Methadone was first synthesized in Germany at the laboratories of the pharmaceutical giant, IG Farben. Two German scientists, Max Bockmühl and Gustav Ehrhart, patented it in September 1941. Bockmühl and Ehrhart were attempting to find an opioid pain killer which would be structurally dissimilar to morphine, non‐addictive, and would escape the strict legal controls placed on opioids at that time. Ironically, methadone was not much used in Germany.  It was only after World War II, that methadone was recognized as both a pain medicaion and a substance very useful in the treatment of opioid abuse.

In 1947, Harris Isbell and his colleagues, who had been experimenting extensively with methadone, discovered that methadone was beneficial in the treatment of opiate‐dependent patients. Several studies from the United Kingdom in the 1940s described methadone’s efficacy in reducing heroin withdrawal symptoms. Ingeborg Paulus and Dr. Robert Halliday, working with the Narcotic Addiction Foundation in Vancouver, established the first methadone maintenance treatment program in the world and published their findings in the Canadian Medical Association Journal in 1967. In the United States, Dr. Vincent Dole and Dr. Marie Nyswander confirmed the feasibility of using methadone as a maintenance medication for heroin dependence.

MYTH: Methadone just replaces one drug for another. You are still an addict.

REALITY: People who take methadone as a treatment for opioid dependence and addiction, are no more addicts than are people who take daily inhalers for chronic asthma, tablets for controlling high blood pressure, or insulin for diabetes. Methadone is a medication. Methadone treatment allows you to live a normal life, work, go to school, or care for your children.

MYTH: Methadone is/is not a cure for opioid addiction.

REALITY: It depends on how you define cure. Methadone is a medication that will control your addiction, so you can get back to normal functioning in life.  If you define cure as absolute abstinence from all opioids, there is no medication or technique that has been shown to achieve that like a magic bullet.  However if you define cure as getting back to normal functioning, work and family life, then methadone maintenance can be viewed as an effective cure since it has been shown more than any other medication or method to achieve these goals.

MYTH: Methadone is only for "hard-core" heroin addiction, not for prescription pain killer addiction.

REALITY: Methadone is useful and used for dependence and addiction to all types of opioid drugs, such as oxycodone (oxycontin® or percocet), fentanyl, hydromorphone (dilaudid®), heroin etc.  All these drugs behave similarly in the body in causing addiction and dependence.  If someone is diagnosed and affected by opioid dependence, methadone maintenance treatment can be an effective option for them.

 

MYTH: Methadone will get you high.

REALITY: If you’re looking for a high, you’ll be disappointed with methadone. When you first start treatment, you may feel lightheaded or sleepy for a few days, but you will quickly develop a tolerance to these effects. Expect to feel “normal” when you’re on methadone.

MYTH: Methadone will make you sick.

REALITY: The only time you might feel sick from methadone is at the beginning of your treatment, when your dose might not be enough to keep you free of withdrawal symptoms. In most cases, if you do feel sick, it’s mild. Your dose will be adjusted and you should feel better within a few days.  When you’re on methadone you can catch a cold or any other illness just like anyone else, but you’re much less prone to illness than illicit drug users. People on methadone are less likely to use needles, and more likely to eat well and take good care of themselves. When you’re on methadone you won’t wake up sick every morning. If anything, methadone will help you to get well.

MYTH: Long-term use of methadone damages the liver, the thyroid gland and the memory.

REALITY: Long-term use of methadone is safe. It will not damage your internal organs, and when you are on the correct  and stable dose, it will not interfere with your thinking. If you have a medical condition such as hepatitis or cirrhosis of the liver, methadone maintenance treatment can improve your access to medical treatment, and help you to manage the illness.  People above age 50 may be at risk for osteoporosis and methadone may increase this risk.  If on long-term methadone treatment, people above this age should be screened for osteoporosis.

MYTH: Methadone rots your teeth and bones.

