Methotrexate is an antitumor agent that has immunosuppressive, cytostatic and antitumor effects.

Available in ampoules for injection and in tablet form for oral administration.

Methotrexate-Ebewe acts on epithelial cells Bladder, malignant tumors, bone marrow, cells of the intestinal mucosa and oral cavity, embryonic cells.

The drug is prescribed for severe psoriasis, rheumatoid arthritis, trophoblastic tumors, lymphomas and leukemias, severe mycosis fungoides.

Clinical and pharmacological group

Anticancer drug.

Terms of dispensing from pharmacies

Released by prescription.

Prices

How much does Methotrexate cost? The average price in pharmacies is at the level of 190 rubles.

Release form and composition

Produced in several forms. One of them are Methotrexate tablets, each containing 2.5 mg of the active ingredient, and Methotrexate-Ebewe tablets with 10 mg of the active substance.

Also, the drug is available in the form of a solution for injection of Methotrexate-Ebeve with 10 mg of the active substance and in the form of a concentrate for the preparation of a solution of Methotrexate-Ebeve, 5 ml of which contains 500 mg of the active ingredient.

Pharmacological effect

An antitumor agent from the group of antimetabolites - antagonists folic acid. Acts in the S-phase of mitosis. The action is associated with inhibition of the synthesis of purine nucleotides and thymidylate by irreversible binding to dihydrofolate reductase, which prevents the reduction of dihydrofolate to active tetrahydrofolate.

Shows activity against rapidly growing cells. Produces some immunosuppressive effect.

Indications for use

What helps? Methotrexate is prescribed for the following diseases:

1. trophoblastic disease.
2. Acute lymphocytic leukemia.
3. Fungal mycosis in severe stages.
4. (in case of ineffectiveness of other methods of treatment).
5. Severe forms (with the ineffectiveness of adequate therapy).
6. Soft cell and osteogenic sarcoma, Ewing's sarcoma.
7. Germinogenic tumors of the ovaries and testis.
8. Medulloblastoma, retinoblastoma, lymphogranulomatosis.
9. Cancer of the skin, vulva and cervix, breast, penis, esophagus, lung, squamous cell carcinoma of the neck and head, cancer of the kidney, ureter and renal pelvis, liver cancer.

Contraindications

Methotrexate has a number of serious contraindications:

• increased bleeding and problems with stopping bleeding against the background of a decrease in the number of platelets;
• immunodeficiency syndrome;
• during the period of vaccination with live vaccines;
• hypersensitivity to the main active substance or auxiliary components;
• severe disorders in the work of the kidneys and liver;
• decrease in the number of leukocytes per unit volume of blood;
• alcohol addiction.

In addition, the drug should be taken with caution in the elderly, as well as in the presence of such diseases:

• oppression of bone marrow hematopoiesis;
• diabetes;
• peptic ulcers of the digestive tract;
• lactose intolerance.

The drug is not used in pediatric practice up to 3 years.

Use during pregnancy and lactation

It has a teratogenic effect: it can cause fetal death, congenital deformities. In the event that a woman becomes pregnant during methotrexate therapy, the issue of terminating the pregnancy should be considered due to the risk of adverse effects on the fetus.

Methotrexate is excreted in breast milk for the duration of the entire course of treatment. breast-feeding should be stopped.

Dosage and method of application

The instructions for use indicate that Methotrexate tablets are used orally. Doses and terms of treatment are set individually depending on the chemotherapy regimen.

Rheumatoid arthritis:

• The initial dose is usually 7.5 mg once a week, which is taken simultaneously or divided into three doses with an interval of 12 hours. For optimal effect, the weekly dose may be increased, while it should not exceed 20 mg. When the optimal clinical effect is achieved, dose reduction should be initiated until the lowest effective dose is reached. The optimal duration of therapy is not known. With juvenile chronic arthritis for children, doses of 10-30 mg / m2 / week (0.3-1 mg / kg) are effective.

Trophoblast tumors:

• 15-30 mg orally daily for 5 days at intervals of one or more weeks (depending on signs of toxicity). Treatment courses are usually repeated 3 to 5 times.
• 50 mg 1 time in 5 days with an interval of at least 1 month. The course of treatment requires 300-400 mg.

Acute lymphoblastic leukemia (composed of complex therapy):

• 3.3 mg/m2 in combination with prednisolone until remission is achieved, then 15 mg/m2 once a week or 2.5 mg/kg every 14 days.

Non-Hodgkin's lymphomas (as part of complex therapy):

• 15-20 mg / m2 for 1 dose 2 times a week;
• 7.5 mg/m2 daily for 5 days.

