Methotrexate for rheumatoid arthritis: instructions for use

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  • 1"Methotrexate" for rheumatoid arthritis: reviews. Instructions for use, description of the preparation
    • 1.1Composition and principle of action
    • 1.2Forms of the preparation
    • 1.3Indications for taking "Methotrexate"
    • 1.4Who should not take the medicine?
    • 1.5Possible side effects
    • 1.6Dosing regimen of tablets
    • 1.7Injections of Methotrexate
    • 1.8Exceeding the permissible dose
    • 1.9Interaction with other substances and preparations
    • 1.10Special instructions
    • 1.11Price range
    • 1.12Consumer opinion
  • 2Methotrexate for rheumatoid arthritis: instructions for use, side effects, analogs, as well as reviews of doctors and patients
    • 2.1Rheumatoid arthritis: the risk of disease
    • 2.2Rheumatoid arthritis - video
    • 2.3Methotrexate: drug efficacy and therapeutic effects
    • 2.4Composition of the drug and its pharmaceutical forms
    • 2.5Security is the main thing
    • 2.6Restrictions in use
    • 2.7Interaction with other means
    • 2.8Adverse reactions and intoxication
    • 2.9Instructions for use of methotrexate in rheumatoid arthritis
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    • 2.10Medication analogues
    • 2.11Table: The basic drugs used in the treatment of rheumatoid arthritis
    • 2.12Analogues of Methotrexate - photo gallery
    • 2.13Opinions of specialists about the preparation
    • 2.14Patient Reviews
    • 2.15Methotrexate - videoinstruction
  • 3Methotrexate in the treatment of rheumatoid arthritis: instructions for use, side effects, analogs + reviews of doctors and patients
    • 3.1Rheumatoid arthritis is a disease requiring effective therapy
    • 3.2Methotrexate - the mechanism of action of the drug
    • 3.3Forms and composition of the preparation
    • 3.4Composition of Methotrexate depending on the dosage form - table
    • 3.5Instructions for use
    • 3.6Contraindications to the use of the drug
    • 3.7Interaction with other drugs
    • 3.8Features of use of the drug during pregnancy and breastfeeding
    • 3.9Possible side effects
    • 3.10Than you can replace Methotrexate
    • 3.11Analogues of Methotrexate - table
    • 3.12Medications prescribed for rheumatoid arthritis - gallery
    • 3.13The opinion of doctors about the drug
    • 3.14Treatment of rheumatoid arthritis - video
    • 3.15Patients who took Methotrexate

"Methotrexate" for rheumatoid arthritis: reviews. Instructions for use, description of the preparation

Rheumatoid arthritis, if translated literally from Greek, indicates a state of inflammation. The question of what factors provoke the development of this disease is still unclear.

Indirect information that the number of leukocytes in the blood increases and the speed increases erythrocyte sedimentation (ESR), makes it possible to conclude that the development of the disease has an infectious nature.

There is an opinion that the impetus for the development of the disease is an infection that provokes irregularities in the functioning of the immune system. However, not all are affected, but only those with hereditary predisposition.

The result of the introduction of this infection in the human body is the formation of immune complexes (from viruses, antibodies, etc.), which accumulate in the tissues and lead to damage to the joints.

In most cases, the treatment of this formidable disease is to alleviate pain, slow the process the course of the disease and the restoration of lesions (as far as possible in each case) with the help of surgical methods.

There are a lot of drugs for treatment at present. One of these is Methotrexate.

With rheumatoid arthritis (reviews of health workers and patients confirm this information), this medication is effective enough, the results of its influence will be felt for a long time.

Composition and principle of action

The main active ingredient of the drug is methotrexate. It is a nitostatic, a folic acid antagonist.

Currently, to slow the development of rheumatoid arthritis, treatment with Methotrexate is used more often than other methods.

In essence, this medicine is an antitumor, cytostatic agent, inhibits mitosis (indirect cell division), slows the growth of actively proliferating tissues, inhibits development tumors.

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According to statistics, the effectiveness of the medication is observed in 80% of patients, the positive dynamics become noticeable in 2-6 weeks after the start of the course of therapy.

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After a long time of treatment (up to 5 years), therapy with Metotraxatom is canceled much less frequently than any other medication used to slow the development of rheumatoid arthritis.

Forms of the preparation

The medication itself is a Russian analogue of the Austrian Methotrexate Ebove. The original drug manufacturer offers its customers in several forms of release.

Tablets are on sale in three dosages: mg, 5 mg and 10 mg of the main active ingredient. All of them are packed in polypropylene bottles of 50 pieces each.

In addition, Methotrexate (Austria - the manufacturer), can be purchased as a solution for injection at a dosage of 50 mg / 5 ml. Ampoules are made of dark glass and packed in a cardboard box.

