Peringatan Keamanan

The oral LD50 in rats is >4600-5000 mg/kg.L44752,L44793 It is over 7500 mg/kg for mice.L44793

Ursodeoxycholic acid (UDCA) is associated with rare hepatotoxicities, such as jaundice, worsening pre-existing liver diseases, and hepatitis.A256272,A256277 There have been no reports of accidental or intentional overdosage with UDCA. A single oral dose of UDCA at 1.5 g/kg was lethal in hamsters. Single oral doses of UDCA at 10 g/kg in mice and dogs and 5 g/kg in rats were not lethal. Symptoms of acute toxicity were salivation and vomiting in dogs, while ataxia, dyspnea, ptosis, agonal convulsions and coma were observed in hamsters.L44627

Ursodeoxycholic acid

DB01586

small molecule approved investigational

Deskripsi

Ursodeoxycholic acid (UDCA), also known as ursodiol, is a naturally-occurring bile acid that constitutes a minor fraction of the human bile acid pool.A256272,A256277 UDCA has been used to treat liver disease for decades: its first use in traditional medicine dates back more than a hundred years.A256267,A256463 UDCA was first characterized in the bile of the Chinese black bear and is formed by 7b-epimerization of chenodeoxycholic acid, which is a primary bile acid.A256272 Due to its hydrophilicity, UDCA is less toxic than cholic acid or chenodeoxycholic acid.A256272

UDCA was first approved by the FDA in 1987 for dissolution of gallstones and for primary biliary cirrhosis in 1996.A256272 UDCA works by replacing the hydrophobic or more toxic bile acids from the bile acid pool.A256272

Struktur Molekul 2D

Berat 392.572
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The estimated half-life ranges from 3.5 to 5.8 days.[A256277,A256678]
Volume Distribusi The volume of distribution of ursodeoxycholic acid (UDCA) has not been determined; however, it is expected to be small since UDCA is mostly distributed in the bile in the gallbladder and small intestines.[A256277,L44627]
Klirens (Clearance) -

Absorpsi

Normally, endogenous ursodeoxycholic acid constitutes a minor fraction (about 5%) of the total human bile acid pool. Following oral administration, the majority of ursodiol is absorbed by passive diffusion, and its absorption is incomplete. Once absorbed, ursodiol undergoes hepatic extraction to about 50% in the absence of liver disease. As the severity of liver disease increases, the extent of extraction decreases. During chronic administration of ursodiol, it becomes a major biliary and plasma bile acid. At a chronic dose of 13 to 15 mg/kg/day, ursodiol constitutes 30-50% of biliary and plasma bile acids.L44627

Metabolisme

Upon administration, ursodeoxycholic acid (UDCA) enters the portal vein and into the liver, where it undergoes conjugation with glycine or taurine.A256277 UDCA is also decreased into bile. Glycine or taurine conjugates are absorbed in the small intestine via passive and active mechanisms. The conjugates can also be deconjugated in the ileum by intestinal enzymes, leading to the formation of free UDCA that can be reabsorbed and re-conjugated in the liver.L44627 Nonabsorbed UDCA passes into the colon, where it undergoes 7-dehydroxylation by intestinal bacteria to lithocholic acid.A256728 Some UDCA is epimerized to chenodeoxycholic acid via a 7-oxo intermediate. Chenodeoxycholic acid also undergoes 7-dehydroxylation to form lithocholic acid. These metabolites are poorly soluble and excreted in the feces. A small portion of lithocholic acid is reabsorbed, conjugated in the liver with glycine or taurine, and sulfated at the 3 position. The resulting sulfated lithocholic acid conjugates are excreted in bile and then lost in feces.L44627

Rute Eliminasi

Ursodeoxycholic acid is excreted primarily in the feces. Renal elimination is a minor elimination pathway. With treatment, urinary excretion increases but remains less than 1% except in severe cholestatic liver disease.A256678,L44627

