Medically reviewed on Nov 15, 2018
(tran eks AM ik AS id)
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Generic: 1000 mg/10 mL (10 mL)
Solution, Intravenous [preservative free]:
Cyklokapron: 1000 mg/10 mL (10 mL)
Generic: 1000 mg/10 mL (10 mL)
Lysteda: 650 mg
Generic: 650 mg
Brand Names: U.S.
- Antifibrinolytic Agent
- Antihemophilic Agent
- Hemostatic Agent
- Lysine Analog
Forms a reversible complex that displaces plasminogen from fibrin resulting in inhibition of fibrinolysis; it also inhibits the proteolytic activity of plasmin
With reduction in plasmin activity, tranexamic acid also reduces activation of complement and consumption of C1 esterase inhibitor (C1-INH), thereby decreasing inflammation associated with hereditary angioedema.
Vd: 9 to 12 L; CSF levels are 10% of plasma
Urine (>95% as unchanged drug)
Time to Peak
Oral: 2.5 hours (range: 1 to 5 hours)
~2 to 11 hours
~3%, primarily to plasminogen
Special Populations: Renal Function Impairment
Following administration of a single IV injection, urinary excretion declines as renal function decreases.
Special Populations: Children
The Cmax and AUC values after a single oral dose of 1,300 mg in adolescent females were 20% to 25% less than those in adult females given the same dose.
In vitro data suggests that neonates require a lower serum tranexamic acid concentration than adults (6.54 mcg/mL vs 17.5 mcg/mL) to completely prevent fibrinolysis (Yee 2013). In pediatric patients weighing 5 to 40 kg undergoing cardiac surgery with by-pass, a target serum concentration range of 20 to 30 mcg/mL has been used in pharmacokinetic analysis (Dowd 2002; Grassin-Deyle 2013).
Use: Labeled Indications
Cyclic heavy menstrual bleeding (oral): Treatment of cyclic heavy menstrual bleeding.
Tooth extraction in patients with hemophilia (injection, oral [Cyklokapron; Canadian product]): Short-term use in hemophilia patients to reduce or prevent hemorrhage and reduce need for replacement therapy during and following tooth extraction
Off Label Uses
Bleeding associated with hip fracture surgery (prevention)
Data from one single-center, double-blinded randomized study suggests that tranexamic acid may be beneficial for the prevention of blood loss associated with hip fracture surgery [Zufferey 2010]. Additional data may be necessary to further define the role of tranexamic acid in this setting.
Hereditary angioedema, long-term prophylaxis
Based on the International World Allergy Organization/European Academy of Allergy and Clinical Immunology (WAO/EAACI) 2017 guideline for the management of hereditary angioedema, tranexamic acid may be considered as a third-line agent for long-term prophylaxis of hereditary angioedema (HAE) when a C1 inhibitor (human or recombinant) is not available and androgens are contraindicated. Efficacy in suppressing attacks appears low but may benefit some patients. Tranexamic acid is not recommended for treatment of acute HAE attacks.
Intracranial hemorrhage associated with thrombolytics (plasminogen-activator) (eg, alteplase, reteplase, or tenecteplase)
Based on the Neurocritical Care Society and the Society of Critical Care Medicine guideline for reversal of antithrombotics in intracranial hemorrhage, tranexamic acid is suggested as a reversal agent for use in intracranial hemorrhage due to thrombolytics (plasminogen-activator) (eg, alteplase, reteplase or tenecteplase) in cases where cryoprecipitate (preferred therapy) is contraindicated or not available in a timely manner.
Perioperative blood loss reduction in total hip arthroplasty
Data from numerous randomized controlled trials analyzed in several meta-analyses demonstrate efficacy of IV tranexamic acid for the reduction of bleeding and transfusion-related complications in patients undergoing total hip arthroplasty. Total blood loss, number of transfusions required, and units of blood transfused were significantly reduced, and hematological indices were significantly improved with administration of tranexamic acid.
