Dosing and uses of Cyklokapron (tranexamic acid injection)
Adult dosage forms and strengths
injectable solution
- 100mg/mL
Dental Extraction in Patients with Hemophilia
Indicated in patients with hemophilia for short-term use (ie, 2-8 days) to reduce/prevent hemorrhage and reduce the need for replacement therapy during and following tooth extraction
10 mg/kg IV immediately before surgery OR 10 mg/kg IV q6-8hr 1 day before surgery
25 mg/kg PO q6-8hr 1 day presurgery AND 2-8 days postsurgery
CABG (Off-label)
10-15 mg/kg IV over 20 minutes, THEN 1 mg/kg/hr continuous infusion for 6-10 hours
Hereditary Angioedema (Off-label)
Long-term prophylaxis: 1000-1500 mg PO q8-12hr; reduce dose to 500 mg/dose PO qDay or q12hr when frequency of attacks reduces
Short term prophylaxis: 75 mg/kg/day PO divided q8-12hr for 5 days before and after the event
Treatment of acute HAE attack: 25 mg/kg/dose PO/IV; not to exceed 1000 mg/dose q3-4hr; not to exceed 75 mg/kg/day or 1000 mg PO q6hr for 48 hr
Total Knee Replacement Surgery, Blood Loss Reduction (Off-label)
10 mg/kg IV over 30 min before inflation of tourniquet and 3 hr after first dose
Hyphema (Off-label)
25 mg/kg PO q8hr for 5-7 days
Renal Impairment
Dental Extraction
- SCr 1.36-2.83 mg/dL (120-250 micromoles/L): 10 mg/kg IV q12hr OR 15 mg/kg PO q12hr
- SCr 2.83-5.66 mg/dL (250-500 micromoles/L): 10 mg/kg IV qDay OR 15 mg/kg PO qDay
- SCr >5.66 mg/dL (>500 micromoles/L): 10 mg/kg IV q48hr OR 15 mg/kg PO q48hr; alternatively, 5 mg/kg IV qDay OR 7.5 mg/kg PO qDay
Pediatric dosage forms and strengths
injectable solution
- 100mg/mL
Dental Extraction in Patients with Hemophilia
10 mg/kg IV immediately before surgery OR 10 mg/kg IV q6-8hr 1 day before surgery
25 mg/kg PO q6-8hr 1 day presurgery AND 2-8 days postsurgery
Hyphema (Off-label)
25 mg/kg PO q8hr for 5-7 days
Hereditary Angioedema (Off-label)
Long term prophylaxis: 20-40 mg/kg/day PO divided q8-12hr; reduce dosing frequency to every other day or twice weekly when frequency of attacks reduces
Short term prophylaxis: 20-40 mg/kg/day PO divided q8-12hr; initiate 2-5 days before and continue for 2 days after the procedure
Cyklokapron (tranexamic acid injection) adverse (side) effects
Frequency not defined
Visual abnormalities
Hypotension (with rapid injection)
Nausea
Vomiting
Diarrhea
Warnings
Contraindications
Hypersensitivity
Acquired defective color vision
Subarachnoid hemorrhage
Active intravascular clotting
Cautions
Use caution in renal impairment, subarachnoid hemorrhage, vascular disease
DIC
Visual defects (color vision change or visual loss) reported
Thrombembolic history
Ureteral obstruction resulting from clot formation reported; use caution in patients with upper urinary tract bleeding
Thromboembolism or venous and arterial thrombosis reported
Ligneous conjunctivitis has been reported
Concurrent use with anti-inhibitor coagulant complex/factor IX complex concentrates
Concurrent use with tretinoin may exacerbate procoagulant effects
Pregnancy and lactation
Pregnancy category: B
Lactation: Excreted in breast milk, not recommended
Pregnancy categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA: Information not available.
Pharmacology of Cyklokapron (tranexamic acid injection)
Mechanism of action
Inhibits fibrinolysis by displacing plasminogen from fibrin
Reduces plasmin activity, which in turn reduces activation of complement and consumption of C1 esterase inhibitor (C1-NH) and subsequently decreases inflammation associated with hereditary angioedema
Pharmacokinetics
Half-Life: 2-11 hr
Duration: 3 hr (after 1 dose)
Peak Plasma time: 3 hr
Plasma concentration: 15 mg/L
Protein Bound: 3%
Vd: 9-27 L
Clearance: 110-116 mL/min
Excretion: Urine (95%)
Administration
IV Incompatibilities
Additive: blood, penicillin
IV Compatibilities
Solution: compatible with most common solutions for infusion
Additive: heparin
IV Preparation
Prepare solution same day it will be used
Dilute a single dose w/t 50 mL compatible fluid (eg, NS, Ringers, dextrose/water)
IV Administration
100 mg or fraction thereof over at least 1 min, usu 5 min
Avoid rapid infusion
Storage
Store at 25°C (77°F)