It is also possible to buy a medication in the form of a concentrate for the preparation of infusions (droppers). Dosage - 100 mg / 1 ml. In this form, "Methotrexate" is sold in vials of 5, 10, 50 ml. One bottle is packed in a cardboard box.

Indications for taking "Methotrexate"

Indication for the use of the medication is quite specific, since its main purpose is to fight against neoplasms.

It is recommended to take "Methotrexate" in cases where the patient suffers from acute lymphoblastic leukemia and non-Hodgkin's lymphomas.

It is also prescribed for trophoblastic tumors, mushroom mycosis and psoriasis (in severe stages).

Also, if other treatments and medicines do not have a significant effect, use Methotrexate in rheumatoid arthritis. Comments of experts-rheumatologists about the medicine are quite positive.

Indications for taking "Methotrexate Ebewe" are somewhat more extensive.

Specialists prescribe it if the patient has malignant neoplasms of various systems and organs: lung cancer and breast, osteosarcoma and soft tissue sarcoma, ovarian and testicular tumors, Jung's sarcoma, retinoblastoma and autoimmune disease.

Who should not take the medicine?

It is inadmissible to take the drug to people with increased sensitivity to the main active ingredient. Contraindicated taking "Methotrexate" pregnant women and nursing mothers.

Do not prescribe the drug with existing abnormalities in the liver and kidneys, with hematologic disorders (anemia, thrombocytopenia, leukopenia).

Do not start treatment with medication for patients in the acute stage of any infectious diseases that suffer from immunodeficiency syndrome.

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Both the Russian analogue and the original "Methotrexate" (Austria) are inadmissible to give children up to three years.

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With a number of diseases, the drug is administered with great care.

Such problems include ulcers of the stomach and duodenum, ulcerative colitis, dehydration of the body.

When viral, fungal and bacterial infections also act very carefully. To the same group of problems carry previously conducted radiation or chemotherapy.

Possible side effects

"Methotrexate" in ampoules, in tablets, with infusions can cause a number of side effects. Sufficiently serious problems can arise from the hemopoietic system (leukopenia, thrombocytopenia, etc.)

) and gastrointestinal tract (dyspepsia, anorexia, hepatotoxicity, pancreatitis). The nervous system can respond with headaches, drowsiness, paresis, convulsions. High doses of medication can trigger the development of encephalopathy.

There may be deviations from the organs of vision and the cardiovascular system (hypotension, pericarditis, thromboembolism).

May develop respiratory failure, chronic obstructive pulmonary disease, shortness of breath, dry, unproductive cough, fever.

On the part of the genitourinary system, there is a possibility of severe forms of nephropathy or kidney failure.

Possible a violation of spermatogenesis and oogenesis, a decrease in libido, the development of infertility, impotence.

If a woman is pregnant, Methotrexate (injections, pills, droppers) can cause miscarriage, developmental defects, or fetal death.

Dosing regimen of tablets

When treating malignant neoplasms, the pill regimen is developed individually and depends on the chemotherapy schedule.

If we are talking about the use of the drug "Methotrexate" in rheumatoid arthritis (reviews of patients are positive), then the initial dose is usually, mg once a week.

You can take the entire dose at once, but you can divide it into 3 doses with a 12-hour interval.

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In some cases (achieving the optimal effect), a weekly dose can be increased. However, it should not exceed 20 mg.

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When the necessary clinical effect is achieved, the dosage should be gradually reduced to a minimum.

The optimal period of the course of therapy was not clinically detected.

Injections of Methotrexate

And how do injections with the drug "Methotrexate"? Injections with rheumatoid arthritis start to do with dosages, mg per week. This can be done subcutaneously, intramuscularly or intravenously.

If the drug is well tolerated by the patient, the dose can be gradually increased weekly to, mg, but not more than 25 mg.

When the therapeutic effect is achieved (usually 1-2 months after the start of treatment), the dose should be gradually reduced to the minimum required.

For any patient with rheumatoid arthritis, dosage can be gradually adjusted to maintain the optimal effect of treatment. Clinical studies have shown that "Methotrexate" is better absorbed and gives a minimal number of adverse reactions if injections are done subcutaneously or intramuscularly.

With the continuous admission of Methotrexate, the initial positive therapeutic effect persists for two years. With the withdrawal of medication, rheumatoid arthritis manifests itself in 3-6 weeks.

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Exceeding the permissible dose

Exceeding the permissible dose of a Russian medication or a medicine "Methotrexate Ebove" (tablets, injections, infusions) does not manifest itself with any specific symptoms. The fact of overdose can be established by the level of methotrexate concentration in blood plasma.

