Antabuse: Clinically Proven Alcohol Deterrent Therapy
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Synonyms | |||
Antabuse (disulfiram) is a prescription medication indicated as an adjunct in the management of chronic alcohol dependence. It functions as an aversive agent, creating a highly unpleasant physiological reaction if alcohol is consumed while the drug is active in the system. This pharmacological deterrent supports patients committed to maintaining sobriety by providing a powerful psychological and physical barrier against impulsive drinking. Its use is integrated into a comprehensive treatment plan that includes counseling and psychosocial support.
Features
- Active Pharmaceutical Ingredient: Disulfiram.
- Mechanism of Action: Irreversible inhibition of the enzyme aldehyde dehydrogenase (ALDH).
- Pharmacokinetics: Slowly and incompletely absorbed from the gastrointestinal tract; elimination is slow, and effects may persist for up to 14 days after the last dose.
- Administration: Oral tablet.
- Available Strengths: 250 mg and 500 mg tablets.
Benefits
- Provides a powerful psychological deterrent against alcohol consumption, reinforcing a patient’s commitment to sobriety.
- Creates a predictable and highly unpleasant physical reaction upon alcohol ingestion, which can help break the cycle of compulsive drinking.
- Allows patients to feel a greater sense of control over their recovery journey within a structured treatment plan.
- Serves as a tangible tool in comprehensive addiction therapy, complementing behavioral interventions and counseling.
- Can help re-establish trust with family and support systems by demonstrating a concrete commitment to abstinence.
Common use
Antabuse is prescribed for the management of chronic alcoholism in patients who wish to remain in a state of enforced sobriety. It is most effective when used as part of a supervised, comprehensive treatment program that includes medical supervision, psychological support, counseling, and social support. The patient must be fully informed, motivated, and voluntarily consent to therapy, fully understanding the consequences of alcohol consumption while on the medication. It is not a cure for alcoholism but an enforcement tool to discourage drinking.
Dosage and direction
Initial dosage must be individualized and initiated only when the patient has abstained from alcohol for at least 12 hours and is in a state of relative sobriety, without evidence of intoxication or withdrawal.
- Initial Maintenance Therapy: A maximum of 500 mg daily is given as a single dose for one to two weeks.
- Maintenance Therapy: The average maintenance dose is 250 mg daily (range 125 mg to 500 mg). The dosage may be adjusted downward based on patient response and the emergence of side effects.
- Administration: The tablet should be taken in the morning, as the temptation to drink may be greater later in the day. It may be crushed and mixed with liquid if necessary.
- Duration of Therapy: The duration of treatment is continuous and individualized, based on the patient’s progress within their overall treatment plan. Discontinuation should be managed by a physician.
The patient must be reminded that the drug-induced sensitivity to alcohol will persist for a significant period (up to 14 days) after the last dose.
Precautions
- Informed Consent: It is imperative that the patient provides fully informed consent, comprehending the disulfiram-alcohol reaction’s nature and risks. A written consent form is often used.
- Supervision: Therapy should be initiated under close medical supervision. Ideally, a family member or caregiver should supervise daily dosing to ensure compliance.
- Alcohol Avoidance: Patients must be explicitly warned to avoid all sources of alcohol, including disguised sources like sauces, vinegars, cough syrups, mouthwashes, aftershaves, and even topical applications or fumes from solvents and varnishes.
- Hepatic Function: Baseline liver function tests (LFTs) should be performed before initiation and periodically during therapy (e.g., every 2-3 months for the first year and semi-annually thereafter) due to the risk of hepatotoxicity.
- Psychiatric Status: Use with caution in patients with diabetes mellitus, hypothyroidism, epilepsy, cerebral damage, chronic and acute nephritis, hepatic disease or impairment, and cardiovascular disease.
- Pregnancy and Lactation: Antabuse is contraindicated in pregnancy. It is not known if disulfiram is excreted in human milk; a decision should be made to discontinue nursing or discontinue the drug.
Contraindications
Antabuse is absolutely contraindicated in the presence of:
- Severe myocardial disease or coronary occlusion.
- Psychosis.
- Hypersensitivity to disulfiram or other thiuram derivatives used in pesticides and rubber vulcanization.
- Concurrent ingestion of alcohol or alcohol-containing products.
- Pregnancy.
Relative contraindications requiring extreme caution include:
- History of severe hepatic impairment or cirrhosis.
- Renal impairment.
- Diabetes mellitus.
- Epilepsy or seizure disorder.
- Hypothyroidism.
