Uses

What is Relistor used for?

Relistor (methylnaltrexone) is commonly used to treat constipation in people who regularly take pain medicines called opioids.

Relistor may also be used for other conditions as determined by your healthcare provider.

How does Relistor work (mechanism of action)?

Relistor works by blocking certain receptors in your intestines so that opioid pain medicines can not attach to those spots in your gut. Normally, opioids attach to certain receptors in your digestive system which causes your intestines to slow down and make it hard to have a bowel movement. By blocking opioid receptors in your intestines, you can have more normal bowel movements without affecting pain relief in other parts of your body. 

How is Relistor supplied (dosage forms)?

Brands and other names

  • Relistor

Dosage forms and strengths

  • 8 mg/0.4 mL pre-filled syringe
  • 12 mg/0.6 mL pre-filled syringe or single-dose vial
  • 150 mg oral tablets

How should I store Relistor?

Oral Tablet. Relistor tablets should be stored at room temperature, between 68 F to 77 F (20 C to 25 C). It can be exposed to temperatures between 59 F to 86 F (15 C to 30 C) for shorter periods of time, such as when transporting it. Store in a cool, dry place. Keep the desiccants inside the bottle to help keep the medicine dry.

Injection. Relistor vials and pre-filled syringes should be stored at room temperature, between 68 F to 77 F (20 C to 25 C). It can be exposed to temperatures between 59 F to 86 F (15 C to 30 C) for shorter periods of time, such as when transporting it. Do not freeze. Store in a place that is away from light. 

Side Effects

What are the most common side effects of Relistor?

The most common side effects of Relistor are listed below. Tell your healthcare provider if you have any of these side effects that bother you.

  • Stomach pain
  • Diarrhea (see below)
  • Headache
  • Swelling or a feeling of fullness or pressure in your stomach
  • Vomiting or nausea
  • Sweating or chills
  • Anxiety
  • Muscle spasms
  • Runny nose
  • Hot flashes (injectable)
  • Gas (injectable)
  • Tremor (injectable)
  • Dizziness (injectable)

There may be other side effects of Relistor that are not listed here. Contact your healthcare provider if you think you are having a side effect of a medicine. In the U.S., you can report side effects to the FDA at www.fda.gov/medwatch or by calling 800-FDA-1088. In Canada, you can report side effects to Health Canada at www.health.gc.ca/medeffect or by calling 866-234-2345.

What are the serious side effects of Relistor?

While less common, the most serious side effects of Relistor are described below, along with what to do if they happen.

Severe Allergic Reactions. Relistor may cause allergic reactions, which can be serious. Stop using Relistor and get help right away if you have any of the following symptoms of a serious allergic reaction.

  • Breathing problems or wheezing
  • Racing heart
  • Fever or general ill feeling
  • Swollen lymph nodes
  • Swelling of the face, lips, mouth, tongue, or throat
  • Trouble swallowing or throat tightness
  • Itching, skin rash, or pale red bumps on the skin called hives
  • Nausea or vomiting
  • Dizziness, feeling lightheaded, or fainting
  • Stomach cramps'
  • Joint pain

Stomach or Intestinal Tears (Perforation). Relistor can increase your risk for developing a hole in the wall of your stomach or intestines. The risk is higher if you have conditions that impact the walls of your digestive tract, such as peptic ulcer diseasediverticulitis, cancer of intestines, Crohn’s disease, and certain other conditions. Stop taking Relistor and get emergency help right away if you have unusual severe, persistent or worsening stomach pain. 

Diarrhea. Some people taking Relistor have severe diarrhea. Stop taking Relistor and call your healthcare provider right away if you have diarrhea that is severe or does not go away.

Opioid Withdrawal. Relistor may cause you to go into withdrawal from your opioid medicine. Tell your healthcare provider right away if you have any of the following symptoms.

  • Sweating or chills
  • Diarrhea
  • Stomach pain
  • Anxiety 
  • Yawning

Warnings & Precautions

Who should not use Relistor?

Allergies to Ingredients. People who are allergic to any of the following should not use Relistor.

  • Relistor
  • Methylnaltrexone
  • Any of the ingredients in the specific product dispensed

Your pharmacist can tell you all of the ingredients in Relistor.

Gut Blockage. Relistor should not be used if you have a blockage of your gut (bowel obstruction) or a history of one. Relistor can increase the risk of developing a tear (perforation) that can lead to death in people with a bowel blockage.

What should I know about Relistor before using it?

