Tranexamic acid (injection)

Tranexamic acid (injection)
Adult Indications & Dosage
Pediatric Indications & Dosage
Contraindications
Warnings & Precautions
Adverse Reactions
Drug Interactions
Use in Specific Populations
Administration & Monitoring
Overdosage
Pharmacology
Clinical Studies
How Supplied
Images
Patient Counseling Information
Precautions with Alcohol
Brand Names
Look-Alike Names

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief: Turky Alkathery, M.D. [2]

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Overview

Tranexamic acid (injection) is an antifibrinolytic agent that is FDA approved for the treatment of 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. Common adverse reactions include abdominal pain, anemia, arthralgia, backache, cramps, musculoskeletal pain, headache, migraine, nasal sinus problem and fatigue.

Adult Indications and Dosage

FDA-Labeled Indications and Dosage (Adult)

Indication

• 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.

Dosage

• Immediately before tooth extraction in patients with hemophilia, administer 10 mg per kg body weight of CYKLOKAPRON intravenously together with replacement therapy.
• 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:

This image is provided by the National Library of Medicine.

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.

Off-Label Use and Dosage (Adult)

Guideline-Supported Use

There is limited information regarding Off-Label Guideline-Supported Use of Tranexamic acid in adult patients.

Non–Guideline-Supported Use

• Dental surgical procedure - Hemophilia - Hemorrhage.

Pediatric Indications and Dosage

FDA-Labeled Indications and Dosage (Pediatric)

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 therapy.

Off-Label Use and Dosage (Pediatric)

Guideline-Supported Use

There is limited information regarding Off-Label Guideline-Supported Use of Tranexamic acid in pediatric patients.

Non–Guideline-Supported Use

There is limited information regarding Off-Label Non–Guideline-Supported Use of Tranexamic acid in pediatric patients.

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.
• 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.

Warnings

Focal areas of retinal degeneration have developed in cats, dogs, and rats following oral or intravenous tranexamic acid at doses between 250 to 1600 mg/kg/day (6 to 40 times the recommended usual human dose) from 6 days to 1 year. The incidence of such lesions has varied from 25% to 100% of animals treated and was dose-related. At lower doses, some lesions have appeared to be reversible.

Limited data in cats and rabbits showed retinal changes in some animals with doses as low as 126 mg/kg/day (only about 3 times the recommended human dose) administered for several days to two weeks.

No retinal changes have been reported or noted in eye examinations in patients treated with tranexamic acid for weeks to months in clinical trials.

However, visual abnormalities, often poorly characterized, represent the most frequently reported postmarketing adverse reaction in Sweden. For patients who are to be treated continually for longer than several days, an ophthalmological examination, including visual acuity, color vision, eye-ground, and visual fields, is advised, before commencing and at regular intervals during the course of treatment. Tranexamic acid should be discontinued if changes in examination results are found.

Convulsions have been reported in association with tranexamic acid treatment, particularly in patients receiving tranexamic acid during cardiovascular surgery and in patients inadvertently given tranexamic acid into the neuraxial system.

PRECAUTIONS

General

• The dose of CYKLOKAPRON Injection should be reduced in patients with renal insufficiency because of the risk of accumulation.

• 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 thrombosis.

• 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.

Adverse Reactions

Clinical Trials Experience

Gastrointestinal disturbances (nausea, vomiting, diarrhea) may occur but disappear when the dosage is reduced. Allergic dermatitis, giddiness, and hypotension have been reported occasionally. Hypotension has been observed when intravenous injection is too rapid. To avoid this response, the solution should not be injected more rapidly than 1 mL per minute.

Postmarketing Experience

Worldwide Postmarketing Reports

Thromboembolic events (e.g., deep vein thrombosis, pulmonary embolism, cerebral thrombosis, acute renal cortical necrosis, and central retinal artery and vein obstruction) have been rarely reported in patients receiving tranexamic acid for indications other than hemorrhage prevention in patients with hemophilia. Convulsion, chromatopsia, and visual impairment have also been reported. However, due to the spontaneous nature of the reporting of medical events and the lack of controls, the actual incidence and causal relationship of drug and event cannot be determined.

Drug Interactions

No studies of interactions between CYKLOKAPRON and other drugs have been conducted.

Use in Specific Populations

Pregnancy

Pregnancy Category (FDA): B 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.
Pregnancy Category (AUS): There is no Australian Drug Evaluation Committee (ADEC) guidance on usage of Tranexamic acid (injection) in women who are pregnant.

Labor and Delivery

See above under Pregnancy.

Nursing Mothers

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.

Pediatric Use

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 therapy.

Geriatic Use

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.

Gender

There is no FDA guidance on the use of Tranexamic acid (injection) with respect to specific gender populations.

Race

There is no FDA guidance on the use of Tranexamic acid (injection) with respect to specific racial populations.

