Sodium aurothiomalate

Absorption

Gold sodium thiomalate solutions are rapidly absorbed following IM injection, with peak serum concentrations occurring in 3-6 hours.

Toxicity

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.

Physical properties

White to yellowish white powder; odorless; metallic taste; highly soluble in water; practically insoluble in ethanol and ether.

The Uses of Sodium aurothiomalate

Sodium aurothiomalate(I) is useful for high mobility group box chromosomal protein 1 western blotting.

The Uses of Sodium aurothiomalate

Medicine (antirheumatic).

Indications

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

What are the applications of Application

Gold sodium thiomalate is a compound useful for high mobility group box chromosomal protein 1 western blotting

Background

Sodium aurothiomalate is a gold compound that is used for its immunosuppressive anti-rheumatic effects. Gold Sodium Thiomalate is supplied as a solution for intramuscular injection containing 50 mg of Gold Sodium Thiomalate per mL. It is most effective in active progressive rheumatoid arthritis and of little or no value in the presence of extensive deformities or in the treatment of other forms of arthritis.

Definition

White to yellowish-white powder; odorless; metallic taste. Affected by light. Very soluble in water; practically insoluble in alcohol and ether; aqueous solutions are colorless to pale yellow; pH (5% solution) 5.8–6.5.

Production Methods

Gold(I) thiomalate is prepared by reacting sodium thiomalate with gold(I) halide. It is stored in the dark and otherwise protected from light.

brand name

Myochrysine (Merck), Aurolate (Pasadena, USA), Myocrisin (Rh?one-Poulenc Rorer, Denmark, Sweden, Finland), Tauredon (BYK Gulden, Germany).

Pharmaceutical Applications

Sodium aurothiomalate is a commonly used gold-based DMARD and is indicated for active progressive RA. It is administered by deep intramuscular injection. Administration is started with a test dose of 10mg followed by weekly intervals of 50 mg doses. An improvement is expected to be seen once 300–500 mg is administered. Treatment should be discontinued if there is no improvement after administering 1 g or 2months. Intervals of administration should be gradually increased to 4weeks in patients in whom an effect can be seen. If any blood disorders or other side effects such as GI bleedings or proteinuria are observed, sodium aurothiomalate should be discontinued.

Pharmacokinetics

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

Clinical Use

Active progressive rheumatoid arthritis in adults

Safety Profile

Poison by subcutaneous and intramuscular routes. Moderately toxic bj intravenous ' route. Human systemic effects: aggression, agranulocytosis, aplastic anemia, cell count changes, changes in circulation, cholestatic jaunhce, dermatitis, encephalitis, fasciculations, flaccid paralysis without anesthesia, hemorrhage, hepatitis (hepatocellular necrosis), increased body temperature, interstitial fibrosis, muscle weakness, proteinuria, recording from peripheral motor nerve, depressed renal function tests, somnolence, structural changes in nerve sheath, thrombocytopenia, uncharacterized allergc reaction, changes in blood, teeth, and supporting structures. Experimental teratogenic and reproductive effects. When heated to decomposition it emits very toxic Na2O and SOx.

Synthesis

Synthesis: a solution of thiomalic acid and 3 equivalents of sodium hydroxide are mixed with an aqueous suspension of gold(I) iodide. The product, a mixture of the mono- and disodium salts, is precipitated by the addition of ethanol.

Drug interactions

Potentially hazardous interactions with other drugs
ACE-inhibitors: flushing and hypotension reported in combination.
Penicillamine: increased risk of toxicity - avoid.

Metabolism

No data available.

Metabolism

Mainly excreted in the urine with smaller amounts in the faeces.