Drug reference

Tranexamic Acid

Hemostatic

Also known as AMCA, Cyclokapron, Lysteda, Transamin

START

Confirm bleeding indication. Screen for thromboembolic history. Baseline creatinine. For menorrhagia: start at onset of menses.

TYPICAL MAX

3.9 g/day (oral); 30 mg/kg/day IV. Do not exceed 5 days per menstrual cycle.

STOP IF

Signs of thrombosis (leg pain, chest pain, dyspnea, visual changes), color vision changes, seizures, severe hypersensitivity

WATCH

Renal function (dose adjustment), signs of thrombosis, visual changes, menstrual bleeding pattern, hemoglobin

CDSCO approvedSchedule HJan AushadhiATC B02AA02

Dose laddermg/d

Renal dose adjustmenteGFR mL/min/1.73m²

KDIGO 2024 + manufacturer label

Pharmacokineticsplasma · t hours

ONSET: 2h · 1-2 h (oral)
PEAK: 3h · 3 h (oral MR)
t½: 2h · ~2 h (plasma)
DURATION: 8h · 6-8 h (q6-8h dosing)

EXCRETION

>95% renal unchanged; minimal metabolism

route + CYP

INTERACTIONS

12 major

incl. contraindicated

PREGNANCY

FDA PLLR: Crosses placenta. No evidence of teratogenicity. Use with caution; benefit should outweigh risk. May be used for postpartum hemorrhage (WOMAN trial showed safety and efficacy).

FDA category + note

Top interactionssee all 12 →

AlteplaseContraindicatedDatabaseDDInter
StreptokinaseContraindicatedDatabaseDDInter
Combined Hormonal ContraceptivesContraindicatedDatabaseKimi deep-research + Cla
UrokinaseContraindicatedDatabaseDDInter

Available in India

324 branded formulations and 392 fixed-dose combinations. Look up specific brands in the Drugs workspace.

Jan Aushadhi — generic available at GoI pharmacies

Mechanism

Tranexamic acid is a synthetic lysine analog that competitively inhibits the activation of plasminogen to plasmin by blocking the lysine-binding sites on plasminogen. This prevents plasmin from binding to and degrading fibrin, thereby stabilizing clots and reducing bleeding. It does not affect platelet function or coagulation factor levels. The antifibrinolytic effect is exerted both systemically and locally at bleeding sites.

Indications

Heavy menstrual bleeding (menorrhagia)Short-term prevention/treatment of bleeding in hemophilia (dental extractions)Hereditary angioedema (prophylaxis — off-label)Trauma-associated hemorrhage (IV — CRASH-2 trial evidence)Surgical bleeding reduction (orthopedic, cardiac, major surgery)Epistaxis (off-label, topical or oral)Postpartum hemorrhage (off-label — WOMAN trial)Melasma (topical — off-label)

Dosing

Adult: Menorrhagia: 1300 mg PO TID (max 5 days during menses) OR 1 g PO TDS. Hemophilia bleeding: 10 mg/kg IV q6-8h OR 25 mg/kg PO q6-8h. Trauma: 1 g IV over 10 min, then 1 g IV over 8 hours (CRASH-2). Postpartum hemorrhage: 1 g IV over 10 min (WOMAN trial).
Pediatric: Hemophilia bleeding (≥1 month): 25 mg/kg PO q6-8h OR 10 mg/kg IV q6-8h. Trauma: same as adult dosing (weight-based).
Renal adjustment: CrCl 30-50: reduce dose by ~50%. CrCl 10-30: reduce dose by ~75%. CrCl <10: 25% of standard dose or avoid. IV dosing requires adjustment based on eGFR.
Hepatic adjustment: No adjustment required (not metabolized hepatically).
Geriatric: No specific adjustment; monitor renal function. Increased thrombosis risk with age.
Max dose: 3.9 g/day (menorrhagia); 30 mg/kg/day (parenteral)

Pharmacokinetics

Onset

Antifibrinolytic effect within 1-2 hours of oral administration.

Peak effect

Oral: peak plasma at 3 hours (modified-release). IV: immediate peak at end of infusion.

Duration

6-8 hours (supports q6-8h dosing).

Half-life

~2 hours (plasma); terminal elimination ~11 hours. 95% excreted unchanged in urine within 24h.

Bioavailability

~43.9% (oral modified-release); food does not significantly affect absorption.

Protein binding

~3% (very low; binds primarily to plasminogen).

Metabolism

Minimal hepatic metabolism (<5% of dose metabolized). Primarily excreted unchanged.

Excretion

Renal: >95% excreted unchanged in urine via glomerular filtration within 24 hours.

Contraindications

Concomitant use of combined hormonal contraceptives (FDA §4.1 — thrombotic risk)
Active thromboembolic disease, or a history of / intrinsic risk of thrombosis or thromboembolism incl. retinal vein/artery occlusion (FDA §4.1 — absolute)
Hypersensitivity to tranexamic acid
Subarachnoid hemorrhage (cerebral edema/infarction risk)

Side effects

Common

Nausea, vomiting, diarrheaHeadacheBack painMuscle crampsAnemia

Serious

Thromboembolic events (DVT, PE, stroke — rare but serious; increased risk with prolonged use or history of thrombosis)
Color vision disturbances/retinal changes (retinal vein/artery occlusion)
Seizures (especially with high IV doses or renal impairment)
Hypersensitivity reactions (anaphylaxis)
Subarachnoid hemorrhage complications (cerebral edema, infarction)

Pregnancy & lactation

Pregnancy

FDA PLLR: Crosses placenta. No evidence of teratogenicity. Use with caution; benefit should outweigh risk. May be used for postpartum hemorrhage (WOMAN trial showed safety and efficacy).

Lactation

Excreted in breast milk at ~1% of maternal dose. Compatible with breastfeeding per AAP. Monitor infant for GI upset.

Drug interactions

Alteplase

Contraindicated

Database

Tranexamic acid inhibits fibrinolysis, directly counteracting the thrombolytic effect of alteplase. This renders alteplase ineffective and may increase the risk of re-thrombosis.

Concomitant use is contraindicated. Tranexamic acid should not be administered with fibrinolytic agents.

Source: DDInter

Streptokinase

Contraindicated

Database

Tranexamic acid inhibits fibrinolysis, directly counteracting the thrombolytic effect of streptokinase. This renders streptokinase ineffective and may increase the risk of re-thrombosis.

Concomitant use is contraindicated. Tranexamic acid should not be administered with fibrinolytic agents.

Source: DDInter

Combined Hormonal Contraceptives

Contraindicated

Database

Both tranexamic acid and hormonal contraceptives increase thromboembolic risk. Combined use may further increase risk of DVT, PE, and stroke.

Assess individual thrombosis risk. Use lowest effective tranexamic acid dose for shortest duration. Consider progestin-only contraception if long-term TXA needed.

Source: Kimi deep-research + Cla

Urokinase

Contraindicated

Database

Tranexamic acid inhibits fibrinolysis, directly counteracting the thrombolytic effect of urokinase. This renders urokinase ineffective and may increase the risk of re-thrombosis.

Concomitant use is contraindicated. Tranexamic acid should not be administered with fibrinolytic agents.

Source: DDInter

Anti Inhibitor Coagulant Complex

Severe

Database

Clinical effect not specified

Source: DDInter

Carfilzomib

Severe

Database

Drug interaction classified as: synergy

Source: DDInter