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Methadone

(meth-uh-dohn)

Trade/other name(s): Dolophine, Methadose

Why would this drug be used?

Methadone is used to treat severe pain. It may also be used for other purposes.

How does this drug work?

Methadone is an opioid pain reliever that works very much like morphine. It binds to opioid receptors in the brain and central nervous system (CNS), which reduces both the perception of and emotional response to pain.

Before taking this medicine

Tell your doctor…

  • If you are allergic to anything, including medicines, dyes, additives, or foods.
  • If you have any medical conditions such as kidney disease, liver disease (including hepatitis), low thyroid function, or Addison’s disease (low adrenal function). These conditions may require that your medicine dose, regimen, or timing be changed.
  • If you have asthma, emphysema, chronic bronchitis, sleep apnea, or other serious breathing problems. Methadone can worsen these problems, and you could even stop breathing.
  • If you have an abnormal heart rhythm, especially a disorder of the heart’s electrical system called long QT syndrome. You may need closer monitoring during treatment.
  • If you have problems with the amount of magnesium or potassium in your blood. Low levels of these minerals can increase the risk methadone will affect heart rhythm.
  • If you have abdominal pain or any disorder with slowed or blocked intestines, such as paralytic ileus. People with these problems shouldn’t take methadone. If you’ve had this kind of problem in the past, tell your doctor so that you can be watched in case it comes back
  • If you have trouble passing urine, a narrow urethra, or if you have an enlarged prostate. Methadone can make it harder to urinate.
  • If you have ever had a seizure, head injury, or if you have had problems with pressure, infection, or a tumor in your head or brain. Methadone can raise your risk of seizures.
  • If you have low blood pressure. Methadone can worsen this.
  • If you have gallstones, gallbladder disease, or pancreatitis. Methadone can sometimes worsen these problems.
  • If you drink alcohol or take any medicine that can affect your brain or nervous system. These may worsen the side effects of methadone or cause other problems.
  • If you have serious mental illness or if you have ever had delirium tremens (severe alcohol withdrawal symptoms). You may have more problems on methadone.
  • If you have taken monoamine oxidase inhibitors (MAOIs) within the past 2 weeks (see “Interactions with other drugs” below). Methadone can cause slow or shallow breathing, low blood pressure, excitability, seizures, coma, or shock if any MAOI is left in the body.
  • If you are planning to have surgery or anything requiring general anesthesia in the near future. (See also “Precautions.”)
  • If you have trouble with addiction, alcohol, or drug abuse now or have had one in the past. Methadone can be habit forming, especially for those who have had problems before.
  • If any family members have or have had an addiction or drug problem. Methadone is sometimes stolen by or for those who are addicted to it or drugs like it.
  • If you are pregnant, trying to get pregnant, or if there is any chance of pregnancy. In animal testing, the offspring of males taking methadone were more likely to die or have behavior changes. There might also be an increased risk of harm to the fetus if a woman takes this drug during pregnancy, especially later in pregnancy (see the “Precautions” section).
  • If you are breastfeeding. The drug passes into breast milk and may affect the baby.
  • About any other prescription or over-the-counter medicines you are taking, including vitamins and herbs. In fact, keeping a written list of each of these medicines (including the doses of each and when you take them) with you in case of emergency may help prevent complications if you get sick.

Interactions with other drugs

Methadone interacts with a number of different drugs, some in very dangerous ways.

Several different medicines can increase the blood level of methadone and raise the risk of serious side effects or overdose:

  • Antibiotics such as erythromycin (E.E.S., E-Mycin, Erythrocin), clarithromycin (Biaxin), and norfloxacin (Noroxin)
  • Anti-fungals such as ketoconazole (Nizoral), itraconazole (Sporanox), voriconazole (Vfend)
  • Antidepressants such as sertraline and fluvoxamine
  • Blood pressure and heart medicines such as verapamil and diltiazem (calcium channel blockers)

There may be other medicines with this effect that are not on this list. When you are on any of these medicines and are being treated with methadone, your dose of methadone may need to be lowered to avoid serious side effects.

Antidepressants of the older MAOI type such as phenelzine (Nardil), tranylcypromine (Parnate), isocarboxazid (Marplan), or selegiline (Emsam) may cause slow or shallow breathing, low blood pressure, excitability, seizures, coma, or shock if methadone is given within 2 weeks of the last MAOI dose.

Medicines or substances that slow down the brain or nervous system, such as these, can cause worse side effects if taken with methadone:

  • Anti-anxiety drugs (sedatives or tranquilizers)
  • Sleeping pills
  • Muscle relaxers
  • Barbiturates
  • Anti-seizure medicines
  • Other opioid drugs
  • Anesthetics
  • Tricyclic antidepressants such as amitriptyline (Elavil), nortriptyline (Pamelor), imipramine (Tofranil), desipramine (Norpramin), doxepin (Sinequan), and others
  • Anti-psychotic drugs
  • Certain anti-nausea medicines
  • Certain antihistamines (those that cause sleepiness)
  • Alcohol-containing drugs or beverages, including beer, wine, and mixed drinks

Some of these drugs can cause slowed breathing, low blood pressure, extreme sleepiness, coma, or even death if taken with methadone.

