Active substances

Rivaroxaban

Chemical name

(S) -5-chloro-N- {2-oxo-3-4- (3-oxomorpholine-4-yl) phenyloxazolidine-5-ylmethyl} thiophene-2-carboxamide

Chemical properties

Rivaroxaban belongs to the group of oral anticoagulants, direct inhibitors Ha factor. This substance was developed by German pharma. by Bayer. The molecular weight of the chemical compound = 435.8 grams per mole. The drug is released in the form of tablets in a film enteric coating.

Pharmachologic effect

Anticoagulant.

Pharmacodynamics and pharmacokinetics

In the process of blood coagulation, the key factor is the coagulation factor of Stuart-Prauer, its activation is carried out by internal and external tenase. Normally, this factor (coagulation factor Xa), together with the non-enzymatic cofactor Va and calcium ions, forms on the surface platelet count specific prothrombinase complex. As a result of the complex formation process, the transformation process is activated prothrombin at thrombin. Thrombin, in turn, is responsible for the polymerization of fibrinogen dissolved in plasma and the formation of a blood clot (blood clot). Rivaroxaban, however, selectively inhibits the coagulation factor Xa, which leads to a suspension of thrombus formation.

In the human body, a dose-dependent inhibition of factor Xa is observed. It is noteworthy that during treatment with this tool there is no need to periodically monitor blood coagulation indicators. During clinical studies of elderly patients, no prolongation of the QT interval was observed with a decrease in IPT.

After taking tablets in a dosage of 10 mg, the bioavailability of the drug reaches 90%. The substance is rapidly and almost completely absorbed, reaching its maximum concentration within 2-4 hours, after taking the tablets.

The medicine does not change its pharmacokinetic parameters while taking it with food. Also, the variation coefficient, depending on the organism, is from 30 to 40%.

The process of absorption of the drug depends on the place of its release in the gastrointestinal tract. There is a noticeable decrease of 30-50% in the maximum concentration and AUC, compared with the whole tablet, if the active substance is released in the ascending colon or distal small intestine.

The degree of binding of the agent to plasma proteins is about 92-95%, mainly the substance binds to albumin. Approximately 0.6% of the dose taken is metabolized by CYP3A4 isoenzymes, CYP2J2. The oxidation of the morpholine group and the hydrolysis of amide bonds occur. Metabolites and unchanged Rivaroxaban is excreted by renal tubular secretion and with feces.

Distortions in pharmacokinetic parameters in elderly patients are observed. Plasma concentration is slightly higher than in young people. Also, dosage adjustment may be needed for various deviations in the functioning of the liver or kidneys.

Indications for use

The medicine is prescribed:

  • for prevention venous thromboembolism in patients undergoing extensive orthopedic surgery on the lower extremities;
  • at deep vein thrombosis and pulmonary embolism;
  • as a prophylactic (may happen stroke) in patients with atrial fibrillation non-valve origin.

Contraindications

The drug is contraindicated in taking:

  • at allergies on the active substance;
  • patients with clinically significant bleeding;
  • if the patient has recently suffered stomach ulcer, injury or surgery of the brain or spinal cord, cerebral hemorrhage;
  • sick with aneurysms vessels or cerebrovascular pathology;
  • in the presence of malignant neoplasms with a high risk of bleeding;
  • with the parallel reception of others anticoagulants;
  • patients with liver failure and coagulopathy;
  • with kidney disease, if the QC is less than 15 ml per minute;
  • pregnant women
  • under the age of 18;
  • during lactation.

Particular care is recommended to observe:

  • in the treatment of patients with an increased tendency to bleeding;
  • at renal failure.

Side effects

The mechanism of action of the substance suggests that the use of this drug may be accompanied by bleeding from any organ or tissue, which as a result can lead to the development of posthemorrhagic anemia. Depending on the severity, duration, and organ in which the bleeding occurred, the symptoms and severity of the side effect will vary significantly. The possibility of a fatal outcome cannot be ruled out. So, in people taking drugs in parallel that affect hemostasis or in patients with uncontrolled severe arterial hypertensionThe risk of bleeding is higher. Symptoms of this adverse reaction: weakness, pallor, dizziness, headaches and asthenia.

Also during treatment with the drug often develop:

  • nausea, rising levels LDH;
  • level up AAT, amylases, blood bilirubin, Alkaline phosphatase or lipases.

Less common are:

  • allergic reactions to the skin, itching and rashes, hives;
  • allergic dermatitis, tachycardialowering blood pressure;
  • hemorrhage, hematomas;
  • gum bleeding hemetemesis;
  • rectal bleeding, hematuria;
  • bleeding from the nose, discharge mixed with blood from the genitals;
  • fatigue, swelling;
  • fever and general weakness, thrombocytopenia;
  • headaches, dizziness, pain in the legs and arms;
  • level increase ureaand creatinine.

Rarely may occur:

  • abdominal pain constipation, diarrhea;
  • discomfort in the digestive tract, indigestiondryness of the oral mucosa;
  • vomiting, impaired liver function;
  • level increase conjugated bilirubin.

Rivaroxaban, instructions for use (Method and dosage)

The tablets are taken orally during meals. The schedule and duration of treatment depends on the type of orthopedic intervention.

Instructions for Rivaroxaban

If the patient has problems swallowing the whole tablet, it can usually be crushed and mixed with water or a neutral liquid diet. After taking the medicine, you must immediately eat something. It is also allowed the introduction of the drug using a gastric tube.

