Peringatan Keamanan

The effects in humans of large doses of sodium thiosulfate have not been thoroughly studied. Sodium thiosulfate administered orally (3 g per day) for 1-2 weeks resulted in reductions in room air arterial oxygen saturation to as low as 75%. One week after discontinuation, subjects returned to baseline oxygen saturations. A single dose of 20 mL of 10% sodium thiosulfate administered intravenously did not have an effect on oxygen saturation.L43332

In rats, the oral LD50 of sodium thiosulfate pentahydrate is 5000 mg/kg.L43327 The carcinogenic activity of sodium thiosulfate has not been evaluated. An in vitro bacterial reverse mutation assay showed that sodium thiosulfate was not mutagenic in the absence nor presence of metabolic activation.L43337

Thiosulfuric acid

DB09499

small molecule approved investigational

Deskripsi

Thiosulfuric acid is available in its salt forms sodium thiosulfate and sodium thiosulfate pentahydrate. Sodium thiosulfate is part of the World Health Organization’s list of essential medicines, and it has a variety of industrial uses, including food preservative, water de-chlorinator and paper pulp bleaching agent.A252827 Sodium thiosulfate is rapidly degraded in the stomach; therefore, it is normally administered through other routes, such as intravenous or topical.A252827 Sodium thiosulfate is approved for the treatment of acute cyanide poisoningL310,L43332,A252832 and it is frequently used in conjunction with sodium nitrite (a salt form of nitrous acid). Sodium thiosulfate is also used to reduce the risk of ototoxicity associated with cisplatin.L43337 When administered 6 hours after cisplatin chemotherapy, Sodium thiosulfate leads to a lower incidence of cisplatin-induced hearing loss among children without affecting its effectiveness.A252837,A252842

Struktur Molekul 2D

Berat 114.144
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The half-life of thiosulfate administered intravenously (1 g sodium thiosulfate) was approximately 20 minutes. However, higher doses may increase this value. In healthy men given 150 mg/kg of sodium thiosulfate, the elimination half-life was 182 minutes.[L43332]
Volume Distribusi Thiosulfate has a mean volume of distribution of 0.23 L/kg.[L43337]
Klirens (Clearance) In patients with fully developed renal function (1 year old approximately), the mean total clearance of thiosulfate is 2.2 mL/min/kg.[L43337]

Absorpsi

Sodium thiosulfate taken orally is not systemically absorbed. Most of the thiosulfate is oxidized to sulfate or is incorporated into endogenous sulphur compounds; a small proportion is excreted through the kidneys.L43332 In pediatric patients given the recommended intravenous dose of sodium thiosulfate, the Cmax of thiosulfate was 13 ± 1.2 mM, and increased proportionally to dose over the range of 4 g/m2 to 20 g/m2. Thiosulfate accumulation is not expected following the intravenous administration of sodium thiosulfate on 2 consecutive days.L43337

Metabolisme

Thiosulfate sulfur transferase and thiosulfate reductase metabolize thiosulfate to form sulfite, which is oxidized to sulfate.L43337

Rute Eliminasi

Approximately 20-50% of exogenously administered sodium thiosulfate is eliminated by the kidneys.L43332,L43337 More than 95% of the thiosulfate eliminated in urine is excreted within the first 4 hours after administration.L43337 When used as an antidote to cyanide poisoning, sodium thiosulfate is eliminated as thiocyanate, a relatively nontoxic compound. Thiocyanate is also excreted in urine at a rate inversely proportional to creatinine clearance.L43332