Treatment consists in immediate (optimally in the first hour) application of the antidote, which is calcium folinate. The volume of the injected substance should be equal to or greater than the dose of "Methotrexate".

Additionally doses of calcium folinate can be prescribed by a doctor as needed. Before you enter each of the following doses, and then every 6 hours throughout the process of eliminating overdose symptoms with an antidote, you must determine the pH of the urine.

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Such measures will minimize the likelihood of developing nephropathy.

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Also in the necessary set of measures to eliminate the effects of an overdose of medicines include hydration and alkalinization of urine. These procedures will accelerate the excretion of methotrexate.

Interaction with other substances and preparations

If the patient has gout and the appointment of medicines "Methotrexate" or "Methotrexate Ebove the dose of antidiagnostic drugs must be adjusted.

Parallel application of salicylates, phenylbutazone, phenytoion, sulfonamides, a number of certain antibiotics (tetracycline, penicillin, chloramphenicol), anticoagulants of indirect influence and lipid-lowering medication can lead to severe intoxication, up to the deadly outcome.

Large volumes of "Methotrexate" in parallel with NSAIDs can cause death from severe hematologic and gastrointestinal intoxication. The combination of NSAIDs and low doses of the drug under consideration can reduce the excretion of the latter by the renal tubules.

Hepatotoxic medicines (based on sulfasalazine, azathioprine, ethanol) increase the risk of hepatotoxicity, hematotoxic - hematotoxicity of Methotrexate. Parallel drug administration and radiotherapy procedures can provoke bone marrow suppression.

Special instructions

Before you start treatment with a drug "Methotrexate" (injections, tablets are used - it is not important), it is necessary to conduct a general analysis of blood (to know the level of platelets), biochemistry (determine the values ​​of liver enzymes, albumin, bilirubin), to make a chest radiograph cells. In addition, it is necessary to investigate the work of the kidneys, in some cases tests for hepatitis and tuberculosis will not be superfluous.

In order not to miss the moment of intoxication development, it is necessary to control the composition of peripheral blood (quantity platelets and leukocytes), kidney function, hepatic transaminase activity, uric acid level in blood serum.

Before each use of Methotrexate, the mucosa of the mouth and throat should be checked for ulcers.

The process of bone marrow hematopoiesis should be checked at the beginning of therapy, once during the course of treatment and after its termination.

Price range

The form of the release (tablets, injections) and dosage are the main factors influencing the cost of the drug "Methotrexate".

The price of packing tablets (50 pcs.) With a dosage, mg can range from 240 to 250 rubles. The same number of tablets with a dose of 5 mg can be purchased for a sum of 390 to 420 rubles. Packaging of the drug with the highest dosage (10 mg) will cost the buyer 530-550 rubles.

Solution for injections is much more expensive, and the spread of prices is much wider. For example, 5 ampoules of medication with a dosage of 50 mg / 5 ml in some pharmacies can cost about 1200-1300 rubles, in others - , 00 rubles.

Consumer opinion

There are both positive and negative opinions of patients about the drug "Methotrexate".

With rheumatoid arthritis, the reviews were mostly fixed in a positive direction (about 80% of patients experienced efficacy in the first 1 months after the start of treatment).

However, you can often hear about the negative effect of the medication on the patient's body, on the development of side effects of varying severity and on the part of different systems and organs.

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To minimize the negative impact, Methotrexate should be prescribed exclusively by the attending physician, and he must develop a treatment regimen and choose an effective dose.

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A source: http://.ru/article/192510/metotreksat-pri-revmatoidnom-artrite-otzyivyi-instruktsiya-po-primeneniyu-opisanie-preparata

Methotrexate for rheumatoid arthritis: instructions for use, side effects, analogs, as well as reviews of doctors and patients

According to doctors, to treat rheumatoid arthritis with Methotrexate is necessary for every patient in the absence of contraindications. Therapy should begin at the earliest stages of the pathology. What is so unique about this drug?

Rheumatoid arthritis: the risk of disease

The exact causes of the disease are still unknown. According to indirect data, this pathology develops against the background of an increase in the number of leukocytes in the blood of the patient, as well as the rate of erythrocyte sedimentation (ESR). Everything speaks of the infectious nature of the process in the joints.

The affected joint with rheumatoid arthritis becomes inflamed, which is accompanied by pain and local fever

It is believed that the disease is the result of an infectious lesion that causes immunity in people with hereditary predisposition.

At the same time, immune complexes are formed in the human body (from antibodies, viruses and other microorganisms) that settle on tissues, leading to damage to the joints.

Ineffectiveness of treatment of rheumatoid arthritis (arthrosis) with antibiotics indicates the reliability of this assumption.

