Cyklokapron

Yes

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.

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.

Cyklokapron is a prescription medicine used to prevent the breakdown of blood clots. Cyklokapron belongs to a group of drugs called antifibrinolytics which work by preventing the breakdown of blood clots.

Cyklokapron is available in an injectable form to be given directly into a vein (IV) by a healthcare professional and is given immediately before tooth extraction and following tooth extraction. Cyklokapron injection is used to reduce or prevent hemorrhage and reduce the need for replacement therapy during and following tooth extraction in patients with hemophilia as short-term use (two to eight days).

• Pharmacia and Upjohn Company

Tell your doctor if you have ever had any unusual or allergic reaction to this medicine or any other medicines. Also tell your health care professional if you have any other types of allergies, such as to foods, dyes, preservatives, or animals. For non-prescription products, read the label or package ingredients carefully.

Call your doctor for instructions if you miss a dose.

Your doctor or pharmacist can provide more information about tranexamic acid (Cyklokapron).

Remember, keep this and all other medicines out of the reach of children, never share your medicines with others, and use this medication only for the indication prescribed.

Every effort has been made to ensure that the information provided by Cerner Multum, Inc. ('Multum') is accurate, up-to-date, and complete, but no guarantee is made to that effect. Drug information contained herein may be time sensitive. Multum information has been compiled for use by healthcare practitioners and consumers in the United States and therefore Multum does not warrant that uses outside of the United States are appropriate, unless specifically indicated otherwise. Multum's drug information does not endorse drugs, diagnose patients or recommend therapy. Multum's drug information is an informational resource designed to assist licensed healthcare practitioners in caring for their patients and/or to serve consumers viewing this service as a supplement to, and not a substitute for, the expertise, skill, knowledge and judgment of healthcare practitioners. The absence of a warning for a given drug or drug combination in no way should be construed to indicate that the drug or drug combination is safe, effective or appropriate for any given patient. Multum does not assume any responsibility for any aspect of healthcare administered with the aid of information Multum provides. The information contained herein is not intended to cover all possible uses, directions, precautions, warnings, drug interactions, allergic reactions, or adverse effects. If you have questions about the drugs you are taking, check with your doctor, nurse or pharmacist.

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Tranexamic acid is a man-made form of an amino acid (protein) called lysine. Tranexamic acid prevents enzymes in the body from breaking down blood clots.

Cyklokapron is used to prevent bleeding in people with hemophilia who need to have a tooth pulled. This medication is usually given just before the dental procedure, and daily for up to 8 days afterward.

Tranexamic acid may also be used for purposes not listed in this medication guide.

Follow all directions on your prescription label. Do not use this medicine in larger or smaller amounts or for longer than recommended.

Cyklokapron is injected into a vein through an IV just before your tooth is pulled. You may need to keep using the medication for up to 8 days afterward.

You may be shown how to use an IV at home. Do not self-inject Cyklokapron if you do not fully understand how to give the injection and properly dispose of used needles, IV tubing, and other items used to inject the medicine.

To be sure this medicine is not causing harmful effects, your vision may need to be tested while you are using tranexamic acid. Follow your doctor's instructions.

Store this medication at room temperature away from moisture and heat.

This medication may impair your vision. Be careful if you drive or do anything that requires you to be able to see clearly.

Tranexamic acid injection is used to control or prevent excessive or heavy bleeding during dental procedures in patients with hemophilia. This medicine is for short-term use only, usually 2 to 8 days.

Tranexamic acid injection is an antifibrinolytic agent. It works by blocking the breakdown of blood clots. It may also be used for other conditions as determined by your doctor.

This medicine is available only with your doctor's prescription.

All drugs may cause side effects. However, many people have no side effects or only have minor side effects. Call your doctor or get medical help if any of these side effects or any other side effects bother you or do not go away:

• Upset stomach or throwing up.
• Loose stools (diarrhea).