Fungal mycosis:

• 25 mg 2 times a week. Reducing the dose or canceling the administration of the drug is determined by the patient's response and hematological parameters.

Psoriasis:

• Therapy with methotrexate is carried out in doses of 10 to 25 mg per week. The dose is usually increased gradually, when the optimal clinical effect is reached, the dose is reduced until the lowest effective dose is reached.

Side effects

expressiveness side effects from taking Methotrexate is different for everyone.

1. Patients often note the appearance of a feeling of fatigue, sometimes headaches, drowsiness, convulsions are noted.
2. On the part of the reproductive system, there is a violation menstrual cycle, decreased libido, development of impotence.
3. From the side digestive system development of ulcerative stomatitis, anorexia, pharyngitis is possible. In rare cases, diarrhea opens or pancreatitis develops. In exceptional situations, cirrhosis, liver necrosis is possible.
4. Other allergic and dermatological reactions may also occur: chills, skin rash, furunculosis, pigmentation disorders.

The severity of complications depends on many circumstances, including the severity of the disease.

Overdose

For an overdose of Methotrexate, specific symptoms are not characteristic, therefore it is determined by the level active substance drug in plasma.

As a treatment, it is recommended to administer a specific antidote - calcium folinate - as soon as possible after taking the drug in high doses, preferably during the first hour. Its dose should be equal to or greater than the corresponding dose of methotrexate. Subsequent doses are administered as needed, depending on the content of methotrexate in the blood serum. To avoid precipitation of methotrexate and / or its metabolites in the renal tubules, alkalinization of the urine and hydration of the body should be carried out, leading to an accelerated elimination of the drug.

To minimize the risk of developing nephropathy due to the formation of a precipitate of methotrexate or its metabolites in the urine, it is recommended to additionally determine the pH of the urine before each administration and every 6 hours during the entire period of use of calcium folinate, which is used as an antidote. The introduction of the latter must be continued until the concentration of methotrexate in plasma decreases to a value not exceeding 0.05 μmol / l, and the pH rises to values ​​​​more than 7.

special instructions

Before initiating or resuming methotrexate therapy, a complete general analysis blood with the determination of the level of platelets, biochemical analysis blood with the determination of the values ​​of liver enzymes, bilirubin, serum albumin, X-ray examination chest, examination of kidney function, if necessary - tests for tuberculosis and hepatitis.

Methotrexate is a cytotoxic drug, so care must be taken when handling it. The drug should be prescribed by a doctor who has experience in the use of methotrexate and is familiar with its properties and features of action. In view of the possible development of severe and even fatal adverse reactions patients should be fully informed by the doctor about possible risks and recommended safety precautions. Patients undergoing methotrexate therapy should be properly monitored so that signs of possible toxic effects and adverse reactions are identified and evaluated in a timely manner.

For the timely detection of symptoms of intoxication, it is necessary to monitor the state of peripheral blood (the number of leukocytes and platelets: first every other day, then every 3-5 days during the first month, then 1 time in 7-10 days, during remission - 1 time in 1-2 weeks), the activity of “liver” transaminases, kidney function (urea nitrogen, creatinine clearance and / or serum creatine), the concentration of uric acid in the blood serum, periodically conduct x-ray of the chest, examination of the oral mucosa and pharynx for the presence of ulceration before every application. It is recommended to monitor the state of bone marrow hematopoiesis before treatment, 1 time during treatment and at the end of the course.

To objectify liver function, along with biochemical parameters, it is recommended to perform a liver biopsy before or 2-4 months after the start of treatment; with a total cumulative dose of 1.5 g and after each additional 1-1.5 g. With moderate liver fibrosis or any degree of cirrhosis, methotrexate therapy is canceled; with fibrosis mild form a follow-up biopsy after 6 months is usually recommended. During initial therapy, minor histological changes in the liver (minor portal inflammation and fatty changes) are possible, which is not a reason for refusing or stopping treatment, but indicates the need for caution when using the drug.

Methotrexate can potentially lead to the development of symptoms of acute or chronic hepatotoxicity (including fibrosis and cirrhosis of the liver). Chronic hepatotoxicity usually develops after long-term use methotrexate (usually for 2 or more years) or reaching a total cumulative dose of at least 1.5 g and may lead to a poor outcome. The hepatotoxic effect may also be due to a burdened concomitant history (alcoholism, obesity, diabetes mellitus) and old age. In view of the toxic effects of the drug on the liver during treatment, patients should be refrained from prescribing other hepatotoxic drugs, unless clearly necessary. Patients taking other hepatotoxic drugs (eg leflunomide) should be closely monitored.

Do not expose unprotected skin to too much sun exposure or abuse the UV lamp (possible photosensitivity reaction). In view of the effect on the immune system, methotrexate may impair the response to vaccination and affect the results of immunological tests. It is necessary to refuse immunization (if it is not approved by a doctor) in the interval from 3 to 12 months after taking the drug; other members of the patient's family living with him should refuse immunization with oral polio vaccine (avoid contact with people who received polio vaccine, or wear a protective mask covering the nose and mouth). Patients of childbearing age of both sexes and their partners should use reliable contraceptive measures during treatment with methotrexate and after treatment for at least 3 months in men and at least one ovulation cycle in women.

With the development of diarrhea and ulcerative stomatitis, methotrexate therapy must be interrupted due to the high risk of developing hemorrhagic enteritis and perforation of the intestinal wall, which can lead to the death of the patient.

After a course of treatment with high doses of methotrexate, the use of calcium folinate is recommended to reduce its toxicity.

Since methotrexate is capable of affecting the central nervous system (feeling tired, dizzy), patients taking the drug should refrain from administering vehicles or potentially dangerous machinery.

drug interaction

When using the drug, it is necessary to take into account the interaction with other drugs:

1. Co-administration with leflunamide increases the incidence of pancytopenia and cases of hepatotoxicity.
2. With alcohol abuse and taking hepatotoxic drugs, increases toxic effect Methotrexate for the liver.
3. Ciprofloxacin, glycopeptides, penicillins, loop diuretics, phenylbutazone reduce the clearance of the drug in the kidneys, which increases its concentration in the blood and enhances toxicity to hematopoiesis.
4. Chloramphenicol, tetracycline oral administration reduce the absorption of methotrexate.
5. Also, the toxicity of Methotrexate increases with simultaneous use with salicylates and non-steroidal anti-inflammatory drugs.
6. Trimethoprim and sulfamethoxazole, which cause folate deficiency, as well as lipid-lowering drugs and indirect anticoagulants, can increase the toxic effect of Methotrexate.
7. Chloramphenicol, sulfonamides, pyrimethamine have a negative effect on the bone marrow, so the combined use with Methotrexate exacerbates hematological disorders.
8. Methotrexate inhibits the immune response to vaccination, and in the case of the introduction of live vaccines, severe antigenic reactions are likely.
9. When taken simultaneously with cytostatics, the clearance of methotrexate is reduced.
10. Combination with radiotherapy increases the likelihood of tissue necrosis.
11. Reception of amiodarone contributes to the appearance of skin ulcers.
12. With the introduction of acyclovir and the simultaneous use of methotrexate intrathecally, the risk of neurological lesions is increased.

Increased consumption of coffee, tea and caffeinated sugary drinks should be avoided during treatment, as the clearance of theophylline may decrease.

Content

The product is one of the best anticancer drugs from the pharmaceutical market. Therapy with this drug should be carried out under the supervision of a physician and in strict accordance with the instructions for use. Self-use can cause serious consequences.

Composition and form of release

pharmachologic effect

According to the instructions for use, Methotrexate belongs to the group of antimetabolites, cytostatics, and is a folic acid antagonist. The drug has an antitumor, immunosuppressive effect. The active substance helps to slow down the synthesis and repair of DNA, cell mitosis. The following are highly sensitive to the drug: bone marrow, mucosal epithelium, tumor tissue, embryonic cells.

The use of the drug contributes to the disruption of the growth of malignant neoplasms, without damaging healthy areas organism. In the treatment of rheumatoid arthritis, methotrexate relieves pain, swelling, stiffness of the joints and other signs of the inflammatory process. In the treatment of psoriasis, plaque keratinocytes are affected. The active substance is excreted through the kidneys and with bile.

Indications for use

The drug belongs to the group of anticancer drugs. According to the instructions for use, the medication has the following indications:

• lymphoblastic, myeloblastic acute leukemias;
• cancer of the skin, breast, lungs, bladder, kidneys, female and male genital organs, esophagus;
• medulloblastoma, squamous cell carcinoma, retinoblastoma;
• neuroleukemia;
• osteogenic and soft tissue sarcoma, lymphosarcoma;
• psoriasis, severe mycosis fungoides;
• trophoblast tumors;
• rheumatoid, psoriatic arthritis;
• ankylosing spondylitis;
• dermatomyositis;
• systemic lupus erythematosus.

How to take Methotrexate

Instructions for use of the drug indicates that the choice of treatment regimen and dosage regimen should be carried out by a specialist. The doctor prescribes the required amount of the drug and the frequency of its use, based on the diagnosis and data from the medical literature.

