What is Naltrexone used for? Naltrexone, which is commonly sold under the brand named ReVia and Vivitrol, is a medication that can be used to treat opioid use disorder and alcohol use disorder. Physicians prescribe it to help people who are addicted to opioids or alcohol remain abstinent. While naltrexone uses include treating opioid use disorder and alcohol use disorder, it is not a “cure” for either condition.
People who are determined to abuse substances will likely return to substance abuse despite taking naltrexone. Instead of relying on naltrexone effects exclusively, addiction treatment centers instead use it as a tool. Naltrexone is an important component in medication-assisted treatment (MAT), a type of addiction treatment plan that emphasizes medicine alongside behavioral health interventions.
Medication-assisted treatment plans are comprehensive and holistic treatment plans that help people deal with every underlying aspect of their addiction, ranging from the physical to the psychosocial. Naltrexone reduces the rate at which people abuse alcohol and opioids, decreasing the chances of relapse and helping people in addiction treatment programs gain more from other treatment modalities.
It may come as some surprise that despite being an effective treatment for opioid use disorder, naltrexone is itself an opioid. However, there is a fine distinction between naltrexone and recreational opioids. Most opioids that result in a high are opioid agonists, a type of opioid that binds to naturally occurring opioid receptors in the brain and then fully activate them. Naltrexone, in contrast, is an opioid antagonist. Opioid antagonists work by attaching to opioid receptors and then blocking them.
They thereby prevent people from getting high from other opioid drugs and decrease cravings as well. However, when people take an opioid antagonist such as naltrexone while they are on opioids or while they are opioid-dependent, they will immediately experience withdrawal symptoms. For this reason, when naltrexone is used to treat opioid use disorder, it is generally prescribed after a person has stopped using recreational opiates and is no longer opioid-dependent.
However, naltrexone is most frequently used in the treatment of alcohol use disorder. While alcohol is not an opiate and naltrexone does not directly block the effects of alcohol, it nonetheless significantly decreases the amount of alcohol a person consumes. This is because alcohol addiction, like many addictions, is in large part driven by surges of dopamine in a person’s brain.
Since opioid receptors play an important role in releasing dopamine, naltrexone’s opioid antagonist effects can stymie the flow of dopamine when a person drinks alcohol. When the release of dopamine is reduced by naltrexone, a person is less likely to be motivated to drink or abuse alcohol. Naltrexone has been shown to lower both the quantity of alcohol consumed and the frequency at which people drink.
Naltrexone is available by prescription. While multiple formulations of naltrexone exist, it is most commonly prescribed in the form of an oral tablet. Other routes of administration that are sometimes used as alternatives to naltrexone tablets include injection and subcutaneous implants.
Sustained-release subcutaneous implants are a relatively new formulation of naltrexone that has been proven effective in recent years for the treatment of opioid use disorder. However, naltrexone for alcohol abuse is most frequently prescribed in the form of a pill, since it is most effective when taken soon before drinking and it is most effective when the effects are quicker.
Individuals with severe substance use disorders sometimes misuse naltrexone. However, it is important to emphasize that naltrexone does not offer a high and is not physically habit-forming. Nonetheless, it is not uncommon for people with highly developed addictions to experiment with medications.
In their desperation to get high, they may take higher doses of naltrexone than are medically recommended or they may take naltrexone alongside other drugs. As a result, physical and mental health problems can occur. Ultimately, naltrexone abuse is likely to make a person’s substance use disorder worse instead of better. It is always best to use naltrexone exactly as prescribed and to do so in the context of a proper addiction treatment program.
Naltrexone was developed in 1963 at Endo Laboratories, a pharmaceutical company based in New York. Two years later, researchers discovered that naltrexone could be effective when taken orally. They learned that the drug was a powerful opioid antagonist and that it was longer-acting than many opioid antagonists then on the market. These other opioid antagonists included nalorphine, naloxone, and cyclazocine.
