Transamin

Transamin

tranexamic acid

Manufacturer:

Daiichi-Sankyo

Distributor:

Zuellig Pharma
Full Prescribing Info
Contents
Tranexamic acid.
Description
Each capsule also contains the following inactive ingredients: Corn starch, colloidal silicon dioxide and magnesium stearate.
Each tablet also contains the following inactive ingredients: Carmellose calcium, polyvinyl alcohol, glyceryl behenate, magnesium stearate, HPMC 2910, PEG 6000, titanium dioxide, silicone resin and talcum.
Each 5-mL ampoule contains tranexamic acid 250 mg (50 mg/mL) and water for injection for a volume of 5 mL. The pH of the solution is 7-8, with an osmotic pressure ratio (to saline solution) of about 1.
Tranexamic acid is 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).
Action
Pharmacology: In physiological and pathologic conditions, fibrinolysis affects enhancement of vascular permeability, and relevant to the development, progression and healing of hemorrhage; allergy and other biological reactions (ampoule) induced by plasmin. Tranexamic acid inhibits the activity of plasmin, thereby exhibiting antihemorrhagic effects.
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 eg, α2-macroglobulin in the plasma, the antifibrinolytic action of tranexamic acid is even further strengthened.
Hemostatic Action: When the blood level of plasmin is abnormally elevated, various phenomena occur eg, 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 2063 out of 2802 patients (73.6%) with a bleeding tendency caused by diseases eg, leukemia, aplastic anemia and purpura, which are considered to be associated with systemic hyperfibrinolysis or abnormal bleeding eg, pulmonary and vaginal hemorrhage, renal, intraoperative and postoperative bleeding.
Pharmacokinetics: Blood Concentration: Capsule/Tablet: When a single dose of tranexamic acid was administered orally to healthy adults, the pharmacokinetic parameters were shown as follows. (See Table 1 and Figure 1.)

Click on icon to see table/diagram/image


Click on icon to see table/diagram/image

Ampoule: When a single dose of tranexamic acid 500 mg was administered IM or 1000 mg was administered IV to healthy adults, the time-plasma concentration were as follows. (See Figure 2 and Table 2.)

