Opioid Replacement Therapy: A Guide

A successful drug abuse treatment program may include pharmaceuticals and behavioral therapies to help you or your loved one.

The Centers for Disease Control and Prevention has labeled prescription drug abuse an epidemic in the U.S., with over 263,000 Americans dying from prescription opioid overdoses from 1999–2020.

Tighter regulations of narcotic painkillers and the introduction of abuse-deterrent medications in recent years have made popular drugs, such as OxyContin, more difficult and expensive to obtain and crush to snort, smoke or inject.

Heroin, a dangerous opioid street drug especially common during the 1960s, has made a comeback. The number of heroin abusers jumped from 373,000–669,000 from 2007–2012, according to an article in TIME magazine. The number of heroin overdose deaths also increased by 45% from 2006–2010. 

Heroin and other street drugs are obtained by illegal or criminal means, which can lead to incarceration. The Bureau of Justice Statistics reported that in 2004, approximately 17% of state and 18% of federal prisoners committed their most recent offenses while trying to obtain money for drugs.

Injecting drugs is the most dangerous method of abuse with the most potential side effects, such as overdose, spread of infectious disease and engaging in criminal activities to obtain and use them. Violent behaviors and crime are often tied to IV drug users. Generally, individuals who inject drugs like heroin or struggle with heroin addiction have trouble retaining jobs and fulfilling family obligations. They also often have legal difficulties and health problems.

Opioid replacement therapy is a treatment option that seeks to replace dangerous drugs like heroin with legal and less euphoric, longer-acting opioids that decrease possible criminal behavior and the potential health risks associated with illicit drug abuse.

What Is Opioid Replacement Therapy?

Opioid replacement therapy, or medication-assisted treatment (MAT), is the gold-standard strategy for helping someone overcome an opioid addiction. In MAT, a short-acting opioid like heroin or fentanyl is replaced by a longer-acting prescription opioid like methadone or buprenorphine. This longer-acting opioid prevents cravings, helping you avoid relapse. Even if you slip up and take an illicit opioid, the long-acting MAT opioid will prevent you from getting high.

Two specific opioids are used in MAT:

• Methadone
• Buprenorphine (in Suboxone, Subutex, Butrans, Buprenex, Belbuca and Sublocade)

Sometimes, other medications may be prescribed to help a person stay away from opioids. These can include naltrexone (Vivitrol, ReVia), an opioid blocker that is an alternative for people who cannot take methadone or buprenorphine.

Types of Opioid Replacement Therapy

The two available types of opioid replacement therapy are methadone and buprenorphine-based products. While methadone is available on its own, buprenorphine is sold on its own or combined with the opioid blocker naloxone. Experts consider methadone and buprenorphine products first-choice agents for opioid replacement therapy.

Methadone 

Methadone is a full opioid agonist with a long half-life, meaning it can be dosed once daily. This medication has been used for many years for opioid replacement therapy because it does not have the same intoxicating effect as other short-acting opioids. Methadone can be dispensed at federally regulated clinics. Being an opioid agonist, methadone still binds to opioid receptors in the brain, activating them and, therefore, largely eliminating withdrawal symptoms and drug cravings.

Numerous studies have indicated that methadone maintenance therapy, or MMT, is an effective treatment for heroin dependence, increasing retention in substance abuse programs and reducing heroin abuse, as published in the Cochrane Database of Systematic Reviews.

The time spent in treatment has long been understood to be related to recovery rates. The more time you spend in an opioid addiction treatment program, the more successful your recovery will likely be.

Methadone is a Schedule II controlled substance by the Drug Enforcement Administration (DEA), indicating its medicinal use and potential for abuse. MMT provides a legal and less dangerous alternative to heroin or injection opioid abuse.

Long-term methadone use is not without its critics, however. Methadone is still an opioid and is often abused or misused with negative consequences. Methadone use should be closely supervised and monitored. It also should always be combined with psychotherapeutic methods to deter abuse, encourage abstinence from drugs and provide a sustainable method of opioid addiction recovery.

How Does Methadone Work

Methadone is a slow-acting opioid that takes up space at the brain’s opioid receptors, not letting other opioids access the receptors. This means other illicit opioids are ineffective at reaching the brain’s receptors to cause a high. Because the effect of other opioids is hampered, methadone helps you maintain abstinence.

Buprenorphine and Buprenorphine/Naloxone

In 2002, the U.S. Food and Drug Administration approved Subutex (buprenorphine) and Suboxone (buprenorphine/naloxone) through the Drug Abuse Treatment Act of 2000. Your doctor can prescribe these opioid dependency treatment medications as an alternative to methadone, which is only available at methadone clinics.

