Tranexamic Acid - Uses, Dosage, and Pharmacology

Overview:

Tranexamic acid is an antifibrinolytic and was initially approved by the Food Drug Administration (FDA) in 1986 to control excessive bleeding in dental surgery. In 1996, the FDA approved the drug for controlling hemorrhage in patients with hemophilia. In 2009 the drug was approved for the treatment of cyclic heavy menstrual bleeding.

How Does Tranexamic Acid Work?

The drug works by breaking down clots and inhibits the activation of plasminogen to plasmin. This helps break down the blood clots and helps maintain clot stability.

Uses:

Tranexamic acid is best used to control bleeding, especially during the menstrual cycle (periods), and it is classified under the group of drugs called antifibrinolytics. It helps break down the blood clots and prevents prolonged bleeding.

Dosage:

The usual drug dosage is 10 mg/kg, given orally twice or thrice a day. In heavy menstrual bleeding, the dosage may vary between one to one and a half grams for a period of five days.

Warnings:

Individuals consuming Tranexamic acid are supposed to inform the doctors in case of any allergic reactions. In addition, previous history of bleeding in the brain, heart conditions, blood clotting, and kidney problems have to be reported to the doctor.

For Patients

What Is the Menstrual Cycle?

It is a natural process occurring in females and is regulated by the interplay of hormones. It usually lasts 28 days and may vary between 21 to 35 days, depending on the individual. It has various stages, which are mentioned below.

• The menstrual phase is the start of the cycle and stays for three to seven days. In this phase, the uterus sheds its lining, which results in menstrual bleeding.

• The follicular phase follows the menstrual phase and lasts approximately fourteen days. In this phase, the follicular stimulating hormone and luteinizing hormone stimulate the growth of follicles in the ovary.

• The ovulation phase occurs when the mature follicles release an egg, traveling down the fallopian tube. It occurs around the fourteenth day and may vary.

• The luteal phase starts after ovulation and stays for fourteen days. The ruptured follicle prepares the uterus for egg implantation. If fertilization does not occur, the corpus luteum degenerates, and the hormonal levels decrease. This results in the shedding of the uterine lining and starts a new menstrual cycle.

When and How Often to Take Tranexamic Acid?

Tranexamic acid is usually available in the form of tablets and has to be taken orally. The drug is to be taken twice or thrice a day with food or after food as instructed by the doctor. Avoid crushing or chewing the drug. It is better to wait until the due date for the menstrual cycle and start the first dose. It is not advised to take Tranexamic acid for more than five days.

How Effective Is Tranexamic Acid?

The drug is highly effective in altering the blood loss caused due to menstrual cycle. It has also been effective in treating traumatic brain injuries and severe bleeding. Administration of the drug has proven to significantly reduce the risk of death due to bleeding. The drug has various proven studies to support its importance in better outcomes. In addition, Tranexamic acid is well tolerated by most individuals. Hence, the drug is used in most surgeries to control bleeding due to its effectiveness.

Things to Inform The Doctor Before They Prescribe Tranexamic Acid:

Inform the doctor of any allergic reaction and current medical and drug history, as it may help the doctor prescribe medications according to the prevailing conditions. Also, informing about any hereditary diseases existing in the family is also quite useful to alter the drug dosage accordingly.

How to Take Tranexamic Acid?

The drug is available in various forms, like tablets and injections. The exact dosage and administration could vary depending on the type of medical condition. A few guidelines to follow before the drug intake are listed below:

• It is crucial to follow the instructions suggested by the doctor regarding the sage, frequency, and duration of treatment.

• It is preferable to take the tablet with food or after a meal to eliminate the risk of stomach upset.

• Take a glass of water and swallow the drug. Avoid chewing or crushing the tablet, as it could obstruct the rate of drug absorption.

• Individuals using injections should avoid self-injecting the drug. The drug will be administered by the healthcare professional.

What Are the Side Effects of Tranexamic Acid?

Some of the following side effects have been reported in individuals taking Tranexamic acid.

• Nausea.

• Vomiting.

• Diarrhea.

