Disulfiram (Antabuse) Side Effects, Dosage and Interactions


About Antabuse

Antabuse is a medication that can help people with an alcohol use disorder stop drinking while they are in the early stages of recovery and beyond.


 

What Is Antabuse?

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Antabuse (disulfiram) is a medication that can be helpful in the treatment of severe alcohol use disorders. It is the first approved medication for the treatment of alcoholism, and its clinical use began in 1951.1

Antabuse is not a cure for an alcohol use disorder . It is a medication that can help people control their drinking while they are adjusting to their new lifestyle in recovery. A person who uses Antabuse should be committed to recovery and enrolled in a formalized treatment program .

How It Works

The physical reaction stops people from wanting to drink.
Disulfiram, the active ingredient in Antabuse, is an aldehyde dehydrogenase inhibitor. It interferes with the way a person's body metabolizes alcohol. When a person drinks alcohol , it is broken down into a compound called acetaldehyde. Acetaldehyde is then broken down by an enzyme that is produced by the liver called aldehyde dehydrogenase. Antabuse prevents aldehyde dehydrogenase from working properly.

Acetaldehyde is acidic, and as it builds up in the Antabuse user's system, it causes a number of unpleasant symptoms that include: 1

  • Feelings of dizziness due to a drop in blood pressure.
  • A racing heartbeat.
  • Headaches.
  • Shortness of breath.
  • Heart palpitations.
  • Nausea.
  • Vomiting.

This physical reaction is enough to stop people from wanting to drink alcohol.1 The reaction occurs within about 10 minutes of drinking alcohol, and the effects can last for several hours. Typically, one will experience the effects of Antabuse if they drink or use alcohol within 24 to 48 hours of taking the medication.

The psychological principle by which Antabuse works is known as aversion therapy. 2 When people associate becoming very ill with drinking alcohol, they become conditioned to not want to drink.

Use of Antabuse

Antabuse is not supposed to be a standalone method of treating an alcohol use disorder, and it is not marketed as a cure. Instead, it can be used with other methods of treatment to help a person remain sober during the early stages of treatment. Antabuse treatment is combined with other types of therapies such as counseling, group therapy and support groups.

Antabuse is only available with a prescription from a physician. It is also being evaluated for its effectiveness in the treatment of cocaine use disorder as well as in the treatment of HIV and certain types of cancer. 3, 4


Dosage Information

Antabuse is initially administered at a maximum of 500 mg daily. It comes in pill form and is taken with liquid. Most people take the drug in the morning in a single dose. But some may take it in the evening because it can produce mild sedation.

After 1 or 2 weeks, people go on a maintenance dose that does not exceed 500 mg daily. Typically, the dose is in the range of 125 to 500 mg per day. The average maintenance dose is 250 mg daily. 1, 5, 6

How to Take Antabuse

Antabuse should be taken exactly as prescribed. It is important to keep taking the medication regularly until formal plans have been made to discontinue it.

Additionally, people who take Antabuse need to be involved in a treatment program that includes counseling, social support and a long-term maintenance plan for recovery.

A good rule of thumb is to take the drug 12 to 24 hours after your last drink of alcohol.

What to Do if You Miss a Dose

You can take the dose if it is within 12 hours of the normal time that you would take the drug. However, if it is more than 12 hours after the time that you would normally take the drug, wait until your next scheduled dose to take it. Do not "double up" on the medication - this can lead to overdose.

Antabuse has a relatively slow half-life that ranges between about 60 and 120 hours. So for most people, it should not be taken within 12 hours of alcohol use. However, people who weigh less than 110 lbs. should wait longer, because body weight can determine how quickly one's body can rid itself of alcohol. 5 Due to its slow rate of elimination, Antabuse can remain effective in the body for up to 2 weeks after it is used. 1, 5

How Long Should You Take It?

There is no set time period for how long you should use the medication.

You should keep taking the drug every day until you have remained abstinent from alcohol for a significant period of time. At this point, you should speak with your treating physician or other alcohol recovery professional about discontinuing the medication. The effects of the drug can continue for up to 2 weeks after discontinuation, so it can still be effective if a person should relapse during that time period. In such cases, the medication can be restarted. 1


Antabuse Side Effects

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Several side effects may occur when using Antabuse:5

  • Acne.
  • Allergic dermatitis.
  • Mild drowsiness.
  • Fatigue.
  • Headache.
  • Impotence (in males).
  • A metallic or garlic-like taste in the mouth.

The side effects typically resolve within a couple of weeks or once the dosage is tapered down to a maintenance level. For most people, any reactions to the skin can be addressed with antihistamines. Hepatic toxicity is rare, but still a possibility in some users (due to problems with the liver metabolizing the drug).

Because of this risk, a blood sample may be required to run liver function testing prior to and throughout the course of Antabuse treatment, to assess for any hepatic injury.

When to Seek Medical Attention

Though rare, there is a small risk for hepatotoxicity with Antabuse use. Users who demonstrate the following signs and symptoms should receive immediate medical attention to preclude any worsening liver problems: 1, 5

  • Extreme tiredness or weakness.
  • Prolonged nausea and/or vomiting.
  • Fever.
  • A prolonged lack of energy.
  • Loss of appetite.
  • Symptoms of jaundice, such as yellowing of the skin and/or eyes.
  • Dark-colored urine.
  • Light-colored stools.
Further, you should let your physician know if you have any signs of mental confusion or psychiatric symptoms, such as hallucinations.

Before using Antabuse, tell your physician about any medical conditions you have and any medications that you are taking.

