Drugs and substances with disulfiram like reactions
Drugs and substances with
Disulfiram like reactions.
Why is so important?
• This topic it’s important because for example
about 64% of adults in the United States
consumed alcohol in 2008. In that same year,
approximately 3.8 billion prescription
medications were dispensed.2 Despite this
high prevalence, few physicians discuss
alcohol use with their patients. In addition,
most patients do not consider alcohol a drug
capable of interacting with medications.
Disulfiram (sold under the trade names Antabuse and Antabus) :
An antioxidant that interferes with the normal metabolic degradation
of alcohol in the body,. Disulfiram is a drug discovered in the 1920s
and used to support the treatment of chronic alcoholism by
producing an acute sensitivity to alcohol. It blocks the processing of
alcohol in the body by inhibiting acetaldehyde dehydrogenase,
resulting in increased acetaldehyde concentrations in blood and
tissues thus causing an unpleasant reaction when alcohol is
consumed. Used in the treatment of chronic alcoholism. Also used as
a chelator in copper and nickel poisoning. Syn: tetraethylthiuram
Disulfiram is also being studied as a treatment for cocaine
dependence, as it prevents the breakdown of dopamine,
a neurotransmitter whose release is stimulated by cocaine
Uses : in alcohol abuse
Under normal metabolism, alcohol is broken down in the liver by the
enzyme alcohol dehydrogenase to acetaldehyde, which is then converted
by the enzyme acetaldehyde dehydrogenase to the harmless acetic acid.
Disulfiram blocks this reaction at the intermediate stage by blocking
acetaldehyde dehydrogenase. After alcohol intake under the influence of
disulfiram, the concentration of acetaldehyde in the blood may be five to
10 times higher than that found during metabolism of the same amount of
alcohol alone. As acetaldehyde is one of the major causes of the
symptoms of a "hangover", this produces immediate and severe negative
reaction to alcohol intake.
Some five to 10 minutes after alcohol intake, the patient may experience
the effects of a severe hangover for a period of 30 minutes up to several
hours. Symptoms include flushing of the skin, accelerated heart rate,
shortness of breath, nausea, vomiting, throbbing headache, visual
disturbance, mental confusion, postural syncope, and circulatory collapse.
La buveuse ("The Drinker"), a portrait of Suzanne
Valadon by Toulouse-Lautrec.
Alcohol flush reaction as a result
of the accumulation of
acetaldehyde, the first metabolite
Disulfiram like reaction:
• In medicine, the term "disulfiram reaction or
effect" refers to an adverse effect of a
particular medication in causing an unpleasant
hypersensitivity to alcohol, similar to the
effect caused by disulfiram administration.
• Hence this is kind of alcohol-drug interaction
and we will check interactions of alcohol with
Drugs that may produce disulfiram like reactions with
ethanol include the following:
(eg, Coprinus atramentarius [inky cap], Clitocybe claviceps)
metronidazole,Tinidazole is chemically similar to metronidazole and so may cause the
some cephalosporins( eg: cephamandole, cefoperazone, cefmenoxime, cefotetan,
Moxalactam)- due to METHYLTETRAZOLETHIOL side chain.
Oral hypoglycemics (eg: chlorpropamide, tolbutamide)- these sulphonylureas compete
with acetaldehyde for binding sites on ALDH.
Pesticides (eg: carbamates, monosulfiram [Tetmosol])
Hence it’s important to consider these before
prescribing or dispensing above drugs.
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