Antiallergic and anti-Inflammatory actions: Tranexamic Serum Creatinine (µmol/L) Tranexamic Acid Inj Dosage cases of central retinal artery and central retinal vein Acid inhibits the production of kinin and other active peptides, obstruction have been reported. Patients taking tranexamic etc. due to plasmin, which causes increase of vascular 120 to 250 (1.36 to 2.83 mg/dL) 10 mg/kg BID acid developed intracranial thrombosis; however, further permeability, allergies, and inflammatory lesions. 250 to 500 (2.83 to 5.66 mg/dL) 10 mg/kg daily observation is needed. (Tranexamic Acid) > 500 (> 5.66 mg/dL) 10 mg/kg every 48 hours Urinary tract obstruction due to clot formations in patients with 250mg, 500mg 500mg/5ml or 5 mg/kg every 24 hours Capsules IM/IV INJECTION PHARMACOKINETICS: severe bleeding from the upper urinary tract has been reported Blood concentrations: Tranexamic acid in concentration up For intravenous infusion, tranexamic acid injection may be in patients taking tranexamic acid. DESCRIPTION: Haemic (Tranexamic Acid) inhibits the action to 10 mg per mL blood has no influence on the platelet count, mixed with most solutions for infusion such as electrolyte Patients with disseminated intravascular coagulation who of plasmin and shows antihemorrhagic, antiallergic, and the coagulation time or various coagulation factors in whole solutions, carbohydrate solutions, amino acid solutions and require treatment with tranexamic acid must be under the strict anti-inflammatory effects. blood or citrated blood from normal subjects. On the other Dextran solutions. The mixture should be prepared the same supervision of a physician experienced in treating this disorder. hand, tranexamic acid in concentrations of 10 mg and 1 mg per day the solution is to be used. Heparin may be added to Patients with irregular menstrual bleeding should not use Structural Formula mL blood pro longs the thrombin time. tranexamic acid injection. Tranexamic acid injection should tranexamic acid until the cause of irregular bleeding has been Molecular Formula: C8H15NO2 The plasma protein binding of tranexamic acid is about 3% at NOT be mixed with blood. The drug is a synthetic amino acid, established. Consider an alternative treatment if menstrual Molecular Weight: 157.2g/mol therapeutic plasma levels and seems to be fully accounted for and should NOT be mixed with solutions containing penicillin. bleeding is not adequately reduced by tranexamic acid. by its binding to plasminogen. Tranexamic acid does not bind For adults 750 to 2000 mg/day of Tranexamic Acid is usually Indissoluble clots may develop in body cavities such as pleural to serum albumin. administered three to four times orally.The dosage should be space, joint spaces and urinary tract (e.g., renal pelvis, COMPOSITION After an intravenous dose of 1 g, the plasma concentration time adjusted according to the age of patients and severity of bladder) due to extravascular clots which may be resistant to Haemic 250mg Capsules: curve shows a triexponential decay with a half-life of about 2 symptoms. physiologic fibrinolysis. Each capsule contains: hours for the terminal elimination phase. The initial volume of Tranexamic Acid BP ...... 250mg distribution is about 9 to 12 liters. STATEMENT ON USAGE FOR HIGH RISK GROUPS DRUG INTERACTION: Haemic 500mg Capsules: The concentrations in the blood, when 250mg and 500mg of Pregnancy Category B. There are no adequate Drug with actions on haemostasis should be given with caution Each capsule contains: Pregnancy: Tranexamic Acid were administered orally to healthy adults, and well controlled studies in pregnant women. However, to patients on antifibrinolytic therapy. The potential for Tranexamic Acid BP ...... 500mg reached peak values 3.9 ug/ml (250mg administration) and 6.0 tranexamic acid crosses the placenta and appears in cord thrombus formation may be increased by oestrogens, for Haemic 500mg/5ml Injection ug/ml (500mg administration) 2,3 hours after administration. blood. Use in pregnancy only if clearly needed. example or the action of the antifibrinolytic antagonised by Each 5ml contains: The biological half-lives were 3.1 hours and 3.3 hours, compounds such as thrombolytics. Tranexamic Acid BP ...... 