Drug intelligence / Profile preview

naltrexone

Development stage
Approved
Lead developer
Alkermes
Modality
Small Molecules
Administration
Oral, Intramuscular, Intravenous
01

Overview

Naltrexone is a synthetic opioid antagonist used primarily in the management of alcohol use disorder (AUD) and opioid use disorder (OUD). It works by competitively binding to opioid receptors—primarily the mu-opioid receptor, but also kappa and delta receptors—in the central nervous system, thereby blocking the euphoric and sedative effects of opioids such as heroin, morphine, and codeine. In alcohol dependence, its mechanism is less well understood but is thought to involve modulation of the endogenous opioid system to reduce cravings. Naltrexone does not have agonist or addictive properties and does not cause withdrawal when stopped. It is available as an oral tablet for daily use or as an extended-release intramuscular injection administered monthly. Naltrexone has also been studied off-label at low doses for conditions such as multiple sclerosis, fibromyalgia, Crohn’s disease, impulse-control disorders (e.g., gambling), self-injurious behavior in developmental disabilities, depersonalization/derealization disorders, sexual addiction, and for mitigating neuropsychiatric effects of interferon alpha therapy[1][2][3][4][6].

Brand names
VivitrolReviaDepade
Other names
naltrexone hydrochloride
02

Targets

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

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