Peringatan Keamanan

There is the possibility of producing major systemic hemorrhages.L1168

Triflusal

DB08814

small molecule approved investigational

Deskripsi

Triflusal is a 2-acetoxy-4-trifluoromethylbenzoic acid and it is an aspirin chemically-related molecule but not a derivative. The benefits of this agent are the lack of action over the arachidonic acid pathway, the driven production of nitric oxide and the increase of cyclic nucleotide concentration on endothelial cells. The latest translates into the expansion of peripheral blood vessels.A31675 It is very important as a secondary prevention of ischemic stroke by offering a lower risk of bleeding.A31676 It was developed by J. Uriach and Company and even though it is commercialized in different countries it is not approved by the FDA, EMA or HealthCanada.

Struktur Molekul 2D

Berat 248.157
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) In the healthy human, the half-life is 0.5 +/- 0.1h, while that of HTB is 34.3 +/- 5.3h.[A7336]
Volume Distribusi The reported volume of distribution for triflusal is of 34L.[A31677]
Klirens (Clearance) Renal clearance is 0.8 +/- 0.2L/h and 0.18 +/1 0.04L/h for triflusal and HTB, respectively.[A7336]

Absorpsi

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.A7337 Triflusal displays a Cmax of 11.6 mcg/ml and a tmax of 0.88 h. The major metabolite of triflusal presents different pharmacokinetic properties by showing a Cmax and tmax of 92.7 mcg/ml and 4.96 h, respectively.A31677

Metabolisme

In the liver, triflusal undergoes deacetylation, forming its main metabolite 2-OH-4-trifluoromethyl benzoic acid (HTB). This major metabolite seems to have marked antiplatelet properties in vitro.T93

Rute Eliminasi

The elimination pathway of triflusal is primarily renal. Urine analysis has shown the presence of unchanged triflusal, HTB and the glycine conjugate of HTB.A7336

Interaksi Makanan

1 Data
  • 1. Avoid herbs and supplements with anticoagulant/antiplatelet activity. Examples include garlic, ginger, bilberry, danshen, piracetam, and ginkgo biloba.

