Adult Dosing

Rheumatoid arthritis (Non-FDA approved)

• Initial regimen
• First week: 10 mg IM; second week: 25 mg IM
• Then 25-50 mg IM qwk until there is major clinical improvement, toxicity, or 1000 mg cumulative dose is reached. Max: 100 mg/dose
• If improvement occurs before administering a cumulative dose of 1000 mg, decrease the dose or increase the interval between injections
• If there is inadequate response during initial therapy, may continue 25-50 mg IM qwk x 10 wks or increase the dose by increments of 10 mg q1-4 wks
• If cumulative dose reaches 1000 mg without improvement, discontinue therapy considering the patient to be unresponsive to gold therapy

• Maintenance therapy
• 25-50 mg IM every other week x 2-20 wks until the clinical course is stable
• On the basis of response, give dose q3-4 wks or q1-3 wks
• Max: 100 mg/dose
• If the arthritis exacerbates during maintenance therapy, resume weekly injections temporarily until disease activity is suppressed

Note:

• Intragluteal injection is preferred

Pediatric Dosing

Juvenile idiopathic arthritis (Non-FDA approved)

• Initial regimen
• First week: 10 mg IM
• Then 1 mg/kg IM qwk until there is major clinical improvement, toxicity, or 1000 mg cumulative dose is reached. Max: 50 mg/dose

• Maintenance therapy
• 1 mg/kg IM every other week x 2-20 wks until clinical course is stable
• On the basis of response, give dose q3-4 wks or q1-3 wks

• Intragluteal injection is preferred
• The guidelines given above for administration to adults also apply to pediatric patients

[Outline]

• Adult Dosing
• Pediatric Dosing

• Treatment of selected cases of active rheumatoid arthritis, both adult and juvenile type (Non-FDA approved)

Note:

• Use only as one part of a complete program of therapy; it is not a complete treatment when used alone

• Hypersensitivity to any of the ingredients of the product
• Severe toxicity resulting from previous exposure to gold
• History of severe heavy metal toxicity
• Severe debilitation
• Systemic lupus erythematosus

• Physicians should be thoroughly familiar with the toxicity and benefits of gold sodium thiomalate and must explain the possibility of toxic reactions to patients prior to therapy. Advise patients to promptly report any symptoms suggesting toxicity
• Prior to each injection, physicians must review results of laboratory work and evaluate patients for adverse reactions since some of them can be severe or even fatal

Renal Dose Adjustment

• Renal Dose Adjustment: Dose adjustments not defined, caution advised

Hepatic Dose Adjustment

• Hepatic impairment: Dose adjustments not defined, caution advised

• Determine the patient's hemoglobin, erythrocyte, white blood cell, differential and platelet counts and perform urinalysis prior to therapy initiation. Analyze urine for protein and sediment changes prior to each injection. Perform CBC including platelet estimation before every second injection throughout the course of therapy
• Rapid reduction of hemoglobin, leukopenia <4000 WBC/mm³, eosinophilia >5%, platelet counts <100,000/mm³, albuminuria, hematuria, pruritus, skin eruption, stomatitis, or persistent diarrhea are possibly associated with gold toxicity. Avoid administration of additional injections of gold sodium thiomalate unless it is clear that these abnormalities are caused by conditions other than gold toxicity
• Before initiation of gold therapy, diabetes mellitus or CHF should be under control
• Avoid concomitant use with penicillamine
• Safety of co-administration with cytotoxic drugs has not been evaluated

Cautions: Use cautiously in

• Renal impairment
• Hepatic impairment
• History of kidney/liver disease
• Cardiovascular disease
• Uncontrolled diabetes mellitus
• Uncontrolled CHF
• Severe hypertension
• Cerebrovascular disease
• Compromised cerebral/cardiovascular circulation
• History of blood dyscrasias such as granulocytopenia or anemia caused by drug sensitivity
• Ulcerative colitis
• Significant dermatitis
• Allergy/hypersensitivity to medications
• Skin rash

Pregnancy Category:C

Breastfeeding: Avoid use. Gold sodium thiomalate is excreted in breast milk in small amounts and is minimally absorbed by infants. If used during lactation, monitoring breastfed infants for possible adverse events would seem prudent. This information is based upon LactMed database (available at http://toxnet.nlm.nih.gov/cgi-bin/sis/htmlgen?LACT). This drug is compatible and considered safe with breastfeeding based upon data from AAP Policy Guidelines (available at http://aappolicy.aappublications.org/cgi/content/full/pediatrics;108/3/77 last accessed 26 July 2011). According to the manufacturer's data, because of the potential for serious adverse reactions in nursing infants, a decision should be made whether to discontinue nursing or to discontinue the drug, analyzing the importance of the drug to the mother. Slow excretion and persistence of gold in the mother, even after therapy is discontinued, must be kept in mind.

• CV: Bradycardia, syncope
• CNS: Elevated CSF protein, seizures, hallucinations, headache, dizziness
• NEURO: Peripheral neuropathy, Guillain-Barre syndrome
• DERM: Exfoliative dermatitis, alopecia, dermatitis, pruritus, flushing, diaphoresis
• GI: Stomatitis, ulcerative enterocolitis, glossitis, gingivitis, metallic taste, nausea, vomiting, anorexia, abdominal cramps, diarrhea, jaundice
• GU: Nephrotic syndrome, glomerulitis with hematuria, proteinuria
• EENT: Corneal ulcer, iritis, conjunctivitis, ocular gold deposits, sensorimotor effects
• HEMA: Blood dyscrasias, granulocytopenia, thrombocytopenia, aplastic or hypoplastic anemia
• RESP: Interstitial pneumonitis, pulmonary fibrosis, gold bronchitis
• HYPERSENSITIVITY: Anaphylaxis, anaphylactoid/nitritoid reactions, angioedema
• MISC: Hepatitis, malaise, weakness, transient arthritis flare

• Gold compound; exact mode of action is unknown; predominant action appears to be a suppressive effect on the synovitis of active rheumatoid disease and may slow disease progression
• Rapidly absorbed following IM administration
• Metabolism: Unknown
• Excretion: Urine 50-90%; feces 10-50%
• Half-Life: 3-27 days, may be prolonged with multiple doses

US Trade Name(s)

• Myochrysine (Discontinued)

US Availability

Myochrysine

• INJ: 50 mg/mL (1, 10 mL vials)

Canadian Trade Name(s)

• Myochrysine

Canadian Availability

sodium aurothiomalate (generic)

• INJ: 10 mg/mL
• INJ: 25 mg/mL
• INJ: 50 mg/mL

Myochrysine

• INJ: 10 mg/mL (1 mL amp)
• INJ: 25 mg/mL (1 mL amp)
• INJ: 50 mg/mL (1 mL amp)

UK Trade Name(s)

• Myocrisin

UK Availability

Myocrisin

• INJ: 20 mg/mL
• INJ: 100 mg/mL

Australian Trade Name(s)

• Myocrisin

Australian Availability

Myocrisin

• INJ: 10 mg/0.5 mL (1 mL amp)
• INJ: 20 mg/0.5 mL (1 mL amp)
• INJ: 50 mg/0.5 mL (1 mL amp)

[Outline]

Rheumatologic

Antirheumatic Agents