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Medications for Heroin Addiction and Detox

Several medications are used to treat addiction to heroin and other opioids such as oxycodone. These drugs are used to help people maintain abstinence and decrease cravings for opioids. Often, they are combined with counseling and other behavioral therapeutic approaches as part of a comprehensive substance abuse treatment program.
Though these medications are FDA-approved for the management of opioid dependence, they come with some side effects and risks that users should be aware of.

What Do These Medications Do?

The 3 major medications used to treat heroin addiction are methadone, buprenorphine (in combination with naloxone as Suboxone), and naltrexone (ReVia, Vivitrol). They help to block the euphoric effects of heroin, relieve cravings, and help the body and brain adjust to no longer having the drug in the system.1
medical drug and needle
These drugs are used as part of a medication-assisted treatment (MAT) regimen, which combines medications with therapy and counseling to help people recover from addiction to heroin and other opioids. Studies show that the combined approach of behavioral intervention and medication is effective at reducing drug use, improving retention in treatment, and reducing HIV transmission.1 In areas where access to MAT services are expanded, the rates of overdose fatalities have declined.2

Only trained health care professionals can make the call on which medication is the most appropriate as part of treatment, and under what conditions a person should withdraw or stop using medication.3

MAT is supported by the Substance Abuse and Mental Health Services Administration (SAMHSA), the Institute of Medicine, and the World Health Organization. Although decades of research demonstrate that the benefits of MAT outweigh the risks, studies confirm that MAT continues to be underused and access to programs remains limited.2,3,4 


Methadone is a synthetic opioid agonist drug. It produces similar effects as morphine, and chronic misuse can result in dependence.5 The drug comes in pill, liquid, and wafer forms. When used as prescribed to manage substance dependence, methadone blocks the euphoric effects of heroin and other opioids, eases withdrawal symptoms, and changes how the brain responds to pain.6

Any licensed doctor can prescribe methadone to treat pain. But methadone may only be dispensed for heroin addiction at licensed methadone treatment programs or opioid treatment programs (OTPs). Almost 95% of OTPs are outpatient programs that offer medication along with behavioral therapies.3

Though methadone is largely safe, side effects can occasionally be serious and include the following:6

  • Difficulty breathing
  • Chest pain
  • Hives or a rash
  • Lightheadedness
  • Hallucinations
  • Confusion
  • Swelling of the face, lips, tongue, or throat
  • Fast or pounding heartbeat

It is possible to overdose on methadone. A person may suffer the following effects:5

  • Respiratory arrest
  • Circulatory collapse
  • Cardiac arrest
  • Death

Methadone has been deemed safe for use in the management of opioid dependence in pregnant women. It helps to prevent withdrawal symptoms, which can decrease the risk of early uterine contractions, premature birth, or miscarriage. Studies show that, while a small amount of methadone does enter breast milk, the benefits of breastfeeding while being treated far outweigh the risks.6

If you are pregnant or breastfeeding and thinking about methadone management for opioid dependence, talk to your doctor first.6


Buprenorphine is a partial opioid agonist drug. It is available as a tablet or dissolvable film form. Buprenorphine is a relatively long-acting opioid, and some people do not have to take it every day. Each dose of buprenorphine increases the effects of the drug until, eventually, the effects level off. This is sometimes referred to as a “ceiling effect,” and it lowers the risk of dependency, abuse, and side effects.7

Buprenorphine is often prescribed as a combination medication along with naloxone. The FDA has approved the following buprenorphine products for the treatment of opioid dependence:7

  • Bunavail (buprenorphine and naloxone)
  • Suboxone (buprenorphine and naloxone)
  • Zubsolv (buprenorphine and naloxone)
  • Generic buprenorphine-containing transmucosal products for opioid addiction

In May 2016, the FDA approved an implantable form (Probuphine) of buprenorphine that delivers a low dose of buprenorphine for 6 months.3

Buprenorphine can be prescribed by doctors who have met Controlled Substances Act requirements and have a waiver. In the first year after they receive the waiver, doctors can provide the treatment to only 30 people. After the first year, doctors can request to treat up to 100 people. However, these limits do not apply to OTPs that dispense buprenorphine on-site.3

Research shows that even though there are nearly 435,000 primary care physicians across the country, roughly only 30,000 have a waiver to provide buprenorphine. In an effort to expand access, on July 8, 2016, Congress ruled that eligible physicians could request approval to treat up to 275 patients.3

