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What is methylnaltrexone?

Methylnaltrexone is a special narcotic drug that blocks certain effects of other narcotic medicines.

Methylnaltrexone reduces constipation caused by narcotic medications that are often used to treat pain in people with terminal illness.

Methylnaltrexone works by preventing this side effect without reducing the pain-relieving effects of the narcotic.

Methylnaltrexone is usually given after laxatives have been tried without successful treatment of constipation.

Methylnaltrexone may also be used for purposes other than those listed in this medication guide.

What is the most important information I should know about methylnaltrexone?

You should not use this medication if you are allergic to methylnaltrexone, or if you have a blockage in your stomach or intestines.

Before you use methylnaltrexone, tell your doctor if you have severe or ongoing diarrhea.

Do not draw your methylnaltrexone dose into a syringe until you are ready to give yourself an injection. After loading a syringe, if you cannot give the injection right away keep it at room temperature and use it within 24 hours.

The pain-relieving effects of any narcotic pain medications you use will be blocked if you use them during your treatment with methylnaltrexone. Harmful side effects could also occur. Before receiving methylnaltrexone, tell your doctor if you use any narcotic medication.

What should I discuss with my health care provider before receiving methylnaltrexone?

You should not use this medication if you are allergic to methylnaltrexone, or if you have a blockage in your stomach or intestines.

If you have certain conditions, you may need a dose adjustment or special tests to safely use this medication. Before you use methylnaltrexone, tell your doctor if you have severe or ongoing diarrhea.

How is methylnaltrexone used?

Methylnaltrexone is given as a shot under the skin of your upper arm, stomach, or thigh. Your doctor, nurse, or other healthcare provider will give you this injection. You may be shown how to inject your medicine at home. Do not self-inject this medicine if you do not fully understand how to give the injection and properly dispose of used needles and syringes.

This medication is usually given once every other day, but not more often than once every 24 hours.

Methylnaltrexone can produce a bowel movement within 30 minutes after injection.

Use each disposable needle only one time. Throw away used needles in a puncture-proof container (ask your pharmacist where you can get one and how to dispose of it). Keep this container out of the reach of children and pets.

A single-use vial (bottle) of methylnaltrexone is for one injection only. Throw the used vial away after one use, even if there is still medicine left in it.

Methylnaltrexone should look clear or slightly yellow in color. Do not use the medication if it has changed colors or has any particles in it. Call your doctor for a new prescription.

What happens if I miss a dose?

Use the missed dose as soon as you remember. If it is almost time for your next dose, wait until then to use the medicine and skip the missed dose. Do not use extra medicine to make up the missed dose.

Do not use this medication more than once in a 24-hour period.

What happens if I overdose?

Seek emergency medical attention if you think you have received too much of this medicine.

Overdose symptoms may include extreme dizziness, or feeling like you might pass out.

What should I avoid while using methylnaltrexone?

Methylnaltrexone can cause side effects that may impair your thinking or reactions. Be careful if you drive or do anything that requires you to be awake and alert. Do not use any other laxatives that your doctor has not prescribed.

Methylnaltrexone side effects

Get emergency medical help if you have any of these signs of an allergic reaction: hives; difficulty breathing; swelling of your face, lips, tongue, or throat. Call your doctor at once if you have severe or ongoing diarrhea, stomach pain that will not go away, or nausea or vomiting that are new or worsening symptoms.

Less serious side effects may include:

• stomach pain, gas;

• mild nausea; or

• mild diarrhea.

This is not a complete list of side effects and others may occur. Tell your doctor about any unusual or bothersome side effect. You may report side effects to FDA at 1-800-FDA-1088.

What other drugs will affect methylnaltrexone?

The pain-relieving effects of any narcotic pain medications you use will be blocked if you use them during your treatment with methylnaltrexone. Harmful side effects could also occur.

Before receiving methylnaltrexone, tell your doctor if you use any narcotic medication, such as:

• buprenorphine (Buprenex, Subutex);

• butorphanol (Stadol);

• codeine (Tylenol with codeine);

• hydrocodone (Lortab, Vicodin);

• dezocine (Dalgan);

• hydromorphone (Dilaudid);

• levorphanol (Levo-Dromoran);

• meperidine (Demerol);

• methadone (Dolophine, Methadose);

• morphine (Kadian, MS Contin, Roxanol);

• nalbuphine (Nubain);

• nalmefene (Revex);

• naloxone (Narcan);

• oxycodone (OxyContin, Roxicodone, Percocet);

• oxymorphone (Numorphan); or

• propoxyphene (Darvon, Darvocet).

This list is not complete and there may be other drugs that can interact with methylnaltrexone. Tell your doctor about all the prescription and over-the-counter medications you use. This includes vitamins, minerals, herbal products, and drugs prescribed by other doctors. Do not start using a new medication without telling your doctor.

Where can I get more information?

• Your doctor or pharmacist can provide more information about methylnaltrexone injection.

• Remember, keep this and all other medicines out of the reach of children, never share your medicines with others, and use this medication only for the indication prescribed.
• Every effort has been made to ensure that the information provided by Cerner Multum, Inc. ('Multum') is accurate, up-to-date, and complete, but no guarantee is made to that effect. Drug information contained herein may be time sensitive. Multum information has been compiled for use by healthcare practitioners and consumers in the United States and therefore Multum does not warrant that uses outside of the United States are appropriate, unless specifically indicated otherwise. Multum's drug information does not endorse drugs, diagnose patients or recommend therapy. Multum's drug information is an informational resource designed to assist licensed healthcare practitioners in caring for their patients and/or to serve consumers viewing this service as a supplement to, and not a substitute for, the expertise, skill, knowledge and judgment of healthcare practitioners. The absence of a warning for a given drug or drug combination in no way should be construed to indicate that the drug or drug combination is safe, effective or appropriate for any given patient. Multum does not assume any responsibility for any aspect of healthcare administered with the aid of information Multum provides. The information contained herein is not intended to cover all possible uses, directions, precautions, warnings, drug interactions, allergic reactions, or adverse effects. If you have questions about the drugs you are taking, check with your doctor, nurse or pharmacist.