Rheumatic, or rheumatoid, arthritis has a characteristic feature only of it - the symmetry of inflammation. The disease affects the peripheral joints:

  • wrists;
  • hips;
  • feet;
  • elbows;
  • shoulders;
  • knees;
  • fingers.

The development of pathology is characterized by a stable inflammation of the synovial fluid in the joints and cartilaginous tissue.As a result, they deform and erode bones. There were recorded cases when the inflammation spread to other organs:

  • a heart;
  • lungs;
  • organs of the digestive tract;
  • nervous system.

For the first time rheumatoid arthritis can manifest itself after heavy physical exertion, psychoemotional shock state (stress), overwork, during the period of hormonal shift, the impact of various adverse factors, serious infectious diseases.

Rheumatoid arthritis undergoes several stages in its development

Rheumatoid arthritis is characterized by a high degree of disability (up to 70%).In addition, withThere is a risk of death from the disease, which is associated with infectious complications and the emergence of kidney failure in the absence of the necessary treatment.

Rheumatoid arthritis - video

Methotrexate: drug efficacy and therapeutic effects

Treatment of rheumatoid arthritis focuses on the removal of pain, inhibition of the development of pathology and recovery appeared lesions with the help of surgical intervention (replacement of joints for prosthesis or excision of synovial shell). The basis of basic therapy is often the drug Methotrexate.He is able to eliminate symptoms of the disease, prolonging the time of remission.

Methotrexate is an effective and inexpensive agent prescribed for rheumatoid arthritis

The drug is aimed at increasing joint mobility and eliminating inflammation.At the same time, the quality of life of the patient improves and the working capacity is maintained.

In the early stages of the disease, Methotrexate is able not only to alleviate the condition of the patient, but also to stop the further development of rheumatoid arthritis.

Composition of the drug and its pharmaceutical forms

The basis of this drug is the active substance methotrexate. Refers to potent antitumor drugs (a group of antimetabolites - structural analogues of folic acid).

The substance itself in its pure form is a crystalline powder of yellow-orange color, insoluble in water, while the light-resistant and hygroscopic material:

  • Suppresses the synthesis of DNA, RNA and protein;
  • inhibits the growth of various neoplasms, including cancer;
  • has teratogenic properties - it has a cytotoxic effect on the human body.

The drug Methotrexate in the pharmaceutical market is represented by various manufacturers. The medicine is produced in different forms:

  • concentrate for solution for infusion (in vials and ampoules);
  • solution ready for intravenous and intramuscular injection;
  • coated tablets (up to 10 mg);
  • substance-powder.

Concentrate and substance-powder for the preparation of solutions are used only in inpatient medical institutions. In the pharmacy, according to the prescription of the doctor, only preparations ready for use are realized.

Methotrexate in the form of an injection solution is used for intramuscular, intravenous, intraarterial and intrathecal administration

Solution for injection - a transparent liquid of yellowish color. In addition to the active substance, it contains the following auxiliary components:

  • sodium hydroxide;
  • sodium chloride;
  • distilled water for injection.

Tablets for oral administration (through the mouth) of the application are coated with a film-quick-dissolving coating of yellow or yellow-orange color. In addition to methotrexate, they include:

  • lactose monohydrate;
  • povidone;
  • modified potato starch;
  • calcium / magnesium stearate.

To make the shell use:

  • sugar;
  • polyethylene glycol;
  • polyvinyl alcohol;
  • talc;
  • titanium dioxide;
  • food colors.

In the concentrate for the preparation of a solution for infusion, water and sodium hydroxide are used as additional components. This preparation is a dense transparent liquid of brownish-yellow color.

Concentrate for the preparation of a solution for infusions is a dense transparent liquid of brownish-yellow color

Substance-powder for the preparation of a solution is a lyophilized powdered preparation of a yellow-brown color. There are no preservatives in its composition. Additional binder components:

  • sodium chloride;
  • sodium hydroxide.

Security is the main thing

Methotrexate is a serious chemical-pharmaceutical preparation, which by its action is equated to chemotherapy.He is able to exert a strong influence on the whole organism. For safety, it is necessary to conduct monthly blood tests, monitoring its composition.

Restrictions in use

There are a number of limitations on the use of Methotrexate. Its use is strictly prohibited in the presence of the following diseases in patients:

  • chronic kidney and liver diseases;
  • allergies to the components of the drug;
  • peptic ulcer disease;
  • leukopenia;
  • anemia;
  • HIV;
  • acquired immunodeficiency;
  • hemorrhagic leukemia;
  • thrombocytopenia.
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In addition, the drug is prohibited for children under the age of three, as well as during pregnancy and lactation.