Buprenorphine is a partial opioid agonist that acts on opioid receptors in the brain to a lesser effect than full agonists, meaning it is effective in reducing drug cravings and withdrawal symptoms but does not produce euphoric or intoxicating feelings. Like methadone, buprenorphine has a longer half-life and can remain in your system for 24–72 hours. It also has a ceiling effect, which means that even if you take more to achieve a high, the effects will plateau at a certain level. Subutex and Suboxone are sublingual film strips that are difficult to alter and abuse.

Subutex contains primarily buprenorphine, and it is often used during opioid detox. Suboxone is four parts of buprenorphine and one part of naloxone, which is a partial opioid antagonist, meaning it blocks opioids from receptors in the brain and can precipitate withdrawal if injected or abused with other opioids.

Another buprenorphine/naloxone product approved by the FDA in 2013 is Zubsolv, which comes in tablet form.

The DEA classifies buprenorphine as a Schedule III controlled substance and published that 9.3 million buprenorphine prescriptions were dispensed in 2012. Like methadone, buprenorphine can increase retention in substance abuse treatment programs while potentially reducing relapse and helping people lead fulfilling and productive lives.

The National Survey on Drug Use and Health (NSDUH) estimates that 43.7 million Americans 12 and older needed treatment for a substance abuse or dependency issue as of 2021. Opioid replacement therapy can help you reach a healthy and stable physical level. It should be combined with psychotherapies and counseling sessions to address the emotional components of drug abuse and addiction.

A successful drug abuse treatment program may include pharmaceuticals and behavioral therapies to help you or your loved one retrain your brain and make healthy lifestyle choices.

The Recovery Village is a frontrunner in evidence-based treatment models. Highly trained professionals utilize traditional and alternative methods to help encourage lifelong recovery. Admission specialists are standing by to answer any questions you may have about the range of substance abuse treatment programs offered. Reach out today for more information.

How Does Buprenorphine Work?

Buprenorphine partially activates the brain’s opioid receptors, blocking cravings and effects of illicit opioids with less risk of side effects than methadone.

When naloxone is combined with buprenorphine in products like Suboxone, the naloxone component remains inert when the drug is taken as directed by mouth. However, if someone attempts to dissolve and inject the drug to get high, the naloxone activates, blocking buprenorphine’s effects.

Benefits of Opioid Replacement Therapy

For someone trying to quit illicit opioids, opioid replacement therapy, known as medication-assisted treatment (MAT), is the top choice for treating addiction. Data show that opioid replacement therapy combined with rehab has the best chance of helping you reach — and keep — abstinent from opioids. Several specific benefits of opioid replacement therapy help it achieve those goals.

1. Help To Manage Opioid Withdrawal Symptoms

As opioids themselves, opioid replacement therapy with methadone or buprenorphine helps control opioid withdrawal symptoms. Because you are on a safer, longer-acting opioid, you can minimize or avoid withdrawal symptoms as your body is weaned from the illicit opioid.

2. Improves Social Functioning and Interactions During Treatment

Because buprenorphine and methadone products are designed to avoid making you high, it is easier to function while taking them. This means that people on buprenorphine or methadone can function normally, even attending work or school while on the medication.

3. Opioid Replacement Therapy Increases the Odds of Long-Term Recovery

Opioid replacement therapy has been linked to a much greater chance of long-term recovery than abstinence attempts alone. For this reason, sometimes your doctor may recommend you continue on opioid replacement therapy indefinitely.

4. Risk Reduction Due to Injection of Opioids

Because opioid replacement therapy blocks the effects of other opioids, it is very hard to get high from illicit opioids, even if you inject them. This dampened effect of illicit opioids helps break the pattern of compulsive opioid use, helping you overcome your addiction.

Challenges of Opioid Replacement Therapy

Opioid replacement therapy isn’t without its challenges. Although experts agree that the benefits of opioid replacement therapy outweigh the risks for many people, it is still important to prepare for the downsides.

1. Slow Opioid Treatment

Opioid replacement therapy isn’t a silver bullet but a slow, long-term strategy for helping you overcome your opioid addiction. As such, you will likely need to remain on opioid replacement therapy over the long term, even indefinitely in some cases.

