Gold Sodium Thiomalate

You should not use this medication if you have ever had an allergic reaction to a gold medication, or if you have:

• lupus;
• if you are severely debilitated; or
• if you are also using penicillamine (Cuprimine, Depen).

To make sure gold sodium thiomalate is safe for you, tell your doctor if you have any of these conditions:

• kidney disease;
• liver disease;
• heart disease, high blood pressure, congestive heart failure;
• circulation problems or a history of stroke;
• cancer;
• diabetes;
• malaria;
• a blood cell disorder such as anemia or low levels of platelets in your blood; or
• a history of allergic reaction or blood cell problems caused by any medication.

FDA pregnancy category C. It is not known whether gold sodium thiomalate will harm an unborn baby. Tell your doctor if you are pregnant or plan to become pregnant while using this medication.

Gold sodium thiomalate passes into breast milk and may affect a nursing infant. Gold sodium thiomalate is not recommended for use during breast-feeding. Do not take gold sodium thiomalate without first talking to your doctor if you are breast-feeding a baby.

Call your doctor for instructions if you miss an appointment for your gold sodium thiomalate injection.

• It is used to treat rheumatoid arthritis.
• It may be given to you for other reasons. Talk with the doctor.

Use gold sodium thiomalate as ordered by your doctor. Read all information given to you. Follow all instructions closely.

• It is given as a shot into a muscle.

What do I do if I miss a dose?

• Call your doctor to find out what to do.

• Gold Compound

Delayed; may require up to 3 months

Time to Peak

Serum: 4-6 hours

Half-Life Elimination

5 days; may be prolonged with multiple doses

Adjunctive treatment of active rheumatoid arthritis

Rheumatoid arthritis: IM: 10 mg first week; 25 mg second week; then 25-50 mg/week until development of toxicity or 1 g cumulative dose has been given; if improvement occurs without adverse reactions, the dose may be decreased or the dosing interval increased; Maintenance: 25-50 mg every other week for 2-20 weeks, then every 3-4 weeks indefinitely

Note: Failure to improve during initial therapy may warrant continuation of 25-50 mg for additional 10 weeks or a dose increase in increments of 10 mg every 1-4 weeks (maximum: 100 mg/injection). Discontinue therapy if no improvement or toxicity develops.

Frequency not defined.

Cardiovascular: Bradycardia, syncope, vasomotor symptoms (nitritoid reaction)

Central nervous system: Confusion, Guillain-Barre syndrome, hallucination, metallic taste, peripheral neuropathy, seizure

Dermatologic: Alopecia, dermatitis, onycholysis, pruritus, skin rash, urticaria

Gastrointestinal: Anorexia, abdominal cramps, cholestasis, diarrhea, dysphagia, gingivitis, glossitis, nausea, stomatitis, ulcerative enterocolitis, vomiting

Genitourinary: Hematuria, nephrotic syndrome, proteinuria

Hematologic & oncologic: Agranulocytosis, aplastic anemia, eosinophilia, leukopenia, purpura, thrombocytopenia

Hepatic: Hepatitis, hepatotoxicity, jaundice

Hypersensitivity: Anaphylactoid reaction, anaphylaxis, angioedema, tongue edema

Neuromuscular & skeletal: Arthralgia

Ophthalmic: Conjunctivitis, corneal ulcer, iritis

Renal: Glomerulonephritis

Respiratory: Bronchitis (gold bronchitis), dyspnea, interstitial pneumonitis, pulmonary fibrosis

Miscellaneous: Fever

Concerns related to adverse effects:

• Dermatologic reactions: Dermatitis and lesions of the mucous membranes are common and may be serious; pruritus may precede the early development of a skin reaction. Consider alternative therapy in patients with dermatitis (urticaria or eczema; relative contraindication); may increase risk and/or symptoms of gold toxicity may be more difficult to detect.

• Gastrointestinal effects: Signs of toxicity include persistent diarrhea, stomatitis, and enterocolitis; avoid use in patients with prior inflammatory bowel disease.

• Hematologic effects: Signs of toxicity include hematologic depression (depressed hemoglobin, eosinophilia >5%, leukocytes, granulocytes, or platelets). Avoid use in patients with a history of blood dyscrasias (anemia, agranulocytosis), hemorrhagic diathesis, or drug induced granulocytopenia. Symptoms of gold toxicity may be difficult to detect in patients with prior abnormalities; consider alternative therapy. Therapy should be discontinued if platelet count falls to <100,000/mm3, WBC <4000, granulocytes <1500/mm3.

• Hepatic effects: May be associated with the development of cholestatic jaundice. Consider alternative therapy in patients with hepatic impairment (relative contraindication); may increase risk and/or symptoms of gold toxicity may be more difficult to detect.

• Hypersensitivity reactions: Rare hypersensitivity reactions, including anaphylactic shock, syncope, bradycardia, thickening of the tongue, difficulty in swallowing and breathing, and angioedema have been reported in association with injections of sodium aurothiomalate; treatment should be discontinued if occur. In addition, a vasomotor (nitritoid) reaction characterized by acute flushing and tachycardia may occur within minutes of injection; this reaction should be differentiated from anaphylaxis and therapy may be continued, but a careful evaluation of risk vs benefit should be undertaken and extreme caution should be exercised before resuming therapy, particularly in patient with cardiovascular disease.

• Pulmonary toxicity: May be associated with interstitial fibrosis; monitor closely.

• Renal effects: Renal toxicity ranges from mild proteinuria to nephrotic syndrome. Consider alternative therapy in patients with renal impairment; may increase risk and/or symptoms of gold toxicity may be more difficult to detect.

Disease-related concerns:

• Cardiovascular disease: Use caution in patients with HF, hypertension, or cerebrovascular disease.

• Systemic lupus erythematosus (SLE): Consider alternative therapy is patients with SLE (relative contraindication); may increase risk and/or symptoms of gold toxicity may be more difficult to detect.

Concurrent drug therapy issues:

• ACE inhibitors: Concurrent use with ACE inhibitors may increase the risk of nitritoid reactions.

• Corticosteroids: In general, corticosteroids may be discontinued after initiation of therapy (corticosteroid tapering may be required).

• NSAIDs: May be discontinued after initiation of therapy.

Dosage form specific issues:

• Benzyl alcohol and derivatives: Some dosage forms may contain benzyl alcohol; large amounts of benzyl alcohol (≥99 mg/kg/day) have been associated with a potentially fatal toxicity (“gasping syndrome”) in neonates; the “gasping syndrome” consists of metabolic acidosis, respiratory distress, gasping respirations, CNS dysfunction (including convulsions, intracranial hemorrhage), hypotension and cardiovascular collapse (AAP ["Inactive" 1997]; CDC, 1982); some data suggests that benzoate displaces bilirubin from protein binding sites (Ahlfors, 2001); avoid or use dosage forms containing benzyl alcohol with caution in neonates. See manufacturer’s labeling.

Other warnings/precautions:

• Administration: Must not be injected IV

• Monitoring: Frequent monitoring of patients for signs and symptoms of toxicity will prevent serious adverse reactions.