Tranexaminezuur

Tranexaminezuur Uses, Dosage, Side Effects, Food Interaction and all others data.

PHARMACOLOGICAL ACTIONS: Tranexamic acid has a strong inhibitory effect on the activation of plasminogen, i.e. the conversion of plasminogen to plasmin, in the fibrinolytic system.The half life is 1-2 hours. Plasma protein binding is 3% at therapeutic plasma levels. The plasma protein binding seems fully accounted by its binding to plasminogen. Tranexamic acid is excreted unchanged in the urine.

PHARMACOKINETICS: Tranexamic acid is rapidly absorbed from the gastrointestinal tract. Maximum serum levels are reached within 2-3 hours. After oral administration, about 40% of the dose is excreted in the urine during the first 24 hours. After intravenous administration 45% of the dose is excreted in the urine during the first day.

Tranexamic acid is an antifibrinolytic that competitively inhibits the activation of plasminogen to plasmin. At much higher concentrations it behaves as a noncompetitive inhibitor of plasmin similar to aminocaproic acid, a similar antifibrinolytic which is 10-fold less potent. Tranexamic acid binds more strongly than aminocaproic acid to both the strong and weak receptor sites of the plasminogen molecule in a ratio corresponding to the difference in potency between the compounds. In patients with hereditary angioedema, inhibition of the formation and activity of plasmin by tranexamic acid may prevent attacks of angioedema by decreasing plasmin-induced activation of the first complement protein (C1).

Off-target antagonism of GABA(A) receptors may be associated with the development of convulsions and hyperexcitability following tranexamic acid administration - the risk appears higher with improper administration or administration during cardiovascular surgery. Consider EEG monitoring of patients with a history of seizure.

Trade Name Tranexaminezuur
Generic Tranexamic Acid
Tranexamic Acid Other Names Acide tranéxamique, ácido tranexámico, Acidum tranexamicum, Tranexamic acid, Tranexamsaeure, Tranexmic acid, Tranhexamic acid, Trans AMCHA, trans-Amcha, trans-Tranexamic acid
Type
Formula C8H15NO2
Weight Average: 157.2102
Monoisotopic: 157.110278729
Protein binding

Tranexamic acid is approximately 3% protein-bound in plasma at therapeutic concentrations. As it does not bind to serum albumin, it is likely that this protein binding is accounted for by tranexamic acid's binding to serum plasminogen.

Groups Approved
Therapeutic Class Anti-fibrinolytic drugs, Haemostatic drugs
Manufacturer
Available Country Netherlands
Last Updated: September 19, 2023 at 7:00 am
Tranexaminezuur
Tranexaminezuur

Uses

Haemorrhage or risk of haemorrhage in increased fibrinolysis or fibrinogenolysis that may occur in conditions:

  • Prostatectomy and bladder surgery
  • Menorrhagia
  • Epistaxis
  • Conisation of the cervix
  • Management of dental extraction in patients with coagulopathies
  • Ulcerative colitis
  • Haematuria
  • Gastrointestinal haemorrhage

General fibrinolysis as in prostatic and pancreatic cancer, after thoracic and other major surgery, in obstetrical complications such as abruptio placentae and post- partum haemorrhage, in leukaemia and liver diseases and in connection with thrombolytic therapy with streptokinase.

Hereditary angioneurotic oedema.

Tranexaminezuur is also used to associated treatment for these conditions: Bleeding, Heavy Menstrual Bleeding, Hereditary Angioedema

How Tranexaminezuur works

Tranexamic acid competitively and reversibly inhibits the activation of plasminogen via binding at several distinct sites, including four or five low-affinity sites and one high-affinity site, the latter of which is involved in its binding to fibrin. The binding of plasminogen to fibrin induces fibrinolysis - by occupying the necessary binding sites tranexamic acid prevents this dissolution of fibrin, thereby stabilizing the clot and preventing hemorrhage.

Dosage

Tranexaminezuur dosage

Intravenous administration is necessary only if it is difficult to give adequate doses by mouth. The recommended standard dose is 1 to 1.5 gm or 5-10 ml by slow intravenous injection at a rate of 1 ml/minute, two to three times daily. For the indications listed below the following doses are recommended.

PROSTATECTOMY: 5-10 ml by slow intravenous injection every eight hours (the first injection being given during the operation) for the first three days after surgery; thereafter 1-1.5 gm orally three to four times daily until macroscopic haematuria is no longer present.

MENORRHAGIA: 1-1.5 gm orally three to four times daily for three to four days.

EPISTAXIS: 1.5 gm orally three times daily for four to ten days.

Tranexaminezuur injection may be applied topically to the nasal mucosa of patients suffering from epistaxis. This can be done by soaking a gauze strip in the solution,and then packing the nasal cavity.

HAEMATURIA: 1-1.5 gm orally 2-3 times daily until macroscopic haematuria is no longer present.

CONISATION OF THE CERVIX: 1.5 gm orally 3 times a day for 12 to 14 days post-operatively.

