Opioid Antagonist

Opioid antagonists are medications that attach to the same receptors in the body that opioids do, but instead of activating them, they block them. Think of it like changing the lock so the key (in this case, the opioid) no longer fits. There are two main types: some work mainly in the brain, while others work in the body.

Whether you are in recovery yourself or supporting someone who is, learning how opioid antagonists work can be an empowering step forward. This article breaks down the most common types, how they work, and how you can benefit from Q Space Detox’s LGBTQ-affirming, trauma-informed care. 

What Medications Are Opioid Antagonists?

Several medications block the body’s opioid receptors, each working a bit differently depending on the goal. Below are three commonly used medications, each with its own role in treatment:

Naloxone
Naloxone (Narcan) is a life-saving opioid antagonist that works by quickly reversing the effects of an opioid overdose. It binds to central opioid receptors and blocks the effects of opioids, especially those that slow down or stop breathing.

Naltrexone
Naltrexone is a full opioid antagonist. It does not help manage withdrawal or cravings the way methadone or buprenorphine does, but it prevents opioids from having any pleasurable effect if used. The long-acting injectable version, Vivitrol®, can be helpful for people who have already detoxed and need ongoing protection but have trouble taking daily medications.

Buprenorphine
Buprenorphine is a partial mixed opioid agonist at the μ-receptor and as an antagonist at the κ-receptor. It has a higher affinity for the μ-receptor than other opioids and can trigger withdrawal symptoms if you take it alongside another opioid. Its mixed actions help reduce cravings and also lower the risk of overdose.

Besides these three, there are opioid blockers that work mostly outside the brain. They include methylnaltrexone, naldemedine, naloxegol, and alvimopan. These drugs are helpful for managing the side effects of opioids, especially digestive troubles like constipation. However, because some pain relief from opioids also happens outside the brain, blocking those peripheral receptors too strongly may cause a sudden, intense return of pain once they wear off.

What are the Benefits of Opioid Antagonists?

Opioid antagonists can help in managing emergencies and long-term recovery. They may be used to keep people safe, reduce harm, and support sobriety in ways like:

• Lowering the Risk of Misuse: Some medications mix opioids with a blocker that only kicks in if someone tries to misuse the drug, like injecting or snorting it. This helps stop the “high” from happening, which makes the drug less appealing to misuse in the first place.
• Reversing Overdoses: Drugs like naloxone can quickly reverse an overdose by helping someone breathe again and regain consciousness. It’s often life-saving and works within minutes.
• Supporting Recovery: Medications such as naltrexone (Vivitrol) reduce cravings and make opioids feel less rewarding. That can help people stay committed to sobriety.
• Managing Side Effects: Some opioid antagonists are used to relieve issues like constipation caused by long-term opioid use without affecting pain relief.

Are Opioid Antagonists Dangerous?

Opioid antagonists are life-saving medications, especially in overdose emergencies or during recovery support. But like any medical intervention, they come with important risks to be aware of. 

• Increased risk of overdose: One concern is the increased risk of overdose after treatment. Because opioid antagonists reduce tolerance, someone who relapses and uses the same amount of opioids they once did may unknowingly take a fatal dose.
• Precipitated withdrawal: If someone who is physically dependent on opioids receives a blocking medication too soon, it can trigger sudden and intense withdrawal symptoms, uncomfortable and sometimes medically risky.
• Diminished pain management: For people who genuinely need opioids to manage severe or chronic pain, opioid antagonists may interfere with those medications, making pain harder to control.

Opioid Antagonists in LGBTQ-Affirming Addiction Treatment

Opioid antagonists can be life-saving in overdose situations and can be used in medication-assisted treatment of opioid addiction. However, these drugs can become dangerous if their use is not monitored. 

Q Space Detox views addiction as layered and complex, so we provide treatment that is specifically developed for each client. We use the principles of trauma-informed care, behavioral therapy, and community connection to provide LGBTQ-affirming addiction treatment. 

If you or a loved one wants to overcome opioid use, then you deserve a space that supports you holistically. Feel free to call us at (305) 745-7768 and get all the information you need to move forward.