REALITY: This is a common myth, and although it’s not true, the reasons behind the myth deserve some consideration. The most likely reason for higher incidence of tooth decay in the addiction community is that like many other daily routines, dental hygiene is not taken care of by the patients. Nevertheless, one of the side-effects of methadone, like many medications, is that it may give you a dry mouth. This can make your teeth more prone to the production of plaque, which is a major cause of gum disease and tooth decay. To protect your teeth, follow the dental routine recommended for everyone: brush and floss every day, rinse your mouth with mouthwash, go to the dentist at least twice a year, and cut sugar from your diet. Drinking plenty of water can also help to relieve dry mouth.  As a side note, the stimulant class of drugs such as cocaine, methamphetamine, and "speed", in contrast to opioids, are more likely to cause tooth decay due to causing severe dry mouth.

If you’re on methadone, and you feel like your bones are rotting, it’s probably because you’re on too low a dose. Bone ache, which may feel like bone “rot,” is a symptom of opioid withdrawal. When your dose is adjusted correctly you should not experience any aching or other symptoms of withdrawal.

MYTH: Methadone makes you gain weight.

REALITY: Not everyone gains weight when they go on methadone, but some do. This is usually because methadone improves your health and appetite, and so you eat more. If you’ve been using drugs for a long time, you may be underweight and need to gain a few pounds. Even though the methadone drink is not “fattening” like sweets and fatty foods, methadone can slow your metabolism and cause water retention, which can lead to weight gain. You can control weight gain by choosing healthy foods that are high in fibre such as whole grains and fruits and vegetables, and by exercising regularly. If you nourish your body, you’ll keep the pounds off, and more important, you’ll feel good.

MYTH: It’s especially hard to get off methadone.

REALITY: Methadone is an opioid like others such as oxycodone (oxycontin® or percocet), fentanyl, hydromorphone (dilaudid®), heroin etc. so getting off methadone will be similar to getting off them. The symptoms of methadone withdrawal come on more slowly than those of heroin withdrawal, and can last longer. If someone has a very difficult time coming off methadone, it means that they are still affected by opioid dependence and addiction.  It means they are not ready.  This is similar to someone with asthma who is well and stable on inhalers, and then claims that it’s too hard to get off the inhalers.  Methadone is a medication to treat and control opioid dependence/addcition.  While being stable on methadone can bring a opioid-dependent patient back to life and function, it does not simply make the condition of opioid dependence go away.  You can visit this section to find out more about: how to get off methadone.

Methadone is indicated and approved for the following uses:

1. Long-term maintenance treatment of dependence and addiction to opioids such as oxycodone (oxycontin® or percocet), fentanyl, hydromorphone (dilaudid®), heroin etc.  Such treatment can happen usually only in certain approved facilities and/or by specially trained/licensed physicians.

2. Detoxification treatment of dependence on opioids such as oxycodone (oxycontin® or percocet), fentanyl, hydromorphone (dilaudid®), heroin etc. Such treatment can happen usually only in certain approved facilities and/or by specially trained/licensed physicians.

3. Management of moderate to severe chronic pain when a continuous, stable-level opioid analgesic is needed for an extended period of time. This should be done under the care of a physician who is very familiar with the unique pharmacology of methadone.

4. Management of pain within the palliative treatment of terminally ill patients by physicians experienced with methadone.

Methadone should not be used in the following circumstances:

1. For any treatment of dependence or addiction to non-opioid drugs.  Examples of drugs whose addiction do not respond to methadone are stimulat class drugs such as cocaine and methamphetamines; sedative class drugs such as diazepam (Valium) and alprazolam (xanax); and THC, LSD, and ecstasy.

2. For pain that is mild or, occasional, or not expected to persist for an extended period of time.

3. For acute pain from any injury.

4. For postoperative pain

Many people use methadone with the term "Methadone Maintenance Treatment" interchangeably.  This is not correct.  Methadone is a pharmaceutical agent with several uses including pain control.  On the other hand, Methadone maintenance treatment or MMT is a long-term program for those patients who have addiction/dependence to the opioid class of drugs such as oxycodone (OxyContin® or Percocet®), fentanyl, hydromorphone (Dilaudid®), heroin, morphine, codeine, etc.   MMT usually integrates non-pharmacological modes such as counseling, social work, and family therapy.

