chapter  38
4 Pages

Disulfiram

WithJames L. Schardein, Orest T. Macina

Disulfiram is a thiuram derivative that is used therapeutically as an antialcoholic agent in the management of chronic alcoholism. Mechanistically, it interferes with aldehyde dehydrogenase and when taken concomitantly with alcohol, the serum acetaldehyde levels are increased, causing uncomfortable symptoms and is the basis for postwithdrawal long-term care of alcoholism. For medicinal purposes, disulfiram is available by prescription under the trade name Antabuse®. It has a pregnancy category risk factor of C. Animal studies by the oral route have been conducted in mice, rats, hamsters, and guinea pigs. Experience in humans with disulfiram has indicated potential teratogenic effects. In summary, while the evidence is not compelling that disulfiram is a potent developmental toxicant in humans, the published case reports of malformations cannot be overlooked. Disulfiram is an average-sized highly hydrophobic compound. It can act as a hydrogen bond acceptor.