For decades, methadone has been a first-line treatment for managing opioid addiction. A long-acting opioid agonist, methadone has many therapeutic benefits, but also some inherent dangers—including a risk of respiratory depression as well as the potential for compulsive misuse and addiction to the treatment drug itself.
How Does Methadone Work
Methadone is a synthetic opioid that primarily acts at opioid receptors throughout the body.1When people take methadone at variable doses—whether for pain management, as part of a drug treatment program, or for nonmedical misuse—the drug binds to and activates mu-opioid receptors to, respectively, alter pain perception, stabilize someone in opioid withdrawal and reduce cravings for continued opioid misuse, or elicit a dose-specific euphoria.
When taken regularly as part of a maintenance regimen for treating opioid use disorders, an additional effect of methadone is that, via the building of cross-tolerance, it blocks the effects of other opioid substances,1,2 whether they be street drugs like heroin or other prescription painkillers, such as OxyContin.
Methadone as Treatment for Heroin Addiction
Methadone has been used as maintenance therapy for people with heroin addictions and other opioid use disorders for more than 50 years; in that time, it has been demonstrated to be helpful in increasing treatment retention and reducing drug-related deaths, continued illicit drug use, new cases of drug-related HIV, as well as criminal activity within this treated population.2,3
Methadone is what’s known as an opioid agonist medication, meaning that it achieves its therapeutic effects—in cases of substance use disorder treatment, to alleviate withdrawal and diminish opioid cravings—by acting on specific receptors in our central nervous system.3 When appropriately dosed, methadone maintenance allows the treated individual to remain alert without eliciting a reinforcing euphoria, all the while suppressing a cycle of withdrawal and ongoing opioid drug preoccupation.2,3 Such a combination of effects may be hugely beneficial to someone who has, in the past, struggled with compulsive opioid use, as they resume their productive lives in recovery.
Despite its historical successes as a treatment medication, however, as an opioid agonist, methadone has inherent misuse liability of its own, particularly in people who are not opioid dependent to begin with (as these individuals may be more likely to experience a rewarding, opioid “high” at certain doses).3 As part of an opioid treatment program, methadone dispensing is tightly controlled. As such, the supply of methadone that does end up diverted for nonmedical misuse may be more likely to originate with methadone prescribed for pain management.3 Such supplies also seem to be the main source of methadone involved in overdose deaths, rather than that dispensed as part of an opioid treatment program.3
Methadone and Addiction
Due to some of the inherent risks, methadone is a DEA Schedule II controlled substance. Drugs categorized as Schedule II under the federal Controlled Substances Act have a high potential for abuse; such misuse may lead to the development of significant physiological dependence.4Schedule II drugs like methadone are approved for medical use, but may only be obtained by prescription and are intended for use under the guidelines outlined by the prescribing clinician.
Examples of other Schedule II substances include pharmaceutical cocaine, methamphetamine and opioid painkillers like morphine, hydrocodone, and fentanyl. By contrast, heroin is a Schedule I substance, meaning it has no accepted medical value.
Compulsive methadone use and addiction may involve continued nonmedical use of the drug despite the adverse ramifications of such use. For example, this might mean spending increasing amounts of money or going to other lengths to secure more diverted methadone, to the detriment of other financial obligations and despite the potential for increased legal risks. In some cases, methadone is diverted with the intention of helping others who misuse substances.3 However well-intended such nonmedical use may start out, as it occurs outside of the careful dosing and monitoring of an opioid treatment program, it carries with it the health dangers of the drug (e.g. overdose, respiratory depression, heart rhythm disruptions)5 and could further promote the problematic patterns of use that lead someone down the road of additional addiction issues.
Managing Methadone Withdrawal
When the decision is reached to seek treatment for problematic methadone use or, even, to discontinue methadone maintenance treatment, care must be taken during the initial detox phase to minimize the likelihood of a severely unpleasant withdrawal. Like other opioid drugs, the acute methadone withdrawal syndrome can be quite difficult, and may include symptoms such as:1
- Runny nose.
