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Gold Sodium Thiomalate

Pronunciation

(gold SOW dee um thye oh MAL ate)

Index Terms

  • Sodium Aurothiomalate

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product

Solution, Intramuscular:

Myochrysine: 50 mg/mL (1 mL [DSC]) [contains benzyl alcohol]

Brand Names: U.S.

  • Myochrysine [DSC]

Pharmacologic Category

  • Gold Compound

Pharmacology

Unknown, may decrease prostaglandin synthesis or may alter cellular mechanisms by inhibiting sulfhydryl systems

Excretion

Urine (60% to 90%); feces (10% to 40%)

Onset of Action

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

Use: Labeled Indications

Adjunctive treatment of active rheumatoid arthritis

Contraindications

Hypersensitivity to gold compounds or any component of the formulation; history of severe toxicity to gold compounds or heavy metals; systemic lupus erythematosus; severe debilitation

Dosing: Adult

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.

Dosing: Geriatric

Refer to adult dosing.

Dosing: Pediatric

Rheumatoid arthritis: IM: Initial: Test dose of 10 mg is recommended, followed by 1 mg/kg/week (maximum: 50 mg/injection); maintenance: 1 mg/kg/dose (maximum: 50 mg/injection) at every-other-week intervals for 2-20 weeks, then every 3-4 weeks. Early improvement may be observed after 6-8 weeks of therapy; months of therapy may be required before clinical improvement is observed.

Dosing: Renal Impairment

Aronoff, 2007:

CrCl 50-80 mL/minute: Administer 50% of normal dose.

CrCl <50 mL/minute: Avoid use.

Dosing: Hepatic Impairment

No dosage adjustment provided in manufacturer’s labeling; use with caution.

Administration

Deep IM injection into the upper outer quadrant of the gluteal region; addition of 0.1 mL of 1% lidocaine to each injection may reduce the discomfort associated with IM administration. Patient should remain in recumbent position for approximately 10 minutes following administration.

Storage

Should not be used if solution is darker than pale yellow.

Drug Interactions

ACE Inhibitors: May enhance the adverse/toxic effect of Gold Sodium Thiomalate. An increased risk of nitritoid reactions has been appreciated. Monitor therapy

Adverse Reactions

Frequency not defined.

Cardiovascular: Bradycardia, syncope

Central nervous system: Confusion, fever, Guillain-Barré syndrome, hallucinations, seizure

Dermatologic: Alopecia, angioedema, dermatitis, nail shedding, pruritus, rash, urticaria

Gastrointestinal: Anorexia, abdominal cramps, diarrhea, dysphagia, enterocolitis (ulcerative), gingivitis, glossitis, nausea, stomatitis, taste disturbance (metallic), thick tongue, vomiting

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

Hepatic: Cholestasis, hepatitis, hepatotoxicity, jaundice

Neuromuscular & skeletal: Arthralgia, peripheral neuropathy

Ocular: Conjunctivitis, corneal ulcers, gold deposits in ocular tissues, iritis

Respiratory: Dyspnea, gold bronchitis, interstitial pneumonitis, pulmonary fibrosis

Renal: Glomerulitis, hematuria, nephrotic syndrome, proteinuria

Miscellaneous: Anaphylactoid reaction, anaphylaxis, nitritoid reaction

Warnings/Precautions

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.

Monitoring Parameters

Patients should have a CBC with differential, platelet count, hemoglobin determination and urinalysis for protein, white cells, red cells and casts; at baseline and prior to each injection. Skin and oral mucosa should be inspected for skin rash, bruising or oral ulceration/stomatitis. Specific questioning for symptoms such as pruritus, rash, stomatitis or metallic taste should be included. Dosing should be withheld in patients with significant gastrointestinal, renal, dermatologic, or hematologic effects (platelet count falls to <100,000/mm3, WBC <4000, granulocytes <1500/mm3

Pregnancy Risk Factor

C

Pregnancy Considerations

Adverse events were observed in animal reproduction studies

Patient Education

• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)

• Patient may experience dyspepsia or lack of appetite. Have patient report immediately to prescriber signs of infection, signs of hepatic impairment, severe nausea, stomatitis, dysgeusia, ecchymosis, hemorrhaging, significant asthenia, considerable headache, flushing, intolerable dizziness, syncope, hyperhidrosis, urinary retention, oliguria, hematuria, considerable diarrhea, vision changes, ophthalmalgia, eye irritation, dysphagia, bradycardia, illogical thinking, hallucinations, dyspnea, angina, paresthesia, or signs of ulcerative enterocolitis (rare) (HCAHPS).

• Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.

Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for healthcare professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience and judgment in diagnosing, treating and advising patients.

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