Pradaxa – composition, action, dosage, indications and contraindications, side effects

Proven content

Pradaxa is a preparation that acts as an anticoagulant. Pradaxa can only be purchased with a prescription issued by a doctor. The active substance in Pradaxa is dabigatran etexilate, which works by blocking a substance that is responsible for the formation of blood clots. What are the indications and contraindications for the use of Pradaxa? How should this preparation be dosed? Can its use cause side effects in a patient?

Pradaxa – general characteristics of the drug

Pradaxa is a medicine with an anticoagulant effect. It can be purchased at a pharmacy only upon presentation of a prescription issued by a doctor.

Pradaxa is available as capsules with 3 possible active ingredient levels: 75 mg, 110 mg and 150 mg. The capsules are hard with a light blue opaque cap and a light blue opaque body printed with the Boehringer Ingelheim logo on the cap and a dose code on the body of the capsule.

The active substance of Pradaxa is dabigatran etexilate, which works by blocking the substances that are responsible for blood clots.

The entity responsible for the production and distribution of Pradaxa is a German pharmaceutical concern Boehringer Ingelheim International GmbH. The company was founded in 1885 by Albert Boehringer in Ingelheim on the Rhine in Germany. It is now one of the world’s 20 leading pharmaceutical companies. The company is still headquartered in Ingelheim and operates worldwide through 140 subsidiaries and employs over 46 people. employees. The most important research areas of Boehringer Ingelheim International GmbH are: respiratory diseases, cardiovascular diseases, HIV, thromboembolism and cerebrovascular diseases.

What is venous thrombosis and how does it manifest itself? Check: Thrombosis

Pradaxa – composition and action of the drug

The active substance of Pradaxy is dabigatran etexilate.

dabigatran is an anticoagulant drug that is a direct thrombin inhibitor. In order to understand the mechanism of action of dabigatran, it is necessary to take a closer look at the blood clotting process. The process is very complex and multi-stage, with the stages following one after the other. At the moment of vessel damage, platelets stick to its walls in the area of ​​the damage. In the next stage, they stick together, creating a hemostatic plug, which may initially inhibit the outflow of blood from the vessel. However, this plug is unstable and must be made stronger in order to be effective in stopping blood loss. Strengthening occurs as a result of the production of fibrin, which creates extensive networks strengthening the plug made of platelets. As a result of these processes, a platelet-fibrin clot is formed.

What is it about action of dabigatran? First of all, it should be remembered that this compound is a prodrug and therefore has no pharmacological activity. However, it requires transforming it into an active form. The active metabolite is formed from a prodrug molecule by enzymatic hydrolysis in plasma and liver. Dabigatran is a thrombin inhibitor. Inhibiting thrombin helps to prevent the formation of blood clots by preventing the conversion of fibrinogen to fibrin. Dabigatran also inhibits free thrombin, fibrin-associated thrombin, and fibrin-induced platelet activation. The strength of the anticoagulant effect is proportional to the plasma concentration of dabigatran.

After oral administration of Pradaxa, the active substance is rapidly and completely converted to dabigatran. After surgery, absorption may be slower on the day of surgery, and the maximum concentration is usually obtained within 6 hours after oral administration. In the days following surgery, the maximum concentration of dabigatran is obtained within 2 hours after taking the preparation. Dabigatran is excreted 85% in the urine, mainly as unchanged drug and 6% in the faeces.

Auxiliary components of the drug Pradaxa includes a filler and a shell of the capsule as well as black ink for printing on the capsule.

Excipients in the capsule filling:

1. tartaric acid;
2. acacia gum;
3. hypromeloza;
4. dimetykon 350;
5. talk;
6. hydroksypropyloceluloza.

Excipients in the capsule shell:

1. karagen;
2. potassium chloride;
3. titanium dioxide;
4. indigo carmine;
5. sunset yellow;
6. hypromeloza;
7. Purified Water.

Excipients in black printing ink:

1. winds;
2. n-butyl alcohol;
3. isopropyl alcohol;
4. methylated ethanol;
5. black iron oxide;
6. Purified Water;
7. propylene glycol.

If you want to learn more about the properties and effects of dabigatran, read on: Dabigatran – an anticoagulant drug

Pradaxa – indications for the use of the drug

Indications for the use of Pradaxa are:

1. prevention of venous thromboembolic complications in adults after elective total knee or hip arthroplasty (primarily a dose of 75 mg);
2. prevention of strokes and systemic embolism in adults with non-valvular atrial fibrillation with one or more risk factors such as: previous stroke or transient ischemic attack, heart failure NYHA class II or higher, age 75 years or older, diabetes or high blood pressure (predominantly 110 mg dose in all);
3. treatment of deep vein thrombosis and pulmonary embolism and prevention of recurrence of deep vein thrombosis and pulmonary embolism in adults (mainly the dose of 150 mg).

