Tranexaminsure

Gefahreninformationscode (GHS)

• Bildanzeige (GHS)

  

• Alarmwort

  Warnung

• Gefahrenhinweise

  H315：Verursacht Hautreizungen.

  H319：Verursacht schwere Augenreizung.

  H335：Kann die Atemwege reizen.

• Sicherheit

  P261：Einatmen von Staub vermeiden.

  P264：Nach Gebrauch gründlich waschen.

  P264：Nach Gebrauch gründlich waschen.

  P271：Nur im Freien oder in gut belüfteten Räumen verwenden.

  P280：Schutzhandschuhe/Schutzkleidung/Augenschutz tragen.

  P302+P352：BEI BERÜHRUNG MIT DER HAUT: Mit viel Wasser/... (Hersteller kann, falls zweckmäßig, ein Reinigungsmittel angeben oder, wenn Wasser eindeutig ungeeignet ist, ein alternatives Mittel empfehlen) waschen.

  P305+P351+P338：BEI KONTAKT MIT DEN AUGEN: Einige Minuten lang behutsam mit Wasser spülen. Eventuell vorhandene Kontaktlinsen nach Möglichkeit entfernen. Weiter spülen.

Tranexamic Acid Chemische Eigenschaften,Einsatz,Produktion Methoden

• R-Sätze Betriebsanweisung:

  R36/37/38:Reizt die Augen, die Atmungsorgane und die Haut.

• S-Sätze Betriebsanweisung:

  S26:Bei Berührung mit den Augen sofort gründlich mit Wasser abspülen und Arzt konsultieren.
  S36:DE: Bei der Arbeit geeignete Schutzkleidung tragen.
  S37/39:Bei der Arbeit geeignete Schutzhandschuhe und Schutzbrille/Gesichtsschutz tragen.

• Beschreibung

  Tranexamic acid is a derivative of aminomethylbenzoic acid, and a kind of antifibrinolytic drugs to stop bleeding. The hemostasis mechanism of tranexamic acid is similar to aminocaproic acid and aminomethylbenzoic acid, but the effect is stronger. The strength is 7 to 10 times of aminocaproic acid, 2 times of aminomethylbenzoic acid, but toxicity is similar.
  The chemical structure of tranexamic acid is similar to lysine, competitive inhibition of plasmin original in fibrin adsorption, to prevent their activation, protection fiber protein not to degrade by plasmin and dissolve, eventually achieve hemostasis. Applicable in the treatment of acute or chronic, localized or systemic primary fiber fibrinolytic hyperthyroidism caused by bleeding, such as obstetric hemorrhage, renal hemorrhage, hemorrhage of hypertrophy of the prostate, hemophilia, pulmonary tuberculosis hemoptysis, stomach bleeding, after operation of liver, lung, spleen and other viscera hemorrhage; also can be used in surgery when abnormal bleeding etc..
  Clinical tranexamic acid has effect significantly to insect bites disease, dermatitis and eczema, simple purpura, chronic urticaria, artificial sex urticaria, toxic eruption and eruption. And also has a certain effect on erythroderma, scleroderma, systemic lupus erythematosus (SLE), Erythema multiforme, shingles and alopecia areata. Treatment of hereditary angioedema effect is also good. In the treatment of Chloasma, general medicine is effective about 3 weeks, markedly effective 5 weeks, a course of 60 days. Given orally in doses of 0.25 ~ 0.5 g, a day 3 ~ 4 times. A few patients can nausea, fatigue, pruritus, abdominal discomfort, and diarrhea side effects after withdrawal symptoms disappear.

• Chemische Eigenschaften

  Tranexamic acid is a White or almost white, crystalline powder. It is freely soluble in water and in glacial acetic acid and is very slightly soluble in ethanol and practically insoluble in ether.

• Originator

  Anvitoff,Knoll,W. Germany,1967

• Verwenden

  Fibrinolysis, the cleavage of fibrin by plasmin, is a normal step in the dissolution of fibrin clots after wound repair. Tranexamic acid is an inhibitor of fibrinolysis that blocks the interaction of plasmin with fibrin (IC50 = 3.1 μM). It is a lysine mimetic that binds the lysine binding site in plasmin. Antifibrinolytic agents have value when fibrinolytic activity is abnormally high or when coagulation is impaired.

• Definition

  ChEBI: Tranexamic acid is a monocarboxylic acid. It has a role as an antifibrinolytic drug and a hematologic agent. It is functionally related to a cyclohexanecarboxylic acid.

• Indications

  Various bleedings caused by acute or chronic, localized or systemic primary hyperfibrinolysis; secondary hyperfibrinolytic state caused by disseminated intravascular coagulation. Generally do not use this product before heparinization.
  Trauma or surgical bleeding in tissue and organs with abundant plasminogen activators such as prostate, urethra, lung, brain, uterus, adrenal glands, and thyroid.
  An antagonist of tissue plasminogen activator (t-PA), streptokinase, and urokinase.
  Fibrinolytic hemorrhage caused by artificial abortion, early placental detachment, stillbirth and amniotic fluid embolism; and increased menorrhagia caused by pathological intrauterine fibrinolysis.
  Cerebral neuropathy mild bleeding, such as subarachnoid hemorrhage and intracranial aneurysm hemorrhage, the effect of Amstat in this condition is better than that of other anti-fibrinolytic agents. Special attention must be paid to the risk of cerebral edema or cerebral infarction.For severe patients with surgical indications, this product can only be used as an adjuvant drug.
  For the treatment of hereditary angioneurotic edema, it can reduce the number and severity of episodes.
  Used in patients with hemophilia for their active hemorrhage in combination with others drug.
  Hemophilia patients with factor VIII or factor IX deficiency in their tooth extraction or oral surgery in case of operating bleeding.