Naltrexone showed promise because, unlike naloxone for example, it could be taken by pill in an oral formulation. As a longer-acting drug, naltrexone was suitable for once-daily administration. Most notably, researchers concluded that naltrexone did not lead to dysphoria, or low mood, a common effect of opioid antagonists. For these reasons, Endo Laboratories decided to continue developing the drug.
In 1967, Endo Laboratories patented naltrexone, using the code name EN-1639A. Shortly thereafter, Endo Laboratories was bought out by DuPont, an international biotechnology company. In 1973, they began clinical trials to determine if naltrexone could alleviate opioid dependence.
The following year, the National Institute on Drug Abuse collaborated in further clinical trials for this same purpose. In 1984, the Food and Drug Administration (FDA) approved naltrexone, under the brand name Trexan, as a medication suitable for the treatment of opioid dependence. It was also approved in 1995 under the brand name ReVia for the treatment of alcohol dependence. In 2006 and 2010, an intramuscular injection formulation of naltrexone, branded as Vivitrol, was approved by the FDA for alcohol dependence and opioid dependence.
Naltrexone continues to be studied and researched, and the protocol for prescribing it continues to change as the drug’s effects become better understood.
Naltrexone is synthesized in laboratories owned and operated by pharmaceutical companies. Unlike many other opioids, it is rarely produced in illicit labs run by drug cartels or other criminal organizations. Instead, it is produced by teams of chemists who manufacture it while following careful medical and legal guidelines.
Naltrexone is an entirely synthetic opioid. Unlike natural and semi-synthetic opioids that are ultimately derived from the naturally occurring opium poppy, naltrexone is synthesized using entirely artificial means. It is a congener (a chemistry term that roughly means “variant”) of oxymorphone.
Oxymorphone is an opioid agonist that is commonly prescribed for its analgesic, or pain-relieving, properties. As an opioid agonist, oxymorphone does lead to euphoric effects and the medication as a high potential for abuse. When naltrexone is synthesized from oxymorphone, the result is a drug with no opioid agonist properties that does not result in a high. For this reason, it is an effective medication for treating alcohol use disorder and opioid use disorder.
Naltrexone is sometimes known by its generic name when it is taken as prescribed. However, given that the medication is produced by numerous companies and is available in a variety of formulations, it goes by many different brand names. When the drug is abused or distributed illicitly on the black market, naltrexone sometimes goes by other names.
These slang names emerge because recreational drug users and drug distributors go to great lengths to avoid detection. Drug culture also contributes to the predominance of street terms and drug slang. As new formulations of naltrexone are manufactured and drug culture changes with every passing year, the terms used for naltrexone are set to continue changing. Nonetheless, below are some of the more common brand and street names used for naltrexone.
A large quantity of studies have been made to determine naltrexone’s efficacy in the treatment of alcohol use disorder and opioid use disorder. The Substance Abuse and Mental Health Services Administration (SAMHSA) conducted 14 studies in 2001 alone to measure the effects of naltrexone treatment on individuals with alcohol use disorder. These studies determined that naltrexone does not have a significant effect compared to placebos on preventing people from relapsing. Individuals who are determined to continue drinking on naltrexone will likely do so despite taking naltrexone.
Nonetheless, the study found that individuals who do relapse while taking naltrexone do so to a significantly less intense degree. The drink in lower quantities and at a reduced frequency, preventing their relapse from reaching a crisis point as easily. Individuals in the study self-reported that the euphoric effects, or “high,” associated with drinking was significantly less intense than it normally is. Only half of relapsers taking naltrexone progressed to heavy drinking.
SAMHSA’s studies concluded that naltrexone, while not capable of preventing relapse, decreases its severity and is therefore helpful for keeping people invested in their treatment programs and preventing serious health consequences.
A number of studies have also concluded that naltrexone is an effective treatment for opioid use disorder. More specifically, injectable slow-release naltrexone, which is sold under the brand name Vivitrol, has been shown to help people with heroin addictions. Vivitrol improves patient adherence in treatment programs, decreases the rate of overdoses, and also reduces the severity of overdoses when they do occur. As such, naltrexone has the ability to save lives.
