Antabuse: A Clinically Proven Deterrent for Alcohol Use Disorder
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Synonyms | |||
Antabuse (disulfiram) represents a cornerstone of pharmacological aversion therapy in the treatment of chronic alcohol use disorder (AUD). It is not a cure for alcoholism, nor does it diminish the craving for alcohol. Instead, it acts as a powerful psychological and physiological deterrent by producing a highly unpleasant reaction when alcohol is consumed. This mechanism supports a patient’s commitment to abstinence by creating a significant negative reinforcement, allowing them to focus on the behavioral and psychosocial aspects of recovery within a comprehensive treatment plan. Its use is always contingent upon full patient informed consent and understanding.
Features
- Active Pharmaceutical Ingredient: Disulfiram.
- Mechanism of Action: Irreversible inhibition of the enzyme aldehyde dehydrogenase (ALDH).
- Dosage Forms: Oral tablets, typically 250 mg or 500 mg.
- Onset of Action: The disulfiram-ethanol reaction (DER) can occur within 5-10 minutes of alcohol ingestion.
- Duration of Effect: The inhibitory effect on ALDH can persist for up to 14 days after the last dose due to irreversible enzyme binding and the slow rate of enzyme regeneration.
- Prescription Status: Available by prescription only, following a thorough medical and psychiatric evaluation.
Benefits
- Creates a Powerful Psychological Barrier: The knowledge of the potential severe reaction serves as a strong deterrent, helping patients resist impulsive drinking.
- Supports Long-Term Abstinence Goals: By providing a consistent physiological consequence for alcohol consumption, it reinforces daily commitment to sobriety.
- Facilitates Engagement in Therapy: The safety net provided by Antabuse allows patients to more fully engage in concurrent counseling, cognitive behavioral therapy (CBT), and support group meetings without the constant fear of relapse.
- Provides a Structured Framework for Recovery: The daily ritual of taking the medication can help re-establish routine and reinforce the patient’s active role in their treatment plan.
- Used as Part of a Comprehensive Treatment Strategy: It is most effective when integrated into a multi-modal approach that addresses the psychological, social, and behavioral components of AUD.
Common use
Antabuse is indicated as an adjunctive therapy in the management of selected patients with a confirmed diagnosis of chronic alcohol use disorder who wish to maintain a state of enforced sobriety. It is prescribed for patients who are highly motivated, have undergone detoxification, and are fully aware of the consequences of alcohol consumption while on the medication. Its use is typically reserved for individuals in a supervised treatment program where the medication administration can be monitored, often by a spouse, family member, or healthcare provider, to ensure adherence and safety. It is not intended for use as a monotherapy.
Dosage and direction
Initialization Protocol: Treatment must never be initiated until the patient has abstained from alcohol for at least 12 hours and a negative baseline breathalyzer or blood alcohol test is confirmed. A typical initial dosing regimen in a medically supervised setting is 500 mg daily for one to two weeks. Maintenance Dosage: The maintenance dose can usually be reduced to 250 mg daily (range 125 mg to 500 mg). The dosage is highly individualized based on patient tolerance and the desired level of ALDH inhibition. Administration: The tablet should be taken orally once daily, preferably in the morning. It may be crushed and mixed with liquid if necessary. To ensure efficacy and prevent relapse, administration should be supervised by a responsible individual who can confirm ingestion. Duration of Therapy: The duration of treatment is indefinite and based on the patient’s ongoing recovery progress, motivation, and the clinical judgment of the prescribing physician. Continuous therapy for months or even years is common.
Precautions
- Informed Consent is Paramount: The patient must be fully educated, verbally and in writing, about the disulfiram-ethanol reaction, its dangers, and the multitude of hidden alcohol sources (e.g., sauces, mouthwashes, tonics, solvents, aftershaves).
- Hepatic Function Monitoring: Baseline liver function tests (LFTs) must be obtained before initiation and at regular intervals (e.g., every 2-3 months) during therapy due to the risk of disulfiram-induced hepatitis.
- Neuropsychiatric Monitoring: Patients should be monitored for the emergence of psychotic symptoms, depression, suicidal ideation, or peripheral neuropathy.
- Pregnancy and Lactation: Antabuse is contraindicated in pregnancy (Pregnancy Category C) and should not be used by nursing mothers.
- Rubber & Epoxy Sensitivity: Disulfiram can cause contact dermatitis for individuals working with or exposed to rubber accelerators or epoxy resins.
Contraindications
- Severe myocardial disease or coronary artery occlusion.
- Psychosis or severe intellectual impairment where the patient cannot comprehend the consequences of the therapy.
