Naltrexone And Opioid Addiction

Naltrexone is a medication approved by the FDA to treat opioid addiction, clinically known as opioid use disorder (OUD). OUD is defined by the inability to cut down or eliminate opioid use despite its harmful effects on multiple aspects of a person’s life.

One of the reasons why people continue to use opioids, despite having the desire to quit, is the strong cravings and urges from the dopamine rush associated with opioid use. Naltrexone, over time, modulates this opioid-fueled dopamine surge.

Naltrexone is an opioid receptor blocker that works on the mu opioid receptor to block opioids from binding to this receptor. If someone uses an opioid while on naltrexone, they will immediately experience withdrawal because naltrexone kicks opioids off the opioid receptors and blocks the symptoms of pain reduction, euphoria, and sedation. When a person no longer experiences these desirable effects, the cravings to use opioids quickly deplete, making naltrexone an effective tool in treating OUD.

The following are the benefits of using naltrexone to help treat opioid use disorder:

  • Naltrexone reduces cravings and urges for opioids
  • Naltrexone has few side effects and is generally well-tolerated
  • Can be taken long term
  • Can be stopped abruptly without any side effects

Side Effects Of Naltrexone

Like any medication, naltrexone does come with side effects; however, they are relatively minimal and generally disappear once your body adjusts to the medicine. Minor side effects that have been reported include:

  • Headache
  • Nausea
  • Fatigue
  • Mild abdominal pain
  • Trouble sleeping
  • Joint or muscle pain at the site of injection

Naltrexone should not be taken if the following conditions are present:

  • Any person who has opioids in their system
  • Any person in acute opioid withdrawal
  • Acute liver injury
  • Decompensated cirrhosis
  • Moderate or severe kidney disease

The Role Of Naltrexone In Maintenance, Detoxification, And Abstinence

People usually obtain opioid abstinence through a step-down approach that involves a progression from maintenance to detoxification and then abstinence. Maintenance usually involves medications such as methadone or buprenorphine as a replacement for strong prescription or illicit opioids as a way to provide stability by reducing cravings but preventing intense withdrawal effects. If a person and their treatment team’s goal is abstinence, then they will slowly be weaned off these medications through detoxification.

Detoxification usually involves an inpatient treatment team that provides medications to ease withdrawal symptoms as well as psychological support. Naltrexone can be given once the person is safely out of the withdrawal stage.

Naltrexone can be used as a long-term treatment medication to help prevent cravings and urges for long-term abstinence once the person has undergone detoxification. Obtaining abstinence for some people can be rapidly achieved, while others require the help of maintenance medication for longer than a few months before they choose to attempt abstinence.

Naltrexone works differently from other opioid use disorder (OUD) medications like buprenorphine and methadone. Those medications reduce cravings by activating opioid receptors in the brain. Buprenorphine is a partial opioid agonist, and methadone is a full opioid agonist, meaning they mimic some effects of opioids but with a lower risk of overdose. While they are highly effective and much safer than misusing opioids, they are still opioids and can lead to tolerance, dependence, and withdrawal.

In contrast, naltrexone is an opioid antagonist. Instead of activating opioid receptors, it blocks them, which helps reduce cravings and prevents the euphoric and sedative effects of opioids. Because naltrexone is not an opioid, it doesn’t cause physical dependence, withdrawal symptoms, or cravings when stopped, making it a suitable option for people who prefer not to take medication long-term.

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What Happens If I Take Naltrexone While There Are Opioids In My System?

Since naltrexone is an opioid antagonist and works by blocking the actions of opioids at their mu receptor, naltrexone will trigger opioid withdrawal if opioids are present in the system when naltrexone is administered.

These opioid withdrawals will occur immediately, clinically known as precipitated withdrawal. Therefore, it’s essential to refrain from taking opioids for a minimum of seven to ten days before taking naltrexone to reduce the risk of withdrawal. This is why the detoxification phase is extremely important and is highly recommended in a clinical setting, so a trained medical professional can monitor the opioid withdrawal side effects and administer medication if needed to help ease them.

Before starting naltrexone, some professionals may require that a person not exhibit any signs of opioid withdrawal and also perform a urine drug test to screen for any opioids in the system. They may even start a half dose of naltrexone before increasing to the therapeutic daily dose.

Can Naltrexone Cause Precipitated Withdrawal?

Yes, naltrexone can cause precipitated withdrawal if opioids are present in the body. This means that withdrawal symptoms will occur immediately. Opioid withdrawal side effects are not life-threatening but are very unpleasant and can entice the person to start using once again as a way to decrease these unwanted side effects. Opioid withdrawal side effects include the following:

  • Nausea
  • Vomiting
  • Chills
  • Abdominal pain

  • Sweating
  • Diarrhea
  • Muscle and bone pain
  • Anxiety

Reduced Tolerance And Risk Of Overdose

People taking naltrexone for opioid use disorder may have a reduced tolerance to opioids since they are no longer taking opioids. If they do relapse, after a period of abstinence, they may be unaware of how sensitive a lower dose can affect them. The dosage of opioids they were once using may have life-threatening consequences, such as respiratory arrest, because of their decreased tolerance. This can cause a deadly overdose.

If anyone is showing signs of opioid overdose, it is important to administer naloxone immediately and call 911.

Who Should Consider Naltrexone For Opioid Addiction Treatment?

Anyone interested in seeking treatment for opioid use disorder may consider treatment with naltrexone. The goal of naltrexone is to adopt abstinence, which requires a lot of dedication and a solid support system. It can also be used in conjunction with psychotherapy in an opioid treatment program. Psychotherapy can teach healthy coping strategies to overcome urges and cravings when they appear.

How Do I Get Naltrexone?

Naltrexone is a prescription medication that can be obtained from a licensed medical provider who is authorized to prescribe medications. Naltrexone for opioid use disorder is usually given in a supervised setting, or if your provider is 100% certain you are opioid free for at least 7 days and they have reviewed your treatment plan with you. Therefore, depending on where you are in treatment, the medication may be administered in an inpatient facility or at your home.

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Many rehab facilities incorporate naltrexone in their treatment for opioid use disorders. If you are ready to get help for your opioid addiction and explore your rehab options, contact a treatment provider today to learn more.