Peringatan Keamanan

There is no information available regarding acute toxicity (LD50) of olsalazine. Symptoms of salicylate toxicity include nausea, vomiting and abdominal pain, tachypnea, hyperpnea, tinnitus, and neurologic symptoms (headache, dizziness, confusion, seizures). Severe intoxication may lead to electrolyte and blood pH imbalance and potentially to organ damage. There is no antidote for olsalazine overdose; however, conventional therapy for salicylate toxicity, such as gastrointestinal tract decontamination, may be beneficial in acute overdosage. Overdose should be managed with proper medical care and appropriate supportive care, including the possible use of emesis, cathartics, and activated charcoal to prevent further absorption. Fluid and electrolyte imbalance may be managed with appropriate intravenous therapy and maintenance of adequate renal function.L45023

Olsalazine

DB01250

small molecule approved

Deskripsi

Olsalazine is an aminosalicylate and a prodrug of mesalamine (5-aminosalicylic acid, 5-ASA).A257063 It was first developed for delivering mesalamine to the colon without the use of sulfapyridine.A257078 Olsalazine comprises two mesalamine molecules joined by an azo bridge, which is cleaved in the colon.A257078 Olsalazine is an anti-inflammatory agent that works by inhibiting cyclooxygenase and lipoxygenase, subsequently reducing the production of pro-inflammatory factors like prostaglandin and leukotriene.A257063 Olsalazine is used in the treatment of ulcerative colitis.L45023,L45151

Struktur Molekul 2D

Berat 302.239
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Olsalazine has a very short serum half-life, approximately 0.9 hours. Olsalazine-S has a half-life of seven days due to slow dissociation from the protein binding site.[A257063,L45023]
Volume Distribusi The steady-state volume of distribution determined in healthy volunteers is approximately 5L.[A257063]
Klirens (Clearance) -

Absorpsi

After oral administration, olsalazine has limited systemic bioavailability, with less than 5% of the oral dose being absorbed.A257063 Based on oral and intravenous dosing studies, approximately 2.4% of a single 1 g oral dose is absorbed. Maximum serum concentrations of olsalazine appear after approximately one hour and, even after a 1 g single dose, are low (e.g., 1.6 to 6.2 µmol/L).L45023 Patients on daily doses of 1 g olsalazine for two to four years show a stable plasma concentration of olsalazine-S (3.3 to 12.4 µmol/L). Olsalazine-S accumulates to a steady state within two to three weeks. Serum concentrations of mesalamine are detected after four to eight hours. The peak levels of mesalamine after an oral dose of 1 g olsalazine are low (i.e., 0 to 4.3 µmol/L).L45023

Metabolisme

Olsalazine is cleaved by colonic bacteria to release its active ingredient, mesalamine. Mesalamine can undergo acetylation to form N-acetyl-5-aminosalicylic acid (N-acetyl-5-ASA, Ac-5-ASA) by the colonic epithelium; however, the extent of acetylation depends on transit time.A257063 Approximately 0.1% of an oral dose of olsalazine is metabolized in the liver to olsalazine-O-sulfate (olsalazine-S).L45023

Rute Eliminasi

Olsalazine and its metabolites are excreted in the urine.A257063 Total recovery of oral 14C-labeled olsalazine in animals and humans ranges from 90 to 97%. Approximately 20% of the total mesalamine is recovered in the urine. Of the total mesalamine found in the urine, more than 90% is N-acetyl-5-ASA. Only small amounts of mesalamine are detected in the urine. The remaining mesalamine is partially acetylated and excreted in the feces. From fecal dialysis, the concentration of mesalamine in the colon following olsalazine has been calculated to be 18 to 49 mmol/L.L45023 The urinary recovery of olsalazine is below 1%.L45023 Less than 5% of an oral dose (0.25 to 2g) was recovered unchanged in the feces; however, more than 50% of the oral dose was excreted in feces as unchanged olsalazine when the whole gut transit time was decreased by approximately 50%.A257063

Interaksi Makanan

1 Data
  • 1. Take with food. Food does not affect drug absorption or exposure, but may mitigate the risk for drug-related adverse effects.

