Sodium aurothiomalate (
INN
Inns are generally establishments or buildings where travelers can seek lodging, and usually, food and drink. Inns are typically located in the country or along a highway; before the advent of motorized transportation they also provided accommo ...
, known in the
United States
The United States of America (U.S.A. or USA), commonly known as the United States (U.S. or US) or America, is a country primarily located in North America. It consists of 50 states, a federal district, five major unincorporated territorie ...
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
Auranofin is a gold salt classified by the World Health Organization as an antirheumatic agent. It has the brand name Ridaura.
Use
Auranofin is used to treat rheumatoid arthritis. It improves arthritis symptoms including painful or tender and ...
, 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 joints. It typically results in warm, swollen, and painful joints. Pain and stiffness often worsen following rest. Most commonly, the wrist and hands are involv ...
although it has also proven itself effective in treating
tuberculosis
Tuberculosis (TB) is an infectious disease usually caused by '' Mycobacterium tuberculosis'' (MTB) bacteria. Tuberculosis generally affects the lungs, but it can also affect other parts of the body. Most infections show no symptoms, in ...
.
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 t ...
,
mouth swelling, nausea, vomiting and taste disturbance), vasomotor (mostly flushing, fainting, dizziness, sweating, weakness, palpitations,
shortness of breath
Shortness of breath (SOB), also medically 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 disc ...
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, is inflammation of the conjunctiva, outermost layer of the white part of the eye and the inner surface of the eyelid. It makes the eye appear pink or reddish. Pain, burning, scratchiness, or itchiness may ...
, blood dyscrasias, kidney damage,
joint pain
Arthralgia (from Greek ''arthro-'', joint + ''-algos'', pain) literally means ''joint pain''. Specifically, arthralgia is a symptom of injury, infection, illness (in particular arthritis), or an allergic reaction to medication.
According to MeSH, ...
,
muscle aches/pains and liver dysfunction are also common.
Less commonly, it can cause GI bleeds, dry mucous membranes and
gingivitis
Gingivitis is a non-destructive disease that causes inflammation of the gums. The most common form of gingivitis, and the most common form of periodontal disease overall, is in response to bacterial biofilms (also called plaque) that is attached ...
.
[ Rarely it can cause: ]aplastic anaemia
Aplastic anemia is a cancer in which the body fails to make blood cells in sufficient numbers. Blood cells are produced in the bone marrow by stem cells that reside there. Aplastic anemia causes a deficiency of all blood cell types: red blood c ...
, ulcerative enterocolitis, 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 liqui ...
, angiooedema
Angioedema is an area of swelling ( edema) of the lower layer of skin and tissue just under the skin or mucous membranes. The swelling may occur in the face, tongue, larynx, abdomen, or arms and legs. Often it is associated with hives, which a ...
, 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 failu ...
, hepatotoxicity, cholestatic jaundice
Jaundice, also known as icterus, is a yellowish or greenish pigmentation of the skin and sclera due to high bilirubin levels. Jaundice in adults is typically a sign indicating the presence of underlying diseases involving abnormal heme metab ...
, peripheral neuropathy
Peripheral neuropathy, often shortened to neuropathy, is a general term describing disease affecting the peripheral nerves, meaning nerves beyond the brain and spinal cord. Damage to peripheral nerves may impair sensation, movement, gland, or or ...
, Guillain–Barré syndrome
Guillain–Barré syndrome (GBS) is a rapid-onset 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 or pain often ...
, encephalopathy
Encephalopathy (; from grc, ἐνκέφαλος "brain" + πάθος "suffering") means any disorder or disease of the brain, especially chronic degenerative conditions. In modern usage, encephalopathy does not refer to a single disease, but r ...
, encephalitis
Encephalitis is inflammation of the brain. The severity can be variable with symptoms including reduction or alteration in consciousness, headache, fever, confusion, a stiff neck, and vomiting. Complications may include seizures, hallucinations, ...
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 phototoxicity. ...
.[
]
Pharmacology
Its precise mechanism of action is unknown but is known that it inhibits the synthesis of prostaglandins
The prostaglandins (PG) are a group of physiologically active lipid compounds called eicosanoids having 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 on vertebrate DNA containing a set of closely linked polymorphic genes that code for cell surface proteins essential for the adaptive immune system. These cell surface proteins are calle ...
-peptide interactions.[ It is also known that it inhibits the following enzymes:]
* Acid phosphatase
* Beta-glucuronidase
* Elastase
In molecular biology, elastase is an enzyme from the class of ''proteases (peptidases)'' that break down proteins. In particular, it is a serine protease.
Forms and classification
Eight human genes exist for elastase:
Some bacteria (includin ...
* Cathepsin G
Cathepsin G is a protein that in humans is encoded by the ''CTSG'' gene. It is one of the three serine proteases of the chymotrypsin family that are stored in the azurophil granules, and also a member of the peptidase S1 protein family. Cathepsin ...
* Thrombin
Thrombin (, ''fibrinogenase'', ''thrombase'', ''thrombofort'', ''topical'', ''thrombin-C'', ''tropostasin'', ''activated blood-coagulation factor II'', ''blood-coagulation factor IIa'', ''factor IIa'', ''E thrombin'', ''beta-thrombin'', ''gamma- ...
* Microsomal prostaglandin E synthase-1
Microsomal prostaglandin E synthase-1 (mPGES-1) or Prostaglandin E synthase is an enzyme that in humans is encoded by the ''PTGES'' gene.
The protein encoded by this gene is a glutathione-dependent prostaglandin E synthase. The expression of this ...
History of use
Reports of favorable use of the compound were published in France in 1929 by Jacques Forestier
Jacques Forestier (27 July 1890, Aix-les-Bains – 17 March 1978) was a French internist who was a pioneer in the field of rheumatology.
Forestier studied medicine in Paris, later working at Hôpital Cochin, where he became interested in rheumat ...
. 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 Fauvism, Fauvist painter. He developed a colorful, decorative style that became fashionable for designs of ceramic art, ceramics and textile as well as decorative schemes for public bu ...
'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."
It was recently discontinued from the US market along with aurothioglucose
Aurothioglucose, also known as gold thioglucose, is a chemical compound with the formula AuSC6H11O5. This derivative of the sugar glucose was formerly used to treat rheumatoid arthritis.
History
Throughout history, gold was used to cure diseases ...
leaving only auranofin
Auranofin is a gold salt classified by the World Health Organization as an antirheumatic agent. It has the brand name Ridaura.
Use
Auranofin is used to treat rheumatoid arthritis. It improves arthritis symptoms including painful or tender and ...
as the only gold salt on the US 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