Dosing & Uses
Dosage Forms & Strengths
injectable solution
- 25mg/mL
- 50mg/mL
Rheumatoid Arthritis
Indicated for rheumatoid arthritis in patients who have failed adequate trials of NSAIDs
10 mg IM the 1st wk, 25 mg IM the 2nd wk, then 25-50 mg IM qWk x 20 wk or until toxicity occurs
Taper to 50 mg IM q2-4wk
CrCl <50 mL/min, not recommended
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Adverse Effects
>10%
Pruritis & rash (30%)
Stomatitis (20%)
Proteinuria (10-15%)
1-10%
Leukopenia
Thrombocytopenia
Frequency Not Defined
Agranulocytosis
Aplastic anemia
Exfoliative dermatitis
Enterocolitis
Liver failure
Anaphylactoid rxn
Nephropathy
Corneal gold deposits (rare)
Warnings
Black Box Warnings
Prescribing physicians should understand severe and fatal toxicities of chrysotherapy
Thorough patient discussion explaining adverse reactions is essential; encourage patients to report any adverse reactions
Monitor for signs of gold toxicity (ie, decreased hemoglobin, leukopenia <4,000/mm³, granulocytes <1,500/mm³, platelets <150,000/mm³, proteinuria, hematuria, pruritus, rash, stomatitis, persistent diarrhea) and establish baseline measurements before prescribing
Should be reserved for use in certain patients with active rheumatoid arthritis
Contraindications
Hypersensitivity to gold
History of previous gold-induced disorders (anaphylaxis, necrotizing enterocolitis, pulmonary fibrosis, dermatitis, bone marrow suppression, or other hematologic disorder)
Cautions
Not to be used as sole agent in treatment of RA
No evidence gold compounds induce remission of RA
Gold toxicity:
- Hemoglobin (decr)
- Leukopenia (WBC <4000/cu.mm) [4 x10^9/L]
- Granulocytes (<1500/cu.mm) [1.5 x10^9/L]
- Platelets (<150 x 10^3/cu.mm) [150 x10^9/L]
- Proteinuria, hematuria, pruritus, rash, stomatitis, chronic diarrhea
Discontinue if evidence of anaphylaxis
If nitritoid reaction (flushing, tachycardia, faintness) within minutes of injection, resume treatment only with caution in patients with compromised CV status
Pregnancy & Lactation
Pregnancy Category: C
Lactation: enters breast milk; not recommended
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available.Pharmacology
Mechanism of Action
Unknown
Gold compound, has anti-inflammatory, antiarthritic and immunomodulating effects; suppresses synovitis in active rheumatoid disease
Pharmacokinetics
Onset of effect: 2-6 months
Protein bound: High
Half-life: 6-25 days
Excretion: 60-90% urine; 10-40% feces