Interaksi Obat

75 Data
Technetium Tc-99m oxidronate Thiosulfuric acid may decrease effectiveness of Technetium Tc-99m oxidronate as a diagnostic agent.
Nicotine The metabolism of Nicotine can be increased when combined with Thiosulfuric acid.
Tramadol The metabolism of Tramadol can be increased when combined with Thiosulfuric acid.
Nevirapine The metabolism of Nevirapine can be increased when combined with Thiosulfuric acid.
Phenytoin The metabolism of Phenytoin can be increased when combined with Thiosulfuric acid.
Valproic acid The metabolism of Valproic acid can be increased when combined with Thiosulfuric acid.
Amitriptyline The metabolism of Amitriptyline can be increased when combined with Thiosulfuric acid.
Methadone The metabolism of Methadone can be increased when combined with Thiosulfuric acid.
Clobazam The metabolism of Clobazam can be increased when combined with Thiosulfuric acid.
Mexiletine The metabolism of Mexiletine can be increased when combined with Thiosulfuric acid.
Meperidine The metabolism of Meperidine can be increased when combined with Thiosulfuric acid.
Imipramine The metabolism of Imipramine can be increased when combined with Thiosulfuric acid.
Fluoxetine The metabolism of Fluoxetine can be increased when combined with Thiosulfuric acid.
Cyclophosphamide The metabolism of Cyclophosphamide can be increased when combined with Thiosulfuric acid.
Mephenytoin The metabolism of Mephenytoin can be increased when combined with Thiosulfuric acid.
Cinnarizine The metabolism of Cinnarizine can be increased when combined with Thiosulfuric acid.
Fenfluramine The metabolism of Fenfluramine can be increased when combined with Thiosulfuric acid.
Diclofenac The metabolism of Diclofenac can be increased when combined with Thiosulfuric acid.
Cisapride The metabolism of Cisapride can be increased when combined with Thiosulfuric acid.
Efavirenz The metabolism of Efavirenz can be increased when combined with Thiosulfuric acid.
Tamoxifen The metabolism of Tamoxifen can be increased when combined with Thiosulfuric acid.
Apomorphine The metabolism of Apomorphine can be increased when combined with Thiosulfuric acid.
Epinastine The metabolism of Epinastine can be increased when combined with Thiosulfuric acid.
Isoflurane The metabolism of Isoflurane can be increased when combined with Thiosulfuric acid.
Clopidogrel The metabolism of Clopidogrel can be increased when combined with Thiosulfuric acid.
Irinotecan The metabolism of Irinotecan can be increased when combined with Thiosulfuric acid.
Propofol The metabolism of Propofol can be increased when combined with Thiosulfuric acid.
Brompheniramine The metabolism of Brompheniramine can be increased when combined with Thiosulfuric acid.
Methylphenobarbital The metabolism of Methylphenobarbital can be increased when combined with Thiosulfuric acid.
Benzphetamine The metabolism of Benzphetamine can be increased when combined with Thiosulfuric acid.
Hydrocodone The metabolism of Hydrocodone can be increased when combined with Thiosulfuric acid.
Norgestimate The metabolism of Norgestimate can be increased when combined with Thiosulfuric acid.
Methoxyflurane The metabolism of Methoxyflurane can be increased when combined with Thiosulfuric acid.
Selegiline The metabolism of Selegiline can be increased when combined with Thiosulfuric acid.
Promethazine The metabolism of Promethazine can be increased when combined with Thiosulfuric acid.
Perhexiline The metabolism of Perhexiline can be increased when combined with Thiosulfuric acid.
Benzocaine The metabolism of Benzocaine can be increased when combined with Thiosulfuric acid.
Bupropion The metabolism of Bupropion can be increased when combined with Thiosulfuric acid.
Halothane The metabolism of Halothane can be increased when combined with Thiosulfuric acid.
Ifosfamide The metabolism of Ifosfamide can be increased when combined with Thiosulfuric acid.
Domperidone The metabolism of Domperidone can be increased when combined with Thiosulfuric acid.
Ketamine The metabolism of Ketamine can be increased when combined with Thiosulfuric acid.
Sevoflurane The metabolism of Sevoflurane can be increased when combined with Thiosulfuric acid.
Antipyrine The metabolism of Antipyrine can be increased when combined with Thiosulfuric acid.
Ethylmorphine The metabolism of Ethylmorphine can be increased when combined with Thiosulfuric acid.
Flunitrazepam The metabolism of Flunitrazepam can be increased when combined with Thiosulfuric acid.
Clotiazepam The metabolism of Clotiazepam can be increased when combined with Thiosulfuric acid.
Lorcaserin The metabolism of Lorcaserin can be increased when combined with Thiosulfuric acid.
Ospemifene The metabolism of Ospemifene can be increased when combined with Thiosulfuric acid.
Banoxantrone The metabolism of Banoxantrone can be increased when combined with Thiosulfuric acid.
Brivaracetam The metabolism of Brivaracetam can be increased when combined with Thiosulfuric acid.
Cenobamate The metabolism of Cenobamate can be increased when combined with Thiosulfuric acid.
Mianserin The metabolism of Mianserin can be increased when combined with Thiosulfuric acid.
Romidepsin The metabolism of Romidepsin can be increased when combined with Thiosulfuric acid.
Prasugrel The metabolism of Prasugrel can be increased when combined with Thiosulfuric acid.
Clomethiazole The metabolism of Clomethiazole can be increased when combined with Thiosulfuric acid.
Artemether The metabolism of Artemether can be increased when combined with Thiosulfuric acid.
Methyltestosterone The metabolism of Methyltestosterone can be increased when combined with Thiosulfuric acid.
Ketobemidone The metabolism of Ketobemidone can be increased when combined with Thiosulfuric acid.
Seratrodast The metabolism of Seratrodast can be increased when combined with Thiosulfuric acid.
Perampanel The metabolism of Perampanel can be increased when combined with Thiosulfuric acid.
Vortioxetine The metabolism of Vortioxetine can be increased when combined with Thiosulfuric acid.
Asunaprevir The metabolism of Asunaprevir can be increased when combined with Thiosulfuric acid.
Velpatasvir The metabolism of Velpatasvir can be increased when combined with Thiosulfuric acid.
Istradefylline The metabolism of Istradefylline can be increased when combined with Thiosulfuric acid.
Esketamine The metabolism of Esketamine can be increased when combined with Thiosulfuric acid.
Osilodrostat The metabolism of Osilodrostat can be increased when combined with Thiosulfuric acid.
Fexinidazole The metabolism of Fexinidazole can be increased when combined with Thiosulfuric acid.
Artemisinin The metabolism of Artemisinin can be increased when combined with Thiosulfuric acid.
Enasidenib The metabolism of Enasidenib can be increased when combined with Thiosulfuric acid.
Testosterone cypionate The metabolism of Testosterone cypionate can be increased when combined with Thiosulfuric acid.
Testosterone enanthate The metabolism of Testosterone enanthate can be increased when combined with Thiosulfuric acid.
Voxelotor The metabolism of Voxelotor can be increased when combined with Thiosulfuric acid.
Zanubrutinib The metabolism of Zanubrutinib can be increased when combined with Thiosulfuric acid.
Thalidomide The metabolism of Thalidomide can be increased when combined with Thiosulfuric acid.

