Tranexamic acid

Heavy Menstrual Bleeding

Tranexamic acid tablets are used to treat cyclic heavy menstrual bleeding (menorrhagia) in women. This medication is not a hormone and is only taken during the menstrual period to help reduce the amount of blood loss.

Dental Procedures in Hemophilia

For individuals with hemophilia, tranexamic acid is used for short-term treatment to prevent or reduce bleeding during and after a tooth extraction. It is typically used for a period of 2 to 8 days to help stabilize blood clots and reduce the need for replacement therapy during the procedure.

How It Works

Tranexamic acid belongs to a class of medications called antifibrinolytics. It works by slowing the breakdown of blood clots, which helps to stop or prevent excessive bleeding in specific medical situations.

Mechanism of Action

Tranexamic acid belongs to a class of medications known as antifibrinolytics. It works by slowing the breakdown of blood clots, a process naturally occurring in the body called fibrinolysis.

When the body experiences bleeding, it forms clots to seal blood vessels. These clots are held together by a protein called fibrin. To eventually clear these clots, the body uses an enzyme called plasmin. Tranexamic acid interferes with this process in the following ways:

• Blocking plasminogen: It prevents the activation of plasminogen, which is the precursor to the enzyme that dissolves clots.
• Inhibiting plasmin: It stops existing plasmin from binding to and breaking down the fibrin mesh that stabilizes a blood clot.

By keeping blood clots intact for a longer period, tranexamic acid helps to decrease the amount of blood lost. In the case of heavy menstrual periods, it reduces the volume of blood flow but does not stop the period entirely. When used during surgery or after an injury, it helps the body maintain the clots necessary to prevent excessive hemorrhage.

Common Side Effects

Some people may experience mild side effects while taking tranexamic acid. These often include:

• Nausea, vomiting, or diarrhea
• Stomach pain
• Headache
• Muscle, back, or joint pain
• Muscle cramps
• Stuffy or runny nose
• Feeling tired

Serious Side Effects

Seek medical attention immediately if you experience any of the following serious symptoms:

• Vision problems: Any changes in your eyesight, including blurred vision or difficulty seeing colors.
• Signs of a blood clot: Sudden shortness of breath, chest pain, coughing up blood, or swelling, warmth, and redness in an arm or leg.
• Allergic reactions: Hives, rash, or swelling of the face, lips, or throat that makes it hard to breathe.
• Seizures: New or worsening tremors or convulsions.
• Dizziness: Feeling lightheaded or fainting.
• Confusion: Sudden changes in mental status.
• Urination issues: Blood in the urine or difficulty urinating.

Risk of Blood Clots

Tranexamic acid can increase the risk of serious blood clots, including deep vein thrombosis, pulmonary embolism, and cerebral thrombosis. It is generally not recommended for individuals with a history of these conditions or active thromboembolic disease. The risk is further increased when used in combination with hormonal contraceptives, such as birth control pills, patches, or rings.

Visual Disturbances

This medication may cause changes in vision, including problems with color perception or retinal vascular occlusion. If visual changes occur, the medication should be discontinued, and a complete eye examination is typically required.

Seizures and Administration Errors

Seizures have been reported with the use of tranexamic acid, particularly at high doses. There is also a significant risk of seizures and other neurological complications if the intravenous form is accidentally administered into the spinal fluid (intrathecal injection). Healthcare professionals must ensure the correct route of administration to prevent these errors.

Additional Precautions

• Kidney Impairment: Since the drug is primarily eliminated through the kidneys, patients with renal issues may require lower doses to avoid accumulation and toxicity.
• Allergic Reactions: Severe hypersensitivity reactions, including anaphylaxis, can occur.
• Subarachnoid Hemorrhage: Use in patients with bleeding around the brain may increase the risk of cerebral swelling or tissue death.

Pregnancy

There is limited information regarding the safety of tranexamic acid use during pregnancy. While animal studies have not shown evidence of harm to the developing fetus or impaired fertility, there are no adequate and well-controlled studies in humans. Because animal studies are not always predictive of human response, tranexamic acid should be used during pregnancy only if a healthcare provider determines it is clearly needed.

Tranexamic acid is known to cross the placenta and can be found in the umbilical cord blood at levels similar to those in the mother's blood.

Breastfeeding

Tranexamic acid is excreted into human breast milk. The concentration found in milk is approximately 1% of the concentration found in the mother's blood. Because the medication passes into breast milk, healthcare providers recommend exercising caution when using it while nursing. It is important to discuss the potential risks and benefits with a doctor before breastfeeding while taking this medication.

Available Forms

Tranexamic acid is supplied in the following formats:

• Oral Tablet: This form is taken by mouth. It is typically used for the treatment of heavy menstrual bleeding.
• Intravenous Injection: This form is a solution administered by a healthcare professional directly into a vein. It is generally used for the short-term prevention or reduction of bleeding during and after medical procedures, such as dental work in patients with certain bleeding disorders.

FDA Approval and Indications

The U.S. Food and Drug Administration (FDA) has approved tranexamic acid in both oral and injectable forms for specific medical conditions. The oral tablet is indicated for the treatment of cyclic heavy menstrual bleeding. The injectable form is approved for short-term use (two to eight days) in patients with hemophilia to reduce or prevent hemorrhage during and after tooth extraction.

Safety Communications

The FDA has issued safety alerts regarding the risk of medication errors involving tranexamic acid injection. There have been reports of the drug being accidentally administered intrathecally (into the spinal canal) when it was mistaken for anesthetic agents like bupivacaine or ropivacaine. Inadvertent spinal administration is a serious error that can lead to:

• Seizures
• Permanent neurological injury
• Death

To prevent these errors, the FDA recommends that healthcare providers implement clear labeling and store tranexamic acid separately from medications intended for spinal administration.

Regulatory Status

Tranexamic acid is a prescription-only medication. It is not currently subject to a Risk Evaluation and Mitigation Strategy (REMS) program. While it is used in various clinical settings, its officially recognized indications are limited to those established during the FDA approval process.

How it Works

Tranexamic acid belongs to a class of medicines called antifibrinolytics. It works by slowing the breakdown of blood clots, which helps to decrease the volume of blood lost during menstruation. It does not stop the menstrual cycle entirely, but rather makes the bleeding less heavy.

Usage and Administration

For the treatment of heavy menstrual bleeding, tranexamic acid is typically taken as an oral tablet. Key usage instructions include:

• Schedule: The medication is only taken during the days of the menstrual period, usually for a maximum of five days. It is not intended for daily use throughout the month.
• Dosage: It is often taken three times a day once heavy bleeding begins.
• Limitations: This medication does not provide contraception and does not protect against sexually transmitted infections. It is also not used to treat symptoms like menstrual cramps.

Safety and Precautions

Because tranexamic acid affects how blood clots, it carries specific risks:

• Blood Clot Risk: There is a risk of developing serious blood clots in the legs, lungs, or brain. This risk may be significantly increased if the medication is taken alongside hormonal contraceptives, such as the pill, patch, or ring.
• Pre-existing Conditions: It is generally avoided in individuals with a history of blood clots or those with certain vision problems.