CYKLOKAPRON- tranexamic acid injection, solution
Pharmacia and Upjohn Company
Antifibrinolytic agent
DESCRIPTION
Each mL of the sterile solution for intravenous injection contains 100 mg tranexamic acid and Water for Injection to 1 mL.
FORMULATION
Chemical Name: trans-4-(aminomethyl)cyclohexanecarboxylic acid
Tranexamic acid is a white crystalline powder. The aqueous solution for injection has a pH of 6.5 to 8.0.
CLINICAL PHARMACOLOGY
Tranexamic acid is a competitive inhibitor of plasminogen activation, and at much higher concentrations, a noncompetitive inhibitor of plasmin, i.e., actions similar to aminocaproic acid. Tranexamic acid is about 10 times more potent in vitro than aminocaproic acid.
Tranexamic acid binds more strongly than aminocaproic acid to both the strong and weak receptor sites of the plasminogen molecule in a ratio corresponding to the difference in potency between the compounds. Tranexamic acid in a concentration of 1 mg per mL does not aggregate platelets in vitro.
Tranexamic acid, in concentrations as low as 1 mg per mL, can prolong the thrombin time. However, tranexamic acid in concentrations up to 10 mg per mL in blood showed no influence on the platelet count, the coagulation time, or other coagulation factors in whole blood or citrated blood from normal subjects.
Cyklokapron Indications and Usage
CYKLOKAPRON Injection is indicated in patients with hemophilia for short-term use (two to eight days) to reduce or prevent hemorrhage and reduce the need for replacement therapy during and following tooth extraction.
CONTRAINDICATIONS
CYKLOKAPRON Injection is contraindicated:
In patients with acquired defective color vision, since this prohibits measuring one endpoint that should be followed as a measure of toxicity (see WARNINGS).
In patients with subarachnoid hemorrhage. Anecdotal experience indicates that cerebral edema and cerebral infarction may be caused by CYKLOKAPRON in such patients.
In patients with active intravascular clotting.
In patients with hypersensitivity to tranexamic acid or any of the ingredients.
OVERDOSAGE
Cases of overdosage of CYKLOKAPRON have been reported. Based on these reports, symptoms of overdosage may be gastrointestinal, e.g., nausea, vomiting, diarrhea; hypotensive, e.g., orthostatic symptoms; thromboembolic, e.g., arterial, venous, embolic; neurologic, e.g., visual impairment, convulsions, headache, mental status changes; myoclonus; and rash.
DOSAGE AND ADMINISTRATION
Immediately before tooth extraction in patients with hemophilia, administer 10 mg per kg body weight of CYKLOKAPRON intravenously together with replacement therapy (see PRECAUTIONS). Following tooth extraction, intravenous therapy, at a dose of 10 mg per kg body weight three to four times daily, may be used for 2 to 8 days.
Note: For patients with moderate to severe impaired renal function, the following dosages are recommended:
Serum Creatinine (�mol/L) Tranexamic Acid Intravenous Dosage
120 to 250 (1.36 to 2.83 mg/dL) 10 mg/kg twice daily
250 to 500 (2.83 to 5.66 mg/dL) 10 mg/kg daily
>500 (>5.66 mg/dL) 10 mg/kg every 48 hoursor5 mg/kg every 24 hours
For intravenous infusion, CYKLOKAPRON Injection may be mixed with most solutions for infusion such as electrolyte solutions, carbohydrate solutions, amino acid solutions, and Dextran solutions. Heparin may be added to CYKLOKAPRON Injection. CYKLOKAPRON Injection should NOT be mixed with blood. The drug is a synthetic amino acid, and should NOT be mixed with solutions containing penicillin.
Single-dose vials and ampules
Discard CYKLOKAPRON vial or ampule and any remaining portion in the vial/ampule after single use.
The diluted mixture may be stored for up to 4 hours at room temperature prior to patient administration.
HOW SUPPLIED
CYKLOKAPRON Injection 100 mg/mL
NDC 0013-1114-10 10 � 10 mL single-dose ampules
CYKLOKAPRON Injection 100 mg/mL
NDC 0013-1114-21 10 � 10 mL single-dose vials
STORAGE
Store at 25�C (77�F); excursions permitted to 15��30�C (59��86�F) [see USP Controlled Room Temperature].