Tranexamic Acid

Tranexamic acid is an antifibrinolytic agent which competitively inhibits the activation of plasminogen to plasmin. The drug has affinity for the five lysine-binding sites of plasminogen. It thus promotes clot stability, and is useful as adjunctive therapy in haemophilia and some other bleeding disorders.

Dose:

3 - 4 GMS IN DEVIDED DOSES PER DAY ORALLY. CHILDREN : 25 MG / KG TDS I.V. DOSE : ADULT - 4 -5 GM I.V. OVER A PERIOD OF ONE HR., THEN THE DOSE IS 1 GM EVERY HRLY IN VEIN UPTO 8 HRS. CHILDREN - 100 MG / KG, THEN 33.3 MG / KG EVERY HRLY.

Monography

Tranexamic acid Tranexamic acid (marketed in the UK under the trade name of "Cyclokapron") is an antifibrinolytic agent which competitively inhibits the activation of plasminogen to plasmin. The drug has affinity for the five lysine-binding sites of plasminogen. It thus promotes clot stability, and is useful as adjunctive therapy in haemophilia and some other bleeding disorders. The use of tranexamic acid has superseded the use of amino caproic acid, which not only has a shorter plasma half-life but is less potent and more toxic. Trials several decades ago established that regular treatment with tranexamic acid alone is of no value in prevention of haemarthroses in haemophilia. It is particularly valuable in controlling bleeding in the mouth in haemophilia and von Willebrand's disease, such as in association with dental surgery. It may also be used to control menorrhagia and epistaxis in von Willebrand's disease. Tranexamic acid is also of use in factor XI deficiency, and its use to cover dental, gynaecological or urological surgery in factor XI-deficient patients may obviate the need for replacement therapy with concentrate or plasma.It should not be used to control haematuria in severe haemophilia, as treatment may precipitate clot colic and even obstruction of the outflow from the urinary pelvis. Similarly, we do not use the drug in the setting of thoracic or abdominal surgery, as this may result in the development of insoluble haematomas. Tranexamic acid may be given alone or together with standard doses of coagulation factor concentrate. However, it should not be given to patients with inhibitory antibodies receiving activated prothrombin factor concentrates (such as FEIBA or Autoplex) as this may provoke thromboembolism. If treatment with both agents is deemed to be necessary, it is recommended that at least six hours should elapse between the last dose of APCC and the administration of tranexamic acid. By contrast, tranexamic acid may be usefully used in combination with recombinant factor VIIa to enhance haemostasis. Tranexamic acid is usually given in tablet form at a typical dose of 3 or 4 grams (in divided doses) daily for an adult. Gastrointestinal upset (nausea, vomiting and diarrhoea) may rarely occur as a side-effect, but these symptoms usually resolve if the dosage is reduced. It may also be given by intravenous injection, but it must be infused slowly as rapid injection may result in dizziness and hypotension. A syrup formulation is also available for paediatric use: the syrup contains 500mg tranexamic acid in each 5ml, and the usual dose for children is 25 mg/kg up to three times daily. The drug may be of particular use in controlling oral bleeding associated with eruption of teeth.The drug is excreted by the kidneys, and the dose must be reduced if there is renal impairment in order to avoid toxic accumulation. Antifibrinolytic (an-tee-fye-bri-noh-LIT-ik) agents are used to treat serious bleeding, especially when the bleeding occurs after dental surgery (particularly in patients with hemophilia) or certain other kinds of surgery. These medicines are also sometimes given before an operation to prevent serious bleeding in patients with medical problems that increase the chance of serious bleeding. Antifibrinolytic agents may also be used for other conditions as determined by your doctor. Antifibrinolytic agents are available only with your doctor's prescription, in the following dosage forms: Oral * Aminocaproic acid o Syrup (U.S. and Canada) o Tablets (U.S. and Canada) * Tranexamic acid o Tablets (U.S. and Canada) Parenteral * Aminocaproic acid o Injection (U.S. and Canada) * Tranexamic acid o Injection (U.S. and Canada) Before Using This Medicine In deciding to use a medicine, the risks of taking the medicine must be weighed against the good it will do. This is a decision you and your doctor will make. For antifibrinolytic agents, the following should be considered: Allergies-Tell your doctor if you have ever had any unusual or allergic reaction to aminocaproic acid or tranexamic acid. Also tell your health care professional if you are allergic to any other substances, such as foods, preservatives, or dyes. Pregnancy-Studies on birth defects have not been done in humans. However, these medicines have been given to pregnant women without causing birth defects or other problems. Studies on effects of aminocaproic acid in pregnancy have not been done in animals. Tranexamic acid has not been shown to cause birth defects or other problems in animal studies. Breast-feeding-These medicines have not been reported to cause problems in nursing babies. However, small amounts of tranexamic acid pass into the breast milk. Children-Although there is no specific information comparing use of aminocaproic acid or tranexamic acid in children with use in other age groups, these medicines are not expected to cause different side effects or problems in children than they do in adults. Older adults- * For aminocaproic acid : Although there is no specific information comparing use of aminocaproic acid in the elderly with use in other age groups, this medicine is not expected to cause different side effects or problems in older people than it does in younger adults. * For tranexamic acid : Tranexamic acid has been tested and has not been shown to cause different side effects or problems in older people than it does in younger adults. Other medicines-Although certain medicines should not be used together at all, in other cases two different medicines may be used