tranexamic acid oral (Rx)

Brand and Other Names:Lysteda
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablet

  • 650mg

Menorrhagia

Indicated for the treatment of cyclic heavy menstrual bleeding

1300 mg PO TID for up to 5 days during menstruation

Renal impairment

  • SCr >1.4 mg/dL and ≤2.8 mg/dL: 1300 mg PO BID
  • SCr >2.8 mg/dL and ≤5.7 mg/dL: 1300 mg PO qDay
  • SCr >5.7 mg/dL: 650 mg PO qDay
  • Each regimen listed above may be administered for up to 5 days during menstruation

Hepatic impairment

  • Dose adjustments not necessary

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

Cone Biopsy (Off-label)

1000-1500 mg q8-12hr x12 days postop

Epistaxis (Off-label)

1000-1500 mg q8-12hr x10 days

Hyphema (Off-label)

1000-1500 mg q8-12hr x7 days

Hereditary Angioedema (Off-label)

1000-1500 mg PO BID/TID

Administration

May take with or without food

Swallow whole, do not chew, break, or crush

Indicated for women of reproductive age and is not intended for use in premenarcheal girls

Based on a pharmacokinetic study in 20 adolescent females, aged 12-16 years, no dose adjustment is needed in the adolescent population

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Interactions

Interaction Checker

and tranexamic acid oral

No Results

     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Contraindicated (3)

            • dienogest/estradiol valerate

              tranexamic acid oral, dienogest/estradiol valerate. Either increases toxicity of the other by pharmacodynamic synergism. Contraindicated. Coadministration of tranexamic acid oral and combination hormonal contraceptives increases thrombotic risk.

            • ethinylestradiol

              tranexamic acid oral, ethinylestradiol. Either increases toxicity of the other by pharmacodynamic synergism. Contraindicated. Coadministration of tranexamic acid oral and combination hormonal contraceptives increases thrombotic risk.

            • mestranol

              tranexamic acid oral, mestranol. Either increases toxicity of the other by pharmacodynamic synergism. Contraindicated. Coadministration of tranexamic acid oral and combination hormonal contraceptives increases thrombotic risk .

            Serious - Use Alternative (4)

            • anti-inhibitor coagulant complex

              tranexamic acid oral, anti-inhibitor coagulant complex. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Coadministration may increase risk for thrombosis.

              anti-inhibitor coagulant complex, tranexamic acid oral. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Coadministration ma.

            • Factor IX

              tranexamic acid oral, Factor IX. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Coadministration may increase risk for thrombosis.

            • Factor IX complex

              tranexamic acid oral, Factor IX complex. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Coadministration may increase risk for thrombosis.

            • Factor IX, recombinant

              tranexamic acid oral, Factor IX, recombinant. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Coadministration may increase risk for thrombosis.

            Monitor Closely (5)

            • alteplase

              tranexamic acid oral, alteplase. Either decreases effects of the other by pharmacodynamic antagonism. Modify Therapy/Monitor Closely.

            • defibrotide

              tranexamic acid oral decreases effects of defibrotide by pharmacodynamic antagonism. Modify Therapy/Monitor Closely. Defibrotide may diminish effects of thrombolytic agents. Consider therapy modification.

            • reteplase

              tranexamic acid oral, reteplase. Either decreases effects of the other by pharmacodynamic antagonism. Modify Therapy/Monitor Closely.

            • tenecteplase

              tranexamic acid oral, tenecteplase. Either decreases effects of the other by pharmacodynamic antagonism. Modify Therapy/Monitor Closely.

            • tretinoin

              tranexamic acid oral, tretinoin. Either increases toxicity of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Coadministration may increase procoagulant effect.

            Minor (0)

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              Adverse Effects

              >10%

              Headache (50.4%)

              Nasal and sinus symptoms (25.4%)

              Back pain (20.7%)

              Abdominal pain (19.8%)

              Musculoskeletal pain (11.2%)

              1-10%

              Arthralgia (6.9%)

              Muscle cramps and spasms (5.8%)

              Migraine (6%)

              Anemia (5.6%)

              Fatigue (5.2%)

              Postmarketing Reports

              Nausea, vomiting, and diarrhea

              Allergic skin reactions

              Anaphylactic shock and anaphylactoid reactions

              Thromboembolic events (eg, DVT, pulmonary embolism, cerebral thrombosis, acute renal cortical necrosis, and central retinal artery and vein obstruction); cases have been associated with concomitant use of combination hormonal contraceptives Impaired color vision and other visual disturbances

              Dizziness

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              Warnings

              Contraindications

              Hypersensitivity

              Women using combination hormonal contraceptives

              Active thromboembolic disease (eg, DVT, pulmonary embolism, or 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, or hypercoagulopathy)

              Cautions

              Increased risk for thrombosis when coadministered with combination oral contraceptive (see Contraindications), Factor IX complex concentrates, anti-inhibitor coagulant concentrates, or oral tretinoin

              Venous and arterial thrombosis or thromboembolism, as well as cases of retinal artery and retinal vein occlusions, have been reported

              Severe allergic reaction reported; anaphylactic shock reported with IV product

              May cause cerebral edema and cerebral infarction in women with subarachnoid hemorrhage

              Ligneous conjunctivitis reported

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              Pregnancy & Lactation

              Pregnancy

              Not indicated for use in pregnant women; there are no available data on use in pregnant women to evaluate for a drug-associated risk of major birth defects, miscarriage or adverse maternal or fetal outcomes; tranexamic acid crosses the placenta; animal reproduction studies have not identified adverse developmental outcomes with oral administration of tranexamic acid to pregnant rats at doses up to 4 times the recommended human dose

              Lactation

              Tranexamic acid is present in the mother’s milk at a concentration of about one hundredth of the corresponding serum concentration; the amount of tranexamic acid a nursing infant would absorb is unknown; there are no adequate data on effects of tranexamic acid on breastfed infant or on milk production; the developmental and health benefits of breastfeeding should be considered along with the mother’s clinical need for therapy and any potential adverse effects on breast-fed child from therapy 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

              Antifibrinolytic; synthetic lysine amino acid derivative, which diminishes the dissolution of hemostatic fibrin by plasmin In the presence of tranexamic acid, the lysine receptor binding sites of plasmin for fibrin are occupied, preventing binding to fibrin monomers, thus preserving and stabilizing fibrin’s matrix structure

              Absorption

              Bioavailability: 45%

              Peak plasma time: 2.5 hr

              Peak plasma concentration: 16.41 mcg/mL (steady-state)

              AUC: 80.19 mcg•hr/mL

              Distribution

              Protein bound: 3%

              Vd: 0.18 L/kg (initial); 0.39 L/kg (steady-state)

              Metabolism

              Small fraction is metabolized

              Elimination

              Half-life: 11.08 hr

              Eliminated by urinary excretion primarily via glomerular filtration

              Excretion: 90% urine; >95% of the dose excreted unchanged

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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
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              Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the 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.