Peringatan Keamanan

Overdose as a result of too rapid increases in dosing with aurothioglucose will be manifested by rapid appearance of toxic reactions, including those that are particular to renal damage, like hematuria and proteinuria, while hematologic effects include thrombocytopenia and granulocytopenia ^L1937.

Other toxic effects, including fever, nausea, vomiting, diarrhea, and various skin disorders like papulovesicular lesions, urticaria, and exfoliative dermatitis, each of which are typically combined with severe pruritus can also develop ^L1937.

The intramuscular TDLo for males is reported to be approximately 3.357 mg/kg when considering sense organs and special senses like eye vision and about 5.5 mg/kg for affects on the lungs, thorax, or respiration ^L1940. For women, the intramuscular TDLo for effects on the liver, gastrointestinal tract, and cholestatic jaundice is between 2.6-2.7 mg/kg while the value for effects on the kidney, ureter, bladder, and acute renal failure, acute tubular necrosis, and other changes in urine composition is about 14.402 mg/kg ^L1940.

Aurothioglucose

DB09121

small molecule approved withdrawn

Deskripsi

Aurothioglucose, also known as gold thioglucose, was formerly used to treat rheumatoid arthritis.

Contemporary research on the effect of gold salts treatment began in 1935, primarily to reduce inflammation and to slow disease progression in patients with rheumatoid arthritis ^A32326. The use of gold compounds has decreased since the 1980s owing to numerous side effects, limited efficacy, and slow onset of action. Many if not most gold compounds that were indicated for rheumatoid arthritis therapy have since been replaced with the use of various current disease modifying anti-rheumatic drugs (DMARDs) like methotrexate and others, which are far more effective.

Struktur Molekul 2D

Berat 392.18

Wujud liquid

Peta Jejaring Molekuler

Obat Target Gen Interaksi Enzim Transporter Carrier

Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

1. Pendahuluan & Konsep

Fitur visualisasi ini dikembangkan menggunakan pendekatan Graph Theory untuk memetakan hubungan polifarmasi dan molekuler. Entitas (Obat, Target, Gen) direpresentasikan sebagai Simpul (Nodes), sedangkan hubungan biologisnya sebagai Sisi (Edges).

2. Sumber Data (Validasi)

Data Obat: Diekstraksi dari elemen drugbank-id dan name pada skema XML DrugBank.
Target Protein: Diambil dari elemen targets/target yang memuat polipeptida sasaran.
Genetik: Disinkronisasi dari sub-elemen gene-name dan varian snp-effects.
Genetik: Jumlah titik node dibatasi pada maksimal 10 (Slice=10) interaksi untuk menghindari tumpukan data.

3. Algoritma Visualisasi

Tata letak grafik menggunakan algoritma Force-Directed Graph (Barnes-Hut). Model fisika ini menerapkan gaya tolak-menolak antar simpul (Gravitasi: -3000) agar tidak tumpang tindih, serta gaya pegas (Spring: 0.04) pada garis penghubung untuk fleksibilitas interaksi.

4. Legenda Visual

Obat Utama (Pusat Analisis)

Target Protein (Mekanisme)

Gen (Faktor Genetik)

Metode ini mendukung analisis Precision Medicine dan evaluasi risiko Drug-Drug Interaction (DDI).

Profil Farmakokinetik

Waktu Paruh (Half-Life) The biological half-life of gold salts (like aurothioglucose) following a single 50 mg dose demonstrates a biological half-life of about 3-27 days, where the half-life seemingly increases with increased number of doses [T147]. Following successive weekly doses, the half-life increases and may become 14-40 days after the third dose and up to 168 days after the eleventh weekly dose [L1925].

Volume Distribusi Readily accessible data regarding the volume of distribution of aurothioglucose is not available.

Klirens (Clearance) When a standard weekly treatment schedule of aurothioglucose administrations is followed, about 40% of the given dose is excreted each week, while the remainder is excreted over a longer period [L1937].

Absorpsi

In general, aurothioglucose is administered via intramuscular injection - preferably intragluteally ^L1947 - after which the resultant absorption is typically slow and erratic T149. Gold is absorbed from injection sites, reaching peak concentration in blood in about 4 to 6 hours ^L1937. After a single intramuscular injection of 50 mg of aurothioglucose suspension in two subjects, peak serum levels were observed at approximately 235 g/dL and 450 g/dL ^L1937. Storage of gold in human tissues depends upon organ mass as well as the concentration of gold ^L1937.Subsequently, tissues having the highest gold levels (w/w) may not necessarily have the largest total amounts of gold ^L1937. The highest concentrations of gold are generally found in the lymph nodes, adrenal glands, liver, kidneys, bone marrow, and spleen ^L1937. Relatively small concentrations are actually found in the articular structures ^L1937. In particular, following the administration of aurothioglucose doses, about 85% of the resultant plasma gold will be stored in the major bodily gold depots, which in decreasing order of total gold content are, the lymph nodes, bone marrow, liver, skin, and bone L1937, L1947.

Metabolisme

Although the exact metabolic fate of aurothioglucose is not formally understood, the principal gold species that can be found in the urine and blood of a patient following the administration of the drug is Au(CN)2- ^L1925.

Rute Eliminasi

Following a single intramuscular injection of 50 mg aurothioglucose in each of two patients, one study determined that approximately 70% of the agent is eliminated in the urine and 30% in the faeces ^L1925. In general, excretion is primarily in the urine T147.