DENTAL SURGERY IN PATIENTS WITH COAGULOPATHIES: Immediately before surgery, 10 mg per kg body-weight should be given intravenously. After surgery, 25 mg per kg body-weight are given orally three to four times daily for six to eight days. Coagulation factor concentrate might be necessary to administrate.

GENERAL FIBRINOLYSIS: 1 gm by slow intravenous injection three to four times daily. With fibrinolysis in conjunction with diagnosed, increased intravascular coagulation i.e. defibrillation syndrome, an anticoagulant such as heparin may be given with caution.

HEREDITARY ANGIONEUROTIC OEDEMA: 1-1.5 gm orally two to three times daily as intermittent or continuous treatment depending on whether the patient has prodromal symptoms or not.

CHILDREN:

  • Oral dose: 25 mg/kg 2 to 3 times daily for 7 to 10 days.
  • Injection: 10 mg/kg 6 to 8 hours for 7 to 10 days

Side Effects

Dose-dependent, gastrointestinal discomfort is the most commonly reported undesirable effect, but it is usually of mild and temporary in nature. Allergic skin reactions have been reported as an uncommon undesirable effect. Hypotension may occur after fast injection.

Toxicity

Reported symptoms of tranexamic acid overdose include severe gastrointestinal symptoms, hypotension, thromboembolism, visual impairment, convulsions, mental status changes, and rash.

Precaution

Patients with irregular menstrual bleeding, patients with a high risk of thrombosis (a previous thromboembolic event and a family history of thromboembolic disease) should use it only if there is a strong medical indication and under strict medical supervision.

Patients with disseminated intravascular coagulation (DIC), who require treatment with it must be under the strict supervision of a physician experienced in treating this disorder.

In the long-term treatment of patients, regular eye examination should be performed. If a colour vision disorder should occur during the course of treatment, the drug should be discontinued.

Interaction

Clinically important interactions have not been observed with Tranexamic acid. Because of the absence of interaction studies, simultaneous treatment with anticoagulants must take place under the strict supervision of a physician experienced in this field.

Food Interaction

  • Take with or without food. The co-administration of food does not significantly affect tranexamic acid disposition.

Volume of Distribution

The initial volume of distribution of tranexamic acid is 0.18 L/kg and its steady-state volume of distribution is 0.39 L/kg. Tranexamic acid distributes into cerebrospinal fluid and the aqueous humor of the eye at concentrations approximately 1/10th of typical plasma concentrations. Tranexamic acid is also able to cross the placenta, found in cord blood at concentrations equivalent to maternal plasma concentrations.

Elimination Route

The bioavailability of tranexamic acid after oral administration in humans is approximately 30 to 50% of the ingested dose and is not affected by food intake. The Cmax and Tmax following multiple oral doses (1300 mg three times daily x 5 days) were 16.41 mcg/mL and 2.5 h, respectively.

Half Life

Following intravenous administration, the apparent elimination half-life is approximately 2 hours and the mean terminal half-life is approximately 11 hours.

Clearance

The plasma clearance of tranexamic acid is 110-116 mL/min.

Elimination Route

Urinary excretion is the primary means of tranexamic acid elimination, with >95% of an administered dose excreted in the urine as unchanged parent drug. The rate of excretion is dependent on the route of administration - approximately 90% of an intravenously administered dose is excreted within 24 hours whereas only 39% of an orally administered dose is excreted within the same time frame.

Pregnancy & Breastfeeding use

Pregnancy: Tranexamic acid crosses the placenta. Clinical experience of use in pregnant women is limited. Animal studies have not supplied any evidence of an increased incidence of fetal damage.

Lactation: Tranexamic acid is excreted into breast milk, but it is not likely to influence the child at therapeutic doses.

Contraindication

  • Active thromboembolic disease, such as deep vein thrombosis, pulmonary embolism and cerebral thrombosis
  • Subarachnoid haemorrhage
  • Hypersensitivity to Tranexamic acid or any of the ingredients

Special Warning

Renal Impairment:

Intravenous : Adjust dose based on the serum-creatinine concentration:

  • 120-250 micromol/l: 10 mg/kg bid daily;
  • 250-500 micromoles/l: 10 mg/kg once daily;
  • >500 micromol/l: 5 mg/kg once daily or 10 mg/kg once every 48 hr.

Oral : Adjust dose based on serum creatinine concentration:

  • 120-250 micromol/l: 15 mg/kg bid daily;
  • 250-500 micromol/l: 15 mg/kg once daily;
  • >500 micromol/l: 7.5 mg/kg once daily or 15 mg/kg once every 48 hr.

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 Tranexamic acid therapy.

Geriatric Use: Clinical studies of Tranexamic acid did not include sufficient numbers of subjects aged 65 and over to determine whether they respond different y from younger subjects. Other reported clinical experien e 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. Drug Interaction Tranexaminezuur is known to interact with other drugs like Factor VIII. These interactions are sometimes beneficial and sometimes may pose threats to life. Always consult your physician for the change of dose regimen or an alternative drug of choice that may strictly be required. Pharmaceutical Precaution Keep in a cool & dry place, protected from light. Keep out of the reach of children.

Acute Overdose

Symptoms: Nausea, vomiting, dizziness, and headache.