• Muscle pain.

• Vision changes.

• Coughing blood.

• Fainting.

• Pain in arms and legs.

• Signs of stroke like difficulty in walking and speaking.

• Trouble speaking.

• Confusion.

• Weakness.

• Trouble speaking.

• Rash.

• Itching.

• Dizziness.

• Breathing difficulty.

Dietary Alterations:

No specific dietary alterations are recommended unless specified by the doctor. Consuming a healthy diet can help to maintain nutrition levels and a balanced lifestyle.

What Should Be Done When a Dose Is Missed?

In case of missing a dose while taking any medication, it is better to take it as soon as an individual remembers. Regular intake of medications has more beneficial effects on the body and helps in speedy recovery.

What Should Be Done to Treat Tranexamic Acid Overdose?

Tranexamic acid overdosing is quite rare; however, in such cases, it is safer to seek medical help at the earliest possible. Some common symptoms of overdosing are mentioned below:

• Seizures.

• Low blood pressure.

• Abnormal heart rhythm.

• Hallucinations.

• Confusions.

• Diarrhea.

• Nausea.

• Vomiting.

Activated charcoal can be administered in conscious patients, as it helps absorb the excess drug from the body and neutralizes it. In some cases, depending on the symptoms, the doctor may treat with intravenous fluids and medication to improve the heart rhythm. Preventing drug overdose can be achieved by strictly following the dose recommended by the healthcare professional.

How to Store Tranexamic Acid?

• Store the tablets at room temperature ranging from 20 degrees Celsius to 25 degrees Celsius.

• The injection vials have to be refrigerated at a temperature between two-degree Celsius to eight-degree Celsius.

• Avoid freezing the drug.

• Always check the label of any expiration before administering any form of Tranexamic acid.

How to Handle Tranexamic Acid?

In order to avoid accidental exposure, it is better to handle the drug carefully. Always use gloves while handling the drug. Follow the instructions suggested by the health professional. Inspect the product for any signs of damage or contamination. In case of injecting the drug, dispose of the needles carefully.

How to Dispose of Tranexamic Acid?

Avoid flushing the drug down the toilet or pouring it down the drain, as it could be a hazard. Contact the local take-back programs for safer drug disposals. Avoid the drug from getting in close contact with pets or children as it may harm them. Keep the drugs to be disposed of in a sealed bag.

Avoid Self-Medication:

Self-medicating any drug has its own side effects. Hence, it is better to thoroughly understand the purpose of the drug, its risks and benefits on health, and administer it carefully. Overlooking the potential damages could lead to life-threatening conditions.

Tips to Stay On Track:

Always set a reminder at the same time every day to avoid skipping the drug intake. Also, ensure to properly coordinate with the health professionals for regular follow-ups.

For Doctors:

Indication:

The drug is used to control bleeding in women experiencing menstruation. It is also used to control heavy bleeding in surgeries and hemorrhage.

Pharmacology:

Mechanism of Action:

The mechanism of action of the drug involves breaking down the blood clots, especially when the body experiences trauma or injury to the blood vessels. The body’s defense mechanism works by converting fibrinogen, a blood protein, into fibrin, which helps to stabilize the clot. Once the bleeding is arrested, the wound begins to heal by itself, and the body dissolves the clot, thereby preventing excessive clotting and restoring normal blood flow to various organs.

The drug acts at this stage and prevents the conversion of plasminogen to plasmin. This enzyme is crucial for breaking down and dissolving clots. Blocking the clot breakdown helps to maintain clot stability and decreases bleeding.

Pharmacodynamics:

The drug is shown to have anti-inflammatory effects and has the ability to cause the release of pro-inflammatory cytokines. It is effective in treating postpartum hemorrhage, menstrual bleeding, and bleeding in patients with hemophilia.

Active Ingredient:

The active ingredient is Tranexamic acid, which is a synthetic derivative of an amino acid called lysine. It works by blocking the breakdown of clots. The drug is available in various formulations like tablets, capsules, and injections for treating various medical conditions. The concentration in each formulation varies depending on the intended use of the drug.

