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Classification: Antiarthritic,oral gold compound
Action/Kinetics: Auranofin is agold-containing (29%) compound for PO administration. It has fewer side effects thaninjectable gold products. Although the mechanism is not known, auranofin will improvesymptoms of rheumatoid arthritis; it is most effective in the early stages of activesynovitis and may act by inhibiting sulfhydryl systems. Other possible mechanisms includeinhibition of phagocytic activity of macrophages and polymorphonuclear leukocytes,alteration of biosynthesis of collagen, and alteration of the immune response. Gold willnot reverse damage to joints caused by disease. Approximately 25% of an oral dose isabsorbed. Plasma t1/2 of auranofin gold: 26 days. Onset: 3-4 months(up to 6 months in certain clients). Approximately 3 months are required for steady-stateblood levels to be achieved. The drug is metabolized and excreted in both the urine andfeces.
Adults and children withrheumatoid arthritis that have not responded to other drugs. Up to 6 months may berequired for beneficial effects to occur. Auranofin should be part of a total treatmentregimen for rheumatoid arthritis, including nondrug treatments.
Capsules Rheumatoid arthritis. Adults, initial: Either 6 mg/day or 3 mg b.i.d. If response is unsatisfactory after6 months, increase to 3 mg t.i.d. If response is still inadequate after 3 additionalmonths, discontinue the drug. Dosages greater than 9 mg/day are not recommended. Children, initial: 0.1 mg/kg/day; maintenance: 0.15 mg/kg/day, not to exceed0.2 mg/kg/day. Transfer from injectable gold. Discontinue injectable gold and begin auranofin at a dose of 6 mg/day.
Pregnancy Category: C
Contraindications: History ofgold-induced disorders including necrotizing enterocolitis, pulmonary fibrosis,exfoliative dermatitis, bone marrow aplasia, or other hematologic severe disorders. Useduring lactation.
Special Concerns: Use withextreme caution in renal or hepatic disease, skin rashes, marked hypertension, compromisedcerebral or CV circulation, or history of bone marrow depression (e.g., agranulocytopenia,anemia). Gold dermatitis may be aggravated by exposure to sunlight. Although used inchildren, a recommended dosage has not been established. Tolerance to gold is oftendecreased in geriatric clients.
GI: N&V, diarrhea (common), abdominal pain, metallic taste, stomatitis, glossitis,gingivitis, anorexia, constipation, flatulence, dyspepsia, dysgeusia, melena. Rarely,dysphagia, GI bleeding, ulcerative enterocolitis. Dermatologic: Skin rashes, pruritus, alopecia, urticaria, angioedema, actinic rash. Hematologic: Leukopenia, anemia, thrombocytopenia (with or without purpura), neutropenia,agranulocytosis, eosinophilia, pancytopenia, hypoplastic anemia, aplasticanemia pure red cell aplasia. Renal: Proteinuria, hematuria. Hepatic: Jaundice (with or without cholestasis, hepatitis with jaundice, toxichepatitis intrahepatic cholestasis. Other: Conjunctivitis,cholestatic jaundice, fever, interstitial pneumonia and fibrosis, peripheral neuropathy.
Symptoms: Rapid appearance of hematuria, proteinuria, thrombocytopenia, granulocytopenia. Also,N&V, diarrhea, fever, urticaria, papulovesicular lesions, urticaria, exfoliativedermatitis, pruritus. Treatment: Discontinue promptly and give dimercaprol.Supportive therapy should be provided for renal and hematologic symptoms. Treat moderatelysevere skin and mucous membrane symptoms with topical corticosteroids, oralantihistamines, and anesthetic lotions. Treat severe stomatitis or dermatitis withprednisone, 10-40 mg daily. Treat serious renal, hematologic, pulmonary, and enterocoliticcomplications with prednisone, 40-100 mg daily in divided doses. The duration of treatmentvaries, depending on the severity of symptoms and the response to steroids. In acuteoverdosage, induce emesis or perform gastric lavage immediately.