Risk Factors

Antabuse is not recommended for people with the following:1, 5

  • An active condition with a psychotic component, such as schizophrenia.
  • Cardiovascular disease or coronary arterial occlusions (blocked arteries).
  • Known liver damage.
  • Allergies to sulfur or nickel or known reactions to thiuram derivatives such as vulcanized rubber products or pesticides.
  • Pregnant or nursing women. Risks to the fetus or young children are unknown, and the drug should not be administered to nursing mothers or women who are pregnant or plan to become pregnant during the administration of the drug.
People with hypothyroidism, diabetes, kidney disease or epilepsy should be monitored closely while on the drug. People who have a history of traumatic brain injury should consult their doctor before using the drug.


Drug Interactions

Consuming any substance that contains alcohol will cause a reaction when taking Antabuse.

Avoid items such as:1, 5

  • Mouthwash.
  • Colognes and perfumes.
  • Certain prepared foods and beverages.
  • Fermented vinegar, marinades, sauces, etc.

In addition, Antabuse may interact with several other drugs.1, 5

  • It may interact produce unexplained bleeding in people who take anticoagulants.
  • It may produce excessive sedation in people who take anticonvulsant medications.
  • People who take central nervous system depressants, such as medications for anxiety or sedative medications to help them sleep, may experience an increased reaction that produces higher levels of sedation.
  • Medications with even low levels of alcohol may cause a reaction (e.g., cold medications, cough syrups, etc.).
  • Using Antabuse while taking Flagyl (metronidazole) may produce a reaction similar to alcohol or may produce confusion and psychosis.
  • People who use clozapine should not take Antabuse due to the potential toxic effects.
  • People who take isoniazid or other monoamine oxidase inhibitor drugs may experience an unsteady gait or mental confusion.
  • People who take tricyclic antidepressant medications may experience increased sedation.

Antabuse should never be administered to someone in a state of alcohol intoxication or alcohol withdrawal, or to someone who is unable to make a commitment to stop using alcohol, such as a person with a developmental disorder or dementia.


Antabuse Cost

The average cost of Antabuse is around $80 for a 30-day supply. Most insurance companies will cover the cost.

However, plans differ, and you should check with your insurance customer service representative to determine if your plan covers the cost of the medication.


How Effective Is It?

Obviously, Antabuse is only effective if the person takes the drug regularly. However, its effectiveness can be enhanced if the person taking the drug:

  • Is committed to total abstinence.
  • Fully understands the consequences of drinking alcohol while they are taking the drug.
  • Is both able to make a decision about its use and is medically appropriate to use the drug.
  • Can opt for supervised dosing (being administered the drug under the supervision of a family member, mental health worker or physician).

Research on Effectiveness

Antabuse is a well-researched medication, and a number of studies support its use. However, a couple things should be noted about the research.

First, much of the earlier research that supported its use produced mixed results. 6 Research studies supporting the effectiveness of Antabuse in reducing drinking in those with chronic alcoholism indicated that when the drug was taken as prescribed, there was a potential for it to be helpful in assisting individuals not to drink.

However, compliance with taking the drug has been a major issue in many studies. 6 Research has indicated that when someone is supervised while they take the drug, it enhances compliance with taking Antabuse and enhances the effectiveness of it. When people are left to take the drug on their own, however, compliance can be a problem. Many users find that they can stop taking Antabuse and begin drinking alcohol again in just a few days, leading to planned Antabuse holidays. 1, 6


Frequently Asked Questions

How Long Does Antabuse Stay in Your System?

Antabuse has a relatively long but variable half-life of between 60 and 120 hours. This means that in that time period, the level of the drug in your system will decrease by one-half.

In many cases, people still experience some portion of the full effects of the drug up to 2 weeks after discontinuing it. However, the drug will be eliminated from people's systems at different rates due to individual differences.

When Should I Stop Taking Antabuse?

Consult with your physician, counselor, treatment provider and/or family members before you stop using Antabuse.

You should establish a sufficient length of time of complete sobriety before stopping the medication. You should also be committed to continued abstinence.

How Do You Stop Using Antabuse?

You are not likely to experience significant withdrawal effects when you stop taking Antabuse. The medication can be discontinued when you have made a commitment to sobriety and your treatment team agrees.


Find an Alcohol Abuse Recovery Program

Having an alcohol use disorder is a serious and troubling issue. If you have questions about alcohol use disorder treatment, please call 1-888-319-2606Who Answers? . A recovery support specialist can verify which types of treatment your insurance will cover and let you know about any co-pays or fees.

If you do not have insurance, can the national helpline for the Substance Abuse and Mental Health Services Administration (SAMHSA) at 1-888-319-2606Who Answers? (HELP). You may qualify for special assistance that can help you find appropriate treatment programs or payment options.

Sources

[1]. Ries, R. K., Fiellin, D. A., Miller, S. C., & Saitz, R. (2014). The ASAM principles of addiction medicine. New York: Lippincott Williams & Wilkins.

[2]. Hatfield, R. C. (2013). The everything guide to the human brain. Avon, MA: Adams publishing.

[3]. Schottenfeld, R. S., Chawarski, M. C., Cubells, J. F., George, T. P., Lappalainen, J., & Kosten, T. R. (2014). Randomized clinical trial of disulfiram for cocaine dependence or abuse during buprenorphine treatment. Drug and alcohol dependence, 136, 36-42.

[4] Doyon, G., Zerbato, J., Mellors, J. W., & Sluis-Cremer, N. (2013). Disulfiram reactivates latent HIV-1 expression through depletion of the phosphatase and tensin homolog. Aid, 27(2), F7-F11.

[5]. Griffith, H. W. & Moore, S. W. (2015). Complete the guide to prescription and nonprescription drugs 2016 - 2017. New York: Random House.

[6]. Suh, J. J., Pettinati, H. M., Kampman, K. M., & O'Brien, C. P. (2006). The status of disulfiram: A half of a century later. Journal of clinical psychopharmacology, 26(3), 290-302.

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