Interaksi Obat

645 Data
Apixaban Apixaban may increase the anticoagulant activities of Triflusal.
Dabigatran etexilate Dabigatran etexilate may increase the anticoagulant activities of Triflusal.
Dasatinib The risk or severity of bleeding and hemorrhage can be increased when Dasatinib is combined with Triflusal.
Deferasirox The risk or severity of gastrointestinal bleeding can be increased when Triflusal is combined with Deferasirox.
Edoxaban The risk or severity of bleeding can be increased when Edoxaban is combined with Triflusal.
Ibrutinib The risk or severity of bleeding and hemorrhage can be increased when Ibrutinib is combined with Triflusal.
Rivaroxaban Triflusal may increase the anticoagulant activities of Rivaroxaban.
Sugammadex The risk or severity of bleeding and hemorrhage can be increased when Triflusal is combined with Sugammadex.
Tibolone Tibolone may increase the anticoagulant activities of Triflusal.
Urokinase Urokinase may increase the anticoagulant activities of Triflusal.
Vorapaxar The risk or severity of bleeding and hemorrhage can be increased when Vorapaxar is combined with Triflusal.
Ursodeoxycholic acid The risk or severity of adverse effects can be increased when Triflusal is combined with Ursodeoxycholic acid.
Glycochenodeoxycholic Acid The risk or severity of adverse effects can be increased when Triflusal is combined with Glycochenodeoxycholic Acid.
Cholic Acid The risk or severity of adverse effects can be increased when Triflusal is combined with Cholic Acid.
Glycocholic acid The risk or severity of adverse effects can be increased when Triflusal is combined with Glycocholic acid.
Deoxycholic acid The risk or severity of adverse effects can be increased when Triflusal is combined with Deoxycholic acid.
Taurocholic acid The risk or severity of adverse effects can be increased when Triflusal is combined with Taurocholic acid.
Obeticholic acid The risk or severity of adverse effects can be increased when Triflusal is combined with Obeticholic acid.
Chenodeoxycholic acid The risk or severity of adverse effects can be increased when Triflusal is combined with Chenodeoxycholic acid.
Taurochenodeoxycholic acid The risk or severity of adverse effects can be increased when Triflusal is combined with Taurochenodeoxycholic acid.
Tauroursodeoxycholic acid The risk or severity of adverse effects can be increased when Triflusal is combined with Tauroursodeoxycholic acid.
Bamet-UD2 The risk or severity of adverse effects can be increased when Triflusal is combined with Bamet-UD2.
Dehydrocholic acid The risk or severity of adverse effects can be increased when Triflusal is combined with Dehydrocholic acid.
Hyodeoxycholic Acid The risk or severity of adverse effects can be increased when Triflusal is combined with Hyodeoxycholic Acid.
Glucosamine Glucosamine may increase the antiplatelet activities of Triflusal.
Ibritumomab tiuxetan The risk or severity of adverse effects can be increased when Triflusal is combined with Ibritumomab tiuxetan.
Obinutuzumab The risk or severity of adverse effects can be increased when Triflusal is combined with Obinutuzumab.
Tipranavir Tipranavir may increase the antiplatelet activities of Triflusal.
Vitamin E Vitamin E may increase the antiplatelet activities of Triflusal.
Ginkgo biloba Ginkgo biloba may increase the anticoagulant activities of Triflusal.
Ifosfamide The risk or severity of bleeding can be increased when Ifosfamide is combined with Triflusal.
Quinine The therapeutic efficacy of Triflusal can be increased when used in combination with Quinine.
Quinidine The therapeutic efficacy of Triflusal can be increased when used in combination with Quinidine.
Tamoxifen The risk or severity of bleeding can be increased when Tamoxifen is combined with Triflusal.
Toremifene The risk or severity of bleeding can be increased when Toremifene is combined with Triflusal.
Pentoxifylline The therapeutic efficacy of Triflusal can be increased when used in combination with Pentoxifylline.
Pentosan polysulfate The risk or severity of adverse effects can be increased when Pentosan polysulfate is combined with Triflusal.
Levocarnitine The therapeutic efficacy of Triflusal can be increased when used in combination with Levocarnitine.
Diethylstilbestrol Diethylstilbestrol may decrease the anticoagulant activities of Triflusal.
Chlorotrianisene Chlorotrianisene may decrease the anticoagulant activities of Triflusal.
Conjugated estrogens Conjugated estrogens may decrease the anticoagulant activities of Triflusal.
Mestranol The risk or severity of adverse effects can be increased when Mestranol is combined with Triflusal.
Estrone sulfate Estrone sulfate may decrease the anticoagulant activities of Triflusal.
Quinestrol Quinestrol may decrease the anticoagulant activities of Triflusal.
Hexestrol Hexestrol may decrease the anticoagulant activities of Triflusal.
Synthetic Conjugated Estrogens, A Synthetic Conjugated Estrogens, A may decrease the anticoagulant activities of Triflusal.
Synthetic Conjugated Estrogens, B Synthetic Conjugated Estrogens, B may decrease the anticoagulant activities of Triflusal.
Polyestradiol phosphate Polyestradiol phosphate may decrease the anticoagulant activities of Triflusal.
Esterified estrogens Esterified estrogens may decrease the anticoagulant activities of Triflusal.
Zeranol Zeranol may decrease the anticoagulant activities of Triflusal.
Equol Equol may decrease the anticoagulant activities of Triflusal.
Methallenestril Methallenestril may decrease the anticoagulant activities of Triflusal.
