Sodium aurothiomalate (
INN, known in the
United States
The United States of America (USA), also known as the United States (U.S.) or America, is a country primarily located in North America. It is a federal republic of 50 U.S. state, states and a federal capital district, Washington, D.C. The 48 ...
as gold sodium thiomalate) is a
gold compound that is used for its immunosuppressive
anti-rheumatic effects. Along with an orally-administered gold salt,
auranofin, it is one of only two gold compounds currently employed in modern medicine.
Medical uses
It is primarily given once or twice weekly by intramuscular injection for moderate-severe
rheumatoid arthritis
Rheumatoid arthritis (RA) is a long-term autoimmune disorder that primarily affects synovial joint, joints. It typically results in warm, swollen, and painful joints. Pain and stiffness often worsen following rest. Most commonly, the wrist and h ...
. It was also once used to treat
tuberculosis
Tuberculosis (TB), also known colloquially as the "white death", or historically as consumption, is a contagious disease usually caused by ''Mycobacterium tuberculosis'' (MTB) bacteria. Tuberculosis generally affects the lungs, but it can al ...
, though later trials showed it to be harmful and ineffective for that purpose.
Adverse effects
Its most common side effects are digestive (mostly
dyspepsia
Indigestion, also known as dyspepsia or upset stomach, is a condition of impaired digestion. Symptoms may include upper abdominal fullness, heartburn, nausea, belching, or upper abdominal pain. People may also experience feeling full earlier ...
,
mouth swelling, nausea, vomiting and taste disturbance), vasomotor (mostly flushing, fainting, dizziness, sweating, weakness, palpitations,
shortness of breath
Shortness of breath (SOB), known as dyspnea (in AmE) or dyspnoea (in BrE), is an uncomfortable feeling of not being able to breathe well enough. The American Thoracic Society defines it as "a subjective experience of breathing discomfort that con ...
and blurred vision) or dermatologic (usually itchiness, rash, local irritation near to the injection site and hair loss) in nature, although
conjunctivitis
Conjunctivitis, also known as pink eye or Madras eye, is inflammation of the conjunctiva, the thin, clear layer that covers the white surface of the eye and the inner eyelid. It makes the eye appear pink or reddish. Pain, burning, scratchiness ...
, blood dyscrasias, kidney damage,
joint pain
Arthralgia () literally means 'joint pain'. Specifically, arthralgia is a symptom of injury, infection, illness (in particular arthritis), or an allergic reaction to medication
Medication (also called medicament, medicine, pharmaceutic ...
,
muscle aches/pains and liver dysfunction are also common.
Less commonly, it can cause
gastrointestinal bleeding
Gastrointestinal bleeding (GI bleed), also called gastrointestinal hemorrhage (GIB), is all forms of bleeding in the gastrointestinal tract, from the mouth to the rectum. When there is significant blood loss over a short time, symptoms may includ ...
, dry mucous membranes and
gingivitis
Gingivitis is a non-destructive disease that causes inflammation of the gums; ulitis is an alternative term. The most common form of gingivitis, and the most common form of periodontal disease overall, is in response to bacterial biofilms (also ...
.
[ Rarely it can cause aplastic anaemia, ulcerative ]enterocolitis
Enterocolitis is an inflammation of the digestive tract, involving enteritis of the small intestine and colitis of the colon. It may be caused by various infections, with bacteria, viruses, fungi, parasites, or other causes. Common clinical mani ...
, difficulty swallowing
Dysphagia is difficulty in swallowing. Although classified under " symptoms and signs" in ICD-10, in some contexts it is classified as a condition in its own right.
It may be a sensation that suggests difficulty in the passage of solids or li ...
, angiooedema, pneumonitis
Pneumonitis describes general inflammation of lung tissue. Possible causative agents include radiation therapy of the chest, exposure to medications used during chemo-therapy, the inhalation of debris (e.g., animal dander), aspiration, herbicide ...
, pulmonary fibrosis
Pulmonary fibrosis is a condition in which the lungs become scarred over time. Symptoms include shortness of breath, a dry cough, feeling tired, weight loss, and nail clubbing. Complications may include pulmonary hypertension, respiratory ...
