Peringatan Keamanan

LD50, oral in mouse: 2690mg/kg L2125.
Ld50, subcutaneous in mouse: 1gm/kg L2125.

Interferes with thyroid function test L2132.

Gastrointestinal (GI) disorders, fatigue, hypersensitivity reactions, skin eruptions, hemolytic anemia, weakness, dyspnoea; local irritation (rectally); Reye's syndrome.

Potentially Fatal: Paroxysmal bronchospasm; hepatotoxicity; renal impairment/failure; thrombocytopenia, iron-deficiency anemia, occult bleeding, leukopenia; mild chronic salicylate intoxication L2132.

Salicylate poisoning is normally associated with plasma concentrations >350 mg/L (2.5 mmol/L). Most adult deaths due to salicylate poisoning occur in patients whose serum concentrations of salicylate are over 700 mg/L (5.1 mmol/L). Single doses of less than 100 mg/kg are very unlikely to lead to serious poisoning. Patients should be provided with supportive therapy or treatment for salicylate poisoning as necessary. This may include treatment like activated charcoal, urinary alkalinization and, in severe cases, hemodialysis L2139.

Choline salicylate

DB14006

small molecule approved nutraceutical

Deskripsi

Choline salicylate is an anti-inflammatory pain reliever agent that is related to aspirin. It is used to decrease swelling and to treat mild-moderate pain. It is used to treat arthritis in both children and adults. This medicine can also be used for fever L2129.

Choline Salicylate is the choline salt of salicylic acid, used as an analgesic, antipyretic and antirheumatic. It relieves mild to moderate pain and reduce fever and inflammation or swelling. Choline salicylate is effective in the treatment of gout, rheumatic fever, rheumatoid arthritis and muscle injuries A245119.

This drug is also a main ingredient in teething gels to relieve pains associated with tooth growth in the infant population L2134. The UK government has regulated its use, due to toxicity in those under 16 years of age. Topical oral salicylate gels are no longer indicated for people younger than 16 years for pain associated with infant teething, orthodontic devices, cold sores, or mouth ulcers L2134.

Struktur Molekul 2D

Berat 241.287
Wujud solid

Peta Jejaring Molekuler
Legenda: ObatTargetGenEnzim(Panah → menunjukkan arah efek / relasi)TransporterCarrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The plasma half-life of salicylic acid is 2-4 hours.[L2139]
Volume Distribusi 0.15 L/kg (salicylate), and widely distributed throughout extracellular water and most tissues [L2139]
Klirens (Clearance) -

Absorpsi

Onset: 1-2 hr after ingestion L2133 In the oral form, choline salicylate is absorbed across the buccal mucosa. There is a need for caution not to exceed the stated dose and monitor for any signs of suggested salicylism, especially when this drug is used for infants L2135. In one study, it was found that this drug was more rapidly absorbed than ASA (absorption t1/2 = 0.1 vs 0.36 h) L2138.

Metabolisme

The metabolism of salicylic acid is by glycine and phenolic or acyl glucuronate conjugation with small amounts of the drug undergoing hydroxylation.L2139

Rute Eliminasi

Both metabolites of choline salicylate, and a small amount of intact salicylic acid are excreted, primarily in the urine.L2139

