Drug intelligence / Profile preview

edetate calcium disodium + dimercaprol

Development stage
Unknown
Lead developer
Rising Pharmaceuticals
Modality
Small Molecules
Administration
Intramuscular, Intravenous
01

Overview

This combination therapy is specifically indicated for severe lead poisoning, particularly when blood lead levels exceed 70 mcg/dL or when symptoms of lead encephalopathy are present[6]. The rationale for using these agents together is that edetate calcium disodium alone may increase lead redistribution into the brain and potentially worsen encephalopathy, while dimercaprol helps prevent this redistribution[5][6]. Dimercaprol works by forming stable chelates with heavy metals like lead, mercury, arsenic, and gold through its sulfhydryl groups, allowing these metals to be excreted in urine[8]. Edetate calcium disodium forms stable chelates with divalent and trivalent metals (including lead) that can displace calcium in the molecule, with the resulting chelate being excreted in urine[3]. When used in combination, these agents decrease blood lead levels more rapidly than either agent alone, though the final post-chelation blood lead levels may be similar to monotherapy[5]. The combination is particularly important in severe cases to prevent the risk of encephalopathy that can occur with edetate calcium disodium monotherapy. For acute lead encephalopathy, the typical regimen involves: - Dimercaprol: 4 mg/kg IM every 4 hours, with the first dose given alone - Edetate calcium disodium: Added starting with the second dose of dimercaprol, at a total daily dose of 1,000 mg/m² given every 8-12 hours IM or once daily IV over an 8-12 hour interval[5] For less severe toxicity, the dimercaprol dose can be decreased to 3 mg/kg after the first dose. Treatment typically continues for 2-7 days depending on clinical response, including decreased blood lead levels, reversal of hematologic effects, and increased urinary lead excretion[5][7]. The combination therapy has been associated with increased side effects compared to monotherapy, particularly elevated liver enzymes and vomiting[5]. Dimercaprol should not be used in patients with hepatic insufficiency (except in cases of arsenical jaundice) and should be used with caution in patients with renal impairment[8]. Edetate calcium disodium is contraindicated during periods of anuria and in patients with active renal disease or hepatitis[6]. Both medications require careful monitoring of urine output throughout therapy, and treatment should be stopped if anuria or severe oliguria develops[6][8].

Other names
calcium disodium edetate + dimercaprolCaNa₂EDTA + BALedetate calcium disodium + British anti-Lewisite
02

Targets

Arsenic ion

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