Triflusal

Mechanism of action

Triflusal is a selective platelet antiaggregant through;

• blocks cyclooxygenase, thereby inhibiting thromboxane A2, and thus preventing platelet aggregation
• preserves vascular prostacyclin, thus promoting anti-aggregant effect
• inhibits activation of nuclear factor kB, which regulates the expression of the mRNA of vascular cell adhesion molecule-1 needed for platelet aggregation
• blocks phosphodiesterase thereby increasing cAMP concentration, thereby promoting anti-aggregant effect due to inhibition of calcium mobilization
• increases nitric oxide synthesis in neutrophils

Indication

Triflusal is indicated for;

• Prevention of cardiovascular events such as stroke
• Acute treatment of cerebral infarction, myocardial infarction
• Thromboprophylaxis due to atrial fibrillation

Prevention of stroke

In the 2008, guidelines for stroke management from the European Stroke Organization, triflusal was for the first time recommended as lone therapy, as an alternative to acetylsalicylic acid (ASA)(Aspirin) plus dipyridamole, or clopidogrel alone for secondary prevention of atherothrombotic stroke. This recommendation was based on the double-blind, randomised TACIP and TAPIRSS trials, which found triflusal to be as effective as Aspirin (acetylsalicylic acid, ASA, which Triflusal is derived from) in preventing post-stroke vascular events, while having a more favourable safety profile.

Pharmacokinetics

It is absorbed in the small intestine and its bio-availability ranges from 83% to 100%. The active metabolite of Triflusal is 2-hydroxy-4-trifluoromethyl-benzoic acid, which is when Triflusal gets metabolized by an esterase.

References

References

1. (2006). "Triflusal: a review of its use in cerebral infarction and myocardial infarction, and as thromboprophylaxis in atrial fibrillation". Drugs.
2. PubChem. "Triflusal".
3. (2023-09-08). "Home - European Stroke Organisation".
4. (April 2003). "Comparison of triflusal and aspirin for prevention of vascular events in patients after cerebral infarction: the TACIP Study: a randomized, double-blind, multicenter trial". Stroke.
5. (April 2004). "Triflusal vs aspirin for prevention of cerebral infarction: a randomized stroke study". Neurology.
6. European Stroke Organisation (ESO) Executive Committee, ESO Writing Committee.. (2008). "Guidelines for management of ischaemic stroke and transient ischaemic attack 2008.". Cerebrovascular Diseases.
7. (1990). "Rat and human plasma protein binding of the main metabolite of triflusal.". Eur J Pharmacol.
8. (1991). "Pharmacokinetics of triflusal and its main metabolite HTB in healthy subjects following a single oral dose". European Journal of Drug Metabolism and Pharmacokinetics.