Cyklokapron Injection

Active ingredient: Tranexamic Acid Ph.Eur 500 mg

Ampoules containing 5ml colourless solution

Local fibrinolysis

For short term use in prophylaxis and treatment in patients at high risk of per - and post-operative haemorrhage following:

a) prostatectomy

b) conisation of the cervix

c) surgical procedures and dental extractions in haemophiliacs

General fibrinolysis

a) haemorrhagic complications in association with thrombolytic therapy.

b) Haemorrhage associated with disseminated intravascular coagulation with predominant activation of the fibrinolytic system.

Route of administration: by slow intravenous injection.

Local fibrinolysis: the recommended standard dose is 5-10ml (500-1000mg) by slow intravenous injection (1 ml/min), three times daily. If treatment continues for more than three days, consideration should be given to the use of Cyklokapron tablets or syrup. Alternatively, following an initial intravenous injection, subsequent treatment may proceed by intravenous infusion. Following addition to a suitable diluent (see Section 4.5), Cyklokapron may be administered at a rate of 25-50 mg/kg body wt/day.

Children: According to body weight (10mg/kg body wt/ 2-3 times daily)

Elderly patients: No reduction in dosage is necessary unless there is evidence of renal failure.

General fibrinolysis

1 In disseminated intravascular coagulation with predominant activation of the fibrinolytic system, usually a single dose of 10ml (1g) is sufficient to control bleeding.

2 Neutralisation of thrombolytic therapy; 10mg/kg body wt by slow intravenous injection.

Cyklokapron is contra-indicated in patients with a history of thromboembolic disease.

In patients with renal insufficiency, because of the risk of accumulation. The dose should be reduced according to the following table:

In massive haematuria from the upper urinary tract (especially in haemophilia) since, in a few cases, ureteric obstruction has been reported.

In patients with disseminated intravascular coagulation (DIC) treatment must be restricted to those in whom there is predominant activation of the fibrinolytic system with acute severe bleeding. Characteristically, the haematological profile approximates to the following: reduced euglobulin clot lysis time; prolonged prothrombin time; reduced plasma levels of fibrinogen, factors V and VIII, plasminogen 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 in this profile. In such acute cases a single dose of 1g tranexamic acid is frequently sufficient to control bleeding. The fibrinolytic activity in the blood will be reduced for about 4 hours if renal function is normal. Anticoagulation with heparin should be instigated in order to prevent further fibrin deposition. Administration of Cyklokapron in DIC should be considered only when appropriate haematological laboratory facilities and expertise are available. Cyklokapron must not be administered in DIC with predominant activation of the coagulation system.

The solution for injection may be mixed with the following solutions: isotonic sodium chloride; isotonic glucose; 20% fructose; 10% invertose; dextran 40; dextran 70; ringer's solution.

Cyklokapron solution for injection may be mixed with Heparin.

Although there is no evidence from animal studies of a teratogenic effect, the usual caution with the use of drugs in pregnancy should be observed.

Tranexamic acid passes into breast milk to a concentration of approximately one hundredth of the concentration in the maternal blood. An antifibrinolytic effect in the infant is unlikely.

None known.

Gastro-intestinal disorders (nausea, vomiting, diarrhoea) may occur but disappear when the dosage is reduced. Rapid intravenous injection may cause dizziness and/or hypotension. Rare cases of thromboembolic events have been reported.

Nervous System Disorders: dizziness, convulsions

No cases of overdosage have been reported. Symptoms may be nausea, vomiting, orthostatic symptoms and/or hypotension. Maintain a high fluid intake to promote renal excretion.

Tranexamic acid is an antifibrinolytic agent, which competitively inhibits the activation of plasminogen to plasmin.

Approximately 90% of an intravenously administered tranexamic acid dose is excreted, largely unchanged, in the urine within 24 hours. The plasma half-life is approximately 2 hours.

There are no preclinical data of relevance to the prescriber which are additional to that already included in other sections of the Summary of Product Characteristics.

Cyklokapron solution for injection should not be added to blood for transfusion, or to injections containing penicillin.

3 years.

None

Type I glass 5ml ampoules packed in outer cardboard carton.

See Section 4.2

Pharmacia Limited

Ramsgate Road

Sandwich

CT13 9NJ

UK

PL 00032/0314

9^th February 1987

July 2009

Company Ref: CK2_0