Perioperative blood loss reduction in bilateral total knee arthroplasty
Data from randomized controlled trials demonstrate efficacy of IV tranexamic acid for the reduction of bleeding and transfusion requirements in patients undergoing simultaneous bilateral total knee arthroplasty. The type of blood conservation protocol may have influenced results in some studies.
Perioperative blood loss reduction in unilateral total knee arthroplasty
Data from numerous randomized controlled trials analyzed in several meta-analyses demonstrate efficacy of IV tranexamic acid for the reduction of bleeding and transfusion-related complications in patients undergoing unilateral total knee arthroplasty. Total blood loss, number of transfusions required, and units of blood transfused were significantly reduced, and hematological indices were significantly improved with administration of tranexamic acid.
Prevention of perioperative bleeding associated with cardiac surgery
Data from multicenter, blinded, randomized, controlled trials support the use of IV tranexamic acid in the prevention of perioperative bleeding associated with cardiac surgery [Fergusson 2008], [Myles 2017]. Tranexamic acid was associated with a lower risk of bleeding, without a higher risk of death or thrombotic complications ≤30 days after surgery compared to placebo [Myles 2017]. Additional clinical data also support the use of tranexamic acid for the prevention of perioperative bleeding associated with cardiac surgery [Gravlee 2008], [Nuttall 2008].
Post-operative bleeding associated with cervical conization
Data from randomized, controlled trials demonstrate the efficacy of tranexamic acid for the reduction or prevention of post-operative bleeding following cervical conization. An absence or reduction in postoperative bleeding has been observed in patients receiving intraoperative IV tranexamic acid followed by postoperative oral treatment and in patients receiving postoperative oral treatment alone [Grunsdell 1984], [Rybo 1972].
Postpartum hemorrhage, treatment
Data from a large international, randomized, double-blind, placebo-controlled trial evaluating the early administration of IV tranexamic acid in women (≥16 years of age) with postpartum hemorrhage following vaginal birth or cesarean section supports the use of tranexamic acid in this condition. A significant reduction in risk of death due to bleeding was observed when treatment was started within 3 hours of birth whereas no apparent risk reduction was seen when given after 3 hours [WOMAN Trial Collaborators 2017].
Based on the American College of Obstetricians and Gynecologists (ACOG) Practice Bulletin for Postpartum Hemorrhage, IV tranexamic acid is recommended for the treatment of obstetric hemorrhage when initial therapy fails [ACOG 183 2017]. In addition, the World Health Organization (WHO) recommends intravenous tranexamic acid to be administered within 3 hours of birth along with standard care, to women diagnosed with postpartum hemorrhage [WHO 2017].
Subarachnoid hemorrhage, prevention of early aneurysmal rebleeding
Data from a randomized, prospective, multicenter, controlled study in patients who suffered aneurysmal subarachnoid hemorrhage (SAH) suggest that the short-term use of tranexamic acid may be beneficial for the prevention of early rebleeding [Hillman 2002].
Based on the American Heart Association/American Stroke Association guidelines for the management of aneurysmal subarachnoid hemorrhage, the short-term use (<72 hours) of an antifibrinolytic is reasonable to reduce the risk of early aneurysm rebleeding [AHA/ASA [Connolly 2012]].
Data from a large randomized placebo-controlled trial evaluating the effects of early administration (ie, within 8 hours, ideally within 3 hours) of tranexamic acid in adult trauma patients with significant hemorrhage or at risk of hemorrhage supports the use of tranexamic acid to reduce the risk of death from bleeding in this patient population [CRASH-2 trial collaborators 2010]. In a post-hoc analysis, treatment beyond 3 hours has been shown to be significantly less effective and may be associated with harm [CRASH-2 trial collaborators 2011]. In a subsequent retrospective observational study in patients suffering combat-related injury, the use of tranexamic acid resulted in improved measures of coagulopathy and survival especially in those patients requiring massive transfusion [Morrison 2012].
