| 词条 | Sodium aurothiomalate |
| 释义 |
| IUPAC_name = Sodium 2-(auriosulfanyl)-3-carboxypropanoate | image=Sodium aurothiomalate.svg | width=200px | verifiedrevid = 462079279 | tradename = Myocrisin | Drugs.com = {{drugs.com|mtm|gold-sodium-thiomalate}} | licence_US = Gold_sodium_thiomalate | pregnancy_AU = B2 | pregnancy_US = C | legal_AU = S4 | legal_CA = Rx-only | legal_UK = POM | legal_US = Discontinued | routes_of_administration = Intramuscular | protein_bound = High[1] | elimination_half-life = 6-25 days[1] | excretion = Urine (60-90%), faeces (10-40%)[1] | CAS_number = 12244-57-4 | PubChem = 16760302 | ChemSpiderID = 7827788 | ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}} | ChEBI_Ref = {{ebicite|correct|EBI}} | ChEBI = 35863 | ATC_prefix = M01 | ATC_suffix = CB01 | StdInChI_Ref = {{stdinchicite|correct|chemspider}} | StdInChI = 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 | StdInChIKey_Ref = {{stdinchicite|correct|chemspider}} | StdInChIKey = LTEMOXGFFHXNNS-UHFFFAOYSA-L | smiles = [Au+].[Na+].[O-]C(=O)C([S-])CC(=O)O | UNII_Ref = {{fdacite|changed|FDA}} | UNII = E4768ZY6GM | chemical_formula = | C=4 | H=4 | Au=1 | Na=1 | O=4 | S=1 | molecular_weight = 367.939350590 }}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 usesIt is primarily given once or twice weekly by intramuscular injection for moderate-severe rheumatoid arthritis although it has also proven itself effective in treating tuberculosis.[5] Adverse effectsIts 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–Barré syndrome, encephalopathy, encephalitis and photosensitivity.[6] PharmacologyIts 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]
History of useReports of favorable use of the compound were published in France in 1929 by Jacques Forestier.[9] 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." [10] It was recently discontinued from the US market along with aurothioglucose leaving only auranofin as the only gold salt on the US market References1. ^1 2 {{cite web|title=aurothiomalate, sodium, Myochrysine (gold sodium thiomalate) dosing, indications, interactions, adverse effects, and more|work=Medscape Reference|publisher=WebMD|accessdate=13 March 2014|url=http://reference.medscape.com/drug/aurothiomalate-sodium-myochrysine-gold-sodium-thiomalate-343218#showall}} {{Antirheumatic products}}{{Gold compounds}}{{DEFAULTSORT:Sodium Aurothiomalate}}2. ^{{Cite journal | doi = 10.1093/rheumatology/37.9.992 | last1 = Jessop | first1 = J. D. | last2 = O'Sullivan | first2 = M. M. | last3 = Lewis | first3 = P. A. | last4 = Williams | first4 = L. A. | last5 = Camilleri | first5 = J. P. | last6 = Plant | first6 = M. J. | last7 = Coles | first7 = E. C. | title = A long-term five-year randomized controlled trial of hydroxychloroquine, sodium aurothiomalate, auranofin and penicillamine in the treatment of patients with rheumatoid arthritis | journal = British Journal of Rheumatology | volume = 37 | issue = 9 | pages = 992–1002 | year = 1998 | pmid = 9783766}} 3. ^{{Cite journal | last1 = Iqbal | first1 = M. S. | last2 = Saeed | first2 = M. | last3 = Taqi | first3 = S. G. | doi = 10.1007/s12011-008-8184-x | title = Erythrocyte Membrane Gold Levels After Treatment with Auranofin and Sodium Aurothiomalate | journal = Biological Trace Element Research | volume = 126 | issue = 1–3 | pages = 56–64 | year = 2008 | pmid = 18649049 | pmc = }} 4. ^1 2 3 {{cite journal|last=Kean|first=WF|author2=Kean, IRL |title=Clinical pharmacology of gold|journal=Inflammopharmacology|date=4 June 2008|volume=16|issue=3|pages=112–125|doi=10.1007/s10787-007-0021-x|pmid=18523733}} 5. ^{{cite journal|last=Benedek|first=TG|title=The history of gold therapy for tuberculosis.|journal=Journal of the History of Medicine and Allied Sciences|date=January 2004|volume=59|issue=1|pages=50–89|doi=10.1093/jhmas/jrg042|pmid=15011812}} 6. ^1 2 {{cite book | editor = Rossi, S | isbn = 978-0-9805790-9-3 | title = Australian Medicines Handbook | place = Adelaide | publisher = The Australian Medicines Handbook Unit Trust | year = 2013 | edition = 2013 }} 7. ^{{cite journal|last=Berners-Price|first=SJ|author2=Filipovska, A |title=Gold compounds as therapeutic agents for human diseases.|journal=Metallomics|date=September 2011|volume=3|issue=9|pages=863–73|doi=10.1039/c1mt00062d|pmid=21755088}} 8. ^{{cite journal | doi = 10.3109/03009742.2014.927917| pmid = 25314295| title = Aurothiomalate inhibits the expression of mPGES-1 in primary human chondrocytes| journal = Scandinavian Journal of Rheumatology| volume = 44| issue = 1| pages = 74–9| year = 2014| last1 = Tuure| first1 = L| last2 = Hämäläinen| first2 = M| last3 = Moilanen| first3 = T| last4 = Moilanen| first4 = E}} 9. ^{{cite journal|last=Freyberg|first=R.H.|title=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 |journal=J Clin Invest|date=July 1941|volume=20|issue=4|pages=401–412|doi=10.1172/jci101235|pmc=435072 |display-authors=etal|pmid=16694848}} 10. ^{{cite journal |last=Lamboley |first=Claude |date=December 6, 2010 |title=Deux rhumatisants au soleil du Midi : Renoir et Dufy |trans-title=Two rheumatic in the Midi sun: Renoir and Dufy |url=http://www.ac-sciences-lettres-montpellier.fr/academie_edition/fichiers_conf/LAMBOLEY-2010.pdf |language= French|journal=Académie des Sciences et Lettres de Montpellier |location=Montpellier |publisher= |access-date=July 7, 2015 }} 6 : Gold(Ⅰ) compounds|Antirheumatic products|Metal-containing drugs|Organic sodium salts|Thiolates|Gold-sulfur compounds |
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