Rheumatology Book

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D-PenicillamineAka: Penicillamine

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  1. Indications
    1. Rheumatoid Arthritis Third-line DMARD agent
    2. Rheumatoid Nodulosis
    3. Wilson's Disease
  2. Contraindications
    1. Penicillin Allergy
  3. Efficacy
    1. Response in 70% of Rheumatoid Arthritis
    2. Slow response requires 4-6 months
  4. 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%)
  5. 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
  6. 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
  7. Monitoring (2-3 times weekly on starting Penicillamine)
    1. Complete Blood Count
    2. Platelet Count
    3. Urinalysis
    4. Body Temperature
  8. Precautions
    1. Observe for Hypersensitivity Reaction
    2. Treat hypersensitivity with prednisone if occurs

Penicillamine (C0030817)

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 (CSP)beta dimethyl analog of cysteine; USP lists as a chelating agent.
Definition (NCI)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 (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)
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)
ConceptsAmino Acid, Peptide, or Protein (T116) , Pharmacologic Substance (T121)
MSHD010396
English3-Mercapto-D-valine, Alpha-amino-beta-methyl-beta-mercaptobutyric Acid, Beta-thiovaline, D 3 Mercaptovaline, D Penicillamine, D-3-Mercaptovaline, D-Mercaptovaline, D-Penicillamine, Depamine, Dimethylcysteine, Mercaptovaline, Penicillamine, PENICILLAMINE PREPARATION
SpanishD-3-mercaptovalina, D-penicilamina, penicilamina
Parent ConceptsAmino Acids, Sulfur (C0002527), Chelating Agents (C0007974), Angiogenesis Activator Inhibitor (C1515993), Antirheumatic Agents (C0003191), Penicillamine (C0030817), Heavy metal antagonist (C0305072), Drugs used in metabolic disorders (C0590169), Drug allergen by structure (C1532645), Immune Suppressants (Non-TNF Inhibitors) (C1579325)
SourcesAOD, CSP, LCH, MSH, MTHSPL, NCI, NDFRT, PDQ, RXNORM, SCTSPA, SNOMEDCT, USPMG, VANDF
Derived from the NIH UMLS (Unified Medical Language System)



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