Peringatan Keamanan

Reported symptoms of tranexamic acid overdose include severe gastrointestinal symptoms, hypotension, thromboembolism, visual impairment, convulsions, mental status changes, and rash.L31853,L31858

Tranexamic acid

DB00302

small molecule approved

Deskripsi

Tranexamic acid is a synthetic derivative of lysine used as an antifibrinolytic in the treatment and prevention of major bleeding. It possesses a similar mechanism of action to aminocaproic acid but is approximately 10-fold more potent.L31883

It was first patented in 1957A230108 and received its initial US approval in 1986.L31858

Struktur Molekul 2D

Berat 157.2102
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Following intravenous administration, the apparent elimination half-life is approximately 2 hours and the mean terminal half-life is approximately 11 hours.[L31858]
Volume Distribusi The initial volume of distribution of tranexamic acid is 0.18 L/kg and its steady-state volume of distribution is 0.39 L/kg.[L31858] Tranexamic acid distributes into cerebrospinal fluid and the aqueous humor of the eye at concentrations approximately 1/10th of typical plasma concentrations. Tranexamic acid is also able to cross the placenta, found in cord blood at concentrations equivalent to maternal plasma concentrations.[L31858]
Klirens (Clearance) The plasma clearance of tranexamic acid is 110-116 mL/min.[L31858]

Absorpsi

The bioavailability of tranexamic acid after oral administration in humans is approximately 30 to 50% of the ingested dose and is not affected by food intake.L31858 The Cmax and Tmax following multiple oral doses (1300 mg three times daily x 5 days) were 16.41 mcg/mL and 2.5 h, respectively.L31858

Metabolisme

Tranexamic acid metabolism is poorly characterized but does not appear to be a significant means of drug elimination. According to prescribing information, approximately 1% and 0.5% of an orally administered dose are excreted as a dicarboxylic acid and acetylated metabolite, respectively.L31858

Rute Eliminasi

Urinary excretion is the primary means of tranexamic acid elimination, with >95% of an administered dose excreted in the urine as unchanged parent drug.L31858 The rate of excretion is dependent on the route of administration - approximately 90% of an intravenously administered dose is excreted within 24 hours whereas only 39% of an orally administered dose is excreted within the same time frame.L31883

Interaksi Makanan

1 Data
  • 1. Take with or without food. The co-administration of food does not significantly affect tranexamic acid disposition.