Epimestrol Epimestrol may decrease the anticoagulant activities of Triflusal.
Moxestrol Moxestrol may decrease the anticoagulant activities of Triflusal.
Estradiol acetate Estradiol acetate may decrease the anticoagulant activities of Triflusal.
Estradiol benzoate Estradiol benzoate may decrease the anticoagulant activities of Triflusal.
Estradiol cypionate Estradiol cypionate may decrease the anticoagulant activities of Triflusal.
Estradiol valerate Estradiol valerate may decrease the anticoagulant activities of Triflusal.
Biochanin A Biochanin A may decrease the anticoagulant activities of Triflusal.
Formononetin Formononetin may decrease the anticoagulant activities of Triflusal.
Estriol Estriol may decrease the anticoagulant activities of Triflusal.
Limaprost The risk or severity of adverse effects can be increased when Limaprost is combined with Triflusal.
Icosapent The risk or severity of bleeding and hemorrhage can be increased when Icosapent is combined with Triflusal.
Mesalazine The risk or severity of bleeding can be increased when Mesalazine is combined with Triflusal.
Indomethacin The risk or severity of bleeding and hemorrhage can be increased when Indomethacin is combined with Triflusal.
Nabumetone The risk or severity of bleeding and hemorrhage can be increased when Nabumetone is combined with Triflusal.
Ketorolac The risk or severity of bleeding and hemorrhage can be increased when Ketorolac is combined with Triflusal.
Tenoxicam The risk or severity of bleeding and hemorrhage can be increased when Tenoxicam is combined with Triflusal.
Celecoxib The risk or severity of bleeding and hemorrhage can be increased when Celecoxib is combined with Triflusal.
Tolmetin The risk or severity of bleeding and hemorrhage can be increased when Tolmetin is combined with Triflusal.
Rofecoxib The risk or severity of bleeding and hemorrhage can be increased when Rofecoxib is combined with Triflusal.
Piroxicam The risk or severity of bleeding and hemorrhage can be increased when Piroxicam is combined with Triflusal.
Fenoprofen The risk or severity of bleeding and hemorrhage can be increased when Fenoprofen is combined with Triflusal.
Valdecoxib The risk or severity of bleeding and hemorrhage can be increased when Valdecoxib is combined with Triflusal.
Diclofenac The risk or severity of bleeding and hemorrhage can be increased when Diclofenac is combined with Triflusal.
Sulindac The risk or severity of bleeding and hemorrhage can be increased when Sulindac is combined with Triflusal.
Flurbiprofen The risk or severity of bleeding and hemorrhage can be increased when Flurbiprofen is combined with Triflusal.
Etodolac The risk or severity of bleeding and hemorrhage can be increased when Etodolac is combined with Triflusal.
Mefenamic acid The risk or severity of bleeding and hemorrhage can be increased when Mefenamic acid is combined with Triflusal.
Naproxen The risk or severity of bleeding and hemorrhage can be increased when Naproxen is combined with Triflusal.
Sulfasalazine The risk or severity of bleeding and hemorrhage can be increased when Sulfasalazine is combined with Triflusal.
Phenylbutazone The risk or severity of bleeding and hemorrhage can be increased when Phenylbutazone is combined with Triflusal.
Meloxicam The risk or severity of bleeding and hemorrhage can be increased when Meloxicam is combined with Triflusal.
Carprofen The risk or severity of bleeding and hemorrhage can be increased when Carprofen is combined with Triflusal.
Diflunisal The risk or severity of bleeding and hemorrhage can be increased when Diflunisal is combined with Triflusal.
Salicylic acid The risk or severity of bleeding and hemorrhage can be increased when Salicylic acid is combined with Triflusal.
Meclofenamic acid The risk or severity of bleeding and hemorrhage can be increased when Meclofenamic acid is combined with Triflusal.
Oxaprozin The risk or severity of bleeding and hemorrhage can be increased when Oxaprozin is combined with Triflusal.
Ketoprofen The risk or severity of bleeding and hemorrhage can be increased when Ketoprofen is combined with Triflusal.
Balsalazide The risk or severity of bleeding and hemorrhage can be increased when Balsalazide is combined with Triflusal.
Olsalazine The risk or severity of bleeding can be increased when Olsalazine is combined with Triflusal.
Lumiracoxib The risk or severity of bleeding and hemorrhage can be increased when Lumiracoxib is combined with Triflusal.
Magnesium salicylate The risk or severity of bleeding and hemorrhage can be increased when Magnesium salicylate is combined with Triflusal.
Salsalate The risk or severity of bleeding and hemorrhage can be increased when Salsalate is combined with Triflusal.
Choline magnesium trisalicylate The risk or severity of bleeding and hemorrhage can be increased when Choline magnesium trisalicylate is combined with Triflusal.
Antrafenine The risk or severity of bleeding and hemorrhage can be increased when Antrafenine is combined with Triflusal.
Aminophenazone The risk or severity of bleeding and hemorrhage can be increased when Aminophenazone is combined with Triflusal.
Antipyrine The risk or severity of bleeding and hemorrhage can be increased when Antipyrine is combined with Triflusal.
Tiaprofenic acid The risk or severity of bleeding and hemorrhage can be increased when Tiaprofenic acid is combined with Triflusal.
Etoricoxib The risk or severity of bleeding and hemorrhage can be increased when Etoricoxib is combined with Triflusal.

