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Pharmacodynamics and pharmacokinetics

Pharmacodynamics

Inhibitor of factor Xa, a key protein that plays a role in blood clotting. To realize the effect of the active substance, the presence of antithrombin III . Inhibits platelet . As a result of the drug's action , prothrombin time aPTT and the formation of blood clots is prevented. If the drug is used in a therapeutic dose, then changes in these indicators are insignificant.

The use of Eliquis is indicated in the treatment of venous thrombosis and for the prevention of thromboembolism in patients with atrial fibrillation , as well as after endoprosthetics of lower extremity joints. During therapy, there is no need to constantly determine its concentration in the blood. The decision to continue treatment is made after testing anti-FXa activity.

Pharmacokinetics

Rapidly absorbed into the gastrointestinal tract. Bioavailability is 50%. Cmax is determined 3–4 hours after administration. For doses of 2.5 mg and 10 mg, the pharmacokinetics are linear. When taken at a dose of more than 25 mg, there is a decrease in absorption and a decrease in bioavailability. Communication with human blood proteins 87%. Metabolized by the isoenzyme CYP3A4/5 . About 25% of the dose is excreted through the intestines.

If renal function is impaired, Cmax in the blood does not change. There were also no significant changes in pharmacodynamic parameters when taking 5 mg of the drug in patients with mild to moderate liver failure. Studies have not been conducted in patients with severe liver failure. Elderly people experience higher concentrations of the active substance in the blood. In patients weighing 120 kg, the concentration in the blood is 30% lower than in patients weighing up to 85 kg.

Mechanism of action of Eliquis

The main active ingredient of the drug is apixaban. The mechanism of action of the active substance is the inhibition of blood clotting factor. That is why the drug is often used to treat and prevent venous thromboembolism, and is also prescribed as a prophylactic agent during knee or hip replacement surgeries.

Apixaban is a direct-acting anticoagulant. It selectively blocks the active center of a special enzyme Xa, thereby preventing the synthesis of thrombin and the formation of blood clots. The maximum activity of the drug is observed when the highest concentration in the blood plasma is reached. During the use of the drug, there is no need to regularly monitor the anticoagulant effect.

Eliquis is available in tablet form. After oral administration, the active component is quickly absorbed from the gastrointestinal system. The maximum amount of the drug in the blood is recorded after approximately 3-4 hours. Eating does not affect the rate of absorption of the active substance. The bulk of the drug is excreted through the intestines. The half-life does not exceed 12 hours.

Contraindications

• active bleeding;
• hypersensitivity;
• liver disease accompanied by a risk of bleeding;
• renal dysfunction;
• pregnancy;
• lactation;
• age up to 18 years.

Prescribed with caution during spinal puncture , epidural anesthesia , while taking inhibitors of the CYP3A4 isoenzyme ( Ketoconazole , voriconazole , Itraconazole ). The risk of bleeding increases with congenital bleeding disorders, thrombocytopenia and hemorrhagic stroke , exacerbations of peptic ulcer disease , and when used simultaneously with NSAIDs .

Side effects

Common adverse reactions:

• nausea;
• anemia;
• bleeding during surgery.

Rarely encountered adverse reactions:

• arterial hypotension;
• thrombocytopenia;
• hypersensitivity;
• hemorrhages in the eye tissue, rectal bleeding, hemoptysis, nasal and gingival bleeding;
• muscle hemorrhage;
• hematuria.

Eliquis, instructions for use (Method and dosage)

Eliquis tablets are taken orally. The dosage depends on the disease.

After planned endoprosthetics, Eliquis 2.5 mg is prescribed twice a day and started 12 hours after the intervention. The duration of treatment is 38 days for hip replacement and 14 days for knee replacement.

For atrial fibrillation - 5 mg 2 times a day. Weight up to 60 kg and age 80 years - 2.5 mg twice a day.

In the treatment of DVT and PE - 7 days, 10 mg 2 times a day, subsequently - 5 mg twice.

To prevent relapses of PE and DVT , take 2.5 mg 2 times a day for 6 months.

Interaction

Combination with Ketoconazole (inhibitor of the CYP3A4 isoenzyme and P-glycoprotein ) leads to an increase in Cmax by almost 1.6 times, but no dose adjustment is required. The drugs Diltiazem , Amiodarone , Naproxen , Quinidine , Verapamil lead to an increase in the concentration of the active substance, but to a lesser extent (1.3-1.4 times). Dose adjustment is also not required.

Use with Rifampicin (inducer of the CYP3A4 isoenzyme ) leads to a decrease in Cmax of the active substance in the blood by 42%. The same effect should be expected when combined with phenytoin , phenobarbital and carbamazepine . in the treatment of PE and DVT .

