tranexamic acid injection (Rx)

Brand and Other Names:Cyklokapron
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

injectable solution

  • 100mg/mL

Dental Extraction in Patients with Hemophilia

Indicated in patients with hemophilia for short-term use (ie, 2-8 days) to reduce/prevent hemorrhage and reduce the need for replacement therapy during and following tooth extraction

10 mg/kg IV immediately before surgery OR 10 mg/kg IV q6-8hr 1 day before surgery  

25 mg/kg PO q6-8hr 1 day presurgery AND 2-8 days postsurgery

CABG (Off-label)

10-15 mg/kg IV over 20 minutes, THEN 1 mg/kg/hr continuous infusion for 6-10 hours  

Hereditary Angioedema (Off-label)

Long-term prophylaxis: 1000-1500 mg PO q8-12hr; reduce dose to 500 mg/dose PO qDay or q12hr when frequency of attacks reduces

Short term prophylaxis: 75 mg/kg/day PO divided q8-12hr for 5 days before and after the event  

Treatment of acute HAE attack: 25 mg/kg/dose PO/IV; not to exceed 1000 mg/dose q3-4hr; not to exceed 75 mg/kg/day or 1000 mg PO q6hr for 48 hr

Total Knee Replacement Surgery, Blood Loss Reduction (Off-label)

10 mg/kg IV over 30 min before inflation of tourniquet and 3 hr after first dose  

Hyphema (Off-label)

25 mg/kg PO q8hr for 5-7 days  

Renal Impairment

Dental Extraction

  • SCr 1.36-2.83 mg/dL (120-250 micromoles/L): 10 mg/kg IV q12hr OR 15 mg/kg PO q12hr
  • SCr 2.83-5.66 mg/dL (250-500 micromoles/L): 10 mg/kg IV qDay OR 15 mg/kg PO qDay
  • SCr >5.66 mg/dL (>500 micromoles/L): 10 mg/kg IV q48hr OR 15 mg/kg PO q48hr; alternatively, 5 mg/kg IV qDay OR 7.5 mg/kg PO qDay

Dosage Forms & Strengths

injectable solution

  • 100mg/mL

Dental Extraction in Patients with Hemophilia

10 mg/kg IV immediately before surgery OR 10 mg/kg IV q6-8hr 1 day before surgery

25 mg/kg PO q6-8hr 1 day presurgery AND 2-8 days postsurgery

Hyphema (Off-label)

25 mg/kg PO q8hr for 5-7 days

Hereditary Angioedema (Off-label)

Long term prophylaxis: 20-40 mg/kg/day PO divided q8-12hr; reduce dosing frequency to every other day or twice weekly when frequency of attacks reduces

Short term prophylaxis: 20-40 mg/kg/day PO divided q8-12hr; initiate 2-5 days before and continue for 2 days after the procedure

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Interactions

Interaction Checker

and tranexamic acid injection

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    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

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            Adverse Effects

            Frequency Not Defined

            Visual abnormalities

            Hypotension (with rapid injection)

            Nausea

            Vomiting

            Diarrhea

            Anaphylaxis

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            Warnings

            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

            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
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            Pregnancy & Lactation

            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.

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            Pharmacology

            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%)

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            Administration

            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)

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            Formulary

            FormularyPatient Discounts

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            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
            QL Quantity Limits
            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
            ST Step Therapy
            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
            OR Other Restrictions
            Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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            Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.