Tranexamic Acid

• Heavy Menstrual Bleeding
• Hemophilia Dental Procedures
• Trauma Hemorrhage
• Perioperative Bleeding

Tranexamic acid is an antifibrinolytic medication that inhibits the breakdown of blood clots. It is used to reduce or prevent bleeding in various clinical situations, including heavy menstrual bleeding, surgery, trauma, and hereditary angioedema.

Mechanism of Action

Tranexamic acid prevents clot breakdown:

• Plasminogen binding inhibition: Binds to lysine-binding sites on plasminogen
• Prevents plasmin formation: Blocks conversion of plasminogen to plasmin
• Stabilizes fibrin clots: Plasmin normally degrades fibrin; blocking this preserves clots
• Antifibrinolytic effect: Net result is reduced bleeding

Unlike aminocaproic acid, tranexamic acid is about 10 times more potent.

Available Formulations

• Tablets: 650 mg (Lysteda)
• Injectable solution: 100 mg/mL
• Oral solution: Various compounded preparations

Medical Uses

FDA-Approved Indications:

• Heavy menstrual bleeding
• Short-term prevention of bleeding in hemophilia patients during dental procedures
• Reduction of perioperative blood loss in cardiac surgery

Off-Label Uses:

• Trauma-associated hemorrhage
• Postpartum hemorrhage
• Epistaxis
• Hereditary angioedema prophylaxis
• Melasma (topical)

Dosing Guidelines

Heavy Menstrual Bleeding:

• 1300 mg (two 650 mg tablets) three times daily for up to 5 days during menstruation
• Maximum: 3900 mg/day

Dental Procedures (Hemophilia):

• 25 mg/kg orally 2-3 times daily starting one day before procedure
• Continue 2-8 days post-procedure

Trauma (IV):

• 1 g IV over 10 minutes, then 1 g IV over 8 hours

Renal Impairment:

• Serum creatinine 1.4-2.8: 1300 mg twice daily
• Serum creatinine 2.9-5.7: 1300 mg once daily
• Serum creatinine >5.7: 650 mg once daily

Important Safety Information

Contraindications:

• Active thromboembolic disease (DVT, PE, cerebral thrombosis)
• History of thrombosis or thromboembolism
• Intrinsic risk of thrombosis (certain thrombophilias)
• Subarachnoid hemorrhage (risk of cerebral edema and infarction)
• Hypersensitivity to tranexamic acid

Warnings and Precautions:

• Thromboembolic events: May increase risk; assess individual risk factors
• Visual disturbances: Discontinue and obtain ophthalmologic evaluation
• Seizures: Risk with high doses or renal impairment
• Concurrent use with hormonal contraceptives: May further increase thrombotic risk

Drug Interactions

• Hormonal contraceptives: Increased thrombotic risk
• Factor IX complex concentrates, anti-inhibitor coagulant concentrates: Increased thrombotic risk
• Tissue plasminogen activators (tPA, alteplase): Antagonizes thrombolytic effects
• Tretinoin (all-trans retinoic acid): May cause fatal thrombosis in promyelocytic leukemia patients

Special Populations

• Hepatic Impairment: No specific adjustment
• Renal Impairment: Reduce dose based on serum creatinine
• Pregnancy: Limited data; use only if clearly needed
• Lactation: Present in milk at low concentrations
• Pediatric: Safety established for dental procedures in hemophilia