Tìm theo
Triflusal
Các tên gọi khác (2) :
  • SID11112328
  • Triflusal
Thuốc tim mạch
Thuốc Gốc
Small Molecule
ATC: B01AC18
Approved by the European Stroke Organization, triflusal is recommended as lone therapy for the secondary prevention of atheroembotic stroke. Triflusal appears to be equally effective with a better safety profile than acetylsalicylic acid plus dypridamole and clopidogrel alone based on a double blind, randomized TACIP and TAPIRSS trials.
Dược Lực Học : 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. systemic hemorrhage) between triflusal and acetylsalsylic acid has shown either no significant difference or a better effacy and safety profile for triflusal. Triflusal has been shown to protect cerebral tissue due to its inhibition of lipid peroxidation resulting from anoxia-reoxygenation.
Cơ Chế Tác Dụng : Approved by the European Stroke Organization, triflusal is recommended as lone therapy for the secondary prevention of atheroembotic stroke. Triflusal appears to be equally effective with a better safety profile than acetylsalicylic acid plus dypridamole and clopidogrel alone based on a double blind, randomized TACIP and TAPIRSS trials. 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 production of nitric oxide, a vasodilator.
Dược Động Học :
▧ 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.
▧ Volume of Distribution :
34L
▧ Protein binding :
Binds to plasma proteins almost entirely (99%)
▧ Metabolism :
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.
Độc Tính : Excessive bleeding. The risk of bleeding is less than that of acetylsalicylic acid.
Chỉ Định :
  • Prevention of cardiovascular events such as stroke
  • Acute treatment of cerebral infarction, myocardial infarction
  • Thromboprophylaxis due to atrial fibrillation
Tương Tác Thuốc :
  • Ibuprofen The 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.
  • Naproxen The 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.
  • Piroxicam The 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.
  • Warfarin The 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.
Liều Lượng & Cách Dùng : Capsule - Oral - 300mg
Capsule - Oral - 600mg
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB08814
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