Naltrexone
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. It has also been found effective in the treatment of other addictions and may be used for them off-label. An opioid-dependent person should not receive naltrexone before detoxification. It is taken by mouth or by injection into a muscle. Effects begin within 30 minutes, though a decreased desire for opioids may take a few weeks to occur. Side effects may include trouble sleeping, anxiety, nausea, and headaches. In those still on opioids, opioid withdrawal may occur. Use is not recommended in people with liver failure. It is unclear if use is safe during pregnancy. 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.
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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% |
Protein binding | 20% |
Metabolism | Liver (non-CYP450) |
Metabolites | 6β-Naltrexol, others |
Onset of action | 30 minutes |
Elimination half-life | Oral (Revia): • Naltrexone: 4 hours • 6β-Naltrexol: 13 hours Oral (Contrave): • Naltrexone: 5 hours IM (Vivitrol): • Naltrexone: 5–10 days • 6β-Naltrexol: 5–10 days |
Duration of action | >72 hours |
Excretion | Urine |
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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. Naltrexone, as naltrexone/bupropion (brand name Contrave), is also used to treat obesity. It is on the World Health Organization's List of Essential Medicines. In 2021, it was the 254th most commonly prescribed medication in the United States, with more than 1 million prescriptions.