The standard dosage is 10 mg. Reception is carried out once a day.

For prophylaxis stroke and systemic thromboembolism in patients with atrial fibrillation take 20 mg of the drug once a day. In case of impaired renal function, it is recommended to adjust the daily dosage to 15 mg. The treatment is long, determined by the attending physician.

If the patient forgot to take the next dose of the drug, then you need to drink a pill immediately. The next day, medication is taken at the usual time. Do not drink a double dose.

In the treatment and prevention Tela and DVTIt is recommended to take 15 mg of the drug, 2 times a day for 3 weeks. Then the transition to a single dose, 20 mg of the drug. The maximum daily dosage in the first 3 weeks is 30 mg, during subsequent treatment - 20 mg. The duration of treatment is from 3 months, depending on the condition of the patient and the effectiveness of the therapy.

If you skip the next dose, if the daily dosage is 30 mg, they can be taken at a time.

In severe renal failure and liver failure, dosage adjustment may be required. During the transition from Rivaroxaban to other anticoagulants or, conversely, a dosage adjustment may also be required. Consultation of the attending physician is required.

Overdose

Taking up to 600 mg of the drug at a time is rarely accompanied by the development of bleeding or other undesirable side reactions.

The medicine does not have a specific antidote. In case of overdose, gastric lavage and administration are indicated. activated carbon, hemodialysis ineffective.

If the patient developed bleeding during therapy, then there is no need to take the next dose of the medicine. Treatment is carried out individually, depending on the severity and location of the bleeding. If necessary, mechanical compression, infusion therapy, surgical hemostasis, red blood cell mass, fresh frozen plasma, etc. can be performed. If the above methods are unsuccessful, it is recommended to appoint specific procoagulants.

Interaction

Intake of this substance and CYP3A4 isoenzyme inhibitors and R-glycoprotein may lead to an increase in AUC of rivaroxaban.

The use of this substance and clarithromycin at a dosage of 1 g per day leads to an increase in the plasma level of Rivarobaxan, however, a change in the pharmacokinetic parameters is not clinically significant.

The simultaneous use of the drug with antifungal agents of the azole series ketoconazole or erythromycin causes an increase in the maximum plasma concentration by almost 2 times, and the remaining pharmacodynamic effects also increase.

Medication with HIV protease inhibitors ritonavira causes an increase in anticoagulant max.

The effectiveness of the drug decreases under the influence of rifampicin - strong inductor CYP3A4 and P-glycoprotein. Also has such an effect. carbamazepine, phenobarbital, phenytoinHypericum preparations.

Drug combination with enoxaparin(dosage of 40 mg) is acceptable and does not lead to a distortion of the pharmacokinetic parameters of both agents.

No drug interaction was found with clopidogrelhowever, during clinical trials, a significant increase in bleeding time was observed with this combination of lek. funds.

With extreme caution, this substance should be combined with naproxen. Depending on the individual characteristics of the body, patients may experience an increase in bleeding time.

At a dosage of 10 mg per day, the drug can be taken both during meals, and separately from it.

Due to the insufficient number of clinical studies, it is not recommended to combine this drug with dronedarone.

The medicine has an effect on laboratory blood coagulation indicators, such as APTTV, PV, PTI and results Heptest.

Terms of sale

You must have a prescription from a doctor.

Storage conditions

Pills are stored in a cool place, away from light and small children.

Shelf life

3 years.

Special instructions

It is highly not recommended to take the drug by people who have kidney failure, and the level of QC is at least 15 ml per minute.

It is also recommended that particular care be taken during the treatment of persons suffering from moderate renal failure, while taking drugs that affect the pharmacokinetics of the drug.

Strict monitoring of the patient's condition should be carried out if he has severe renal failure or is taking antifungal drugs of the azole group or HIV protease inhibitors. In this case, it will be possible to timely identify hemorrhagic complications that may develop during treatment.

When combining this substance with NSAIDs, platelet aggregation inhibitors, antithrombotic agents or drugs that affect hemostasiscaution is recommended.

If during the course of the drug there was a need for an invasive procedure or operation, the medication should be stopped one day before the intervention, in accordance with the doctor’s recommendation.

The question of using an epidural catheter or urgent surgery should be decided by the attending physician.

For children

In pediatric practice, the drug is not used.

With antibiotics

When combined with some antibiotics, it is necessary to adjust the dosage or completely replace the drug.

During pregnancy and lactation

The medicine is contraindicated during lactation and during pregnancy.

Preparations that contain (Rivaroxaban Analogs)

Matches for ATX Level 4 code:Arikstra

The structural analogue of Rivaroxaban is a drug Xarelto.

Reviews

Reviews about the use of this drug are mostly good. With prolonged use, on the recommendation of a doctor, the medicine helps resorption of blood clots and normalizes the work of the cardiovascular system. Adverse reactions are rare. The only thing that patients complain about in the reviews is the high cost of the drug. The tool often begins to be taken as an alternative to the known analogue. Warfarin.

Rivaroxaban price, where to buy

The price of Rivaroxaban in the form of a drug Xarelto, film-coated tablets are about 900-1500 rubles per 10 tablets of 10 mg each. Tablets with a dosage of 15 mg can be purchased at a price of 1350 rubles for 14 pieces.

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