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QuickView for Triflusal (compound)


PubChem
Name: triflusal
PubChem Compound ID: 9458
Molecular formula: C10H7F3O4
Molecular weight: 248.155 g/mol
Synonyms:
NCGC00016431-01; Triflusal; 2-Acetoxy-4-trifluoromethylbenzoic acid; BRN 2945374; alpha,alpha,alpha-Trifluoro-2,4-creosotic acid acetate; 4-Trifluoromethylsalicylic acid acetate; Triflusal [INN]; 3-Acetoxy-alpha,alpha,alpha-trifluoro-p-toluic acid; Prestwick_851; Prestwick0_000528.
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DrugBank
Identification
Name: triflusal
Name (isomeric): DB08814
Drug Type: small molecule
Category: Anticoagulants, Antithrombotics, Antiplatelet Agents
Pharmacology
Indication: <ul> <li>Prevention of cardiovascular events such as stroke</li> <li>Acute treatment of cerebral infarction, myocardial infarction</li> <li>Thromboprophylaxis due to atrial fibrillation</li> </ul>
Pharmacology:
Triflusal is an antithrombotic anticoagulant. It irreversibly inhibits the production of thromboxane-B2 in platelets by acetylating cycloxygenase-1. Triflusal affects many other targets such as NF kappa B, which is a gene expression regulatory factor for cycloxygenase-a and cytokines. Numerous studies comparing the efficacy and safety profile (i.e....
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Mechanism of Action:
Triflusal is chemically related to acetylsalicylic acid (ASA) and irreversibly inhibits cycloxygenase-1 (COX-1) in platelets. Acetylation of the active group of COX-1 prevents the formation of thromboxane-B2 in platelets. However, it is unique because it spares the arachidonic acid metabolic pathway in endothelial cells. In addition, it favors the ...
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Absorption: Absorbed in the small intestine with a bioavailability range from 83% to 100%. There is no significant difference between the absorption of the oral solution and capsule formulation.
Protein binding: Binds to plasma proteins almost entirely (99%)
Biotransformation: In the liver, triflusal undergoes deacetylation, forming its main metabolite 2-OH-4-trifluoromethyl benzoic acid (HTB).
Route of elimination: Primarily renal.
Half Life: In healthy human, the half life is 0.5 +/- 0.1h, while that of HTB is 34.3 +/- 5.3h.
Clearance: Renal clearance is 0.8 +/- 0.2L/h and 0.18 +/1 0.04L/h for triflusal and HTB, respectively.
Toxicity: Excessive bleeding. The risk of bleeding is less than that of acetylsalicylic acid.
Interactions
Food interaction:
Herbs with anticoagulant/antiplatelet activity such as alfalfa, feverfew, ginger, ginseng, grape seed, green tea, horseradish
Gingko bilboa
Drug interaction:
PiroxicamThe metabolite of triflusal, 2-hydroxy-4-trifluoro-methyl-benzoic acid (HTB), impairs the serum protein binding of glisentide to the same extent as acetylsalisylic acid. Thus, the free fraction of glisentide may be increased. A dosage reduction may be required if used in combination.
WarfarinThe metabolite of triflusal, 2-hydroxy-4-trifluoro-methyl-benzoic acid (HTB), impairs the serum protein binding of warfarin to the same extent as acetylsalisylic acid. Thus, the free fraction of glisentide may be increased. A dosage reduction may be required if used in combination.
NaproxenThe metabolite of triflusal, 2-hydroxy-4-trifluoro-methyl-benzoic acid (HTB), impairs the serum protein binding of naproxen to the same extent as acetylsalisylic acid. Thus, the free fraction of glisentide may be increased. A dosage reduction may be required if used in combination.
IbuprofenThe metabolite of triflusal, 2-hydroxy-4-trifluoro-methyl-benzoic acid (HTB), impairs the serum protein binding of ibuprofen to the same extent as acetylsalisylic acid. Thus, the free fraction of glisentide may be increased. A dosage reduction may be required if used in combination.

Targets