Drug for alcohol use disorder, aldehyde dehydrogenase inhibitor
Brand names: Antabuse
Updated · Methodology
Second line
Disulfiram is used in chronic alcohol use disorder as a second-line drug after naltrexone and acamprosate. Prescribed for motivated patients ready for full abstinence, usually combined with psychotherapy and a support group. SOCIDROGALCOHOL stresses mandatory patient education about the alcohol reaction and supervised dosing (often by a family member).
ICD-10: F10.2 · ICD-11: 6C40.2
Irreversibly inhibits mitochondrial aldehyde dehydrogenase (ALDH2). With alcohol intake, acetaldehyde accumulates and causes nausea, vomiting, facial flushing, tachycardia, hypotension and anxiety – the disulfiram-ethanol reaction. Also inhibits dopamine beta-hydroxylase and CYP2E1. Effect persists 7–14 days after withdrawal.
Limited data. Use only if benefit outweighs risk.
No milk excretion data. Breastfeeding not recommended.
Reference information, not a clinical decision. Discuss feeding pauses or changes with your physician or an IBCLC.
2 pairs found. Sorted from critical to minor.
Mechanism
The disulfiram label attributes the interaction to a possible synergistic effect of the two drugs that causes an acute psychotic reaction and confusion. Psychotic reactions have been reported in patients with alcohol dependence who took metronidazole together with disulfiram.
Symptoms
Confusion and acute psychotic reactions in a patient who takes disulfiram or has recently taken it.
Management
The combination is contraindicated in the disulfiram label and in the US Food and Drug Administration () labels for disulfiram and metronidazole. Do not start disulfiram in a patient who is taking metronidazole or has recently taken it (disulfiram label). Do not give metronidazole to a patient who has taken disulfiram within the last two weeks (metronidazole FDA label). The Spanish metronidazole label also says the combination must be avoided (metronidazole label).
Sources
Verbatim lines from the interaction sections, in the language of the label
«CONTRAINDICATIONS: Patients who are receiving or have recently received metronidazole, paraldehyde, alcohol, or alcohol-containing preparations, e.g., cough syrups, tonics and the like, should not be…»FDA, section 4 · Open on DailyMed
«Drug Interactions: It may be necessary to adjust the dosage of oral anticoagulants upon beginning or stopping disulfiram, since disulfiram may prolong prothrombin time.»FDA, section 7 · Open on DailyMed
«Drug Interactions: DISULFIRAM SHOULD BE USED WITH CAUTION IN THOSE PATIENTS RECEIVING PHENYTOIN AND ITS CONGENERS, SINCE THE CONCOMITANT ADMINISTRATION OF THESE TWO DRUGS CAN LEAD TO PHENYTOIN…»FDA, section 7 · Open on DailyMed
«Psychotic Reaction with Disulfiram: Use of oral metronidazole is associated with psychotic reactions in alcoholic patients who were using disulfiram concurrently. Do not administer metronidazole to…»FDA, section 4 · Open on DailyMed
«Potential Effects of Tinidazole on Other Drugs: Alcohols, Disulfiram: Alcoholic beverages and preparations containing ethanol or propylene glycol should be avoided during tinidazole therapy and for 3…»FDA, section 7 · Open on DailyMed
«disulfiram;»AEMPS, section 4.3 · Open on CIMA
«El disulfiram inhibe el metabolismo de la cafeína. Por lo tanto, se debe advertir a los pacientes alcohólicos que deben evitar la utilización de cafeína para evitar la aparición de excitación…»AEMPS, section 4.5 · Open on CIMA
«Disulfiram: La administración simultánea de disulfiram puede causar estados de confusión o incluso reacciones psicóticas. Debe evitarse la combinación de ambos agentes.»AEMPS, section 4.5 · Open on CIMA
«Inhibidores de CYP3A4/AEMPS, section 4.5 · Open on CIMA
«Disulfiram: Dosis crónicas o altas de Ácido ascórbico pueden interferir con la eficacia del disulfiram.»AEMPS, section 4.5 · Open on CIMA
«Becloforte contiene una pequeña cantidad de etanol. Existe un teórico potencial de interacción en pacientes particularmente sensibles que estén tomando disulfiram o metronidazol.»AEMPS, section 4.5 · Open on CIMA
«Inhibidores enzimáticos: El disulfiram inhibe el metabolismo del diazepam (disminución de la mediana del aclaramiento a 41%, aumento en semivida 37%), y probablemente el mayor metabolismo de los…»AEMPS, section 4.5 · Open on CIMA
«Drugs that Affect Phenytoin Concentrations: Other Acute alcohol intake, amiodarone, chloramphenicol, chlordiazepoxide, disulfiram, estrogen, fluvastatin, isoniazid, methylphenidate, phenothiazines…»FDA, section 7 · Open on DailyMed
«Drug Interactions:: Disulfiram Decreases theophylline clearance by inhibiting hydroxylation and demethylation. 50% increase»FDA, section 7 · Open on DailyMed
«Inhibidores enzimáticos: pueden potenciar el efecto anticoagulante, con riesgo de hemorragias, debido a una inhibición de su metabolismo hepático, cuando se administra conjuntamente con: alopurinol…»AEMPS, section 4.5 · Open on CIMA
«CYP450 Interactions: CYP1A2 acyclovir, allopurinol, caffeine, cimetidine, ciprofloxacin, disulfiram, enoxacin, famotidine, fluvoxamine, methoxsalen, mexiletine, norfloxacin, oral contraceptives…»FDA, section 7 · Open on DailyMed
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Disulfiram is evaluated for the following indications with varying evidence strength: Alcohol use disorder (evidence tier B). See the full indication matrix with dosing and citations above on this page.
Common side effects of Disulfiram (≥ 1 in 100): Drowsiness, Metallic taste, Skin rash, Decreased libido. See the Safety section for uncommon and serious reactions.
Limited data. Use only if benefit outweighs risk.
No milk excretion data. Breastfeeding not recommended.
Disulfiram is contraindicated in: Alcohol intake in any form (including syrups, mouthwashes, alcohol-containing medicines); Combination with metronidazole, tinidazole (fatal psychosis); Severe hepatic impairment; Psychosis, severe depression; Ischemic heart disease. Full list in the Safety section.
Direct links to regulator labels. Open in a new tab.
Betahistine, Choline alfoscerate, Cinnarizine, Flunarizine, Methadone, Nicotine