These are not all of the side effects that may occur. If you have questions about side effects, call your doctor. Call your doctor for medical advice about side effects.

You may report side effects to the FDA at 1-800-FDA-1088. You may also report side effects at http://www.fda.gov/medwatch.

• If your symptoms or health problems do not get better or if they become worse, call your doctor.
• Do not share your drugs with others and do not take anyone else's drugs.
• Keep a list of all your drugs (prescription, natural products, vitamins, OTC) with you. Give this list to your doctor.
• Talk with the doctor before starting any new drug, including prescription or OTC, natural products, or vitamins.
• Keep all drugs in a safe place. Keep all drugs out of the reach of children and pets.
• Check with your pharmacist about how to throw out unused drugs.
• Some drugs may have another patient information leaflet. Check with your pharmacist. If you have any questions about this medicine, please talk with your doctor, nurse, pharmacist, or other health care provider.
• If you think there has been an overdose, call your poison control center or get medical care right away. Be ready to tell or show what was taken, how much, and when it happened.

This information should not be used to decide whether or not to take Cyklokapron or any other medicine. Only the healthcare provider has the knowledge and training to decide which medicines are right for a specific patient. This information does not endorse any medicine as safe, effective, or approved for treating any patient or health condition. This is only a brief summary of general information about this medicine. It does NOT include all information about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to Cyklokapron. This information is not specific medical advice and does not replace information you receive from the healthcare provider. You must talk with the healthcare provider for complete information about the risks and benefits of using this medicine.

Review Date: October 4, 2017

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:

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

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.

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.

Summary of Use during Lactation

Amounts of tranexamic acid in breastmilk appear to be low. Although an international consensus panel recommended against using tranexamic acid during breastfeeding,[1] a subsequent controlled study found no adverse outcomes among breastfed infants whose mothers took tranexamic acid in dosages up to 4 grams daily during breastfeeding. One center in Canada reports routine use of tranexamic acid 3 grams daily in nursing mothers with bleeding disorders until bleeding stops.[2] If tranexamic acid is required by a mother, it is not a reason to discontinue breastfeeding; however, until more data become available, medical supervision and follow-up of the breastfed infant is recommended.[3]

Drug Levels

Maternal Levels. Unpublished data from the manufacturer indicates that the concentration of tranexamic acid in breastmilk is 1% of the peak serum concentration 1 hour after the last dose of a 2-day treatment course.[4] Further details of the study have not been published. Infant Levels. Relevant published information was not found as of the revision date.

Effects in Breastfed Infants

Twenty-one mothers who took tranexamic acid during breastfeeding were compared to 42 mothers who took amoxicillin during breastfeeding. In the study population, the tranexamic acid dosage ranged between 1.5 and 4 grams daily at an average of 4.2 months of age and 81% exclusively breastfed their infants. The average time of follow-up of the infants of study mothers was 35.7 months of age. No statistically significant difference were found between the study and control groups in possible drug side effects, neurological development or general health.[3]

Effects on Lactation and Breastmilk

Relevant published information was not found as of the revision date.

References

1. Caballero T, Farkas H, Bouillet L et al. International consensus and practical guidelines on the gynecologic and obstetric management of female patients with hereditary angioedema caused by C1 inhibitor deficiency. J Allergy Clin Immunol. 2012;129:308-20. PMID: 22197274

2. Hawke L, Grabell J, Sim W et al. Obstetric bleeding among women with inherited bleeding disorders: A retrospective study. Haemophilia. 2016;22:906-11. PMID: 27704714

3. Gilad O, Merlob P, Stahl B, Klinger G. Outcome following tranexamic acid exposure during breastfeeding. Breastfeed Med. 2014;9:411-2. PMID: 25025926

4. Verstraete M. Clinical application of inhibitors of fibrinolysis. Drugs. 1985;29:236-61. PMID: 2580684

Substance Name

Tranexamic Acid

CAS Registry Number

1197-18-8

Drug Class

Antifibrinolytic Agents