Four chelating agents that have been used most commonly for the treatm
ent of humans intoxicated with lead, mercury, arsenic or other heavy m
etals and metalloids are reviewed as to their advantages, disadvantage
s, metabolism and specificity. Of these, CaNa(2)EDTA and dimercaprol (
British anti-lewisite, BAL) are becoming outmoded and can be expected
to be replaced by meso-2,3-dimercaptosuccinic acid (DMSA, succimer) fo
r treatment of lead intoxication and by the sodium salt of 2,3-dimerca
pto-1-propanesulfonic acid (DMPS, Dimaval(R)) for treating lead, mercu
ry or arsenic intoxication, Meso-2,3-DMSA and DMPS are biotransformed
differently in humans. More than 90% of the DMSA excreted in the urine
is found in the form of a mixed disulfide in which each of the sulfur
atoms of DMSA is in disulfide linkage with an L-cysteine molecule. Af
ter DMPS administration, however, acyclic and cyclic disulfides of DMP
S are found in the urine, The Dimaval-mercury challenge test holds gre
at promise as a diagnostic test for mercury exposure, especially for l
ow level mercurialism. Urinary mercury after Dimaval challenge may be
a better biomarker of low level mercurialism than unchallenged urinary
mercury excretion.