Treatment of overdose: If justified, initiate vomiting, then gastric lavage, charcoal therapy, and symptomatic treatment. Maintain adequate diuresis.

Storage Condition

Store at a cool and dry place, protected from light and moisture.

Innovators Monograph

You find simplified version here Tranexaminezuur

Tranexaminezuur contains Tranexamic Acid see full prescribing information from innovator Tranexaminezuur Monograph, Tranexaminezuur MSDS, Tranexaminezuur FDA label

FAQ

What is Tranexaminezuur used for?

Tranexaminezuur is used to control heavy menstrual bleeding. It helps your blood to clot and is used for nosebleeds and heavy periods. If you're having a tooth taken out, using Tranexaminezuur mouthwash can help stop bleeding.

How safe is Tranexaminezuur?

Gennerally using Tranexaminezuur for a long time doesn't cause harmful side effects.The medicine was well-tolerated when used properly.

What are the common side effects of Tranexaminezuur?

The more common side effects of Tranexaminezuur include:

  • nausea
  • diarrhea
  • stomach pain or discomfort
  • vomiting
  • chills
  • fever
  • severe headache (throbbing)
  • back or joint pain
  • muscle pain
  • muscle stiffness
  • difficulty moving
  • runny or stuffy nose

Is Tranexaminezuur safe during pregnancy?

Tranexaminezuur seems to be safe and effective in the prevention and management of bleeding during pregnancy.

Is Tranexaminezuur safe during breastfeeding?

No increase in adverse long-term outcomes was found in infants exposed through breastfeeding to Tranexaminezuur. Our data in conjunction with previous estimates of very low drug exposure support continuation of breastfeeding in women requiring treatment with Tranexaminezuur.

How long does Tranexaminezuur stay in my system?

The mean terminal half-life of Tranexaminezuur is approximately 11 hours.

How long does it take for Tranexaminezuur to start working?

It can take up to 24 hours for the medicine to take full effect.Tranexaminezuur is usually used for a short time to treat bleeding. Usually you will take this medicine for 4 days for heavy periods, or for 7 days to treat other bleeding that does not stop by itself.

Does Tranexaminezuur stop bleeding completely?

Tranexaminezuur is given to stop or reduce heavy bleeding. When you bleed, your body forms clots to stop the bleeding. In some people, these clots break down and the bleeding continues. Tranexaminezuur works by stopping the clots from breaking down and so reduces the unwanted bleeding.

Who should not take Tranexaminezuur?

You should not use this medication if you are also using combination hormonal contraception because it may increase your chance of having a blood clot, heart attack, or stroke. Your risk is even higher if you are overweight, if you smoke cigarettes, or if you are over 35 years of age.

When is the best time to take Tranexaminezuur?

Tranexaminezuur comes as a tablet to take by mouth. It is usually taken with or without food three times a day for up to 5 days during monthly menstruation. You should begin taking this medication each month when your period starts.

Does Tranexaminezuur cause stroke?

Some studies have shown that Tranexaminezuur increases the risk of stroke.

Does Tranexaminezuur lighten skin?

The skin whitening effects of tranexamic acid was incidentally found when it was used in the treatment of aneurysmal subarachnoid hemorrhage.

Can I use Tranexaminezuur every night?

Tranexaminezuur recommends you use the treatment two to three nights a week. This is because their formula doesn't layer well alongside moisturisers and oils, so to prevent dehydration you should only use it a few times a week.

What does Tranexaminezuur do for skin?

Tranexaminezuur is primarily used as an ingredient that helps brighten dark spots and improve pigmentation.

What happen If I missed Tranexaminezuur?

If you forget to take your dose of Tranexaminezuur, take it as soon as you remember, unless it's nearly time for your next dose. In this case, skip the missed dose and take the next one at the usual time. Do not take 2 doses at the same time.

Is it safe to take Tranexaminezuur every month?

Do not take Tranexaminezuur tablets for more than 5 days in a menstrual cycle or take more than 6 tablets in a 24 hour period of time.

How many days should I take Tranexaminezuur?

Tranexaminezuur tablets are usually taken 3 times a day for a maximum of 4 days. You start taking the tablets as soon as your period starts

Can Tranexaminezuur stop working?

Tranexaminezuur isn't for everyone. If it stops working or doesn't decrease heavy menstrual bleeding within two cycles, your doctor might suggest other medications for heavy periods.

What happen if I overdose on Tranexaminezuur?

Overdose symptoms may include headache, confusion, vision problems, vomiting, diarrhea, numbness or weakness, problems with speech or balance, feeling light-headed, or fainting.

Can I drink alcohol with Tranexaminezuur?

Yes, you can drink alcohol while taking Tranexaminezuur.

Will Tranexaminezuur affect my fertility?

There is no firm evidence to suggest that taking Tranexaminezuur will reduce fertility in either men or women.

Can I drive or ride after taking Tranexaminezuur?

Taking Tranexaminezuur will not affect your ability to drive a car or ride a bike.

Is there any food or drink I should avoid?

You can eat and drink normally while taking Tranexaminezuur.

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*** Taking medicines without doctor's advice can cause long-term problems.
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