Pronunciation: TRAN-ex-AM-ik AS-id
- Injection 100 mg/mL
- Tablets 650 mg
Inhibits fibrinolysis to stop bleeding.
Absolute bioavailability is 45%. T max is approximately 3 h and C max is approximately 16 mcg/mL following multiple oral doses. Food increased C max and AUC by 7% and 16%, respectively. Tranexamic acid may be given without regard to meals.
Protein binding is 3%, with no apparent binding to albumin. Vd is about 0.39 L/kg (oral) and 9 to 12 L (IV). Tranexamic acid crosses the placenta; concentration in cord blood after IV injection is as high as in maternal blood.
Only a small fraction is metabolized.
Renally eliminated. 95% is recovered in the urine as unchanged drug. Cl is 110 to 116 mL/min. Half-life is about 2 h.
Special PopulationsRenal Function Impairment
Following administration of a single IV injection, the 24-h urinary fractions of tranexamic acid with serum creatinine concentrations 1.4 to 2.8, 2.8 to 5.7, and more than 5.7 mg/dL were 51%, 39%, and 19%, respectively. The 24-h plasma concentrations demonstrated a direct relationship to degree of renal impairment.Hepatic Function Impairment
The effect of hepatic impairment has not been evaluated. Because only a small fraction of tranexamic acid is metabolized, no dosage adjustment is needed in patients with hepatic impairment.Elderly
Not intended for use by postmenopausal women (oral).Children
Tranexamic acid has not been studied in adolescents younger than 18 years of age with heavy menstrual bleeding.
Indications and Usage
For short-term use in patients with hemophilia to reduce or prevent hemorrhage and reduce the need for replacement therapy during and following tooth extraction (injection only); treatment of cyclic heavy menstrual bleeding (oral only).
Treatment of GI hemorrhage, hereditary angioneurotic edema, primary or intrauterine device–induced menorrhagia, or recurrent epistaxis; prevention of perioperative bleeding or rebleeding after subarachnoid hemorrhage.
Acquired defective color vision; subarachnoid hemorrhage; active intravascular clotting.Oral
Active thromboembolic disease (eg, deep vein thrombosis, pulmonary embolism, cerebral thrombosis); history of thrombosis or thromboembolism, including retinal vein or artery occlusion; intrinsic risk of thrombosis or thromboembolism (eg, thrombogenic valvular disease, thrombogenic cardiac rhythm disease, hypercoagulopathy); hypersensitivity to tranexamic acid.
Dosage and AdministrationCyclic Heavy Menstrual Bleeding
PO 1,300 mg 3 times daily for a max of 5 days during monthly menstruation.Dental Extraction in Hemophilia Patients
Adults and Children
IV 10 mg/kg immediately before dental extraction, followed by 10 mg/kg 3 to 4 times daily for 2 to 8 days, together with replacement therapy.Renal Function Impairment
- Serum creatinine 1.5 to 2.8 mg/dL: 1,300 mg twice daily;
- serum creatinine 2.9 to 5.7 mg/dL: 1,300 mg once daily;
- serum creatinine greater than 5.7 mg/dL: 650 mg once daily.
- Serum creatinine 1.36 to 2.83 mg/dL: 10 mg/kg twice daily;
- serum creatinine 2.83 to 5.66 mg/dL: 10 mg/kg once daily;
- serum creatinine greater than 5.66: 10 mg/kg every 48 h or 5 mg/kg every 24 h.
- IV infusion
- Compatible with most solutions for infusion. Heparin may be added to tranexamic acid injection.
- Do not mix tranexamic acid injection with blood or solutions containing penicillin.
- Do not inject at a more rapid rate than 1 mL/min.
- Administer without regard to meals.
- Swallow tablets whole; do not break, chew, or crush.
Store at 59° to 86°F. Tranexamic acid injection should be prepared the same day the solution is to be infused.
Drug InteractionsFactor IX complex concentrates, anti-inhibitor coagulant concentrates
Coadministration of tranexamic acid and factor IX complex concentrates or anti-inhibitor coagulant concentrates may increase the risk of thrombosis. Avoid coadministration.Hormonal contraceptives
Coadministration of tranexamic acid and hormonal contraceptives may exacerbate the increased thrombotic risk associated with combination hormonal contraceptives. Coadminister only if there is a strong medical need and if the benefit of treatment outweighs the potential for the increased risk of a thrombotic event. Additional clinical monitoring is warranted.Tissue plasminogen activators
Coadministration may decrease the efficacy of both tranexamic acid and tissue plasminogen activators. Use with caution. Additional clinical monitoring is warranted.Tretinoin
Coadministration of tretinoin with tranexamic acid may increase the risk of severe thromboembolic reactions. Use with caution. Additional clinical monitoring is warranted.
Laboratory Test Interactions
None well documented.
Hypotension (with rapid IV infusion); thromboembolic events (eg, acute renal cortical necrosis, central retinal artery and vein obstruction, cerebral thrombosis, deep venous thrombosis, pulmonary embolism) (postmarketing).
Headache (50%); migraine (6%); fatigue (5%).
Impaired color vision and visual disturbances (postmarketing)
Abdominal pain (20%); diarrhea, nausea, vomiting.
Back pain (21%); musculoskeletal pain (11%); arthralgia, muscle cramps and spasms (7%).
Nasal and sinus symptoms (25%).
Anaphylactic shock and anaphylactoid reactions (postmarketing).
Monitor for symptoms of severe allergic reaction and changes in vision. Patients treated continually for longer than several days should undergo ophthalmologic evaluation (eg, visual acuity, color vision, eye-ground and visual fields) prior to starting therapy and at regular intervals.
Category B .
Excreted in breast milk.
Safety and efficacy not established for cyclic heavy menstrual bleeding.
Not intended for use by postmenopausal women (oral).
Severe allergic reaction (dyspnea, facial flushing, tightening of throat) and anaphylactic shock have been reported.
Dosage adjustment needed because of the risk of accumulation.
May be caused by use of tranexamic acid in patients with subarachnoid hemorrhage.
Patients with DIC must be under strict supervision of a health care provider while on therapy with tranexamic acid.
Retinal venous and arterial occlusion has been reported. Discontinue therapy if suspected and refer patient to ophthalmologist for evaluation.
Has been reported in patients with upper urinary tract bleeding treated with tranexamic acid.
Arterial, embolic, or venous thromboembolism; diarrhea, nausea, vomiting; hypotension or orthostatic symptoms; mental status changes; myoclonus; rash; visual impairment.
- Inform patients that they should immediately stop therapy if they notice any eye symptoms or changes in vision. Instruct them to report such problems promptly to their health care provider and to follow up with an ophthalmologist.
- Inform patients that they should stop therapy and seek immediate medical attention if they notice symptoms of severe allergic reaction (eg, shortness of breath, throat tightening).
- Instruct patients to report any of the following symptoms to their health care provider: chest pain, leg pain or swelling, shortness of breath, sudden severe headache, or vision changes.
- Instruct patients not to exceed 6 tablets in a 24 h period or to take for more than 5 days in a menstrual cycle.
- Advise patients to contact their health care provider if heavy menstrual bleeding symptoms persist or worsen.
Copyright © 2009 Wolters Kluwer Health.
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