Referensi & Sumber

Synthesis reference: Sherman, C., et al. (2016). Sodium thiosulfate-containing pharmaceutical compositions (U.S. Patent No. 2016/0235782 A1). U.S. Patent and Trademark Office. https://patentimages.storage.googleapis.com/0c/2a/58/edc43adab43077/US20160235782A1.pdf
Artikel (PubMed)
  • PMID: 34208631
    Zhang MY, Dugbartey GJ, Juriasingani S, Sener A: Hydrogen Sulfide Metabolite, Sodium Thiosulfate: Clinical Applications and Underlying Molecular Mechanisms. Int J Mol Sci. 2021 Jun 16;22(12). pii: ijms22126452. doi: 10.3390/ijms22126452.
  • PMID: 28041825
    Bebarta VS, Brittain M, Chan A, Garrett N, Yoon D, Burney T, Mukai D, Babin M, Pilz RB, Mahon SB, Brenner M, Boss GR: Sodium Nitrite and Sodium Thiosulfate Are Effective Against Acute Cyanide Poisoning When Administered by Intramuscular Injection. Ann Emerg Med. 2017 Jun;69(6):718-725.e4. doi: 10.1016/j.annemergmed.2016.09.034. Epub 2016 Dec 29.
  • PMID: 27914822
    Freyer DR, Chen L, Krailo MD, Knight K, Villaluna D, Bliss B, Pollock BH, Ramdas J, Lange B, Van Hoff D, VanSoelen ML, Wiernikowski J, Neuwelt EA, Sung L: Effects of sodium thiosulfate versus observation on development of cisplatin-induced hearing loss in children with cancer (ACCL0431): a multicentre, randomised, controlled, open-label, phase 3 trial. Lancet Oncol. 2017 Jan;18(1):63-74. doi: 10.1016/S1470-2045(16)30625-8. Epub 2016 Dec 1.
  • PMID: 29924955
    Brock PR, Maibach R, Childs M, Rajput K, Roebuck D, Sullivan MJ, Laithier V, Ronghe M, Dall'Igna P, Hiyama E, Brichard B, Skeen J, Mateos ME, Capra M, Rangaswami AA, Ansari M, Rechnitzer C, Veal GJ, Covezzoli A, Brugieres L, Perilongo G, Czauderna P, Morland B, Neuwelt EA: Sodium Thiosulfate for Protection from Cisplatin-Induced Hearing Loss. N Engl J Med. 2018 Jun 21;378(25):2376-2385. doi: 10.1056/NEJMoa1801109.

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