Target Protein

Prostaglandin G/H synthase 1 PTGS1
Nuclear factor NF-kappa-B p105 subunit NFKB1
Nitric oxide synthase, inducible NOS2
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A PDE10A

Referensi & Sumber

Artikel (PubMed)
  • PMID: 19465361
    Anninos H, Andrikopoulos G, Pastromas S, Sakellariou D, Theodorakis G, Vardas P: Triflusal: an old drug in modern antiplatelet therapy. Review of its action, use, safety and effectiveness. Hellenic J Cardiol. 2009 May-Jun;50(3):199-207.
  • PMID: 20184225
    Izquierdo I, Borja J, Rovira S, Pelagio P, Torres F, Cebrecos J, Garcia-Rafanell J: Comparative bioavailability study of triflusal oral solution vs. triflusal capsules in healthy subjects. A single, randomized, two-way cross-over, open-label phase I study. Arzneimittelforschung. 2010;60(1):36-41. doi: 10.1055/s-0031-1296246.
  • PMID: 18503633
    Duran X, Sanchez S, Vilahur G, Badimon L: Protective effects of triflusal on secondary thrombus growth and vascular cyclooxygenase-2. J Thromb Haemost. 2008 Aug;6(8):1385-92. doi: 10.1111/j.1538-7836.2008.03036.x. Epub 2008 May 22.
  • PMID: 18677970
    Quetglas EG, Campanero MA, Sadaba B, Escolar M, Azanza JR: Bioequivalence of two oral formulations of triflusal capsules in healthy volunteers. Arzneimittelforschung. 2008;58(6):283-7. doi: 10.1055/s-0031-1296508.
  • PMID: 16939630
    Gonzalez-Correa JA, De La Cruz JP: Triflusal: an antiplatelet drug with a neuroprotective effect? Cardiovasc Drug Rev. 2006 Spring;24(1):11-24.
  • PMID: 18053020
    Fraj J, Valero A, Vives R, Perez I, Borja J, Izquierdo I, Picado C: Safety of triflusal (antiplatelet drug) in patients with aspirin-exacerbated respiratory diseases. Allergy. 2008 Jan;63(1):112-5.
  • PMID: 15186390
    Sanchez-Machin I, Garcia Robaina JC, Torre Morin F: Widespread eczema from triflusal confirmed by patch testing. Contact Dermatitis. 2004 Apr;50(4):257.
  • PMID: 12649515
    Matias-Guiu J, Ferro JM, Alvarez-Sabin J, Torres F, Jimenez MD, Lago A, Melo T: 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. 2003 Apr;34(4):840-8. Epub 2003 Mar 20.
Menampilkan 8 dari 13 artikel.
Textbook
  • Bogousslavsky J. (2001). Drug Therapy for Stroke Prevention. Taylor and Francis.
Link

Contoh Produk & Brand

Produk: 0 • International brands: 3
International Brands
  • Aflen
  • Disgren
  • Grendis

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