gold sodium thiomalate (aurothiomalate, sodium, Myochrysine, sodium aurothiomalate)

Dosing and uses of Aurothiomalate, sodium, Myochrysine (gold sodium thiomalate)

• Adult
• Pediatric

 

Adult dosage forms and strengths

injectable solution

• 25mg/mL
• 50mg/mL

 

Rheumatoid Arthritis

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

 

Other Indications & Uses

JRA, psoriatic arthritis, Felty's syndrome

Usually for patients who have failed adequate trials of NSAIDs

 

Pediatric dosage forms and strengths

injectable solution

• 25mg/mL
• 50mg/mL

 

Rheumatoid Arthritis

10 mg IM the 1st wk, then 1 mg/kg IM qWk (NMT 50 mg/dose)

 

Aurothiomalate, sodium, Myochrysine (gold sodium thiomalate) adverse (side) 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)

 

Other Information

Gold toxicity, see Cautions

 

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/cu.mm, granulocytes <1,500/cu.mm, platelets <150,000/cu.mm, 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

Pts who have had 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 Tx 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

D/C if evidence of anaphylaxis

If nitritoid reaction (flushing, tachycardia, faintness) w/in minutes of inj, resume Tx only with caution in pts w/compromised CV status

 

Pregnancy and 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 of Aurothiomalate, sodium, Myochrysine (gold sodium thiomalate)

Half-Life: 6-25 d

Onset: 2-6 mth

Protein Bound: high

 

Excretion

Urine: 60-90%

Feces: 10-40%

 

Mechanism of action

Unknown

Gold compound, has anti-inflammatory, antiarthritic & immunomodulating effects; suppresses synovitis in active rheumatoid dz