Interaksi Obat

106 Data
Nonoxynol-9 Tranexamic acid may increase the thrombogenic activities of Nonoxynol-9.
Segesterone acetate Tranexamic acid may increase the thrombogenic activities of Segesterone acetate.
Alpha-1-proteinase inhibitor Alpha-1-proteinase inhibitor may increase the thrombogenic activities of Tranexamic acid.
Menadione Menadione may increase the thrombogenic activities of Tranexamic acid.
Aminocaproic acid Tranexamic acid may increase the thrombogenic activities of Aminocaproic acid.
Aprotinin Tranexamic acid may increase the thrombogenic activities of Aprotinin.
Hydrogen peroxide Tranexamic acid may increase the thrombogenic activities of Hydrogen peroxide.
Aminomethylbenzoic acid Tranexamic acid may increase the thrombogenic activities of Aminomethylbenzoic acid.
Camostat Tranexamic acid may increase the thrombogenic activities of Camostat.
Menadione bisulfite Tranexamic acid may increase the thrombogenic activities of Menadione bisulfite.
Diethylstilbestrol Diethylstilbestrol may increase the thrombogenic activities of Tranexamic acid.
Etonogestrel Etonogestrel may increase the thrombogenic activities of Tranexamic acid.
Desogestrel Desogestrel may increase the thrombogenic activities of Tranexamic acid.
Megestrol acetate Megestrol acetate may increase the thrombogenic activities of Tranexamic acid.
Levonorgestrel Levonorgestrel may increase the thrombogenic activities of Tranexamic acid.
Progesterone Progesterone may increase the thrombogenic activities of Tranexamic acid.
Medroxyprogesterone acetate Medroxyprogesterone acetate may increase the thrombogenic activities of Tranexamic acid.
Norethisterone Norethisterone may increase the thrombogenic activities of Tranexamic acid.
Estradiol Estradiol may increase the thrombogenic activities of Tranexamic acid.
Ethynodiol diacetate Ethynodiol diacetate may increase the thrombogenic activities of Tranexamic acid.
Mifepristone Mifepristone may increase the thrombogenic activities of Tranexamic acid.
Norgestimate Norgestimate may increase the thrombogenic activities of Tranexamic acid.
Ethinylestradiol Ethinylestradiol may increase the thrombogenic activities of Tranexamic acid.
Mestranol Mestranol may increase the thrombogenic activities of Tranexamic acid.
Drospirenone Drospirenone may increase the thrombogenic activities of Tranexamic acid.
Estrone sulfate Estrone sulfate may increase the thrombogenic activities of Tranexamic acid.
Octylphenoxy polyethoxyethanol Octylphenoxy polyethoxyethanol may increase the thrombogenic activities of Tranexamic acid.
Cyproterone acetate Cyproterone acetate may increase the thrombogenic activities of Tranexamic acid.
Trestolone Trestolone may increase the thrombogenic activities of Tranexamic acid.
Norelgestromin Norelgestromin may increase the thrombogenic activities of Tranexamic acid.
Gestodene Gestodene may increase the thrombogenic activities of Tranexamic acid.
Hydroxyprogesterone caproate Hydroxyprogesterone caproate may increase the thrombogenic activities of Tranexamic acid.
Ulipristal Ulipristal may increase the thrombogenic activities of Tranexamic acid.
Dienogest Dienogest may increase the thrombogenic activities of Tranexamic acid.
Norethynodrel Norethynodrel may increase the thrombogenic activities of Tranexamic acid.
Norgestrel Norgestrel may increase the thrombogenic activities of Tranexamic acid.
Cloprostenol Cloprostenol may increase the thrombogenic activities of Tranexamic acid.
Gestrinone Gestrinone may increase the thrombogenic activities of Tranexamic acid.
Nomegestrol Nomegestrol may increase the thrombogenic activities of Tranexamic acid.
Lynestrenol Lynestrenol may increase the thrombogenic activities of Tranexamic acid.
Gossypol Gossypol may increase the thrombogenic activities of Tranexamic acid.
Ormeloxifene Ormeloxifene may increase the thrombogenic activities of Tranexamic acid.
Chlormadinone Chlormadinone may increase the thrombogenic activities of Tranexamic acid.
Norgestrienone Norgestrienone may increase the thrombogenic activities of Tranexamic acid.
Quingestanol Quingestanol may increase the thrombogenic activities of Tranexamic acid.
Demegestone Demegestone may increase the thrombogenic activities of Tranexamic acid.
Etynodiol Etynodiol may increase the thrombogenic activities of Tranexamic acid.
Testosterone enanthate Testosterone enanthate may increase the thrombogenic activities of Tranexamic acid.
Estradiol benzoate Estradiol benzoate may increase the thrombogenic activities of Tranexamic acid.
Estradiol cypionate Estradiol cypionate may increase the thrombogenic activities of Tranexamic acid.
Estradiol valerate Estradiol valerate may increase the thrombogenic activities of Tranexamic acid.
Nomegestrol acetate Nomegestrol acetate may increase the thrombogenic activities of Tranexamic acid.
Norethindrone enanthate Norethindrone enanthate may increase the thrombogenic activities of Tranexamic acid.
Fibrinogen human The therapeutic efficacy of Fibrinogen human can be increased when used in combination with Tranexamic acid.
Antihemophilic factor, human recombinant Tranexamic acid may increase the thrombogenic activities of Antihemophilic factor, human recombinant.
Coagulation factor VIIa Recombinant Human Tranexamic acid may increase the thrombogenic activities of Coagulation factor VIIa Recombinant Human.
Coagulation Factor IX (Recombinant) Tranexamic acid may increase the thrombogenic activities of Coagulation Factor IX (Recombinant).
Calcium Tranexamic acid may increase the thrombogenic activities of Calcium.
Pantothenic acid Tranexamic acid may increase the thrombogenic activities of Pantothenic acid.
Formic acid Tranexamic acid may increase the thrombogenic activities of Formic acid.
Platelet Activating Factor Tranexamic acid may increase the thrombogenic activities of Platelet Activating Factor.
Turoctocog alfa Tranexamic acid may increase the thrombogenic activities of Turoctocog alfa.
Catridecacog Tranexamic acid may increase the thrombogenic activities of Catridecacog.
Antihemophilic factor (recombinant), PEGylated Tranexamic acid may increase the thrombogenic activities of Antihemophilic factor (recombinant), PEGylated.
Prothrombin Tranexamic acid may increase the thrombogenic activities of Prothrombin.
Factor IX Complex (Human) Tranexamic acid may increase the thrombogenic activities of Factor IX Complex (Human).
Susoctocog alfa Tranexamic acid may increase the thrombogenic activities of Susoctocog alfa.
Eftrenonacog alfa Tranexamic acid may increase the thrombogenic activities of Eftrenonacog alfa.
Rusalatide acetate Tranexamic acid may increase the thrombogenic activities of Rusalatide acetate.
Vatreptacog alfa Tranexamic acid may increase the thrombogenic activities of Vatreptacog alfa.
Factor XIII (human) Tranexamic acid may increase the thrombogenic activities of Factor XIII (human).
Von Willebrand factor human Tranexamic acid may increase the thrombogenic activities of Von Willebrand factor human.
Coagulation factor X human Tranexamic acid may increase the thrombogenic activities of Coagulation factor X human.
Coagulation factor VII human Tranexamic acid may increase the thrombogenic activities of Coagulation factor VII human.
Anti-inhibitor coagulant complex Tranexamic acid may increase the thrombogenic activities of Anti-inhibitor coagulant complex.
Coagulation Factor IX Human Tranexamic acid may increase the thrombogenic activities of Coagulation Factor IX Human.
Antihemophilic factor human Tranexamic acid may increase the thrombogenic activities of Antihemophilic factor human.
Kallidinogenase Tranexamic acid may increase the thrombogenic activities of Kallidinogenase.
Trenonacog alfa Tranexamic acid may increase the thrombogenic activities of Trenonacog alfa.
Albutrepenonacog alfa Tranexamic acid may increase the thrombogenic activities of Albutrepenonacog alfa.
Emicizumab Tranexamic acid may increase the thrombogenic activities of Emicizumab.
Nonacog beta pegol Tranexamic acid may increase the thrombogenic activities of Nonacog beta pegol.
Moroctocog alfa Tranexamic acid may increase the thrombogenic activities of Moroctocog alfa.
Beroctocog alfa Tranexamic acid may increase the thrombogenic activities of Beroctocog alfa.
Andexanet alfa Tranexamic acid may increase the thrombogenic activities of Andexanet alfa.
Calcium cation Tranexamic acid may increase the thrombogenic activities of Calcium cation.
Damoctocog alfa pegol Tranexamic acid may increase the thrombogenic activities of Damoctocog alfa pegol.
Turoctocog alfa pegol Tranexamic acid may increase the thrombogenic activities of Turoctocog alfa pegol.
Alteplase The therapeutic efficacy of Tranexamic acid can be decreased when used in combination with Alteplase.
Urokinase The therapeutic efficacy of Tranexamic acid can be decreased when used in combination with Urokinase.
Reteplase The therapeutic efficacy of Tranexamic acid can be decreased when used in combination with Reteplase.
Anistreplase The therapeutic efficacy of Tranexamic acid can be decreased when used in combination with Anistreplase.
Tenecteplase The therapeutic efficacy of Tranexamic acid can be decreased when used in combination with Tenecteplase.
Streptokinase The therapeutic efficacy of Tranexamic acid can be decreased when used in combination with Streptokinase.
Lanoteplase The therapeutic efficacy of Tranexamic acid can be decreased when used in combination with Lanoteplase.
Amediplase The therapeutic efficacy of Tranexamic acid can be decreased when used in combination with Amediplase.
Saruplase The therapeutic efficacy of Tranexamic acid can be decreased when used in combination with Saruplase.
Tretinoin The risk or severity of hypercoagulability can be increased when Tretinoin is combined with Tranexamic acid.
Protein S human Tranexamic acid may increase the thrombogenic activities of Protein S human.
Rurioctocog alfa pegol Tranexamic acid may increase the thrombogenic activities of Rurioctocog alfa pegol.