What is an endoprosthesis? Check: Knee and hip prosthesis

Pradaxa – contraindications to the use of the drug

Pradaxa, despite its effectiveness in combating the risk of blood clots, cannot be used by every patient struggling with this type of condition.

Contraindications to the use of the drug Pradaxa are:

1. allergy and pre-existing allergic reactions to the active substance of the drug or to any of the excipients;
2. diagnosed with severe renal failure; 
3. active, clinically significant bleeding;
4. lesions or disease states of any organ, which may constitute a significant risk factor for major bleeding;
5. increased bleeding tendency, both congenital and of unknown cause or caused by the medications used;
6. the presence of severe liver problems or liver disease that may be fatal;
7. taking orally ketoconazole, itraconazole, cyclosporine, dronedarone;
8. concomitant therapy with any other anticoagulants – warfarin, rivaroxaban, apixaban, heparin or heparin derivatives, except in special circumstances;
9. an artificial heart valve postoperative condition requiring anticoagulant therapy;
10. age of the patient – the drug should not be used in children and adolescents under 18 years of age;
11. the period of pregnancy and breastfeeding.

How to recognize and treat thrombosis? Check: Thrombosis – causes, treatment and prevention. The six most common symptoms of thrombosis [EXPLAIN]

Pradaxa – precautions

Before and during the use of PRADAXA, follow the precautions included in the package leaflet.

Precautions to keep in mind include:

1. some illnesses may prevent you from taking this medicine or may require you to change the dosage of Pradaxa;
2. overt and latent bleeding, as well as haematological disturbances may occur during the use of PRADAXA. You should monitor your health and consult your doctor immediately of any worrying symptoms, such as low blood pressure, weakness, pallor or shortness of breath;
3. if you experience heavy bleeding without delay, consult your doctor;
4. people weighing less than 50 kg, with moderate renal impairment, concurrently using glycoprotein inhibitors, are at risk of increased dabigatran concentration in the blood;
5. report the simultaneous use of drugs that inhibit platelet aggregation, non-steroidal anti-inflammatory drugs, drugs that inhibit serotonin reuptake and other drugs that affect haemostasis;
6. be especially careful in patients with diseases or procedures associated with the risk of bleeding;
7. patient’s age – over 75 years of age;
8. the patient should remain under careful medical observation throughout the treatment period;
9. in people using the preparation, INR determinations (normalized coefficient characterizing the blood coagulation process) should not be performed, because the obtained results will not be reliable;
10. Before a planned surgical or dental procedure, consult your doctor and inform him that you are taking dabigatran.
11. in patients after surgery, treatment with dabigatran should be resumed as soon as possible, if the clinical situation allows it and the achieved haemostasis;
12. due to the lack of data, it is not recommended for use in people operated on for a fracture of the neck of the femur;
13. the drug should be used with caution in people with liver disease, which may be prone to bleeding;
14. the preparation is not recommended for patients with thrombosis diagnosed with antiphospholipid syndrome;
15. the efficacy and safety of the preparation has not been established in patients with active neoplastic disease and deep vein thrombosis or pulmonary embolism;
16. the medicine should not be used after the expiry date which is stated on the carton. The expiry date refers to the last day of that month;
17. this medicine should not be disposed of via wastewater or household waste. It’s best to ask your pharmacist how to dispose of medicines you no longer use.

What should you know about proper drug storage? Check: Medications that are stored wrongly are poisonous

Pradaxa – correct dosage

Always use Pradaxa exactly as described in the package leaflet or as directed by the doctor or pharmacist.

Pradaxa is only to be used by adult patients. This preparation can be taken with or without food. Pradaxa capsules should be taken orally and whole, without chewing them, with a glass of water, as they are easier to transport to the stomach. Under no circumstances should you open the capsules and consume substances directly from them, as this increases the risk of side effects in the form of bleeding.

Also, the capsules should not be pushed through the blister foil, and the foil should not be peeled off until a capsule is needed. If the medicine is contained in a bottle, the bottle should be tightly closed immediately after removing the capsule.

The dosage of the drug depends on the ailment for which the prescription was issued.

