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Washington
(H24N).
Naltrexone, one of only two medications approved by the
Food and Drug Administration (FDA) to treat alcoholism, may have
an offspring that works better and is easier to take than its parent
drug.
The
compound 6-beta naltrexol is produced when Naltrexone is processed
by the liver. Since everyone’s liver works differently and alcoholism
damages the liver, the amount of Naltrexone an alcoholic can metabolize
varies highly. If an alcoholic’s liver is in bad shape it won’t
break down the drug so it can be used, and the patient will not
receive enough medication to help stop drinking.
Since
people who have damaged livers need to stop drinking the most, researchers
at the University of Pennsylvania’s VA Treatment Research Center
decided to test 6-beta naltrexol (which is already broken down and
could bypass the liver) to see if, by itself, it had any effect
on how much an individual drank. They found that it did.
Rats
drank less alcohol as the amount of 6-beta naltrexol they were given
increased. According to the study, which was published in the October
issue of Alcoholism: Clinical & Experimental Research, the dose
range tested was comparable to a standard 50mg oral dose of Naltrexone
for humans.
Margaret
Rukstalis, MD, the lead author of the study, is excited about 6-beta
naltrexol’s potential as an anti-alcoholic agent. "Six-beta
naltrexol may be easier to give and more effective than currently
available medications that help prevent alcohol relapses,"
said Rukstalis.
"One
of the benefits of 6-beta naltrexol is that it is longer acting.
It is possible that it can be given less frequently [than Naltrexone],
or, if someone misses a dose, it can still provide some protection
against ‘slip’ drinking," Rukstalis said. "One nice thing
about Naltrexone, even now, is that it needs to be taken only once
a day, which is very important for medication compliance, especially
in an alcoholic population who may be ambivalent about taking medications
to begin with. If 6 beta-naltrexol shows promise, it could potentially
be given every other day, or maybe produced in a skin-patch or a
long-term injectable format."
Six-beta
naltrexol blocks opioid receptors in the brain, keeping alcohol
from affecting brain cells and producing an alcoholic "high."
The other anti-alcohol drug, Antabuse, causes severe nausea if someone
who is taking it on a regular basis drinks alcohol. It is considered
an aversive therapy. Naltrexone works by diminishing the desire
to drink.
According
to Raymond Anton, MD, professor of psychiatry and scientific director
of the Alcohol Research Center at the Medical University of South
Carolina, most people’s brain cells return to normal after alcohol
leaves the system, but the brain cells of people at risk for developing
alcoholism are more permanently changed. The more such a person
drinks, the more changed and dependent on alcohol their brain cells
become.
"Unfortunately,
the opioid neurotransmitter system probably does not explain all
of the types of alcohol dependency," Anton said. "Other
people may have changes in other cells and transmitters that are
not impacted by drugs like Naltrexone and 6-beta naltrexol. Future
research will begin subtyping alcoholics, perhaps by using a genetic
approach, so that more specific medications can be used [for a given
individual]."
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