Tranexamic Acid

A synthetic derivative of the amino acid lysine.

Used to treat or prevent excessive blood loss during surgery and other medical conditions.

An antifibrinolytic that competitively inhibits the activation of plasminogen to plasmin.

Itcompetes with lysine residues on fibrin for the binding of plasminogen, inhibiting the interaction of plasmin with fibrin and preventing the dissolution of fibrin clots.

Binds to specific sites of both plasminogen and plasmin.

Exerts its antifibrinolytic effect through the reversible blockade of lysine-binding sites on plasminogen.

Inhibits endothelial plasminogen activator and thus prevents fibrinolysis and the breakdown of blood clots.

Plasmin is responsible for the degradation of fibrin.

In the presence of the tranexamic acid,lysine receptor binding sites of plasmin for fibrin are occupied, preventing by binding to fibrin monomers, thus maintaining fibrin’s structure and prevent think it’s breakdown.

Has approximately 8 times the antifibrinolytic activity of ε-aminocaproic acid.

Frequently used in surgeries with high risk of blood loss such as cardiac, liver, vascular and large orthopedic procedures.

Used to prevent bleeding in patients undergoing elective orthopedic surgeries, including major surgery on the hip or knee.

In surgical patients are given tranexamic acid just before surgery, patients bleed less than if you give a placebo.

Among patients undergoing noncardiac surgery, the incidence of bleeding  outcome was significantly lower with tranexamic acid than with placebo (POISE-3 investigators).

Reduces the risk of death from bleeding in randomized trials of patients with traumatic or postpartum hemorrhage.

Research has also shown that TXA reduces risk of bleeding in women with postpartum hemorrhage.

It can be given systemically or locally and reduces the need for blood products.

IV-TXA significantly reduces intraoperative blood loss following total joint arthroplasty.

IV-TXA minimizes postoperative anemia, facilitating improved early ambulation following total joint arthroplasty.

Not presently used in emergency orthopedic surgeries.

Decreases the risk of death in people who have significant bleeding due to trauma.

Used to treat or prevent excessive blood loss, significantly reduces mortality from traumatic brain injury (TBI).

In a randomized controlled study of patients with moderate or severe traumatic brain injury the use of out-of-hospital  tranexamic acid did not improve outcomes (Rowell SE).

Among adults with major trauma and suspected trauma induced coagulopathy, prehospital administration of tranexamic acid, followed by infusion over eight hours did not result in a greater number of patients surviving with a favorable functional outcome at six months, than placebo (AMZIS  Clinical Trial Group).

In cardiac surgery it replaces aprotinin.

Used in orthopedic surgery to reduce blood loss.

Helps in the clearing the field of surgery and reducing pre- and postoperative blood loss in orthopedic surgery.

Side effects, uncommon.

Prolonged use may increase the risk of thromboembolic changes, such as deep vein thrombosis.

Has been used as first-line non-hormonal therapy for dysfunctional uterine bleeding, and had the bleeding due to fibroids.

In severe epistaxis can be used by inserting a tampon saturated with tranexamic acid and a local vasoconstrictor such as metolazone into the nose.

Oral agent Lysteda.

Used in dentistry in the form of a 5% mouth rinse in patients with prolonged bleeding time.

In obstetrics, may be used after delivery to reduce bleeding, often with oxytocin and fundal massage.

Can be used to treat hyphema, the bleeding into the anterior chamber of the eye.

Tranexamic acid is effective at preventing perioperative blood loss compared with the placebo in patients undergoing TURP: this treatment was not effective neither at preventing the need for transfusions nor to increase hemoglobin values at the end of the procedure. 

CRASH-2 study a randomized multinational trial of tranexamic acid versus placebo in adult trauma patients with significant bleeding: when given within eight hours of injury, this agent significantly reduced the risk of all caused mortality by about 1/10 and death due to bleeding by 1/6, with no increased risk of thromboembolic phenomena.

CRASH-2 did not reduce number of blood transfusions.

Some trauma centers use tranexamic acid with hemorrhage and trauma and others administered it in emergency trauma cases accompanied by shock.

TXA is administered within the first three hours after trauma.