500mg respectively. Lactation: Tranexamic acid is present in breast milk at 1% of the corresponding serum levels. Exercise caution when OVERDOSE: INDICATIONS: Excretion: Urinary excretion is the main route of elimination administering to breastfeeding women. There is no known case of overdosage of Tranexamic Acid. Hemorrhagic tendency considered to involve systemically via glomerular filtration. Over all renal clearance is equal to Symptoms of overdosage may be nausea, vomiting, orthostatic exacerbated fibrinolysis (leukemia, hypoplastic anemia, overall plasma clearance (110 to 116 mL/min) and more than Tranexamic acid has had limited use in children, symptoms and/or hypotension. purpura or abnormal hemorrhages during or after operation). Children: 95% of the dose is excreted in the urine as unchanged drug. principally in tooth extraction. Limited data suggest that dosing Abnormal bleeding considered to involve locally exacerbated Excretion of tranexamic acid is about 90% at 24 hours after instructions for adults can be used for children needing fibrinolysis (Pulmonary, nasal, genital, or renal hemorrhages or CONTRAINDICATIONS: intravenous administration of 10 mg per kg body weight. tranexamic acid therapy. Tranexamic Acid is contraindicated: In patients with acquired abnormal hemorrhages during or after prostate surgery). 1- When 500mg of Tranexamic Acid was administered orally to defective color vision, since this prohibits measuring one Symptoms such as erythema, swelling or itchiness in the healthy adults the rate of excretion in the urine was about No dosage reduction is necessary unless there is endpoint that should be followed as a measure of toxicity. In following diseases: Eczema or similar diseases, urticarial, drug Elderly: 2- 30-52% by 24 hours after administration. evidence of renal failure. patients with subarachnoid hemorrhage. Anecdotal experience rash or toxic exanthema. indicates that cerebral edema and cerebral infarction may be Symptoms such as pharyngodynia, redness, hyperemia or Side effects: Hypotension has been observed when caused by Tranexamic Acid in such patients. In patients with swelling in the following diseases: Tonsillitis, pharyngolaryngitis. WARNINGS AND PRECAUTIONS 3- intravenous injection is too rapid. To avoid this response, the For patients on prolonged treatment with tranexamic acid, active intravascular clotting. Pain in the oral cavity or mucosal aphtha in cases of stomatitis. solution should not be injected more rapidly than 1 mL per perform an ophthalmological examination (including visual minute. acuity, color vision, eyeground, and visual fields) before and at STORAGE: PHARMACOLOGY: Gastrointestinal symptoms (nausea, vomiting, and diarrhea) regular intervals during treatment. Store below 30°c. Protect from heat, light & moisture. Antiplasmin action: Tranexamic Acid binds strongly with the occur but disappear when the dose is reduced. Reduce dose in patients with renal insufficiency because of the lysine binding site (LBS), the site of fibrin affinity of plasmin and Isolated cases of dizziness or reduced blood pressure have risk of drug accumulation. plasminogen, and inhibits the binding of plasmin and plasmino- PRESENTATION: been reported. Allergic skin reactions have been reported less Treatment with tranexamic acid is not indicated in hematuria Haemic 250mg Capsules are available in Alu/PVC blister pack of gen to fibrin. Therefore, the degradation of fibrin by plasmin is commonly. caused by diseases of the renal parenchyma. Intravascular 10x10’s. strongly inhibited. In the presence of antiplasmins, such as α precipitation of fibrin frequently occurs and may aggravate the Haemic 500mg Capsules are available in Alu/PVC blister pack 2-macro globulin, in the plasma, the antifibrinolytic action of DOSAGE AND ADMINISTRATION: disease. Furthermore, antifibrinolytic treatment carries the risk of 2x10’s. Tranexamic Acid even further strengthened. Usual dose for adults is 2.5ml - 5ml divided in 1-2 times a day of clot retention in the renal pelvis in cases of massive renal Haemic 500mg/5ml Injection is available in ampoules pack of intravenously or intramuscularly. During or after operation, if hemorrhage of any cause. 2x5’s. Hemostatic action: Abnormally exacerabated plasmin causes necessary, 5-10ml at a time is given intravenously or 5-25ml at Patients with a high risk for thrombosis (a previous thromboem- inhibition of platelet aggregation, decomposition of coagulation For detailed information a time in given by intravenous drip infusion. bolic event and a family history of thromboembolic disease) please contact: factors, etc, but even mild exacerbation causes characteristic Dosage should be individualized in accordance with the should use tranexamic acid only if there is a strong medical fibrin degeneration to occur first. Therefore, in cases of patient’s age and clinical condition. indication and under strict medical supervision. ordinary hemorrhages. Tranexamic Acid appears to cause Note: For patients with moderate to severe impaired renal There are reports of venous and arterial thrombosis or GENIX PHARMA PRIVATE LIMITED hemostasis by suppressing this fibrin degradation. 44,45-B, Korangi Creek Road, Karachi-75190, Pakistan. function, the following dosages are recommended: thromboembolism in patients given tranexamic acid. Also, UAN: +92-21-111-10-10-11, Fax: +92-21-111-10-10-22 E-mail: [email protected] Web.: www.genixpharma.com 157-618-01