No

Antidote

Treatment of lead poisoning in children with blood levels >45 mg/dL. It is not indicated for prophylaxis of lead poisoning in a lead-containing environment. Following oral administration, succimer is generally well tolerated and produces a linear dose-dependent reduction in serum lead concentrations. This agent appears to offer advantages over existing lead chelating agents.

C

Known hypersensitivity to succimer

Caution in patients with renal or hepatic impairment; adequate hydration should be maintained during therapy

>10%:

Central nervous system: Fever

Gastrointestinal: Nausea, vomiting, diarrhea, appetite loss, hemorrhoidal symptoms, metallic taste

Neuromuscular & skeletal: Back pain

1% to 10%:

Central nervous system: Drowsiness, dizziness

Dermatologic: Rash

Endocrine & metabolic: Serum cholesterol

Gastrointestinal: Sore throat

Hepatic: Elevated AST/ALT, alkaline phosphatase

Respiratory: Nasal congestion, cough

Miscellaneous: Flu-like symptoms

<1%: Arrhythmias

Symptoms of overdose include anorexia, vomiting, nephritis, hepatotoxicity, renal tubular necrosis, GI bleeding

Not recommended for concomitant administration with edetate calcium disodium or penicillamine

Succimer is an analog of dimercaprol. It forms water soluble chelates with heavy metals which are subsequently excreted renally. Initial data have shown encouraging results in the treatment of mercury and arsenic poisoning. Succimer binds heavy metals; however, the chemical form of these chelates is not known.

Absorption: Rapid but incomplete

Metabolism: Rapidly and extensively to mixed succimer cysteine disulfides

Half-life, elimination: 2 days

Time to peak serum concentration: ~1-2 hours

Elimination: ~25% in urine with peak urinary excretion occurring between 2-4 hours after dosing; of the total amount of succimer eliminated in urine, 90% is eliminated as mixed succimer-cysteine disulfide conjugates; 10% is excreted unchanged; fecal excretion of succimer probably represents unabsorbed drug

Children and Adults: Oral: 10 mg/kg/dose every 8 hours for an additional 5 days followed by 10 mg/kg/dose every 12 hours for 14 days

Concomitant iron therapy has been reported in a small number of children without the formation of a toxic complex with iron (as seen with dimercaprol); courses of therapy may be repeated if indicated by weekly monitoring of blood lead levels; lead levels should be stabilized <15 mg/dL; 2 weeks between courses is recommended unless more timely treatment is indicated by lead levels

Blood lead levels, serum aminotransferases

False-positive ketones (U) using nitroprusside methods, falsely elevated serum CPK; falsely decreased uric acid measurement

May cause drowsiness or dizziness

None noted

Maintain adequate fluid intake; notify physician if rash occurs; capsules may be opened and contents sprinkled on food or put on a spoon

Adequately hydrate patients; rapid rebound of serum lead levels can occur; monitor closely

Capsule: 100 mg

Dart RC, Hurlburt KM, Maiorino RM, et al, "Pharmacokinetics of Meso-2,3-Dimercaptosuccinic Acid in Patients With Lead Poisoning and in Healthy Adults," J Pediatr, 1994, 125(2):309-16.

Fournier L, Thomas G, Garnier R, et al, "2,3-Dimercaptosuccinic Acid Treatment of Heavy Metal Poisoning in Humans," Med Toxicol Adverse Drug Exp, 1988, 3(6):499-504.

Glotzer DE, "The Current Role of 2,3 Dimercaptosuccinic Acid (DMSA) in Management of Childhood Lead Poisoning," Drug Saf, 1993, 9(2):85-92.

Graziano JH, Lolacono NJ, Moulton T, et al, "Controlled Study of Meso-2,3-Dimercaptosuccinic Acid for the Management of Childhood Lead Intoxication," J Pediatr, 1992, 120(1):133-9.

Mann KV and Travers JD, "Succimer, An Oral Lead Chelator," Clin Pharm, 1991, 10(12):914-22.

"Treatment Guidelines for Lead Exposure in Children. American Academy of Pediatrics Committee on Drugs," Pediatrics, 1995, 96(1 Pt 1):155-60.