With caution, you should use the drug in the adolescent period.

Other features:

  1. It is recommended to avoid contact with persons who received a vaccine against poliomyelitis. To limit contact with strangers during treatment, a special bandage on the face should be worn.
  2. Accuracy requires the use of sharp objects in everyday life, since accidental cuts can cause serious bleeding in the background of the use of Methotrexate.
  3. During the period of therapy, dental and dental procedures are undesirable, since there is a risk of bleeding and bleeding gums.
  4. Strictly prohibited simultaneous use of alcohol and drugs, which is associated with increased negative effects on the liver.This is especially pronounced in patients suffering from various liver diseases and metabolism (obesity, diabetes).
  5. Due to the influence of the drug on the central nervous system during therapy, it is desirable to abandon the management of vehicles and potentially dangerous mechanisms.

Interaction with other means

Methotrexate can interact with other medications and dietary supplements, because of what appears the likelihood of a toxic effect on the patient's body, or, conversely, effectiveness. It is impossible to use simultaneously with this medicine:

  • non-steroidal anti-inflammatory drugs;
  • corticosteroids;
  • barbiturates;
  • antibiotics of tetracycline and penicillin series;
  • Acyclovir.

Adverse reactions and intoxication

If the product is used improperly or because of the individual characteristics of the patient's body, a number of side effects may occur.

Among the possible reactions of the body to the drug are the following:

  1. From the nervous system and sensory organs:
    • encephalopathy (especially when multiple doses are administered intrathecally, as well as in patients after brain irradiation);
    • dizziness;
    • headache;
    • impaired vision;
    • drowsiness;
    • aphasia;
    • pain in the back;
    • stiff neck muscles;
    • convulsions;
    • paralysis;
    • hemiparesis;
    • in some cases:
      • fatigue;
      • weakness;
      • confusion of consciousness;
      • ataxia;
      • tremor;
      • irritability;
      • coma.
  2. From the cardiovascular system (hematopoiesis, hemostasis):
    • anemia;
    • leukopenia;
    • thrombocytopenia;
    • neutropenia;
    • lymphopenia (especially T-lymphocytes);
    • hypogammaglobulinemia;
    • hemorrhage;
    • septicemia due to leukopenia;
    • rarely:
      • pericarditis;
      • exudative pericarditis;
      • hypotension;
      • thromboembolic changes (arterial thrombosis, cerebral thrombosis, deep vein thrombosis, renal vein thrombosis, thrombophlebitis, pulmonary embolism).
  3. On the part of the respiratory system:
    • interstitial pneumonitis;
    • fibrosis of the lungs;
    • exacerbation of pulmonary infections.
  4. On the part of the digestive system:
    • gingivitis;
    • ulcerative stomatitis;
    • anorexia;
    • nausea;
    • vomiting;
    • diarrhea;
    • difficulty swallowing;
    • melena;
    • ulceration of the mucosa of the gastrointestinal tract;
    • gastrointestinal bleeding;
    • enteritis;
    • liver damage;
    • fibrosis and cirrhosis of the liver.
  5. From the genitourinary system:
    • cystitis;
    • nephropathy;
    • azotemia;
    • hematuria;
    • hyperuricemia or severe nephropathy;
    • dysmenorrhea;
    • unstable oligospermia;
    • violation of the process of oogenesis and spermatogenesis;
    • fetal defects.
  6. From the skin:
    • cutaneous erythema;
    • itching;
    • hair loss;
    • photosensitization;
    • ecchymosis;
    • acne eruption;
    • furunculosis;
    • peeling;
    • hyperpigmentation of the skin;
    • blistering;
    • folliculitis;
    • telangiectasia;
    • toxic epidermal necrolysis;
    • Stevens-Johnson syndrome.
  7. Allergic reactions:
    • fever;
    • chills;
    • rash;
    • hives;
    • anaphylaxis.

Experimental studies have shown the following negative effects of the drug:

  • embryotoxic;
  • mutagenic;
  • carcinogenic.

Symptoms of toxicity are:

  • unexpected bleeding and hemorrhage of any kind;
  • the presence of blood in the urine and feces;
  • red dots on the skin;
  • black fecal masses of oozinglike consistency;
  • disturbance of bone marrow functions.

Instructions for use of methotrexate in rheumatoid arthritis

The drug should be administered under the strict supervision of medical staff. This will help in a timely manner to identify a possible manifestation of an adverse reaction and to correct further treatment.

Treatment, as a rule, lasts at least 3 months. Over the next year after discontinuation of therapy should be refrained from immunization.

Methotrexate - a serious drug, during the use of which requires supervision of a specialist

Usually, with rheumatoid arthritis, Methotrexate is used in tablet form. The initial dose is minimal. Subsequently, it is gradually increased to the point at which a pronounced positive effect appears, but there are no side reactions.

