Methadone has been a cornerstone of safe and effective opioid addiction treatment for decades. One of the biggest obstacles to overcoming opioid addiction is navigating the difficult withdrawal phase with heroin, morphine and prescription opioids all producing powerful and potentially dangerous withdrawal symptoms. These symptoms can pose a significant barrier to cessation and also greatly increase the risk of relapse. Methadone can offer a solution to these challenges by mitigating the severity of withdrawal symptoms and reducing cravings for opioids. Methadone can be a life-changing treatment course which has helped tens of millions of people around the world overcome addiction to heroin and a number of other opioids.

What is methadone?

Methadone is a synthetic opioid that is most commonly used to treat opioid dependence and, occasionally, as a pain management solution. The history of methadone dates back to the late 1930s in Germany, with its development part of a search for an effective analgesic that was easier to produce and less addictive to morphine. Initially named “Hoechst 10820,” methadone was introduced to the market under the trade name “Dolophine”, a name derived from the Latin “dolor” (pain) and “finis” (end), meaning “end of pain.”

Methadone was used for pain management in Germany during the Second World War due to the shortage of alternative painkillers. It was not until the 1960s that methadone began to be used to treat opioid dependence, but in the subsequent decades, this has become its primary purpose.

Methadone is available in various forms, including oral, dispersible, concentrated, and injectable tablets. This allows for versatile administration depending on the unique needs of the individual.

Methadone’s supply is highly regulated in the UK, with the drug available on prescription from a GP or professional addiction treatment centre only. Common methadone brand names include Methadose and Dolophine.

How does methadone work in addiction treatment?

Physical dependence on drugs or alcohol stems from their profound impact on the brain’s reward system. Opioids, in particular, bind to specific receptors in the brain, mimicking the effects of naturally occurring pain-relief substances. Over time, excessive use of opioids alters the brain’s chemistry, leading to a physical dependence where the individual needs to continue using opioids to function.

If the individual stops or reduces opioid intake, the brain, which has adapted to the presence of opioids, struggles to maintain balance. This results in opioid withdrawal symptoms, which can be both uncomfortable and, in some cases, life-threatening. Opioid withdrawal symptoms include severe physical discomforts such as nausea, sweating and shaking and psychological distress, including anxiety and depression. The severity of withdrawal is a significant barrier to overcoming opioid addiction, often leading individuals back to drug use to alleviate their discomfort.

Methadone’s role in this process is multifaceted. By acting on the same opioid receptors in the brain as heroin and prescription opioids, methadone blunts withdrawal symptoms and reduces cravings. However, unlike other opioids, methadone does so without producing a euphoric high.

It also has a slow onset of action and a long half-life, meaning it stays in the body for an extended period, allowing for once-daily dosing that provides a stable effect over 24 hours. This helps in normalising the body’s functions and reducing the impulse to use opioids. Not only does this aid in managing withdrawal symptoms, but it also plays a crucial role in breaking the cycle of addiction as the individual is able to focus on recovery efforts, such as therapy and counselling, without being overwhelmed by cravings and withdrawal.

Methadone side effects

Methadone is a powerful medication, and side effects are not uncommon. These can vary from mild to severe and may affect individuals differently based on factors such as dosage, the duration of treatment and their general overall health. Understanding these side effects is crucial for managing them effectively and ensuring the safety and well-being of those undergoing methadone treatment.

Common methadone side effects include:

    Constipation

    Drowsiness
    Dizziness
    Nausea
    Vomiting
    Sweating

These symptoms often diminish or cease as treatment continues and the body begins to adjust to methadone.

Methadone can also cause more serious side effects such as respiratory depression, a condition where breathing becomes slow and shallow and potentially stops altogether. This is one of the most critical dangers associated with methadone, with a higher risk at the start of treatment or just after the dosage has been increased.

Other serious methadone side effects may include:

    Changes in heart rhythm

    Severe constipation leading to bowel obstruction
    Changes in mood or mental state, such as confusion or depression.

To minimise the risk of side effects, individuals must follow their treatment plan closely, including taking methadone exactly as prescribed, attending regular check-ups with their healthcare provider and communicating openly about any side effects they experience. This will allow for adjustments to the dosage or treatment plan, which may be necessary to alleviate discomfort.

Methadone dependence and withdrawal symptoms

Methadone, while used to treat opioid dependence, can itself lead to dependence if used for a long duration or not strictly according to medical advice. Dependence on methadone can result in withdrawal symptoms if the medication is abruptly stopped or significantly reduced without medical oversight.

Withdrawal symptoms from methadone can be uncomfortable and, in some cases, severe. They often include symptoms similar to those experienced with withdrawal from other opioids, including:

    Sweating

    Nausea
    Vomiting
    Diarrhoea
    Muscle aches
    Restlessness
    Irritability
    Insomnia
    Anxiety

Due to methadone’s long half-life, these withdrawal symptoms may not appear until several days after the last dose and can last longer than those associated with shorter-acting opioids.