Interaksi Makanan

1 Data
  • 1. Take with food.

Interaksi Obat

262 Data
Lepirudin The risk or severity of bleeding and bruising can be increased when Lepirudin is combined with Ursodeoxycholic acid.
Bivalirudin The risk or severity of bleeding and bruising can be increased when Bivalirudin is combined with Ursodeoxycholic acid.
Alteplase The risk or severity of bleeding and bruising can be increased when Alteplase is combined with Ursodeoxycholic acid.
Urokinase The risk or severity of bleeding and bruising can be increased when Urokinase is combined with Ursodeoxycholic acid.
Reteplase The risk or severity of bleeding and bruising can be increased when Reteplase is combined with Ursodeoxycholic acid.
Anistreplase The risk or severity of bleeding and bruising can be increased when Anistreplase is combined with Ursodeoxycholic acid.
Tenecteplase The risk or severity of bleeding and bruising can be increased when Tenecteplase is combined with Ursodeoxycholic acid.
Drotrecogin alfa The risk or severity of bleeding and bruising can be increased when Drotrecogin alfa is combined with Ursodeoxycholic acid.
Streptokinase The risk or severity of bleeding and bruising can be increased when Streptokinase is combined with Ursodeoxycholic acid.
Dicoumarol The risk or severity of bleeding and bruising can be increased when Dicoumarol is combined with Ursodeoxycholic acid.
Argatroban The risk or severity of bleeding and bruising can be increased when Argatroban is combined with Ursodeoxycholic acid.
Ardeparin The risk or severity of bleeding and bruising can be increased when Ardeparin is combined with Ursodeoxycholic acid.
Phenindione The risk or severity of bleeding and bruising can be increased when Phenindione is combined with Ursodeoxycholic acid.
Fondaparinux The risk or severity of bleeding and bruising can be increased when Fondaparinux is combined with Ursodeoxycholic acid.
Warfarin The risk or severity of bleeding and bruising can be increased when Warfarin is combined with Ursodeoxycholic acid.
Pentosan polysulfate The risk or severity of bleeding and bruising can be increased when Pentosan polysulfate is combined with Ursodeoxycholic acid.
Phenprocoumon The risk or severity of bleeding and bruising can be increased when Phenprocoumon is combined with Ursodeoxycholic acid.
Heparin The risk or severity of bleeding and bruising can be increased when Heparin is combined with Ursodeoxycholic acid.
Enoxaparin The risk or severity of bleeding and bruising can be increased when Enoxaparin is combined with Ursodeoxycholic acid.
Acenocoumarol The risk or severity of bleeding and bruising can be increased when Acenocoumarol is combined with Ursodeoxycholic acid.
4-hydroxycoumarin The risk or severity of bleeding and bruising can be increased when 4-hydroxycoumarin is combined with Ursodeoxycholic acid.
Coumarin The risk or severity of bleeding and bruising can be increased when Coumarin is combined with Ursodeoxycholic acid.
Ximelagatran The risk or severity of bleeding and bruising can be increased when Ximelagatran is combined with Ursodeoxycholic acid.
Desmoteplase The risk or severity of bleeding and bruising can be increased when Desmoteplase is combined with Ursodeoxycholic acid.
Ancrod The risk or severity of bleeding and bruising can be increased when Ancrod is combined with Ursodeoxycholic acid.
Rivaroxaban The risk or severity of bleeding and bruising can be increased when Rivaroxaban is combined with Ursodeoxycholic acid.
Sulodexide The risk or severity of bleeding and bruising can be increased when Sulodexide is combined with Ursodeoxycholic acid.
Semuloparin The risk or severity of bleeding and bruising can be increased when Semuloparin is combined with Ursodeoxycholic acid.
Idraparinux The risk or severity of bleeding and bruising can be increased when Idraparinux is combined with Ursodeoxycholic acid.
Astaxanthin The risk or severity of bleeding and bruising can be increased when Astaxanthin is combined with Ursodeoxycholic acid.
Apixaban The risk or severity of bleeding and bruising can be increased when Apixaban is combined with Ursodeoxycholic acid.
Otamixaban The risk or severity of bleeding and bruising can be increased when Otamixaban is combined with Ursodeoxycholic acid.
Amediplase The risk or severity of bleeding and bruising can be increased when Amediplase is combined with Ursodeoxycholic acid.