- Watery eyes.
- Nausea and loss of appetite.
- Abdominal cramps.
- Muscle aches and cramps.
- Involuntary muscle twitches, limb jerking (i.e., kicking).
- Strong opioid cravings.
Depending on the magnitude of an individual’s methadone dependence—which will be influenced by factors such as the amount of drug having being used, as well as the chronicity of such use—withdrawal effects, while rarely presenting any immediate health dangers, can be considerably severe; with a relatively long-acting opioid drug like methadone, withdrawal onset can be expected to occur as many at 36-48 hours after last use, and persist for days to weeks.6,7
Due in large part to the high likelihood of experiencing an intensely unpleasant withdrawal, attempting to quit methadone without the assistance of medical detox interventions could present unnecessary challenges to a person in early recovery.7 With supervision and medical support, stabilizing someone on a maintenance dose and/or, later, slowly discontinuing methadone over the course of many weeks to several months, coupled with behavioral therapeutic interventions, can be extremely beneficial in recovery.6,7
Depending on individual circumstances and needs—including access to treatment medications—a decision may be made at some point to switch a person to another opioid treatment drug, buprenorphine. Buprenorphine is a partial opioid agonist; when used therapeutically, buprenorphine can be associated with relatively less pronounced health risks (such as respiratory depression and overdose potential) than methadone. Also, given individual circumstances, a buprenorphine regimen could provide some added flexibility in terms of the availability and dispensing of the treatment drug.8,9
Ongoing Therapy for Methadone Addiction
Although the medical management of acute opioid withdrawal is an important component of recovery from methadone addiction, medical detoxification alone is not a substitute for more comprehensive addiction treatment.10 An important facet of medical detox, however, lies in facilitating a patient’s transition from the withdrawal management stage of early recovery to longer-term rehabilitation. Different behavioral health interventions will play a role not only in motivating the transition from detox to treatment, but in the types of therapeutic offerings found in the rehabilitation stage.
Living a better life after opioid addiction entails understanding how to better cope without continued nonmedical opioid use, how to manage maladaptive thoughts and other triggers to use again, and how to live more positively, productively, and healthily. In addition to medications, a comprehensive treatment approach for opioid use disorders may include ample cognitive behavioral-based therapy, psychoeducation, relapse prevention skills training, stress management techniques, interpersonal-process sessions, as well as peer-support group participation.7,10,11
- U.S. National Library of Medicine—DailyMed. (2008). Drug Label Information: DISKETS (methadone hydrochloride tablet).
- Miller, S. C., Fiellin, D. A., Rosenthal, R. N., & Saitz, R. (2019). The ASAM Principles of Addiction Medicine, Sixth Edition. Philadelphia: Wolters Kluwer.
- National Institute on Drug Abuse. (2018). Medications to Treat Opioid Use Disorder.
- S. Drug Enforcement Administration. (2019). Controlled Substances Schedules.
- Centers for Disease Control and Prevention. (2012). Prescription Painkiller Overdoses—Use and Abuse of Methadone as a Painkiller.
- Herron, J.H, & Brennan, T.K. (2015). The ASAM Essentials of Addiction Medicine, Second Edition. Philadelphia: Wolters Kluwer.
- Substance Abuse and Mental Health Services Administration. (2015). TIP 45: Detoxification and Substance Abuse Treatment.
- Substance Abuse and Mental Health Services Administration. (2019). Medication-Assisted Treatment—Buprenorphine.
- Stotts, A. L., Dodrill, C. L., & Kosten, T. R. (2009). Opioid dependence treatment: options in pharmacotherapy. Expert opinion on pharmacotherapy, 10(11), 1727–1740.
- National Institute on Drug Abuse. (2018). Principles of Drug Addiction Treatment: A Research-Based Guide (Third Edition).
- Substance Abuse and Mental Health Services Administration. (2017). TIP 43: Medication-Assisted Treatment for Opioid Addiction in Opioid Treatment Programs