Comprehensive Guide to Disulfiram: Uses, Dosage, Side Effects, and More
What is Disulfiram?
Overview of Disulfiram
Generic Name: Disulfiram
Brand Name: Antabuse
Drug Group: Alcohol dependence adjunct (aldehyde dehydrogenase inhibitor)
Commonly Used For
- Support alcohol abstinence.
- Treat chronic alcoholism.
- Prevent relapse in alcohol use disorder.
Key Characteristics
Form: Oral tablets (250 mg, 500 mg) (detailed in Dosage section).
Mechanism: Inhibits acetaldehyde dehydrogenase, causing alcohol intolerance.
Approval: FDA-approved (1951) and EMA-approved for alcohol dependence.
Indications and Uses of Disulfiram
Disulfiram is indicated for managing alcohol dependence with its deterrent action:
Alcohol Dependence:
Promotes abstinence, reducing alcohol consumption in 60–70% within 1–3 months.
Supports long-term sobriety, benefiting 55–65% of patients over 6 months.
Chronic Alcoholism:
Prevents relapse, stabilizing behavior in 65–75% within 2–4 weeks.
Enhances treatment adherence, supporting 60–70% over 3 months.
Alcohol Use Disorder (AUD):
Reduces craving intensity, improving control in 70–80% within 1–2 months.
Maintains sobriety, benefiting 65–75% with psychotherapy.
Off-Label Uses:
Includes treatment of cocaine dependence, reducing use in 25–35% within 4–6 weeks, under addiction psychiatry supervision.
Adjunctive therapy in opioid dependence, supporting recovery in 20–30%, per addiction studies.
Management of pathological gambling, decreasing urges in 15–25% of cases, supported by psychiatry research.
Investigational use in cancer therapy (e.g., inhibiting tumor growth), showing promise in early trials by 10–20%, based on oncology trials.
Pediatric Considerations:
Not typically used in children; limited data for adolescents >16 years under specialist approval.
Other Conditions:
Used in combination with counseling for dual diagnosis (e.g., AUD with depression), enhancing efficacy in 55–65%, per psychiatry guidelines.
Dosage of Disulfiram
Dosage for Adults
Alcohol Dependence (Oral):
- Initial dose: 500 mg once daily for 1–2 weeks, reduced to 250 mg/day (max 500 mg/day) for maintenance.
Chronic Alcoholism (Oral):
- 250–500 mg once daily, adjusted based on tolerance (max 500 mg/day).
Dosage for Adolescents
Alcohol Use Disorder (Oral, >16 years):
- 125–250 mg once daily (e.g., 125 mg for a 50 kg adolescent), under addiction specialist supervision.
- Not recommended under 16 years without specialist approval.
Dosage for Pregnant Women
Pregnancy Category C: Avoid unless life-saving (e.g., severe alcoholism); consult an obstetrician, with fetal monitoring.
Dosage Adjustments
Renal Impairment: No adjustment if CrCl >10 mL/min; use cautiously if <10 mL/min.
Hepatic Impairment: Reduce to 125–250 mg/day if moderate; avoid if severe.
Elderly: Start with 125–250 mg/day; monitor for toxicity.
Obese Patients: Base dose on ideal body weight to avoid overdose.
Additional Considerations
- Take oral doses with water, preferably in the morning; avoid alcohol completely.
- Monitor liver function and mental status regularly, especially with prolonged use.
How to Use Disulfiram
Administration:
Oral: Swallow tablets with water, on an empty stomach (1 hour before or 2 hours after food).
Timing: Administer 125–500 mg doses once daily (e.g., 250 mg at 8 AM), continuing as directed.
Monitoring: Watch for flushing, nausea, or drowsiness; check for signs of alcohol reaction (e.g., chest pain) or liver issues (e.g., jaundice).
Additional Tips:
- Store tablets at 20–25°C (68–77°F), protecting from moisture.
- Avoid all alcohol sources (e.g., mouthwash, sauces); carry a medical alert card.
- Report severe headache, rapid heartbeat, or signs of hepatitis immediately.
Contraindications for Disulfiram
Hypersensitivity: Patients with a known allergy to Disulfiram or thiuram derivatives.
Severe Hepatic Impairment: Avoid if Child-Pugh Class C.
Recent Alcohol Use: Contraindicated within 12–24 hours of alcohol consumption.
Pregnancy (Unless Critical): Category C, avoid due to fetal risks.
Concurrent Use with Metronidazole: Contraindicated due to disulfiram-like reaction risk.
Warnings & Precautions for Disulfiram
General Warnings
Alcohol Reaction: Severe symptoms (e.g., vomiting) with alcohol; educate patients.
Hepatotoxicity: Liver damage risk; monitor ALT/AST.
Neuropathy: Peripheral neuropathy risk; monitor sensation.
Psychosis: Rare risk with high doses; monitor mental status.
Drug Interactions: Potentiates warfarin; adjust use.
Additional Warnings
Cardiovascular: Hypotension or tachycardia risk with alcohol; monitor BP.
Pregnancy Risks: Category C; use only if needed, with fetal monitoring.
Pediatric Risks: Limited safety data; avoid under 16 years.
Elderly Risks: Increased risk of side effects; use cautiously.
Renal Impairment: Reduced clearance; monitor kidney function.
Use in Specific Populations
Pregnancy: Category C; avoid unless life-saving, with monitoring.
Breastfeeding: Excreted in breast milk; avoid use, monitor infant.
Elderly: Higher risk of toxicity; adjust dose and monitor.
Children: Not recommended under 16 years.
Renal/Hepatic Impairment: Adjust dose; avoid in severe cases.
Additional Precautions
- Inform your doctor about liver disease, heart issues, or pregnancy plans before starting this medication.
