Antabus - Disulfiram

Disulfiram is the generic name for Antabuse, a drug used in the treatment of chronic alcoholism. Disulfiram potentiates the toxic and carcinogenic effects of 1,2-dibromoethane in experimental animals. Presumably, this occurs by blocking conversion of the aldehyde metabolite as with acetaldehyde from ethanol. There is no evidence that similar effects occur in humans. Based on animal data, however, Ayerst Laboratories, producers of Antabuse (disulfiram), recommended the following in the package insert "Patients taking Antabuse tablets should not be exposed to ethylene dibromide or its vapors" (PDR 1991). 

As discussed in Section 2.6, chronic alcoholics receiving Antabuse (disulfiram) therapy are potentially more susceptible to toxic and neoplastic effects of 1,2-dibromoethane. It also follows that individuals with compromised liver or renal function or with asthma or other chronic respiratory diseases may have increased susceptibility to the toxic effects of 1,2-dibromoethane however, chemical-specific effects have not been identified. 

The final class of pharmacotherapy drugs alters the metabolism of certain target drugs, thereby causing a build up of toxic metabolic products that make a person feel extremely ill. The best known of these metabolism-modifiers is Antabuse (disulfiram), a drug primarily used to discourage people from drinking alcohol. 

Product Information, (1996), Antabuse (disulfiram), Wyeth-Ayerst Company Philadelphia, PA, Retrieved April 7, 2004 from http // www.aicohotmd.com/fam/medic/disutfiramfam.asp... 

We have already discussed a therapeutic application of inhibition in the example of ethanol being used as an antidote to ethylene glycol or methanol poisoning. There are many other such cases which could also be cited. Antabuse , disulfiram, prevents the metabolism of ethanol. As a result a person under treatment with Antabuse will become violently ill if s/he consumes ethanol. Barbiturates are rapidly metabolized especially if a person has been on a prescription for some time. Administering the antibacterial chloramphenicol will inhibit the breakdown of barbiturates and in so doing prolong their sedative action. 

The causes of human copper deficiency include (1) low intake - malnutrition, total parenteral nutrition (TPN) (2) high loss - cystic fibrosis, nephrotic syndromes and (3) genetic factors — Menkes disease. Copper deficiency may also be associated with chronic malabsorption, a situation which is made much worse in cases of gastric and bowel resection. Several special diets, including powdered milk, liquid protein and standard hospital diets are a means of inducing copper deficiency. The amount of copper in US food has decreased steadily since 1942, and may be related to the rising incidence of coronary artery disease. A copper deficiency may also occur as the result of the use of chelators for other purposes for example, diethyl dithiocarbamate is an in vivo metabolite of ANTABUSE (disulfiram). 

Antabuse (Disulfiram). Actavis UK Ltd UK Summary of product characteristics, Ai ust... 

Antabuse (Disulfiram). Odyssey Pharmaceuticals, Inc. US Prescribing infcnnation, December 2003. 

Kiorboe E. Phenytoin intoxication during treatment with Antabuse (Disulfiram). Epilepsia (1966) 7, 246-9. 

Oral medications taken by athletes may also be allergenic, particularly the non-steroidal agents (especially piroxicam) and antibiotics (ciprofloxacin, nalidixic acid, sulfonamides, tetracyclines), which are photosensitizers (Wainwright et al. 1993). Prior sensitization to thiuram rubber accelerators makes athletes susceptible to systemic eczematous dermatitis if Antabuse (disulfiram - a thiuram derivative) is given orally (Pirila 1957 Shelley 1961). 

An effective but painful part of the treatment for alcohol abuse is to administer disulfiram, marketed under the name Antabuse. Disulfiram blocks the action of ALDH, preventing the conversion of acetaldehyde to acetic acid. The resulting buildup of acetaldehyde causes the patient to feel very sick almost immediately, making the next cocktail/or less appealing. The action of disulfiram was discovered accidentally when Danish pharmaceutical researchers who were taking the drug as an experimental treatment for parasitic diseases became very iU every time they consumed alcohol. 

Sometimes alcoholics are treated with a drug called Antabuse (disulfiram), which prevents the oxidation of acetaldehyde to acetic acid. As a result, acetaldehyde accumulates in the blood, which causes nausea, profuse sweating, headache, dizziness, vomiting, and respiratory difficulties. Because of these unpleasant side effects, the patient is less likely to use alcohol. 

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