Fibrino

Approved Indications:

• Menorrhagia (Heavy Menstrual Bleeding): To reduce blood loss in women with cyclic heavy menstrual periods.
• Hereditary Angioedema: Adjunct in preventing or treating episodes.
• Dental Extraction in Hemophiliacs: To prevent or reduce bleeding in patients with hemophilia undergoing dental procedures.
• Traumatic Bleeding: Control of acute hemorrhage due to trauma.
• Postpartum Hemorrhage (PPH): Management of postpartum bleeding when uterotonics fail.
• Surgical Hemostasis: Reduction of bleeding in cardiac surgery, orthopedic surgery (e.g., total knee replacement), and otolaryngologic surgery.

Clinically Accepted Off-label Uses:

• Epistaxis (Nasal Bleeding): Topical or oral use to reduce bleeding frequency and severity.
• Melasma (Chloasma): Oral or topical use as adjunct therapy.
• Prostate Surgery: To reduce blood loss during transurethral resection of the prostate (TURP).
• Intracerebral Hemorrhage: Investigated use in reducing hematoma expansion in non-traumatic brain bleeds.

Adults:

• Menorrhagia: 1 g orally three times daily for up to 5 days during menstruation.
• Postoperative or Traumatic Bleeding: 10–15 mg/kg IV every 6–8 hours; infusion rate not exceeding 1 mL/min.
• Postpartum Hemorrhage: 1 g IV over 10 minutes; may repeat once after 30 minutes if bleeding persists.
• Surgical Bleeding Prevention: 10–15 mg/kg IV prior to surgery and then every 8 hours for up to 2–3 doses.

Pediatrics:

• Cardiac Surgery: 10–15 mg/kg IV every 6–8 hours.
• Use must be carefully calculated based on body weight and bleeding risk.

Elderly:

• Dose as in adults; monitor renal function due to increased risk of accumulation.

Renal Impairment:

• Serum Creatinine 120–250 µmol/L (1.4–2.8 mg/dL): 10 mg/kg twice daily
• 250–500 µmol/L (2.8–5.6 mg/dL): 10 mg/kg daily
• >500 µmol/L (>5.6 mg/dL): 10 mg/kg every 48 hours or per hemodialysis schedule.

Hepatic Impairment:

• No dose adjustment typically required.

Routes of Administration:

• Oral tablets
• Intravenous injection
• Topical solution (less commonly used for epistaxis or dermatological uses)

Tranexamic acid is a synthetic derivative of the amino acid lysine. It exerts antifibrinolytic effects by reversibly binding to lysine receptor sites on plasminogen and plasmin. This inhibits the activation of plasminogen to plasmin, the enzyme responsible for fibrin degradation. By stabilizing fibrin clots and preventing excessive fibrinolysis, it promotes hemostasis in various bleeding disorders. Tranexamic acid does not promote clot formation but instead preserves existing clots.

• Absorption: Rapid and nearly complete oral absorption with bioavailability of ~30–50%.
• Peak Plasma Time: 3 hours (oral); immediate (IV).
• Distribution: Widely distributed in tissues including synovial fluid and cerebrospinal fluid; low plasma protein binding (~3%).
• Metabolism: Minimal hepatic metabolism.
• Elimination Half-life: 2–3 hours (plasma); prolonged in renal impairment.
• Excretion: Primarily via kidneys (~90–95% excreted unchanged in urine).

• Pregnancy:
• Former FDA Category B.
• No evidence of teratogenicity in animal studies. Limited human data; use only if clearly needed, especially in the first trimester.
• Often used to control postpartum hemorrhage under medical supervision.
• Lactation:
• Excreted in breast milk in low concentrations.
• No adverse effects reported in breastfed infants; considered compatible with breastfeeding, especially with short-term use.
• Caution advised with prolonged use.

• Primary Class: Antifibrinolytic Agent
• Subclass: Synthetic Lysine Analog
• Other Identifiers: Hemostatic Agent

• Hypersensitivity to tranexamic acid or any excipients
• Active intravascular clotting (e.g., deep vein thrombosis, pulmonary embolism)
• History or presence of thromboembolic disease
• Subarachnoid hemorrhage (risk of cerebral edema or infarction)
• Severe renal impairment without dose adjustment
• Acquired defective color vision (may affect monitoring)

• Thromboembolic Risk: Use cautiously in patients with history of thrombosis, coagulation disorders, or on estrogen therapy.
• Ocular Effects: Rare risk of visual disturbances; discontinue if changes in color vision occur.
• Seizures: High-dose IV use associated with seizure risk, especially in cardiac surgery patients.
• Renal Monitoring: Essential in long-term or high-dose therapy due to renal excretion.
• Hematuria: Use cautiously in patients with hematuria due to risk of ureteral obstruction from clots.
• Postoperative Patients: Monitor for signs of thromboembolism.

Common (by system):

• Gastrointestinal: Nausea, vomiting, diarrhea, abdominal pain
• Neurological: Headache, dizziness
• Ophthalmologic: Blurred vision (rare, reversible)

Serious & Rare:

• Cardiovascular: Thrombosis (deep vein thrombosis, pulmonary embolism), hypotension (with rapid IV injection)
• Neurological: Seizures (particularly with high IV doses)
• Renal: Hematuria or obstruction due to clot formation
• Allergic: Skin rash, pruritus, anaphylaxis (rare)

Onset: Side effects usually occur within hours to days of starting therapy; seizure risk may be delayed.

• Anticoagulants & Antiplatelet Agents (e.g., warfarin, aspirin):
• May antagonize effects; use with caution to avoid thrombotic events.
• Estrogen-containing Products (oral contraceptives, hormone therapy):
• Additive prothrombotic risk.
• Tretinoin + Arsenic Trioxide: Theoretical increased risk of thrombosis.
• No significant CYP450 interactions: Tranexamic acid is not a CYP450 substrate or inhibitor.

• WHO Guidelines (2022): Strongly recommend use of IV tranexamic acid in postpartum hemorrhage within 3 hours of birth to reduce maternal mortality.
• Trauma Guidelines: CRASH-2 trial reinforced early IV administration (within 3 hours of injury) improves survival.
• Dermatological Use (Melasma): Increasing recognition of oral and topical tranexamic acid as adjunctive therapy for refractory melasma, though still off-label.

• Oral Tablets:
• Store below 30°C.
• Protect from moisture and direct light.
• IV Solution:
• Store at 15°C to 30°C.
• Do not freeze.
• Use diluted solutions immediately or store refrigerated (2°C–8°C) and use within 24 hours.
• Handling Precautions:
• Avoid rapid IV injection (risk of hypotension).
• Inspect visually for particulate matter and discoloration before administration.