Click on icon to see table/diagram/image


Click on icon to see table/diagram/image

Distribution: Reference Information (Animal Study): Capsule/Tablet: 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 hrs. Levels in kidney and liver were higher, and those of other organs were lower than that of the blood.
Ampoule: When 14C-tranexamic acid was administered IV or IM 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.
Metabolism and Excretion: When a single dose of tranexamic acid (250 mg or 500 mg) was administered orally, or 500 mg and 1000 mg administered IM or IV, respectively, to healthy adults, it was rapidly absorbed and about 40-70% orally, and about 80% and 76%, IM and IV, respectively, of the administered dose was excreted as unchanged form in the urine within 24 hrs of administration.
Indications/Uses
Abnormal bleeding and its symptoms in hemorrhagic disease (purpura, aplastic anemia, cancer, leukemia). Bloody sputum and hemoptysis in pulmonary tuberculosis. Renal and genital bleeding. Bleeding in prostatomegaly. Abnormal bleeding during operation.
Menorrhagia [(heavy menstrual bleeding) for tablets and capsules only].
Dosage/Direction for Use
Oral: Adults: Usual Dose: 1-2 capsules (250 mg) 3 times a day or 1 tab (500 mg) 3-4 times a day.
Menorrhagia (Heavy Menstrual Bleeding): Adults: Recommended Dose: 4 capsules or 2 tablets (1 g) 3 times a day starting on the 1st day of period for days of heavy flow.
IV or IM: 1-2 amps/day (5-10 mL) (250-500 mg/day) in 1-2 divided doses. During or after surgery, 2-10 amps (10-50 mL) (500-2500 mg) are given by IV drip infusion, if necessary.
The dosage of Transamin should be individualized in accordance with patient's age and clinical condition.
Administration: Precautions for IV Administration: With regard to IV administration, inject Transamin slowly. (Symptoms eg, nausea, chest discomfort, palpitations and a fall in blood pressure may rarely occur.)
Precautions for IM Administration: With regard to IM injection, pay careful attention to the following points to avoid injuring tissues, nerves: Inject Transamin carefully to avoid contact with nerves.
If repeated injection is required, change the injection site (eg, alternate between the right and left arms). Special care should be observed when Transamin is administered to premature infants, newborns, suckling infants and children.
If insertion of the injection needle induces intense pain or blood flows back into the syringe, withdraw the needle immediately and perform injection at a different site.
Overdosage
No safety information.
Contraindications
Hypersensitivity to tranexamic acid or to any other components of Transamin. Patients receiving thrombin. (See Interactions.)
Special Precautions
Careful Administration: Transamin should be administered with care in the following patients: Patients with thrombosis (eg, cerebral thrombosis, myocardial infarction or thrombophlebitis) and patients at risk of thrombosis. Transamin may stabilize thrombosis.
Patients with consumption coagulopathy (use concomitantly with heparin). Transamin may stabilize thrombosis.
Post-operative, 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.
Patients with renal failure. Blood concentration may increase.
Patients with a history of hypersensitivity to any of the component of Transamin.
Other Precautions: Retinal degeneration has been reported with tranexamic acid in dogs after long-term, high-dose administration.
Use in Pregnancy & Lactation: Pregnancy Category: B. No safety information.
Use in the Elderly: Since elderly patients often have reduced physiological function, careful supervision and measures eg, reducing the dose are recommended.
Use In Pregnancy & Lactation
Pregnancy Category: B. No safety information.
Adverse Reactions
Capsule/Tablet: The most frequently observed adverse reactions reported in a total of 2954 patients were anorexia 0.61% (18 events), nausea 0.41% (12 events), vomiting 0.2% (6 events), heartburn 0.17% (5 events), itching 0.07% (2 events) and rash 0.07% (2 events).
Clinically Significant Adverse Reactions (Frequency Unknown*): Convulsion: Incidence of convulsion was reported in dialysis patients. Patients should be carefully monitored, and appropriate measures eg, discontinuing treatment, should be taken if any abnormality is observed.
The following adverse reactions may occur. Patients should be carefully monitored and appropriate measures eg, discontinuing treatment, should be taken if any abnormality is observed.
Hypersensitivity (<0.1%): Itching, rash.
Gastrointestinal (0.1% to <1%): Anorexia, nausea, vomiting, diarrhea, heartburn.
Other (<0.1%): Drowsiness.
*The frequency of adverse reactions on the basis spontaneous reports is unknown.
Ampoule: Summary of the incidence of adverse reactions: The most frequently observed adverse reactions reported in a total of 2972 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).
Clinically Significant Adverse Reactions (Frequency Unknown*): Shock: Since shock may occur, patients should be carefully monitored and appropriate measures eg, discontinuing treatment, should be taken if any abnormality is observed. (See also Other Adverse Reactions as follows.)
Convulsion: Incidence of postsurgical convulsion was reported in patients underwent cardiac macrovascular surgery assisted with cardiopulmonary bypass and received perioperative Transamin treatment. Incidence of convulsion was reported in dialysis patients. Patients should be carefully monitored, and appropriate measures eg, discontinuing treatment, should be taken if any abnormality is observed.
Other Adverse Reactions: Hypersensitivity (<0.1%): Itching, rash.
Gastrointestinal (0.1% to <1%): Nausea, vomiting. (<0.1%): Anorexia, diarrhea.
Ocular (Unknown*): Transient defective color vision (IV injection).
Others (<0.1%): Drowsiness, headache.
*The frequency of adverse reactions on the basis spontaneous reports or overseas resources is unknown.
Drug Interactions
Contraindications for Co-Administration: Transamin should not be co-administered with thrombin. Co-administration may cause a thrombosis tendency. It increases the tendency towards thrombosis due to the thrombogenic property of Transamin.
Precautions for Co-Administration: Transamin should be administered with care when co-administered with the following drugs.
Hemocoagulase: Co-administration at high doses may cause a thrombosis tendency. Due to the antiplasmin action of Transamin, fibrin clots formed by hemocoagulase may persist in the blood stream for a relatively long period of time, which may result in a prolonged thrombotic state.
Batroxobin: Co-administration may cause thromboembolism. Transamin inhibits the decomposition of desA fibrin polymer produced by batroxobin.
Coagulation Factor Agents (Eptacog-α): Coagulation may be further activated at sites with enhanced local fibrinolysis eg, the oral cavity. Coagulation factors exert hemostatic actions by activating the coagulation system, where as tranexamic acid exerts hemostatic actions by inhibiting the fibrinolytic system.
Caution For Usage
Instructions for Use and Handling: Tablet: Instructions must be given to remove Transamin from the press-through package (PTP) 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 eg, mediastinitis.
Ampoule: Precautions When Opening the Ampoule: To avoid contamination with foreign matter, wipe with an alcohol swab before opening the ampoule.
A 'one-point-cut ampoule' is used for Transamin. Hold the ampoule with the mark on the neck upwards and break it open by pressure.
Storage
Capsule/Tablet: Store below 30°C.
Ampoule: Store below 25°C.
MIMS Class
ATC Classification
B02AA02 - tranexamic acid ; Belongs to the class of amino acid antifibrinolytics. Used in the treatment of hemorrhage.
Presentation/Packing
Cap 250 mg (orange cap, yellow body, with identification code D605; white cap and body) x 10 x 10's. FC tab 500 mg (white to light yellowish white, caplet type, with identification code D608) x 10 x 10's. Soln for inj (amp) 50 mg/mL (clear, colorless solution) x 5 mL x 1's.
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