Name: | triflusal |
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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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Name: | triflusal |
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Name (isomeric): | DB08814 |
Drug Type: | small molecule |
Category: | Anticoagulants, Antithrombotics, Antiplatelet Agents |
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> |
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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. |
Food interaction: |
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Drug interaction: |
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