, hepatotoxicity, cholestatic jaundice, peripheral neuropathy
Peripheral neuropathy, often shortened to neuropathy, refers to damage or disease affecting the nerves. Damage to nerves may impair sensation, movement, gland function, and/or organ function depending on which nerve fibers are affected. Neuropa ...
, Guillain–Barré syndrome
Guillain–Barré syndrome (GBS) is a rapid-onset Paralysis, muscle weakness caused by the immune system damaging the peripheral nervous system. Typically, both sides of the body are involved, and the initial symptoms are changes in sensation ...
, encephalopathy
Encephalopathy (; ) means any disorder or disease of the brain, especially chronic degenerative conditions. In modern usage, encephalopathy does not refer to a single disease, but rather to a syndrome of overall brain dysfunction; this syndrome ...
, encephalitis
Encephalitis is inflammation of the Human brain, brain. The severity can be variable with symptoms including reduction or alteration in consciousness, aphasia, headache, fever, confusion, a stiff neck, and vomiting. Complications may include se ...
and photosensitivity Photosensitivity is the amount to which an object reacts upon receiving photons, especially visible light. In medicine, the term is principally used for abnormal reactions of the skin, and two types are distinguished, photoallergy and phototoxicit ...
.[
]
Pharmacology
Its precise mechanism of action is unknown but is known that it inhibits the synthesis of prostaglandins
Prostaglandins (PG) are a group of physiologically active lipid compounds called eicosanoids that have diverse hormone-like effects in animals. Prostaglandins have been found in almost every tissue in humans and other animals. They are derive ...
.[ It also modulates ]phagocytic cells
Phagocytes are cells that protect the body by ingesting harmful foreign particles, bacteria, and dead or dying cells. Their name comes from the Greek ', "to eat" or "devour", and "-cyte", the suffix in biology denoting "cell", from the Greek ...
and inhibits class II major histocompatibility complex
The major histocompatibility complex (MHC) is a large Locus (genetics), locus on vertebrate DNA containing a set of closely linked polymorphic genes that code for Cell (biology), cell surface proteins essential for the adaptive immune system. The ...
-peptide interactions.[ It is also known that it inhibits the following enzymes:]
* Acid phosphatase
Acid phosphatase (EC 3.1.3.2, systematic name ''phosphate-monoester phosphohydrolase (acid optimum)'') is an enzyme that frees attached phosphoryl groups from other molecules during digestion. It can be further classified as a phosphoric monoeste ...
* Beta-glucuronidase
* Elastase
In molecular biology, elastase is an enzyme from the class of proteases (peptidases) that break down proteins, specifically one that can break down elastin. In other words, the name only refers to the substrate specificity (i.e. what proteins i ...
* Cathepsin G
* Thrombin
Prothrombin (coagulation factor II) is encoded in the human by the F2-gene. It is proteolytically cleaved during the clotting process by the prothrombinase enzyme complex to form thrombin.
Thrombin (Factor IIa) (, fibrose, thrombase, throm ...
* Microsomal prostaglandin E synthase-1
History of use
Reports of favorable use of the compound were published in France in 1929 by Jacques Forestier. The use of gold salts was then a controversial treatment and was not immediately accepted by the international community. Success was found in the treatment of Raoul Dufy
Raoul Dufy (; 3 June 1877 – 23 March 1953) was a French painter associated with the Fauvist movement. He gained recognition for his vibrant and decorative style, which became popular in various forms, such as textile designs, and public build ...
's joint pain by the use of gold salts in 1940; "(the treatment) brought in a few weeks such a spectacular sense of healing, that Dufy ... boasted of again having the ability to catch a tram on the move."
Along with aurothioglucose, sodium aurothiomalate was discontinued in the United States, leaving auranofin as the only gold salt remaining on the U.S. market.
References
{{DEFAULTSORT:Sodium Aurothiomalate
Gold(I) compounds
Antirheumatic products
Metal-containing drugs
Organic sodium salts
Thiolates
Gold–sulfur compounds
French inventions
Disease-modifying antirheumatic drugs