Dabigatran etexilate The risk or severity of bleeding and bruising can be increased when Dabigatran etexilate is combined with Ursodeoxycholic acid.
Danaparoid The risk or severity of bleeding and bruising can be increased when Danaparoid is combined with Ursodeoxycholic acid.
Dalteparin The risk or severity of bleeding and bruising can be increased when Dalteparin is combined with Ursodeoxycholic acid.
Tinzaparin The risk or severity of bleeding and bruising can be increased when Tinzaparin is combined with Ursodeoxycholic acid.
(R)-warfarin The risk or severity of bleeding and bruising can be increased when (R)-warfarin is combined with Ursodeoxycholic acid.
Ethyl biscoumacetate The risk or severity of bleeding and bruising can be increased when Ethyl biscoumacetate is combined with Ursodeoxycholic acid.
Nadroparin The risk or severity of bleeding and bruising can be increased when Nadroparin is combined with Ursodeoxycholic acid.
Ditazole The risk or severity of bleeding and bruising can be increased when Ditazole is combined with Ursodeoxycholic acid.
Edoxaban The risk or severity of bleeding and bruising can be increased when Edoxaban is combined with Ursodeoxycholic acid.
Sodium citrate The risk or severity of bleeding and bruising can be increased when Sodium citrate is combined with Ursodeoxycholic acid.
Dextran The risk or severity of bleeding and bruising can be increased when Dextran is combined with Ursodeoxycholic acid.
Bemiparin The risk or severity of bleeding and bruising can be increased when Bemiparin is combined with Ursodeoxycholic acid.
Parnaparin The risk or severity of bleeding and bruising can be increased when Parnaparin is combined with Ursodeoxycholic acid.
Desirudin The risk or severity of bleeding and bruising can be increased when Desirudin is combined with Ursodeoxycholic acid.
Antithrombin Alfa The risk or severity of bleeding and bruising can be increased when Antithrombin Alfa is combined with Ursodeoxycholic acid.
Protein C The risk or severity of bleeding and bruising can be increased when Protein C is combined with Ursodeoxycholic acid.
Antithrombin III human The risk or severity of bleeding and bruising can be increased when Antithrombin III human is combined with Ursodeoxycholic acid.
Letaxaban The risk or severity of bleeding and bruising can be increased when Letaxaban is combined with Ursodeoxycholic acid.
Darexaban The risk or severity of bleeding and bruising can be increased when Darexaban is combined with Ursodeoxycholic acid.
Betrixaban The risk or severity of bleeding and bruising can be increased when Betrixaban is combined with Ursodeoxycholic acid.
Nafamostat The risk or severity of bleeding and bruising can be increased when Nafamostat is combined with Ursodeoxycholic acid.
Monteplase The risk or severity of bleeding and bruising can be increased when Monteplase is combined with Ursodeoxycholic acid.
Gabexate The risk or severity of bleeding and bruising can be increased when Gabexate is combined with Ursodeoxycholic acid.
Fluindione The risk or severity of bleeding and bruising can be increased when Fluindione is combined with Ursodeoxycholic acid.
Protein S human The risk or severity of bleeding and bruising can be increased when Protein S human is combined with Ursodeoxycholic acid.
Brinase The risk or severity of bleeding and bruising can be increased when Brinase is combined with Ursodeoxycholic acid.
Clorindione The risk or severity of bleeding and bruising can be increased when Clorindione is combined with Ursodeoxycholic acid.
Diphenadione The risk or severity of bleeding and bruising can be increased when Diphenadione is combined with Ursodeoxycholic acid.
Tioclomarol The risk or severity of bleeding and bruising can be increased when Tioclomarol is combined with Ursodeoxycholic acid.
Melagatran The risk or severity of bleeding and bruising can be increased when Melagatran is combined with Ursodeoxycholic acid.
Saruplase The risk or severity of bleeding and bruising can be increased when Saruplase is combined with Ursodeoxycholic acid.
(S)-Warfarin The risk or severity of bleeding and bruising can be increased when (S)-Warfarin is combined with Ursodeoxycholic acid.
Tocopherylquinone The risk or severity of bleeding and bruising can be increased when Tocopherylquinone is combined with Ursodeoxycholic acid.
