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succimer (Chemet)

 

Classes: Chelators

Dosing and uses of Chemet (succimer)

 

Adult dosage forms and strengths

capsule

  • 100mg

 

Lead Poisoning (Off-label)

10 mg/kg PO q8hr for 5 days; follow by 10 mg/kg/dose q12hr for 14 days; not to exceed 500 mg/dose

Chemical name: meso 2,3-dimercaptosuccinic acid (DMSA)

 

Arsenic Poisoning (Off-label)

300 mg PO q6hr for 3 days

End point: urinary arsenic <50 mcg/L

 

Cystine Kidney Stone (Orphan)

Prevention of cystine kidney stone formation in patients with homozygous cystinuria prone to stone development

Orphan indication sponsor

  • Sanofi Winthrop, Inc; 90 Park Ave; New York, NY 10016-1389

 

Mercury Intoxication (Orphan)

Treatment of mercury intoxication

Orphan indication sponsor

  • Sanofi Winthrop, Inc; 90 Park Ave; New York, NY 10016-1389

 

Other Information

Key point: Patient should maintain PO fluids

Forms water-soluble chelate with heavy metal (lead, also mercury and arsenic)

Recheck blood lead levels q14Days

 

Other Indications & Uses

Lead poisoning (child: >45-69 mcg/dL [2.17-3.33 micromoles/L])

Off-label: arsenic poisoning (in combination with BAL)

 

Pediatric dosage forms and strengths

capsule

  • 100mg

 

Lead Poisoning

<1 year: Safety and efficacy not established

1 year or older: Blood lead levels above 45 mcg/dL, 10 mg/kg or 350 mg/sq.meter q8hr for 5 days, then 10 mg/kg or 350 mg/sq.meter q12hr for 14 days

 

Other Information

Key point: patient should maintain PO fluids

Recheck blood lead levels q14Days

Chemet: no data for combination with Na2CaEDTA

 

Geriatric dosage forms and strengths

 

Lead Poisoning (Off-label)

10 mg/kg PO q8hr for 5 days; follow by 10 mg/kg/dose q12hr for 14 days; not to exceed 500 mg/dose

 

Arsenic Poisoning (Off-label)

300 mg PO q6hr for 3 days

End point: urinary arsenic <50 mcg/L

 

Chemet (succimer) adverse (side) effects

Frequency not defined

Nausea/vomiting

Diarrhea

Abd gas/pain

Transient LFTs incr (AST, AP)

Rash

Pruritus

Sore throat

Rhinorrhea

Drowsiness

Paresthesia

Thrombocytosis

Eosinophilia

Possible decr renal function

Fever

 

Pregnancy and lactation

Pregnancy category: C

 

Pregnancy categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

 

Pharmacology of Chemet (succimer)

Mechanism of action

2 sulfhydryl groups capable of complexing to lead making it water soluble

 

Pharmacokinetics

Rapid but incomplete

Protein binding: Highly bound to albumin

Excretion: Feces (39%), urine (9%)

Time to peak: 1-2 hr (serum)

Half-life elimination: 2 days

Metabolism: Metabolized extensively to succimer cysteine sulfides