Gold sodium thiomalate

390.08

389.92100

235-479-7

White to yellowish-white powder; mixture of mono- and disodium salts

M - Musculo-skeletal system

2930909090

105.56000

-2.56010

Very soluble in water. Practically insoluble in alcohol, ether

... Gold sodium thiomalate injection should be protected from light and stored at a temperature less than 40C, preferably at 1530C; freezing should be avoided.

Odorless

Metallic taste

Aqueous solutions are colorless to pale yellow; pH of 5% aq solution: 5.8-6.5|Affected by light

3

20/21/22-43

36

MD5435000

Xn

Following the date of manufacture, ... gold sodium thiomalate injection /has an expiration date/ of 5 years.

SRP: The most favorable course of action is to use an alternative chemical product with less inherent propensity for occupational exposure or environmental contamination. Recycle any unused portion of the material for its approved use or return it to the manufacturer or supplier. Ultimate disposal of the chemical must consider: the material's impact on air quality; potential migration in soil or water; effects on animal, aquatic, and plant life; and conformance with environmental and public health regulations.

|Warning|H302 (100%): Harmful if swallowed [Warning Acute toxicity, oral]|P261, P264, P270, P271, P272, P280, P301+P312, P302+P352, P304+P312, P304+P340, P312, P321, P330, P333+P313, P363, and P501|Aggregated GHS information provided by 6 companies from 1 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.

Overdosage symptoms are those of heavy metal toxicity; they include pruritus, dermatitis, stomatitis, vague gastrointestinal discomfort, albuminuria with or without a nephrotic syndrome, hematuria, agranulocytosis, thrombocytopenic purpura, and aplastic anemia.

About 85-90% of the drug is protein bound.

Small amounts of gold have been shown to be distributed into milk in women receiving ... gold sodium thiomalate.

A disease-modifying antirheumatic drug (DMARD) indicated for the symptomatic treatment of arthritis.

... Gold sodium thiomalate ... /is/ indicated in the treatment of adult or juvenile rheumatoid arthritis. ... /This agent is/ usually used for treating patients who show evidence of continued or additional disease activity despite conservative therapy, e.g., with salicylates (especially aspirin) or other nonsteroidal anti-inflammatory agents, glucocorticoids, etc. /Included in US product labeling/|Gold compounds are used in the treatment of these rheumatic conditions / psoriatic arthritis, Felty's syndrome/. /Gold compounds; NOT included in US product labeling/

Patients with an impaired sulfoxidation ability (decreased ability to oxidize sulfhydryl-containing compounds) may be predisposed to ... /gold sodium thiomalate/ toxicity.|Vasomotor rections follow injections within minutes to hours and consist of weakness, dizziness, nausea, sweating and flushing, frequently accompanied by hypotension. Slower onset reactions consist of an exacerbation of joint pain and swelling, fatigue, and malaise that usually occur 6-24 hr after injection.|Dermatitis is the most common reaction. Any eruption, especially if pruritic, that develops with treatment with myochrysine should be considered a reaction to gold until proven otherwise. Pruritus often exists before dermatitis becomes apparent, and there fore should be considered a warning signal of impending cutaneous reaction. The most serious form of cutaneous reaction is generalized exfoliative dermatitis which may lead to alopecia and shedding of nails. Gold dermatitis may be aggravated by exposure to sunlight or an actinic rash may develop.|Stomatitis is the second most common adverse reaction. Shallow ulcers on the buccal membranes, on the borders of the tongue and on the palate, or on the pharynx may occur as the only adverse reaction, or along with dermatitis. Sometimes diffuse glossitis or gingivitis develops. A metallic taste may precede these oral mucous membrane reactions and should be considered a warning signal.|For more Drug Warnings (Complete) data for GOLD SODIUM THIOMALATE (11 total), please visit the HSDB record page.

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

Drugs that are used to treat RHEUMATOID ARTHRITIS. (See all compounds classified as Antirheumatic Agents.)

