II. Indications

  1. Rheumatoid Arthritis Third-line DMARD agent
  2. Rheumatoid Nodulosis
  3. Wilson's Disease

III. Contraindications

IV. Efficacy

  1. Response in 70% of Rheumatoid Arthritis
  2. Slow response requires 4-6 months

V. Adverse Effects

  1. Adverse effects are common and require stopping drug
  2. Nausea
  3. Gastrointestinal upset
  4. Rash
  5. Stomatitis
  6. Dysgeusia
  7. Cytopenia (5%)
  8. Proteinuria in membranous nephritis (5-20%)

VI. Dosing: Rheumatoid Arthritis

  1. Start low and increase very slowly
  2. Month 1: 250 mg per day
  3. Month 2: 500 mg per day
  4. Month 3: 750 mg per day
  5. Month 4: 1000 mg per day
  6. Maintenance Dose: 750 to 1000 mg per day
  7. Lowest Effective Dose: 500 mg per day

VII. Dosing: Wilson's Disease

  1. Penicillamine 1 g PO before meals and at bedtime
  2. Keep Serum free copper <2 umol/L (<10 ug/dl)
  3. Continue life-long in Wilson's Disease

VIII. Monitoring (2-3 times weekly on starting Penicillamine)

IX. Precautions

  1. Observe for Hypersensitivity Reaction
  2. Treat hypersensitivity with Prednisone if occurs

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Ontology: Penicillamine (C0030817)

Definition (NCI_NCI-GLOSS) A drug that removes copper from the body and is used to treat diseases in which there is an excess of this metal. It is also being studied as a possible angiogenesis inhibitor in brain tumors.
Definition (NCI) A beta dimethyl analog of the amino acid cysteine. As a degradation product of penicillin antibiotics, penicillamine chelates with heavy metals and increases their urinary excretion. Possessing antineoplastic properties, penicillamine induces apoptosis by a p53-mediated mechanism and inhibits angiogenesis by chelating with copper, a cofactor for angiogenesis. (NCI04)
Definition (CSP) beta dimethyl analog of cysteine; USP lists as a chelating agent.
Definition (MSH) 3-Mercapto-D-valine. The most characteristic degradation product of the penicillin antibiotics. It is used as an antirheumatic and as a chelating agent in Wilson's disease.
Definition (PDQ) A beta dimethyl analog of the amino acid cysteine. As a degradation product of penicillin antibiotics, penicillamine chelates with heavy metals and increases their urinary excretion. Possessing antineoplastic properties, penicillamine induces apoptosis by a p53-mediated mechanism and inhibits angiogenesis by chelating with copper, a cofactor for angiogenesis. Check for "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=42546&idtype=1" active clinical trials or "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=42546&idtype=1&closed=1" closed clinical trials using this agent. ("http://nciterms.nci.nih.gov:80/NCIBrowser/ConceptReport.jsp?dictionary=NCI_Thesaurus&code=C729" NCI Thesaurus)
Concepts Pharmacologic Substance (T121) , Amino Acid, Peptide, or Protein (T116)
MSH D010396
SnomedCT 329465002, 330024005, 387235007, 4219002
English beta,beta Dimethylcysteine, beta,beta-Dimethylcysteine, D 3 Mercaptovaline, D Penicillamine, D-3-Mercaptovaline, D-Penicillamine, Dimethylcysteine, Mercaptovaline, Penicillamine, D-Valine, 3-mercapto-, Penicillamine [metabolic], Penicillamine [musculo-skel], Beta-thiovaline, 3-Mercapto-D-valine, Alpha-amino-beta-methyl-beta-mercaptobutyric Acid, Beta,Beta-dimethylcysteine, D-Mercaptovaline, Depamine, Penicillamine [musculoskeletal use], D penicillamine, D-penicillamine (medication), PENICILLAMINE, Penicillamine [Chemical/Ingredient], d penicillamine, d-penicillamine, penicillAMINE, penicillamine, Penicillamine [metabolic] (product), Penicillamine [musculoskeletal use] (product), .beta.,.beta.-Dimethylcysteine, D-3-mercaptovaline, D-penicillamine, beta, beta-Dimethylcysteine, Penicillamine (product), Penicillamine (substance), Penicillamine [metabolic] (substance), Penicillamine [musculoskeletal use] (substance)
Swedish Penicillamin
Czech penicilamin
Finnish Penisillamiini
Russian MERKAPTOVALIN, PENITSILLAMIN, DIMETILTSISTEIN, ДИМЕТИЛЦИСТЕИН, МЕРКАПТОВАЛИН, ПЕНИЦИЛЛАМИН
Japanese メルカプトバリン, L-ペニシラミン, ペニシラミン, D-ペニシラミン, β,β-ジメチルシステイン, ベータ,ベータ-ジメチルシステイン, ジメチルシステイン
French D-Pénicillamine, bêta-Thiovaline, bêta-Mercaptovaline, Diméthylcystéine, Pénicillamine
Polish Penicylamina, Artamin, Merkaptowalina
Spanish penicilamina (metabólico), penicilamina (uso musculoesquelético) (producto), penicilamina (metabólico) (producto), penicilamina (uso musculoesquelético), D-3-mercaptovalina, D-penicilamina, beta,beta-dimetilcisteína, penicilamina (producto), penicilamina (sustancia), penicilamina, Mercaptovalina, Penicilamina, Dimetilcisteína, betadimetilcisteína beta
German Beta,Beta-Dimethylcystein, Dimethylcystein, Mercaptovalin, Penicillamin
Italian Penicillamina
Portuguese beta,beta-Dimetilcisteína, Dimetilcisteína, Mercaptovalina, Penicilamina