Naltrexone is a proven, FDA-approved medication used to treat Alcohol Use Disorder (AUD) by reducing cravings and the rewarding effects of alcohol. It works by blocking the brain’s opioid receptors, making alcohol less pleasurable and helping individuals stay committed to recovery without developing a new dependency. In states like Ohio, where AUD affects over 500,000 residents annually, medications like naltrexone play a critical role in recovery.
Treatment begins after a person has detoxed from alcohol or opioids to prevent withdrawal complications. Naltrexone is available as a daily oral tablet (50 mg) or a long-acting monthly injection (380 mg), offering flexible options to support adherence. While side effects such as nausea, headache, and drowsiness are relatively common, rare but serious risks like liver damage must be monitored.
What Is Naltrexone?
Naltrexone is a non-addictive medication that helps you manage alcohol dependence and opioid use disorder by blocking the brain’s opioid receptors. This action stops the euphoric and sedative effects of alcohol and opioids, reducing cravings and lowering the risk of relapse.
It’s available as Revia (daily oral tablet) or Vivitrol (monthly injection), giving you flexible options depending on your treatment plan. Unlike methadone or opioids, naltrexone doesn’t cause a high or lead to physical dependence, making it a safer long-term choice.
Used as part of medication-assisted treatment (MAT), it works best when combined with counselling and support. With proper medical guidance, naltrexone helps you stay focused on recovery without replacing one substance with another.
How Is Naltrexone Consumed?
Naltrexone is consumed in two primary forms: oral tablets and intramuscular injections. The oral tablet (ReVia) is taken daily, while the injectable form (Vivitrol) is administered monthly. Both forms require strict adherence to dosing schedules to ensure effectiveness.
Ways naltrexone is consumed include the following:
- Oral tablet: Taken once daily with a full glass of water, with or without food to minimize gastrointestinal discomfort 347.
- Intramuscular injection: Administered by a healthcare provider into the gluteal muscle every 4 weeks (380 mg dose), alternating buttocks for subsequent injections 268.
Adherence to prescribed schedules is critical; missing doses reduces efficacy, and opioid use must be avoided for 7–10 days before starting naltrexone.
What Is the Mechanism of Action of Naltrexone?
The mechanism of action of Naltrexone works by blocking the brain’s opioid receptors, especially the mu receptors (MORs), and also affects kappa (KOR) and delta (DOR) receptors.
Occupying these sites prevents opioids and alcohol from triggering the brain’s reward system, stopping the euphoria, pain relief, and other reinforcing effects that fuel addiction.
This blockade interrupts the cycle of craving and reward, making it harder for substances to deliver the effects your brain expects. Naltrexone also helps reduce alcohol cravings by modulating the endogenous opioid system, which plays a role in how alcohol affects the brain.
With its long-lasting receptor coverage, naltrexone offers steady protection, supporting recovery by removing the chemical “reward” tied to substance use.
Which Addiction Treatment Is Naltrexone Used in?
Naltrexone is used in addiction treatment for alcohol use disorder and opioid use disorder. These involve medication-assisted therapy, craving reduction mechanisms, and relapse prevention strategies.
The addiction treatment naltrexone is used in are explained below:
Alcohol Use Disorder
Alcohol use disorder is a chronic condition characterized by an inability to control alcohol consumption despite negative consequences. According to the Centers for Disease Control and Prevention (CDC), Pennsylvania’s alcohol poisoning death rate stands at 6.5 per 1 million people.
Naltrexone is used in alcohol addiction treatment by reducing the craving for alcohol and decreasing the pleasure associated with drinking.
Opioid Addiction
Opioid Addiction or Opioid use disorder involves the compulsive use of opioids, leading to significant impairment or distress. Naltrexone is used to treat opioid use disorder by blocking the effects of opioids, thereby preventing opioid-induced euphoria and intoxication. The main benefits of naltrexone in opioid addiction include reducing the risk of relapse and helping individuals maintain abstinence.
What Is the Recommended Dosage for Naltrexone?
The recommended dosage of Naltrexone is 50 mg once daily for both alcohol dependence and opioid use disorder. Alternative dosing schedules: 100 mg every other day or 150 mg every third day.