Gold sodium thiomalate solutions are rapidly absorbed following IM injection, with peak serum concentrations occurring in 3-6 hours.|The major route of elimination of an IV dose of gold sodium thiomalate is urinary excretion, with a mean of 35% of the dose found in the urine in ten days. Fecal elimination accounts for an additional 9.4% of the IV dose excreted in ten days, probably as a result of biliary secretion.|The apparent volume of distribution is 0.26 +/- 0.051 kg-1|7.0 ml/ kg/day|Higher tissue levels occur with parenteral gold salts, with a mean steady state plasma level of 1 to 5 ug/ml. Drug is distributed widely throughout the body in lymph nodes, bone marrow, kidneys, liver, spleen, and tissues. About 85% to 90% is protein-bound.|Gold has been shown to cross the placenta in pregnant women receiving gold sodium thiomalate. Small amounts of gold have been shown to be distributed into milk in women receiving ... gold sodium thiomalate.|Following single 10-mg doses of gold sodium thiomalate, serum gold concentrations showed a biphasic decline with a relatively rapid early phase (serum half-life about 43 hours) and a slow late phase (serum half-life about 6 days). The slow phase of decline may result from excretion and the rapid phase of decline may result from tissue distribution. The true potential of gold compounds, including ... gold sodium thiomalate, to cumulate has not been clearly defined, but it is clear that substantially larger amounts of gold are retained in the body during therapy with parenteral gold compounds than during therapy with auranofin.|For more Absorption, Distribution and Excretion (Complete) data for GOLD SODIUM THIOMALATE (8 total), please visit the HSDB record page.

No data available.|For a patient receiving gold sodium thiomalate the principal gold species in the urine is [Au(CN)2]-, which is also seen in a low molecular weight infiltrate of the blood

12.5 days|Following single 10-mg doses of gold sodium thiomalate, serum gold concentrations showed a biphasic decline with a relatively rapid early phase (serum half-life about 43 hours) and a slow late phase (serum half-life about 6 days).|...Terminal log-linear phases corresponded to a mean disposition half-life of 25 days...|... the mean alpha half-lives were 0.738 and 1.78 hr for the iv and im routes, respectively. The corresponding terminal (beta) half-lives were 54.1 and 63.0 hr...|Four normal male volunteers participated in a study designed to examine the disposition of gold given intramuscularly as gold sodium thiomalate. Blood samples were collected for 32 days following the administration of 10 mg of gold sodium thiomalate. .... Terminal log-linear phases corresponded to a mean disposition half-life of 25 days. ...

The precise mechanism of action is unknown. It is known that sodium aurothiomalate inhibits the synthesis of prostaglandins. The predominant action appears to be a suppressive effect on the synovitis of active rheumatoid disease.|...The effects of aurothiomalate, on basal and forskolin-activated adenylyl cyclase activity in human total lymphocyte membranes and in membranes of T and B lymphocyte subsets /was studied/. The gold compounds inhibited adenylyl cyclase activity. This inhibitory effect required the presence of both the sulfhydryl ligands and aurous cation. Regulation of lymphocyte adenylyl cyclase by gold compounds represents a potential mode of action of these drugs in rheumatic disease.|Transcription factor NF-kappaB controls the expression of a number of genes including those for cell adhesion molecules such as E-selectin, ICAM- 1 and VCAM- 1. These cell adhesion molecules are known to play important roles in a critical step of tumor metastasis; the arrest of tumor cells on the venous or capillary bed of the target organ. NF-kappaB is activated by extracellular signals such as those elicited by the proinflammatory cytokines, TNF and IL-1. ...The adhesion of tumor cells to IL-1 beta-treated HUVEC /human umbilical vein endothelial cells/ was inhibited by gold compounds such as aurothiomalate.|Gold dermatosis is mediated, at least in part, by allergic mechanisms

When severe reactions to gold occur, corticosteroids, dimercaprol (a chelating agent), or penicillamine may be given to aid recovery. Prednisone ... is recommended to manage severe renal, hematologic, pulmonary, or enterocolic reactions to gold. Dimercaprol may be used together with corticosteroids to facilitate removal of the gold when corticosteroid treatment alone is ineffective.|Treatment with myochrysine /gold sodium thiomalate/ should be discontinued immediately when toxic reactions occur. Minor complications such as localized dermatitis, mild stomatitis or slight proteinuria generally require no other therapy and resolve spontaneously with suspension of myochrysine /gold sodium thiomalate/. Moderately severe skin and mucous membrane reactions often benefit from topical corticosteroids, oral antihistaminics, and soothing or anesthetic lotions.|For serious renal, hematologic, pulmonary, and enterocolitic complications, high doses of systemic corticosteroids are recommended. The optimum duration of corticosteroid treatment varies with response of the individual patient. Therapy may be required for many months when adverse effects are unusually severe or progressive.|In patients whose complications do not improve with high dose corticosteroid treatment, or who develop significant steroid related adverse reactions, a chelating agent may be given to enhance gold excretion. Dimercaprol (BAL) has been used successfully, but patients must be monitored carefully as numerous untoward reactions may attend it use. Corticosteroids and chelating agents may be used concomitantly.|For more Antidote and Emergency Treatment (Complete) data for GOLD SODIUM THIOMALATE (7 total), please visit the HSDB record page.

