Description

Pharmacological action

PRADAXA – dabigatran etexilate is a low molecular weight prodrug that does not have pharmacological activity. After oral administration, it is rapidly absorbed and by hydrolysis catalyzed by esterases, turns into dabigatran. Dabigatran is an active, competitive, reversible direct thrombin inhibitor and has an effect mainly in plasma.

Since thrombin (serine protease) converts fibrinogen into fibrin during the coagulation cascade, inhibition of its activity prevents the formation of a thrombus. Dabigatran inhibits free thrombin, fibrin-binding thrombin and thrombin-induced platelet aggregation.

In vivo and ex vivo in animal studies using various models of thrombosis demonstrated the antithrombotic efficacy and anticoagulant activity of dabigatran after intravenous administration and dabigatran etexilate after oral administration.

A close correlation was found between the concentration of dabigatran in plasma and the severity of the anticoagulant effect. Dabigatran lengthens activated partial thromboplastin time (APTT).

Indications

Prevention of venous thromboembolism in patients after orthopedic surgery.

Contraindications

Known hypersensitivity to dabigatran or dabigatran etexilate or to one of the excipients.

Patients with severe renal failure (creatinine clearance less than 30 ml / min).

Hemorrhagic disorders, patients with hemorrhagic diathesis, patients with spontaneous or pharmacologically induced hemostasis.

Active clinically significant bleeding.

Dysfunction of the liver and liver disease that may affect survival.

Concurrent administration of quinidine.

Organ damage due to clinically significant bleeding, including hemorrhagic stroke, within the previous 6 months before starting therapy.

Patients are under 18 years old.

Special instructions

Risk of developing hemorrhages: Unfractionated heparin can be used to maintain the functioning of a central venous or arterial catheter.

Should not be used simultaneously with PRADAXA®: unfractionated heparins or its derivatives, low molecular weight heparins, fondaparinux sodium, desirudin, thrombolytic agents, GPIIb / IIIa receptor antagonists, clopidogrel, ticlopidine, dextran, sulfinpyrazone and vitamin K. antagonists

The combined use of PRADAX® in doses recommended for the treatment of deep vein thrombosis and acetylsalicylic acid in doses of 75-320 mg increases the risk of bleeding. There is no evidence of an increased risk of bleeding associated with dabigatran when taking PRADAX® in the recommended dose for patients receiving small doses of acetylsalicylic acid in order to prevent cardiovascular diseases. However, the available information is limited, therefore, with the combined use of low dose acetylsalicylic acid and PRADAXA®, it is necessary to monitor the condition of patients with the goal of

timely diagnosis of bleeding.

Close monitoring (for symptoms of bleeding or anemia) should be carried out in cases in which there may be an increased risk of hemorrhagic complications: – A recent biopsy or trauma.

– The use of drugs that increase the risk of hemorrhagic complications. The combination of PRADAXA® with drugs that affect hemostasis or coagulation processes.

– Bacterial endocarditis

Short-term administration of NSAIDs when used together with PRADAXA® for analgesia after surgery does not increase the risk of bleeding. Limited data are available on the systematic administration of NSAIDs with a half-life of less than 12 hours in combination with PRADAXA®, there is no evidence of an increased risk of bleeding.

Renal failure: pharmacokinetic studies have shown that in patients with impaired renal function, including associated with age, there was an increase in the effectiveness of the drug. In patients with moderately reduced renal function (creatinine clearance of 50-30 ml / min), it is recommended to reduce the daily dose to 150 mg per day. PRADAXA® is contraindicated in patients with severe impairment of renal function (creatinine clearance Spinal anesthesia / Epidural anesthesia / Lumbar puncture: In the case of traumatic or repeated spinal puncture and prolonged use of an epidural catheter, the risk of developing cerebrospinal bleeding or epidural hematoma should not be taken. earlier than 2 hours after removal of the catheter, such patients should be monitored for the possible detection of neurological symptoms.

Effect on the ability to drive mechanisms

The effects of dabigatran etexilate on the ability to drive vehicles and drive mechanisms have not been studied.

Composition

1 caps.: – dabigatran etexilate mesylate 172.95 mg, respectively. dabigatran etexilate 150 mg

Excipients: acacia gum – 8.86 mg, tartaric acid (coarse-grained) – 44.28 mg, tartaric acid (powder) – 59.05 mg, tartaric acid (crystalline) – 73.81 mg, hypromellose – 4.46 mg, dimethicone – 0.08 mg, talc – 34.31 mg, hyprolose (hydroxypropyl cellulose) – 34.59 mg.

Capsule shell composition: carrageenan (E407) – 0.285 mg, potassium chloride – 0.4 mg, titanium dioxide (E171) – 5.4 mg, indigo carmine (E132) – 0.054 mg, sunset sunset yellow (E110) – 0.004 mg, hypromellose (hydroxypropyl methylcellulose) – 79.35 mg, purified water – 4.5 mg.

Composition of black ink Colorcon S-1-27797: shellac 52.5%, butanol 6.55%, ethanol denatured (methylated alcohol) 0.65%, dye iron oxide black (E172) 33.77%, isopropanol 3.34%, propylene glycol 1.25%, purified water 1.94% .

Dosage and administration

Inside, with food or on an empty stomach, washed down with water

Special instructions for removing capsules from

blister Remove capsules from blister, peeling foil Do not squeeze the capsules through the foil. Remove the foil so that it is convenient to remove the caps

Adults

Prevention of venous thromboembolism (BT) in patients after orthopedic surgery

The recommended dose is 220 mg once daily (2 capsules, 110 mg each).

Side effects

Disorders from the hematopoietic and lymphatic systems: anemia, thrombocytopenia.

Immune system disorders: hypersensitivity reactions, including urticaria, rash and itching, bronchospasm.

Disorders of the nervous system: intracranial bleeding.

Vascular disorders: hematoma, bleeding.

Disorders of the respiratory system, chest and mediastinum: nosebleeds, hemoptysis.

Gastrointestinal disorders: gastrointestinal bleeding, rectal bleeding, hemorrhoidal bleeding, abdominal pain, diarrhea, dyspepsia, nausea, ulceration of the gastrointestinal mucosa, gastroesophagitis, gastroesophageal reflux disease, vomiting, dysphagia.

Disorders from the hepatobiliary system: increased activity of “hepatic” transaminases, impaired liver function, hyperbilirubinemia.