Drugs used in the Treatment
of Alcohol Abuse/Addiction
Tristan Knowles
Alcoholism Treatment
 Lots of alcoholism treatments use a combination
of psychological means (such as CBT) in
combination with aversion therapy aided by
drugs.
 Most drugs used in treating alcoholism are
aimed at creating adverse reaction to imbibing
alcohol.
 Currently on the market, there are a limited
number of drugs to treat alcoholism.
Disulfiram (Antabuse)
 Under normal conditions,
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alcohol is broken down
by alcohol
dehydrogenase into
acetaldehyde, which is
further broken down into
acetic acid by
acetaldehyde
dehydrogenase.
 Antabuse works by
blocking acetaldehyde
dehydrogenase, causing
an excess build up of
acetaldehyde.
Symptoms/Effects of Antabuse
 Due to the excess build up of
acetaldehyde in the bloodstream, patients
may feel nausea, vomit, have headaches,
chest pain, and several other symptoms
after only five to ten minutes after drinking.
 There appears to be no “tolerance” to
Antabuse; extended use of the drug only
adds to its effect as it is both absorbed
and excreted slowly by the body.
More Antabuse
 Due to its slow excretion from the body,
Antabuse can be effective 5-7 days from the last
dose.
 Therefore, patients using Antabuse to treat
alcoholism must continually take the drug (this
drug can be court mandated).
 Antabuse also shows some effects as a
dopamine breakdown inhibitor, and therefore is
also being investigated as a treatment for
cocaine addiction.
Negative Aspects of Antabuse
 Due to its interaction with the enzyme dopamine-betahydroxylase , which breaks down doapmine, Antabuse
adverse affects when combined with drugs affecting the
release and re-uptake of dopamine (Such as Ritalin,
Adderall, and Cocaine).
 Metabolism of other drugs may be inhibited by Antabuse
(such as Benzodiazepines, morphine, and barbituates).
 Extremely important to take under consideration when
someone is undergoing other medical treatment along
with the treatment for alcohol addiction.
Naltrexone (Revia or Vivitrol)
 Naltrexone is
metabolized in the liver
into a variety of
metabolites, with the 6-βnaltrexol being the
metabolite useful in
treating alcoholism.
 The mechanism of action
is not quite fully
understood.
 Approved for use in the
treatment of alcoholism in
April of 2006.
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rexone
Naltrexone
Proposed Mechanisms of Action
 After metabolizing into the 6-β-naltrexol,
the metabolite is believed to act as a
competetive antagonist at opiod receptors.
 It is because of this reaction that
Naltrexone is believed to interact with the
dopaminergic mesolimbic pathway, which
alcohol activates, therby causing
pleasurable feelings.
Naltrexone Actions
 Naltrexone is aimed at reducing the
psychological need or craving for alcohol.
 Naltrexone can be administered in a 50mg
tablet with some nauseating side effects.
 A Naltrexone shot, administerd intrmuscularly, is also available.
 Naltrexone has been shown to be effective
for up to 30 days.
Naltrexone Safety
 Naltrexone is considered a relatively safe drug
for the treatment of Alcoholism.
 Little drug-drug interactions have been shown
and do not seem significant, except for
Naltrexone’s interaction with opiod analgetics.
 Some patients, while on Naltrexone have been
shown to turn away from alcohol only to pick up
another drug.
 After treatment with naltrexone, opiod receptors
are very sensitive and can lead patients to
overdose on some other drug.
Acamprosate (Campral)
 First approved by the
FDA in 2004,
although it has been
approved in Europe
since 1989
 Part of the reason for
the delay of approval
in the US was due to
the action of
Acamprosate not
being fully understood
Action of Acamprosate
 Alcohol inhibits the activity of receptors known as NMethy-D-aspartate receptors (or NMDARs), causing the
brain to create more NMDARs
 Absence of alcohol, or no inhibition of the receptor,
causes these receptors to be overly active and cause
symptoms such as delirium tremens (DT).
 Acamprosate is thought to reduce glutamate surges that
excite NMDARs. This property makes Acamprosate
useful in treating the withdrawal symptoms in alcoholics.
 Acamprosate has also been shown in some studies to
act as a neuro-protectant and protect neurons from
damage caused by alcohol withdrawal
Other Drugs
 Benzodiazepines have also been used to
treat alcohol withdrawal due to their
interaction with the GABA receptor.
 Emetine can be used in combination with
other drugs (creating a literal “drug
cocktail”) and be used in aversion therapy
as the “cocktail” will induce nausea and
vomiting.
Drugs Alone Are Not the Answer
 Because of the complexity of alcoholism, drugs
alone are not effective in “curing” alcoholism.
 Cases must also be treated on a case by case
basis, there is no set proven effective method for
everyone.
 Psychological measures (CBT) in combination
with drugs are usually employed, although
sometimes addictions are treated without drug
use.
An Example of a Program
 Shick Shadel Hospital’s program outline
for addiction treatment