What is Naltrexone?
The opioid antagonist Naltrexone (brand names: ReVia, Vivitrol, and Depade) is a medication that is FDA-approved to treat those who suffer from alcohol use disorders and opioid use disorders. The drug comes in a pill form (Depade and the more popular version ReVia) and as an extended-release injectable form (Vivitrol). Naltrexone is designed to reduce and suppress cravings for alcohol or opiate drugs. It does this by binding to the opioid receptors in the person’s brain (thereby removing any opiate drugs on these receptors) and suppressing cravings.
Naltrexone is considered to have no abuse potential and does not result in the development of physical dependence. An individual must obtain a prescription to legally obtain it, and the medication is typically used in situations where individuals are actively recovering from alcohol use disorders or opiate abuse.
Naltrexone does not treat withdrawal symptoms; instead, it is designed to suppress cravings for alcohol or opiate drugs. Individuals with moderate to severe alcohol use disorders who are using naltrexone may experience withdrawal symptoms if they stop drinking that can be potentially fatal due to the development of seizures. These individuals should consult with an addiction medicine physician or psychiatrist before discontinuing their use of alcohol.
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Intramuscular extended-release Naltrexone is a prescription drug approved by the Food and Drug Administration (FDA) as a medication-assisted treatment (MAT) option for both opiate addiction treatment and alcoholism treatment. Vivitrol is the brand name of Naltrexone. Vivitrol shot can be used to help people maintain abstinence while recovering from alcohol use disorder or heroin addiction. While naltrexone hydrochloride is for both daily and once-a-month dosages, Vivitrol is injected once a month.
Naltrexone (Vivitrol) can be prescribed and administered by any medical practitioner licensed to prescribe medications. It is available in a pill form for alcohol use disorder or as an extended-release intramuscular injectable for either alcohol or opioid use disorder.
A Risk Evaluation and Mitigation Strategy (REMS) is required for the long-acting injectable formulation to ensure that the benefits of the prescription drug outweigh its risks. The pill form can be taken daily for alcoholism treatment, but the extended-release injectable formulation is only approved for opioid or heroin addiction treatment. The pill form is taken daily and the extended-release injectable is administered every four weeks, or once a month, by a medical practitioner.
Is Naltrexone Addictive?
Naltrexone functions by blocking the effect that opioids, such as heroin or opioid prescription drugs, have on the brain. It reduces the cravings that many individuals experience after they quit. With alcohol, it is not certain how Naltrexone works, but it seems to change how the brain responds to alcohol consumption. Is Naltrexone Addictive? No. Naltrexone is not habit-forming or a drug of abuse. In addition, it does not cause users to become physically or psychologically dependent.
There is an opioid epidemic occurring in the U.S. Drug overdoses in 2016 killed more Americans than the entire Vietnam War. In 2016 it was estimated that as many as 65,000 people died from drug overdoses. Even as lawmakers and health officials try to find solutions to the tens of thousands of lives lost each year from opioids, the numbers continue to rise.
Why are opioids so dangerous? These drugs bind to opioid receptors in the central nervous system which cause a euphoric high, but also respiratory depression. That respiratory depression can cause a coma or death during an overdose. There is no way to know what’s being bought on the streets, either. Increasingly, many products are laced with fentanyl, which is highly potent and deadly.
Opioids are problematic not just because of respiratory depression, but also because they’re extremely physically and psychologically addictive. Once someone takes opioids, whether it’s prescription painkillers or heroin, there are certain chemicals released in the brain that trigger a very rapid descent into addiction. It’s easy and takes very little time for many people to lose control of their intake of opioids.
Dealing with an opioid addiction typically requires a comprehensive treatment program, because of the complexity of addiction. Naltrexone is one potential component of a treatment program. Naltrexone is a prescription medicine that can be used in medication-assisted treatment or MAT. Naltrexone is FDA-approved to aid in opioid addiction as well as alcohol use disorder. This medication is available as a pill and also as a once-monthly injection.
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Side Effects Of Naltrexone
Naltrexone is considered safe to use and associated with few side effects; however, all medications have a side effect profile. Side effects as a result of naltrexone use are reported to be relatively rare, but they do occur in some instances. Some include:
- Individuals should not use opiate drugs while taking naltrexone. People who use opiate drugs and take naltrexone may experience opioid withdrawal symptoms as naltrexone is an opioid antagonist. The Food and Drug Administration (FDA) recommends that individuals who use naltrexone should be abstinent from opioid drugs for a week to 10 days. Because naltrexone is an opioid antagonist, people using it and who also use opioid medications for their psychoactive effects will not experience the typical “high” that they get from opiate drugs. This may result in individuals taking more opiate drugs than they normally would and potentially overdosing on opiates.
