PENICILLAMINE

Disease modifying antirheumatic medicine and chelator for copper and lead poisoning

Dosage Forms

Tablet

250 mg

Uses

  • Treatment of severe rheumatoid arthritis
  • Copper poisoning and lead poisoning
  • Wilson’s disease
  • Cystinuria

Dose and Duration

Rheumatoid arthritis

Adult: by mouth, initially 125–250 mg once daily before food for 1 month, then increased by the same amounts at intervals of at least 4 weeks to a usual maintenance dose of 500–750 mg daily in divided doses (max 1500 mg daily).
If remission occurs after 6 months, attempt dose reduction by 125–250 mg every 12 weeks

Child 8–12 years: initially 2.5–5 mg/kg daily, gradually increased at least every 4 weeks to a usual maintenance dose of 15–20 mg/kg daily over 3–6 months

Elderly: initially 125 mg daily before food for 1 month, then increased with the same amounts at least every 4 weeks (max 1 g daily)

Copper and lead poisoning

Adult: 1–2 g daily in divided doses before food, until urinary lead is stabilized at less than 500 micrograms/day

Child: 20 mg/kg/day in divided doses

Wilson’s disease

Adult and child over 12 years: 1.5–2 g daily in divided doses before food (max 2 g daily for 1 year), thereafter 0.75–1 g daily

Child 1 month–12 years: 2.5 mg/kg every 12 hours before food, increased at 1–2 week intervals to 10 mg/kg every 12 hours

Elderly: 20 mg/kg daily in divided doses adjusted according to response

Cystinuria

Adult and child over 12 years: therapeutic, 1000–3000 mg daily in divided doses before food, adjusted to maintain urinary cystine below 200 mg/l

Prophylactic (maintain urinary cystine below 300 mg/l) → 500 mg–1000 mg at bedtime

Child 1 month–12 years: prophylaxis, 20–30 mg/kg/day in 2–3 divided doses adjusted to keep urinary cystine below 200 mg/l

Elderly: lowest dose to keep urinary cystine < 200 mg/l

Contraindications

  • Lupus erythematosus
  • Hypersensitivity to penicillamine

Side Effects

  • Nausea, taste loss
  • Anorexia, fever
  • Thrombocytopenia
  • Proteinuria
  • Rash
  • Stevens-Johnson syndrome

Interactions

  • Clozapine (increased risk of agranulocytosis)

Patient Instructions

  • Take your medicine before food or at bedtime
  • Report to your doctor immediately if signs or symptoms of bone marrow depression such as unexplained bruising or bleeding, purpura, infection or sore throat occur
  • When used for cystinuria, take at least 3 litres of water per day

Pregnancy

  • Can be used

Breast-feeding

  • Can be used

⚠️ Caution

  • Monitor blood and urine throughout treatment
  • Avoid concomitant use of nephrotoxic drugs, gold, chloroquine or immunosuppressive treatment
  • Avoid administration of oral iron within 2 hours of a dose
  • Use with caution in penicillin-sensitive patients as they may also react to penicillamine
  • Reduce dose in mild renal impairment and avoid use in moderate to severe renal impairment