Additional Off-Label Uses
Bleeding associated with dental procedures in patients on oral anticoagulant therapy (topical mouth rinse); Prevention of bleeding associated with craniosynostosis surgery, extracorporeal membrane oxygenation (ECMO), orthognathic surgery, spinal surgery (eg, spinal fusion), or transurethral prostatectomy; Traumatic hyphema
Hypersensitivity to tranexamic acid or any component of the formulation
Injection: Acquired defective color vision; active intravascular clotting; subarachnoid hemorrhage. Note: Although subarachnoid hemorrhage (SAH) is listed in the manufacturer’s labeling as a contraindication due to risk of cerebral edema and cerebral infarction, use has been described in the literature for aneurysmal SAH (Roos 2000; Roos 2003). When definitive treatment of the aneurysm is unavoidably delayed and no other contraindications exist, short-term use (<72 hours) of tranexamic acid is a reasonable treatment option to reduce the risk of early rebleeding without an increased risk of vasospasm and delayed ischemia; however, clinical trial data regarding improved outcomes are not conclusive at this time and an increased risk of deep venous thrombosis has been reported (ASA [Connolly 2012]; Chwajol 2008; Starke 2011;).
Oral: Active thromboembolic disease (eg, cerebral thrombosis, DVT, or PE); history of thrombosis or thromboembolism, including retinal vein or retinal artery occlusion; intrinsic risk of thrombosis or thromboembolism (eg, hypercoagulopathy, thrombogenic cardiac rhythm disease, thrombogenic valvular disease); concurrent use of combination hormonal contraception
Canadian labeling: Additional contraindications (not in the US labeling): Injection, oral: History or risk of thrombosis (unless concurrent anticoagulation therapy is possible); hematuria
Cyclic heavy menstrual bleeding: Oral:
Lysteda: 1,300 mg 3 times daily (3,900 mg/day) for up to 5 days during monthly menstruation
Cyklokapron [Canadian product]: 1,000 to 1,500 mg 3 to 4 times daily
Hereditary angioedema (HAE), long-term prophylaxis (off-label use): Oral: 1,000 to 1,500 mg 2 to 3 times daily; reduce to 500 mg/dose once or twice daily when frequency of attacks reduces (Gompels 2005; Levy 2010) or 25 mg/kg/dose administered 2 to 3 times daily (Bowen 2004)
Hip fracture surgery, blood conservation (off-label use): IV: 15 mg/kg administered at the time of skin incision followed by a second dose (15 mg/kg) 3 hours later (Zufferey 2010). Additional data may be necessary to further define the role of tranexamic acid in this setting.
Intracranial hemorrhage associated with thrombolytics (plasminogen-activator) (eg, alteplase, reteplase, or tenecteplase) (off-label use): IV: 10 to 15 mg/kg over 20 minutes (as an alternative to cryoprecipitate); check fibrinogen levels after administration, if fibrinogen <150 mg/dL, cryoprecipitate is recommended (NCS/SCCM [Frontera 2016]).
Orthognathic surgery, blood loss reduction (off-label use): IV: 20 mg/kg over 15 minutes prior to incision (Choi 2009)
Perioperative blood loss reduction in bilateral total knee arthroplasty (off-label use): IV:
Three-dose regimen: 10 mg/kg administered as a slow IV infusion 30 minutes before tourniquet deflation for the first operation, 30 minutes before tourniquet deflation for the second operation, and 3 hours after commencement of the second dose (Kim 2014).
Two-dose regimen: 10 or 15 mg/kg administered over 10 minutes before deflation of the first tourniquet, with the second dose administered 3 hours after the first dose (MacGillivray 2011).
Perioperative blood loss reduction in unilateral total knee arthroplasty (off-label use): IV:
Intra- and postoperative regimen: 10 mg/kg at least 10 to 30 minutes prior to tourniquet release (deflation) and 10 mg/kg at 3 hours after the first dose (Alvarez 2008; Camarasa 2006; Maniar 2012). Instead of the second dose, a postoperative infusion may be administered at 1 mg/kg/hour for 6 hours (Alvarez 2008).
