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Opioid Blockers | What Are the Best Options?

Opioid blockers are medications that block the effects of opioids in the brain and body. Doctors call them opioid receptor antagonists, which means they bind to opioid receptors and prevent them from being activated. They can also kick opioids off their receptors, stopping their effects on the body and nervous system almost immediately. 

Opioid blockers are used to treat problems related to opioid use disorders, including overdose, withdrawal, and addiction. There are several brands of drugs that are used to block the effects of opioids, but they all contain one common chemical: naloxone.

Naloxone is an opioid antagonist that’s used on its own or combined with other drugs, depending on its intended use. However, the right medication for you will depend on the facet of overdose you may be struggling with. 

Opioid Overdose

An opioid overdose occurs when you take a high dose of the drug or when you take too many doses in close succession. Overdose can be deadly, and opioids are the leading cause of the current overdose epidemic in the United States. 

Opioids work by binding to opioid receptors which are responsible for pain relief and sedation. They slow down your nervous system to achieve these effects. However, high doses of an opioid can slow down important functions like your heart rate and breathing. In most fatal opioid overdoses, breathing slows to the point of oxygen deprivation, coma, and death. 

However, naloxone can be administered to someone during an opioid overdose to reverse the effects of an overdose, if it’s taken early enough. Naloxone is sold under the brand name Narcan, which is a nasal spray that contains the drug. It’s often carried by first responders like firefighters and paramedics. 

In some states, Narcan is sold over the counter for people to use in emergencies. Naloxone is also administered through intravenous injection, but the nasal spray is preferred for people that are unconscious. 

Opioid Addiction

Naloxone is also included in medicines that are used to treat opioid use disorders. However, in these medications, naloxone is a safety net rather than the primary active ingredient. Medications like Suboxone, Zubsolv, and Bunavail combine naloxone and buprenorphine to treat addiction. Buprenorphine is a partial opioid agonist, which means it has a weak activating effect on opioid receptors. 

These medications are used to provide relief from opioid cravings and withdrawal without the intoxicating effects of illicit and prescription opioids. This can help people get out from under active addiction so they can pursue normal responsibilities and addiction treatment. 

Naloxone is included in the drug to make it more difficult to abuse. Suboxone is taken sublingually (under the tongue), which makes it difficult for naloxone to make it into your bloodstream, so it remains inactive. If you try to take the drug in a way that makes the buprenorphine’s effects more intoxicating, the naloxone becomes active and stops the opioid’s effects. 

Opioid Withdrawal

Medications like Suboxone may also be used during an opioid tapering period. Tapering is intended to safely NCBI from an opioid medication to avoid extremely uncomfortable withdrawal symptoms. Tapering is more effective with help from a medical professional.

Sources

The National Center for Biotechnology Information. Retrieved from https://www.ncbi.nlm.nih.gov/books/NBK64119/

National Institute on Drug Abuse. (n.d.). Opioids. Retrieved from https://www.drugabuse.gov/drugs-abuse/opioids

National Institute on Drug Abuse. (2018, April 4). Opioid Overdose Reversal with Naloxone (Narcan, Evzio). Retrieved from https://www.drugabuse.gov/related-topics/opioid-overdose-reversal-naloxone-narcan-evzio

RxList. (2019, November 11). Suboxone (Buprenorphine HCl and naloxone HCl): Uses, Dosage, Side Effects, Interactions, Warning. Retrieved from https://www.rxlist.com/suboxone-drug.htm

SAMHSA. (2019, November 22). Buprenorphine. Retrieved from https://www.samhsa.gov/medication-assisted-treatment/treatment/buprenorphine

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