Possible side effect
The most significant “side effect” is the intentional disulfiram-ethanol reaction (DER), detailed below. Other non-DER related adverse reactions include:
- Dermatological: Skin eruptions, acneiform eruptions, allergic dermatitis, urticaria.
- Neurological: Drowsiness, fatigue, headache, peripheral neuropathy (including paresthesia, muscle weakness), polyneuritis, optic neuritis.
- Psychiatric: Psychotic reactions, memory impairment, confusion, restlessness.
- Hepatic: Hepatitis (including cholestatic and cytotoxic types), hepatic failure (rare but potentially fatal).
- Gastrointestinal: Metallic or garlic-like aftertaste, halitosis, nausea, vomiting.
- Other: Impotence.
The Disulfiram-Ethanol Reaction (DER): This is a pharmacologically expected outcome, not an allergic reaction. Symptoms occur within 5-10 minutes of alcohol ingestion and can last from 30 minutes to several hours. Severity is proportional to the amount of disulfiram and alcohol ingested. Symptoms include:
- Flushing of the face
- Throbbing headache
- Respiratory difficulty, hyperventilation
- Tachycardia, hypotension
- Sweating, thirst
- Nausea and violent vomiting
- Chest pain, palpitations
- Vertigo, blurred vision
- Confusion, weakness, anxiety
- In severe cases: respiratory depression, cardiovascular collapse, arrhythmias, acute congestive heart failure, unconsciousness, convulsions, myocardial infarction, and death.
Drug interaction
Antabuse can interact with numerous medications due to its inhibition of several liver enzyme systems, including CYP450 enzymes.
- Alcohol: Any product containing ethanol (see Precautions).
- Warfarin: Disulfiram may potentiate the anticoagulant effect of warfarin by inhibiting its metabolism, increasing the risk of bleeding. Prothrombin time (PT/INR) must be monitored closely.
- Phenytoin: Disulfiram can inhibit the metabolism of phenytoin, leading to phenytoin toxicity. Monitor phenytoin levels closely.
- Benzodiazepines: Metabolism of certain benzodiazepines (e.g., chlordiazepoxide, diazepam) may be inhibited, potentiating their sedative effects.
- Isoniazid: Increased risk of unsteadiness, dizziness, and behavioral changes.
- Theophylline: Disulfiram may decrease theophylline metabolism, increasing the risk of theophylline toxicity.
- Tricyclic Antidepressants: Metabolism may be inhibited.
- Metronidazole: Concomitant use may induce confusion and psychotic reactions; avoid combination.
- CNS Depressants: Additive sedative effects with barbiturates and other sedatives.
Missed dose
If a dose is missed, it should be taken as soon as possible on the same day. However, if it is not remembered until the next day, the missed dose should be skipped. The patient should never double the dose to make up for a missed one. The patient should inform their physician or supervising family member of the missed dose. The protective effect against alcohol may be diminished if doses are missed.
Overdose
Overdose may present as an extension of its pharmacological effects and adverse reactions.
- Symptoms: Nausea, vomiting, GI upset, dizziness, ataxia, lethargy, incoordination, seizures, extrapyramidal symptoms, stupor, and coma. Neurological symptoms are prominent. Hepatic damage may be delayed.
- Management: There is no specific antidote for disulfiram overdose. Management is supportive and symptomatic. Gastric lavage may be considered if performed soon after ingestion. Support respiratory and cardiovascular function. Monitor vital signs and fluid/electrolyte balance. Hemodialysis is not likely to be effective due to disulfiram’s high protein binding and large volume of distribution. Treat seizures with intravenous benzodiazepines.
Storage
- Store at controlled room temperature, 20°C to 25°C (68°F to 77°F).
- Keep in the original container, tightly closed, and protected from light and moisture.
- Keep out of reach of children and pets.
- Do not flush medications down the toilet or pour them into a drain unless instructed to do so.
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 consequences from the application of this information.
Reviews
- Clinical Efficacy (5/5): “As an addiction specialist for over 20 years, Antabuse remains a cornerstone tool for motivated patients within a structured program. Its efficacy is unparalleled as a psychological and physical deterrent. It provides a concrete ’line in the sand’ that many patients need, especially in early recovery.”
- Patient Experience (4/5): “It gave me the fear I needed to get through the first year. Knowing the severe reaction was a constant, powerful reminder that stopped me from making impulsive decisions. The metallic taste was bothersome but a small price to pay for my sobriety.”
- Safety Profile (3/5): “A highly effective but serious medication. Requires vigilant monitoring for hepatotoxicity and neuropathic side effects. Patient selection and education are paramount. It is not a drug to be prescribed lightly; the risks are significant but manageable under close supervision for the right candidate.”