In the treatment of rheumatoid arthritis, the drug is used no more often than once a week.Sometimes this single dose is divided into 3 receptions with an interval of no more than 12 hours.

Duration of treatment is up to three months.

If there was an overdose of Methotrexate, which is determined by its concentration in the plasma, it is necessary to urgently cancel the drug and administer the antidote calcium folinate.

Medication analogues

If you cancel Methotrexate, you need to choose a replacement.The use of structural analogues in such cases is impractical due to the possible occurrence of identical side reactions against the background of a single active substance.

Structural analogues of Methotrexate:

  • The methodical;
  • Métortrite;
  • Treksan;
  • Zexate;
  • Эветрекс;
  • Emtexate.

There are non-structural analogs that are used when the substance of methotrexate causes undesirable toxic reactions.

Table: The basic drugs used in the treatment of rheumatoid arthritis

Analogues of Methotrexate - photo gallery

Azathioprine - a substitute for Methotrexate Arava is a highly effective medicine from a German manufacturer for the treatment of rheumatoid arthritis. It is a highly effective expensive new generation for the treatment of arthritisMetipred - one of the analogues of MethotrexateRemicade - the most expensive tool in the treatment of rheumatic arthritis Sulfasalazine is an inexpensive but effective analogue of Methotrexate Taudedon is a medicine for the treatment of diseases based on gold salts. Ekoral is an affordable remedy for the treatment of arthritis

Opinions of specialists about the preparation

According to most rheumatologists, Methotrexate is the optimal choice for both therapeutic parameters and pricing policy.

The earlier the disease is identified, the higher the chances of improving the patient's health without surgery.

Patient Reviews

Methotrexate - videoinstruction

It is a mistake to assume that Methotrexate alone will help to overcome the disease. A complex treatment is required. However, this drug can prevent the spread of the pathological process to other systems and organs. The main thing is to strictly follow all the doctor's recommendations.

  • Evgenia Yablokova
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A source: http://sovdok.ru/nevrologiya/metotreksat-pri-revmatoidnom-artrite.html

Methotrexate in the treatment of rheumatoid arthritis: instructions for use, side effects, analogs + reviews of doctors and patients

The creation of drugs effective in the treatment of rheumatoid arthritis (RA) remains one of the important tasks of modern rheumatology and pharmaceutics.

The increased attention to this serious disease can be explained by the wide spread of the RA (studies of recent years prove that this pathology affects about 2% of the adult population of developed countries), early disability, deterioration in quality and a decrease in life expectancy patients. The drug Methotrexate, used as a means of "basic" therapy, has proved effective in rheumatological diseases.

Rheumatoid arthritis is a disease requiring effective therapy

Rheumatoid arthritis, characterized by chronic inflammation of the joints, is a disease, the causes of which have not been adequately studied.

The main danger of the disease is determined not only by disorders of the musculoskeletal system (destruction of joints, concomitant lesion of periarticular tissues), but also by systemic lesion organism.

Rheumatoid arthritis

An important sign of rheumatoid arthritis is symmetrical joint damage, which results in damage to articular cartilage and bone tissue, which disrupts the function of the affected organs.

When exposed to provoking factors (ecology, genetic predisposition, etc.), the immune system the organism ceases to react normally to its own tissues, taking them for alien objects that are subject to destruction.

As a result, autoimmune inflammation occurs, which can be influenced by drugs, directly influencing the immune system - they are able to inhibit the activity of the pathological process by suppressing active and aggressive cells.

Rheumatoid arthritis is a systemic disease of connective tissue with a predominant lesion of small joints

Methotrexate - the mechanism of action of the drug

Medicinal product Methotrexate refers to preparations of basic therapy of rheumatoid arthritis - such medicines not only suppress the severity of the symptoms of the disease, but also have the ability to prevent the destruction of bone tissue and the development of persistent deformities joints.

In general, the drug substance affects the cells of the body, which can quickly divide.

Under the influence of the drug violated the cycle of metabolism of folic acid in cells, due to what Methotrexate has antitumor and anti-inflammatory effect.

With rheumatoid arthritis, reproduction of lymphocytes triggering an autoimmune inflammation, as well as fibroblasts and cells of the synovial membrane of the joints, which are damaged by disease.

At the same time, the production of substances that support inflammation in the body is inhibited, and the production of anti-inflammatory compounds is stimulated.

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The action of Methotrexate is aimed at improving the mobility of joints and eliminating inflammation

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When Methotrexate is used in patients with rheumatoid arthritis, the severity of symptoms decreases joint damage (stiffness after rest, pain intensity, swelling of the articular structures).