The extended-release injectable formulation contains 380 mg administered intramuscularly in the gluteal area once monthly for both conditions. Patients require a 7-10 day opioid-free period before initiating treatment, confirmed through a naloxone challenge test.
What Are the Side Effects of Naltrexone?
The side effects of Naltrexone include nausea, headaches, dizziness, drowsiness, muscle discomfort, anxiety, digestive disturbances, and sleep problems, which are considered common reactions to the medication.
Here are the side effects of Naltrexone in detail below:
- Nausea and Vomiting: Nausea is an uncomfortable sensation in the stomach that leads to the urge to vomit. These effects occur as a response to Naltrexone treatment, impacting the patient’s comfort and adherence to the medication.
- Headache: A headache is characterized by pain or discomfort in the head or neck region, which varies in intensity and duration. As a side effect of Naltrexone, headaches arise from changes in brain chemistry or other physiological reactions to the medication.
- Dizziness: Dizziness is a sensation of lightheadedness or unsteadiness that affects balance and coordination. In the context of Naltrexone use, dizziness results from alterations in blood pressure or central nervous system activity.
- Drowsiness or Fatigue: Drowsiness refers to an increased tendency to sleep or a lack of energy. These side effects hinder daily activities and are associated with the sedative effects of Naltrexone on the central nervous system.
- Muscle Pain or Cramps: Muscle pain, known as myalgia, involves discomfort or soreness in the muscles, while cramps are involuntary muscle contractions that cause sharp pain.
- Nervousness or Anxiety: Nervousness is a feeling of unease or apprehension. Naltrexone influences neurotransmitter levels, contributing to these psychological side effects.
- Sleep Disturbances (insomnia or excessive sleepiness): Sleep disturbances encompass disruptions in normal sleep patterns, including insomnia. These effects are linked to Naltrexone’s influence on sleep-regulating neurotransmitters and overall sleep architecture.
What Are the Alternatives to Naltrexone?
The alternatives to Naltrexone include buprenorphine, methadone, acamprosate, disulfiram, topiramate, gabapentin, and nalmefene. These medications offer various approaches to managing addiction, from partial opioid agonists to deterrents that create negative associations with alcohol.
Here are the main alternatives to Naltrexone:
Buprenorphine
Buprenorphine is a partial opioid agonist used primarily in the treatment of opioid addiction. It works by binding to opioid receptors in the brain, reducing cravings and withdrawal symptoms without producing the same intense euphoria as full opioid agonists. This “ceiling effect” reduces the risk of overdose, making it a safer option for many individuals.
Methadone
Methadone is a full opioid agonist and is also used for opioid addiction treatment. It effectively reduces opioid cravings and withdrawal, stabilizing individuals with severe opioid dependence. While it carries a risk of overdose, when administered under strict medical supervision, it significantly improves quality of life and reduces illicit opioid use.
Acamprosate (Campral)
Acamprosate is a medication specifically used for alcohol dependence. It works by stabilizing the chemical imbalances in the brain that occur due to chronic alcohol use. This stabilization helps reduce alcohol cravings and withdrawal symptoms, supporting individuals in maintaining abstinence.
Disulfiram (Antabuse)
Disulfiram acts as a deterrent to alcohol consumption. It interferes with the body’s metabolism of alcohol, causing unpleasant side effects like nausea, vomiting, and flushing if alcohol is ingested. This creates a strong negative association with alcohol, helping individuals avoid relapse.
Topiramate (Topamax)
Topiramate, originally an anticonvulsant, has shown effectiveness in treating alcohol addiction. It helps reduce alcohol cravings and withdrawal symptoms, potentially by modulating neurotransmitter activity in the brain. Its use supports individuals in reducing alcohol consumption and maintaining abstinence.
Gabapentin (Neurontin)
Gabapentin, another anticonvulsant, is sometimes used in alcohol addiction treatment to manage withdrawal symptoms and reduce cravings. It helps alleviate certain discomforts associated with withdrawal, potentially making it easier for individuals to maintain abstinence.
Nalmefene
Nalmefene is an opioid antagonist, similar to naltrexone, and is used in the treatment of alcohol dependence. It works by blocking opioid receptors in the brain, which reduces the rewarding effects of alcohol and helps individuals decrease their consumption.
Can You Take Disulfiram and Naltrexone Together?
