tranexamic acid

Absorption: IV administration results in complete bioavailability; 45% absorbed following oral administration.

Distribution: Penetrates readily into joint fluid and synovial membranes.

Metabolism/Excretion: 95% excreted unchanged in urine.

Half-Life: IV: 2 hr (↑ in renal impairment); Oral: 11 hr.

Time/Action Profile ⬆ ⬇

(plasma concentrations)

ROUTE	ONSET	PEAK	DURATION
IV	unknown	unknown	7–8 hr
PO	unknown	2.5 hr	unknown

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Hypersensitivity;
Thromboembolic disorders (current, history of, or at risk for);
Acquired defective color vision (IV);
Subarachnoid hemorrhage;
Concurrent use of combination hormonal contraception (PO).

Use Cautiously in:

Renal impairment (↑ dosing interval);
Hematuria originating in the upper urinary tract;
Conditions associated with ↑ thrombus formation;
OB: Use during pregnancy only if potential maternal benefit justifies potential fetal risk;
Lactation: Use while breastfeeding only if potential maternal benefit justifies potential risk to infant.

Adv. Reactions/Side Effects ⬆ ⬇

CV: hypotension, thromboembolism

EENT: visual abnormalities

GI: diarrhea, nausea, vomiting

MS: pain

Neuro: headache, dizziness, SEIZURES

Misc:

ANAPHYLAXIS

Interactions ⬆ ⬇

Drug-drug:

Concurrent use of hormonal contraceptives with oral tranexamic acid may ↑ risk of thrombosis; concurrent use contraindicated.
Concurrent use of clotting factor complexes may ↑ the risk of thrombotic complications (give tranexamic acid 8 hr following clotting factor replacement therapy).
May ↑ the procoagulant effects of all-trans retinoic acid.
↓effectiveness with thrombolytic agents.

Route/Dosage ⬆ ⬇

IV (Adults and Children ): 10 mg/kg just prior to surgery with appropriate replacement therapy; then 10 mg/kg 3–4 times daily for 2–8 days.

Renal Impairment

IV (Adults and Children ): SCr 1.36–2.83 mg/dL: 10 mg/kg twice daily; SCr 2.83–5.66 mg/dL: 10 mg/kg daily; SCr >5.66 mg/dL: 10 mg/kg every 48 hr or 5 mg/kg once daily.
PO (Adults ): 1300 mg 3 times daily for a maximum of 5 days during menstruation.

Renal Impairment

PO (Adults ): SCr 1.41–2.8 mg/dL: 1300 mg twice daily for a maximum of 5 days during menstruation; SCr 2.81–5.7 mg/dL: 1300 mg daily for a maximum of 5 days during menstruation; SCr >5.7 mg/dL: 650 mg daily for a maximum of 5 days during menstruation.

Availability ⬆ ⬇

(Generic available)

Premixed infusion: 1 g/100 mL 0.7% NaCl
Solution for injection: 100 mg/mL
Tablets: 500 mg; 650 mg

Assessment ⬆ ⬇

Prevention of postsurgical hemorrhage: Observe site of surgery for excessive bleeding.
Heavy menstrual bleeding: Monitor menstrual flow prior to and during therapy.
Patients taking tranexamic acid for more than several days should have ophthalmologic examinations to detect visual abnormalities prior to and at regular intervals during and after therapy. Discontinue therapy if visual changes occur.

Implementation ⬆ ⬇

Serious adverse reactions, including seizures and arrhythmias, have occurred when administering tranexamic acid incorrectly via the intrathecal route instead of through the IV route. Confirm the correct route of administration for tranexamic acid, and avoid confusion with other injectable solutions that might be administered at the same time.
PO: Administer 3 times daily without regard to food. Swallow tablets whole; do not crush, break, or chew.

IV Administration:

Intermittent Infusion: Diluent: May be diluted with most solutions, such as electrolyte, carbohydrate, amino acid, and dextran solutions. Prepare mixture on day of infusion.
Rate: Infuse at a rate not to exceed 100 mg (1 mL)/min. More rapid administration has resulted in hypotension.

Patient/Family Teaching ⬆ ⬇

Instruct patient to take medication as directed; do not take more than 6 tablets/day, for longer that 5 days in any menstrual cycle, or when not menstruating. Take missed doses as soon as remembered; then take next dose as least 6 hr later; do not double doses. Advise patient to read Patient Information before starting and with each Rx refill in case of changes.
Advise patient to stop medication and inform health care professional of any changes in vision. Inform patients on prolonged therapy of the importance of regular ophthalmologic follow-up.
Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and consult health care professional before taking any new medications. Caution patient to avoid taking hormonal contraceptives and products containing aspirin or NSAIDs without consulting health care professional.
Instruct patient to notify health care professional if signs and symptoms of thrombosis (severe, sudden headache; pains in chest, groin, or legs, especially calves; sudden loss of coordination; sudden and unexplained shortness of breath; slurred speech; visual changes; weakness or numbness in arm or leg) or anaphylaxis (shortness of breath, throat tightness, rash) occur.
Instruct patient to notify health care professional if heavy menstrual bleeding persists or worsens or if bleeding does not lessen after 2 cycles or tranexamic acid seems to stop working.
Rep: Advise females of reproductive potential to notify health care professional if pregnancy is planned or suspected or if breastfeeding.

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Pronunciation ⬇

Classifications ⬆ ⬇

Indications ⬆ ⬇

Action ⬆ ⬇

Pharmacokinetics ⬆ ⬇