When enoxaparin and apixaban are used together, an enhanced effect on FXa . significant interaction with acetylsalicylic acid was observed in healthy individuals.

The combination with Clopidogrel and acetylsalicylic acid does not lead to an increase in bleeding time and the parameters of the coagulation system remain the same as with apixaban monotherapy. However, such a triple combination of drugs is contraindicated in patients with acute coronary syndrome and concomitant diseases. In atrial fibrillation, the triple combination also leads to the risk of bleeding.

It is not recommended to use Heparin or its derivatives, fondaparinux , desirudin , Dipyridamole , sulfinpyrazone , dextran vitamin K antagonists and thrombolytic drugs due to the risk of bleeding.

clinically significant interaction with Atenolol and Famotidine was identified. However, combination with Atenolol is accompanied by a decrease in Cmax of apixaban. In studies, apixaban did not affect the pharmacokinetics of naproxen and digoxin .

pharmachologic effect

Manufacturer: Pfizer, USA
Release form: film-coated tablets

Active ingredient: Apixaban

Eliquis has an anticoagulant effect by blocking a special enzyme, factor Xa, which promotes blood clotting and prevents blood clots.

This property of Eliquis is relevant not only for thrombosis, but also for endoprosthetics, when in response to the entry of a foreign body into the body, which is a prosthesis, blood clots are reflexively formed at the site of tissue damage as a protective reaction.

Analogs

Level 4 ATC code matches:
Xarelto

• Warfarin
• rivaroxaban
• Xarelto
• Dabigatran
• Pradaxa
• Edoxaban

Analogs are cheaper than Eliquis: Warfarin , the cost of which is much lower even taking into account INR tests (80-100 rubles for 50 tablets) and Dabigatran .

The cheapest analogues of Eliquis

All of the Eliquis substitutes listed above, although they are cheaper than the drug described, still have a high cost. If it is impossible to purchase expensive drugs, the attending physician will select a drug with an even lower price. Below is a list of inexpensive Eliquis synonyms, as well as analogues of cheaper Russian and foreign production:

All of these drugs should be used with caution in patients with diagnosed pathologies of the liver and kidneys. Elderly patients may require dose adjustment.

Eliquis reviews

Venous, arterial and cardiac thrombosis , thromboembolism are an important medical problem. About 10% of patients diagnosed with thromboembolism are at risk of another episode, which can be fatal. It is in such situations that this drug is prescribed, which has shown good results in reducing the risk of systemic embolism, especially in patients with concomitant congestive heart failure, a stroke , impaired renal function, as well as in the elderly.

Moreover, taking the drug is associated with a significantly lower risk of bleeding when compared with Warfarin , rivaroxaban or vitamin K . For example, the latter block the formation of many coagulation factors, while new direct anticoagulants, which include Eliquis, block only one stage of coagulation. Unlike Warfarin, they interact less with medications and their doses are easily adjusted.

This drug is convenient to use - a fixed dose twice a day every day without the need for laboratory monitoring. This is important for patients with atrial fibrillation who require lifelong anticoagulation to prevent cardioembolic stroke . Here are some reviews from patients who use this drug.

• “... Left ventricular fibrillation, atrial fibrillation. I was prescribed this drug, and so far I’m tolerating it well.”
• “... I take Eliquis 5 mg twice a day (prescribed by a cardiologist after stenting). There is a burning sensation in the stomach after taking it.”
• “...I have a permanent form of atrial fibrillation, the tachysystolic variant. In addition to other medications, I also take Eliquis 5 mg 2 times a day. I feel normal."

One of the complications of direct anticoagulant therapy is bleeding. To reduce its risk, it is necessary to reduce the period of antithrombotic therapy: up to 12 months after acute coronary syndrome and up to 6 months after stenting with a covered stent.

Popular analogues of Eliquis

Eliquis is an effective and quite expensive drug. A package of 60 tablets costs more than 2,500 rubles. That is why patients have to look for a replacement for the prescribed drug. Below are the most common and cheaper analogues of the described drug.

Anticoagulant Warfarin

This domestic drug is also an anticoagulant, but unlike Eliquis, it is of indirect action. It is used for the prevention of ischemic stroke when a patient is diagnosed with atrial fibrillation. Prescribed as a prophylactic agent to prevent the development of thromboembolism and thrombosis. Can be used in combination with antiplatelet agents.

Treatment begins with a minimum dose of 2.5 mg per day. Next, under the control of blood parameters, the optimal dosage is selected. However, tests are required every 30 days to prevent bleeding.

The drug is not prescribed to pregnant, lactating women, children, as well as patients with a predisposition to bleeding.

