No

Gold Compound

Management of active stage of classic or definite rheumatoid arthritis in patients that do not respond to or tolerate other agents; psoriatic arthritis; adjunctive or alternative therapy for pemphigus

C

Renal disease, history of blood dyscrasias, congestive heart failure, exfoliative dermatitis, necrotizing enterocolitis, history of anaphylactic reactions

NSAIDs and corticosteroids may be discontinued after starting gold therapy; therapy should be discontinued if platelet count falls to <100,000/mm³; WBC <4000, granulocytes <1500/mm³, explain possibility of adverse effects and their manifestations; use with caution in patients with renal or hepatic impairment

>10%:

Dermatologic: Itching, rash

Gastrointestinal: Stomatitis

Ocular: Conjunctivitis

Renal: Proteinuria

1% to 10%:

Dermatologic: Urticaria, alopecia

Gastrointestinal: Glossitis

Hematologic: Eosinophilia, leukopenia, thrombocytopenia

Renal: Hematuria

<1%: Angioedema, ulcerative enterocolitis, GI hemorrhage, gingivitis, dysphagia, metallic taste, agranulocytosis, anemia, aplastic anemia, hepatotoxicity, peripheral neuropathy, interstitial pneumonitis

Symptoms of overdose include hematuria, proteinuria, fever, nausea, vomiting, diarrhea; signs of gold toxicity include decrease in hemoglobin, leukopenia, granulocytes and platelets, proteinuria, hematuria, pruritus, stomatitis or persistent diarrhea; advise patients to report any symptoms of toxicity; metallic taste may indicate stomatitis

Mild gold poisoning: Dimercaprol 2.5 mg/kg 4 times/day for 2 days or for more severe forms of gold intoxication, dimercaprol 3 mg/kg every 4 hours for 2 days, should be initiated; after 2 days the initial dose should be repeated twice daily on the third day and once daily thereafter for 10 days; other chelating agents have been used with some success

Increased toxicity: Penicillamine, antimalarials, hydroxychloroquine, cytotoxic agents, immunosuppressants

Store in tight, light-resistant containers at 15°C to 30°C

The exact mechanism of action of gold is unknown; gold is taken up by macrophages which results in inhibition of phagocytosis and lysosomal membrane stabilization; other actions observed are decreased serum rheumatoid factor and alterations in immunoglobulins. Additionally, complement activation is decreased, prostaglandin synthesis is inhibited, and lysosomal enzyme activity is decreased.

Onset of action: Delayed; may require as long as 3 months

Duration: Prolonged

Therapeutic response may not be seen for 3-4 months after start of therapy

Absorption: Oral: ~20% gold in dose is absorbed

Protein binding: 60%

Half-life: 21-31 days (half-life dependent upon single or multiple dosing)

Time to peak serum concentration: Peak blood gold concentrations seen within 2 hours

Elimination: 60% of absorbed gold is eliminated in urine; remainder eliminated in feces

Oral:

Adults: 6 mg/day in 1-2 divided doses; after 3 months may be increased to 9 mg/day in 3 divided doses; if still no response after 3 months at 9 mg/day, discontinue drug

Dosing adjustment in renal impairment:

Cl_cr 50-80 mL/minute: Reduce dose to 50%

Cl_cr <50 mL/minute: Avoid use

Monitor urine for protein; CBC and platelets; monitor for mouth ulcers and skin reactions; may monitor auranofin serum levels

Gold: Normal: 0-0.1 mg/mL (SI: 0-0.0064 mmol/L); Therapeutic: 1-3 mg/mL (SI: 0.06-0.18 mmol/L); Urine: <0.1 mg/24 hours

May enhance the response to a tuberculin skin test

None reported

May rarely produce agranulocytosis; use caution with clozapine and carbamazepine

No information available to require special precautions

No effects or complications reported

Take exactly as directed. Drug effects may not be seen for as long as 3 weeks to 3 months. You may experience metallic taste or mouth sores (frequent mouth care and sucking lozenges may help); gray-blue color or irritation and reddening of skin (avoid excessive exposure to sunlight; use sunscreen, sunglasses, and protective clothing); nausea, bloating, or loss of appetite (small frequent meals, chewing gum, or sucking on lozenges may help); or loss of hair (reversible). Report unusual bruising; blood in mouth, urine, stool, vomitus; persistent fatigue; persistent metallic taste; abdominal cramping, vomiting, diarrhea; sores in mouth; skin rash or itching; or irritated or painful eyes. Pregnancy/breast-feeding precautions: Inform prescriber if you are or intend to be pregnant. Do not breast-feed.

Discontinue therapy if platelet count falls <100,000/mm³

Capsule: 3 mg [29% gold]

Bell RA and Dale IM, "Gold Secretion in Maternal Milk," Arthritis Rheum, 1976, 19(6):1374.

Bunch TW, "Gold Overdose Treated With BAL," Arthritis Rheum, 1974, 19(1):123-5.

Cook NJ, Owen ET, and Donlon JB, "A Further Possible Cause of Diarrhoea Caused by Oral Gold," Br J Rheumatol, 1995, 34(4):395-6.

Davis CM, "D-Penicillamine for the Treatment of Gold Dermatitis," Am J Med, 1969, 46(3):472-6.

Fernandez-Herlihy L, "Requiem for Gold?" Ann Intern Med, 1991, 114(11):993-4.

Godfrey NF, Peter A, Simon TM, et al, "I.V. N-acetylcysteine Treatment of Hematologic Reactions to Chrysotherapy," J Rheumatol, 1982, 9(4):519-26.

Kozloff M, Votaw M, and Penner JA, "Gold-Induced Thrombocytopenia Responsive to Cyclophosphamide," South Med J, 1979, 72(11):1490-2.

Parez MC, Gomez C, Mataix R, et al, "Bone Marrow Splasia and Gold Salts. Report of Two Cases and Review of the Literature," Rev Clin Esp, 1995, 194:540-2.

Ulmeanu V, Toma M, Eugah B, et al, "Severe Thrombocytopenia Following Treatment With Gold Salts," Clin Exp Rheumatol, 12(Suppl 11):112.