Transamin

Tablet: Each tablet contains Tranexamic Acid J.P. 500 mg.
Product description: See Table 1.

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PHYSICOCHEMISTRY: 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).
Excipients/Inactive Ingredients: Capsule: Each capsule also contains the following inactive ingredients: Corn starch, colloidal silicon dioxide and magnesium stearate.
Tablet: Each tablet contains the following inactive ingredients: Carmellose calcium, Polyvinyl alcohol,Glyceryl behenate, Magnesium stearate, HPMC 2910, PEG 6000, Titanium dioxide, Siliconeresin, Talcum.

PHARMACOLOGY: In physiological and pathologic conditions, fibrinolysis affects enhancement of vascular permeability and relevant to the development, progression and healing of hemorrhage induced by plasmin. Tranexamic acid inhibits the activity of plasmin, thereby exhibiting antihemorrhagic 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 α₂-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.
Even a 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 types of hemorrhage.
Tablet: CLINICAL STUDIES: Hemostatic Action: A hemostatic effect of Transamin was observed in 2,063 out of 2,802 patients (73.6%) with a bleeding tendency caused by diseases such as leukemia, aplastic anemia and purpura, which are considered to be associated with systemic hyperfibrinolysis or abnormal bleeding, such as pulmonary hemorrhage, vaginal hemorrhage, renal bleeding and intraoperative and postoperative bleeding.
PHARMACOKINETICS: 1. Blood concentration: The concentration in the blood, when 1,000 mg and 2,000 mg of tranexamic acid were administered orally to healthy adults, reached peak values 7 μg/ml and 14.4 μg/ml within 2-3 hours after administration.
When a single dose of tranexamic acid was administered orally to healthy adults, the pharmacokinetic parameters were as shown as follows. (See Table 2 and figure.)

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2. Distribution: Reference information (animal study): When a single dose of ¹⁴C-tranexamic acid was administered orally to rats, the concentration in most organs reached the peak values as well as the blood concentration after 2 hours. Levels in kidney and liver were higher and those of other organs were lower than that of the blood.
3. Metabolism and excretion: When a single dose (250 mg or 500 mg) of tranexamic acid was administered orally to healthy adults, it was rapidly absorbed and about 40 to 70% of the administered dose was excreted as unchanged form in the urine within 24 hours.

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; Menorrhagia.

Usual oral dose for adult is 1-2 capsules (250 mg) 3 times a day or 1 tablet 3-4 times a day. In menorrhagia indication, the recommended dose for adult is 4 capsules or 2 tablets (1 gm) 3 times a day starting on the first day of period for days of heavy flow.
Dosage of Transamin should be individualized in accordance with patient's age and clinical condition.

No safety information.

Transamln Is contraindicated In the following patients: Hypersensitivity to tranexamic acid or to any other components of Transamin.
Patients receiving thrombin. (See Interactions.)

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].
(5) Patients with a history of hypersensitivity to any of the components of this product.
Precautions concerning Use: For drugs that are dispensed in a press-through package (PTP), instruct the patient to remove the drug from the package prior to use. [It has been reported that, if the PTP sheet is swallowed, the sharp corners of the sheet may puncture the esophageal mucosa, resulting in severe complications such as mediastinitis.]
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.

The most frequently observed adverse reactions reported in a total of 2,954 patients were anorexia 0.61% (18 events), nausea 0.41% (12 events), vomiting 0.20% (6 events), heartburn 0.17% (5 events), itching 0.07% (2 events) and rash 0.07% (2 events) (Based on data obtained from the literature [outside the scope of reexamination]).
(1) Clinically significant adverse reactions (frequency unknown^Note): Convulsion: 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 reaction: 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 3.)

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^Note)The frequency of adverse reactions on the basis of spontaneous report is unknown.

1) Contraindications for coadministration (Transamin should not be coadministered with the following drugs): See Table 4.

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2) Precautions for coadministration (Transamin should be administered with care when coadministered with the following drugs): See Table 5.

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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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