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Methylnaltrexone Injection

What is this medication?

METHYLNALTREXONE (METH il nal TREX one) treats constipation caused by opioids. It works by blocking the effect of opioids in your intestine, which helps the muscles in your intestine move stool. This helps produce a bowel movement. It belongs to a group of medications called opioid blockers.

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This medicine may be used for other purposes; ask your health care provider or pharmacist if you have questions.

COMMON BRAND NAME(S): Relistor

What should I tell my care team before I take this medication?

They need to know if you have any of these conditions:

  • Kidney disease
  • Liver disease
  • Stomach or intestine problems, including a blockage or ulcer
  • An unusual or allergic reaction to methylnaltrexone, other medications, foods, dyes, or preservatives
  • Pregnant or trying to get pregnant
  • Breast-feeding

How should I use this medication?

This medication is for injection under the skin. It is usually given in a hospital or clinic setting. If you get this medication at home, you will be taught how to prepare and give it. Use exactly as directed. Do not take your medication more often than directed.

It is important that you put your used needles and syringes in a special sharps container. Do not put them in a trash can. If you do not have a sharps container, call your pharmacist or care team to get one.

A special MedGuide will be given to you by the pharmacist with each prescription and refill. Be sure to read this information carefully each time.

Talk to your care team about the use of this medication in children. Special care may be needed.

Overdosage: If you think you have taken too much of this medicine contact a poison control center or emergency room at once.

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NOTE: This medicine is only for you. Do not share this medicine with others.

What if I miss a dose?

This does not apply; this medication is not for regular use.

What may interact with this medication?

  • Alvimopan
  • Naloxone
  • Naltrexone

This list may not describe all possible interactions. Give your health care provider a list of all the medicines, herbs, non-prescription drugs, or dietary supplements you use. Also tell them if you smoke, drink alcohol, or use illegal drugs. Some items may interact with your medicine.

What should I watch for while using this medication?

Be close to a bathroom after you get this medication. You may need to use the toilet soon after getting this medication.

Your condition will be monitored carefully while you are receiving this medication. Tell your care team if your symptoms do not start to get better or if they get worse.

You may get drowsy or dizzy. Do not drive, use machinery, or do anything that needs mental alertness until you know how this medication affects you. Do not stand or sit up quickly, especially if you are an older patient. This reduces the risk of dizzy or fainting spells. Alcohol may interfere with the effect of this medication. Avoid alcoholic drinks.

What side effects may I notice from receiving this medication?

Side effects that you should report to your care team as soon as possible:

  • Allergic reactions—skin rash, itching, hives, swelling of the face, lips, tongue, or throat
  • Stomach pain that is severe, does not go away, or gets worse

Side effects that usually do not require medical attention (report to your care team if they continue or are bothersome):

  • Chills
  • Diarrhea
  • Excessive sweating
  • Headache
  • Nausea
  • Stomach pain

This list may not describe all possible side effects. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Where should I keep my medication?

Keep out of the reach of children and pets.

Store at room temperature between 20 and 25 degrees C (68 and 77 degrees F). Do not freeze and protect from light. Throw away any unused medication after the expiration date.

NOTE: This sheet is a summary. It may not cover all possible information. If you have questions about this medicine, talk to your doctor, pharmacist, or health care provider.

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Note: Introduction and Additional Common Questions written and medically approved by Cleveland Clinic professionals.

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