Brands, Medical Use, Clinical Data
- Alcohol Deterrents
- Enzyme Inhibitors
Brands / Synonyms
Abstensil; Abstinil; Abstinyl; Accel Tet; Accel Tet-R; Akrochem Tetd; Alcophobin; Alk-Aubs; Ancazide Et; Antabus; Antabuse; Antadix; Antaenyl; Antaethan; Antaethyl; Antaetil; Antalcol; Antetan; Antethyl; Antetil; Anteyl; Anthethyl; Anti-Ethyl; Antiaethan; Anticol; Antietanol; Antietil; Antikol; Antivitium; Aversan; Averzan; Bonibal; Contralin; Contrapot; Cronetal; Dicupral; Disetil; Disulfan; Disulfiram; Disulfram; Disulfuram; Disulphuram; Dupon 4472; Dupont Fungicide 4472; Ekagom Dtet; Ekagom Teds; Ekagom Tetds; Ekaland Tetd; Ephorran; Espenal; Esperal; Etabus; Ethyl Thiram; Ethyl Thiudad; Ethyl Thiurad; Ethyl Tuads; Ethyl Tuads Rodform; Ethyl Tuex; Ethyldithiourame; Ethyldithiurame; Etyl Tuex; Exhoran; Exhorran; Gababentin; Hoca; Hocakrotenalnci-C02959; Krotenal; Nocbin; Nocceler Tet; Nocceler Tet-G; Noxal; Perkacit Tetd; Perkait Tetd; Refusal; Ro-Sulfiram; Sanceler Tet; Sanceler Tet-G; Soxinol Tet; Stopaethyl; Stopethyl; Stopety; Stopetyl; Super Rodiatox; TATD; Tenurid; Tenutex; TETD; Tetidis; Tetradin; Tetradine; Tetraethylthioperoxydicarbonic Diamide; Tetraethylthiram Disulfide; Tetraethylthiram Disulphide; Tetraethylthiuram; Tetraethylthiuram Disulfide; Tetraethylthiuram Disulphide; Tetraethylthiuram Sulfide; Tetraethylthiuran Disulfide; Tetraetil; Teturam; Teturamin; Thiocid; Thiophos; Thiosan; Thioscabin; Thireranide; Thiuram Disulfide, Tetraethyl-; Thiuram E; Thiuranide; Tillram; Tiuram; TTD; TTS; Tts X; Tuads, Ethyl; Usaf B-33
For the treatment and management of chronic alcoholism
Disulfiram produces a sensitivity to alcohol which results in a highly unpleasant reaction when the patient under treatment ingests even small amounts of alcohol. Disulfiram blocks the oxidation of alcohol at the acetaldehyde stage during alcohol metabolism following disulfiram intake, the concentration of acetaldehyde occurring in the blood may be 5 to 10 times higher than that found during metabolism of the same amount of alcohol alone. Accumulation of acetaldehyde in the blood produces a complex of highly unpleasant symptoms referred to hereinafter as the disulfiram-alcohol reaction. This reaction, which is proportional to the dosage of both disulfiram and alcohol, will persist as long as alcohol is being metabolized. Disulfiram does not appear to influence the rate of alcohol elimination from the body. Prolonged administration of disulfiram does not produce tolerance; the longer a patient remains on therapy, the more exquisitely sensitive he becomes to alcohol.
Mechanism of Action
Disulfiram blocks the oxidation of alcohol at the acetaldehyde stage during alcohol metabolism following disulfiram intake causing an accumulation of acetaldehyde in the blood producing highly unpleasant symptoms. Disulfiram blocks the oxidation of alcohol through its irreversible inactivation of aldehyde dehydrogenase, which acts in the second step of ethanol utilization. In addition, disulfiram competitively binds and inhibits the peripheral benzodiazepine receptor, which may indicate some value in the treatment of the symptoms of alcohol withdrawal, however this activity has not been extensively studied.
Disulfiram is absorbed slowly from the gastrointestinal tract (80 to 90% of oral dose).
LD50=8.6g/kg (orally in rats). Symptoms of overdose include irritation, slight drowsiness, unpleasant taste, mild GI disturbances, and orthostatic hypotension.
Biotrnasformation / Drug Metabolism
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 given disulfiram.
Disulfiram is contraindicated in the presence of severe myocardial disease or coronary occlusion, psychoses, and
hypersensitivity to disulfiram or to other thiuram derivatives used in pesticides and rubber vulcanization.
Disulfiram appears to decrease the rate at which certain drugs are metabolized and therefore may increase the blood
levels and the possibility of clinical toxicity of drugs given concomitantly.
DISULFIRAM SHOULD BE USED WITH CAUTION IN THOSE PATIENTS REVEIVING PHENYTOIN AND ITS CONGENERS. SINCE THE
CONCOMITANT ADMINISTRATION OF THESE TWO DRUGS CAN LEAD TO PHENYTOIN INTOXICATION, PRIOR TO ADMINISTERING DISULFIRAM
TO A PATIENT ON PHENYTOIN THERAPY, A BASELINE PHENYTOIN SERUM LEVEL SHOULD BE OBTAINED. SUBSEQUENT TO INITIATION OF
DISULFIRAM THERAPY. SERUM LEVELS OF PHENYTOIN SHOULD BE DETERMINED ON DIFFERENT DAYS FOR EVIDENCE OF AN INCREASE OR
FOR A CONTINUING RISE IN LEVELS. INCREASED PHENYTOIN LEVELS SHOULD BE TREATED WITH APPROPRIATE DOSAGE
It may be necessary to adjust the dosage of oral anticoagulants upon beginning or stopping disulfiram. since
disulfiram may prolong prothrombin time..
Patients taking isoniazid when disulfiram is given should be observed for the appearance of unsteady gait or
marked changes in mental status; the disulfiram should be discontinued if such signs appear.
In rats, simultaneous ingestion of disulfiram and nitrite in the diet for 78 weeks has been reported to cause
tumors, and it has been suggested that disulfiram may react with nitrites in the rat stomach to form a nitrosamine,
which is tumorigenic. Disulfiram alone in the ratís diet did not lead to such tumors. The relevance of this
finding to humans is not known at this time.