Do not use Relistor unless it has been prescribed to you by a healthcare provider. Use it as prescribed.

Do not share Relistor with other people, even if they have the same condition as you. It may harm them.

Keep Relistor out of the reach of children.

Since Relistor can cause diarrhea, stay close to the toilet after you take the medicine.

Tell your healthcare provider if you stop taking your opioid pain medicine. You will need to also stop Relistor.

Most patients should stop taking all laxatives before starting Relistor. This is because you may  not be able to tell how well Relistor is working if you are taking a laxative when you start the medicine. Talk to your healthcare provider to see if you should stop taking laxatives before starting Relistor.

If you use Relistor injection, this medicine is injected under the skin. Make sure that you or a caregiver understand how to properly use Relistor. If you have any questions, talk to your healthcare provider.

If you are giving yourself Relistor injections, inject the medicine into your thigh or abdomen. Do not inject Reslitor into your upper arm. This should only be done by your healthcare professional or caregiver. 

Use a different injection site each time you use Relistor. Do not give the injection into tender areas, bruises, scars, red skin, or stretch marks.

If you draw your dose of Relistor from a vial into a syringe and you do not use the medicine right away, keep the syringe at room temperature for up to 24 hours. 

Inspect the liquid in the pre-filled syringe or vial before injecting Relistor. The solution should be colorless or slightly yellow. Do not use Relistor if you see discoloration, cloudiness, or floating particles in the solution.

Throw away Relistor after you give yourself a dose, even if there is medicine left in the pre-filled syringe or vial. Throw away Relistor in a sharps container or in a household container made of heavy-duty plastic that is able to close tightly and is puncture- and leak-resistant. 

People who are 65 and older can be at greater risk for some side effects from Relistor. Talk to your healthcare provider about your risks if you are in this age group.

What should I tell my healthcare provider before using Relistor?

Tell your healthcare provider about all of your health conditions and any prescription or over-the-counter (OTC) medicines, vitamins/minerals, herbal products, and other supplements you are using. This will help them determine if Relistor is right for you.

In particular, make sure that you discuss any of the following.

Current and Past Health Conditions. Tell your healthcare provider if you have any of the following.

  • Kidney or liver problems
  • Stomach or intestinal problems 
  • Stomach ulcer
  • Crohn’s disease
  • Inflammation in parts of the large intestine (diverticulitis)
  • Stomach or intestinal cancer

Other Medicines and Supplements. Relistor may interact with other medicines and supplements. Before taking Relistor, tell your healthcare provider about any prescription or over-the-counter (OTC) medicines, vitamins/minerals, herbal products, and other supplements you are using. See the Interactions section for more details.

Pregnancy. Relistor may cause harm to your unborn baby. If you take Relistor during pregnancy, your baby may have opioid withdrawal symptoms. Tell your healthcare provider if you are or plan to become pregnant.

Breastfeeding. It is not known if Relistor passes into breast milk. Tell your healthcare provider if you are breastfeeding or plan to breastfeed. Your healthcare provider will advise you if you should stop breastfeeding or stop Relistor.

How can I get more information about Relistor?

For more information about Relistor, you can visit the manufacturer’s website at www.relistor.com or call them at 800-321-4576.

Interactions

Does Relistor interact with foods or drinks?

Relistor tablets should be taken on an empty stomach. Take Relistor tablets at least 30 minutes before your first meal of the day.

It is unknown if drinking alcohol will affect Relistor.

Does Relistor interact with other medicines (drug interactions)?

Relistor may interact with certain medicines. Always tell your healthcare provider about any prescription or over-the-counter (OTC) medicines, vitamins/minerals, herbal products, and other supplements you are using.

In particular, make sure that you discuss if you use an opioid antagonist, such as naloxone, which is a medicine used to reverse the effects of an opioid pain medicine.

This may not be a complete list of medicines that can interact with Relistor. Always check with your healthcare provider.

Does Relistor (methylnaltrexone) interact with other drugs you are taking?
Enter your medication into the WebMD interaction checker

Overdose/Missed Dose

What should I do if I accidentally use too much Relistor?

If you or someone else has used too much Relistor, get medical help right away, call 911, or contact a Poison Control center at 800-222-1222.

What should I do if I miss a dose of Relistor?

If you miss a dose, take it as soon as you remember, as long as it is 30 minutes before a meal. If it is almost time for your next dose, skip the missed dose and only take the next dose. Do not take double or extra doses.