- Nausea, stomach cramps, and diarrhea are the most common reported side effects; however, these typically resolve over time.
- Some individuals may experience muscle stiffness, cramps, and headaches.
- Sleep disruptions (including both insomnia and hypersomnia), anxiety, and dizziness have also been reported.
- Pregnant women should not use naltrexone.
Long-Term Effects Of Naltrexone
Medication-assisted treatments can have short- and long-term side effects. Short-term side effects of naltrexone may include:
In rare cases, naltrexone users may have serious side effects such as:
- Severe vomiting or diarrhea
- Blurry vision
- Extreme confusion
- Muscle or joint pain
- Poor appetite
- Depressed mood
- Changes in sleep
- Changing energy levels
For some users, naltrexone may cause:
- Liver damage. The risk of liver damage may increase with higher doses of naltrexone and for people with a history of hepatitis or liver disease.
- Allergic pneumonia.
- Infections or skin reactions. Users who take Vivitrol (the injectable form of the drug) may have reactions at the injection site that require medical evaluation.
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Naltrexone Drug Interactions
You should not use naltrexone treatment if:
- You are receiving opioid (narcotic) analgesics.
- If you are in an acute opioid withdrawal or have any symptoms of opioid withdrawal.
- If you have failed a naloxone challenge test or have a positive urine screen for opioids.
- You have acute hepatitis or hepatic failure.
- If you are allergic or have had a hypersensitivity reaction to naltrexone, polylactide-co-glycolide (PLG), or any other diluent or inactive ingredient in the product.
Tell your doctor or other health care provider of any recent use of opioids or any history of opioid dependence before starting naltrexone to avoid having an opioid withdrawal. Your doctor may require that you pass a naloxone challenge test and/or a urine screen for opioids before naltrexone use.
People using naltrexone should not:
- Use ANY opioid (heroin, morphine, codeine, oxycodone, tramadol, hydrocodone, or other prescription or illegal opioids)
- Use illicit drugs
- Drink alcohol
- Take CNS depressants such as sedatives, tranquilizers, or other drugs.
If you attempt to self-administer opioids, in small doses while on naltrexone, you will not perceive any effect. Naltrexone blocks the euphoric and sedative effects of the abused drug and prevents feelings of euphoria (“high”). However, using large doses of any opioid to try to bypass the opioid-blocking effect of naltrexone may lead to serious injury, overdose, coma, or death. You may be more sensitive to smaller doses of opioids once you stop using them, so taking any dose of an opioid can be dangerous.
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Naltrexone for opioid and alcohol dependence
For Opioid Dependence
Naltrexone is an opioid antagonist with the highest affinity for the mu-opioid receptor. Naltrexone has little or no opioid agonist activity. It is believed that the occupation of opioid receptors by naltrexone may block the effects of endogenous opioid peptides. In addition, it markedly attenuates or completely blocks, reversibly, the subjective effects of exogenous opioids. This makes the blockade produced potentially surmountable. Naltrexone has few, if any, intrinsic actions besides its opioid blocking properties.
For Alcohol Dependence
Occupation of opioid receptors by naltrexone may block the effects of endogenous opioid peptides. Thus, it markedly attenuates or completely blocks, reversibly, the subjective effects of exogenous opioids. The neurobiological mechanisms responsible for reducing alcohol consumption observed in alcohol-dependent clients treated with naltrexone are not entirely understood. However, the involvement of the endogenous opioid system is suggested by preclinical data.
Vivitrol is not suitable for everyone. In addition, there are significant risks from Vivitrol shots, including the risk of opioid overdose, injection site reactions, and sudden opioid withdrawal.
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 Substance Abuse and Mental Health Services Administration. (2015). Medication and counseling treatment.
 Center for Substance Abuse Treatment. (2009). Incorporating alcohol pharmacotherapies into medical practice. HHS Publication No. (SMA) 09-4380. Rockville, MD: Substance Abuse and Mental Health Services Administration.
 National Institute on Drug Abuse. (2014). Principles of adolescent substance use disorder treatment: A research-based guide.
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