What is an Opioid Antagonist- Uses, Side Effects & Risks

Medications like Naltrexone and Naloxone that block opioid receptors, preventing the effects of opioid drugs, are called Opioid antagonists. According to the Centers for Disease Control and Prevention, opioid abuse was the sole reason behind 80,000 deaths in the year 2021. While opioid addiction is tricky to understand and complicated to treat, using medications like opioid antagonists can greatly aid doctors. 

 This article will further explore:

1. Types of Opioid Antagonists
2. The side effects of Opioid Antagonists
3. Their uses and risks
4. Different types of treatment for opioid addiction

Demi Lovato once said, ‘One of the hardest things was learning that I was worth recovery.’ So do not waste your time and contact ChoicePoint, a co-occurring addiction rehab in Fairlawn, New Jersey, and begin your recovery journey today! 

CALL NOW FOR FREE SCREENING

What is an Opioid Antagonist and Its Role in Addiction Treatment

The literal meaning of the Antagonist is ‘hostile.’ Their purpose is to attach to opioid receptors in the body without activating them. So, if a person uses opioids while taking an antagonist, the euphoric and rewarding effects will be greatly reduced or blocked. This helps eliminate the motivation to continue using.

So, what is an opioid antagonist? Put simply, these are medications that can support recovery by blocking the effects of opioids. When used properly under medical supervision, these medications can be highly effective at managing withdrawal symptoms and preventing relapse. 

Opioid antagonists may be used during addiction treatment in the following ways: 

• To reverse opioid overdoses
• Aiding in sustaining abstinence by blocking the euphoric effects of opioids
• Reduce cravings for opioids
• Reversing opioid overdoses in emergencies
• Minimize withdrawal symptoms during detoxification
• An essential component of Medication-Assisted Treatment (MAT) programs, offering a holistic approach to addiction recovery

Types of Opioid Antagonists and Their Uses

Let’s take a look into What is an Opioid Antagonist and their use during opioid addiction treatment. The two of the most commonly used opioid antagonists are naltrexone and naloxone;

Naltrexone

• Naltrexone is a “full antagonist.” 
• It means it completely blocks opioid receptors throughout the body so that opioids have no effect. 
• By blocking the opioid receptors, naltrexone eliminates the reward if relapse occurs, supporting recovery. 
• Even if a patient relapses while on naltrexone, they will not feel any euphoric effects from the opioids.
• It is often used after completing withdrawal and is taken daily in the form of a pill or as a monthly injection to reduce cravings.

Naloxone

• Naloxone is a “partial antagonist”. 
• It reverses life-threatening overdoses by quickly kicking other opioids off receptors and restoring breathing. 
• Naloxone is available as an injectable as well as a nasal spray. 
• While the effects only last 30-90 minutes, it provides a rapid rescue from overdoses.
• It is an emergency medication that rapidly reverses life-threatening respiratory depression from opioids.

Has it come to your attention that Opioids caused almost 69,000 deaths in the United States in 2020 – nearly 75% of the country’s drug overdose deaths that year?

Risks Associated with Opioid Antagonists

While opioid antagonists are highly effective when used properly, there are some risks in case of abuse: 

Withdrawal

Starting naltrexone immediately after the last opioid use can cause a rapid, intensely uncomfortable withdrawal episode. This is why medical protocols often have a 7-10-day waiting period after last use. 

Increased Risk

Some patients may try to increase opioid use, try dangerous combinations with sedatives, or opt for higher doses in an attempt to override the blocking effects of antagonists. This puts them at added medical risk.

Allergic Reactions

Some patients may face allergic reactions, headaches, joint/muscle pain, or other side effects from naltrexone. While rare, these reactions can be managed by adjusting the dosage or additional medications.

Limited Retention

Some studies show that more than half of the patients stop taking oral forms of naltrexone. However, using a monthly injectable version instead of an oral pill has led to better results and more people sticking with the treatment.

Opioid Antagonist Drug Example

Long-Term Effects of Using Opioid Antagonists

Long-term use of antagonist drugs, as part of a comprehensive treatment plan, can be very helpful in preventing relapse and providing stability during the early stages of recovery from addiction. Behavioral therapies alone might not be enough for those heavily affected by addiction. Combining them with drugs that block opioid effects can greatly assist individuals during the challenging initial phases of recovery. Listed below are some long-term benefits of using opioid antagonists;

Reduced Relapse Rates

Various studies find significantly lower relapse rates over 6-12 months than behavioral treatment alone. The blocking effect helps “rewire” reward pathways to reduce addiction over time.

Increased Retention in Treatment

Injections instead of daily pills boost treatment retention amongst patients and help them keep up with their counseling and rehab better.

Improved Social/Family Functioning

Opioid antagonists help people fix broken relationships, continue to go to work or school regularly, and take care of their duties as they recover from addiction.

Reduced Infectious Disease Transmission

Opioid Antagonist drugs help people who might use opioids through injection. By using opioid antagonists, they avoid drug injections, which reduces the chance of catching diseases like HIV and hepatitis.

Possible Change in Brain Chemistry

Long-term antagonist use may support brain repair mechanisms and restore dopamine pathways damaged by chronic opioid misuse.

Read this encouraging comment by one of our patients, ‘If you ask what progress I have made, I would say that I have begun to be a friend to myself. I live a sober life where I know my surroundings, family, and friends.’