/CASE REPORTS/ A 53-year-old male was accidentally injected with an intramuscular dose of 450 mg of ... /gold sodium thiomalate/. Palpebral edema and rash were observed within 30 minutes. The blood gold levels reach 2970 ug/dlL without significant toxicity. The patient was treated with BAL (British anti-lewisite) and recovered.|/HUMAN EXPOSURE STUDIES/ .../The authors/ investigated whether allergic mechanisms are involved in dermatosis induced by gold sodium thiomalate (GSTM). Thirteen gold dermatosis patients, 15 arthritis patients without any side-effects from GSTM and 11 healthy controls participated in the study. Venous blood lymphocytes from these subjects were cultured with GSTM and gold sodium thiosulfate (GSTS) in the lymphocyte proliferation test (LPT). In some cases, interferon-gamma-producing cells were enumerated in vitro (T-cell ELISpot). The subjects were also patch-tested with GSTM and GSTS. The LPT to either GSTM, GSTS or both was positive in 12 of 13 patients with gold dermatosis. In the arthritis patient group without side-effects from gold, the LPT gave two false-positive results and in the healthy control group the LPT was falsely positive with one subject. T-cell ELISpot was positive in four of six gold dermatosis patients and negative in the arthritis and healthy control groups. Only one patient who also developed contact dermatitis from gold jewelry was positive to gold in the patch test.|/SIGNS AND SYMPTOMS/ Dermatitis is the most common reaction. Any eruption, especially if pruritic, that develops with treatment with myochrysine should be considered a reaction to gold until proven otherwise. Pruritus often exists before dermatitis becomes apparent, and there fore should be considered a warning signal of impending cutaneous reaction. The most serious form of cutaneous reaction is generalized exfoliative dermatitis which may lead to alopecia and shedding of nails. Gold dermatitis may be aggravated by exposure to sunlight or an actinic rash may develop.|/SIGNS AND SYMPTOMS/ Stomatitis is the second most common adverse reaction. Shallow ulcers on the buccal membranes, on the borders of the tongue and on the palate, or on the pharynx may occur as the only adverse reaction, or along with dermatitis. Sometimes diffuse glossitis or gingivitis develops. A metallic taste may precede these oral mucous membrane reactions and should be considered a warning signal.|For more Human Toxicity Excerpts (Complete) data for GOLD SODIUM THIOMALATE (6 total), please visit the HSDB record page.

Aurolate

Parenteral: Injection, for IM use only, 50 mg/ml; Aurolate (with benzyl alcohol 0.5%), Taylor|Myochrysine is supplied as a solution for intramuscular injection containing 50 mg of gold sodium thiomalate per ml.

Analyte: gold sodium thiomalate; matrix: chemical identification; procedure: visual reaction (white precipitate) with calcium nitrate, nitric acid, and ammonium acetate|Analyte: gold sodium thiomalate; matrix: chemical identification; procedure: visual reaction (yellow precipitate) with silver nitrate and ammonium hydroxide|Analyte: gold sodium thiomalate; matrix: chemical identification; procedure: visual reaction with ammonium hydroxide and hydrogen peroxide, and evaporation resulting in particles of gold|Analyte: gold sodium thiomalate; matrix: chemical purity; procedure: dissolve in water, filter, react with nitric and sulfuric acids, heat, cool, react with hydrogen peroxide, heat, cool, filter, dry, weigh residue|For more Analytic Laboratory Methods (Complete) data for GOLD SODIUM THIOMALATE (7 total), please visit the HSDB record page.