Interaksi Obat

1059 Data
Ammonium chloride The serum concentration of Choline salicylate 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 Choline salicylate.
Methotrexate The serum concentration of Methotrexate can be increased when it is combined with Choline salicylate.
Pralatrexate The serum concentration of Pralatrexate can be increased when it is combined with Choline salicylate.
Probenecid The therapeutic efficacy of Probenecid can be decreased when used in combination with Choline salicylate.
Treprostinil The risk or severity of bleeding can be increased when Treprostinil is combined with Choline salicylate.
Bupropion The excretion of Choline salicylate can be decreased when combined with Bupropion.
Ketoprofen The risk or severity of bleeding and gastrointestinal bleeding can be increased when Choline salicylate is combined with Ketoprofen.
Dexketoprofen The risk or severity of bleeding and gastrointestinal bleeding can be increased when Choline salicylate is combined with Dexketoprofen.
Dicoumarol Choline salicylate may increase the anticoagulant activities of Dicoumarol.
Phenindione Choline salicylate may increase the anticoagulant activities of Phenindione.
Phenprocoumon Choline salicylate may increase the anticoagulant activities of Phenprocoumon.
Acenocoumarol Choline salicylate may increase the anticoagulant activities of Acenocoumarol.
4-hydroxycoumarin Choline salicylate may increase the anticoagulant activities of 4-hydroxycoumarin.
Coumarin Choline salicylate may increase the anticoagulant activities of Coumarin.
(R)-warfarin Choline salicylate may increase the anticoagulant activities of (R)-warfarin.
Ethyl biscoumacetate Choline salicylate may increase the anticoagulant activities of Ethyl biscoumacetate.
Fluindione Choline salicylate may increase the anticoagulant activities of Fluindione.
Clorindione Choline salicylate may increase the anticoagulant activities of Clorindione.
Diphenadione Choline salicylate may increase the anticoagulant activities of Diphenadione.
Tioclomarol Choline salicylate may increase the anticoagulant activities of Tioclomarol.
(S)-Warfarin Choline salicylate may increase the anticoagulant activities of (S)-Warfarin.
Acetyldigitoxin The serum concentration of Acetyldigitoxin can be decreased when it is combined with Choline salicylate.
Deslanoside The serum concentration of Deslanoside can be decreased when it is combined with Choline salicylate.
Ouabain The serum concentration of Ouabain can be decreased when it is combined with Choline salicylate.
Digitoxin The serum concentration of Digitoxin can be decreased when it is combined with Choline salicylate.
Oleandrin The serum concentration of Oleandrin can be decreased when it is combined with Choline salicylate.
Cymarin The serum concentration of Cymarin can be decreased when it is combined with Choline salicylate.
Proscillaridin The serum concentration of Proscillaridin can be decreased when it is combined with Choline salicylate.
Metildigoxin The serum concentration of Metildigoxin can be decreased when it is combined with Choline salicylate.
Lanatoside C The serum concentration of Lanatoside C can be decreased when it is combined with Choline salicylate.
Gitoformate The serum concentration of Gitoformate can be decreased when it is combined with Choline salicylate.
Acetyldigoxin The serum concentration of Acetyldigoxin can be decreased when it is combined with Choline salicylate.
Peruvoside The serum concentration of Peruvoside can be decreased when it is combined with Choline salicylate.
Tioguanine The metabolism of Tioguanine can be decreased when combined with Choline salicylate.
Mercaptopurine The metabolism of Mercaptopurine can be decreased when combined with Choline salicylate.
Azathioprine The metabolism of Azathioprine can be decreased when combined with Choline salicylate.
Lepirudin The risk or severity of bleeding can be increased when Choline salicylate is combined with Lepirudin.
Bivalirudin The risk or severity of bleeding can be increased when Choline salicylate is combined with Bivalirudin.
Alteplase The risk or severity of bleeding can be increased when Choline salicylate is combined with Alteplase.
Urokinase The risk or severity of bleeding can be increased when Choline salicylate is combined with Urokinase.
Reteplase The risk or severity of bleeding can be increased when Choline salicylate is combined with Reteplase.
Anistreplase The risk or severity of bleeding can be increased when Choline salicylate is combined with Anistreplase.
Tenecteplase The risk or severity of bleeding can be increased when Choline salicylate is combined with Tenecteplase.
Abciximab The risk or severity of bleeding can be increased when Choline salicylate is combined with Abciximab.
Drotrecogin alfa The risk or severity of bleeding can be increased when Choline salicylate is combined with Drotrecogin alfa.
Streptokinase The risk or severity of bleeding can be increased when Choline salicylate is combined with Streptokinase.
Argatroban The risk or severity of bleeding can be increased when Choline salicylate is combined with Argatroban.
Ardeparin The risk or severity of bleeding can be increased when Choline salicylate is combined with Ardeparin.
Fondaparinux The risk or severity of bleeding can be increased when Choline salicylate is combined with Fondaparinux.
Pentosan polysulfate The risk or severity of bleeding can be increased when Choline salicylate is combined with Pentosan polysulfate.
Dipyridamole The risk or severity of bleeding can be increased when Choline salicylate is combined with Dipyridamole.
Heparin The risk or severity of bleeding can be increased when Choline salicylate is combined with Heparin.
Enoxaparin The risk or severity of bleeding can be increased when Choline salicylate is combined with Enoxaparin.
Epoprostenol The risk or severity of bleeding can be increased when Choline salicylate is combined with Epoprostenol.
Ximelagatran The risk or severity of bleeding can be increased when Choline salicylate is combined with Ximelagatran.
Desmoteplase The risk or severity of bleeding can be increased when Choline salicylate is combined with Desmoteplase.
Defibrotide The risk or severity of bleeding can be increased when Choline salicylate is combined with Defibrotide.
Ancrod The risk or severity of bleeding can be increased when Choline salicylate is combined with Ancrod.
Beraprost The risk or severity of bleeding can be increased when Choline salicylate is combined with Beraprost.
Prasugrel The risk or severity of bleeding can be increased when Choline salicylate is combined with Prasugrel.
Rivaroxaban The risk or severity of bleeding can be increased when Choline salicylate is combined with Rivaroxaban.
Sulodexide The risk or severity of bleeding can be increased when Choline salicylate is combined with Sulodexide.
Semuloparin The risk or severity of bleeding can be increased when Choline salicylate is combined with Semuloparin.
Idraparinux The risk or severity of bleeding can be increased when Choline salicylate is combined with Idraparinux.
Cangrelor The risk or severity of bleeding can be increased when Choline salicylate is combined with Cangrelor.
Astaxanthin The risk or severity of bleeding can be increased when Choline salicylate is combined with Astaxanthin.
Apixaban The risk or severity of bleeding can be increased when Choline salicylate is combined with Apixaban.
Otamixaban The risk or severity of bleeding can be increased when Choline salicylate is combined with Otamixaban.
Amediplase The risk or severity of bleeding can be increased when Choline salicylate is combined with Amediplase.
Dabigatran etexilate The risk or severity of bleeding can be increased when Choline salicylate is combined with Dabigatran etexilate.
Danaparoid The risk or severity of bleeding can be increased when Choline salicylate is combined with Danaparoid.
Dalteparin The risk or severity of bleeding can be increased when Choline salicylate is combined with Dalteparin.
Tinzaparin The risk or severity of bleeding can be increased when Choline salicylate is combined with Tinzaparin.
Nadroparin The risk or severity of bleeding can be increased when Choline salicylate is combined with Nadroparin.
Triflusal The risk or severity of bleeding can be increased when Choline salicylate is combined with Triflusal.
Ticagrelor The risk or severity of bleeding can be increased when Choline salicylate is combined with Ticagrelor.
Ditazole The risk or severity of bleeding can be increased when Choline salicylate is combined with Ditazole.
Vorapaxar The risk or severity of bleeding can be increased when Choline salicylate is combined with Vorapaxar.
Edoxaban The risk or severity of bleeding can be increased when Choline salicylate is combined with Edoxaban.
Potassium citrate Potassium citrate may increase the excretion rate of Choline salicylate which could result in a lower serum level and potentially a reduction in efficacy.
Sodium citrate The risk or severity of bleeding can be increased when Choline salicylate is combined with Sodium citrate.
Dextran The risk or severity of bleeding can be increased when Choline salicylate is combined with Dextran.
Bemiparin The risk or severity of bleeding can be increased when Choline salicylate is combined with Bemiparin.
Parnaparin The risk or severity of bleeding can be increased when Choline salicylate is combined with Parnaparin.
Desirudin The risk or severity of bleeding can be increased when Choline salicylate is combined with Desirudin.
Antithrombin Alfa The risk or severity of bleeding can be increased when Choline salicylate is combined with Antithrombin Alfa.
Protein C The risk or severity of bleeding can be increased when Choline salicylate is combined with Protein C.
Antithrombin III human The risk or severity of bleeding can be increased when Choline salicylate is combined with Antithrombin III human.
Letaxaban The risk or severity of bleeding can be increased when Choline salicylate is combined with Letaxaban.
Darexaban The risk or severity of bleeding can be increased when Choline salicylate is combined with Darexaban.
Betrixaban The risk or severity of bleeding can be increased when Choline salicylate is combined with Betrixaban.
Monteplase The risk or severity of bleeding can be increased when Choline salicylate is combined with Monteplase.
Gabexate The risk or severity of bleeding can be increased when Choline salicylate is combined with Gabexate.
Protein S human The risk or severity of bleeding can be increased when Choline salicylate is combined with Protein S human.
Brinase The risk or severity of bleeding can be increased when Choline salicylate is combined with Brinase.
Melagatran The risk or severity of bleeding can be increased when Choline salicylate is combined with Melagatran.
Saruplase The risk or severity of bleeding can be increased when Choline salicylate is combined with Saruplase.
Tocopherylquinone The risk or severity of bleeding can be increased when Choline salicylate is combined with Tocopherylquinone.
Dabigatran The risk or severity of bleeding can be increased when Choline salicylate is combined with Dabigatran.