In order to prevent methadone reliance and alleviate withdrawal symptoms, it is typically recommended to reduce the medication gradually. This method enables the body to adapt gradually to diminishing doses of methadone, thereby lessening the severity and duration of withdrawal symptoms. It is crucial to carry out the tapering process under the supervision of a healthcare professional, who can modify the tapering schedule according to the individual’s reaction to the dose reductions.

It is also worth noting that the psychological aspect of dependence can be challenging. Individuals may become accustomed to the routine of taking methadone or may fear the return of withdrawal symptoms associated with their primary opioid abuse. This is why methadone should always be used as part of a comprehensive treatment programme that includes behavioural therapy, counselling and ongoing support services for addressing the psychological components of addiction.

Potential health risks of methadone use

Methadone also carries potential health risks that require careful consideration and management. Understanding these risks is crucial for individuals to make informed decisions and healthcare providers to ensure methadone’s safe and effective use. Health risks include:

Respiratory depression
One of the most severe risks associated with methadone, as with other opioids, is respiratory depression. This condition involves a reduction in the urge to breathe and can be life-threatening if not promptly addressed. The risk is higher at the initiation of methadone treatment or following a dose increase. Individuals with underlying respiratory conditions or those taking other medications that depress respiratory function are at an increased risk.
Cardiac arrhythmias
Methadone has been associated with the potential to cause prolongation of the QT interval, a measure of heart rhythm. In some cases, this can lead to serious and potentially fatal heart arrhythmias, such as torsades de pointes. Individuals with a history of heart disease or those on medications that affect heart rhythm may require monitoring with electrocardiograms (ECGs) during methadone treatment.
Neonatal abstinence syndrome (NAS)
Pregnant women on methadone treatment may give birth to babies with NAS, a condition characterised by withdrawal symptoms in the newborn. While methadone is considered safer for pregnant women and their unborn babies than continuing illicit opioid use, careful monitoring and treatment of NAS are necessary to reduce the risks as much as possible.

Potential methadone drug interactions

There are a number of potential Methadone drug interactions that can lead to increased side effects, reduced efficacy of either drug and in some cases, serious health risks. Understanding these potential interactions is crucial for anyone undergoing methadone treatment, emphasising the importance of comprehensive medication management:

Methadone and CNS depressants
The concurrent use of methadone with other central nervous system (CNS) depressants, such as benzodiazepines, alcohol, other opioids and certain sleeping pills, can significantly impair breathing, consciousness and heart rate. This can increase the risk of respiratory depression, sedation and even fatal overdose.
Methadone and serotonergic drugs
Methadone can interact with medications that affect serotonin levels in the brain, such as certain antidepressants (SSRIs and SNRIs), migraine medications (triptans) and some pain medications (tramadol). This interaction can lead to serotonin syndrome, a potentially life-threatening condition characterised by symptoms like confusion, rapid heart rate, high blood pressure, dilated pupils and muscle stiffness.
Cytochrome P450 3A4 inhibitors and inducers
Methadone is metabolised by the liver enzyme cytochrome P450 3A4. Drugs that inhibit this enzyme can lead to increased levels of methadone in the body, raising the risk of side effects. Conversely, drugs that induce P450 3A4 can decrease methadone levels, potentially leading to withdrawal symptoms.
Antiretroviral drugs
Individuals with HIV/AIDS on antiretroviral therapy may experience interactions with methadone. Some antiretroviral drugs can alter the metabolism of methadone, necessitating adjustments in methadone dosage to maintain efficacy and prevent withdrawal or toxicity.
Cardiac medications
Given methadone’s potential to affect heart rhythm, it can interact with medications that have a similar effect, such as those used to treat arrhythmias. This interaction may increase the risk of QT prolongation and subsequent serious cardiac arrhythmias.

To prevent adverse outcomes from these interactions, individuals must inform their healthcare providers about all medications, supplements and substances they are using. Healthcare providers, in turn, should regularly review the individual’s medication regimen to identify potential interactions and make necessary adjustments.

Get help for opioid addiction today

If you or someone you know is struggling with opioid addiction, methadone, as part of a comprehensive treatment plan, can provide significant support in managing withdrawal symptoms and reducing the risk of relapse. The first step is to contact your GP or a professional addiction treatment centre for more information. They can open the door to a range of treatment options that fit your individual recovery needs.

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FAQ’s

What is methadone used for?
Methadone is primarily used as a medication-assisted treatment for opioid dependence and as a pain management solution for moderate to severe pain. In the context of opioid addiction treatment, methadone helps reduce withdrawal symptoms and curb cravings for opioids, facilitating a smoother transition to recovery. For pain management, it provides long-lasting analgesia, especially in cases where other pain relievers are ineffective. Methadone’s unique properties and long half-life make it a valuable tool in both treating opioid use disorders and managing chronic pain conditions.