Dosage of Pradaxa in preventing venous thromboembolism after orthopedic surgery:

1. in patients after elective knee replacement surgery, treatment should begin 1-4 hours after the end of the procedure. The first dose is 1 capsule containing 110 mg of the active ingredient. Maintenance treatment should begin the day after surgery. Then, 220 mg of the drug is administered daily in 2 capsules of 110 mg. The recommended duration of maintenance treatment is 10 days;
2. in patients undergoing hip replacement surgery, treatment is started within 1 – 4 hours after surgery from a single dose of 110 mg. The next day, switch to the 220 mg maintenance dose, i.e. 2 capsules of 110 mg per day. The duration of the maintenance treatment is 28-35 days.

If complete haemostasis is not achieved after surgery, Pradaxa should not be started. If it is postponed to a day later than the day of the operation completion, the administration of Pradaxy should be started with 2 capsules of 110 mg once a day.

Some patients should be given PRADAXA in lower doses than indicated in this package leaflet. These are patients who have been diagnosed with moderate renal impairment who are taking concomitant verapamil, amiodarone or quinidine and have reached the age of over 75 years. In these cases, postoperative treatment should commence 1-4 hours after surgery with 1 capsule of 75 mg, and from the first day after surgery, use a maintenance dose of 150 mg, i.e. 2 capsules of 75 mg once a day. The duration of treatment should be the same as for the rest of patients: 10 days for a knee replacement and 28-35 days for a hip replacement.

Dosage of Pradaxa for the prevention of stroke and systemic embolism in patients with atrial atrial fibrillation and risk factors for stroke, and for the treatment and prevention of recurrent deep vein thrombosis and pulmonary embolism:

1. patients are recommended to take 300 mg Pradaxa daily divided into 2 doses of 150 mg;
2. long-term intake of the preparation in the prevention of stroke in atrial fibrillation;
3. in the treatment and prophylaxis of recurrences of deep vein thrombosis and pulmonary embolism, the drug should be introduced after the administration of parenteral anticoagulant for a minimum of 5 days, and the duration of treatment is determined by the doctor individually; 
4. the longer duration of use of the drug applies to people with constant risk factors, and the shorter duration of at least 3 months is used for temporary risk factors, such as a recent injury, surgery or immobilization.

Patients 80 years or older or who are taking verapamil at the same time should take lower doses of Pradaxa. It is recommended that the dose of Pradaxa is reduced to 220 mg per day in 2 doses of 1 110 mg capsule.

Lower doses of Pradaxa should also be considered in patients:

1. aged between 75 and 80;
2. with moderate renal impairment;
3. with gastritis;
4. with inflammation of the esophagus mucosa;
5. with gastroesophageal reflux;
6. with an increased risk of bleeding. 

If you miss a dose of Pradaxy, it can be taken up to 6 hours before the next scheduled dose. If the remaining time is not sufficient, do not make up for the missed portion. Under no circumstances should a double dose be taken. If you take more than the prescribed dose of Pradaxa, there is an increased risk of bleeding.

How to take medication correctly? Check: How to take medications effectively?

Pradaxa – side effects of using the drug

Pradaxa, like any other drug, may cause side effects in patients. It is important to report any suspected adverse reactions after authorization of the medicinal product so that the benefit / risk balance of the medicinal product can be monitored.

The frequency classification of adverse body reactions (ADRs) is based on the following principles: very common (≥1 / 10), common (≥1 / 100 to <1/10), uncommon (≥1 / 1 to <000/1), rare (≥ 100 / 1 to <10 / 000), very rare (<1 / 1), not known (cannot be estimated from the available data).

Due to the frequency of side effects, the following are indicated:

1. very common side effects of Pradaxa (more than 1 in 10 people): bleeding e.g. from the nose, stomach or intestines, penis / vagina or urinary tract, bleeding under the skin, decreased number of red blood cells in the blood, stomach or stomach pain, indigestion, frequent passing loose or liquid stools, nausea;
2. uncommon side effects of Pradaxa (may affect up to 1 in 100 patients): bleeding, bleeding may occur from lumps in the rectum, into the brain, hematoma formation, coughing up blood or blood in the sputum, decrease in the number of platelets in the blood, decrease in hemoglobin in the blood, blood reaction allergic, sudden change in color or appearance of the skin, itching, ulcer in the stomach or intestines (including ulceration of the esophagus), inflammation of the esophagus and stomach, regurgitation of food from the stomach into the esophagus (reflux), vomiting. difficulty swallowing, abnormal laboratory tests for liver function
3. rare side effects of Pradaxa (may affect up to 1 in 1000 people): bleeding may occur in a joint, from a surgical incision, from a wound, from an injection site or from the site of a catheter into a vein, severe allergic reactions which cause difficulty in breathing or dizziness, serious allergic reactions causing swelling of the face or throat, skin rash of dark red raised itchy lumps due to an allergic reaction, reduction in the number of red blood cells in the blood, increase in liver enzymes, yellowing of the skin or whites of the eyes due to liver or blood problems.

