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Sodium aurothiomalate (INN, known in the United States as gold sodium thiomalate) is a gold compound that is used for its immunosuppressive anti-rheumatic effects.^[2]^[3] Along with an orally-administered gold salt, auranofin, it is one of only two gold compounds currently employed in modern medicine.^[4]

Medical uses

It is primarily given as a once or twice weekly by intramuscular injection for moderate-severe rheumatoid arthritis although it has also proven itself effective in treating tuberculosis.^[5]

Adverse effects

Its most common side effects are digestive (mostly dyspepsia, mouth swelling, nausea, vomiting and taste disturbance), vasomotor (mostly flushing, fainting, dizziness, sweating, weakness, palpitations, shortness of breath and blurred vision) or dermatologic (usually itchiness, rash, local irritation near to the injection site and hair loss) in nature, although conjunctivitis, blood dyscrasias, kidney damage, joint pain, muscle aches/pains and liver dysfunction are also common.^[6] Less commonly, it can cause GI bleeds, dry mucous membranes and gingivitis.^[6] Rarely it can cause: aplastic anaemia, ulcerative enterocolitis, difficulty swallowing, angiooedema, pneumonitis, pulmonary fibrosis, hepatotoxicity, cholestatic jaundice, peripheral neuropathy, Guillain-Barre syndrome, encephalopathy, encephalitis and photosensitivity.^[6]

Pharmacology

Its precise mechanism of action is unknown but is known that it inhibits the synthesis of prostaglandins.^[4] It also modulates phagocytic cells and inhibits Class II major histocompatibility complex-peptide interactions.^[4] It is also known that it inhibits the following enzymes:^[4]^[7]

Acid phosphatase
Beta-glucuronidase
Elastase
Cathepsin G
Thrombin

History of use

Reports of favorable use of the compound were published in France in 1929 by Jacques Forestier. ^[8] 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'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." ^[9]

In popular culture

The compound was used as a poison by a patient's wife in an episode of House ("Clueless", season 2 episode 15).

References

^ ^a ^b ^c "aurothiomalate, sodium, Myochrysine (gold sodium thiomalate) dosing, indications, interactions, adverse effects, and more". Medscape Reference. WebMD. Retrieved 13 March 2014.
^ Jessop, J. D.; O'Sullivan, M. M.; Lewis, P. A.; Williams, L. A.; Camilleri, J. P.; Plant, M. J.; Coles, E. C. (1998). "A long-term five-year randomized controlled trial of hydroxychloroquine, sodium aurothiomalate, auranofin and penicillamine in the treatment of patients with rheumatoid arthritis". British journal of rheumatology 37 (9): 992–1002. doi:10.1093/rheumatology/37.9.992. PMID 9783766.
^ Iqbal, M. S.; Saeed, M.; Taqi, S. G. (2008). "Erythrocyte Membrane Gold Levels After Treatment with Auranofin and Sodium Aurothiomalate". Biological Trace Element Research 126 (1–3): 56–64. doi:10.1007/s12011-008-8184-x. PMID 18649049.
^ ^a ^b ^c ^d Kean, WF; Kean, IRL (4 June 2008). "Clinical pharmacology of gold". Inflammopharmacology 16 (3): 112–125. doi:10.1007/s10787-007-0021-x. PMID 18523733.
^ Benedek, TG (January 2004). "The history of gold therapy for tuberculosis.". Journal of the History of Medicine and Allied Sciences 59 (1): 50–89. doi:10.1093/jhmas/jrg042. PMID 15011812.
^ ^a ^b ^c Rossi, S, ed. (2013). Australian Medicines Handbook (2013 ed.). Adelaide: The Australian Medicines Handbook Unit Trust. ISBN 978-0-9805790-9-3.
^ Berners-Price, SJ; Filipovska, A (September 2011). "Gold compounds as therapeutic agents for human diseases.". Metallomics 3 (9): 863–73. doi:10.1039/c1mt00062d. PMID 21755088.
^ FREYBERG, R.H.; et al. (July 1941). "METABOLISM, TOXICITY AND MANNER OF ACTION OF GOLD COMPOUNDS USED IN THE TREATMENT OF ARTHRITIS. I. HUMAN PLASMA AND SYNOVIAL FLUID CONCENTRATION AND URINARY EXCRETION OF GOLD DURING AND FOLLOWING TREATMENT WITH GOLD SODIUM THIOMALATE, GOLD SODIUM THIOSULFATE, AND COLLOIDAL GOLD SULFIDE". J Clin Invest 20 (4): 401–412. doi:10.1172/jci101235. PMC 435072. line feed character in |title= at position 60 (help)
^ Lamboley, Claude (December 6, 2010). "Deux rhumatisants au soleil du Midi : Renoir et Dufy" [Two rheumatic in the Midi sun: Renoir and Dufy] (PDF). Académie des Sciences et Lettres de Montpellier (in French) (Montpellier). Retrieved July 7, 2015.

