Tranexamic Acid (tranexamic acid)
Last reviewed · Source: First Databank (FDB) drug data
Overview
Tranexamic acid, a synthetic derivative of lysine, is an antifibrinolytic agent.
Tranexamic acid, a synthetic lysine derivative, is an antifibrinolytic agent that reduces bleeding by preventing the breakdown of fibrin clots. The drug blocks the lysine binding sites of plasminogen, thereby inhibiting fibrin binding to plasminogen and impairing the endogenous fibrinolytic process; as a result, the fibrin matrix structure is preserved and stabilized. The binding affinity of tranexamic acid to plasminogen and plasmin is about 6-10 times more potent than aminocaproic acid.
The antifibrinolytic effects of tranexamic acid are manifested by reductions in D-dimer levels. Thrombin time is prolonged at tranexamic acid blood concentrations of 1 and 10 mg/mL. At concentrations less than 10 mg/mL, no effects on platelet counts, coagulation time, or various coagulation factors are observed.
Following oral administration, peak plasma concentrations of tranexamic acid are obtained in approximately 3 hours. The absolute bioavailability following oral administration is approximately 45%. Administration of a single oral dose of tranexamic acid 1.3 g with food increased the maximum serum concentration and AUC of the drug by 7 and 16%, respectively; tranexamic acid tablets may be administered with or without food.
Plasma protein binding is about 3% with no apparent binding to albumin. Only a small fraction of the drug is metabolized. Tranexamic acid is eliminated principally by urinary excretion via glomerular filtration; more than 95% of the dose is excreted as unchanged drug.
Mean terminal half-life of orally administered tranexamic acid is about 11 hours. Following IV administration, apparent elimination half-life is approximately 2 hours.
Generic name: tranexamic acid
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on Tranexamic Acid
Indications
The following indications are listed for Tranexamic Acid:
- Bleeding Prevention In Hemophilia
- Hemorrhaging In Hemophilia
Also known as: Bleeding Prophylaxis In Hemophilia, Hemorrhage Prophylaxis In Hemophilia.
Dosing
No dosing information is available for this tab.
Tranexamic acid is administered orally or by slow IV injection or IV infusion. The drug also has been administered topically+ (as a solution via irrigation, mouthwash, or gauze pad) for local application such as during dental procedures; however, a topical preparation is not commercially available in the US.
No dosing information is available for this tab.
No dosing information is available for this tab.
Drug interactions
The manufacturers state that no drug interaction studies have been conducted with tranexamic acid.
There are no contraindication interactions for this drug.
There are no severe interactions for this drug.
There are no moderate interactions for this drug.
Contraindications
*Neuraxial (i.e., intrathecal, epidural) injection.
*Patients with subarachnoid hemorrhage; tranexamic acid may cause cerebral edema and cerebral infarction in such patients.
*Patients with active thromboembolic disease (e.g., deep-vein thrombosis, pulmonary embolism, cerebral thrombosis, active intravascular clotting) or a history or risk of thromboembolism, including retinal vein or artery occlusion; intrinsic risks include thrombogenic valvular disease, thrombogenic cardiac rhythm disease, or hypercoagulopathy.
*Concomitant use of oral tranexamic tablets with combination hormonal contraceptives.
*Hypersensitivity reactions to tranexamic acid or any other ingredients in the preparation.
There are no contraindication contraindications for this drug.
There are no severe contraindications for this drug.
There are no moderate contraindications for this drug.
Adverse reactions
The manufacturer states that the most common adverse effects of IV tranexamic acid include nausea, vomiting, diarrhea, allergic dermatitis, giddiness, hypotension, and thromboembolic events.
The manufacturer states that the most common adverse effects of oral tranexamic acid include headache, sinus and nasal symptoms, back pain, abdominal pain, musculoskeletal pain, joint pain, muscle cramps, migraine, anemia, and fatigue.
There are no severe adverse reactions for this drug.
There are no less severe adverse reactions for this drug.
Precautions
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There are limited data on the use of tranexamic acid in pediatric patients with hemophilia undergoing tooth extraction.
The manufacturer of tranexamic acid tablets states that the drug is indicated for use in females of reproductive age and is not intended for premenarchal girls.
The available information suggests that there are no significant pharmacokinetic differences between adults and pediatric patients.
It is not known whether tranexamic acid use is associated with a risk of adverse maternal or fetal outcomes; however, the drug is known to cross the placenta and appears in cord blood in concentrations similar to maternal concentrations. The potential risks to the fetus should be considered along with potential benefits of the drug and the mother's clinical need for tranexamic acid.
There are no adequate and well-controlled studies of tranexamic acid in pregnant women. Fatal structural abnormalities have been reported in 2 cases when tranexamic acid was used during conception or the first trimester of pregnancy; however, it is not clear whether these effects were related to the drug or other factors. Animal reproduction studies have not revealed any evidence of adverse fetal or developmental effects from in utero exposure to tranexamic acid.
Tranexamic acid is distributed into human milk. It is not known whether the drug has any effects on the breastfed infant or on milk production. The known benefits of breast-feeding should be considered along with the mother's clinical need for tranexamic acid and the potential adverse effects on the infant from the drug or underlying maternal condition.
Care should be taken in dosage selection in geriatric patients because they are more likely to have decreased renal function.
Clinical studies of tranexamic acid injection did not include sufficient numbers of patients 65 years of age and older to determine whether they respond differently from younger patients. Other reported clinical experience has not identified differences in responses between geriatric and younger patients.
Tranexamic acid is substantially excreted by the kidneys; because geriatric patients are more likely to have decreased renal function, dosage should be selected carefully and renal function monitoring should be considered in such patients.
The manufacturer of tranexamic acid tablets states that the drug is indicated for use in women of reproductive age and is not intended for use by postmenopausal women.
ICD codes
No ICD codes are available for this drug.
Formulary status
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Last reviewed · Source: First Databank (FDB) drug data
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