

Less commonly occur

  • pain or discomfort in the stomach
  • sour or acidic stomach
  • belching
  • heartburn
  • hiccups
  • upset stomach
  • indigestion

These are not all the possible side effects. Side effects may not occur all at once and all of them may not occur in one patient. If you experience any unusual symptom that is bothersome or does not go away, tell your doctor or other healthcare professional. You may ask about ways to prevent or reduce side effects.

Side effects may also be reported to the FDA by calling 1-800-FDA-1088.

Dosage

How supplied

Rolapitan (Varubi) is supplied as a single dose blister packet containing two 90 mg oral tablets.

The following is a general dosage guide. Your exact dose will be on the prescription label of your medication. If the strength of your dose and dosing schedule are different, do not change them unless your doctor or pharmacist directs you to. Follow all other directions given by your doctor or healthcare professional.

Taking the tablet

Adults:

Take two 90 milligram (mg) tablets (totaling 180 mg) 1 to 2 hours before starting cancer treatment. Take it only 1 time in each 14-day period.

Children:

Not recommended for children. Use and dose must be determined by a doctor.

Missed dose

This medicine is designed to prevent nausea and vomiting and must be taken well in advance of the start of each chemotherapy session. If you miss your dose, and it is still within 1-2 hours of the chemotherapy, you may take it. Talk to your doctor if you are not sure what to do.

Overdose

Call your local poison control center at 1-800-222-1222 if you overdose on this drug. If the patient collapses or is not breathing, call 911.

Interactions

Telling your doctor or pharmacist about all medications you take is important. This helps them take the necessary precautions to reduce or prevent their interaction with Rolapitant. The following medicines were selected because they have the potential to significantly interact with Rolapitant.

  • Thioridazine

Using Thioridazine during your treatment is not recommended. Your doctor may decide to treat you but may change the dose and how often you use of any of your medications.

Rolapitant is not recommended to be used with the following other medicines, but use may be necessary in some cases. If any of them is prescribed together with your anti-nausea tablet, your doctor may change the dose or how often you use any of your medication.

  • Nebivolol
  • Carbamazepine
  • Fosphenytoin
  • Pimozide
  • Digoxin
  • Rifampin
  • Phenytoin

There may be other drugs not mentioned here which may interact with the anti-nausea medication. You may ask your doctor about them.

Other Interactions

Food, alcohol, and tobacco

Rolapitant can be safely taken with or without food. There is no known risk of interaction. Your doctor or pharmacist may tell you if you should avoid using alcohol or tobacco during treatment.

Other medical problems

The following medical condition may interact with and affect the way Rolopitant is intended to work. Tell your doctor if you have this disease:

  • liver disease (severe)

Your doctor may still decide to treat you with this drug but may use it with caution since it can make the medical condition worse.

Warnings

  • On day 1 of your chemotherapy cycle, remember to take Rolapitant by mouth at least 1 to 2 hours before the start of chemotherapy.
  • Do not take this medicine again until 14 days have passed since you last took it.
  • If you experience severe nausea and vomiting that continue after leaving the hospital or cancer treatment center, you should call your doctor.
  • Do not take it with any other drug or substance known to cause interaction, unless your doctor determines it is best for your health.
  • Do not use it after it expires.
  • Do not share this drug with anyone, even if they have similar symptoms.

Storage

Store the medicine in a closed container at room temperature of about 20-25 degrees Celcius (68-77 degrees Fahrenheit).

Avoid exposure to heat, moisture, and direct light. Keep from freezing. Keep out of the reach of children.

Stop storing the medicine once it expires or is no longer needed. You may ask your healthcare professional or local waste disposal company how to dispose of it.

Summary

Rolapitant (Varubi) is indicated in adults for preventing delayed nausea and vomiting associated with initial and repeat courses of emetogenic cancer chemotherapy. It is approved by the FDA and proven effective when used in combination with other anti-nausea medications not discussed here.

There are few known side effects, even though some may require medical attention. There is also minimal interaction with other drugs or medical problems.

The medicine should be taken at least 1-2 hours before the start of chemotherapy for it to be effective in blocking receptors in the brainstem that trigger nausea and vomiting. If a dose is missed the patient may experience the nausea and vomiting this drug is intended to prevent.

Rolapitant will not relieve nausea or vomiting that has started, and should not be taken more than once in 14 days.

 

Resources
Last Reviewed:
January 29, 2018
Last Updated:
January 27, 2018
Content Source: