Generic Name
Tranexamic acid
Brand Names
Cyklokapron
Lysteda
Transamin
Hemoclar
Caprol
Exacyl
TXA (abbreviation commonly used in medical settings)
Available in both brand-name and generic forms worldwide
Drug Class
Antifibrinolytic agent
Synthetic lysine analogue
Hemostatic agent
Mechanism of Action
Tranexamic acid (TXA) is a synthetic derivative of the amino acid lysine that exerts antifibrinolytic effects by reversibly binding to lysine-binding sites on plasminogen
It inhibits the conversion of plasminogen to plasmin
Prevents plasmin from degrading fibrin clots (fibrinolysis inhibition)
Stabilizes blood clots and prevents excessive bleeding
Does not affect clot formation itself (not procoagulant)
Also possesses mild anti-inflammatory effects by reducing plasmin-mediated activation of complement and inflammatory mediators
Indications
Approved Uses
Menorrhagia (heavy menstrual bleeding) – oral TXA (e.g., Lysteda)
Tooth extraction bleeding in hemophilia – oral or IV
Hereditary angioedema (off-label in some countries)
Perioperative bleeding prophylaxis – especially in orthopedic, cardiac, spinal, gynecologic, and liver transplant surgeries
Trauma-associated hemorrhage (e.g., CRASH-2 trial evidence)
Postpartum hemorrhage (e.g., WOMAN trial evidence)
Epistaxis – topical TXA
Hematuria (adjunct)
Bleeding associated with dental or ENT surgery
Bleeding from oral mucosa in thrombocytopenia
Transurethral resection of the prostate (TURP) bleeding prophylaxis
Gynecologic surgery (e.g., hysterectomy, cesarean delivery)
Liver surgery or liver transplantation
Off-label / Investigational Uses
Subarachnoid hemorrhage
Intracerebral hemorrhage
Hypermenorrhea due to IUD
Melasma (topical or oral use in dermatology)
Epilepsy-related menstrual bleeding exacerbation
Intravesical hemorrhagic cystitis
Adjunctive treatment in bleeding disorders such as von Willebrand disease
Dosage and Administration
Menorrhagia
Oral: 1,000–1,300 mg 3 times daily for up to 5 days during menses
Maximum duration: 5 days per cycle
Initiate at onset of menstruation
Surgical Prophylaxis
IV: 10–15 mg/kg prior to incision
Repeat intraoperatively if needed (based on half-life and procedure length)
Orthopedic surgery: IV bolus or infusion protocols used; some regimens use topical irrigation
Trauma and Postpartum Hemorrhage
IV: 1 gram over 10 minutes as soon as possible within 3 hours of bleeding onset
Repeat dose after 30 minutes to 24 hours if bleeding continues
Dental Extraction in Hemophilia
Oral: 25 mg/kg three to four times daily for 6–8 days post-procedure
Can be combined with clotting factor replacement
Melasma (Off-label dermatological use)
Oral: 250 mg twice daily for 3–6 months
Topical: 2–5% solution or cream applied twice daily
Topical Application
Crushed tablets or ampoules mixed with sterile water for direct nasal, oral, or surgical site application
Nasal spray formulations available in some countries
Route of Administration
Available in oral tablets, IV injection, and topical formulations
Intravenous form must be diluted and given slowly (over 10 minutes)
Rapid IV injection may cause hypotension
Pharmacokinetics
Absorption
Orally bioavailable (~30–50%)
Peak plasma concentration reached in 2–3 hours
Distribution
Widely distributed, including in joints, cerebrospinal fluid, and menstrual blood
Low protein binding (~3%)
Crosses placenta and is secreted in breast milk
Metabolism
Minimally metabolized
Elimination
Primarily renal excretion as unchanged drug
Half-life ~2–3 hours (oral), extended in renal impairment
Dose adjustment required in patients with renal dysfunction
Contraindications
Active thromboembolic disease (deep vein thrombosis, pulmonary embolism)
History of arterial or venous thrombosis