Interaksi Obat

972 Data
Ammonium chloride The serum concentration of Olsalazine can be increased when it is combined with Ammonium chloride.
Ginkgo biloba The risk or severity of bleeding can be increased when Ginkgo biloba is combined with Olsalazine.
Pralatrexate The serum concentration of Pralatrexate can be increased when it is combined with Olsalazine.
Desmopressin Olsalazine may decrease the excretion rate of Desmopressin which could result in a higher serum level.
Digoxin Olsalazine may decrease the excretion rate of Digoxin which could result in a higher serum level.
Metildigoxin The serum concentration of Metildigoxin can be decreased when it is combined with Olsalazine.
Acetyldigoxin The serum concentration of Acetyldigoxin can be decreased when it is combined with Olsalazine.
Haloperidol Olsalazine may decrease the excretion rate of Haloperidol which could result in a higher serum level.
Hydralazine Olsalazine may decrease the excretion rate of Hydralazine which could result in a higher serum level.
Lithium citrate The risk or severity of nephrotoxicity can be increased when Lithium citrate is combined with Olsalazine.
Lithium carbonate The risk or severity of nephrotoxicity can be increased when Lithium carbonate is combined with Olsalazine.
Methotrexate The risk or severity of nephrotoxicity can be increased when Methotrexate is combined with Olsalazine.
Pemetrexed Olsalazine may decrease the excretion rate of Pemetrexed which could result in a higher serum level.
Probenecid The therapeutic efficacy of Probenecid can be decreased when used in combination with Olsalazine.
Treprostinil The risk or severity of bleeding can be increased when Treprostinil is combined with Olsalazine.
Vancomycin The risk or severity of nephrotoxicity can be increased when Vancomycin is combined with Olsalazine.
Foscarnet The risk or severity of nephrotoxicity can be increased when Olsalazine is combined with Foscarnet.
Mannitol The risk or severity of nephrotoxicity can be increased when Mannitol is combined with Olsalazine.
Tenofovir disoproxil The risk or severity of nephrotoxicity can be increased when Tenofovir disoproxil is combined with Olsalazine.
Tenofovir alafenamide The risk or severity of nephrotoxicity can be increased when Tenofovir alafenamide is combined with Olsalazine.
Tenofovir The risk or severity of nephrotoxicity can be increased when Tenofovir is combined with Olsalazine.
Alendronic acid The risk or severity of nephrotoxicity and hypocalcemia can be increased when Olsalazine is combined with Alendronic acid.
Lepirudin The risk or severity of bleeding can be increased when Olsalazine is combined with Lepirudin.
Bivalirudin The risk or severity of bleeding can be increased when Olsalazine is combined with Bivalirudin.
Alteplase The risk or severity of bleeding can be increased when Olsalazine is combined with Alteplase.
Urokinase The risk or severity of bleeding can be increased when Olsalazine is combined with Urokinase.
Reteplase The risk or severity of bleeding can be increased when Olsalazine is combined with Reteplase.
Anistreplase The risk or severity of bleeding can be increased when Olsalazine is combined with Anistreplase.
Tenecteplase The risk or severity of bleeding can be increased when Olsalazine is combined with Tenecteplase.
Abciximab The risk or severity of bleeding can be increased when Olsalazine is combined with Abciximab.
Drotrecogin alfa The risk or severity of bleeding can be increased when Olsalazine is combined with Drotrecogin alfa.
Streptokinase The risk or severity of bleeding can be increased when Olsalazine is combined with Streptokinase.
Dicoumarol Olsalazine may increase the anticoagulant activities of Dicoumarol.
Argatroban The risk or severity of bleeding can be increased when Olsalazine is combined with Argatroban.
Ardeparin The risk or severity of bleeding can be increased when Ardeparin is combined with Olsalazine.
Phenindione Olsalazine may increase the anticoagulant activities of Phenindione.
Fondaparinux The risk or severity of bleeding can be increased when Olsalazine is combined with Fondaparinux.
Warfarin The risk or severity of bleeding can be increased when Warfarin is combined with Olsalazine.
Pentosan polysulfate The risk or severity of bleeding can be increased when Olsalazine is combined with Pentosan polysulfate.
Phenprocoumon Olsalazine may increase the anticoagulant activities of Phenprocoumon.
Dipyridamole The risk or severity of bleeding can be increased when Olsalazine is combined with Dipyridamole.
Heparin The risk or severity of bleeding can be increased when Heparin is combined with Olsalazine.
Enoxaparin The risk or severity of bleeding can be increased when Enoxaparin is combined with Olsalazine.
Epoprostenol The risk or severity of bleeding can be increased when Olsalazine is combined with Epoprostenol.
Acenocoumarol The risk or severity of bleeding can be increased when Acenocoumarol is combined with Olsalazine.
4-hydroxycoumarin Olsalazine may increase the anticoagulant activities of 4-hydroxycoumarin.
Coumarin Olsalazine may increase the anticoagulant activities of Coumarin.
Ximelagatran The risk or severity of bleeding can be increased when Olsalazine is combined with Ximelagatran.
Desmoteplase The risk or severity of bleeding can be increased when Olsalazine is combined with Desmoteplase.