If you are taking “water pills” (diuretics) or laxatives, methadone is more likely to affect your heart rhythm.

Some substances may lower the blood level of methadone:

  • Anti-seizure medicines such as phenobarbital, carbamazepine, and phenytoin
  • TB medicines rifampin and rifabutin
  • HIV medicines such as ritonavir, indinavir, nelfinavir, efavirenz, nevirapine
  • Steroid drugs such as dexamethasone
  • St. John’s wort

Your doctor will decide if your methadone dose should be changed to control pain and avoid withdrawal symptoms.

Buprenorphine (Subutex, Suboxone), butorphanol (Stadol), nalbuphine (Nubain), or pentazocine (Talwin, Talacen) may reduce the effectiveness of methadone. They can cause withdrawal symptoms if you have taken methadone for some time.

Methadone can also affect other drugs that you may be taking; for instance, methadone can cause desipramine (Norpramin, an antidepressant) and zidovudine (Retrovir or AZT, an HIV drug) to build up in the body and raise your risk of problem side effects. It can lower the levels of other drugs such as didanosine (Videx, an HIV drug).

Check with your doctor, nurse, or pharmacist about whether other medicines, vitamins, herbs, and supplements can cause problems with this medicine.

Do not start or stop any medicines while on methadone without talking with the prescribing doctor(s) about all of the medicines you take, including methadone.

Interactions with foods

Grapefruit or grapefruit juice may raise the level of this drug in your body. This can worsen any bad effects the drug may have on you.

Beverages that contain alcohol, including beer, wine, and mixed drinks, can raise the risk of harmful effects and death if taken while you’re being treated with methadone.

Check with your doctor, nurse, or pharmacist about whether other foods may be a problem.

Tell all the doctors, dentists, nurses, and pharmacists you visit that you are taking this drug.

How is this drug taken or given?

Methadone is given several ways: as a pill or liquid by mouth, or as an injection in a vein, muscle, or under the skin. If you are taking the oral concentrate solution, measure carefully using the dropper from the pharmacy, and mix your dose in at least an ounce or two of water or juice. If you are using dissolving tablets, place your dose into water or juice and wait a minute for the tablet to dissolve before you drink it. If any bits are left behind, swirl in a bit more fluid and drink it.

Your doctor will select your dose depending on how well your pain is controlled by methadone. You may be started on a lower dose and have it slowly increased over a few days or weeks.

Take this drug exactly as prescribed by your doctor. If you have any questions or do not understand the instructions, talk to your doctor or nurse. Store the medicine in a tightly closed container away from heat and moisture and out of the reach of children, pets, and others. Never let anyone else share your medicine.

Precautions

When you first start taking this drug, or when the dose is increased, it builds up in the body over the course of the first few days. Pain relief and side effects will increase over that time, although the risk of slowed breathing can last longer than pain relief.

If you have never taken opioid pain relievers before, be sure your doctor or nurse knows that before you start using methadone. Only people who have taken opioid pain medicines regularly and recently should take methadone.

Always talk with your doctor before starting or stopping any medicines while on methadone. Because some drugs cause methadone to keep building up in the body, you can get too much methadone and have serious side effects or even overdose. Other drugs can cause methadone to leave the body faster so that your pain is not controlled.

Since methadone affects the central nervous system, do not take other drugs or substances that slow down the brain or nervous system such as alcohol, sedatives, muscle relaxers, and sleeping medicines unless your doctor tells you to do so (see “Interactions with other drugs”). Combining these drugs with methadone can slow down breathing and lower blood pressure even more. Keep in mind that methadone’s effects on your breathing often last longer than the pain relief. Pain relief effects start to last longer after you have taken it for several days.

This medicine can cause drowsiness and lightheadedness. Do not drive, operate machinery, or perform other activities that require alertness until you know how you react to this medicine.

Methadone can make you feel dizzy or faint, and increase your risk of falling or fainting. Be careful getting up, changing position, or walking. Get up slowly and hold onto something or someone to keep you steady. If you feel lightheaded or dizzy, it may help to lie down. It is best to have a responsible adult with you for the first few days after starting the methadone or after any increase in dose, until you know how you will respond to it.

Call your doctor right away if you have trouble breathing, get short of breath, dizzy, faint, get confused, feel very drowsy, or start seeing or hearing things that aren’t there. These may be signs your dose is too high, or you could have gotten an accidental overdose of the medicine.

Tell your doctor or nurse right away if you have trouble passing urine, trouble walking, vision problems, trouble swallowing, or other problems.