together even if an interaction might occur. In these cases, your doctor may want to change the dose, or other precautions may be necessary. Tell your health care professional if you are taking any other prescription or nonprescription (over-the-counter [OTC]) medicine. Other medical problems-The presence of other medical problems may affect the use of antifibrinolytic agents. Make sure you tell your doctor if you have any other medical problems, especially: * Blood clots or a history of medical problems caused by blood clots or * Blood in the urine or * Color vision problems or * Heart disease or * Kidney disease or * Liver disease-The chance of side effects may be increased Proper Use of This Medicine Take this medicine only as directed by your doctor . Do not take more or less of it, do not take it more often, and do not take it for a longer time than your doctor ordered. To do so may increase the chance of unwanted effects. Dosing-The dose of these medicines will be different for different patients. Follow your doctor's orders or the directions on the label . The following information includes only the average doses of these medicines. If your dose is different, do not change it unless your doctor tells you to do so. For aminocaproic acid * To prevent or treat serious bleeding: o For oral dosage forms (syrup or tablets): * Adults-For the first hour, the dose is 5 grams. Then the dose is 1 or 1.25 grams per hour for eight hours. * Children-Dose is based on body weight or size and must be determined by your doctor. For the first hour, the dose is usually 100 milligrams (mg) per kilogram (kg) (45.4 mg per pound) of body weight. Then the dose is 33.3 mg per kg (15.1 mg per pound) of body weight per hour. o For injection dosage form: * Adults-At first, the dose is 4 to 5 grams injected into a vein, over a period of one hour. Then the dose is 1 gram per hour, injected into a vein over a period of eight hours. * Children-Dose is based on body weight or size and must be determined by your doctor. At first, the dose is usually 100 mg per kg (45.4 mg per pound) of body weight, injected into a vein over a period of one hour. Then the dose is 33.3 mg per kg (15.1 mg per pound) of body weight per hour, injected into a vein. For tranexamic acid * To prevent or treat serious bleeding after dental surgery: o For oral dosage form (tablets): * Adults and children-Dose is based on body weight and must be determined by your doctor. The dose is usually 25 milligrams (mg) per kilogram (kg) (11.4 mg per pound) of body weight every six to eight hours, beginning one day before surgery. After surgery, the dose is usually 25 mg per kg (11.4 mg per pound) of body weight every six to eight hours for seven to ten days. o For injection dosage form: * Adults and children-Dose is based on body weight and must be determined by your doctor. The dose is usually 10 mg per kg (4.5 mg per pound) of body weight, injected into a vein just before surgery. After surgery, the dose is usually 10 mg per kg (4.5 mg per pound) of body weight, injected into a vein every six to eight hours for seven to ten days. Missed dose- * For aminocaproic acid (e.g., Amicar): If you miss a dose, take it as soon as possible. However, if you do not remember until it is almost time for your next dose, double the next dose. Then go back to your regular dosing schedule. * For tranexamic acid (e.g., Cyklokapron): If you miss a dose, take it as soon as possible. Then take any remaining doses for the day at regularly spaced times. Do not double doses. If you have any questions about this, check with your doctor. Storage-To store this medicine: * Keep out of the reach of children. * Store away from heat and direct light. * Do not store the tablet form of this medicine in the bathroom, near the kitchen sink, or in other damp places. Heat or moisture may cause the medicine to break down. * Do not keep outdated medicine or medicine no longer needed. Be sure that any discarded medicine is out of the reach of children. Precautions While Using This Medicine If you will be taking tranexamic acid for longer than several days, your doctor may want you to have your eyes checked regularly by an ophthalmologist (eye doctor). This will allow your doctor to check for unwanted effects that may be caused by this medicine. If you are using aminocaproic acid syrup as a mouth rinse to control oral bleeding, and you are in the first or second trimester of pregnancy, you should spit out the syrup after rinsing without swallowing it. Side Effects of This Medicine Along with its needed effects, a medicine may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention. The same effect that makes aminocaproic acid or tranexamic acid help prevent or stop bleeding also may cause blood clots that could be dangerous. Check with your doctor immediately if any of the following possible signs and symptoms of blood clots occur: Less common or rare Headache (severe and sudden); loss of coordination (sudden); pains in chest, groin, or legs, especially the calves; shortness of breath (sudden); slurred speech (sudden); vision changes (sudden); weakness or numbness in arm or leg Also, check with your doctor as soon as possible if any of the following side effects occur: Less common or rare For aminocaproic acid Dizziness; headache; muscle pain or weakness (severe and continuing); ringing or buzzing in ears; skin rash; slow or irregular heartbeat-with the injection only; stomach cramps or pain; stuffy nose; sudden decrease in amount of urine; swelling of face, feet, or lower legs; unusual tiredness or weakness; weight gain (rapid) For tranexamic acid Blurred vision or other changes in vision; dizziness or lightheadedness; unusual tiredness or weakness Other side effects may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. However, check with your doctor if any of the following side effects continue or are bothersome: Diarrhea; dry ejaculation; nausea or vomiting; unusual menstrual discomfort; watery eyes Other side effects not listed above may also occur in some patients. If you notice any other effects, check with your doctor.