Dabigatran The risk or severity of bleeding and bruising can be increased when Dabigatran is combined with Ursodeoxycholic acid.
Troxerutin The risk or severity of bleeding and bruising can be increased when Troxerutin is combined with Ursodeoxycholic acid.
Edetic acid The risk or severity of bleeding and bruising can be increased when Edetic acid is combined with Ursodeoxycholic acid.
Reviparin The risk or severity of bleeding and bruising can be increased when Reviparin is combined with Ursodeoxycholic acid.
Dermatan sulfate The risk or severity of bleeding and bruising can be increased when Dermatan sulfate is combined with Ursodeoxycholic acid.
SR-123781A The risk or severity of bleeding and bruising can be increased when SR-123781A is combined with Ursodeoxycholic acid.
Abciximab The risk or severity of adverse effects can be increased when Abciximab is combined with Ursodeoxycholic acid.
Eptifibatide The risk or severity of adverse effects can be increased when Eptifibatide is combined with Ursodeoxycholic acid.
Ticlopidine The risk or severity of adverse effects can be increased when Ticlopidine is combined with Ursodeoxycholic acid.
Anagrelide The risk or severity of adverse effects can be increased when Anagrelide is combined with Ursodeoxycholic acid.
Clopidogrel The risk or severity of adverse effects can be increased when Clopidogrel is combined with Ursodeoxycholic acid.
Tirofiban The risk or severity of adverse effects can be increased when Tirofiban is combined with Ursodeoxycholic acid.
Pentoxifylline The risk or severity of adverse effects can be increased when Pentoxifylline is combined with Ursodeoxycholic acid.
Acetylsalicylic acid The risk or severity of adverse effects can be increased when Acetylsalicylic acid is combined with Ursodeoxycholic acid.
Dipyridamole The risk or severity of adverse effects can be increased when Dipyridamole is combined with Ursodeoxycholic acid.
Sulfinpyrazone The risk or severity of adverse effects can be increased when Sulfinpyrazone is combined with Ursodeoxycholic acid.
Cilostazol The risk or severity of adverse effects can be increased when Cilostazol is combined with Ursodeoxycholic acid.
Ridogrel The risk or severity of adverse effects can be increased when Ridogrel is combined with Ursodeoxycholic acid.
Epoprostenol The risk or severity of adverse effects can be increased when Epoprostenol is combined with Ursodeoxycholic acid.
Resveratrol The risk or severity of adverse effects can be increased when Resveratrol is combined with Ursodeoxycholic acid.
Nimesulide The risk or severity of adverse effects can be increased when Nimesulide is combined with Ursodeoxycholic acid.
Tesmilifene The risk or severity of adverse effects can be increased when Tesmilifene is combined with Ursodeoxycholic acid.
Defibrotide The risk or severity of adverse effects can be increased when Defibrotide is combined with Ursodeoxycholic acid.
Beraprost The risk or severity of adverse effects can be increased when Beraprost is combined with Ursodeoxycholic acid.
Ibudilast The risk or severity of adverse effects can be increased when Ibudilast is combined with Ursodeoxycholic acid.
Andrographolide The risk or severity of adverse effects can be increased when Andrographolide is combined with Ursodeoxycholic acid.
Caplacizumab The risk or severity of adverse effects can be increased when Caplacizumab is combined with Ursodeoxycholic acid.
Prasugrel The risk or severity of adverse effects can be increased when Prasugrel is combined with Ursodeoxycholic acid.
Cangrelor The risk or severity of adverse effects can be increased when Cangrelor is combined with Ursodeoxycholic acid.
Tranilast The risk or severity of adverse effects can be increased when Tranilast is combined with Ursodeoxycholic acid.
Triflusal The risk or severity of adverse effects can be increased when Triflusal is combined with Ursodeoxycholic acid.
Ticagrelor The risk or severity of adverse effects can be increased when Ticagrelor is combined with Ursodeoxycholic acid.
Icosapent ethyl The risk or severity of adverse effects can be increased when Icosapent ethyl is combined with Ursodeoxycholic acid.
Vorapaxar The risk or severity of adverse effects can be increased when Vorapaxar is combined with Ursodeoxycholic acid.

