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Searching for new medications to treat alcoholism

  • Naltrexone is a prescription medication taken by mouth that helps reduce drinking in alcoholics.
  • Naltrexone is quickly metabolized in humans by the liver to a metabolite called 6-beta naltrexol.
  • Researchers have provided the first direct evidence that 6-beta naltrexol may itself effect alcohol consumption.
  • These results suggest that 6-beta naltrexol is a potential new medication for alcohol dependence.
Since its 1994 approval by the federal Food and Drug Administration, naltrexone remains the sole prescription medication used to reduce drinking in alcoholics. Naltrexone is taken by mouth and quickly metabolized in the liver to a number of different compounds or metabolites that can be measured in blood or urine. Naltrexone's major metabolite is called 6-beta naltrexol. A study in the October issue of Alcoholism: Clinical & Experimental Research examines if 6-beta naltrexol itself can reduce alcohol consumption.

"Although 6-beta naltrexol is a metabolite that can be measured in human plasma and urine after administering naltrexone," explained Margaret R. Rukstalis, assistant professor of psychiatry at the University of Pennsylvania-VA Treatment Research Center and lead author of the study, "it is not known if 6-beta-naltrexol is independently pharmacologically active in reducing alcohol consumption. Studies have shown that high plasma levels of 6-beta naltrexol are critical in preventing relapse to alcoholism. Yet human plasma levels of both naltrexone and 6-beta naltrexol are highly variable following standardized oral doses of naltrexone. This is probably related to individual differences in the ability of the liver to metabolize naltrexone." The variable metabolism of naltrexone in individuals may explain why the medication doesn't work for everyone.

Treatments for alcohol dependence have helped scientists understand more about the biology of this brain disorder. First and foremost, as noted
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Contact: Margaret R. Rukstalis, M.D.
rukstalis@research.trc.upenn.edu
215-222-3200 x180
Alcoholism: Clinical & Experimental Research
14-Oct-2000


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