Drug intelligence / Profile preview

naloxone

Development stage
Approved
Lead developer
Daiichi Sankyo
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Intravenous, Intramuscular, Subcutaneous, Intranasal
01

Overview

Naloxone is a synthetic opioid antagonist used to rapidly reverse the effects of opioid overdose. It works by competitively binding to opioid receptors—primarily the μ-opioid receptor—with high affinity and acts as an inverse agonist or antagonist. This action displaces opioids from these receptors and blocks their effects on the central nervous system and respiratory system. Naloxone can quickly restore normal breathing in individuals whose respiration has slowed or stopped due to opioid toxicity. It is not effective in people without opioids in their system and does not treat opioid use disorder itself. Naloxone is available as an injectable solution and as a prepackaged nasal spray for emergency use[1][2][3][4][5]. The drug was originally derived from oxymorphone.

Brand names
NarcanKloxxadoZimhiRezenopyPrenoxadNyxoid
Other names
17-allyl-4,5α-epoxy-3,14-dihydroxymorphinan-6-one
02

Targets

KOR (Kappa opioid receptor)DOR (Opioid Receptor Delta 1)MOR (Mu opioid receptor)

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