The dose of CYKLOKAPRON Injection should be reduced in patients with renal insufficiency because of the risk
of accumulation (see DOSAGE AND ADMINISTRATION).
Ureteral obstruction due to clot formation in patients with upper urinary tract bleeding has been reported in
patients treated with CYKLOKAPRON.
Venous and arterial thrombosis or thromboembolism has been reported in patients treated with CYKLOKAPRON.
In addition, cases of central retinal artery and central retinal vein obstruction have been reported.
Patients with a previous history of thromboembolic disease may be at increased risk for venous or arterial
CYKLOKAPRON should not be administered concomitantly with Factor IX Complex concentrates or Anti-inhibitor
Coagulant concentrates, as the risk of thrombosis may be increased.
Patients with disseminated intravascular coagulation (DIC), who require treatment with CYKLOKAPRON, must
be under strict supervision of a physician experienced in treating this disorder.
Tranexamic acid may cause dizziness and therefore may influence the ability to drive or use machines.
Carcinogenesis, Mutagenesis, Impairment Of Fertility
An increased incidence of leukemia in male mice receiving tranexamic acid in food at a concentration of 4.8%
(equivalent to doses as high as 5 g/kg/day) may have been related to treatment. Female mice were not
included in this experiment.
Hyperplasia of the biliary tract and cholangioma and adenocarcinoma of the intrahepatic biliary system have
been reported in one strain of rats after dietary administration of doses exceeding the maximum tolerated dose
for 22 months. Hyperplastic, but not neoplastic, lesions were reported at lower doses. Subsequent long-term
dietary administration studies in a different strain of rat, each with an exposure level equal to the maximum
level employed in the earlier experiment, have failed to show such hyperplastic / neoplastic changes in the
liver. No mutagenic activity has been demonstrated in several in vitro and in vivo test systems.
There are no clinical data to assess the effects of tranexamic acid on fertility.
Reproduction studies performed in mice, rats, and rabbits have not revealed any evidence of impaired fertility
or adverse effects on the fetus due to tranexamic acid.
There are no adequate and well-controlled studies in pregnant women. However, tranexamic acid is known to
pass the placenta and appears in cord blood at concentrations approximately equal to maternal concentration.
Because animal reproduction studies are not always predictive of human response, this drug should be used
during pregnancy only if clearly needed.
Labor And Delivery
See above under Pregnancy.
Tranexamic acid is present in the mother's milk at a concentration of about a hundredth of the corresponding
serum levels. Caution should be exercised when CYKLOKAPRON is administered to a nursing woman.
The drug has had limited use in pediatric patients, principally in connection with tooth extraction. The limited
data suggest that dosing instructions for adults can be used for pediatric patients needing CYKLOKAPRON
Clinical studies of CYKLOKAPRON did not include sufficient numbers of subjects aged 65 and over to determine
whether they respond differently from younger subjects. Other reported clinical experience has not identified
differences in responses between the elderly and younger patients. In general, dose selection for an elderly
patient should be cautious, usually starting at the low end of the dosing range, reflecting the greater frequency
of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy.
This drug is known to be substantially excreted by the kidney, and the risk of toxic reactions to this drug may
be greater in patients with impaired renal function. Because elderly patients are more likely to have decreased
renal function, care should be taken in dose selection, and it may be useful to monitor renal function (see
CLINICAL PHARMACOLOGY and DOSAGE AND ADMINISTRATION).