Gold Sodium Thiomalate
Pronunciation: gold SO-dee-uhm thigh-oh-MAL-ate
Class: Gold compound
- Injection 50 mg/mL
Mechanism unknown; suppresses symptoms of rheumatoid arthritis and may slow progression of this disease.
Mean C ss is 1 to 5 mcg/mL. T max is 2 to 6 h.
Protein binding is 95% to 99%.
Plasma t 1/ 2 is 3 to 27 d (single dose); 14 to 40 d (third dose); up to 168 d (11 th dose). 70% is excreted in urine, 30% in feces.
Indications and Usage
Symptomatic relief of active adult and juvenile rheumatoid arthritis not adequately controlled by other therapies.
Treatment of pemphigus and psoriatic arthritis.
Previous severe reaction to gold compounds or other heavy metals; uncontrolled diabetes mellitus or CHF; severe debilitation; kidney disease; liver disease; severe hypertension; agranulocytosis or bleeding disorder; recent radiation exposure; systemic lupus erythematosus; urticaria; eczema.
Dosage and AdministrationAdults
IM As weekly injections: First wk, 10 mg; second wk, 25 mg; third and following wks, 25 to 50 mg until major clinical improvement or toxicity occurs. If cumulative dose reaches 1 g without improvement, re-evaluate use of gold therapy. Once improvement occurs, dose may be decreased or dosing interval increased. Maintenance therapy: 25 to 50 mg every other wk for 2 to 20 wk. On basis of response, dosage interval may be increased to every third and subsequently fourth wk (maximum dose per injection: 100 mg).Children
After test dose of 10 mg, give 1 mg/kg (maximum dose per injection: 50 mg). Dosage schedule similar to that for adults.
- Color of solution is pale yellow. Do not administer drug if it has darkened in color or contains precipitate.
- Mix contents of vial thoroughly before withdrawing into syringe.
- Administer drug only by IM injection into upper outer quadrant of gluteus maximus muscle.
- Instruct patient to remain lying down for 10 to 15 min after injection.
Store in light-resistant containers at room temperature.
Drug InteractionsAntimalarials, penicillamine
Safety of combination antirheumatic therapy is unknown.Cytotoxic drugs, immunosuppressives (except steroids), phenylbutazone
May increase risk of blood dyscrasias.
Laboratory Test Interactions
None well documented.
May occur months after therapy is discontinued.
Dermatitis; pruritus; exfoliative dermatitis; angioedema; chrysiasis (gray-blue skin pigmentation).
Stomatitis; corneal gold deposition; corneal ulceration; iritis; conjunctivitis; metallic taste. Children: Safety and efficacy in children younger than 6 yr of age have not been established.
Diarrhea; nausea; cholestatic jaundice; ulcerative enterocolitis; GI bleeding; difficulty swallowing; abdominal pain and cramping.
Nephrotic syndrome or glomerulitis with proteinuria and hematuria.
Anemia; thrombocytopenia; leukopenia; aplastic anemia.
Interstitial pneumonitis; pulmonary fibrosis.
Anaphylactoid reactions within minutes of injection, arthralgias for several days after injection, “nitritoid reaction” (eg, vasomotor reaction with flushing, fainting, weakness, dizziness, sweating, nausea, vomiting, malaise and headache).
Review patient's laboratory values for indications of gold toxicity such as decreased hemoglobin, WBC less than 4,000 mm 3 , platelets less than 100,000 to 150,000/mm 3 , granulocytes less than 1,500/mm 3 , proteinuria and elevated liver enzymes.Preinjection assessment
Prior to each injection, assess patient for early signs and symptoms of toxicity: pruritus, dermatitis, stomatitis, metallic taste, indigestion, diarrhea.
Category C .
Excreted in breast milk.
Use with caution. Tolerance to gold decreases with age.
Special Risk Patients
Use with caution in patients with diabetes mellitus, CHF, history of blood dyscrasias, CV or cerebral circulation problems, skin rash, previous kidney or liver disease, marked hypertension, compromised circulation, or inflammatory bowel disease.
Confusion; hallucinations; seizures.
Hematuria, proteinuria, thrombocytopenia, granulocytopenia, fever, nausea, vomiting, diarrhea, skin lesions, urticaria, exfoliative dermatitis, severe pruritus.
- Explain that adverse reactions can occur any time during therapy, even months after drug has been discontinued.
- Caution patient to minimize exposure to sun and other sources of ultraviolet light (eg, sunlamp). Explain need to wear protective clothing outdoors.
- Advise patient of importance of continued assessment of disease status and monitoring of renal, hepatic, and hematologic functions.
- Teach patient to perform good oral hygiene, including use of soft toothbrush and daily flossing. If mild stomatitis develops, isotonic sodium chloride and sodium bicarbonate solution can be used. Advise patient to avoid strong commercial mouthwashes and spicy or acidic foods.
- Inform patient that joint pain may continue for 1 to 2 days after injection but will usually decrease after first few injections. Therapeutic effects may not be seen until after 3 to 6 mo of treatment. Explain that drug will not reverse damage or cure disease but may slow or stop its progression.
- Instruct patient to report these symptoms to health care provider: dermatitis, pruritus, weakness, metallic taste, fatigue, hematuria, unusual bruising or ecchymosis, nose bleeds, sore mouth, dark-colored stools.
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