Transamin Injection

Tranexamic acid.

Each 5 ml ampoule of Transamin Injection solution for infusion contains 250 mg of Tranexamic acid (50 mg/mL) as active ingredient and water for injection for a volume of 5 mL.
Content of Tranexamic acid in 1 ampoule: 250mg/5mL (5%W/V).
pH: 7.0-8.0.
Osmotic pressure ratio (to Saline Solution): About 1.
PHYSICOCHEMISTRY: Nonproprietary name: Tranexamic acid.
Chemical name: trans-4-(Aminomethyl) cyclohexanecarboxylic acid.
Molecular formula: C₈H₁₅NO₂.
Molecular weight: 157.21.
Tranexamic acid occurs as white crystals or powder. It is freely soluble in water and practically insoluble in ethanol (99.5).

PHARMACOLOGY: In physiological and pathologic conditions, fibrinolysis affects enhancement of vascular permeability and relevant to the development, progression and healing of hemorrhage and other biological reactions induced by plasmin. Tranexamic acid inhibits the activity of plasmin, thereby exhibiting anti-hemorrhagic effects.
1. Antiplasmin action: Tranexamic acid inhibits the binding of plasmin or plasminogen to fibrin by strongly binding to the lysine binding site (LBS) of fibrin which is also the binding site for plasmin and plasminogen. Therefore, Tranexamic acid strongly inhibits fibrinolysis induced by plasmin. In addition, in the presence of antiplasmins, such as a₂-macroglobulin in the plasma, the antifibrinolytic action of tranexamic acid is even further strengthened.
2. Hemostatic action: When the blood level of plasmin is abnormally elevated, various phenomena occur, such as inhibition of platelet aggregation and decomposition of coagulation factors occur. Even slight elevation in the blood level of plasmin specifically induces fibrinolysis. Tranexamic acid is considered to exhibit a hemostatic effect by inhibiting fibrinolysis in common hemorrhages.
PHARMACOKINETICS: 1. Blood concentration: When a single dose of 500 mg Tranexamic acid was administered intramuscularly or 1,000 mg was administered intravenously to healthy adults, the time plasma concentration were as follows. (See figure and Table 1.)

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2. Distribution: Reference information (animal study): When ¹⁴C-tranexamic acid was administered intravenously or intramuscularly to mice, the distribution in the tissue was highest in the liver, kidneys and lungs, followed by pancreas, adrenals, spleen, prostate, colon, uterus, heart and muscle. Levels in the brain were low.
3. Metabolism and excretion: When a single dose of 500 mg Tranexamic acid was administered intramuscularly or 1,000 mg was administered intravenously to healthy adults, it was rapidly absorbed and about 80% and 76% of the administered dose was respectively excreted unchanged form in the urine within 24 hours of administration.

Abnormal bleeding and its symptoms in hemorrhagic disease (purpura, aplastic anemia, cancer, leukemia etc.); Bloody sputum and hemoptysis in pulmonary tuberculosis; Renal bleeding; Genital bleeding; Bleeding in prostatomegaly; Abnormal bleeding during operation.

Transamin Injection: One to two ampoules (5-10 mL) a day are administered intravenously or intramuscularly, divided in 1 to 2 doses. During or after operation, if necessary, 2 to 10 ampoules (10-50 mL) are given by intravenous drip infusion.
Dosage of Transamin should be individualized in accordance with patient's age and clinical condition.

No safety information.

Transamin is contraindicated in the following patients: 1. Patients receiving thrombin (See Interactions).
2. Patients with a history of hypersensitivity to any of the ingredients of the product.

Careful Administration (Transamin should be administered with care in the following patients): (1) Patients with thrombosis (e.g., cerebral thrombosis, myocardial infarction or thrombophlebitis, etc.) and patients at risk of thrombosis [Transamin may stabilize thrombosis].
(2) Patients with consumption coagulopathy (Use concomitantly with heparin, etc.) [Transamin may stabilize thrombosis].
(3) Postoperative, recumbent ridden patients and patients undergoing astriction [Venous thrombosis is likely to occur in these patients, and Transamin may stabilize thrombosis. Pulmonary embolism has been reported in association with resolution of recumbency or removal of astriction].
(4) Patients with renal failure [Blood concentration may increase].
Precautions concerning Use: (1) Precautions for intravenous administration: With regard to intravenous administration, inject the drug slowly. (Symptoms such as nausea, chest discomfort, palpitations and a fall in blood pressure may rarely occur.)
(2) Precautions for intramuscular administration: With regard to intramuscular injection, pay careful attention to the following points to avoid injuring tissues, nerves, etc.: 1) Inject the drug carefully to avoid contact with nerves.
2) If repeated injection is required, change the injection site (e.g. alternate between the right and left arms).
Special care should be observed when the drug is administered to premature infants, newborns, suckling infants and children.
3) If insertion of the injection needle induces intense pain or if blood flows back into the syringe, withdraw the needle immediately and perform injection at a different site.
(3) Precautions when opening the ampoule: To avoid contamination with foreign matter, wipe them off with an alcohol swab before opening the ampoule.
Other Precautions: Retinal degeneration has been reported with Tranexamic acid in dogs after long-term, high-dose administration.
Use in Pregnancy & Lactation: No safety information.
Use in the Elderly: Since elderly patients often have reduced physiological function, careful supervision and measures such as reducing the dose are recommended.

No safety information.

Summary of the incidence of adverse reactions: The most frequently observed adverse reactions reported in a total of 2,972 patients were nausea 0.07% (2 events), vomiting 0.17% (5 events), anorexia 0.03% (1 event), diarrhea 0.07% (2 events) and drowsiness 0.03% (1 event) (based on data obtained from the literature [outside the scope of reexamination]).
(1) Clinically significant adverse reactions (frequency unknown*): 1) Shock: Since shock may occur, patients should be carefully monitored, and appropriate measures, such as discontinuing treatment should be taken if any abnormality is observed.
2) Convulsion: Incidence of postsurgical convulsion was reported in patients who underwent cardiac macrovascular surgery assisted with cardiopulmonary bypass and received perioperative Transamin treatment. An incidence of convulsion was reported in dialysis patients. Patients should be carefully monitored, and appropriate measures, such as discontinuing treatment, should be taken if any abnormality is observed.
(2) Other adverse reactions: The following adverse reactions may occur. Patients should be carefully monitored, and appropriate measures, such as discontinuing treatment should be taken if any abnormality is observed. (See Table 2.)

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1) Contraindications for coadministration (Transamin should not be coadministered with the following drugs): See Table 3.

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2) Precautions for coadministration (Transamin should be administered with care when coadministered with the following drugs): See Table 4.

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A "one-point-cut ampoule" is used for this product. Hold the ampoule with the mark on the neck upwards and break it open by pressure.

Store below 30°C.

Haemostatics

B02AA02 - tranexamic acid ; Belongs to the class of amino acid antifibrinolytics. Used in the treatment of hemorrhage.

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