- Hypersensitivity to disulfiram or other thiuram derivatives used in pesticides or rubber vulcanization.
- Concurrent use of alcohol or alcohol-containing products (parabens as preservatives in some liquid medications are a concern).
- Pregnancy and lactation.
Possible side effect
Without Alcohol Ingestion:
- Common: Drowsiness, fatigue, headache, metallic or garlic-like aftertaste, acneiform eruptions.
- Less Common: Hepatotoxicity (ranging from transient transaminase elevations to fulminant hepatitis and hepatic failure), peripheral neuropathy, optic neuritis, psychotic reactions, polyneuritis.
Disulfiram-Ethanol Reaction (DER): This is an expected pharmacologic effect, not a side effect, but its severity constitutes a medical adverse event.
- Mild to Moderate: Facial flushing, throbbing headache, sweating, nausea, copious vomiting, thirst, chest pain, palpitations, tachycardia, hypotension, vertigo, blurred vision.
- Severe: Respiratory depression, cardiovascular collapse, acute congestive heart failure, convulsions, myocardial infarction, arrhythmias, and death.
Drug interaction
Antabuse inhibits several hepatic microsomal enzymes, including CYP450 2E1, and can alter the metabolism of numerous concomitant medications.
- Warfarin: Potentiates anticoagulant effect; prothrombin time must be monitored closely and warfarin dosage reduced.
- Phenytoin: Increases phenytoin serum levels and risk of toxicity; monitor levels.
- Benzodiazepines: Metabolism of certain benzodiazepines (e.g., chlordiazepoxide, diazepam) may be inhibited, potentiating their sedative effects.
- Isoniazid & Other CYP2E1 Substrates: Increased risk of neurotoxicity and adverse effects.
- Theophylline: Metabolism may be decreased, increasing the risk of theophylline toxicity.
- Tricyclic Antidepressants: Metabolism may be inhibited.
- Metronidazole: Concomitant use is contraindicated due to increased risk of psychotic reactions.
Missed dose
If a daily dose is missed, it should be taken as soon as remembered that same day. If it is not remembered until the next day, the missed dose should be skipped, and the regular dosing schedule resumed. Do not double the dose. The long duration of enzyme inhibition means a single missed dose does not immediately eliminate the protective effect against alcohol. However, consistent adherence is critical for the psychological deterrent to remain effective.
Overdose
Symptoms: Overdose without alcohol consumption may present as nausea, vomiting, GI upset, dizziness, ataxia, and neurological symptoms. In severe cases, it can lead to seizures, coma, and the clinical picture of acute hepatic failure. Management: There is no specific antidote for disulfiram overdose. Management is entirely supportive and symptomatic. Gastric lavage may be considered if ingestion was recent. Activated charcoal can be administered. Supportive care includes maintaining respiration, treating hypotension with IV fluids and vasopressors, managing seizures with benzodiazepines, and providing comprehensive supportive care for acute liver failure if it develops.
Storage
Store at controlled room temperature, 20°C to 25°C (68°F to 77°F). Excursions are permitted between 15°C and 30°C (59°F and 86°F). Dispense in a tight, light-resistant container as defined in the USP. Keep securely closed and out of sight and reach of children. Do not flush medications down the toilet or pour them into a drain.
Disclaimer
This information is for educational and informational purposes only and does not constitute medical advice. It is not a substitute for professional medical advice, diagnosis, or treatment. Always seek the advice of your physician or other qualified health provider with any questions you may have regarding a medical condition or medication. Never disregard professional medical advice or delay in seeking it because of something you have read here. The author and publisher are not responsible for any errors or omissions or for any outcomes related to the use of this information.
Reviews
- Clinical Evidence: “Numerous studies and decades of clinical use confirm that supervised disulfiram administration is highly effective in promoting continuous abstinence periods. Its efficacy is directly correlated with adherence, which is why supervised dosing is a critical success factor.” – Journal of Addiction Medicine
- Patient Experience (Composite): “Knowing the pill was in my system every morning gave me the strength to say ’no’ throughout the day. It wasn’t the pill that did the work, but it gave me the time and space to learn how to live without drinking. The fear of the reaction is very real and very effective.” – Anonymous, 4 years sober
- Clinician Perspective: “Antabuse is not a drug to be prescribed lightly. It requires a strong therapeutic alliance, thorough education, and a motivated patient. In the right candidate, it is an invaluable tool that provides a concrete biochemical ‘circuit breaker’ for impulsive behavior, allowing deeper psychological work to proceed.” – Board-Certified Addiction Psychiatrist