Anticoagulant Xarelto for the treatment and prevention of thrombosis and PE

Xarelto is a direct-acting anticoagulant. This group of drugs, promotes suppression of blood clotting activity and prevents thrombogenesis, due to the reduced formation of fibrin.

They affect the biosynthesis of certain elements of the body, allowing to change the viscosity of the blood, which leads to inhibition of coagulation processes.

Anticoagulant Xarelto is allowed to be used with both therapeutic and prophylactic purposes.

Components of the drug

The tablet of the Xarelto preparation is biconvex, round in shape, covered with a pink-brown filmth shell.

Each contains:

• micronized rivaroxaban - the main active agent;
• as additional elements is present: microcrystalline cellulose, magnesium stearate, croscarmellose sodium, hypromellose 5cP, lactose monohydrate, sodium lauryl sulfate;
• tablet shell consists of: iron hypromellose 15cR, macrogol 3350, red oxide E172, titanium dioxide E171.

Pharmacological profile of

Xarelto is classified as a highly selective direct factor Xa inhibitor that is bioavailable when ingested, that is of primary importance in the coagulation cascade.

A study involving a test group confirmed the existence of a dose-dependent inhibition of X-factor activity by rivaroxaban, an active active substance of Xarelto, it was found that it increases APTT( partial thromboplastin activation).

Indicators may differ if Neoplastin® or HepTest® is used for analysis. The device data are taken in seconds, since the INR is calibrated and validated solely for coumarins, therefore it is inadmissible to use other anticoagulants.

Like all direct anticoagulants Xarelto exert direct influence on thrombin to reduce its activity. The drug is an inhibitor of thrombin, prothrombin deactivators, due to which they functionally delay the development of thrombus formation.

The drug quickly affects the body, it is well absorbed into the digestive system, with blood flow reach the liver, and together with the urine go outside, having its therapeutic effect.

To whom the medicine is necessary, and to whom it is forbidden

The medicine Xarelto is prescribed in such cases:

• prophylactic therapy of venous thrombosis and thromboembolism after operative intervention on the lower extremities, orthopedic;
• threat of stroke;
• prophylaxis of systemic thromboembolism, including pulmonary artery, risk of recurrence of DVT and PE.

List of contraindications:

• individual susceptibility to the main active or other constituent substances of the remedy;
• bleeding is clinically significant( gastrointestinal, intracranial, internal);
• diagnosed liver disease accompanied by coagulopathy, and possible bleeding risks;
• for children and adolescents, the drug is contraindicated until age 18.

Dosage and application chart for

Xarelto in a dosage of 15 or 20 mg is taken orally once a day, during meals. The recommended daily dosage is 20 mg.

Patients with moderate renal impairment( creatinine clearance is below 50-30 mL / min) the desired daily dose is 15 mg.

For orthopedic surgery, Xarelto is prescribed at a dosage of 1 table / 10 mg per day. A drug containing 10 mg can be taken, regardless of food intake.

Duration of treatment:

• hip joint surgery - 5 weeks;
• operation of the knee joint - 2 weeks.

The primary dose should be taken within 6-10 hours after the operation, when reaching the hemostasis.

If the next dose was not drunk in a timely manner, the patient should take the pill immediately, the next method should be taken at the usual time.

Individual patient groups

There is no need to adjust the dosage of Xarelto depending on the age of the patient( over 65 years), body weight, gender.

Clinical data on the use of the drug in childhood and adolescence are not available.

No efficacy and safety indicators have been established for this age group of patients, for this reason the drug is not recommended until age 18.

Because of the increased risk of internal bleeding, as well as on the basis of available laboratory results about the possibility of rivaroxaban penetrating through the placental barrier, Xarelto is contraindicated in the treatment of pregnant women.

During lactation, taking the drug is also unfavorable, since the main active substance is secreted into breast milk. Prescribe treatment with this drug can only be after stopping breastfeeding.

Cases of overdose

Overdose Xarelto is capable of provoking complications of hemorrhagic nature, which is directly related to the pharmacodynamic features of the drug.

There have been several cases of overdose of rivaroxaban up to 600 mg, which did not lead to bleeding or any other negative responses. Because absorption is limited, a rapid saturation process is anticipated, which will not be accompanied by a further increase in the total value of the medical substance in plasma, if hyperthermia dosages amounting to 50 mg or more are consumed.

Specific antidote for today is not found, in an overdose situation, use activated charcoal to reduce the absorption of rivaroxaban.

Specific recommendations of

In the course of treatment with a drug containing rivaroxaban, it is not necessary to keep a record of blood clotting indices, but, like other antithrombotic drugs, Xarelto should be used prudently to treat patients prone to risk of bleeding.

Among them, special attention to patients with:

• congenital or acquired tendency to bleeding;
• severe uncontrolled hypertension;
• recently suffered, or having, a stomach or duodenal ulcer, located in a recurrent phase;
• vascular retinopathy;
• recently occurred intracranial hemorrhage;
• pathology of cerebral vessels;
• postoperative period from surgical intervention on the eyes, brain or spinal cord.

Drug compatibility with alcohol

The use of the drug is categorically unacceptable along with the use of alcoholic beverages, under the threat of development of undesirable consequences.

If renal and hepatic function is impaired

When administration of the drug to patients with renal insufficiency is mild( KK 80-50 ml / min) or moderate( KK <50-30 ml / min) form, the daily average dose can not be reduced.

Restrictions are necessary in severe cases( QC & lt; 30-15 ml / min), in such cases the dosage of rivaroxaban is selected individually. Not recommended in patients with a KK <15 ml / min.

As mentioned above, the use of the drug is contraindicated in liver diseases that are aggravated by coagulopathy. In the case of other pathologies of this organ, no changes in dosage are required.

Drug Interaction

Caution is necessary when taking medications that affect hemostasis( NSAIDs, platelet aggregation inhibitors), including anti-thrombotic drugs.

Erythromycin, Clarithromycin, Fluconazole may lead to a change in the concentration of rivaroxaban, although this is provided in the order of variability of the standards, and accordingly are not clinically significant.

There is an opinion of

Reviews of patients, as well as attending physicians about the drug Xarelto.

Doctors and ordinary people agree on the effectiveness of the drug, but, as in most other cases, it is necessary to prescribe the dosage with caution, individually assessing the patient's condition, various factors that can affect blood coagulability.

In pharmacy

Storage of tablets is recommended in dark places, with a temperature below 30 ° C.Shelf life of the drug is 3 years. Keep away from children.

Through the pharmacy network is sold exclusively on the prescription, the price for Xarelto in the RF at the time of writing the article is proposed in the table.

The market also has a structural analogue of Xarelto and a cheaper drug - Rivaroxaban, its price for a package of 14 tablets varies within two thousand rubles.