Defibrotide The risk or severity of bleeding can be increased when Olsalazine is combined with Defibrotide.
Ancrod The risk or severity of bleeding can be increased when Olsalazine is combined with Ancrod.
Beraprost The risk or severity of bleeding can be increased when Olsalazine is combined with Beraprost.
Prasugrel The risk or severity of bleeding can be increased when Olsalazine is combined with Prasugrel.
Rivaroxaban The risk or severity of bleeding can be increased when Olsalazine is combined with Rivaroxaban.
Sulodexide The risk or severity of bleeding can be increased when Sulodexide is combined with Olsalazine.
Semuloparin The risk or severity of bleeding can be increased when Semuloparin is combined with Olsalazine.
Idraparinux The risk or severity of bleeding can be increased when Olsalazine is combined with Idraparinux.
Cangrelor The risk or severity of bleeding can be increased when Olsalazine is combined with Cangrelor.
Astaxanthin The risk or severity of bleeding can be increased when Olsalazine is combined with Astaxanthin.
Apixaban The risk or severity of bleeding can be increased when Olsalazine is combined with Apixaban.
Otamixaban The risk or severity of bleeding can be increased when Olsalazine is combined with Otamixaban.
Amediplase The risk or severity of bleeding can be increased when Olsalazine is combined with Amediplase.
Dabigatran etexilate The risk or severity of bleeding can be increased when Olsalazine is combined with Dabigatran etexilate.
Danaparoid The risk or severity of bleeding can be increased when Danaparoid is combined with Olsalazine.
Dalteparin The risk or severity of bleeding can be increased when Dalteparin is combined with Olsalazine.
Tinzaparin The risk or severity of bleeding can be increased when Tinzaparin is combined with Olsalazine.
(R)-warfarin The risk or severity of bleeding can be increased when (R)-warfarin is combined with Olsalazine.
Ethyl biscoumacetate Olsalazine may increase the anticoagulant activities of Ethyl biscoumacetate.
Nadroparin The risk or severity of bleeding can be increased when Nadroparin is combined with Olsalazine.
Triflusal The risk or severity of bleeding can be increased when Olsalazine is combined with Triflusal.
Ticagrelor The risk or severity of bleeding can be increased when Olsalazine is combined with Ticagrelor.
Ditazole The risk or severity of bleeding can be increased when Olsalazine is combined with Ditazole.
Vorapaxar The risk or severity of bleeding can be increased when Olsalazine is combined with Vorapaxar.
Edoxaban The risk or severity of bleeding can be increased when Olsalazine is combined with Edoxaban.
Sodium citrate The risk or severity of bleeding can be increased when Olsalazine is combined with Sodium citrate.
Dextran The risk or severity of bleeding can be increased when Olsalazine is combined with Dextran.
Bemiparin The risk or severity of bleeding can be increased when Bemiparin is combined with Olsalazine.
Parnaparin The risk or severity of bleeding can be increased when Parnaparin is combined with Olsalazine.
Desirudin The risk or severity of bleeding can be increased when Olsalazine is combined with Desirudin.
Antithrombin Alfa The risk or severity of bleeding can be increased when Olsalazine is combined with Antithrombin Alfa.
Protein C The risk or severity of bleeding can be increased when Olsalazine is combined with Protein C.
Antithrombin III human The risk or severity of bleeding can be increased when Olsalazine is combined with Antithrombin III human.
Letaxaban The risk or severity of bleeding can be increased when Olsalazine is combined with Letaxaban.
Darexaban The risk or severity of bleeding can be increased when Olsalazine is combined with Darexaban.
Nafamostat The risk or severity of bleeding can be increased when Olsalazine is combined with Nafamostat.
Monteplase The risk or severity of bleeding can be increased when Olsalazine is combined with Monteplase.
Gabexate The risk or severity of bleeding can be increased when Olsalazine is combined with Gabexate.
Fluindione Olsalazine may increase the anticoagulant activities of Fluindione.
Protein S human The risk or severity of bleeding can be increased when Olsalazine is combined with Protein S human.
Brinase The risk or severity of bleeding can be increased when Olsalazine is combined with Brinase.
Clorindione Olsalazine may increase the anticoagulant activities of Clorindione.
Diphenadione Olsalazine may increase the anticoagulant activities of Diphenadione.
Tioclomarol Olsalazine may increase the anticoagulant activities of Tioclomarol.
Melagatran The risk or severity of bleeding can be increased when Olsalazine is combined with Melagatran.
Saruplase The risk or severity of bleeding can be increased when Olsalazine is combined with Saruplase.
(S)-Warfarin The risk or severity of bleeding can be increased when (S)-Warfarin is combined with Olsalazine.
Tocopherylquinone The risk or severity of bleeding can be increased when Olsalazine is combined with Tocopherylquinone.
Dabigatran The risk or severity of bleeding can be increased when Olsalazine is combined with Dabigatran.
Reviparin The risk or severity of bleeding can be increased when Reviparin is combined with Olsalazine.
Troxerutin The risk or severity of bleeding can be increased when Olsalazine is combined with Troxerutin.