UpToDate Contents

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1. スルファサラジンによる関節リウマチの治療 sulfasalazine in the treatment of rheumatoid arthritis

English Journal

Protein kinase C iota as a therapeutic target in alveolar rhabdomyosarcoma.

Kikuchi K, Soundararajan A, Zarzabal LA, Weems CR, Nelon LD, Hampton ST, Michalek JE, Rubin BP, Fields AP, Keller C.SourcePediatric Cancer Biology Program, Papé Family Pediatric Research Institute, Department of Pediatrics, Oregon Health & Science University, Portland, OR, USA.
Oncogene.Oncogene.2013 Jan 17;32(3):286-95. doi: 10.1038/onc.2012.46. Epub 2012 Feb 20.
Alveolar rhabdomyosarcoma is an aggressive pediatric cancer exhibiting skeletal-muscle differentiation. New therapeutic targets are required to improve the dismal prognosis for invasive or metastatic alveolar rhabdomyosarcoma. Protein kinase C iota (PKCι) has been shown to have an important role in
PMID 22349825

The biological activity of auranofin: implications for novel treatment of diseases.

Madeira JM, Gibson DL, Kean WF, Klegeris A.SourceDepartment of Biology, Irving K. Barber School of Arts and Sciences, University of British Columbia Okanagan Campus, Kelowna, BC, Canada.
Inflammopharmacology.Inflammopharmacology.2012 Dec;20(6):297-306. doi: 10.1007/s10787-012-0149-1. Epub 2012 Sep 11.
More than 30 years ago, auranofin was developed for the treatment of rheumatoid arthritis as a substitution for the injectable gold compounds aurothiomalate and aurothioglucose. Both the ease of oral administration over intramuscular injections and more potent anti-inflammatory effects in vitro mad
PMID 22965242

Effects of aurothiomalate and gold(III) complexes on spontaneous motility of isolated human oviduct.

Janković SM, Djeković A, Bugarčić Z, Janković SV, Lukić G, Folić M, Canović D.SourceDepartment of Pharmacology and Toxicology, Medical Faculty, University of Kragujevac, Ul. Svetozara Markovica 69, 34000, Kragujevac, Serbia. slobodan.jankovic@medf.kg.ac.rs
Biometals : an international journal on the role of metal ions in biology, biochemistry, and medicine.Biometals.2012 Oct;25(5):919-25. doi: 10.1007/s10534-012-9558-2. Epub 2012 May 19.
Organic gold complexes have different biological activity, depending on their potential for interactions with key functional molecules.The aim of this study was to investigate potential of several newly synthesized organic gold complexes to influence spontaneous motility of the Fallopian tubes.The e
PMID 22610585

Japanese Journal

関節リウマチの経過中に発症した急性リンパ性白血病の一例

日本臨床免疫学会会誌 = Japanese journal of clinical immunology 30(6), 461-466, 2007-12-31
NAID 10021242128

関節リウマチに多彩な腎組織像を呈した１例

日本腎臓学会誌 48(2), 67-73, 2006
NAID 130004170749

抗リウマチ薬のエスケープ現象の検討

藥學雜誌 125(3), 293-297, 2005-03-01
NAID 110003667407

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拡張検索	「sodium aurothiomalate」

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Sodium aurothiomalate
Systematic (IUPAC) name
	Sodium 2-(auriosulfanyl)-3-carboxypropanoate
Clinical data
Trade names	Myocrisin
AHFS/Drugs.com
License data	US FDA: Gold_sodium_thiomalate;
Pregnancy; category	AU: B2; US: C (Risk not ruled out); ;
Routes of; administration	Intramuscular
Legal status
Legal status	AU: S4 (Prescription only); CA: ℞-only; UK: POM (Prescription only); US: ℞-only;
Pharmacokinetic data
Protein binding	High
Biological half-life	6-25 days
Excretion	Urine (60-90%), faeces (10-40%)
Identifiers
CAS Number	12244-57-4
ATC code	M01CB01 (WHO)
PubChem	CID 16760302
ChemSpider	7827788
UNII	E4768ZY6GM
ChEBI	CHEBI:35863
Chemical data
Formula	C4H4AuNaO4S
Molar mass	367.939350590
	SMILES [Au+].[Na+].[O-]C(=O)C([S-])CC(=O)O ;
	InChI InChI=1S/C4H6O4S.Au.Na/c5-3(6)1-2(9)4(7)8;;/h2,9H,1H2,(H,5,6)(H,7,8);;/q;2*+1/p-2 ; Key:LTEMOXGFFHXNNS-UHFFFAOYSA-L ;
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