Get medical help right away if you notice symptoms that suggest a heart rhythm problem, such as palpitations (especially a slow, irregular, or fast heartbeat), dizziness, lightheadedness, or fainting when taking methadone.

If you are planning to have any kind of surgery or dental procedure, be sure to tell the doctor or dentist in charge that you are using this medicine. Some anesthesia drugs can cause a dangerous drop in blood pressure when used with this drug.

Constipation is a very common side effect of taking opioid pain medicines. While you're taking methadone, your doctor may advise you to take a stool softener, bulk-forming agent, and a laxative to help keep bowel movements regular. Talk to your nurse or doctor about this when you first start this medicine. Drink plenty of fluids throughout the day, and try to eat foods high in fiber such as whole grains, bran, fruits, and vegetables. Call your doctor or nurse if you have not moved your bowels in 2 days.

Most cancer pain can be controlled. Tell your cancer team if your medicines do not control your pain, and keep them informed about any side effects you are having. Your cancer team may need to adjust your medicines several times before they find the medicines that work best for you.

If you have chronic (long term) cancer pain, talk with your doctor or nurse about taking your pain medicines on a regular schedule to keep it from worsening. If you wait until the pain is bad, it takes more medicine to get it under control. If pain comes back between doses, talk to your cancer team about changing your medicine or adding an extra one for “breakthrough” pain.

Talk to your doctor or nurse about using the smallest effective dose to reduce side effects. Tolerance (when larger doses are needed to give the same effect) and physical dependence (when the body goes into withdrawal if drug is suddenly stopped) develop when strong (opioid) medicines are taken over several weeks to treat chronic pain. But this is different from addiction, which starts when the drug is taken for pleasure rather than for relief of pain. Tell your doctor or nurse if you still have pain even though you are taking the medicine as prescribed. Do not adjust your dose without talking to your doctor or nurse first.

Do not stop taking this medicine without talking to your doctor or nurse. When no longer needed, this medicine should be stopped gradually with the help of your doctor. If it is stopped suddenly, withdrawal symptoms may occur, such as restlessness, irritability, anxiety, runny nose, watering eyes, yawning, sweating, chills, gooseflesh, aches, nausea, vomiting, poor appetite, diarrhea, high blood pressure, fast heartbeat, and fast breathing.

Acetaminophen or aspirin are often taken along with methadone to increase the pain relief action. It is important to know if any of your other medicines contain either of these drugs. Aspirin and acetaminophen are in many remedies, and it is easy to accidentally get too much of them. Check with your doctor, nurse, or pharmacist to find out if these drugs are included in your daily medicines.

Using opioid drugs such as methadone during pregnancy, especially near the end of the pregnancy, can cause neonatal opioid withdrawal. This can be life-threatening to a newborn if it’s not recognized and treated.

This drug is a controlled substance, and may be habit forming. Keep your medicine in a safe place, away from other people, and do not let anyone else take your medicine. A person who has taken opioid medicines such as methadone for a long time often needs large doses for pain relief, while the same amount could quickly kill someone else.

If you think you or someone else may have taken an overdose of methadone, or if someone else has taken even one dose, get emergency help right away. Symptoms of methadone overdose may include extreme drowsiness, slow heartbeat, slow or irregular breathing, cold clammy skin, or coma. Methadone overdose can cause the heart or breathing to stop. The patient may need to be watched and treated for many hours because of how long methadone stays in the body.

Possible side effects

You will probably not have most of the following side effects, but if you have any talk to your doctor or nurse. They can help you understand the side effects and cope with them.

Common

  • Constipation*
  • Drowsiness
  • Sedation*
  • Nausea
  • Dizziness*
  • Dry mouth

Less common

  • Vomiting
  • Changes in mood, such as euphoria (happiness) or depression
  • Mental clouding, confusion*
  • Slow or shallow breathing*
  • Low blood pressure with dizziness when sitting up or standing*
  • Delayed digestion
  • Slow heart rate
  • Itching, rash

Rare

  • Trouble urinating
  • Seizures
  • Decreased sexual interest
  • Impotence
  • Allergic reaction, with hives, dizziness, or swelling of the face, mouth, or throat
  • Opioid withdrawal and even death in the newborn if it’s taken during pregnancy*
  • Death due to slow or shallow breathing, low blood pressure, heart rhythm problems, drug interactions, allergic reactions, or other causes*

*See “Precautions” section for more detailed information.

There are some other side effects not listed above that can also occur in some patients. Tell your doctor or nurse if you develop these or any other problems.

FDA approval

Yes – first approved before 1984. (The FDA cannot verify dates of drugs approved before 1984.)

Disclaimer: This information does not cover all possible uses, actions, precautions, side effects, or interactions. It is not intended as medical advice, and should not be relied upon as a substitute for talking with your doctor, who is familiar with your medical needs.


Last Medical Review: 06/18/2014
Last Revised: 06/18/2014