Pre- and intraoperative regimen: 10 mg/kg at least 20 minutes or immediately before tourniquet inflation and repeated at least 15 minutes prior to deflation or immediately after release of tourniquet (Lozano 2008; Maniar 2012).
Pre-, intra-, and postoperative regimen: 10 mg/kg at least 20 minutes before tourniquet inflation, repeated at least 15 minutes prior to deflation and postoperatively at 3 hours after the second dose (Maniar 2012).
Post-operative bleeding associated with cervical conization (prevention/reduction) (off-label use):
IV/Oral: Intra- and postoperative regimen: 1 g IV infusion during procedure followed by oral therapy 1 g 3 times daily for 14 days, beginning the day after procedure (Grunsdell 1984).
Oral: Postoperative regimen: 1500 mg every 8 hours beginning the evening following the procedure and continuing for 12 days (Rybo 1972).
Postpartum hemorrhage, treatment (off-label use): IV: 1,000 mg over 10 minutes given within 3 hours of vaginal birth or cesarean section; if bleeding continues after 30 minutes or stops and restarts within 24 hours after the first dose, a second dose of 1,000 mg may be given (WOMAN Trial Collaborators 2017).
Prevention of dental procedure bleeding in patients on oral anticoagulant therapy (off-label use): Oral rinse: 4.8% solution: Hold 10 mL in mouth and rinse for 2 minutes then spit out. Repeat 4 times daily for 2 days after procedure. Note: Patient should not eat or drink for 1 hour after using oral rinse (Carter 2003).
Prevention of perioperative bleeding associated with cardiac surgery (off-label use): IV:
50 mg/kg administered >30 minutes after induction of anesthesia (Myles 2017)
Loading dose of 30 mg/kg over 30 minutes (total loading dose includes a test dose administered over the first 10 minutes followed by the remainder of dose) prior to incision, followed by 16 mg/kg/hour until sternal closure; add an additional 2 mg/kg to cardiopulmonary bypass circuit (Fergusson 2008)
Loading dose of 10 mg/kg over 20 minutes prior to incision followed by 2 mg/kg/hour continued for 2 hours after transfer to ICU; add a prime dose of 50 mg for a 2.5 L cardiopulmonary bypass circuit; maintenance infusion adjusted for renal insufficiency (Nuttall 2008)
Loading dose of 10 to 15 mg/kg over 10 to 15 minutes, followed by 1 to 1.5 mg/kg/hour. The authors suggest adding 2 to 2.5 mg/kg to cardiopulmonary bypass circuit; however, amounts have varied widely in clinical trials (Gravlee 2008).
Prevention of perioperative bleeding associated with spinal surgery (eg, spinal fusion) (off-label use): IV: 2,000 mg over 20 minutes prior to incision followed by 100 mg/hour during surgery and for 5 hours postoperatively (Elwatidy 2008) or 10 mg/kg prior to incision followed by 1 mg/kg/hour for the remainder of the surgery; discontinue at time of wound closure (Wong 2008)
Subarachnoid hemorrhage (SAH), prevention of early aneurysmal rebleeding (off-label use): Note: For use when definitive treatment of the aneurysm is unavoidably delayed: IV: 1,000 mg as soon as diagnosis of SAH has been verified, followed by 1,000 mg every 6 hours until the aneurysm is occluded; maximum duration of treatment: 72 hours (AHA/ASA [Connolly 2012]; Hillman 2002).
Tooth extraction in patients with hemophilia (in combination with appropriate factor replacement therapy): IV: 10 mg/kg immediately before surgery, then 10 mg/kg 3 to 4 times daily; may be used for 2 to 8 days. Alternatively, the following dosing has been recommended: 10 mg/kg as a single dose 2 hours prior to procedure (in conjunction with Factor VIII and IX); following procedure, administer oral tranexamic acid for 6 to 8 days (Canadian manufacturer's labeling).
