Tranexamic acid is a synthetic derivative of the amino acid lysine. It is used to treat or prevent excessive blood loss during surgery and in various other medical conditions.

目錄

Basic Information

Properties

Pharmacology

Applications

Risk & Safety Info.

Specifications

Basic Information

Name： Tranexamic acid
Alternative Names：trans-4-(Aminomethyl)cyclohexanecarboxylic acid; AMCA;
CASN：1197-18-8
Formula：C8H15NO2
M.W.：157.21
EINECS： 214-818-2
MDL number：MFCD00001466
PubChem Substance ID：24888448

Properties

Appearance: White crystalline powder
Solubility: Easy to dissolve in the water and the glacial acetic acid, difficult to dissolve in the acetone and the ethyl alcohol
mp：>300 °C (lit.)

Pharmacology

Applications

Tranexamic acid is frequently used in surgeries with high risk of blood loss such as cardiac, liver, vascular and large orthopedic procedures. Its oral form is now being evaluated for use in outpatient conditions involving heavy bleeding.
Trauma
Tranexamic acid has been found to decrease the risk of death in people who have significant bleeding due to trauma. However, it may actually increase the risk of death due to bleeding if administered more than 3 hours after the injury.
Heart surgery
Tranexamic acid is commonly used in cardiac surgery, both with and without cardiopulmonary bypass. It replaces aprotinin.
Orthopedic surgery
Tranexamic acid is used in orthopedic surgery to reduce bloodloss. It is of proven value in clearing the field of surgery and reducing pre- and postoperative blood loss. Drain and number of transfusions are reduced. However, the hidden blood loss is not reduced. Still, it is becoming an important tool in the anaesthetist's arsenal. It is commonly used in joint replacement surgery.
Menstrual bleeding
Used as firstline nonhormonal treatment of dysfunctional uterine bleeding, and heavy bleeding associated with uterine fibroids. A recent study showed patients treated with tranexamic acid are more likely to develop thrombosis and necrosis in their fibroids, and may result in pain and fever. Moreover, the histological appearance of the necrosis in women treated by tranexamic acid is no different from the spontaneous incidence of thrombosis. The U.S. Food and Drug Administration (FDA) approved tranexamic acid oral tablets (brand name Lysteda) for treatment of heavy menstrual bleeding on 13 November 2009.
Dentistry
Tranexamic acid is used in dentistry in the form of a 5% mouth rinse after extractions or surgery in patients with prolonged bleeding time, e.g. from acquired or inherited disorders.
Other uses
In obstetrics, tranexamic acid is used after delivery to reduce bleeding, often with syntocinon/oxytocin and fundal massage. A major trial is in progress worldwide to establish the efficacy of the drug to arrest postpartum haemorrhage (PPH). Since the drug can be administered orally, it has great potential to reduce maternal mortality rates in developing countries where primary healthcare is often unavailable.

In cardiac surgery, e.g. coronary artery bypass surgery, it is used to prevent excessive blood loss.

In hemophilia - Tranexamic acid is also useful in the treatment of bleeding as a second line treatment after factor VIII in patients (e.g. tooth extraction).
Whitening effect
Clinical studies for years have proved that tranexamic acid can dilute spot effectively and rapidly, which helps to demonstrate a perfect white and bright skin. The spot-removing effect of tranexamic acid is about 50 times over Vitamin C, and 10 times over AHA. The concentration limit of usage is 2%-3%, and in cosmetics the amount is around 0.5%.

Risk & Safety Info.

Pictogram

GHS07

Signal Word

Warning

Risk statement

H315
H319
H335

Precautionary statement

P261
P305 + P351 + P338

Personal proctection equipment

dust mask type N95 (US), Eyeshields, Gloves

Hazardous code

Xi

Risk phrases

36/37/38

Safety phrases

26-36

WGK Germany

3

RTECS

3

Specifications

Items of Test

Specifications

Characteristics

White crystalline powder

Identification

Infrared absorption spectrophotometry (2.2.24)IR spectrum is in concordance with Tranexamic acid CRS

Solubility

Easy to dissolve in the water and the glacial acetic acid, difficult to dissolve in the acetone and the ethyl alcohol

PH

7.0–8.0

Chloride

≤0.014%

Heavy metals

≤10ppm

Sulfated ash

≤0.1%

Loss on drying

≤0.5%

Related substances (HPLC)

Impurity A : ≤0.1%

Impurity B

<0.2%

Any other impurity

<0.1%

All other impurity

<0.2%

Assay

99.0%–101.0%