The most abused drug in the United States is alcohol by a high margin. While naltrexone does not stop people from relapsing, it is nonetheless an essential medication given how high the relapse rate is in alcohol addiction treatment. Opioid use disorder is also a prevalent condition. In fact, the United States currently suffers from an opioid epidemic driven by the ubiquity of synthetic prescription opioids like fentanyl. With opioid overdoses in the United States numbering 46,802 in 2018 alone, medications like naltrexone are more necessary now than ever.
Individuals who suffer from opioid use disorder are rarely successful when they try to manage their addictions on their own. Given that opioid use disorder is a medical condition that affects the brain’s decision-making centers, exerting personal willpower is rarely sufficient. Instead, the best course of action is to enroll in an outpatient addiction treatment center.
Outpatient treatment centers usually begin by evaluating each individual to determine their unique needs and circumstances. Thereafter, addiction treatment professionals coordinate with physicians and psychologists to design an individualized treatment program for each person.
One common approach is medication-assisted treatment (MAT), a type of treatment plan that combines medication with elements of behavioral therapy. This kind of comprehensive treatment plan provides a “whole patient” approach that addresses the neurological, physical, interpersonal, and psychological driving forces behind a person’s substance use disorder.
Naltrexone is sometimes used in a medication-assisted treatment plan. It is generally prescribed 7-14 days after a person has stopped using recreational opiates, otherwise individuals risk suffering from withdrawal symptoms. As such, it is important that individuals have a strong treatment program and support system in place so that they can get through those initial days of withdrawal. This is all the more important because naltrexone takes some time to become effective. After several weeks, however, an individual taking naltrexone will experience a decreased desire for opioids. In addition to mitigating cravings, naltrexone reduces the risks of relapse by decreasing the likelihood of an overdose.
Long-acting injectable naltrexone has been found to be particularly effective, since it only requires a dose once a month. Oral formulations of naltrexone, which are prescribed in single daily doses, were found in some studies to have variable efficacy. This is because if a person is determined to abuse recreational opiates, they can simply opt to skip their dose for that day. However, for individuals who are motivated and determined to achieve sobriety, even naltrexone pills can be a valuable tool.
It is important to emphasize that naltrexone cannot cure opioid use disorder. Instead, it simply reduces cravings and lowers the risks of relapse. However, most people suffering from opioid use disorder have a wide range of issues behind their addiction, and a reduction in cravings is never sufficient for managing an addiction. It is for this reason that medication-assisted treatment programs emphasize behavioral therapy approaches in addition to naltrexone treatment.
Cognitive-behavioral therapy, group therapy, skills training, and support groups can help people develop the psychological coping tools they need to avoid relapse. Naltrexone aids that process by removing the painful distractions that occur when a person is constantly beset by opioid cravings.
Naltrexone’s most common use is in the treatment of alcohol use disorder. It is generally prescribed after a person has stopped using alcohol entirely for a sufficient period. Once an individual is no longer physically dependent upon alcohol, they can begin taking naltrexone. If an individual takes naltrexone while alcohol dependence persists, they may experience negative naltrexone side effects, including nausea and vomiting.
However, if they wait until alcohol dependence subsides, they can take naltrexone and immediately experience the benefits. Naltrexone works by binding to the endorphin receptors located in the brain and body. It thereby blocks the feelings and effects associated with imbibing alcohol. As a result, individuals on naltrexone tend to experience reduced alcohol cravings, reducing their likelihood of relapsing. Naltrexone also reduces the risks that generally accompany relapse itself, because the medication makes alcohol less pleasurable and causes people to drink in lower quantities.
However, it is important that a person take naltrexone in the context of a proper outpatient treatment center, where they can receive other therapeutic treatments that will support their naltrexone treatment.