Target Protein

Choline-phosphate cytidylyltransferase B PCYT1B
Acetylcholinesterase ACHE
Choline-phosphate cytidylyltransferase A PCYT1A
Phospholipase D2 PLD2
Cholinesterase BCHE
Phospholipase D1 PLD1
Neuronal acetylcholine receptor subunit alpha-7 CHRNA7

Referensi & Sumber

Artikel (PubMed)
  • PMID: 7249509
    Bochner F, Graham GG, Cham BE, Imhoff DM, Haavisto TM: Salicylate metabolite kinetics after several salicylates. Clin Pharmacol Ther. 1981 Aug;30(2):266-75.
  • PMID: 3888490
    Needs CJ, Brooks PM: Clinical pharmacokinetics of the salicylates. Clin Pharmacokinet. 1985 Mar-Apr;10(2):164-77. doi: 10.2165/00003088-198510020-00004.
  • PMID: 16258079
    Kuehl GE, Bigler J, Potter JD, Lampe JW: Glucuronidation of the aspirin metabolite salicylic acid by expressed UDP-glucuronosyltransferases and human liver microsomes. Drug Metab Dispos. 2006 Feb;34(2):199-202. doi: 10.1124/dmd.105.005652. Epub 2005 Oct 28.
  • PMID: 31877863
    Wroblewska KB, Plewa S, Derezinski P, Muszalska-Kolos I: Choline Salicylate Analysis: Chemical Stability and Degradation Product Identification. Molecules. 2019 Dec 22;25(1). pii: molecules25010051. doi: 10.3390/molecules25010051.

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Sekuens Gen/Protein (FASTA)

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