Disulfiram: profile and news

Disulfiram and Carbimide help patients achieve high rates of long ... Feb 3, 2006
...of abstinence, lapse, and relapse among chronic alcoholics while exploring the role that "alcohol deterrents" – specifically, Disulfiram and Calcium ... - Xagena.it,

Nalmefene May Reduce Relapse Feb 4, 2006
...is not new, but until 1994 there were no Food and Drug Administration-approved medications for the treatment of alcoholism other than disulfiram (Antabuse). ... - About - News & Issues,

Other information

Indication
For the treatment and management of chronic alcoholism

Pharmacology
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.

Drug Category
Alcohol Deterrents; Enzyme Inhibitors; ATC:N07BB01; ATC:P03AA04

Brand Names/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; NCI-C02959; NSC 190940; 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; TETD; TTD; TTS; Tenurid; Tenutex; 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; Tts X; Tuads, Ethyl; Usaf B-33

Dosage Forms
TABLET

Absorption
Disulfiram is absorbed slowly from the gastrointestinal tract (80 to 90% of oral dose).

Interactions
-->Interactions for Disulfiram:

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 ADJUSTMENT.

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.

Chemical IUPAC Name
1-(diethylthiocarbamoyldisulfanyl)-N,N-diethyl-methanethioamide

Chemical Formula
C10H20N2S4

Half Life
Not Available

Drug Type
Approved Drug

# Accession No
APRD00767

CAS Registry Number
97-77-8