Naltrexone
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Naltrexone, sold under the brand name Revia among others, is a medication primarily used to manage alcohol use or opioid use disorder by reducing cravings and feelings of euphoria associated with substance use disorder.[9] It has also been found effective in the treatment of other addictions and may be used for them off-label.[12] An opioid-dependent person should not receive naltrexone before detoxification.[9] It is taken by mouth or by injection into a muscle.[9] Effects begin within 30 minutes,[9] though a decreased desire for opioids may take a few weeks to occur.[9] Side effects may include trouble sleeping, anxiety, nausea, and headaches.[9] In those still on opioids, opioid withdrawal may occur.[9] Use is not recommended in people with liver failure.[9] It is unclear if use is safe during pregnancy.[9][13] Naltrexone is an opioid antagonist and works by blocking the effects of opioids, including both opioid drugs as well as opioids naturally produced in the brain.[9]
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Pronunciation | /ˌnælˈtrɛksoʊn/ |
Trade names | Revia, Vivitrol, Depade, others |
Other names | EN-1639A; UM-792; ALKS-6428; N-cyclopropylmethylnoroxymorphone; N-cyclopropylmethyl-14-hydroxydihydromorphinone; 17-(cyclopropylmethyl)-4,5α-epoxy-3,14-dihydroxymorphinan-6-one |
AHFS/Drugs.com | Monograph |
MedlinePlus | a685041 |
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Routes of administration | By mouth, intramuscular injection, subcutaneous implant |
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Bioavailability | 5–60%[6][7] |
Protein binding | 20%[6][3] |
Metabolism | Liver (non-CYP450)[8] |
Metabolites | 6β-Naltrexol, others[6] |
Onset of action | 30 minutes[9] |
Elimination half-life | Oral (Revia):[3] • Naltrexone: 4 hours • 6β-Naltrexol: 13 hours Oral (Contrave):[4] • Naltrexone: 5 hours IMTooltip Intramuscular injection (Vivitrol):[5] • Naltrexone: 5–10 days • 6β-Naltrexol: 5–10 days |
Duration of action | >72 hours[6][10][11] |
Excretion | Urine[3] |
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ECHA InfoCard | 100.036.939 |
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Formula | C20H23NO4 |
Molar mass | 341.407 g·mol−1 |
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Melting point | 169 °C (336 °F) |
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Naltrexone was first made in 1965 and was approved for medical use in the United States in 1984.[9][14] Naltrexone, as naltrexone/bupropion (brand name Contrave), is also used to treat obesity.[15] It is on the World Health Organization's List of Essential Medicines.[16] In 2021, it was the 254th most commonly prescribed medication in the United States, with more than 1 million prescriptions.[17][18]