Xarelto

The new generation anticoagulant Xarelto is also available in tablet form in dosages of 2.5, 10, 15 and even 20 mg. The treatment is a course, the drug is used once a day. The main advantage of the drug is that there is no need for regular monitoring of blood counts. The drug is prescribed for the treatment and prevention of ischemic strokes and other complications in patients with fibrillation.

Recommended use in patients before heart valve replacement to prevent thromboembolism and thrombosis.

Xarelto reduces the risk of developing myocardial infarction and reduces the likelihood of death due to cardiac pathologies.

Side effects sometimes occur when taking the drug. These include the risk of bleeding, hemorrhage in various systems and organs, thrombocytopenia, and allergic reactions. Contraindications for use are the same as for other anticoagulants.

Pradaxa

The active ingredient of the drug is dabigatran etexilate. It is used to prevent thromboembolism in patients after various orthopedic operations, as well as in patients with atrial fibrillation. Double use of the drug is required. Quite quickly after administration, the drug blocks blood clotting factor Xa, preventing blood clots.

During treatment, negative side reactions develop. Among the most common: disorders of the kidneys, liver, anaphylactic shock, angioedema, dyspeptic disorders. Discontinuation of the drug is required before surgery.

Edoxaban

The drug is prescribed when necessary to reduce the risk of developing stroke and pre-stroke conditions, as well as systemic embolism in patients with diagnosed non-valvular fibrillation. The drug is also indicated for deep vein thrombosis and pulmonary embolism. Prescribed 5-10 days after taking a course of treatment with parenteral anticoagulants.

The safety of the drug has not been studied in patients with mechanical valves.

The recommended daily dosage is 60 mg orally as a single dose. In patients with a creatinine clearance of 15-50 ml/min, the daily dose is halved. When Edoxaban is discontinued in patients with non-valvular fibrillation, there is a risk of developing ischemic events.

Therefore, patients should be prescribed adequate alternative therapy with other anticoagulants. During spinal anesthesia while using the drug, there is a possibility of hematoma and, as a consequence, prolonged paralysis.

Dabigatran etexilate

The drug is intended for the prevention of systemic venous thromboembolism in patients in the postoperative period during joint replacement. It is used to prevent stroke conditions, systemic thromboembolism, and reduces the risk of death as a result of cardiovascular diseases. Helps with recurrent deep vein thrombosis.

The drug should be prescribed with caution to elderly patients (over 75 years of age), as well as when a moderate decrease in creatinine clearance is diagnosed. For congenital defects of the blood coagulation system, dose adjustment is required. Not used during pregnancy and childhood.

Eliquis price, where to buy

Where to buy Eliquis? You can purchase it in the pharmacy chain of the Russian Federation. The cost of 60 tablets of 5 mg in Moscow pharmacies ranges from 2,400 rubles. The same number of Eliquis tablets in St. Petersburg can be purchased for about 2,500 rubles.

• Online pharmacies in RussiaRussia
• Online pharmacies in UkraineUkraine

ZdravCity

• Eliquis tab.
  p/o captivity. 2.5 mg 20 pcs. Bristol-Myers Squibb/Pfizer Manufacturing Deutschland GmbH RUB 829 order
• Eliquis tab. p/o captivity. 5 mg 60 pcs. Bristol-Myers Squibb/Pfizer Manufacturing Deutschland GmbH

  RUB 2,548 order

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• Eliquis tab. p/o film.5mg No. 60 Pfizer Ireland Pharmaceutical

  RUB 2,475 order

• Eliquis tab. p/o captivity. 5mg 20pcs Pfizer Ireland Pharmaceuticals/Pfizer Manufacturing Deutschland

  840 rub. order

• Eliquis tab. p/o captivity. 5 mg 20 pcs. Bristol-Myers Squibb/Pfizer Manufacturing Deutschland GmbH

  RUB 836 order

Pharmacy Dialogue

• Eliquis tablets 5mg No. 20Bristol Myers

  860 rub. order

• Eliquis tablets 2.5 mg No. 60Bristol Myers

  RUB 2,519 order

• Eliquis (tab.p.pl/vol.5mg No. 20) Pfizer Ireland Pharmaceuticals

  RUB 897 order

• Eliquis tablets 5mg No. 60Bristol Myers

  RUB 2,427 order

• Eliquis tablets 2.5 mg No. 20Bristol Myers

  RUR 827 order

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Pharmacy24

• Eliquis 5 mg No. 60 tablets Bristol-Myers Squibb Company, USA/Bristol-Myers Squibb S.r.l..Italy
  1931 UAH.order
• Eliquis 2.5 mg No. 20 tablets Bristol-Myers Squibb Company, USA/Bristol-Myers Squibb S.r.l..Italy

  622 UAH. order