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Drugs and substances with
Disulfiram like reactions.
Salum Mkata
CSEE, ACSEE,B.pham.
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.
Definitions
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
disulfide.
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
Structure
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.
Reaction it interfered
Cont.

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
of alcohol
Cont.
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
medications .
Drugs that may produce disulfiram like reactions with
ethanol include the following:
Mushrooms :

(eg, Coprinus atramentarius [inky cap], Clitocybe claviceps)

Antibiotics :
•
•
•
•
•
•
•
•
•
•
•

metronidazole,Tinidazole is chemically similar to metronidazole and so may cause the
same reaction
sulfonamides( trimethoprim-sulfamethoxazole)
some cephalosporins( eg: cephamandole, cefoperazone, cefmenoxime, cefotetan,
Moxalactam)- due to METHYLTETRAZOLETHIOL side chain.
nitrofurantoin,
chloramphenicol
furazolidine
Antimalarial Quinacrine
Oral hypoglycemics (eg: chlorpropamide, tolbutamide)- these sulphonylureas compete
with acetaldehyde for binding sites on ALDH.
Pesticides (eg: carbamates, monosulfiram [Tetmosol])
Chloral hydrate
Antifungals (griseofulvin)
Cont.
Hence it’s important to consider these before
prescribing or dispensing above drugs.
Thank you
• Please add comments or any addition
information to this presentation. Or you can
support me to do more.

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Drugs and substances with disulfiram like reactions

  • 1. Drugs and substances with Disulfiram like reactions. Salum Mkata CSEE, ACSEE,B.pham.
  • 2. 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.
  • 3. Definitions 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 disulfide. 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
  • 5. 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.
  • 7. Cont. 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 of alcohol
  • 8. Cont. 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 medications .
  • 9. Drugs that may produce disulfiram like reactions with ethanol include the following: Mushrooms : (eg, Coprinus atramentarius [inky cap], Clitocybe claviceps) Antibiotics : • • • • • • • • • • • metronidazole,Tinidazole is chemically similar to metronidazole and so may cause the same reaction sulfonamides( trimethoprim-sulfamethoxazole) some cephalosporins( eg: cephamandole, cefoperazone, cefmenoxime, cefotetan, Moxalactam)- due to METHYLTETRAZOLETHIOL side chain. nitrofurantoin, chloramphenicol furazolidine Antimalarial Quinacrine Oral hypoglycemics (eg: chlorpropamide, tolbutamide)- these sulphonylureas compete with acetaldehyde for binding sites on ALDH. Pesticides (eg: carbamates, monosulfiram [Tetmosol]) Chloral hydrate Antifungals (griseofulvin)
  • 10. Cont. Hence it’s important to consider these before prescribing or dispensing above drugs.
  • 11. Thank you • Please add comments or any addition information to this presentation. Or you can support me to do more.