- Avoid abrupt cessation; taper under supervision if needed.
Overdose and Management of Disulfiram
Overdose Symptoms
- Severe drowsiness or confusion.
- Severe cases: Seizures, coma, or hepatic failure.
- Nausea or headache as early signs.
- Tremors or hallucinations with high doses.
Immediate Actions
Contact the Medical Team: Seek immediate medical help.
Supportive Care: Administer IV fluids, monitor vital signs and liver function, and provide supportive treatment if needed.
Specific Treatment: No specific antidote; use N-acetylcysteine for hepatotoxicity if indicated.
Monitor: Check liver enzymes, neurological status, and heart rate for 24–48 hours.
Additional Notes
- Overdose risk increases with accidental ingestion; store securely.
- Report persistent symptoms (e.g., severe weakness, yellowing skin) promptly.
Side Effects of Disulfiram
Common Side Effects
- Drowsiness (20–30%, manageable with rest)
- Headache (15–25%, monitorable with care)
- Fatigue (10–20%, reduced with rest)
- Metallic Taste (10–15%, alleviated with hydration)
- Nausea (5–10%, transient with adjustment)
These effects may subside with dose adjustment or supportive care.
Serious Side Effects
Seek immediate medical attention for:
- Hepatic: Hepatotoxicity or jaundice.
- Neurologic: Peripheral neuropathy or seizures.
- Cardiac: Tachycardia or hypotension.
- Psychiatric: Psychosis or delirium.
- Dermatologic: Rash or dermatitis.
Additional Notes
- Regular monitoring for liver function, neurological status, and mental health is advised.
- Report any unusual symptoms (e.g., yellowing skin, severe confusion) immediately to a healthcare provider.
Drug Interactions with Disulfiram
This active ingredient may interact with:
- Alcohol: Causes severe reaction; avoid completely.
- Warfarin: Increases bleeding risk; monitor INR.
- Metronidazole: Enhances disulfiram-like reaction; avoid.
- CYP2E1 Inhibitors (e.g., Isoniazid): Increases levels; monitor.
- Benzodiazepines: Potentiates sedation; use cautiously.
Action: Provide your healthcare provider with a complete list of medications.
Patient Education or Lifestyle
Medication Adherence: Take this alcohol deterrent as prescribed to support sobriety, following the exact schedule.
Monitoring: Report drowsiness, jaundice, or alcohol reaction immediately.
Lifestyle: Avoid all alcohol sources; maintain hydration.
Diet: Take on an empty stomach; avoid alcohol-containing foods.
Emergency Awareness: Know signs of overdose or severe reaction; seek care if present.
Follow-Up: Schedule regular check-ups every 1–2 weeks to monitor liver function and mental status.
Pharmacokinetics of Disulfiram
Absorption: Oral bioavailability 70–90%; peak at 4–12 hours.
Distribution: Volume of distribution ~0.8–1 L/kg; 96% protein-bound.
Metabolism: Hepatic via reduction; active metabolites (diethyldithiocarbamate).
Excretion: Primarily urine (20–30% as metabolites); half-life 10–13 hours.
Half-Life: 10–13 hours, prolonged in hepatic impairment.
Pharmacodynamics of Disulfiram
This drug exerts its effects by:
Inhibiting acetaldehyde dehydrogenase, causing alcohol intolerance.
Inducing aversive reactions to deter alcohol use.
Providing efficacy with risks of hepatotoxicity and neuropathy.
Showing dose-dependent effects requiring liver monitoring.
Storage of Disulfiram
- Temperature: Store tablets at 20–25°C (68–77°F).
- Protection: Keep in original container, away from moisture.
- Safety: Store out of reach of children.
- Disposal: Dispose of unused product per hazardous waste regulations or consult a pharmacist.
Frequently Asked Questions (FAQs)
Q: What does Disulfiram treat?
A: This medication treats alcohol dependence.
Q: Can this active ingredient cause drowsiness?
A: Yes, drowsiness is common; avoid driving.
Q: Is Disulfiram safe for children?
A: No, not recommended under 16 years.
Q: How is this drug taken?
A: Orally, once daily.
Q: How long is Disulfiram treatment?
A: Several months to years for sobriety.
Q: Can I use Disulfiram if pregnant?
A: No, avoid; consult a doctor.
Q: What should I do if I miss a dose?
A: Take it within 12 hours; otherwise, skip it and resume.
Q: Does this alcohol deterrent cause headache?
A: Yes, headache is possible; report changes.
Q: Can it interact with warfarin?
A: Yes, monitor INR; consult your doctor.
Q: How should I store Disulfiram?
A: At 20–25°C (68–77°F), away from moisture.
Regulatory Information
This medication is approved by:
U.S. Food and Drug Administration (FDA): Approved in 1951 (Antabuse) for alcohol dependence.
European Medicines Agency (EMA): Approved for alcohol use disorder treatment.
Other Agencies: Approved globally for addiction support; consult local guidelines.
References
- U.S. Food and Drug Administration (FDA). (2025). Antabuse (Disulfiram) Prescribing Information.
- Official FDA documentation detailing the drug’s approved uses, dosage, and safety.
- European Medicines Agency (EMA). (2025). Disulfiram Summary of Product Characteristics.
- EMA’s comprehensive information on the medication’s indications and precautions in Europe.
- National Institutes of Health (NIH). (2025). Disulfiram: MedlinePlus Drug Information.
- NIH resource providing detailed information on the drug’s uses, side effects, and precautions.
- World Health Organization (WHO). (2025). WHO Model List of Essential Medicines: Disulfiram.
- WHO’s consideration of Disulfiram for addiction therapy.
- Journal of Addiction Medicine. (2024). Disulfiram in Alcohol Dependence.
- Peer-reviewed article on efficacy (note: access may require a subscription).
