How Does Methadone Work? Understanding This Key Tool in Opioid Recovery

For many people in recovery, medication-assisted treatment (MAT) that combines FDA-approved medications with counseling and behavioral therapies is one of the most effective treatment methods available. 

Out of all of the medications used in MAT, methadone has the longest history, having been used to treat opioid addiction since the 1960s. Many people, however, still have questions about how methadone works and what to expect from treatment. 

In this article, we’ll break down the science behind methadone, how it’s used in recovery, potential side effects, and what makes it such a powerful tool in overcoming opioid addiction.What Is Methadone?

Methadone is a synthetic opioid drug that the FDA has approved for two independent purposes: treatment of moderate to severe pain and the treatment of opioid use disorder (OUD), a chronic illness that is characterized by the compulsive use of opioid drugs regardless of the harmful consequences.[1] 

Methadone is sometimes sold under the brand name Dolophine when it is prescribed for pain. When used for the treatment of OUD, it is frequently referred to as simply methadone. 

In order to understand how methadone works, you must first understand how opioids affect the brain and how dependence on opioids develops.

How Does Methadone Work in the Brain?

Opioid drugs, such as heroin, fentanyl, oxycodone, hydrocodone, and codeine, produce their effects by binding to the opioid receptors in the brain and throughout the body. The opioid receptors are part of the body’s pain regulation and reward circuitry. When opioids bind to those receptors, they trigger a flood of dopamine (a neurotransmitter), leading to sensations of euphoria and the relief of pain. Over time, the brain adapts to this artificial dopamine presence and reduces its own natural production of dopamine, eventually leaving the person dependent on opioids just to feel normal.[2]

Methadone is classified as a full opioid agonist, meaning it binds to the same opioid receptors that all other opioids activate.[3] However, since methadone is long-acting and absorbed more slowly by the body, it does not produce the sudden and intense euphoric feeling that most short-acting opioids produce. Instead, methadone produces steady and stable levels of the drug in the bloodstream. This accomplishes two critical things: (1) it relieves withdrawal symptoms, and (2) it reduces or eliminates cravings for opioids that can cause someone to relapse.

Research conducted by the Substance Abuse and Mental Health Services Administration (SAMHSA) reports that patients receiving methadone maintenance therapy have substantially improved function, including much lower rates of illicit opioid use, lower rates of overdose, and better social functioning than people trying to quit opioids without medication-based support.[4]

How Does Methadone Reduce Cravings and Withdrawal Symptoms?

One primary barrier to recovering from opioid addiction is the intensely uncomfortable withdrawal.[5] Symptoms of opioid withdrawal can include strong cravings, anxiety, muscle aches, nausea, vomiting, sweating, insomnia, and severe discomfort that can start within a few hours after the last dose of a short-acting opioid. For many people, the fear of these intense symptoms makes them unwilling to attempt to stop using opioids.

Methadone works to directly address those fears of withdrawal. Because methadone activates the same opioid receptors that other opioids activate, an appropriate dose will prevent the withdrawal symptoms entirely. At the same time, methadone maintains a stable baseline of opioid receptor activity. According to the National Institute on Drug Abuse (NIDA), methadone’s ability to occupy opioid receptors also creates a “blockade” effect, meaning that because opioid receptors are already occupied, taking another opioid produces little to no effect, significantly reducing the psychological pull toward other, additional opioid use, which is often a driving force behind relapse.[6]

Research conducted by the Substance Abuse and Mental Health Services Administration (SAMHSA) reports that patients receiving methadone maintenance therapy have substantially improved function, including much lesser rates of illicit opioid use, lesser rates of overdose, and better social functioning than people trying to quit opioids without medication-based support.[7]

Why Is Methadone Long-Acting?