2. Opioid Addiction Emotional and Psychological Factors Are Not Impacted by Opioid Replacement Therapy

Although opioid replacement therapy can dampen your opioid cravings and reduce your relapse risk, it cannot address the emotional components of an addiction. For example, anxiety and depression occur frequently in addiction and cannot be treated by opioid replacement therapy. Instead, a dual-diagnosis rehab program can help.

3. Opioid Replacement Therapy Should Be Used Alongside Other Forms of Treatment 

Opioid replacement therapy on its own is often not sufficient to overcome an addiction. Instead, experts recommend pairing it with behavioral treatments like psychosocial counseling and community-based services. 

4. The Opioid Replacement Solution May Create an Addiction to the Substitute Medications

Because opioid replacement therapy consists of opioids, a person can sometimes become addicted to the methadone or buprenorphine prescribed to help them overcome addiction in the first place.

Opioids and the Brain

Short-acting, opioid-containing drugs, such as heroin, Vicodin and Percocet, have relatively short half-lives, meaning they take effect quickly and leave the bloodstream within a few hours. Regular use of opioids can create a tolerance to them, so people will need to take higher doses each time to produce the desired effects. This can also lead to a dependence on opioids, as regular use alters the brain’s motivation and reward centers and pathways.

Opioid drugs act on opioid receptors in the brain that are partially responsible for emotional regulation and pain sensations. When the production of natural neurotransmitters, or the brain’s chemical messengers, is disrupted with repeated opioid drug use over time, changes occur in the brain’s chemical pathways, as the brain will now rely on the drugs instead of naturally occurring chemicals.

When opioids are removed, drug cravings and uncomfortable withdrawal symptoms will set in as the brain struggles to regain balance without drugs. These withdrawal symptoms are physical and psychological and will differ in intensity and duration depending on the type of drug taken, length of time abused, amount taken, method of abuse and personal physiological factors.

Opioid withdrawal symptoms often include:

• Nausea and/or vomiting
• Diarrhea
• Abdominal cramps
• Muscle aches
• Sweating and chills
• Runny nose
• Yawning
• Dilated pupils
• Increased heart rate
• Restlessness
• Anxiety
• Depression
• Irritability
• Trouble sleeping
• Drug cravings

In many cases, these negative side effects are so uncomfortable that people will start using opioids again to relieve the symptoms of opioid withdrawal. To help lower the risk of repeat use, opioid abuse should not be stopped suddenly. Instead, opioids with longer half-lives can be introduced to engage opioid receptors without producing a high, allowing the individual to detox and regain healthy brain function gradually. For optimal results, detox, or removing opioid drugs from the system, should be monitored by a medical professional and undergone at a specialized detox facility.

Medical detox programs may be inpatient, where you stay on-site and receive 24-hour medical supervision, or outpatient, where you go home to sleep at night. The use of medications during detox to relieve opioid withdrawal symptoms is called medically assisted detox. Patients undergoing medically assisted detox should be closely monitored and continually reevaluated to ensure the safety and effectiveness of the treatment. Opioid replacement therapy usually utilizes methadone or buprenorphine/naloxone during medical detox and maintenance treatment programs. These are longer-acting opioids that stay in the system for prolonged periods.

Opioid Addiction Treatment

The Recovery Village offers a continuum of services to help you overcome opioid addiction. This means we support you every step through all stages of your recovery:

• Medical detox: This is the first step in overcoming your addiction. In medical detox, you are weaned off illicit opioids, with MAT prescribed if medically appropriate.
• Rehab: Starting with inpatient rehab and progressing through partial hospitalization and outpatient rehab, we offer group therapy and a sober living environment to help you address the core issues that led to your addiction.
• Aftercare: Even after rehab, aftercare keeps your focus on your continued sobriety through alumni and support groups and continued therapy.

How The Recovery Village Treats Opioid Addiction?

The Recovery Village believes in treating addiction holistically: not only treating the opioid cravings themselves but also the root causes of your addiction. By focusing on helping you recover and create healthy new habits, we help you overcome your addiction and put you on the road to a lifelong recovery. Don’t wait: contact us today to learn more.

Editor – Theresa Valenzky

Theresa Valenzky graduated from the University of Akron with a Bachelor of Arts in News/Mass Media Communication and a certificate in psychology. She is passionate about providing genuine information to encourage and guide healing in all aspects of life. Read more

Medically Reviewed By – Dr. Jessica Pyhtila, PharmD

Dr. Jessica Pyhtila is a Clinical Pharmacy Specialist based in Baltimore, Maryland with practice sites in inpatient palliative care and outpatient primary care at the Department of Veteran Affairs. Read more