Methadone was first synthesized in Germany in the 1930s in an effort to find better alternatives to morphine. By the 1960s, methadone treatment was popularized for its efficacy at treating heroin addiction. While individuals can become addicted to methadone, its use as an addiction treatment medication is still warranted today.

What Is Methadone?

Methadone is a synthetically produced pain medication that predominantly activates the mu subtype of opioid receptors in the brain. Opioids are a drug class that includes heroin, fentanyl, codeine, hydrocodone and oxycodone, among many others. Opioid receptors can be activated by various means. Natural chemicals like endorphins can stimulate the release of neurotransmitters that activate these receptors and opioids from external sources can either activate or deactivate these receptors.

Background and History

Methadone has a long history beginning in the 21st century. It was first developed in the 1930s by a team of German scientists who sought to find an alternative to morphine that would have similar pain-relieving properties, but not lead to addiction. By World War II, morphine and other pain medications were in short supply. Thus, Germany began synthesizing methadone again to fill this pharmacological void.

It was not until the 1960s heroin addiction resurgence in New York City that methadone’s practical utility for treating narcotic addictions was fully realized. By 1964, methadone maintenance treatment was developed to decrease or eliminate heroin use. The overall goal of such maintenance treatments was to “maintain” or prevent withdrawal side effects in people who were addicted to heroin.

In the 1970s, the United States government created regulations for the use of methadone in heroin addiction treatment. In recent years, the government has modified these regulations to increase the efficacy of methadone treatment for opioid addiction.

Methadone for Opioid Addiction

While methadone has historically been used for heroin addiction over other opioids, this has changed in recent years. Methadone has several advantages in the treatment of opioid addiction. Some of these include:

  • Methadone is a legally controlled substance, unlike heroin
  • Methadone prevents opiate withdrawal symptoms
  • Methadone blocks the “high” achieved from heroin and other opioids
  • Methadone decreases cravings for heroin and other opioids

How Methadone Works

How exactly does methadone work? Methadone’s mechanism of action is similar to other opioid receptor agonists. Upon activation, opioid receptors have a role in regulating various normal and pathological processes, including:

  • Pain
  • Addiction
  • Cell proliferation
  • Immune system regulation
  • Obesity
  • Epilepsy
  • Neurodegenerative disorders

After acting on the mu subtype of opioid receptors, methadone stimulates the release of neurotransmitters like dopamine, acetylcholine and norepinephrine from brain cells. These neurotransmitters are responsible for methadone’s pain-relieving activity and hormonal regulation.

How Can Patients Receive Methadone?

Individuals who desire to stop using heroin or other opioids can receive methadone through a medication-assisted treatment program. Methadone can only be dispensed through opioid treatment programs certified by the Substance Abuse and Mental Health Services Administration (SAMHSA).

Individuals can also go to certified methadone clinics to receive daily methadone in liquid or pill form. Different countries have their own versions of methadone clinics. Generally speaking, these clinics:

  • Maintain low costs of methadone per dose
  • Have accessible hours (early morning to night)
  • Allow individuals to start treatment without meeting extensive criteria
  • Emphasize that the clinic is a judgment-free area

Methadone Side Effects

Methadone has many reported side effects, though not all individuals will experience them. Some of the most common methadone side effects include:

  • Stomach issues (nausea, vomiting, constipation)
  • Increased sweating
  • Dry mouth
  • Weight gain
  • Alterations in the menstrual cycle (women only)
  • Sexual dysfunction

However, if individuals experience more dangerous side effects, like difficulty breathing, chest pain, mental confusion, fainting or severe dizziness, rash, swelling, hives or heart palpitations, they should consult a medical professional or emergency services immediately.

While the long-term effects of methadone use are not well understood, studies suggest an association with long-term use and decreased cognitive function and memory.

Taking Methadone While Pregnant

Women can safely take methadone while pregnant or breastfeeding. Heroin and other opioids may cause premature birth or miscarriages if a woman suddenly withdraws. Methadone can be used to help counteract uterine contractions that occur due to withdrawal.

Additionally, methadone is not known to cause birth defects. Despite its safety, infants are likely to go through withdrawal symptoms after birth, but only for a short time. Methadone also enters breast milk in small amounts but has not been shown to affect infants negatively.

How Effective Is Methadone?

Relative to detoxification programs, methadone maintenance treatment has been shown to be quite effective, particularly at treating heroin addiction. In a study conducted in 1982, 41% of individuals that received methadone maintenance treatment were no longer addicted to opioids, including heroin, nor were they involved in major crimes. This number was significantly lower in individuals that did not receive treatment (~27%). These results indicate that methadone is an effective treatment for opioid addiction if used properly and under the supervision of licensed medical professionals.

Methadone Safety Guidelines

The extensive amount of research that has been conducted on the use of methadone to treat opioid addiction has shown it to be relatively safe. Licensed medical professionals follow specific methadone treatment guidelines that have been well established since the 1960s. These guidelines include:

  • Individuals must take methadone as prescribed (as methadone can be addictive if misused)
  • Alcohol should not be consumed while taking methadone
  • Use caution while driving or operating machinery and taking methadone
  • If an overdose of methadone is suspected, contact emergency services (911)
  • Store methadone in a safe place away from light and not easily accessible by children
  • Dispose of unused methadone by flushing it down the toilet
  • Be aware that methadone may interact with other medications

Methadone Administration Guidelines

Strict federal guidelines are in place for the administration of methadone. Individuals are administered methadone gradually and weaned off of it slowly to prevent withdrawal symptoms. In a study conducted in 2005, higher methadone doses (50–150 milligrams) were more effective at curbing cravings for heroin. Thus, licensed medical professionals aim to provide 60–100 milligrams of methadone daily to “maintain”  individuals with opioid addiction. After a period of 6–12 months of methadone use, individuals may have their methadone doses lowered gradually as part of their medication-assisted treatment program.

Resources on Methadone

For more information and facts on methadone treatment for opioid addiction, please see the following resources:

How The Recovery Village Uses Methadone

The Recovery Village offers medication-assisted treatment programs at some of our facilities. Reach out to a representative today to find out if a facility near you offers methadone-assisted treatment or similar programs for opioid addiction.

Methadone
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