Oral: Cyklokapron [Canadian product]: 25 mg/kg as a single dose 2 hours prior to procedure, then 25 mg/kg 3 to 4 times daily for 6 to 8 days
Total hip replacement surgery, blood conservation (off-label use): IV: 10 to 15 mg/kg (or 1,000 mg) administered over 5 to 10 minutes immediately before the operation or 15 minutes before skin incision; the preoperative dose may be followed by 10 mg/kg administered 3 to 12 hours after the operation. Postoperative doses ranged from a 10 mg/kg IV bolus (or 1,000 mg) to a 1 mg/kg/hour infusion over 10 hours (Gandhi 2013; Oremus 2014).
Note: Multiple regimens have been evaluated in varying degrees of evidence quality. The regimen listed here reflects the more commonly used dosing based on a number of prospective randomized controlled trials (Johansson 2005; McConnell 2011; Niskanen 2005; Oremus 2014). Metaanalyses have also been conducted demonstrating significant reduction in blood loss perioperatively without an increased risk of thromboembolic events (Gandhi 2013; Sukeik 2011; Zhou 2013). The use of intra-articular tranexamic acid (ie, 1,000 mg/50 mL of NaCl 0.9% sprayed into the wound at the end of the procedure) has also been evaluated demonstrating effectiveness (Alshryda 2014a; Alshryda 2014b).
Transurethral prostatectomy, blood loss reduction (off-label use): Oral: 2,000 mg 3 times daily on the operative and first postoperative day (Rannikko 2004)
Trauma-associated hemorrhage (off-label use): IV: Loading dose: 1,000 mg over 10 minutes, followed by 1,000 mg over the next 8 hours. Note: Clinical trial included patients with significant hemorrhage (SBP <90 mm Hg, heart rate >110 bpm, or both) or those at risk of significant hemorrhage. Treatment began within 8 hours of injury; however, every effort should be made to give as soon as possible (ideally within 3 hours of injury since treatment beyond 3 hours has been shown to be significantly less effective and may be associated with harm) (CRASH-2 Trial Collaborators 2010; CRASH-2 Trial Collaborators 2011).
Traumatic hyphema (off-label use): Oral: 25 mg/kg administered 3 times daily for 5 to 7 days (Rahmani 1999; Vangsted 1983; Varnek 1980). Note: This same regimen may also be used for secondary hemorrhage after an initial traumatic hyphema event.
Refer to adult dosing.
Cyclic heavy menstrual bleeding: Children ≥12 years (postmenarche) and Adolescents: Oral: Refer to adult dosing.
Hereditary angioedema (HAE) (off-label use): Oral:
Long-term prophylaxis: 20 to 40 mg/kg/day in 2 to 3 divided doses (maximum dose: 3,000 mg daily) (Farkas 2007) or 50 mg/kg/day (or 1,000 to 2,000 mg daily; depending on age and size of patient); may consider alternate-day regimen or twice-weekly regimen when frequency of attacks reduces; diarrhea may be a dose-limiting side effect (Gompels 2005)
Short-term prophylaxis: 20 to 40 mg/kg/day in 2 to 3 divided doses (maximum dose: 3,000 mg daily) (Farkas 2007) or 500 mg 4 times daily (Gompels 2005). Note: For short-term prophylaxis (eg, dental work), initiate 2-5 days before and continue for 2 days after the procedure (Bowen 2004; Gompels 2005).