Renal Impairment

The dose of CYKLOKAPRON Injection should be reduced in patients with renal insufficiency because of the risk of accumulation.

Hepatic Impairment

There is no FDA guidance on the use of Tranexamic acid (injection) in patients with hepatic impairment.

Females of Reproductive Potential and Males

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.

Immunocompromised Patients

There is no FDA guidance one the use of Tranexamic acid (injection) in patients who are immunocompromised.

Administration and Monitoring

Administration

• Intravenous.

Monitoring

• Monitor renal function in elderly patients because they are more likely to have decreased renal function, care should be taken in dose selection.

IV Compatibility

There is limited information regarding the compatibility of Tranexamic acid (injection) and IV administrations.

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.

Pharmacology

Mechanism of Action

There is limited information regarding Tranexamic acid (injection) Mechanism of Action in the drug label.

Structure

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

Structural Formula:

This image is provided by the National Library of Medicine.

Tranexamic acid is a white crystalline powder. The aqueous solution for injection has a pH of 6.5 to 8.0.

Pharmacodynamics

There is limited information regarding Tranexamic acid (injection) Pharmacodynamics in the drug label.

Pharmacokinetics

There is limited information regarding Tranexamic acid (injection) Pharmacokinetics in the drug label.

Nonclinical Toxicology

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.

Clinical Studies

There is limited information regarding Tranexamic acid (injection) Clinical Studies in the drug label.

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].

Images

Drug Images

{{#ask: Page Name::Tranexamic acid (injection) |?Pill Name |?Drug Name |?Pill Ingred |?Pill Imprint |?Pill Dosage |?Pill Color |?Pill Shape |?Pill Size (mm) |?Pill Scoring |?NDC |?Drug Author |format=template |template=DrugPageImages |mainlabel=- |sort=Pill Name }}

Package and Label Display Panel

fizer Injectables

Rx only

NDC 0013-1114-01

10 mL ampule Cyklokapron® tranexamic acid injection 1000 mg/10 mL (100 mg/mL) Solution for intravenous injection Single-Dose ONLY Discard any remaining portion after single use

PAA058409

This image is provided by the National Library of Medicine.

NDC 0013-1114-01

Contains 1 Ampule 10 mL Cyklokapron® tranexamic acid injection

1000 mg/10 mL (100 mg/mL)

Solution for intravenous injection

Single-Dose ONLY Discard any remaining portion after single use

Rx only

Pfizer Injectables

This image is provided by the National Library of Medicine.

NDC 0013-1114-10

Contains 10 of NDC 0013-1114-01

10 x 10 mL ampules

Cyklokapron®

tranexamic acid injection

1000 mg/10 mL (100 mg/mL) Solution for intravenous injection

Single-Dose ONLY

Discard any remaining

portion after single use

Rx only

This image is provided by the National Library of Medicine.

NDC 0013-1114-20

10 mL Vial

Cyklokapron®

(tranexamic acid injection)

1000 mg/10 mL

(100 mg/mL) Rx only

This image is provided by the National Library of Medicine.

NDC 0013-1114-20

Contains 1 Vial 10 mL

Cyklokapron® (tranexamic acid injection)

1000 mg/10 mL (100 mg/mL)

Solution for intravenous injection

Single-Dose ONLY Discard any remaining portion after single use

Rx only

Pfizer Injectables

This image is provided by the National Library of Medicine.

LOT/EXP

Store at 25°C (77°F); excursions permitted to 15°-30°C (59°-86°F) [see USP Controlled Room Temperature].

DOSAGE AND USE: See accompanying prescribing information.

Each vial contains 1 g tranexamic acid.

MADE IN JAPAN

Distributed by Pharmacia & Upjohn Co Division of Pfizer Inc, NY, NY 10017

NDC 0013-1114-21 Contains 10 of NDC 0013-1114-20

10 x 10 mL Vials

Cyklokapron®

(tranexamic acid injection) 1000 mg/10 mL (100 mg/mL)

Solution for intravenous injection

Single-Dose ONLY Discard any remaining portion after single use

Rx only

PAA057067

This image is provided by the National Library of Medicine.

Ingredients and Appearance

This image is provided by the National Library of Medicine.

{{#ask: Label Page::Tranexamic acid (injection) |?Label Name |format=template |template=DrugLabelImages |mainlabel=- |sort=Label Page }}

Patient Counseling Information

There is limited information regarding Tranexamic acid (injection) Patient Counseling Information in the drug label.

Precautions with Alcohol

Alcohol-Tranexamic acid interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.

Brand Names

• CYKLOKAPRON ®

Look-Alike Drug Names

There is limited information regarding Tranexamic acid (injection) Look-Alike Drug Names in the drug label.

Drug Shortage Status

Price

References

The contents of this FDA label are provided by the National Library of Medicine.