Acquired defective color vision (may affect detection of ocular complications)
Subarachnoid hemorrhage (may increase risk of cerebral ischemia or seizures)
Hypersensitivity to TXA or formulation components
Severe renal impairment without dose adjustment
Warnings and Precautions
Thrombosis risk: use cautiously in patients with history or risk factors for thrombosis (e.g., Factor V Leiden, antiphospholipid syndrome)
Seizure risk: particularly with high-dose IV use or in cardiac surgery
Hypotension: avoid rapid IV administration
Visual disturbances: monitor for changes in vision, especially with prolonged use
Renal impairment: adjust dose based on creatinine clearance
Monitor closely when used concurrently with prothrombotic agents (e.g., oral contraceptives, factor concentrates, antifibrinolytics like aminocaproic acid)
Adverse Effects
Common
Nausea
Vomiting
Diarrhea
Abdominal pain
Headache
Back pain
Sinus symptoms or nasal congestion (oral)
Less Common
Fatigue
Dizziness
Muscle cramps
Menstrual discomfort
Serious (Rare)
Deep vein thrombosis
Pulmonary embolism
Myocardial infarction
Cerebral thrombosis
Seizures (mainly with high IV doses in cardiac surgery)
Visual changes (retinal thrombosis, color vision changes)
Allergic reactions or angioedema
Overdose
Symptoms
Nausea
Vomiting
Hypotension (especially with rapid IV infusion)
Seizures
Management
Supportive care
Seizure control with benzodiazepines or antiepileptics
Monitor renal function and electrolytes
Drug Interactions
Oral contraceptives – increased risk of thrombosis
Estrogenic agents – additive thrombotic potential
Procoagulant agents (e.g., recombinant factor VIIa) – increased clot formation risk
Tretinoin (oral) – theoretical increased thrombosis risk
No significant CYP450 metabolism – low risk of interaction with hepatic enzyme inducers/inhibitors
No known interactions with NSAIDs or anticoagulants but use with caution
Use in Special Populations
Pregnancy
Category B (FDA)
Not teratogenic
Used in obstetrics for postpartum hemorrhage
Crosses placenta
Use only if clearly needed
Lactation
Excreted in breast milk in low amounts
Generally considered safe by WHO and ACOG
Pediatrics
Used in pediatric surgeries and bleeding disorders
Doses based on body weight (10–15 mg/kg)
Safe and effective in children when appropriately dosed
Geriatrics
No special precautions but assess renal function
Renal Impairment
Dose reduction is necessary
CrCl 50–80 mL/min → 50% of normal dose
CrCl 10–50 mL/min → 25% of dose
CrCl <10 mL/min → 10% of dose
Monitoring Parameters
Signs of thrombosis
Renal function (especially with long-term or high-dose use)
Visual disturbances in long-term use
Seizure activity in high-risk settings (e.g., cardiac surgery)
Bleeding control effectiveness
Comparative Pharmacology
Compared to ε-aminocaproic acid
– TXA is more potent, better oral bioavailability
Compared to desmopressin
– Desmopressin acts by increasing vWF and factor VIII, used in hemophilia A or vWD
– TXA acts on fibrinolysis pathway
Compared to hormonal therapy for menorrhagia
– TXA provides non-hormonal option
– Effective for acute heavy bleeding and in patients contraindicated for hormonal therapy
Formulations Available
Oral tablets (250 mg, 500 mg, 650 mg, 1,000 mg depending on brand)
Oral granules/sachets in some markets
IV solution (100 mg/mL in 5 mL or 10 mL ampoules)
Topical formulations (crushed tablets for ENT use)
Available globally under various trade names
Regulatory and Legal Status
Prescription-only medicine
Approved by FDA, EMA, MHRA for various indications
Included in WHO Model List of Essential Medicines
Not a controlled substance
Available in hospital formularies and emergency protocols
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