Prevention of perioperative bleeding associated with cardiac surgery (off-label use): IV: 10 mg/kg given over 30 minutes prior to incision, 10 mg/kg while on cardiopulmonary bypass, and 10 mg/kg administered after protamine reversal (Chauhan 2004a; Chauhan 2004b)
Loading dose of 100 mg/kg over 15 minutes prior to incision, followed by 10 mg/kg/hour infusion (continued until ICU transport); add 100 mg/kg to pump reservoir when cardiopulmonary bypass initiated (Reid, 1997)
Prevention of perioperative bleeding associated with craniosynostosis surgery (off-label use): IV: Loading dose of 50 mg/kg over 15 minutes prior to incision, followed by 5 mg/kg/hour (Goobie 2011) or 15 mg/kg over 15 minutes prior to incision, followed by 10 mg/kg/hour until skin closure (Dadure 2011)
Prevention of perioperative bleeding associated with spinal surgery (eg, spinal fusion) (off-label use): Children and Adolescents: IV: 10 mg/kg given over 15 minutes prior to incision followed by 1 mg/kg/hour for the remainder of the surgery; discontinue at time of wound closure (Neilipovitz 2001; Verma 2010)
100 mg/kg over 15 minutes prior to incision followed by 10 mg/kg/hour until skin closure (Sethna 2005)
30 mg/kg over 20 minutes prior to incision followed by 1 mg/kg/hour during surgery and for 5 hours postoperatively (Elwatidy 2008)
Tooth extraction in patients with hemophilia (in combination with appropriate factor replacement therapy): Children and Adolescents: IV: Refer to adult dosing.
Traumatic hyphema (off-label use): Oral: Refer to adult dosing.
Dosing: Renal Impairment
Tooth extraction in patients with hemophilia:
Serum creatinine 1.36 to 2.83 mg/dL: Maintenance dose of 10 mg/kg/dose twice daily
Serum creatinine 2.83 to 5.66 mg/dL: Maintenance dose of 10 mg/kg/dose once daily
Serum creatinine >5.66 mg/dL: Maintenance dose of 10 mg/kg/dose every 48 hours or 5 mg/kg/dose once daily
Cardiac surgery (the following dose adjustments have been recommended [Nuttall 2008]):
Serum creatinine 1.6 to 3.3 mg/dL: Reduce maintenance infusion to 1.5 mg/kg/hour (based on a 25% reduction from 2 mg/kg/hour)
Serum creatinine 3.3 to 6.6 mg/dL: Reduce maintenance infusion to 1 mg/kg/hour (based on a 50% reduction from 2 mg/kg/hour)
Serum creatinine >6.6 mg/dL: Reduce maintenance infusion to 0.5 mg/kg/hour (based on a 75% reduction from 2 mg/kg/hour)
Serum creatinine >1.4 to 2.8 mg/dL: 1,300 mg twice daily (2,600 mg/day) for up to 5 days
Serum creatinine 2.9 to 5.7 mg/dL: 1,300 mg once daily for up to 5 days
Serum creatinine >5.7 mg/dL: 650 mg once daily for up to 5 days
Cyklokapron [Canadian product]:
Serum creatinine 1.4 to 2.8 mg/dL (120 to 250 micromol/L): 15 mg/kg twice daily
Serum creatinine 2.8 to 5.7 mg/dL (250 to 500 micromol/L): 15 mg/kg every 24 hours
Serum creatinine ≥5.7 mg/dL (≥500 micromol/L): 15 mg/kg every 48 hours
Dosing: Hepatic Impairment
No dosage adjustment is necessary.
Tranexamic acid doses may be diluted in 50 to 250 mL of NS or D5W (CRASH-2 Trial Collaborators 2010; Ducloy-Bouthors 2011; Elwatidy 2008; Fergusson 2008). According to the manufacturer, tranexamic acid may be mixed with most solutions for infusion such as electrolyte solutions, carbohydrate solutions, amino acid solutions, and dextran solutions.
A 5% (50 mg/mL) oral solution may be prepared by diluting 5 mL of 10% (100 mg/mL) tranexamic acid injection with 5 mL sterile water. Label “refrigerate”. Stable for 5 days refrigerated.
