Cyklokapron

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  • Generic Name & Formulations
  • Indications
  • Dosage and Administration
  • Contraindications
  • Boxed Warnings
  • Warnings/Precautions
  • Pharmacokinetics
  • Interactions
  • Adverse Reactions
  • Clinical Trials
  • Note
  • Patient Counseling

    • Cyklokapron Generic Name & Formulations

    Legal Class

    Rx

    General Description

    Tranexamic acid 100mg/mL; soln for IV inj.

    Pharmacological Class

    Plasminogen activation inhibitor.

    How Supplied

    Single-dose amps (10mL)—1, 10; single-dose vials (10mL)—10

    Storage

    Store at 20º-25° C (68º-77° F); excursions permitted to 15°-30° C (59°-86° F).

    Manufacturer

    Pfizer Inc.

    Generic Availability

    YES

    Cyklokapron Indications

    Indications

    Short-term use in hemophilia to reduce or prevent hemorrhage, and reduce the need for replacement therapy during and following tooth extraction.

    Cyklokapron Dosage and Administration

    Adults and Children

    Give by IV inj. Max injection rate: 1mL/min. Pre-extraction: 10mg/kg; post-op: 10mg/kg 3–4 times daily for 2–8 days. Renal impairment: serum creatinine 1.36–2.83mg/dL: 10mg/kg twice daily; 2.83–5.66mg/dL: 10mg/kg once daily; >5.66mg/dL: 10mg/kg every 48hrs or 5mg/kg every 24hrs.

    Adults and Children

    The recommended dose of Cyklokapron is:

    • 10 mg/kg actual body weight intravenously administered as a single dose, immediately before tooth extractions. 

    • Infuse no more than 1 mL/minute to avoid hypotension. 

    • Following tooth extraction, Cyklokapron may be administered for 2 to 8 days at a dose of 10 mg/kg actual body weight 3 to 4 times daily, intravenously.

    Renal Impairment

    Reduce the dosage of Cyklokapron in patients with renal impairment, based on the patient’s serum creatinine.

    Other Modifications

    Females and Males of Reproductive Potential 

    Concomitant use of Cyklokapron, which is an antifibrinolytic, with hormonal contraceptives may increase the risk for thromboembolic adverse reactions. 

    Advise patients to use an effective alternative (nonhormonal) contraceptive method.

    Cyklokapron Contraindications

    Contraindications

    Subarachnoid hemorrhage. Active intravascular clotting.

    Cyklokapron Boxed Warnings

    Not Applicable

    Cyklokapron Warnings/Precautions

    Warnings/Precautions

    For IV use only. Confirm the correct route of administration. Therapy longer than 3 months: do ophthalmologic exam at regular intervals; discontinue if visual changes occur. Risk of seizures esp. during cardiovascular surgery or inadvertent neuraxial administration. Renal impairment: reduce dose. History of thromboembolic disease. Pregnancy. Nursing mothers.

    Warnings/Precautions

    Thromboembolic Risk 

    Tranexamic acid is an antifibrinolytic and may increase the risk of thromboembolic events. Venous and arterial thrombosis or thromboembolism has been reported in patients treated with Cyklokapron. 

    Risk of Medication Errors Due to Incorrect Route of Administration 

    Cyklokapron is for intravenous use only. Serious adverse reactions including seizures and cardiac arrythmias have occurred when Cyklokapron was inadvertently administered intrathecally instead of intravenously. 

    Confirm the correct route of administration for Cyklokapron and avoid confusion with other injectable solutions that might be administered at the same time as Cyklokapron. Syringes containing Cyklokapron should be clearly labeled with the intravenous route of administration.

    Seizures 

    Cyklokapron may cause seizures, including focal and generalized seizures. The most common setting for tranexamic acid-induced seizures has been during cardiovascular surgery (a setting in which Cyklokapron is not FDA-approved and which uses doses of up to 10-fold higher than the recommended human dose and in patients inadvertently given tranexamic acid into the neuraxial system). Cyklokapron is not approved and not recommended for neuraxial administration. Consider dose reduction during surgery and dose adjustments for patients with clinical conditions such as renal dysfunction. Closely monitor the patient during surgery. Consider electroencephalogram (EEG) monitoring for patients with a history of seizures or who experience myoclonic movements, twitching, or show evidence of focal seizures. Discontinue Cyklokapron if seizures occur.

    Hypersensitivity Reactions 

    Cases of hypersensitivity reactions, including anaphylactic reactions, have occurred with use of intravenous tranexamic acid. Discontinue treatment with Cyklokapron if a serious reaction occurs, provide appropriate medical management, and do not restart treatment. Cyklokapron is contraindicated in patients with a history of hypersensitivity to tranexamic acid.

    Visual Disturbances 

    Although not seen in humans, focal areas of retinal degeneration have been observed in cats and dogs following oral or intravenous tranexamic acid at doses between 250-1600 mg/kg/day (1.6-22 times the recommended usual human dose based on body surface area) from 6 days to 1 year. No retinal changes have been observed in eye examinations of patients treated with tranexamic acid for up to 8 years. Patients expected to be treated for greater than 3 months may consider ophthalmic monitoring including visual acuity and optical coherence tomography at regular intervals. Discontinue Cyklokapron if changes in ophthalmological examination occur.