Target Protein

Aldo-keto reductase family 1 member C2 AKR1C2
Biliverdin reductase A BLVRA
Solute carrier family 23 member 2 SLC23A2
Bile acid receptor NR1H4

Referensi & Sumber

Synthesis reference: Antonio Bonaldi, Egidio Molinari, "Process for preparing high purity ursodeoxycholic acid." U.S. Patent US4379093, issued July, 1980.
Artikel (PubMed)
  • PMID: 31424887
    Achufusi TGO, Safadi AO, Mahabadi N: Ursodeoxycholic Acid. .
  • PMID: 31643632
    Authors unspecified: Ursodiol (Ursodeoxycholic Acid). .
  • PMID: 22942741
    Kotb MA: Molecular mechanisms of ursodeoxycholic acid toxicity & side effects: ursodeoxycholic acid freezes regeneration & induces hibernation mode. Int J Mol Sci. 2012;13(7):8882-8914. doi: 10.3390/ijms13078882. Epub 2012 Jul 17.
  • PMID: 33342564
    Trampert DC, van de Graaf SFJ, Jongejan A, Oude Elferink RPJ, Beuers U: Hepatobiliary acid-base homeostasis: Insights from analogous secretory epithelia. J Hepatol. 2021 Feb;74(2):428-441. doi: 10.1016/j.jhep.2020.10.010. Epub 2020 Oct 24.
  • PMID: 18690863
    Festi D, Montagnani M, Azzaroli F, Lodato F, Mazzella G, Roda A, Di Biase AR, Roda E, Simoni P, Colecchia A: Clinical efficacy and effectiveness of ursodeoxycholic acid in cholestatic liver diseases. Curr Clin Pharmacol. 2007 May;2(2):155-77. doi: 10.2174/157488407780598171.
  • PMID: 12198643
    Paumgartner G, Beuers U: Ursodeoxycholic acid in cholestatic liver disease: mechanisms of action and therapeutic use revisited. Hepatology. 2002 Sep;36(3):525-31. doi: 10.1053/jhep.2002.36088.
  • PMID: 11825540
    Angulo P: Use of ursodeoxycholic acid in patients with liver disease. Curr Gastroenterol Rep. 2002 Feb;4(1):37-44. doi: 10.1007/s11894-002-0036-9.
  • PMID: 7824870
    Hofmann AF: Pharmacology of ursodeoxycholic acid, an enterohepatic drug. Scand J Gastroenterol Suppl. 1994;204:1-15. doi: 10.3109/00365529409103618.

Contoh Produk & Brand

Produk: 138 • International brands: 9
Produk
  • Actigall
    Capsule • 300 mg/1 • Oral • US • Approved
  • Actigall
    Capsule • 300 mg/1 • Oral • US • Approved
  • Ag-ursodiol
    Tablet • 250 mg • Oral • Canada • Generic • Approved
  • Ag-ursodiol
    Tablet • 500 mg • Oral • Canada • Generic • Approved
  • BAMBOO SALT Eunganggo Jook Yeom
    Paste • - • Dental • US • OTC
  • BAMBOO SALT Eunganggo Jook Yeom Toothpaste
    Paste • - • Dental • US • OTC
  • Dom-ursodiol C
    Tablet • 250 mg • Oral • Canada • Generic • Approved
  • Dom-ursodiol C
    Tablet • 500 mg • Oral • Canada • Generic • Approved
Menampilkan 8 dari 138 produk.
International Brands
  • Cholit-ursan
  • Delursan
  • Destolit
  • Deursil
  • Litursol
  • Solutrat
  • Ursacol
  • Ursochol
  • Ursolvan

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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