Target Protein

Plasminogen PLG

Referensi & Sumber

Synthesis reference: Noa Zerangue, Bernd Jandeleit, Yunxiao Li, "Acyloxyalkyl carbamate prodrugs of tranexamic acid, methods of synthesis and use." U.S. Patent US20070027210, issued February 01, 2007.
Artikel (PubMed)
  • PMID: 11907171
    Furtmuller R, Schlag MG, Berger M, Hopf R, Huck S, Sieghart W, Redl H: Tranexamic acid, a widely used antifibrinolytic agent, causes convulsions by a gamma-aminobutyric acid(A) receptor antagonistic effect. J Pharmacol Exp Ther. 2002 Apr;301(1):168-73. doi: 10.1124/jpet.301.1.168.
  • PMID: 25797505
    Ng W, Jerath A, Wasowicz M: Tranexamic acid: a clinical review. Anaesthesiol Intensive Ther. 2015;47(4):339-50. doi: 10.5603/AIT.a2015.0011. Epub 2015 Mar 23.
  • PMID: 15730382
    Gompels MM, Lock RJ, Abinun M, Bethune CA, Davies G, Grattan C, Fay AC, Longhurst HJ, Morrison L, Price A, Price M, Watters D: C1 inhibitor deficiency: consensus document. Clin Exp Immunol. 2005 Mar;139(3):379-94. doi: 10.1111/j.1365-2249.2005.02726.x.

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Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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