Succimer

Succimer (2,3-dimercaptosuccinic acid, chemet) is an orally effective chelator that is chemically similar to dimercaprol but contains two carboxylic acids that modify both the distribution and chelating spectrum of the drug. After its absorption in humans, succimer is biotransformed to a mixed disulfide with cysteine.

Succimer produces a lead diuresis with a subsequent lowering of blood lead levels and attenuation of the untoward biochemical effects of lead, manifested by normalization of S-aminolevuli-nate (S-ALA) dehydrase activity. The succimer—lead chelate also is eliminated in bile and enters enterohepatic circulation.

A desirable feature of succimer is that it does not significantly mobilize essential metals such as zinc, copper, or iron. Animal studies suggest that succimer is effective as a chelator of arsenic, cadmium, mercury, and other metals. Succimer has been approved in the U.S. for treatment of children with blood lead levels >45 jlg/dL.

Toxicity with succimer is less than that with dimercaprol, perhaps because its relatively lower lipid solubility minimizes its uptake into cells. Nonetheless, transient elevations in hepatic transaminases are observed following treatment with succimer. The most commonly reported adverse effects of succimer treatment are nausea, vomiting, diarrhea, and loss of appetite. Rashes also have been reported that may necessitate discontinuation of therapy.

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