Which medications in the drug class Opioid Antagonists are used in the treatment of Opioid Abuse?

Updated: Jun 21, 2018
  • Author: David W Dixon, DO; Chief Editor: Glen L Xiong, MD  more...
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Answer

Opioid Antagonists

Reverses opioid effects by inhibiting opioid agonists at receptor sites.

Naloxone (Evzio, Narcan)

Pure opioid antagonist. Used to reverse opioid intoxication.

If patients do not respond to multiple doses of naloxone, consider alternative causes of unconsciousness. Need of ongoing substance abuse treatment should be established while caring for overdose. The injectable solution is available in vials and syringes (0.4 mg/mL, 1 mg/mL) for IV/IM/SC administration by healthcare providers. It is also available as an autoinjector (delivers 0.4 mg IM/SC) for home use by family or caregivers.

Naloxone intranasal (Narcan Nasal Spray)

Competitive opioid antagonist that antagonizes opioid effects by competing for the same receptor sites. The intranasal form is indicated for the emergency treatment of known or suspected opioid overdose, as manifested by respiratory and/or central nervous system depression.

Naltrexone (ReVia, Vivitrol)

Used in combination with clonidine for rapid (4-5 d) detoxification.

Very effective long-acting opioid antagonist that was thought to be an ideal maintenance agent because it blocks receptor sites and, hence, opioid reinforcing properties. However, clinical results are not very promising when compared with methadone maintenance. Craving may continue during naltrexone maintenance. For groups of patients such as health care professionals or business executives for whom external incentives to stay away from drugs are important, naltrexone therapy has been very effective.

Indicated for prevention of relapse to opioid dependence following opioid detoxification.


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