Penicillamine

Administration

• Type: Antidote, anti-rheumatic
• Dosage Forms:
• Routes of Administration: Oral
• Common Trade Names: Cuprimine, Depen

Adult Dosing

• Mercury toxicity: 250mg PO QID x 1-2wks
• Arsenic toxicity: 100 mg/kg/day PO divided q6hr x 5 days
• Lead toxicity: 1-1.5 g daily PO or divided BID-TID x 1-6 months
• Cystinuria: 1-4g/day PO, goal urinary cysteine excretion 100 to 200 mg/day in patients with no stone history, <100mg/day if history of stones/pain
• Rheumatoid arthritis: 125-1500mg/day PO
• Wilson's disease: 750-1500mg/day, based on urinary copper excretion

Pediatric Dosing

• Lead toxicity (3rd line): 20-40 mg/kg/day PO divided q8hr
• Wilson's disease: 20 mg/kg/day PO divided q12hr
• Cystinuria: 30 mg/kg/day PO divided BID/QID, max 1g/day

Special Populations

• Pregnancy Rating: D
• Lactation risk: Infant risk cannot be ruled out
• Renal dosing: avoid in moderate to severe renal impairment
• Hepatic dosing: no adjustment

Contraindications

• Allergy to class/drug
• Pregnancy
• History of penicillamine-related aplastic anemia or agranulocytosis
• Rheumatoid arthritis with renal insufficiency

Adverse Reactions

Serious

• SJS/TEN, pemphigus
• Agranulocytosis, aplastic anemia, thrombocytopenia, TTP, ALL
• Liver failure, toxic hepatitis, cholestatic hepatitis, pancreatitis
• Renal failure, renal vasculitis, nephrotic syndrome
• Myasthenia gravis, optic neuritis
• Extrinsic allergic alveolitis, interstitial pneumonia, obliterative bronchiolitis
• Drug fever

Common

• Nausea/vomiting, decreased appetite, oral ulcers, diarrhea, epigastric pain
• Rash
• Proteinuria
• Myelosuppression

Pharmacology

• Half-life:
• Metabolism: Hepatic
• Excretion: Renal and fecal

Mechanism of Action

• As chelator: binds to heavy metals to form stable, soluble complexes that are readily excreted in the urine

See Also

• Antidotes
• Lead toxicity, Arsenic toxicity, Mercury toxicity

References

Authors

Claire