How do Opioid Antagonists Work?


Medication-assisted treatment for opioid addiction comes in many forms using various FDA-approved medications, which all work differently. A popular and common form of therapy uses opioid antagonist medications such as Suboxone® to ease withdrawal symptoms in patients so they can focus on long-term recovery and overall wellness, including mental and emotional health, through substance use counseling.


What is an Opioid Antagonist?

Opioid antagonists are an invaluable tool in helping people with opioid use disorder. When someone misuses opioid agonists like heroin, oxycodone, morphine, or similar, the drugs flood the brain with unnaturally high levels of dopamine that bind to the brain's opioid receptors, producing a euphoric feeling or high when activating them.


It's important to note that not all opioid agonists are misused substances, and they have their place in medicine, especially partial agonists. A key component of Suboxone is buprenorphine, a highly effective partial agonist that initially became popular in the 1960s as an alternative pain reliever to morphine. Partial agonists work similarly to full agonists by activating receptors in the brain that control pain; however, the effects are less aggressive and lose their effectiveness at higher doses with a "ceiling effect," making them safer for the user.


Finally, an opioid antagonist binds receptors in the brain that otherwise are simulated by partial and full agonists and blocks other opioid substances from creating a response in the body. Suboxone® is a combination of buprenorphine (partial agonist) and naloxone (antagonist). That means medications like Suboxone®, Zubsolv®, and several others don't cause a euphoric high, which lowers the risk of misuse and addiction and increases effectiveness compared to other medications.


Other Uses for Naloxone

In addition to blocking other opioids from binding with receptors in the brain when ingested, naloxone also kicks users into withdrawal if it's taken outside of its directed use serving as a powerful relapse deterrent. This is incredibly useful for those who struggle with chronic relapse because the precipitated withdrawals can be highly uncomfortable and something patients will most likely never try more than once.


Naloxone also has the power to reverse an opioid overdose almost instantly, making it a life-saving drug for millions who struggle with opioid addiction. Sometimes this formulation is known as the brand name Narcan®, although generic versions are also available, which comes as a nasal spray or auto-injector similar to an EpiPen.


Who are the Best Candidates for Opioid Antagonists?

A medical provider who prescribes Suboxone® at Middlesex Recovery facilities is specialized in addiction treatment and will know if a patient is a suitable candidate for medications containing buprenorphine and naloxone, an opioid antagonist, based on specific criteria. Most often, medications containing buprenorphine and naloxone are prescribed for take-home use, where a patient is given a prescription they can fill at a pharmacy of their choice. They then self-dispense the medication at home every 24-72 hours as directed. Provided the patient has no contraindicated health conditions and is willing to follow the safety precautions, medicines containing buprenorphine and naloxone are generally safe for all people with opioid use disorder.


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