Interaksi Obat

727 Data

Cyclosporine	Cyclosporine may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Icosapent	Icosapent may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Cefotiam	Cefotiam may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Mesalazine	Mesalazine may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Cefmenoxime	Cefmenoxime may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Cefmetazole	Cefmetazole may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Pamidronic acid	Pamidronic acid may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Tenofovir disoproxil	Tenofovir disoproxil may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Indomethacin	Indomethacin may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Cidofovir	Cidofovir may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Cefpiramide	Cefpiramide may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Ceftazidime	Ceftazidime may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Loracarbef	Loracarbef may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Cefalotin	Cefalotin may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Nabumetone	Nabumetone may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Ketorolac	Ketorolac may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Tenoxicam	Tenoxicam may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Celecoxib	Celecoxib may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Cefotaxime	Cefotaxime may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Tolmetin	Tolmetin may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Foscarnet	Foscarnet may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Rofecoxib	Rofecoxib may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Piroxicam	Piroxicam may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Methotrexate	Methotrexate may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Cephalexin	Cephalexin may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Fenoprofen	Fenoprofen may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Valaciclovir	Valaciclovir may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Valdecoxib	Valdecoxib may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Diclofenac	Diclofenac may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Sulindac	Sulindac may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Bacitracin	Bacitracin may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Amphotericin B	Amphotericin B may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Cephaloglycin	Cephaloglycin may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Flurbiprofen	Flurbiprofen may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Adefovir dipivoxil	Adefovir dipivoxil may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Pentamidine	Pentamidine may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Etodolac	Etodolac may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Mefenamic acid	Mefenamic acid may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Acyclovir	Acyclovir may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Naproxen	Naproxen may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Sulfasalazine	Sulfasalazine may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Phenylbutazone	Phenylbutazone may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Meloxicam	Meloxicam may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Carprofen	Carprofen may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Cefaclor	Cefaclor may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Diflunisal	Diflunisal may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Tacrolimus	Tacrolimus may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Ceforanide	Ceforanide may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Salicylic acid	Salicylic acid may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Meclofenamic acid	Meclofenamic acid may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Acetylsalicylic acid	Acetylsalicylic acid may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Carboplatin	Carboplatin may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Oxaprozin	Oxaprozin may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Ketoprofen	Ketoprofen may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Balsalazide	Balsalazide may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Ibuprofen	Ibuprofen may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Cefditoren	Cefditoren may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Atazanavir	Atazanavir may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Colistimethate	Colistimethate may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Cefuroxime	Cefuroxime may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Cefapirin	Cefapirin may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Cefadroxil	Cefadroxil may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Cefprozil	Cefprozil may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Ceftriaxone	Ceftriaxone may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Olsalazine	Olsalazine may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Lumiracoxib	Lumiracoxib may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Cefamandole	Cefamandole may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Cefazolin	Cefazolin may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Cefonicid	Cefonicid may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Cefoperazone	Cefoperazone may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Cefotetan	Cefotetan may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Cefoxitin	Cefoxitin may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Ceftizoxime	Ceftizoxime may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Cefradine	Cefradine may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Magnesium salicylate	Magnesium salicylate may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Salsalate	Salsalate may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Choline magnesium trisalicylate	Choline magnesium trisalicylate may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Cefepime	Cefepime may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Cefacetrile	Cefacetrile may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Ceftibuten	Ceftibuten may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Cefpodoxime	Cefpodoxime may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Antrafenine	Antrafenine may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Aminophenazone	Aminophenazone may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Antipyrine	Antipyrine may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Tiaprofenic acid	Tiaprofenic acid may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Lopinavir	Lopinavir may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Etoricoxib	Etoricoxib may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Hydrolyzed Cephalothin	Hydrolyzed Cephalothin may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Cephalothin Group	Cephalothin Group may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Oxyphenbutazone	Oxyphenbutazone may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Latamoxef	Latamoxef may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Nimesulide	Nimesulide may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Benoxaprofen	Benoxaprofen may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Metamizole	Metamizole may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Zomepirac	Zomepirac may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Ceftobiprole	Ceftobiprole may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Cimicoxib	Cimicoxib may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Ceftaroline fosamil	Ceftaroline fosamil may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Lornoxicam	Lornoxicam may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.
Aceclofenac	Aceclofenac may decrease the excretion rate of Aurothioglucose which could result in a higher serum level.

Target Protein

Adenylate cyclase type 1 ADCY1

Adenylate cyclase type 2 ADCY2

Adenylate cyclase type 5 ADCY5

Referensi & Sumber

Artikel (PubMed)

PMID: 25048575
Botz B, Bolcskei K, Kereskai L, Kovacs M, Nemeth T, Szigeti K, Horvath I, Mathe D, Kovacs N, Hashimoto H, Reglodi D, Szolcsanyi J, Pinter E, Mocsai A, Helyes Z: Differential regulatory role of pituitary adenylate cyclase-activating polypeptide in the serum-transfer arthritis model. Arthritis Rheumatol. 2014 Oct;66(10):2739-50. doi: 10.1002/art.38772.
PMID: 11749494
Shaw III CF: Gold-based therapeutic agents. Chem Rev. 1999 Sep 8;99(9):2589-600.

Textbook

ISBN: 9780323511216
Arthur H. Jeske (2017). Mosby's Dental Drug Reference - E-Book (pp. 120-122). Elsevier Health Sciences.
ISBN: 9781437710359
Ronald I. Shorr (2007). Drugs for the Geriatric Patient . Elsevier Health Sciences.

Link

Contoh Produk & Brand

Produk: 1 • International brands: 5

Produk

Solganal Inj 50mg/ml

Suspension • 50 mg / mL • Intramuscular • Canada • Approved

International Brands

Brenol
Oronol
Romosol
Solganal
Solganal B

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.