Gavril W Pasternak

NALTREXONE Naltrexone (brand name ReVia) is an OPIOID ANTAGONIST (i.e., a blocker of substances with morphine-like actions), with a structure very similar to another antagonist, NALOXONE. It also closely resembles the potent ANALGESIC (painkiller) OXYMORPHONE. The differences between naloxone and naltrexone are restricted to a simple substitution on the nitrogen atom, with naltrexone having a methylcyclopropyl group, yet this small substitution changes the pharmacology of the compound dramatically. Naltrex-one has no analgesic actions by itself and has the ability to antagonize, or reverse, virtually all the effects of morphine-like drugs. Like naloxone, naltrexone will precipitate WITHDRAWAL in physically dependent people.

Naltrexone is rapidly metabolized in the liver, but one of its metabolites is 6-naltrexol, which has some activity and a longer duration of action. In the 1990s, naltrexone was used to treat opiate addiction and for rapid opioid detoxification. Its greater potency than naloxone, along with its greater and longer activity after oral administration, has made this the antagonist of choice (for clinicians) in the treatment of opioid addiction.

In the early 1990s, several research groups reported that naltrexone, when given to alcoholic men following detoxification, reduced the likelihood of relapse to ALCOHOL. This finding secured to support the hypothesis that some of the reinforcing (euphoric) effects of alcohol are due to interactions with naturally occurring opioid systems in the brain.

A study published in 1999 supported this conclusion (Davidson et al., 1999). The findings suggested that naltrexone reduces the desire and craving for alcohol while sometimes increasing the negative side effects, including headaches. Naltrex-one has been shown to be especially effective when combined with behavioral therapy.

(SEE ALSO: Naltrexone in Treatment of Drug Dependence; Treatment: Alcohol; Treatment Types: Pharmacotherapy)


Davidson, D., ET AL. (1999). Naltrexone reduces craving in heavy drinkers. The Brown University Digest of Addiction Theory and Application, 18, 1.

Jaffe, J. H., & Martin, W. R. (1990). Opioid analgesics and antagonists. In A. G. Gilman et al. (Eds.), Goodman and Gilman's the pharmacological basis of therapeutics, 8th ed. New York: Pergamon.

MesZAROS, Liz (1999). New Treatments for Addictions: The Long Road to Acceptance. Behavioral Health Management, 19, 28.

Naltrexone for Alcoholism (2000). American Family Physician, 61, 1883.

NALTREXONE STILL HAS LOW ACCEPTANCE LEVEL IN CLIENTS WITH HEROIN ADDICTION (2000). The Brown University Digest of Addiction Theory and Application, 19, 4.

Study says naltrexone effective when combined with THERAPY (1999). Alcoholism & Drug Abuse Weekly, 11, 3.

Vassiliadis, J., ETAL. (1999). Naltrexone misadventures in opioid-addicted individuals: prolonged opioid-withdrawal with delirium. Journal of Toxicology: Clinical Toxicology, ST, 651.

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