Side Effects

Using buprenorphine can result in the following side effects:7

  • Cravings
  • Insomnia
  • Irritability
  • Fever
  • Nausea
  • Vomiting
  • Constipation
  • Muscle aches

Despite the ceiling effect, it is possible to overdose on buprenorphine—particularly if the drug is used with sedatives and/or alcohol.3 Overdose symptoms include pinpoint pupils, pronounced drowsiness, dizziness, blurred vision, and slowed breathing.8

There is limited evidence on the efficacy and safety of buprenorphine for use by pregnant women. However, case reports do not demonstrate any significant problems from use of buprenorphine during pregnancy. Pregnant women should use buprenorphine or Suboxone only if their doctor deems that the benefit outweighs the potential risk to the fetus. Breastfeeding is not advised in women being treated with buprenophine.9

It is possible for people to switch from using methadone to using buprenorphine. Studies have shown that buprenorphine is equally as effective as moderate doses of methadone but may not be as effective for people with strong physical dependence. If you are thinking of switching from one of these drugs to the other, discuss this with your doctor.7 


Naltrexone is an opioid antagonist that does not produce opioid-like effects and has no misuse liability. It blocks other drugs from attaching to opioid receptors in the brain and also stops the effects of other opioids in a person’s body, which can lead to withdrawal. For use in cases of opioid dependence, it may be administered 2 ways—as an oral tablet or an extended-release injectable.10

Naltrexone is often used when a person has completed methadone or buprenorphine treatment and wants to stop taking these medications, but still discourage relapse. It can also be an appropriate treatment for people who have detoxed and completed a rehabilitation program, and are going back into an environment where they may be exposed to drug use.3

Side effects of naltrexone may include:10

  • Headache.
  • Nervousness.
  • Upset stomach.
  • Vomiting.
  • Diarrhea.
  • Sleep problems.
  • Tiredness.
  • Joint or muscle pain.
  • Opioid withdrawal (if opioids are still actively being used).

Those who experience side effects should talk to their health care provider or substance abuse counselor to change the dose or discontinue the medication.10

Any healthcare provider can prescribe naltrexone without special training. Like all MAT medications, naltrexone should be incorporated into a comprehensive treatment plan, including counseling and social support programs.10

Other Medications for Detox

Many medications are used off-label during heroin withdrawal to help with common symptoms such as insomnia and depression.

Below are a few examples of commonly used medications:11

  • Clonidine: This medication relieves some opioid withdrawal symptoms but is not as effective in relieving symptoms such as insomnia, muscle and bone pain, cravings, and headache.
  • Antidepressants: Medications such as Zoloft, Celexa, and Lexapro may be prescribed if someone develops depression during withdrawal.
  • Sleep medications: Medications such as diphenhydramine (Benadryl) or trazodone can help people sleep.
  • Anti-diarrhea medication: Diarrhea is a common withdrawal symptom, and people may use over-the-counter medications such as bismuth subsalicylate (Pepto-Bismol) to help manage it.

If you’d like to learn more about rehab programs that offer medication-assisted treatment, contact our helpline today.

Let’s verify your coverage for treatment at an American Addiction Centers location. Your information is always confidential.


1Substance Abuse and Mental Health Services Administration. (2015). Medication and Counseling Treatment. 

2 Olsen, Y., & Sharfstein, J. M. (2014). Confronting the stigma of opioid use disorder—and its treatmentJama311(14), 1393-1394.

3 Substance Abuse and Mental Health Services Administration. (2016). Facing addiction in America: The Surgeon General’s report on alcohol, drugs, and health.

4 National Council for Integrated Health. (2014). Expanding the Use of Medications to Treat Individuals With Substance Use Disorder in Safety-Net Settings.

5 DrugBank. (2018). Methadone.

6 Substance Abuse and Mental Health Services Administration. (2015). Methadone.

7 Substance Abuse and Mental Health Services Administration. (n.d.). Buprenorphine.

8 U.S. National Library of Medicine. (2018). Buprenorphine Sublingual and Buccal (opioid dependence).

9 Food and Drug Administration. (n.d.). Suboxone.

10 Substance Abuse and Mental Health Services Administration. (2016). Naltrexone.

11 Substance Abuse and Mental Health Services Administration. (2013). Detoxification and Substance Abuse Treatment.

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