A 25 mg/mL oral suspension may be prepared with tablets. Place one 500 mg tablet (strength not available in U.S.) into 20 mL water and let stand ~2 to 5 minutes. Begin stirring and continue until the tablet is completely disintegrated, forming a fine particulate suspension (dispersion time for each 500 mg tablet is ~2 to 5 minutes). Administer immediately after preparation.Lam MS, "Extemporaneous Compounding of Oral Liquid Dosage Formulations and Alternative Drug Delivery Methods for Anticancer Drugs," Pharmacotherapy 2011, 31(2):164-92.21275495
Injection: May be administered by direct IV injection at a maximum rate of 100 mg/minute (Crash-trial collaborators 2010; Elwatidy 2008; WOMAN Trial Collaborators 2017).
In general, do not inject more rapidly than 1 mL/minute to avoid hypotension.
Oral: Administer without regard to meals. Swallow tablet whole; do not break, chew, or crush.
Store at 25°C (77°F); excursions permitted to 15°C to 30°C (59°F to 86°F).
Injection: Diluted mixture may be stored for up to 4 hours at room temperature. However, solutions prepared in NS are chemically stable for up to 180 days at room temperature (McCluskey 2014). In another study, tranexamic acid (undiluted) was shown to be chemically stable for up to 12 weeks when stored at -20°C, 4°C, 22°C, and 50°C; freezing tranexamic acid in original ampules is unacceptable due to cracking of the ampules (de Guzman 2013). Freezing tranexamic acid in original vials has not been evaluated.
Anti-inhibitor Coagulant Complex (Human): Antifibrinolytic Agents may enhance the thrombogenic effect of Anti-inhibitor Coagulant Complex (Human). Avoid combination
Estrogen Derivatives (Contraceptive): May enhance the thrombogenic effect of Tranexamic Acid. Avoid combination
Progestins (Contraceptive): May enhance the thrombogenic effect of Tranexamic Acid. Avoid combination
Tretinoin (Systemic): May enhance the thrombogenic effect of Antifibrinolytic Agents. Monitor therapy
Central nervous system: Headache (oral: 50%)
Gastrointestinal: Abdominal pain (oral: 20%)
Neuromuscular & skeletal: Back pain (oral: 21%), musculoskeletal pain (oral: 11%)
Respiratory: Nasal signs and symptoms (oral: 25%; including sinus symptoms)
1% to 10%:
Central nervous system: Fatigue (oral: 5%)
Hematologic & oncologic: Anemia (oral: 6%)
Neuromuscular & skeletal: Arthralgia (oral: 7%), muscle cramps (oral: ≤7%), muscle spasm (oral: ≤7%)
<1%, postmarketing, and/or case reports: Allergic dermatitis, allergic skin reaction, anaphylactic shock, anaphylactoid reaction, anaphylaxis, cerebral thrombosis, chromatopsia, conjunctivitis (ligneous), deep vein thrombosis, diarrhea, dizziness, hypersensitivity reaction, hypotension (with rapid IV injection), nausea, pulmonary embolism, renal cortical necrosis, retinal artery occlusion, retinal vein occlusion, seizure, ureteral obstruction, visual disturbance, vomiting
Concerns related to adverse effects:
• CNS depression: May cause CNS depression, which may impair physical or mental abilities; patients must be cautioned about performing tasks which require mental alertness (eg, operating machinery or driving).
• Hypersensitivity reactions: Severe hypersensitivity reactions, including anaphylaxis or anaphylactoid reaction have been reported.
• Ocular effects: Visual defects (eg, color vision change, visual loss) and retinal venous and arterial occlusions have been reported; discontinue treatment if ocular changes occur; prompt ophthalmic examination should be performed by an ophthalmologist. Use of the injection is contraindicated in patients with acquired defective color vision. Ligneous conjunctivitis has been reported with the oral formulation, but resolved upon discontinuation of therapy.
• Seizure: Seizures have been reported with use; most often with intraoperative use (eg, open chamber cardiac surgery) and in older patients (Murkin 2010). The mechanism by which tranexamic acid use results in seizures may be secondary to neuronal GABA and glycine inhibition or cerebral emboli (Levy 2018).
