Literature DB >> 226020

Comparison of the inhibitory effects of acetylsalicylic acid and trifusal on enzymes related to thrombosis.

J Garcia Rafanell, J M Planas, P Puig-Parellada.   

Abstract

Triflusal is a new antithrombotic agent, structurally similar to acetylsalicylic acid (ASA), which has been shown to possess a different pharmacological profile, suggesting a different mechanism of action for both compounds. To confirm this hypothesis we have studied, comparatively, the inhibition by triflusal and ASA of the activity of several enzymes involved in the equilibrium of platelet haemostasis, namely, prostaglandin-synthetase system (PG-synthetase), cyclo-oxygenase, thromboxane-synthetase and cAMP-phosphodiesterase. Results indicate that trilfusal is 60% less potent as inhibitor of cyclooxygenase (biological method) and of prostaglandin biosynthesis (spectrophotometric method ) than ASA. On the contrary, triflusal is five times more potent than ASA as inhibitor of cAMP phosphodoesterase. Inhibition of thromboxane-synthetase by both compounds is negligible and without physiological significance. These results suggest a mechanism of action of trifusal that might explain the different pharmacological profile between triflusal and ASA as antithrombotic agents.

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Year:  1979        PMID: 226020

Source DB:  PubMed          Journal:  Arch Int Pharmacodyn Ther        ISSN: 0003-9780


  7 in total

Review 1.  Triflusal: a review of its use in cerebral infarction and myocardial infarction, and as thromboprophylaxis in atrial fibrillation.

Authors:  David Murdoch; Greg L Plosker
Journal:  Drugs       Date:  2006       Impact factor: 9.546

2.  Access of HTB, main metabolite of triflusal, to cerebrospinal fluid in healthy volunteers.

Authors:  M Valle; M J Barbanoj; A Donner; I Izquierdo; U Herranz; N Klein; H G Eichler; M Müller; M Brunner
Journal:  Eur J Clin Pharmacol       Date:  2005-02-12       Impact factor: 2.953

3.  Cyclic nucleotide phosphodiesterase inhibition by a benzoic acid derivative.

Authors:  J J Killackey; B A Killackey; R B Philp
Journal:  Agents Actions       Date:  1985-12

Review 4.  Triflusal.

Authors:  W McNeely; K L Goa
Journal:  Drugs       Date:  1998-06       Impact factor: 9.546

5.  Effects of triflusal and its main metabolite HTB on platelet interaction with subendothelium in healthy volunteers.

Authors:  J P De La Cruz; M A Villalobos; P J García; J M Smith-Agreda; F Sánchez de la Cuesta
Journal:  Eur J Clin Pharmacol       Date:  1995       Impact factor: 2.953

6.  Pharmacokinetics of triflusal and its main metabolite HTB in healthy subjects following a single oral dose.

Authors:  J Ramis; R Mis; J Forn; J Torrent; E Gorina; F Jané
Journal:  Eur J Drug Metab Pharmacokinet       Date:  1991 Oct-Dec       Impact factor: 2.441

7.  Pharmacokinetics of triflusal and its main metabolite in rats and dogs.

Authors:  J Ramis; R Mis; J Forn
Journal:  Eur J Drug Metab Pharmacokinet       Date:  1991 Oct-Dec       Impact factor: 2.441

  7 in total

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