    Dizziness 

    Cyklokapron may cause dizziness. Concomitant use of other drugs that may also cause dizziness may worsen this effect. Advise patients to avoid driving or using machines until they know how Cyklokapron affects them.

    Pregnancy Considerations

    Available data from published studies, case series and case reports with tranexamic acid use in pregnant women in the 2nd and 3rd trimester and at the time of delivery have not clarified whether there is a drug-associated risk of miscarriage or adverse maternal or fetal outcomes.

    It is not known whether tranexamic acid use in pregnant women may cause a drug-associated risk of miscarriage or adverse maternal or fetal outcomes. For decisions regarding the use of Cyklokapron during pregnancy, the potential risk of Cyklokapron administration on the fetus should always be considered along with the mother’s clinical need for Cyklokapron; an accurate risk-benefit evaluation should drive the treating physician’s decision.

    Nursing Mother Considerations

    Published literature reports the presence of tranexamic acid in human milk. There are no data on the effects of tranexamic acid on the breastfed child or the effects on milk production. The developmental and health benefits of breastfeeding should be considered along with the mother’s clinical need for Cyklokapron and any potential adverse effects on the breastfed child from Cyklokapron or from the underlying maternal condition.

    Pediatric Considerations

    There are limited data concerning the use of Cyklokapron in pediatric patients with hemophilia who are undergoing tooth extraction. The limited data suggest that there are no significant pharmacokinetic differences between adults and pediatric patients.

    Geriatric Considerations

    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.

    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.

    Renal Impairment Considerations

    Reduce the dosage of Cyklokapron in patients with renal impairment, based on the patient’s serum creatinine.

    Other Considerations for Specific Populations

    Females and Males of Reproductive Potential 

    Concomitant use of Cyklokapron, which is an antifibrinolytic, with hormonal contraceptives may increase the risk for thromboembolic adverse reactions. 

    Advise patients to use an effective alternative (nonhormonal) contraceptive method.

    Cyklokapron Pharmacokinetics

    Distribution

    The plasma protein binding of tranexamic acid is about 3% at therapeutic plasma levels and seems to be fully accounted for by its binding to plasminogen. Tranexamic acid does not bind to serum albumin.

    Elimination

    After an intravenous dose of 1 g, the plasma concentration time curve shows a triexponential decay with a half-life of about 2 hours for the terminal elimination phase. 

    Urinary excretion is the main route of elimination via glomerular filtration. Overall renal clearance is equal to overall plasma clearance (110 to 116 mL/min), and more than 95% of the dose is excreted in the urine as unchanged drug.

    Cyklokapron Interactions

    Interactions

    Avoid concomitant Factor IX complex concentrates, Anti-inhibitor coagulant concentrates, or hormonal contraceptives; increased risk of thrombosis. Do not mix with solutions containing penicillin or with blood products.

    Interactions

    Avoid concomitant use of Cyklokapron with medical products that are prothrombotic because concomitant use can further increase the risk of thromboembolic adverse reactions associated with tranexamic acid. These medications include but are not limited to, Factor IX Complex concentrates, Anti-inhibitor Coagulant concentrates, and hormonal contraceptives.

    Do not mix with solutions containing penicillin or with blood products.

    Cyklokapron Adverse Reactions

    Adverse Reactions

    GI upset, allergic dermatitis, giddiness, hypotension, visual abnormalities; thromboembolic events (rare), dizziness, convulsions, anaphylaxis.

    Cyklokapron Clinical Trials

    See Literature

    Cyklokapron Note

    Not Applicable

    Cyklokapron Patient Counseling

    Patient Counseling

    Thromboembolic Risk 

    Cyklokapron may increase the risk of venous and arterial thrombosis or thromboembolism and patients should contact their healthcare provider for any signs or symptoms suggestive of thromboembolism. Advise patients using hormonal contraception that combined use with Cyklokapron may increase the risk for thromboembolic adverse reactions and to use effective alternative (nonhormonal) contraception during therapy with Cyklokapron.

    Seizures 

    Cyklokapron may cause seizures and patients should contact their healthcare provider for any signs or symptoms suggestive of seizures. 

    Hypersensitivity Reactions 

    Cyklokapron may cause hypersensitivity reactions and patients should contact their healthcare provider for any signs or symptoms of hypersensitivity reactions. 

    Visual Disturbances 

    Cyklokapron can cause visual disturbance and patients should report any eye symptoms or change in their vision to their healthcare provider and to follow-up with an ophthalmologist for a complete ophthalmologic evaluation, including dilated retinal examination of the retina. 

    Risk of Driving and Operating Machinery 

    Cyklokapron may cause dizziness, and patients should be cautioned about driving, operating machinery, or performing hazardous tasks while taking Cyklokapron.

    Cost Savings Program

    The Cyklokapron savings program is available here.

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