Naltrexone has a low potential for abuse because it does not produce any of the euphoric effects associated with an opioid high. It also does not release dopamine, the neurotransmitter that reinforces drug-taking behavior in the brain. However, it is still possible for a person to develop an unhealthy relationship with naltrexone. This occurs when a person is prescribed naltrexone without a strong treatment program in place, or when a person takes naltrexone without a desire to achieve sobriety. In these cases, a person may use naltrexone for brief periods of time.
However, as soon as they decide they want to engage in substance abuse, they can simply stop taking naltrexone. Naltrexone blocks the effects of opioids and reduces cravings while it is active in the body, but when it is not, a person is still free to abuse opioids. Engaging in naltrexone treatment intermittently in this manner is likely to complicate the addiction treatment process and can exacerbate an individual’s opioid use disorder.
The greatest risk, however, lies in the fact that when a person stops using opioids for periods of time their tolerance decreases. When they cease taking naltrexone and again pick up recreational opioids, they may have a lower tolerance than they expect, and the result can be a life-threatening overdose. For this reason, it is crucial for individuals taking this medication to understand what to avoid when taking naltrexone.
Few people become addicted to naltrexone, due to the fact that it does not offer a high. However, a high percentage of people fail to use naltrexone properly. This can entail inconsistent usage of naltrexone, such as when a person goes off naltrexone periodically in order to engage in substance abuse. It can also mean taking naltrexone for longer than medically recommended or taking higher doses. Individuals who do so may experience more of the negative side effects associated with naltrexone abuse.
Naltrexone is rarely abused on its own and does not present any withdrawal symptoms. However, naltrexone, despite not offering the typical effects associated with an opioid high, is nonetheless a potent medication. As such, naltrexone treatment sometimes leads to a number of side effects. These physical and mental symptoms can occur whether a person uses naltrexone as directed or not.
Naltrexone use can also lead to more severe symptoms. These include:
The greatest risk of naltrexone abuse, however, is overdose. While naltrexone itself cannot lead to an overdose, individuals who continue to engage in substance abuse during the course of naltrexone treatment expose themselves to a number of risks. It is common for people taking naltrexone to be frustrated when they try to abuse recreational opiates, since naltrexone blocks the euphoric effects of these drugs. As such, they may take abnormally high doses of recreational opiates to compensate for the blocking effects of naltrexone. Doing so can result in an overdose.
A more strategic approach for individuals who have planned a relapse in advance is to stop taking naltrexone entirely. However, during the course of naltrexone treatment, most people experience a decrease in their opioid tolerance. When a person returns to opioid abuse after a period of abstinence, their lowered tolerance can put them at risk for a fatal overdose when they take their accustomed dose of recreational opiates.
Individuals who abuse naltrexone and continue to relapse generally fit into one of two categories: individuals who lack a strong desire to get sober, and individuals who are taking naltrexone without access to a strong comprehensive addiction treatment program. The first class of people, those with no desire to get sober, may nonetheless benefit from naltrexone to some degree, since the medication does lower the risks of overdose and decrease a person’s desire for alcohol and opioids.
This approach to substance abuse treatment is sometimes known as harm reduction. However, it is unlikely to result in lasting sobriety, and addiction is a medical condition that generally worsens over time. Unfortunately, individuals who fail to recognize an urgent need to treat their substance use disorder are often reluctant to seek help.
However, the vast majority of people with alcohol use disorder and opioid use disorder have experienced the negative consequences of regular substance abuse. While social stigmas surrounding addiction cause many addicts to be reluctant to reach out for help, most are unable to stay sober through sheer force of will for any significant length of time. Instead, it is best to reach out to an outpatient treatment program. Taking naltrexone alone may reduce the amount of cravings a person experiences, but it does not address the root causes of a substance use disorder.
Outpatient treatment programs can not help a person get the medication they need, but they help individuals develop the skills and coping tools they need to avoid relapse. By engaging in a variety of treatment modalities, including counseling, support groups, and skills training workshops, individuals who suffer from addiction can begin to pick up the pieces of their lives and start anew.