• Manufacturing Process

  In an autoclave, 2 grams of a mixture of cis- and trans-4- aminomethylcyclohexane-1-carboxylic acid, which is obtained by catalytic reduction of p-aminomethylbenzoic acid in the presence of platinum catalyst and contains 60% by weight of cis-isomer was reacted at 200°C, for 8 hours with 20 ml of ethyl alcohol in which 0.44 gram of sodium metal had been dissolved. After cooling, the reaction solution was concentrated under a reduced pressure to give a white residue. This residue was dissolved in 40 ml of water and passed through a column of a strongly acidic cation ion_x0002_exchanger resin (NH4+). The eluate was concentrated under reduced pressure to form a white mass. An adequate amount of acetone was added thereto and 1.95 grams of white powder was obtained. This powder was recrystallized from water-acetone to give 1.85 grams (yield, 92.5%) of white crystalline powder having a melting point of 380° to 390°C (decomposition). This product was identified as trans-4-aminomethylcyclohexane-1-carboxylic acid by means of infrared spectrum.

• Therapeutic Function

  Coagulant

• Allgemeine Beschreibung

  Tranexamic acid is an antifibrinolytic agent and is commonly used for heavy menstrual bleeding.

• Mechanism of action

  Tranexamic acid is a synthetic lysine amino acid derivative, which diminishes the dissolution of hemostatic fibrin by plasmin. In the presence of tranexamic acid, the lysine receptor binding sites of plasmin for fibrin are occupied, preventing binding to fibrin monomers, thus preserving and stabilizing fibrin’s matrix structure. This agent has a longer half-life, is approximately ten times more potent, and is less toxic than aminocaproic acid, which possesses similar mechanisms of action.

• Clinical Use

  Haemostatic agent

• Nebenwirkungen

  Tranexamic acid is mostly well-tolerated.
  Common
  nausea (upset stomach)
  vomiting (throwing up)
  diarrhea
  headache
  
  Occasional
  dizziness
  giddiness
  vision changes
  
  Rare
  stroke
  blood clots in undesired areas
  deep vein thrombosis

• Synthese

  Tranexamic acid, trans-4-(aminomethyl)cyclohexane carboxylic acid (24.4.5), is synthesized from 4-methylbenzonitrile. Oxidation of the methyl group gives the mononitrile of terephthalic acid 24.4.2. The cyano group in this compound is reduced by hydrogen using Raney nickel as a catalyst. The benzene ring of the resulting 4- aminomethylbenzoic acid (24.4.3) is reduced to a cyclohexane moiety by hydrogen and a platinum catalyst, which forms an isomeric mixture of 4-aminomethylcyclohexane carboxylic acids (24.4.4), and the desired trans-isomer 24.4.5 is isolated by crystallization of the mixture of its sodium salts.

  

• target

  GABA Receptor

• Stoffwechsel

  Tranexamic acid is excreted as unchanged drug mainly by urinary excretion via glomerular filtration.

• Pharmakokinetik

  Tranexamic acid 1 g was given intravenously to three healthy volunteers. Plasma concentrations decayed in three monoexponential phases. Most elimination occurred during the first eight hours, giving an apparent elimination half-life of approximately two hours. Plasma clearance ranged between 110-116 ml/min. The urinary recovery of tranexamic acid exceeded 95% of the dose. The oral bioavailability of tranexamic acid, calculated from 24-hour urinary excretion after oral and intravenous administration, was 34% of the dose[1].

• Einzelnachweise

  Intravenous use of tranexamic acid reduces postoperative blood loss in total knee arthroplasty DOI:10.1007/s00402-014-2081-x
  www.childrensmn.org
  dermnetnz.org
  Tranexamic acid for the prevention and treatment of postpartum haemorrhage. DOI:10.1097/01.aoa.0000552886.12061.3c
  Sittig's Pharmaceutical Manufacturing Encyclopedia
  The Renal Drug Handbook
  Synthesis of Essential Drugs (2006, Elsevier) - libgen.lc
  Spectrophotometric and spectrofluorimetric methods for the determination of tranexamic acid in pharmaceutical formulation. DOI:10.1248/CPB.55.364
  Determination of plasma tranexamic acid using cation-exchange high-performance liquid chromatography with fluorescence detection. DOI:10.1016/S0378-4347(00)84573-9
  [1] A Pilbrant, J Vessman, M Schannong. “Pharmacokinetics and bioavailability of tranexamic acid.” European Journal of Clinical Pharmacology 20 1 (1981): 65–72.    

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