Cycloxid

Tranexamic acid.

Each mL contains: Tranexamic acid 100 mg.

Pharmacology: Antihemophilic factor: As an inhibitor of plasminogen activation to antifibrin, the potency of this formula is 7 to 8 times superior than the ε-aminocaproic acid in vitro, and 5 to 10 time superior than the ε-aminocaproic acid in vivo, but it contains lesser side effects. The formula not only act to stabilize the fiberization process maintain the blood coagulation function, but can inhibit to sustain blood vessel weakening, platelet mutation or coagulant factor breakdown, to offer blood clotting property against membrane saturation.
Anti-infection & anti-histamine: Bacterial or viral infections or foreign irritants entering the body tend to result in hyperactive blood plasma, which tends to trigger mutative allergic or infectious symptoms as tissue albumins separate from the blood, a phenomenon that can be suppressed by this formula.
Pharmacokinetics: Tranexamic acid is absorbed from the gastrointestinal tract with peak plasma concentrations occurring after about 3 hours. Bioavailability is about 30 to 50%. Tranexamic acid is widely distributed throughout the body and has very low protein binding. It diffuses across the placenta and is distributed into breastmilk. Tranexamic acid has a plasma elimination half-life of about 2 hours. It is excreted in the urine mainly as unchanged drug.

Prevention and treatment of haemorrhage due to general or local fibrinolysis in adults and children from one year.
Specific indications include: Haemorrhage caused by general or local fibrinolysis such as: Menorrhagia and metrorrhagia, Gastrointestinal bleeding, Haemorrhagic urinary disorders, further to prostate surgery or surgical procedures affecting the urinary tract.
Ear, Nose, Throat surgery (adenoidectomy, tonsillectomy, dental extractions).
Gynecological surgery or disorders of obstetric origin.
Thoracic and abdominal surgery and other major surgical intervention such as cardiovascular surgery.
Management of hemorrhage due to the administration of a fibrinolytic agent.

Adults: Unless otherwise prescribed, the following doses are recommended: Standard treatment of local fibrinolysis: 0.5 g (1 ampule of 5 ml) to 1 g (1 ampule of 10 ml or 2 ampules of 5 ml) tranexamic acid by slow intravenous injection (1 mL/minute) two to three daily. Tranexamic acid is given by continuous infusion at a rate of 25 to 50 mg/kg daily.
Standard treatment of general fibrinolysis: 1 g (1 ampule of 10 ml or 2 ampules of 5 ml) tranexamic acid by slow intravenous injection (1 mL/minute) every 6 to 8 hours, equivalent to 15 mg/kg body weight.
Renal impairment: In renal insufficiency leading to a risk of accumulation, the use of tranexamic acid is contraindicated in patient with severe renal impairment. For patient with mild to moderate renal impairment, the dosage of tranexamic acid should be reduced according to the serum creatinine level: See Table 1.

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Hepatic impairment: No dose adjustment is required for patients with hepatic impairment.
Pediatric Population: In children from 1 year, for current approved indications, the dosage is in the region of 20 mg/kg/day. However, data on efficacy, posology and safety for these indications are limited.
The efficacy, posology and safety of tranexamic acid in children undergoing cardiac surgery have not been fully established.
Elderly: No reduction in dosage necessary unless there is evidence of renal failure.
Method of Administration: The administration is strictly limited to slow intravenous injection.

No case of overdose has been reported. Signs and symptoms may include dizziness, headache, hypotension, and convulsions. It has been shown that convulsions tend to occur at higher frequency with increasing dose. Management of overdose should be supportive.

Hypersensitivity to the active substance or to any of its excipients; acute venous or arterial thrombosis; Fibrinolytic conditions following consumption coagulopathy except in those with predominant activation of the fibrinolytic system with acute severe bleeding. Severe renal impairment (risk of accumulation); History of convulsions; Intrathecal and intraventricular injection, intracerebral application (risk of cerebral edema and convulsions).