The drug can be taken orally (through the mouth) or used as injections - in both cases, the active ingredient the drug actively binds to blood proteins, is delivered to the liver cells and converted into hepatocytes into active metabolites. It is these compounds that have antitumor and immunosuppressive effects.

Methotrexate is used with caution in the treatment of patients with renal insufficiency

From the body, Methotrexate is excreted in the urine, so if there is a pronounced impairment of the excretory function of the kidneys (renal failure), the risk of complications and side effects increases in several time.

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Forms and composition of the preparation

Currently, Methotrexate is produced by several pharmaceutical companies in the following dosage forms:

  • pills;
  • injection;
  • concentrate for the preparation of infusion.

For the treatment of rheumatoid arthritis, the drug Methotrexate is used in the form of tablets in dosages of 5 mg and 10 mg. In other forms of release, the drug is prescribed to patients suffering from oncological diseases.

Composition of Methotrexate depending on the dosage form - table

Instructions for use

Methotrexate dosage as a means of basic therapy rheumatologist calculates based on the activity of inflammatory process, the age of the patient suffering from rheumatoid arthritis, the duration of the disease, the intake of other medicinal products means.

Methotrexate - a means of basic therapy of rheumatic arthritis

It is recommended to take the calculated dose of the drug with an interval of 7 days (on the prescription rheumatologists often indicate which day of the week you need to drink a pill).

Given the mechanism and peculiarities of the action of Methotrexate, treatment should be conducted under the supervision of a qualified doctor who has special training and experience in using the drug.

Only a doctor can correlate the positive and negative properties of the medicine, evaluate what medicines can increase the risk of complications, take contraindications to the appointment.

Contraindications to the use of the drug

Do not prescribe Methotrexate to patients with a number of diseases and conditions, among which:

  • intolerance of any substance included in the preparation - allergic reactions can provoke the development of anaphylactic shock (a condition that directly threatens the patient's life);
  • severe degrees of renal and hepatic insufficiency - the liver converts methotrexate into an active metabolite, and the decay products of the drug are excreted by the kidneys. Failure to comply with these rules leads to the accumulation of substances in the body and the appearance of symptoms of drug overdose;
  • detection of signs of oppression of hematopoiesis in the bone marrow in a patient - Methotrexate intensively affects exactly the stem cells brain responsible for restoring the normal blood composition, and manifestations of anemia, thrombocytopenia or leukopenia will be progress;
  • alcoholism in the patient - ethyl alcohol increases the toxicity of the drug due to exposure to liver cells;
  • Detection of acute and chronic infectious diseases in a patient - Methotrexate directly affects the cells of the immune system responsible for suppressing microbial and viral infections;
  • the need for vaccination with live vaccines - such vaccines include vaccinations against poliomyelitis, hepatitis B, etc .;
  • the presence of bleeding from the digestive tract, exacerbation of peptic ulcer of the stomach and duodenum;
  • detection of lactose intolerance;
  • simultaneous administration of drugs that have a toxic effect on the liver parenchyma cells (hepatocytes).

Precautions Methotrexate is recommended for patients with concomitant diabetes mellitus (regardless of type), herpetic infection, recently transferred measles, chicken pox, gout, parasitic infections of the digestive system tract.

Prescribe the drug to children under 7 years old and elderly patients need with great care - regular examinations of a rheumatologist recommending preparation, as well as conducting laboratory studies to monitor the effectiveness of the drug and to monitor in a timely manner possible complications.

Interaction with other drugs

Methotrexate interacts with many medicinal substances - the result of this can be:

  • a significant increase in the effect of taking the drug, which increases the risk of side effects;
  • The absence of the expected action, as a result of which the doctor is forced to increase the dose of the drug.

If the doctor recommends a patient suffering from rheumatoid arthritis, taking Methotrexate, then he should definitely check with the patient what other medications he takes continuously. Also, a rheumatologist explains what medications can affect the outcome of therapy.

Drugs that increase the concentration of methotrexate in the blood serum are:

  • non-steroidal anti-inflammatory drugs, including those drugs that are traditionally prescribed for the symptomatic treatment of joint pain;
  • other immunosuppressive medications (regardless of their type and mechanism of action);
  • antibiotics - penicillin or tetracycline drugs, fluoroquinolones (ciprofloxacin and its analogues);
  • medicines used in gastroenterology (proton pump inhibitors) due to the slowing down of the drug from the blood plasma.

To drugs that reduce the impact of Methotrexate on the body, include folic acid and its derivatives.

With caution, the medication is prescribed concomitantly with the drugs used to treat epilepsy and convulsive syndromes. It is also possible to reduce the effectiveness of the drugs recommended for gout.