Yes, you can take disulfiram and naltrexone together, but careful medical supervision is necessary due to potential risks and interactions.
Both medications treat alcohol dependence but work differently: disulfiram creates an aversion to alcohol by causing unpleasant side effects when alcohol is consumed, while naltrexone reduces cravings and the pleasurable effects of alcohol by blocking opioid receptors
Can You Take Acamprosate And Naltrexone Together?
Yes, you take acamprosate and naltrexone together. These medications work through different mechanisms to address alcohol dependence, with acamprosate stabilizing brain chemistry to reduce withdrawal symptoms and naltrexone blocking the pleasurable effects of alcohol.
How Does Naltrexone Work For Alcohol Addiction Treatment?
Naltrexone works for alcohol addiction treatment by reducing the pleasurable effects and cravings associated with alcohol consumption.
It functions as an opioid antagonist, meaning it blocks the brain’s opioid receptors, which are involved in the rewarding effects of alcohol. By diminishing the brain’s association between alcohol and pleasure, naltrexone helps decrease the desire to drink and makes alcohol consumption less reinforcing.
This mechanism allows individuals to reduce their alcohol use gradually and supports their efforts to maintain sobriety. Importantly, naltrexone does not eliminate cravings or withdrawal symptoms but instead weakens the rewarding “buzz” linked to alcohol, making it easier for individuals to control their drinking behavior.
Who Should Avoid Taking Naltrexone?
Taking Naltrexone should be avoided if you actively use opioid medications, have acute hepatitis or liver disease, or are pregnant or breastfeeding without medical approval. Naltrexone worsens liver conditions and presents uncertain risks during pregnancy and lactation.
People who should avoid taking naltrexone are explained below:
- Individuals currently using opioids: Contraindicated due to the risk of precipitated withdrawal. Naltrexone blocks opioid receptors, causing abrupt withdrawal symptoms if opioids are present in the system.
- Patients with acute hepatitis or severe liver disease: Contraindicated because naltrexone is metabolized in the liver, increasing the risk of toxicity and liver damage.
- Pregnant or breastfeeding individuals: Use only if benefits outweigh risks. Limited safety data suggest potential risks to fetal development or infants, requiring medical evaluation.
Can You Use Naltrexone While Still Taking Opioids?
No, you cannot use naltrexone while still taking opioids because it triggers precipitated withdrawal. Naltrexone blocks opioid receptors, and if opioids are present in the body, this blockade forces the drugs to detach abruptly, causing intense withdrawal symptoms.
Can You Drink Alcohol While on Naltrexone?
Yes, you can drink alcohol while on Naltrexone because it does not cause adverse reactions like disulfiram. While drinking alcohol while on Naltrexone is physically safe, it diminishes the medication’s effectiveness if the goal is to reduce alcohol consumption.
Is Naltrexone A Controlled Substance?
No, naltrexone is not a controlled substance in Pennsylvania. It is not classified as a narcotic and does not carry a risk of addiction, misuse, or dependence. According to the Controlled Substances Act, naltrexone is unscheduled, meaning it is not subject to the same regulatory restrictions as controlled substances like opioids or benzodiazepines.
Do You Need a Prescription for Naltrexone?
Yes, you need a doctor’s prescription for Naltrexone in Pennsylvania because it is a prescription-only medication. It must be obtained through a licensed healthcare provider, such as a physician or psychiatrist, who evaluates your condition and determines if Naltrexone is appropriate for your treatment plan.
Is Naltrexone Addictive?
No, naltrexone is not addictive. Naltrexone is classified as an opioid receptor antagonist, meaning it blocks the effects of opioids rather than producing euphoria or other addictive effects. Naltrexone cannot cause a “high” and, therefore, has no potential for addiction.
Does Naltrexone Have Withdrawal Symptoms?
Yes, naltrexone has withdrawal symptoms when used in opioid-dependent patients. Agitation was identified as the most prominent and difficult symptom to manage. The study concludes that emergency physicians should be aware of “naltrexone-precipitated hyperacute withdrawal” and its proper management.
How Long Does Naltrexone Stay in Your System?
Naltrexone stays in your system for 1-2 days in its oral form, while the injectable extended-release formulation remains active for 5-6 weeks.