The indications and method of administration indicated above should be followed strictly: Intravenous injections should be given very slowly.
Tranexamic acid should not be administered by the intramuscular route.
Convulsions: Cases of convulsions have been reported in association with tranexamic acid treatment. In coronary artery bypass graft (CABG) surgery; most of these cases were reported following intravenous (I.V) injection of tranexamic acid in high doses. With the use of recommended lower doses of tranexamic acid, the incidence of post-operative seizures was the same as that in untreated patients.
Visual Disturbances: Attention should be paid to possible visual disturbances including visual impairment, vision blurred, impaired color vision and if necessary the treatment should be discontinued. With continuous long-term use of tranexamic acid solution for injection, regular ophthalmologic examinations (eye examinations including visual acuity, color vision, fundus, and visual filed etc.) are indicated. With pathological ophthalmic changes, particularly with disease of the retina, the physician must decide after consulting a specialist on the necessity for the long-term use of tranexamic acid solution for injection in each individual case.
Haematuria: In case of haematuria from the upper urinary tract, there is a risk for urethral obstruction.
Thromboembolic events: Before use of tranexamic acid, risk factors of thromboembolic disease should be considered. In patients with a history of thromboembolic disease or in those with increased incidence of thromboembolic events in their family history (patients with a high risk of thrombophilia), tranexamic acid solution for injection should only be administered if there is a strong medical indication after consulting a physician experienced in hemostaseology and under strict medical supervision.
Tranexamic acid should be administered with care in patients receiving oral contraceptives because of the increased risk of thrombosis.
Disseminated intravascular coagulation: Patients with disseminated intravascular coagulation (DIC) should in most cases not be treated with tranexamic acid. If tranexamic acid is given it must be restricted to those in whom there is predominant activation of the fibrinolytic system with acute severe bleeding.
Characteristically, the hematological profile approximates to the following: Reduced euglobin clot lysis time; prolonged prothrombin time; reduced plasma levels of fibrinogen, factor V and VIII, plasminogen fibrinolysis and alpha-2 macroglobulin; normal plasma levels of P and P complex; i.e. factors II (prothrombin), VIII and X; increased plasma levels of fibrinogen degradation products; a normal platelet count. The foregoing presumes that the underlying disease state does not of itself modify the various elements of this profile. In such acute cases, a single dose of 1 g tranexamic acid is frequently sufficient to control bleeding. Administration of tranexamic acid in DIC should be considered only when appropriate hematological laboratory facilities and expertise are available.
Interaction with other medical products and other forms of interaction: No interaction studies have been performed. Simultaneous treatment with anticoagulants must take place under the strict supervision of a physician experienced in this field. Medicinal products that act on hemostasis should be given with caution to patients treated with tranexamic acid. There is a theoretical risk of increased thrombus-formation potential, such as with estrogens. Alternatively, the fibrinolytic action of the drug may be antagonized with thrombolytic drugs.
Effects on Ability to Drive and Use Machines: No studies have been performed on the ability to drive and use machines.

Women of childbearing potential have to use effective contraception during treatment.
Pregnancy: There is insufficient clinical data on the use of tranexamic acid in pregnant women. As a result, although studies do not indicate teratogenic effects, as precaution for use, tranexamic acid is not recommended during the first trimester of pregnancy. Limited clinical of the use of tranexamic acid in different clinical hemorrhage settings during the second and third trimesters did not identify deleterious effect for the fetus.
Tranexamic acid should be used throughout pregnancy only if the expected benefit justifies the potential risk.
Breastfeeding: Tranexamic acid is excreted in human milk. Therefore, breastfeeding is not recommended.
Fertility: There are no clinical data on the effects of tranexamic acid on fertility.

Adverse reactions reported are presented in Table 2. Adverse reactions are listed according to MedDRA primary system organ class.
Within each system organ class, adverse reactions are ranked by frequency. Within each frequency grouping, adverse reactions are presented in the order of decreasing seriousness. Frequencies were defined as follows: very common (>1/10): common (>1/100 to <1/10): uncommon (>1/1,000 to <1/100), not know (cannot be estimated from the available data) (see Table 2).

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Tranexamic acid appears to be well tolerated. It can produce dose-related gastrointestinal disturbances. Hypotension has occurred, particularly after rapid intravenous dosage. Thrombotic complications have been reported in patients receiving tranexamic acid, but these are usually a consequence of its inappropriate use. There have been a few instances of transient disturbance of color vision associated with use of tranexamic acid; in such cases, the drug should be stopped. Hypersensitivity skin reactions have also been reported.

Drugs with actions on haemostasis should be given with caution to patients on antifibrinolytic therapy. The potential for thrombus formation may be increased by estrogens, for example, or the action of the antifibrinolytic antagonized by compounds such as thrombolytics.

Store at temperatures not exceeding 30°C.

Haemostatics

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

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