HEMOCOT Injection

                                                            HEMOCOT INJECTION

Tranexamic Acid Injection BP 500 mg/5ml (For IV injection use only)

COMPOSITION

Each 5 ml contains:
Tranexamic Acid                                  BP        500 mg
Water for Injections                               BP        q. s.

DESCRIPTION
A clear, colorless to almost colorless solution.

PHARMACODYNAMIC
Pharmacotherapeutic group: Antihemorrhagics, Antifibrinolytics, Amino acids.
ATC code: B02AA02

Tranexamic Acid exerts an anti-hemorrhagic activity by inhibiting the fibrinolytic properties of plasmin. A complex involving tranexamic acid being linked to plasminogen when transformed into plasmin.

PHARMACOKINETICS

Absorption
Peak plasma concentration of tranexamic acid is obtained rapidly after a short intravenous infusion after which plasma concentrations decline in a multiple exponential manner.

Distribution
The plasma protein binding of tranexamic acid is about 3% at therapeutic plasma levels and seems to be fully accounted for by its binding to plasminogen. Tranexamic acid does not bind to serum albumin. The initial volume of distribution is about 9 to 12 litres.

Tranexamic acid passes through the placenta. Following administration of an intravenous injection of 10 mg/kg to 12 pregnant women, the concentration of tranexamic acid in serum ranged 10-53 μ g/mL while that in cord blood ranged 4-31 μ g/mL. Tranexamic acid diffuses rapidly into joint fluid and the synovial membrane. Following administration of an intravenous injection of 10 mg/kg to 17 patients undergoing knee surgery, concentrations in the joint fluids were similar to those seen in corresponding serum samples. The concentration of tranexamic acid in a number of other tissues is a fraction of that observed in the blood (breast milk, one hundredth; cerebrospinal fluid, one tenth; aqueous humor, one tenth). Tranexamic acid has been detected in semen where it inhibits fibrinolytic activity but does not influence sperm migration.

Excretion
It is excreted mainly in the urine as unchanged drug. Urinary excretion via glomerular filtration is the main route of elimination. Renal clearance is equal to plasma clearance (110 to 116 ml/min). Excretion of tranexamic acid is about 90% within the first 24 hours after intravenous administration of 10mg/kg body weight. Half-life of tranexamic acid is approximately 3 hours.

THERAPEUTIC INDICATION

• Prevention and treatment of hemorrhages due to general or local fibrinolysis in adults and children from one year.
• Ear Nose Throat surgery (adenoidectomy, tonsillectomy, dental extraction).
• Gynecological surgery or disorder of obstetric origin.
• Thoracic and abdominal surgery.
• Management of hemorrhage due to administration of a fibrinolytic agent.

DOSAGE AND ADMINISTRATION

• 5 gm to 1 gm of tranexamic acid by slow intravenous injection two or three times a day in the treatment of local fibrinolysis.
• 1 gm of tranexamic acid by intravenous injection every 6 to 8 hours, equivalent to 15 mg/kg BW in the treatment of general fibrinolysis.
• Patient with mild to moderate renal impairment, the dosage of tranexamic acid should be adjusted according to the serum creatinine level.

• No dose adjustment is required in patient with hepatic impairment.

 Method of administration: The administration is strictly limited to slow intravenous injection.

OVERDOSE
No cases of overdose have been reported.

Symptoms
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
Management of overdose should be supportive.

 CONTRAINDICATION

• Hypersensitivity to the active substance or to any of the 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 oedema and convulsions).

WARNING AND PRECAUTIONS

• Tranexamic acid should not be administered by the intramuscular route.
• Convulsion have been reported with tranexamic acid treatment. In coronary artery bypass graft (CABG) surgery, most of these cases were reported following I.V. injection of tranexamic acid in high doses.
• Attention should be paid to possible visual disturbances including visual impairment, vision blurred, impaired colour vision and if necessary, the treatment should be discontinued.
• With long term use of tranexamic acid regular ophthalmologic examinations (eye examinations including visual acuity, colour vision, fundus, visual field etc.) are indicated.
• In case of haematuria from the upper urinary tract, there is a risk for urethral obstruction.
• Tranexamic acid should be administered with care in patients receiving oral contraceptives because of the increased risk of thrombosis.

PREGNANCY, LACTATION AND ABILITY TO DRIVE

Pregnancy
Tranexamic acid is not recommended during the first trimester of pregnancy.

Breast-feeding
Tranexamic acid is excreted in human milk. Therefore, breastfeeding is not recommended.

Effect on ability to drive and use machines
No studies have been performed on the ability to drive and use machines.

DRUG INTERACTION

• Simulated treatment with anticoagulants must take place under the strict supervision of a physician.
• Medical products that act on haemostasis should be given with caution to patients treated with tranexamic acid.
• There is a theoretical risk of increased thrombus formation potential, such as with oestrogens. Alternatively, the antifibrinolytic action of the drug may be antagonized with thrombolytic drugs.

 ADVERSE EFFECTS

• Hypersensitivity reaction including anaphylaxis.
• Dizziness, convulsions particularly in case of misuse and visual disturbances including impaired colour vision.
• Malaise with hypotension with or without loss of consciousness.
• Arterial or venous thrombosis at any sites.
• Diarrhoea, vomiting and nausea.
• Dermatitis allergic.

PRESENTATION
HEMOCOT Injections are supplied in 5 ml flint, Type-I USP Ampoule.

STORAGE AND OTHER INFORMATION
Store in a cool and dry place. Protect from light.
Store at below 30°C temperature.
Caution: Not to be used if container is found leaking or solution is hazy or contain any visible solid particles. Keep this medicine out of the sight and reach of children.