• Thrombotic events: Venous and arterial thrombosis or thromboembolism, including central retinal artery/vein obstruction, has been reported. Use the injection with caution in patients with thromboembolic disease; oral formulation is contraindicated in patients with a history of or active thromboembolic disease or with an intrinsic risk of thromboembolic events (eg, thrombogenic valvular disease, thrombogenic cardiac rhythm disease, hypercoagulopathy). Concomitant use with certain procoagulant agents (eg, anti-inhibitor coagulant complex/factor IX complex concentrates, oral tretinoin, hormonal contraceptives) may further increase the risk of thrombosis; concurrent use with either the oral or injectable formulation may be contraindicated, not recommended, or to be used with caution.
• Ureteral obstruction: Use the injection with caution in patients with upper urinary tract bleeding, ureteral obstruction due to clot formation has been reported.
• Disseminated intravascular coagulation (DIC): Use with extreme caution in patients with DIC requiring antifibrinolytic therapy; patients should be under strict supervision of a health care provider experienced in treating this disorder.
• Renal impairment: Use with caution in patients with renal impairment; dosage modification necessary.
• Subarachnoid hemorrhage: Use with caution in patients with subarachnoid hemorrhage (SAH); cerebral edema and infarction may occur. According to the manufacturer’s labeling, use of the injection is contraindicated in patients with SAH; however, use has been described in the literature for aneurysmal SAH and is considered a reasonable treatment option in select patients (ASA [Connolly 2012]).
• Vascular disease: Use with caution in patients with uncorrected cardiovascular or cerebrovascular disease due to the complications of thrombosis.
Concurrent drug therapy issues:
• Drug-drug interactions: Potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy. Consult drug interactions database for more detailed information.
Ophthalmic examination (visual acuity, color vision, eye-ground, and visual fields) at baseline and regular intervals during the course of therapy in patients being treated for longer than several days; signs/symptoms of hypersensitivity reactions, seizures, thrombotic events, and ureteral obstruction
Tranexamic acid crosses the placenta; concentrations within cord blood are similar to maternal serum.
Use of oral tranexamic acid for the long-term prophylaxis of HAE in pregnant females has been reported (González-Quevedo 2016; Machado 2017; Milingos 2009). Tranexamic acid may be considered for long-term prophylaxis when preferred treatment is not available (WAO/EEACI [Maurer 2017]).
Intravenous tranexamic acid has been evaluated for the treatment of postpartum hemorrhage (Ducloy-Bouthors 2011; WOMAN Trial Collaborators 2017). A significant reduction in risk of death due to bleeding was observed when treatment was started within 3 hours of vaginal birth or cesarean section (WOMAN Trial Collaborators 2017). Tranexamic acid is recommended for the treatment of obstetric hemorrhage when initial therapy fails (ACOG 183 2017; WHO 2017). IV tranexamic acid has also been studied for prophylaxis of postpartum hemorrhage in low-risk females prior to vaginal or cesarean delivery (Novikova 2015; Sentilhes 2018; Simonazzi 2016). However, available data related to prophylactic use is insufficient and use for routine prophylaxis against postpartum hemorrhage is not currently recommended outside of the context of clinical research (ACOG 183 2017).
• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)
• Patient may experience abdominal pain, back pain, muscle pain, joint pain, rhinitis, muscle cramps, nausea, vomiting, or diarrhea. Have patient report immediately to prescriber signs of blood clots (numbness or weakness on one side of the body; pain, redness, tenderness, warmth, or swelling in the arms or legs; change in color of an arm or leg; angina; shortness of breath; tachycardia; or coughing up blood), signs of severe cerebrovascular disease (change in strength on one side is greater than the other, difficulty speaking or thinking, change in balance, or vision changes), flushing, severe headache, vision changes, eye pain, severe eye irritation, severe loss of strength and energy, seizures, severe dizziness, or passing out (HCAHPS).
• Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.
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Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.
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