Antifibrinolytics Explained: Agents, Mechanisms, Uses, and Safety Profile

Antifibrinolytics: List of Agents, Mechanism of Action, Indications, Adverse Effects & Contraindications

Introduction to Antifibrinolytics

Definition: Antifibrinolytics are drugs that inhibit fibrinolysis (the breakdown of fibrin), stabilizing clots.
Purpose: Reduce bleeding in surgery, trauma, or disorders with hyperfibrinolysis.

List of Antifibrinolytic Agents

Synthetic Lysine Analogs:

Epsilon Aminocaproic Acid (EACA)
Tranexamic Acid (TXA)

Protease Inhibitor:

Aprotinin (Bovine origin)

Mechanism of Action

EACA & TXA:

Inhibit activation of plasminogen to plasmin.
Block lysine binding sites on plasminogen/plasmin.

Aprotinin:

Serine protease inhibitor.
Inhibits plasmin, kallikrein, and trypsin.

Indications

EACA:

Cardiac surgery
Hemophilia
Urinary bleeding

Tranexamic Acid:

Trauma-associated bleeding
Heavy menstrual bleeding
Dental procedures in hemophilia
Surgery (e.g., orthopedic, cardiac)

Aprotinin (historical use):

Cardiac surgery to reduce blood loss (limited due to safety concerns)

Adverse Effects

EACA:

Hypotension (if given IV too rapidly)
Muscle necrosis
Thrombosis

Tranexamic Acid:

Nausea, vomiting
Visual disturbances (rare)
Risk of thrombosis (controversial)

Aprotinin:

Anaphylaxis (especially with repeat use)
Renal dysfunction
Increased mortality (led to withdrawal in some regions)

Contraindications

EACA:

Active intravascular clotting
Disseminated intravascular coagulation (DIC) without heparin

Tranexamic Acid:

History of thrombosis
Subarachnoid hemorrhage (risk of cerebral edema)

Aprotinin:

Previous hypersensitivity
Use cautiously in patients with renal impairment

Important Point

TXA is widely used in trauma and orthopedic surgeries with good safety profile.
EACA is cheaper but less potent than TXA.
Aprotinin is restricted due to safety concerns but may still be used in select cases.

END OF THE CHAPTER

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