tranexamic acid injection (Rx)

Frequency Not Defined

Visual abnormalities

Hypotension (with rapid injection)

Nausea

Vomiting

Diarrhea

Anaphylaxis

Contraindications

Hypersensitivity

Acquired defective color vision

Subarachnoid hemorrhage

Active intravascular clotting

Cautions

Use caution in renal impairment, subarachnoid hemorrhage, vascular disease, thromboembolic history, and DIC

Ureteral obstruction resulting from clot formation reported; use caution in patients with upper urinary tract bleeding

Thromboembolism or venous and arterial thrombosis reported

Ligneous conjunctivitis has been reported

Concurrent use with anti-inhibitor coagulant complex/factor IX complex concentrates may further increase risk of thrombosis

Concurrent use with tretinoin may exacerbate procoagulant effects

Anaphylaxis reported with intravenous administration

For intravenous use only; serious adverse reactions including seizures and cardiac arrythmias have occurred when drug inadvertently administered intrathecally instead of intravenously; confirm correct route of administration and avoid confusion with other injectable solutions that might be administered at same time as the drug; syringes containing drug should be clearly labeled with intravenous route of administration

Visual disturbances

• Visual defects (color vision change or visual loss) reported
• In addition, although not seen in humans, focal areas of retinal degeneration have been observed in cats and dogs following oral or intravenous tranexamic acid at doses between 250 to 1600 mg/kg/day (1.6 to 22 times recommended usual human dose based on body surface area) from 6 days to 1 year
• No retinal changes observed in eye examinations of patients treated with tranexamic acid for up to 8 years; patients expected to be treated for greater than 3 months may consider ophthalmic monitoring including visual acuity and optical coherence tomography at regular intervals; discontinue tranexamic acid in sodium chloride injection if changes in ophthalmological examination occur

Seizures

• May cause seizures, including focal and generalized seizures; the most common setting for tranexamic acid-induced seizures has been during cardiovascular surgery (a setting in which drug is not FDA approved and which uses doses of up to ten-fold higher than recommended human dose and in patients inadvertently given tranexamic acid into the neuraxial system)
• Consider dose reduction during surgery and dose adjustments for patients with clinical conditions such as renal dysfunction; closely monitor patient during surgery
• Consider electroencephalogram (EEG) monitoring for patients with history of seizures or who experience myoclonic movements, twitching, or show evidence of focal seizures; discontinue drug if seizures occur

Pregnancy

Available data from published studies, case series and case reports with tranexamic acid use in pregnant women in second and third trimester and at time of delivery have not clarified whether there is a drug-associated risk of miscarriage or adverse maternal or fetal outcomes

There are 2 (0.02%) infant cases with structural abnormalities that resulted in death when tranexamic acid was used during conception or first trimester of pregnancy; however, due to other confounding factors the risk of major birth defects with use of tranexamic acid during pregnancy is not clear

Drug is known to pass the placenta and appears in cord blood at concentrations approximately equal to maternal concentration

Animal data

• Reproduction studies performed in mice, rats, and rabbits have not revealed any adverse effects on fetus due to tranexamic acid administered during organogenesis; doses examined were multiples of up to 3 times (mouse), 6 times (rat), and 3 times (rabbit) maximum human dose based on body surface area in the mouse, rat, and rabbit, respectively

Contraception

• Concomitant use of drug, which is an antifibrinolytic, with hormonal contraceptives may increase risk for thromboembolic adverse reactions; advise patients to use an effective alternative (nonhormonal) contraceptive method

Lactation

Published literature reports presence of tranexamic acid in human milk; there are no data on effects of drug on breastfed child or effects on milk production; developmental and health benefits of breastfeeding should be considered along with mother’s clinical need for drug and any potential adverse effects on breastfed child from drug or from underlying maternal condition

Pregnancy Categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

Mechanism of Action

Inhibits fibrinolysis by displacing plasminogen from fibrin

Reduces plasmin activity, which in turn reduces activation of complement and consumption of C1 esterase inhibitor (C1-NH) and subsequently decreases inflammation associated with hereditary angioedema

Pharmacokinetics

Half-Life: 2-11 hr

Duration: 3 hr (after 1 dose)

Peak Plasma time: 3 hr

Plasma concentration: 15 mg/L

Protein Bound: 3%

Vd: 9-27 L

Clearance: 110-116 mL/min

Excretion: Urine (95%)

IV Incompatibilities

Additive: blood, penicillin

IV Compatibilities

Solution: compatible with most common solutions for infusion

Additive: heparin

IV Preparation

Prepare solution same day it will be used

Dilute a single dose w/t 50 mL compatible fluid (eg, NS, Ringers, dextrose/water)

IV Administration

100 mg or fraction thereof over at least 1 min, usually 5 minutes

Avoid rapid infusion

Storage

Store at 25°C (77°F)