One of the drugs, which belongs to the pharmacological group of anticoagulant drugs, is the drug "Xarelto". This drug inhibits factor Xa, and it, in turn, is a component of the prothrombin activator and one of the components that ensure timely blood coagulation (Xarelto analogs also have these properties).
To date, many vain attempts have been made to withdraw a drug that will have a similar effect and at the same time have a minimum of side effects. After numerous laborious efforts, a worthy analogue appeared - the drug "Pradaxa". This medicine is the only substitute that can be fully used instead of Xarelto. Its characteristics are almost identical to the above, the only difference is the content of the active substance, which is rivaroxaban in both drugs.
Pharmacodynamics
All analogues of "Xarelto" have a similar effect. The only thing they differ in is a quantitative and qualitative indicator of side effects. The only worthy analogue of this drug, which has a similar effect with it, is the drug "Pradax".
This drug and its Russian counterpart “Xarelto” are direct highly selective drugs that slow down the action of factor Xa, that is, inhibit it. This drug has high bioavailability when administered orally, therefore, the enteral route of administration for it is the main.
The central role in the cascade of the coagulation system is played by the activation of factor X followed by the biotransformation of factor Xa using the internal and external coagulation pathways.
Indications
As a rule, Xarelto analogues and the drug itself are used in the following situations:
- Prevention and prevention of stroke.
- Prevention and relief of systemic embolism.
(In such cases, this drug is indicated for patients with atrial fibrillation, which is of non-valve origin.)
- Elimination or prevention of clogging of deep veins with blood clots.
- Prevention of relapse of pulmonary embolism.
The drug "Pradax", which is an analogue, is also indicated for the prevention of venous thromboembolic complications in patients who underwent surgery to replace one of the joints of the lower limb.
Contraindications
Any Russian analogue of “Xarelto” has the following contraindications (they may differ, but only to a small extent):
- hypersensitivity or the risk of allergic reactions to substances contained in this drug;
- active bleeding, which have significant informational content during a clinical examination (for example, intracavitary bleeding or cerebral hemorrhage);
- situations in which there is an increased risk of volume bleeding, for example, with active ulcerative processes in the gastrointestinal tract;
- drug therapy with drugs that have similar properties - preventing coagulation;
- when using non-fractional heparin in the dosage necessary for the satisfactory functioning of the catheter;
- various liver diseases, the development of which can provoke bleeding of various etiologies;
- absolutely all Xarelto analogues are contraindicated in patients with renal failure occurring in any phase;
- lactose intolerance, insufficient galactose content in the body;
- pregnancy and lactation;
- there is also an age limit of 18+ for this drug and various Xarelto analogs.
The category of people who can take this drug with caution and under the supervision of a specialist
With caution and under the supervision of a doctor, it is recommended to use the "Xarelto" instructions for use (analogues also) in the following cases:
- treating patients who are at increased risk for bleeding;
- recent ulcer diseases with a predisposition to relapse;
- treatment of renal failure of varying degrees in combination with drugs that increase the content of rivaroxaban in the patient's body;
- patients who are treated with drugs that can increase hemostasis;
- drugs that can increase the level of rivaroxaban, for example, antifungal drugs of the azole group;
- this drug and the analogue of the Xarelto tablets are contraindicated in patients with HIV infection if they took various protease inhibitors of this virus shortly.
Pregnancy and lactation
To date, it has not been precisely established how “Xarelto”, analogues of the drug, affect the effectiveness and safety of treatment in pregnant women.
The experiments that were conducted on animals in laboratories demonstrated the pronounced toxicity of the active substance of this drug on the body of the future mother, since the drug leads to pronounced reproductive toxicity of the female body.
According to laboratory findings, the drug "Xarelto", an analogue that is similar to it in pharmacological action, has the ability to penetrate the placenta, therefore this drug is contraindicated.
Also, during the use of Xarelto, women should not forget about effective contraceptive measures, since the conception that accompanies the course of this drug can adversely affect the fetal development.
There are currently no objective judgments about how the use of this drug affects the lactation period, but laboratory studies in experimental animals suggest that the active substance, rivaroxaban, has the ability not to metabolize and excreted in breast milk. Therefore, at the time of breastfeeding, it is worth abandoning the use of this drug.
Based on the data provided by laboratory studies, it can be said that rivaroxaban does not affect the ability of a sexually mature organism to create viable offspring in rats, but no experiments have been conducted on humans of this kind.
Metabolism and excretion routes
With enteral administration, there are three ways of excretion, which correspond to a third of the total amount of non-metabolized drug:
- excretion with urine;
- excretion with feces;
- excretion by direct excretion of the kidneys (in this case, the substances are practically not metabolized and excreted unchanged).
Biotransformation of rivaroxab is carried out through mechanisms that are independent of the cytochrome system.
The main metabolic pathways are the oxidation of the morpholine group and also the decomposition of amide bonds with water.
In vitro studies suggest that rivaroxaban is the basis for P-glycoprotein and protein, which provides resistance to breast cancer.
As a rule, excretion of metabolites is carried out for 5-9 hours.
Side effects
As the instructions for use say to the drug: Xarelto analogues or the drug itself should be taken only as directed by the doctor. The instruction itself describes in detail the dosage of the drug or its analogues. Be sure to read the instructions before admission!
Below are reflected all the undesirable processes and reactions that had the drug "Xarelto" analogues. The price of tablets is from 900 rubles. This is inexpensive, given that most side effects are exceptions to the rule.
- Side effects that were observed when checking the circulatory and lymphatic systems are anemia and thrombocythemia, which are rare.
- Tachycardia is the only adverse reaction when taking this drug.
- Hemorrhage.
These are indications of contraindications to the drug "Xarelto" instruction.
Analogues of this drug can cause disturbances in the digestive tract: bleeding, localized pain, dyspeptic manifestations, and sometimes - dry mouth.
Due to the introduction of rivaroxaban, local reactions can be observed: fever, swelling at the injection site with the parenteral method, weakness and malaise.
The occurrence of these processes contribute to the drug "Xarelto" analogues. The price of this drug, as a rule, is standard for all pharmacy chains.
Dosage and administration
Detailed information on the correct intake can be provided by absolutely any instruction for the Xarelto preparation. Analogues of this drug in this regard are not fundamentally different.
This drug is available in tablet form, so the pill is taken by the enteral route. If for some reason the patient cannot swallow the tablet, it can be crushed and mixed with a suitable liquid (tea, water).
After taking this drug, a meal should immediately follow.
Overdose
If the “Xarelto” intake is not observed, an overdose is possible, which, as a rule, is treated symptomatically, since this drug does not have a specific antidote.
In order to reduce the adsorption of this drug in the small intestine, any sorbent, for example, activated carbon, can be used. Also, for the speedy elimination of metabolites, it is necessary to ensure forced diuresis, which is carried out using large amounts of fluid and the use of diuretics.
Prices
Depending on the manufacturer, the price of the drug "Xarelto" ranges from 899.00 rubles. for 10 tablets, which contain 10 mg of active substance, up to 1740.49 rubles.
A pack of 30 tablets can be purchased for 3,300.00 rubles.
The largest package contains 100 capsules, its cost is 8600 rubles.
The pricing policy of the drug "Pradax" depends on the quantitative content of the active substance in one capsule:
- 75 mg - 716.00 rubles;
- 110 mg - 1,574.00 rubles;
- 150 mg - 1676.00 rubles.