Opioid antagonists

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Opioid antagonists


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Opioid antagonists

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External References

First Aid









dextromethorphan overdose p. 711

heroin detoxification p. 600

for opioid toxicity p. 249, 572, 594


Opioid antagonists, like the name suggests, are medications used mainly to reverse the side effects of opioid agonists and to prevent opioid addicts from relapsing after they’ve recovered.

Now, all opioids work by binding to opioid receptors in the brain, spinal cord, and gastrointestinal tract.

Some are endogenous, meaning they are produced naturally by the body, like endorphin, short for endogenous morphine.

But others are exogenous, meaning they come from outside the body, like heroin and morphine, which come from the opium poppy; a flowering plant that oozes a milky white liquid.

To understand how opioids work, let’s zoom into a region of the brain tissue that has opioid receptors.

Normally, in the absence of endorphins, inhibitory neurons secrete a neurotransmitter called gamma-aminobutyric acid, or GABA, that prevents nearby neurons from releasing neurotransmitters like dopamine, serotonin, and norepinephrine.

Now, let’s say someone goes to play a rigorous game of badminton. Exercise releases endorphins which activate the three major opioid receptors located on the inhibitory neurons, called the mu, kappa, and delta receptors.

As endorphins bind to these receptors, they block the inhibitory neuron from releasing GABA, allowing the dopamine, serotonin, and norepinephrine secreting neurons to freely unload their neurotransmitters, which then gets picked up by another neuron in the same area.

Norepinephrine and serotonin release takes place in pain processing regions of the brain like the thalamus, brainstem, and spinal cord, resulting in a decreased sensitivity to pain.


Opioid antagonists are drugs that strongly bind to opioid receptors and prevent their activation. They are used to treat opioid overdose and addiction, and can also help to reverse respiratory depression and other adverse effects of opioids. Examples include drugs like naloxone, naltrexone, methylnaltrexone, and alvimopan.


  1. "Katzung & Trevor's Pharmacology Examination and Board Review,12th Edition" McGraw-Hill Education / Medical (2018)
  2. "Rang and Dale's Pharmacology" Elsevier (2019)
  3. "Goodman and Gilman's The Pharmacological Basis of Therapeutics, 13th Edition" McGraw-Hill Education / Medical (2017)
  4. "Naloxone treatment in opioid addiction: the risks and benefits" Expert Opin Drug Saf (2007)
  5. "Methylnaltrexone" Drugs (2010)
  6. "Naltrexone: A Pan-Addiction Treatment?" CNS Drugs (2016)
  7. "Approach to buprenorphine use for opioid withdrawal treatment in the emergency setting" The American Journal of Emergency Medicine (2019)

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