Inactive Ingredients:

The following are some of the ingredients present in Tranexamic acid.

• Povidone.

• Magnesium stearate.

• Colloidal silicon dioxide.

• Polyethylene glycol.

• Iron oxide.

• Titanium dioxide.

• Hypromellose.

In the injection type, the inactive ingredients also include water for injection, hydrochloric acid, or sodium hydroxide to maintain the pH levels.

Absorption:

When administered orally, the drug is well absorbed and reaches a peak plasma concentration within two or three hours. The bioavailability of the drug is approximately 30 to 50 percent. The drug is primarily eliminated unchanged in the urine. The half-life of the drug is two hours in healthy individuals; however, it may vary in patients with renal impairment.

Distribution:

The drug is rapidly distributed throughout the body and has a moderate volume of distribution. It is mainly distributed in extracellular fluid and does not penetrate the blood-brain barrier. It has a high affinity to plasminogen and fibrinogen, thereby contributing to the antifibrinolytic effect.

Elimination:

The drug is cleared from the body predominantly by renal excretion. The overall metabolism is limited, as the pharmacokinetics of the drug depend on renal elimination. Patients with renal impairment should be closely monitored for side effects, and dosage alterations are to be made based on their renal functions.

Toxicity:

The toxicity of the drug is rare as it is generally well tolerated when used at lower levels. However, all medications can cause side effects and toxicity in individuals. In rare cases, serious adverse effects may result in renal failure.

Contraindications:

The drug is contraindicated in patients with the following conditions:

• Any previous history of thromboembolic events like deep vein thrombosis, pulmonary embolism, and stroke.

• Hematuria or blood in urine due to unknown origin, as the drug may mask the underlying condition.

• Women with a previous history of arterial or venous thromboembolism.

• In patients with subarachnoid hemorrhage, the drug may increase the risk of cerebral ischemia and infarction.

• Patients suffering from epilepsy or seizure should avoid taking Tranexamic acid.

Clinical Studies for Tranexamic Acid:

The drug has been subjected to numerous clinical studies and safety in medical conditions. The drug has been shown to reduce the risk of postpartum hemorrhage in multiple clinical trials. The study was conducted on 20,000 women, and the results concluded that Tranexamic acid reduces the risk of death due to bleeding in women with postpartum hemorrhage.

Drug Interactions:

Tranexamic acid is known to cause interactions with the following drugs:

• Tissue plasminogen activator.

• Aminocaproic acid.

• Non-steroidal anti-inflammatory drugs.

• Hormonal contraceptives.

• Anticoagulants.

Other Specifications:

• Tranexamic Acid in Pregnant Women: The drug is usually not prescribed to pregnant women. In extreme cases, if the drug is prescribed, strictly adhere to the instructions suggested by the healthcare professional.

• Tranexamic Acid in Lactating Women: The drug is contraindicated in lactating women as it could affect the child's growth and development. Lactating women should priorly inform the doctor, so they can prescribe an alternate medication.

• Tranexamic Acid in Pediatric Patients: The exact use of the drug in pediatric patients is yet to be understood. Currently, the drug is not prescribed in pediatric patients.

• Tranexamic Acid in Geriatric Patients: In elderly patients undergoing surgery, the drug may be prescribed occasionally to control excessive bleeding, as Tranexamic acid helps with blood clotting and prevents heavy loss of blood.

• Tranexamic Acid in Renal Impairment Patients: The drug is eliminated by the kidneys, so caution is to be taken while prescribing the medication to renal-impaired patients. Also, patients with end-stage renal disease should avoid using the drug as it could cause accumulation and toxicity. Patients with renal impairment are to be closely monitored post-drug administration for any potential adverse effects. In such cases, the drug administration should be re-evaluated, and appropriate action is to be taken.

• Tranexamic Acid in Hepatic Impairment Patients: Necessary caution is to be taken before administering the drug in hepatic-impaired patients. Patients suffering from mild to severe hepatic impairment should have lesser doses of Tranexamic acid. Close monitoring for side effects is required in patients with hepatic impairment.