Target Protein

Human Cyclooxygenases PTGS1
Thiopurine S-methyltransferase TPMT
Xanthine dehydrogenase/oxidase XDH

Referensi & Sumber

Artikel (PubMed)
  • PMID: 1711964
    Wadworth AN, Fitton A: Olsalazine. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic potential in inflammatory bowel disease. Drugs. 1991 Apr;41(4):647-64. doi: 10.2165/00003495-199141040-00009.
  • PMID: 3067340
    Campbell DE, Berglindh T: Pharmacology of olsalazine. Scand J Gastroenterol Suppl. 1988;148:7-12. doi: 10.3109/00365528809101539.
  • PMID: 1685260
    Horn H, Preclik G, Stange EF, Ditschuneit H: Modulation of arachidonic acid metabolism by olsalazine and other aminosalicylates in leukocytes. Scand J Gastroenterol. 1991 Aug;26(8):867-79. doi: 10.3109/00365529109037024.
  • PMID: 12950415
    Allgayer H: Review article: mechanisms of action of mesalazine in preventing colorectal carcinoma in inflammatory bowel disease. Aliment Pharmacol Ther. 2003 Sep;18 Suppl 2:10-4.

Contoh Produk & Brand

Produk: 6 • International brands: 0
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Sekuens Gen/Protein (FASTA)

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