Methadone belongs to the opioid family of drugs. Examples of other opioids are oxycodone (OxyContin or Percocet), fentanyl, hydromorphone (Dilaudid), heroin, morphine, codeine, etc. This is the reason why methadone works similarly as a pain reliever.

While methadone is an opioid as mentioned, there are some differences between methadone and the other opioids. The main difference is methadone's much slower metabolism. While the other opioids reach peak action within minutes or seconds (if injected or inhaled), methadone can take 3-4 hours to reach its peak action. Due this slower metabolism, methadone stays in the body much longer too -often days as opposed to hours for the other opioids. This allows a more even and stable action of the medication as opposed to the rapid onset and offset of a short acting opioid such as morphine or oxycodone. So while methadone exerts its opiate-like effect, it does it in a slower and more controlled way. This effect is one that is desired for an individual addicted to the euphoria or "high" achieved from the rapid-acting opioids. While methadone provides a relief from the symptoms of withdrawal such as aches, chills, and cramps and the mental effects of craving for the high, it does not produce a high itself. Further, since methadone at an adequate dose binds the opioid receptors in the brain, there is no much room for the other opioids to bind themselves. In this manner, methadone is said to block the other opioids if taken.

The other way that methadone is different than the other opioids is that in addition to its opioid effects and unlike the other opioids, it has action against a separate nervous system in the body referred to as the NMDA receptor system. By blocking these receptors, methadone user are able to achieve a stable dose of methadone without need for any ever-increasing dosage to reproduce the same mental effects, as seen in the nature of morphine or oxycodone. This is the reason why patients on a stable dose of methadone are able to do stay on this dose for months or even years.

Most of methadone's side effects are likely to be more pronounced at the beginning of treatment — during the two- to six-weeks of treatment. The most frequently reported side-effects include drowsiness and light-headedness, nausea and vomiting, excessive sweating, dry mouth, weakness, constipation and change in sex drive. Most patients build tolerance to these side effects as the treatment goes on and the dose is adjusted by the physician.  The physician can also investigate and prescribe other medications to alleviate these side effects, if they tend to persist.

This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.

The following is a list of the most common drug interactions for methadone.  This is by no means a complete list. Consult a physician or pharmacist for a complete list.  Always inform your physician or pharmacist about the complete list of your medications so that you could be alerted to any dangerous interactions.

Sedatives/hypnotics (downers/sleepers):

Concurrent use of methadone and such medications can increase the risk of respiratory depression, hypotension, and profound sedation , coma and death. Of particular concern among these drugs are the benzodiazepines.  Deaths have been reported when methadone has been taken in conjunction with benzodiazepines.  Closer monitoring is needed if these medications are used/abuses along with methadone. There are many drugs within the class of benzodiazepines but the mostly commonly used ones are: diazepam (Valium), lorazepam (Ativan), clonazepam (Klonipin), alprazolam (Xanax), oxazepam (Serax), temazepam (Restoril), chlordiazepoxide (Librium), etc. 

 

Potentially Arrhythmogenic Agents:

Closer monitoring is needed for patients taking higher doses of methadone along with any drugs known to have the potential to prolong the QT interval.  Consult your physician or pharmacist about these. 

 

Opioid Antagonists, Mixed Agonist/Antagonists, and Partial Agonists:

Withdrawal symptoms, sometimes severe and prolonged, can be induced when someone on methadone is given opioid antagonists or mixed agonist/antagonists. Examples of pure antagonists are naloxone (Narcan), naltrexone (Revia or Vivitrol); and examples of mixed or partial agonists are pentazocine (Talwin) and buprenorphine (Suboxone or Subutex)