Category: pharmacological
Aliases: TXA, Lysteda, Cyklokapron
Antifibrinolytic — synthetic lysine analog that competitively inhibits the lysine-binding sites on plasminogen, blocking its conversion to plasmin + plasmin-mediated fibrin degradation. Clinical use: heavy menstrual bleeding (PO), surgical bleeding (IV — orthopedic, cardiac, trauma; CRASH-2 + CRASH-3 trials showed mortality reduction in trauma + TBI when given within 3 hours), postpartum hemorrhage (WOMAN trial), epistaxis (topical), hereditary angioedema. T½ ~2 h, renally cleared. Contraindicated in active intravascular clotting + acquired defective color vision. Distinct from the topical cosmetic application (tranexamic-acid-topical slug) which targets PAR-2 in melanocytes for hyperpigmentation. PK (Lysteda label, 1300 mg PO multiple-dose SS in women): Cmax 13.83 → 16.41 µg/mL after 5 days SS, AUC 78 µg·h/mL, Tmax 3 h, t½ ~11 h (initial phase ~2 h), F 45%. Protein binding 3% (minimal — nearly all unbound). Renally cleared (>95% unchanged in urine) — dose-adjust in CKD. IV formulation has different PK (instant Cmax, F=1.0).
PO: 2h, IV: 2h