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Disulfiram

Trade name Antabuse.

Administration by oral, and subdermal implant.

Metabolism by liver changes to diethylthiocarbamate.

Biological half-life 60–120 hours.

Used to support the treatment of chronic alcoholism by producing an acute sensitivity to alcohol.

Inhibits the enzyme acetaldehyde dehydrogenase, which manifests many of the effects of a hangover immediately after alcohol is consumed.

Alcohol is broken down in the liver by the enzyme alcohol dehydrogenase to acetaldehyde, which is then converted by the enzyme acetaldehyde dehydrogenase to a harmless acetic acid derivative acetyl coenzyme A.

After ingestion alcohol is converted to acetaldehyde, which is then broken down by aldehyde dehydrogenase.

If the dehydrogenase enzyme is inhibited, acetaldehyde builds up and causes unpleasant effects.

Should be used in conjunction with counseling and support.

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”.

Produces immediate and severe negative reaction to alcohol intake.

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, accelerated heart rate, shortness of breath, nausea, vomiting, throbbing headache, visual disturbance, mental confusion, postural syncope, and circulatory collapse.

Should not be taken if alcohol has been consumed in the last 12 hours.

There is no tolerance to disulfiram.

Absorbed slowly through the digestive tract and eliminated slowly.

A nine-year study found that incorporation of supervised disulfiram resulted in an abstinence rate of over 50%.

Disulfiram does not reduce alcohol cravings.

The most common side effects in the absence of alcohol are headache, and a metallic or garlic taste in the mouth.

Tryptophol, a chemical compound that induces sleep in humans, is formed in the liver after disulfiram treatment.

Cases of disulfiram neurotoxicity causing extrapyramidal and other symptoms have been reported.

Disulfiram disrupts metabolism of other compounds, including: acetaminophen, theophylline, and caffeine.

Disulfiram 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.

Antibiotics-metronidazole

First-generation sulfonylureas-tolbutamide and chlorpropamide

Several cephalosporin drugs, including cefoperazone, cefamandole and cefotetan, that have a N-methylthio-tetrazole moiety.

Griseofulvin

Procarbazine

Citrated calcium carbimide, has the same function as disulfiram, but is weaker and safer.

Administration is oral, or subdermal implant

Metabolism is hepatic.

Biological half-life 60–120 hours

Used to support the treatment of chronic alcoholism by producing an acute sensitivity to ethanol.

Disulfiram plus alcohol, even small amounts, produce flushing, throbbing in head and neck, throbbing headache, respiratory difficulty, nausea, copious vomiting, sweating, thirst, chest pain, palpitation, dyspnea, hyperventilation, tachycardia, hypotension, syncope, marked uneasiness, weakness, vertigo, blurred vision, and confusion.

Severe reactions there may be associated with respiratory depression, cardiovascular collapse, arrhythmias, myocardial infarction, acute congestive heart failure, unconsciousness, convulsions, and death

In the body, alcohol is converted to acetaldehyde, which is then broken down by aldehyde dehydrogenase. If the dehydrogenase enzyme is inhibited, acetaldehyde builds up and causes unpleasant effects.

Disulfiram is also a treatment for cocaine dependence, as it prevents the breakdown of dopamine, a neurotransmitter whose release is stimulated by cocaine.

There is no tolerance to disulfiram.

The longer it is taken, the stronger its effects.

As disulfiram is absorbed slowly through the digestive tract and eliminated slowly by the body.

Its effects may last for up to two weeks after the initial intake.

Does not reduce alcohol cravings.

Associated with this drug is extremely poor compliance at only 20%.

Often replaced or accompanied with newer drugs, primarily combination of naltrexone and acamprosate. which addresses physiological processes in the brain associated with alcohol abuse.

The most common side effects in the absence of alcohol are headache, and a metallic or garlic taste in the mouth.

Disulfiram neurotoxicity can occur, causing extrapyramidal symptoms.

Disulfiram disrupts metabolism of acetaminophen, theophylline and caffeine.

Works in motivated individuals with alcoholism if they can be monitored every day for adherence.

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