What Drugs Do Opioid Antagonists Counteract?

Opioid antagonists are known to block the effects of common opioid drugs and opioid-stimulating substances, including:

1. Heroin
2. Oxycodone
3. Fentanyl
4. Codeine
5. Morphine
6. Hydrocodone
7. Alcohol

Free Addiction Assessment

Please note this assessment is an initial self-screening, and it is not meant to be a medical assessment or clinical diagnosis of addiction. For proper diagnosis and treatment, schedule an appointment with ChoicePoint.

Opioid Abuse Treatment & Management

As discussed earlier, the Opioid antagonist is a type of medication that blocks the effects of opioids in the brain. Here are the best treatments for Opioid addiction:

Detox

• Detox is the initial step in overcoming addiction. 
• It involves eliminating addictive substances from the body under medical supervision.
• Depending on the substance, this process can last a few days to several weeks.
• It’s a critical phase that prepares individuals for further treatment, whether in inpatient or outpatient settings, by clearing the physical dependence on the substance.

MAT (Medication-Assisted Treatment)

Medication-assisted treatment (MAT) is a comprehensive approach to treating substance use disorders, primarily opioid addiction. MAT includes medications such as Suboxone, buprenorphine, and naltrexone, amongst others, paired with counseling and behavioral therapies. MAT’s goal is to;

•     Normalize brain chemistry
•     Block the euphoric effects of opioids
•     Relieve physiological cravings
•     Stabilize body functions

 It may effectively retain people in treatment and improve their ability to gain and maintain employment.

Outpatient Setting

Outpatient treatment allows individuals to receive therapy and support for addiction while continuing to live at home and, in many cases, maintain their work or school commitments. This form of treatment includes;

•     Regular meetings with addiction counselors
•     Participation in group therapies
•     Medication management

It’s suitable for those with a strong support network and a less severe Opiate addiction. Outpatient programs offer flexibility and are often used as a step down from more intensive treatment options or as ongoing support after completing inpatient treatment.

Inpatient Level of Care

Inpatient treatment involves staying at a residential facility for a period. It may typically range from 30 days to several months. This treatment provides a structured environment and supervision, ideal for individuals with severe addiction or co-occurring mental health disorders. Patients receive round-the-clock medical and emotional support, participate in group and individual therapies, and are isolated from environments that may trigger substance use.

Intensive Outpatient

Intensive outpatient treatment may be a rigorous form of outpatient care. It is designed for patients suffering from severe substance abuse. This treatment involves staying in a specialized facility where patients may receive highly structured and intensive therapy.

Seeking professional medical advice is crucial for determining the most suitable treatment plan. ChoicePoint’s DEA-certified staff is ever-ready to answer all your questions about What is an Opioid Antagonist and more. Call us now at 844.445.2565. 

What is an Opioid Antagonist- Take Away…

When combined with Behavioral therapies (CBT, DBT) and FDA-approved medications, opioid antagonists provide a data-driven strategy to: 

• managing withdrawal
• preventing relapse
• supporting long-term recovery from opioid addictions

The US is amid an opioid pandemic, with the number of casualties from opioid abuse increasing each year. Therefore, if you or your loved ones are struggling with opioid addiction, get help today!

We Accept Most Insurance Programs

Q&A Section

Got more questions about What is an Opioid Antagonist? Check out our section below: 

What is an Opiate Antagonist, and How Does it Work?

An opioid antagonist is a type of medication that blocks the effects of opioids in the body. Opioid antagonists bind to opioid receptors, preventing opioids from attaching and exerting their effects.

When is Naloxone Used, and Can Anyone Administer it?

Naloxone is used in emergencies to reverse opioid overdose effects, restoring normal breathing rapidly. Many places allow bystanders, including friends and family, to administer naloxone in an overdose situation. However, it is advised to speak to a professional healthcare provider before administering Naloxone. 

Do Opioid Antagonists Lead to Withdrawal Symptoms?

Yes! Opioid antagonists can induce withdrawal symptoms if administered to someone dependent on opioids. 

What Are the Two Most Commonly Used Centrally-acting Opioid Receptor Antagonists?

Naloxone and naltrexone are the two most commonly used centrally-acting opioid receptor antagonists. Naloxone is available in intravenous, intramuscular, and intranasal formulations and is FDA-approved for use in opioid overdose and the reversal of opioid-related respiratory depression.

Is There an Age Limit for Using Opioid Antagonists?

Yes! Age restrictions may apply, and following medical guidelines for safe use is important. 

Are there Side Effects of Opioid Antagonists, and Can Opioid Antagonists Be Used Preventively?

Common side effects associated with opioid antagonists include nausea, headache, and dizziness. However, these are generally mild. Yes! Opioid antagonists can be used preventively in some cases, especially for high-risk individuals; preventive use of naloxone is considered.

REFERENCES

1. https://www.cdc.gov/opioids/data/index.html#:~:text=The%20number%20of%20overdose%20deaths,times%20the%20number%20in%201999.&text=Overdoses%20involving%20opioids%20killed%20more,those%20deaths%20involved%20synthetic%20opioids. 
2. https://www.fda.gov/drugs/information-drug-class/information-about-medication-assisted-treatment-mat 
3. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5755382/