Penicillamine

Table of contents

  • Brand Names
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Unlabeled Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Drug Interactions
  • Genes that may be involved
  • Nutrition/Nutraceutical Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Europe

Austria: Artamin; Cyprus: Artamin; Czech Republic: Metalcaptase; Denmark: Atamir; France: Trolovol; Germany: Metalcaptase; Greece: Cuprimine, Cupripen, Helpocillan, Penicillamine, Reostatum; Ireland: Distamine; Italy: Pemine; Lihuania: Cuprenil; Luxembourg: Kelatin, Metalcaptase; Netherlands: Gerodyl; Poland: Artamin, Cuprenil; Portugal: Kelatine, Trolovol; Romania: Cuprenil; Slovakia: Metalcaptase; Spain: Cupripén; UK: Distamine.

North America

Canada: Cuprimine; USA: Cuprimine, Depen.

Latin America

Argentina: Cuprimine, Cupripen; Brazil: Cuprimine; Mexico: Adalken, Sufortan.

Asia

Japan: Metalcaptase.

Drug combinations

Chemistry

Penicillamine: C~5~H~11~NO~2~S. Mw: 149.21. D-3-Mercaptovaline. CAS-52-67-5 (1963).

Pharmacologic Category

Heavy Metal Antagonists. Disease-modifying Antirheumatic Drugs. Chelating Agent. (ATC-Code: M01CC01).

Mechanism of action

Chelates with lead, copper, mercury and other heavy metals to form stable, soluble complexes, excreted in urine. Depresses circulating IgM rheumatoid factor, depresses T-cell but not B-cell activity. Combines with cystine to form a more soluble compound, thus cystine calculi are prevented.

Therapeutic use

Treatment of Wilson’s disease, cystinuria. Adjunctive treatment of rheumatoid arthritis.

Pregnancy and lactiation implications

Use during pregnancy for treatment of rheumatoid arthritis contraindicated. Use contraindicated during lactation.

Unlabeled use

Chelation therapy for treatment of lead poisoning (third-line agent). Treatment of arsenic poisoning.

Contraindications

Hypersensitivity to penicillamine or any component of the formulation. Renal insufficiency (in rheumatoid arthritis). Previous penicillamine-related aplastic anemia or agranulocytosis. Pregnancy (in rheumatoid arthritis).

Warnings and precautions

Allergic reactions common. Penicillamine associated with fatalities due to Goodpasture’s syndrome, and to hematologic toxicities (agranulocytosis, aplastic anemia, and thrombocytopenia. Rare reports of intrahepatic cholestasis or toxic hepatitis. Proteinuria or hematuria may develop. Penicillamine associated with fatalities due to myasthenia gravis. Toxicity (fever, sore throat, chills, bruising, or bleeding) may be dose-related. Penicillamine considered to be a third-line agent for treatment of lead poisoning in children due to overall toxicity associated with its use. Use with caution in patients on other hematopoietic-depressant drugs (e.g. gold, immunosuppressants, antimalarials, phenylbutazone). Use with caution in the elderly.

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