Skip to content

Understanding the Science: What is the mechanism of action of Antabus?

3 min read

According to the National Institute on Alcohol Abuse and Alcoholism, almost 30 million people in the U.S. had alcohol use disorder in 2022. For some individuals, a medication called Antabus (disulfiram) is used as a deterrent, and its effectiveness is rooted in a specific pharmacological process, explaining what is the mechanism of action of Antabus.

Quick Summary

Antabus (disulfiram) functions by inhibiting the enzyme aldehyde dehydrogenase, which prevents the proper breakdown of alcohol's toxic byproduct, acetaldehyde. This metabolic disruption leads to a severe, unpleasant physical reaction when alcohol is consumed, creating a powerful deterrent against drinking.

Key Points

  • Enzyme Inhibition: Antabus (disulfiram) works by irreversibly inhibiting the enzyme aldehyde dehydrogenase (ALDH) in the liver.

  • Acetaldehyde Accumulation: Without functional ALDH, the toxic intermediate product of alcohol metabolism, acetaldehyde, builds up in the bloodstream.

  • Aversive Reaction: The accumulation of acetaldehyde causes a highly unpleasant physical reaction, including flushing, nausea, and headache, which acts as a deterrent to drinking.

  • Sustained Effect: The inhibitory effect of Antabus can last for up to two weeks after the last dose, meaning a reaction can still occur long after a patient has stopped taking the medication.

  • Deterrent, Not a Cure: Antabus is not a cure for alcoholism and does not address cravings; instead, it provides a psychological barrier against relapse.

  • Comprehensive Treatment: It is most effective when used as part of a supervised, comprehensive treatment plan that includes counseling and therapy.

In This Article

The Core Mechanism of Antabus (Disulfiram)

Antabus, also known by its generic name disulfiram, is a medication used in the treatment of chronic alcoholism. Its primary function is to create a negative physical reaction if alcohol is consumed, acting as a deterrent rather than directly reducing cravings. Disulfiram interferes with the body's process of metabolizing alcohol by inhibiting a key enzyme, resulting in the build-up of a toxic compound. This leads to an unpleasant reaction that discourages drinking, supporting individuals in their commitment to sobriety.

Normal Alcohol Metabolism

Under normal conditions, the body metabolizes alcohol (ethanol) in a two-step process, mainly in the liver:

  1. Alcohol dehydrogenase (ADH) converts ethanol into acetaldehyde, a toxic substance.
  2. Aldehyde dehydrogenase (ALDH) rapidly converts acetaldehyde into harmless acetate. Acetate is then further broken down and eliminated from the body.

The Disulfiram-Alcohol Reaction

Antabus inhibits the ALDH enzyme, preventing the conversion of acetaldehyde to acetate. When alcohol is consumed while taking Antabus:

  • ADH still produces acetaldehyde.
  • The inhibited ALDH cannot process acetaldehyde, leading to its significant accumulation in the bloodstream.
  • This build-up triggers a severe and unpleasant reaction within 10 to 30 minutes.

The severity of this disulfiram-alcohol reaction depends on the amounts of alcohol and disulfiram present.

Symptoms of the Disulfiram-Alcohol Reaction

The unpleasant symptoms, which serve as a deterrent, can include:

  • Flushing
  • Headache
  • Nausea and vomiting
  • Sweating
  • Chest pain and heart palpitations
  • Difficulty breathing
  • Rapid heart rate and low blood pressure
  • Dizziness and blurred vision
  • Weakness and confusion

In rare but severe cases, this reaction can be life-threatening. Therefore, patients must be fully informed about the risks of drinking while taking this medication.

Pharmacokinetics and Sustained Effects

Disulfiram is absorbed and eliminated slowly from the body. Its active metabolites continue to inhibit ALDH for an extended period. This means that the deterrent effect can last for up to two weeks after the last dose of Antabus, providing a sustained barrier against impulsive drinking.

Antabuse vs. Other Medications for Alcohol Use Disorder

Antabuse is one of several medications for alcohol use disorder (AUD) and is often used alongside other therapies. Its mechanism differs from other common AUD medications:

Feature Antabuse (Disulfiram) Naltrexone (oral and Vivitrol) Acamprosate (Campral)
Mechanism of Action Inhibits aldehyde dehydrogenase, causing a severe physical reaction to alcohol. Blocks the euphoric and sedative effects of alcohol by affecting opioid receptors in the brain. Helps restore the natural balance of neurotransmitters in the brain that may be altered by long-term alcohol use.
Main Effect Creates an aversive reaction to deter drinking. Reduces cravings and the pleasure associated with drinking. Reduces symptoms of prolonged withdrawal, helping to maintain abstinence.
Patient Profile Best for individuals committed to abstinence with a supportive environment or supervised dosing. Useful for patients who want to reduce their alcohol consumption, including those not yet abstinent. Works best after a person has already gone through detox and achieved initial abstinence.
Frequency Once daily oral tablet. Once daily oral tablet or once-monthly injection. Three times daily oral tablet.

Conclusion: The Deterrent Effect

The mechanism of action of Antabus creates a powerful pharmacological deterrent by interfering with alcohol metabolism and causing an unpleasant reaction upon consumption. This effect supports motivated individuals in maintaining sobriety, particularly as part of a comprehensive treatment program that includes counseling. Patients must be aware of the potentially severe side effects and the importance of complete abstinence from alcohol, as the medication's effects can last for a significant time, providing a sustained barrier against relapse.

For Further Reading

For more detailed information on disulfiram, its pharmacology, and use in treating alcohol dependence, refer to the following resource:

Frequently Asked Questions

Consuming alcohol while on Antabus causes a severe and highly unpleasant reaction, including facial flushing, throbbing headache, nausea, vomiting, sweating, chest pain, and rapid heart rate.

The duration of the reaction varies from 30 to 60 minutes for mild cases, but can last for several hours in more severe instances or until the alcohol is fully metabolized.

Disulfiram and its active metabolites are eliminated slowly, and its deterrent effects on alcohol metabolism can last for up to two weeks after the last dose.

Patients should avoid all products containing alcohol, including mouthwash, cough syrups, aftershave, certain foods cooked with alcohol, and even some hand sanitizers.

No, Antabus is not a cure for alcoholism. It is a tool used as part of a broader treatment plan, serving as a deterrent to drinking rather than addressing the underlying causes of addiction.

Antabus is most effective when used in conjunction with other forms of treatment, such as counseling and behavioral therapy, and often requires supervision to ensure adherence.

Common side effects without alcohol exposure can include a garlic-like or metallic taste in the mouth, skin rashes, mild headaches, drowsiness, and fatigue.

Antabus is contraindicated for those with severe heart disease, psychosis, or hypersensitivity to disulfiram. It should also be used with caution in patients with liver or kidney disease, diabetes, or epilepsy.

References

  1. 1
  2. 2
  3. 3
  4. 4
  5. 5
  6. 6
  7. 7
  8. 8
  9. 9

Medical Disclaimer

This content is for informational purposes only and should not replace professional medical advice.