PRADAXA may also cause side effects, the frequency of which is unknown. These side effects include:

1. difficulty breathing or wheezing;
2. decrease in the amount of hemoglobin in the blood (a substance in red blood cells);
3. decrease in the number of red blood cells in the blood;
4. yellowing of the skin or whites of the eyes caused by liver or blood problems.

Do you know what an artery is and what role it plays in the human body? Read: Artery – what it is and what role it plays in the human body

Pradaxa and pregnancy and breastfeeding

The use of any medications or dietary supplements during pregnancy requires consultation with the attending physician. If you are pregnant or breastfeeding, think you may be pregnant or are planning to have a baby, ask your doctor or pharmacist for advice before taking Pradaxa.

Pradaxa should not be used during pregnancy. This is only allowed in cases of absolute necessity. Women of childbearing potential who are under treatment with dabigatran should make every effort not to become pregnant until the end of treatment.

Animal studies have shown that the active substance in Pradaxa has effects on female fertility. At the same time, it causes a decrease in the body weight of fetuses, reduces their survival rate, increases mortality and increases the risk of developmental defects. Pradaxa capsules had no effect on fertility in males. Due to the above test results, the drug should not be used in pregnant women.

For women who are breastfeeding, wean the baby first before taking PRADAXA. You must not breast-feed while taking PRADAXA.

What is worth knowing about proper supplementation during pregnancy? Check: Conscious choices. Diet and supplementation in pregnancy

Pradaxa – interactions with other drugs

Before starting treatment with Pradaxa, please inform your doctor or pharmacist about all the medicines you are taking or have recently taken. You should also inform what medications the patient plans to take in the near future.

The active substances in Pradaxa may interact with other medicines and the substances contained in medicinal products. First of all, you should not take PRADAXA together with:

1. P-glycoprotein inhibitors e.g. ketoconazole, dronaderone, itraconazole, cyclosporine, tacrolimus – increase the concentration of dabigatran;
2. drugs increasing the activity of P-glycoprotein e.g. rifampicin, St. John’s wort, carbamazepine, phenytoin – increase the concentration of dabigatran;
3. protease inhibitors e.g .: ritonavir – can either lower or increase dabigatran levels;
4. verapamil, amiodarone, quinidine, clarithromycin, ticagrelor, posaconazole – may cause a risk of increased levels of dabigatran;
5. acetylsalicylic acid;
6. non-steroidal anti-inflammatory drugs;
7. clopidogrel;
8. antidepressants from the group of serotonin, serotonin and norepinephrine reuptake;
9. other drugs that may interfere with haemostasis.

Which drugs should never be combined with each other? Check: Dangerous interactions

Pradaxa — dinner

Dinner at Pradaxa may differ depending on the city in which the preparation will be purchased or the pharmacy chosen by the patient. The price of the product also depends on the amount of active substance contained in the capsule.

It should be noted that the packaging of the preparation containing 10 and 30 capsules has been reimbursed and is free for people over 75 years of age, regardless of the dose of the active substance in the capsule. In addition, the packages of Pradaxa 75 mg 10 and 30 pieces and Pradaxa 110 mg 10 and 30 pieces have a lower flat-rate price for people after arthroplasty procedures. In the case of the hip joint, it is due up to 30 days after the procedure, and in the case of the knee joint – up to 14 days. The versions of Pradaxa 110 mg and 150 mg in packs of 30 are reimbursed in 30% for adults in the treatment and prevention of recurrence of deep vein thrombosis or pulmonary embolism.

In addition to the reimbursement of the price of Pradaxa are as follows:

1. Pradaxa 75 mg: 10 capsules cost around PLN 50, and 30 capsules around PLN 130;
2. Pradaxa 110 mg: 10 capsules cost about PLN 45, 30 capsules around PLN 130, and 60 capsules around PLN 200;
3. Pradaxa 150 mg: 30 capsules cost around PLN 130, and 60 capsules around PLN 160. 

How much money does the average Pole spend on treatment? Check: The Pole does not have a doctor’s appointment