One of methadone’s key characteristics is its long half-life (the amount of time it takes for the amount of active substance in the body to decrease by 50%) 

While the half-life of other short-acting opioids, such as heroin, is only a few hours, the half-life of methadone varies from 24 to 36 hours and can be longer in certain individuals.[8]

This extended half-life makes methadone ideally suited for long-term treatment. A single daily dose of methadone from an opioid addiction treatment program or methadone clinic may keep withdrawal symptoms and cravings under control all day long. Consistency is critical not only for a patient’s comfort but for keeping them in treatment. Someone is much more likely to stay in treatment when they don’t have to deal with the physical and emotional turmoil of withdrawal.

Since methadone has a long half-life, the dosage also must be carefully adjusted. Due to methadone accumulating in the body, the prescribing physician must closely monitor each of their patients for several weeks to determine the optimal dose that provides adequate relief of symptoms without excessive sedation or other serious adverse reactions.

How Long Does Methadone Take To Work?

Patients who take a dose of methadone should feel some relief within 30 minutes to 1 hour, with peak effects reached within 2–4 hours. The long half-life of methadone produces steady therapeutic levels of the drug in the patient after several days of consistent dosing.

This means that in the first several days of treatment, the medication may not fully control cravings or prevent withdrawal symptoms. Healthcare providers usually start patients at a lower dose and gradually increase by small amounts until the most effective and stable dose is reached, a process called dose titration. This is a slow process that helps minimize risk while reaching the desired therapeutic effect of the medication. Full stabilization, meaning consistent relief from cravings and withdrawal without significant side effects, usually takes 1–2 weeks or longer.

Side Effects of Methadone

Methadone is a medication, and like all medications, it can have side effects, especially during the initial part of the treatment period when the patient is adjusting. The most common side effects are:

• Drowsiness
• Constipation
• Dry mouth
• Sweating
• Nausea

Most patients experience significant decreases in adverse side effects once their body adjusts to the methadone. Additionally, there are significant additional risks that should be understood regarding methadone. 

Methadone can slow down breathing, and when taken with other medications, such as benzodiazepines, sedatives, or alcohol, the risk of respiratory depression (shallow, slow breathing that leads to a lack of oxygen) and overdose increases.[9] Signs of a methadone overdose include:

• Extreme drowsiness
• Slow or stopped breathing (respiratory depression)
• Blue-tinged lips or fingertips
• Limpness
• Unresponsiveness

Experiencing any of these clinical signs is a medical emergency and requires immediate intervention. Women considering methadone for MAT who are pregnant or breastfeeding should speak with their healthcare provider since methadone does pass into breast milk. In many cases, the benefits of using MAT during pregnancy outweigh potential risks.

Methadone vs. Other MAT Medications

Methadone is one of the three medications approved by the FDA as MAT for opioid use disorder. The other two are naltrexone and buprenorphine (which is commonly referred to by its brand name Suboxone when combined with naloxone).

• Buprenorphine is a partial opioid agonist because it activates opioid receptors but at less intense levels than methadone. It has a limiting effect on respiratory depression and euphoria. It also blocks other opioids. Buprenorphine can be prescribed by qualified physicians and taken at home, making it much easier for patients to obtain than methadone. 
• Naltrexone completely blocks opioid receptors, so that opioids do not have any effect. However, it requires a full detox before treatment can begin, and it is not appropriate for all patients. 

Which medication is best will depend on the patient’s history of opioid use, current health status, lifestyle, and personal preferences. A qualified treatment provider can help determine which option makes the most sense as part of a comprehensive treatment plan.

Getting Help for Opioid Addiction in New Jersey

If you have an opioid addiction or know someone who does, MAT may be a life-changing step in recovery. The Garden Recovery & Wellness in Cherry Hill, New Jersey, offers medication-assisted treatment as part of an individual and compassionate approach to care. We treat the whole person, not just the substance abuse, in a warm, welcoming environment that encourages genuine healing.You don’t have to go through this alone. Contact The Garden today and find out about our MAT program and how we can help you or someone else you care about on the journey toward long-term recovery.