It is difficult to rapidly establish the presence of fibrinolysis with present laboratory methods

Many randomized controlled trials have shown efficacy in preventing bleeding in heart surgery, liver transplant, elective orthopedic surgery, and probably in trauma cases.

It is the main anti-fibrogenic agent for mitigating bleeding in patients undergoing cardiac surgery

TXA may allow reversal of bleeding more quickly and the use of less blood components in patients with severe shock.

Among women who undergo cesarean delivery tranexamic acid treatment result in significant lower incidence of blood loss greater than 1000cc or red cell transfusions by day 2 than placebo, but it does not result in a lower incidence of hemorrhage related secondary clinical outcomes.

The incidence of induced thrombosis with the use of TXA is unknown, but the CRASH-2 study showed no increase in incidence of thrombosis.

Non-randomized controlled trials have shown increased incidence of venous thromboembolism and the hypercoagulable state can manifest hours, days, or even weeks after trauma.

It is possible this hypercoagulable state, named fibrinolytic shut down, develops an increased risk for mortality due to the obstruction of the microvasculature that may be related to TXA.

Associated with increased seizures and strokes attributable to local cerebral thrombotic complications caused by TXA during cardiac surgery.

TXA significantly reduces mortality in combat injuries and uses less blood, but there is a 9-12 increase in venous thromboembolism.

Tranexamic acid appears to improve quality of life for adolescents with heavy menstrual bleeding.

Can be administered orally (typical dose 15-25 mg/kg, 3 times a day), as a mouthwash (typical dose 10 mL of 5% weight-to-volume ratio solution, 4 times a day), or IV (typical dose 15 mg/kg, 3 times a day) for von Willebrand disease.

Adverse effects associated with use of tranexamic acid include nausea, vomiting, and abdominal pain.

It is generally avoided in patients with significant hematuria to prevent ureteric clot colic and obstruction.

Although concerns regarding possible thromboembolic risk with tranexamic acid therapy have been expressed, recent systematic reviews have failed to demonstrate any significant increased risk.

Drug Delivers ‘Remarkable’ Reduction in Head Injury Deaths

Tranexamic acid (TXA) is an antifibrinolytic agent used to treat or prevent excessive blood loss, significantly reduces mortality from traumatic brain injury (TBI).

Administration of tranexamic acid within 3 hours of head trauma is associated with a 20% reduction in deaths among those with mild to moderate TBI, with no evidence of adverse effects or complications.

No apparent reduction in mortality among those with severe head injury with tranexamic acid therapy.

It is the first drug can reduce mortality after traumatic brain injury.

It could save hundreds of thousands of lives worldwide, if all trauma patients get tranexamic acid at the scene of the injury or as soon as possible thereafter.

More than 60 million new cases of traumatic brain injuries occur worldwide every year, and the number is rising.

Motor vehicle accidents and falls are the main causes of traumatic brain injuries.

Intracranial bleeding is a common complication of TBI, and can lead to an increase in intracranial pressure, as well as brain herniation and death.

In the perioperative ischemic evaluation-3 (POISE-3) trial of 9535 patients at increased cardiovascular risk scheduled to undergo noncardiac surgery and who were randomly assigned to receive tranexamic acid or placebo at the start and end of surgery: at 30 days  incidence of composite bleeding outcome of life-threatening bleeding, major bleeding, bleeding into a critical organ was 24% lower with tranexamic acid them when placebo.

With respect to the composite cardiovascular outcome, noninferiority was not met with the cardiovascular outcome event occurring in 14.2% of the patients in the tranexamic acid group acid group, and 13.9% in the placebo group (Devereaux PJ).

Among patients who underwent cardiac surgery with cardiopulmonary bypass, high dose tranexamic acid infusion versus low-dose tranexamic infusion resulted in significant reduction in the proportion of patients who received red blood cell transfusions and make criteria for non inferiority with respect to primary safety endpoint consisting of 30 day mortality, seizure, kidney dysfunction, and thrombotic events (Shi J).

The prophylactic use of tranexamic acid during cesarean delivery does not lead to significantly lower risk of outcome of maternal death or blood transfusion than placebo.

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