Naloxone is an opioid antagonist, a medication used to reverse or reduce the effects of opioids, commonly given to restore breathing after an opioid overdose; its effect begins within about two minutes when given intravenously, five minutes intramuscularly, and three to seven minutes intranasally. It is a non-selective, competitive opioid receptor antagonist that blocks opioid receptors without producing any opioid effect itself, reversing the central nervous system and respiratory depression opioids cause. Mozes Lewenstein and Jack Fishman, working with the Sankyo company, patented naloxone in 1961, and it was approved for treating opioid use disorder in the United States in 1971; it is marketed under the brand name Narcan and appears on the World Health Organization's List of Essential Medicines.
Facts
Mechanism of ActionNon-selective, competitive opioid receptor antagonist 1 Approved UseReversing or reducing the effects of opioids 1 First Approved / Isolated Year Significant RiskRapid-onset opioid withdrawal when given to a person who has used opioids 1 Classification
Approval Status ATC ClassSourced to the subject's own account Route of Administration WHO Essential MedicineSourced to the subject's own account Connections
Sources
1. Naloxone - Wikipedia
Lead section, first sentence (drug class)
is an opioid antagonist
Article body, sentence beginning 'Naloxone is a lipophilic compound'
Naloxone is a lipophilic compound that acts as a non-selective and competitive opioid receptor antagonist.
Lead section, first sentence (medical use)
a medication used to reverse or reduce the effects of opioids
Article body, sentence beginning 'It was approved for opioid use disorder treatment'
It was approved for opioid use disorder treatment in the United States in 1971.
Article body, sentence beginning 'Administration of naloxone to somebody who has used opioids'
Administration of naloxone to somebody who has used opioids may cause rapid-onset opioid withdrawal.
https://en.wikipedia.org/wiki/Naloxone, lead section
r an opioid overdose. Effects begin within two minutes when given intravenously, five minutes when injected into a muscle, and ten minutes as a nasal spray. Naloxone has also been said to have an onset of action of 3-7 minutes as an intranasal. Naloxone blocks
- Regulatory approval status
View the Source2. Anatomical Therapeutic Chemical Classification System (Wikipedia)
WikipediaFirst-level anatomical group codes, Code NQuote, First-level anatomical group codes, Code N
Nervous system
3. Wikipedia
Wikipedia contributors, Wikimedia Foundation
4. WHO Model List of Essential Medicines (Wikipedia)
WikipediaWHO Model List of Essential Medicines, Specific sectionQuote, WHO Model List of Essential Medicines, Specific section
Naloxone
Frequently Asked Questions
Why can naloxone cause sudden withdrawal symptoms?
It blocks opioid receptors and displaces the opioid there; giving it to someone who has used opioids may cause rapid-onset opioid withdrawal.
Naloxone is a competitive opioid receptor antagonist: it occupies opioid receptors without producing any opioid effect itself, which reverses the breathing and central nervous system depression that opioids cause. Because it displaces the opioid from those receptors, giving it to somebody who has used opioids may cause rapid-onset opioid withdrawal. That is a recorded risk of the drug, and it is why its action is described as reversal rather than treatment of the underlying use.
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