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Tranexamic acid (CYKLOKAPRON®)
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|NS, D5W, others (see below)|
Standard Dilutions [Amount of drug] [Infusion volume] [Infusion rate]
| [Beta] monograph - future revisions possible.
Update: Oct 14,2014.
[Usual dose: 1-2 grams] [ 50 - 250 mL] [ Max 100 mg/min]
[1000 mg] [50-100mL] [10 to 30 minutes or as directed]
[2000 mg] [50-250 mL] [20 minutes or longer]
Note: Repeated doses must be adjusted for renal function.
Protocols also exist for continuous infusions after a loading dose
e.g. 1 to 4.5 mg/kg/hr
Lexi-Comp, Inc. (Lexi-Drugs). Lexi-Comp, Inc.; October 14, 2014.
Note: Many of the Indications listed below are considered 'unlabeled' uses in the U.S.
"For adult cardiac surgery, a loading dose is administered prior to surgery followed by a prolonged infusion during surgery. The recommended rate of prolonged infusion is 4.5 mg/kg patient body weight per hour. For a patient who weighs 100 kg, undiluted Cyklokapron solution for injection (100 mg/mL) may be administered at 4.5 mL/hour. Solutions diluted to 1% tranexamic acid may be administered at 45 mL/hour and solutions diluted to 2% tranexamic acid may be administered at 22.5 mL/hour."2
Stability / Miscellaneous
| Mechanism of Action1
Tranexamic acid is a competitive inhibitor of plasminogen activation and at much higher concentrations a noncompetitive inhibitor of plasmin, thus implying that tranexamic acid interferes with the fibrinolytic process in the same way as aminocaproic acid. Tranexamic acid is about 10 times more potent in vitro than aminocaproic acid.
Tranexamic acid binds considerably more strongly than aminocaproic acid to both the strong and weak 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/mL does not aggregate platelets in vitro. Tranexamic acid in concentrations up to 10 mg/mL blood has no influence on the platelet count, the coagulation time or various coagulation factors in whole blood or citrated blood in normal subjects. On the other hand tranexamic acid in concentrations of 10 mg/mL and 1 mg/mL blood prolongs the thrombin time.
DOSAGE AND ADMINISTRATION2
Dental Surgery in Patients with Coagulopathies
Adult Total Knee Arthroplasty
Adult Total Hip Arthroplasty
Immediately before tooth extraction in patients with hemophilia6, 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:
Use in Special Populations
Use in Renal Impairment2
Compatibilities & Stability:
The required volume of Cyklokapron solution for injection may be added to the chosen infusion solution to achieve final concentrations of 1 or 2 g in 100 mL (10 or 20 mg/mL, 1% or 2%). The mixture should be used immediately after preparation. If storage is necessary, the mixture should be stored at 2 - 8oC for a maximum of 24 hours. Mixture not used within 24 hours of preparation, should be discarded.
2] PRODUCT MONOGRAPH -CYKLOKAPRON® Tranexamic acid. 500 mg tablets, 500 mg/5 mL & 1000 mg/10 mL solution for injection. Pfizer New Zealand Ltd. P O Box 3998. Auckland, New Zealand, 1140. DATE OF PREPARATION: 25 February 2013. Accessed April 2013.
3] Seeber P, Shander A. Basics of Blood Management. 2nd ed. Chichester, UK: Wiley-Blackwell; 2013.
4] Lacy CF, Armstrong LL, Goldman MP, Lance LL, eds. Lexi-Comp Online. 14th ed. Hudson, OH: Lexi-Comp; 2013.
5] ASHP: Current Shortages - Bulletin. Accessed April 2013.
6] PRODUCT MONOGRAPH: CYKLOKAPRON Injection 100 mg/mL. Pfizer Injectables: Distributed by Pharmacia and Upjohn Company - Division of Pfizer Inc. New York, NY 10017. Revised Jan 2011. Accessed April 2013.