Features of use of the drug during pregnancy and breastfeeding

Methotrexate has a damaging effect on the hereditary apparatus of the reproductive cells of all patients.

It is strictly forbidden to prescribe Methotrexate to women bearing a child. Before the start of the course of basic therapy with the drug, the gynecologist should exclude the possibility of pregnancy in the patient.

Methotrexate is contraindicated in women during pregnancy

In the course of treatment, the use of methods for preventing pregnancy is mandatory.

If the patient becomes pregnant during the therapy, the rheumatologist should inform her about the high probability of having a child with developmental defects, to send for a consultation with a geneticist.

Contraindicated taking Methotrexate and during breastfeeding - the drug, getting through the mother's milk in the body of the child, can provoke severe intoxication in the baby.

Possible side effects

Complications arising during the treatment of rheumatoid arthritis can affect the functioning of various body systems:

  • on the part of the nervous system, there are often attacks of dizziness, headache, sleep disorder (drowsiness), fatigue, irritability. Less often, patients complain of visual disturbances, pain in the back and neck, trembling of the limbs;
  • on the part of the hematopoietic system, there are disorders associated with the oppression of hemopoiesis in the bone marrow - anemia can be detected (decrease the number of red blood cells and the level of hemoglobin), a decrease in the number of leukocytes, platelets (can trigger clotting disorders blood);
  • from the side of the cardiovascular system is often revealed a decrease in blood pressure, damage to the heart muscle (myocarditis) and the cardiac bag (pericarditis).In addition, there may be thromboses in arteries and veins of different caliber - such complications pose a serious danger to the life of the patient;
  • On the part of the respiratory organs, fibrotic changes in the lungs are detected;
  • From the side of the digestive tract, ulcerative necrotic lesions of the mucous membranes are recorded (pharyngitis, stomatitis). Quite often, patients complain of lack of appetite, nausea, upset of the stool, vomiting. Less often mark the development of bleeding from the digestive tract, gastritis, duodenitis, colitis. With prolonged treatment, the patient may experience toxic hepatitis;
  • from the side of the urinary system, the development of inflammation of the bladder (cystitis), toxic damage to kidney tissue (nephritis);
  • on the part of the reproductive system, menstrual cycle disorders, damage to germ cells (at the level of DNA and RNA), which is fraught with various malformations and congenital diseases in the children of patients undergoing treatment Methotrexate;
  • the skin and its appendages of patients are concerned about redness and flaking, hair loss, spread of pustular diseases (acne, boils);
  • In the course of treatment, various allergic reactions (up to anaphylactic shock) can develop.

In addition, the patient receiving Methotrexate must understand that the drug depresses all links of immunity - this is in many times increases the likelihood of developing severe infectious pathologies, exacerbation of foci of chronic infection in organism.

Than you can replace Methotrexate

In the treatment of rheumatoid arthritis today use:

  • non-steroidal anti-inflammatory drugs - stop the pain and to a small extent inhibit the autoimmune process;
  • steroidal anti-inflammatory drugs - hormones of the adrenal cortex, capable of suppressing the activity of inflammation;
  • means of basic therapy;
  • genetically engineered biological preparations - are able to act directly on the internal structures of the cells of the immune system involved in the development of autoimmune inflammation.

Analogues of Methotrexate - table

Medications prescribed for rheumatoid arthritis - gallery

Diclofenac is a non-steroidal anti-inflammatory drug Movalys-a non-steroid analogue of MethotrexateMabter is an effective preparation with rheumatoid arthritisAzathioprine - immunosuppressive drug Active substance Metipreda is methylprednisolone

The opinion of doctors about the drug

Modern rheumatologists consider Methotrexate to be the "gold standard" in the therapy of rheumatoid arthritis.

This opinion is confirmed by numerous domestic and foreign medical studies, which prove the high effectiveness of the drug.

When evaluating the effectiveness of a medicine, it is estimated:

  • improvement of the subjective state of the patient and a reduction in the severity of objective symptoms of the disease with adherence to the regimen (achieved in 85% of RA patients);
  • less risk of side effects than with other medications;
  • prevention of development of complications leading to disability (this is especially important for young patients).

Treatment of rheumatoid arthritis - video

Patients who took Methotrexate

The appointment of Methotrexate to patients who suffer from rheumatoid arthritis not only improves the condition of the affected joints, but also prevents the development of systemic manifestations of the disease. Basal therapy positively affects the quality of life of patients, but the decision to start taking the medication is taken exclusively by the doctor.

  • Olga Rudomenko
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A source: http://lechenie-simptomy.ru/metotreksat-sredstvo-bazisnoy-terapii-revmatoidnogo-artrita