Tablets

Methotrexate for rheumatoid arthritis is prescribed orally. According to the instructions for use, the pills should be taken before meals, without chewing. It is recommended to drink the medicine with water. The initial dose is 7.5 mg 1 time / week. It is allowed to use at the same time or divided into 3 doses, observing an interval of 12 hours. During therapy, the doctor may increase the weekly dose. The maximum allowed amount is 20 mg.

Methotrexate tablets for trophoblastic tumors should be taken at 15-30 mg for 5 days. Then there is a break of 1-2 weeks. The course is repeated 3-5 times. The doctor may prescribe 50 mg tablets 1 time / 5 days. This requires an interval of 1 month. For a course of therapy, the patient will need 300-400 mg of medication. In the treatment of psoriasis, 10-25 mg / week is prescribed. Increasing the dose occurs gradually until the desired clinical effect is achieved.

For the treatment of mycosis fungoides, it is indicated to use 25 mg twice a week. The basis for dose reduction or discontinuation of the drug may be hematological parameters and the patient's response. As part of complex therapy, the instructions for use prescribe the use of Methotrexate for lymphoblastic leukemia in acute form, non-Hodgkin's lymphomas. The course and dosage regimen is set by the attending physician.

Ampoules

Methotrexate solution is administered intramuscularly, intravenously, intrathecally, intraarterially. Injections are carried out with the following diseases:

• Trophoblastic tumors - 30 mg daily, intramuscularly. The course of treatment is 5 days. Need a week break. Therapy is carried out until a dose of 400 mg is reached.
• Leukemias, lymphomas - administered intravenously at 200-500 mg / m2 once a month.
• Neuroleukemia - intrathecally, 12 mg / m2 1-2 times / week.
• Psoriasis - administered intramuscularly or intravenously in a jet at 25 mg / week.
• Fungal mycosis - intramuscularly, 50 mg / 7 days once or divided into 2 procedures.

special instructions

Methotrexate can only be prescribed by an oncologist who is experienced in chemotherapy. The physician should warn the patient about the likelihood of developing severe, leading to impaired health or death, adverse reactions, manifested by toxic lesions. If the patient has an accumulation of fluid inside the pleural or abdominal cavity, it must be removed before starting drug therapy.

If symptoms of stomatitis appear, which are evidence of toxic damage to the gastrointestinal tract, it is necessary to stop taking Methotrexate for a while to prevent perforation and ulceration of the intestine. Before starting therapy, a clinical, biochemical analysis of the patient's blood, a chest x-ray, and a study of kidney function are required. In the process of treatment, it is necessary to carry out the following diagnostic measures every month:

• examination of the oral cavity;
• study of the functionality of the liver;
• detailed blood test;
• examination of the respiratory system;
• Analysis of urine;
• study of the state and functioning of the kidneys.

Methotrexate should be stopped 7 days before the proposed surgical intervention, it is recommended to resume treatment 2 weeks after the operation. When prescribing a medication, it should be taken into account that it increases the risk of the formation of malignant lymphomas. Before starting therapy, it is necessary to exclude the patient's pregnancy. Patients of reproductive age are advised to use contraceptives during the treatment period, since the drug negatively affects the reproductive system.

With the introduction of the drug intrathecally, complications that threaten the life of the patient may occur. At the first sign of development side effects the medication must be stopped immediately. Do not mix Methotrexate in the same vial with other substances. In case of contact with the mucous membranes or skin, it must be immediately washed off with water. When treating with a drug, patients need to be careful when performing actions that require quick reactions, increased attention.

During pregnancy

Methotrexate should not be taken during pregnancy and lactation. The drug has an embryotoxic effect, can cause fetal defects internal organs. The drug in high concentrations, dangerous to the health of the baby, penetrates into breast milk. If a woman needs methotrexate therapy, breastfeeding should be stopped so as not to harm the health of the child.

drug interaction

Some drugs in combination with Methotrexate have a negative effect on the patient's body. When interacting with other medicines, the following effects may occur:

• The toxic effect of the drug on the liver is enhanced if the patient has alcohol dependence, while taking hepatoxic drugs, Leflunamide.
• The absorption of Methotrexate is reduced with the combined use of oral forms of Tetracycline, Chloramphenicol.
• Glycopeptides, Ciprofloxacin penicillins, Phenylbutazone, loop diuretics increase the concentration of the active substance in the blood, reducing the clearance of the drug in the kidneys.
• The toxicity of Methotrexate increases when combined with non-steroidal anti-inflammatory drugs, salicylates.
• Hematological disorders are aggravated by the interaction of the drug with sulfonamides, Chloramphenicol, Pyrimethamine.
• Trimethoprim, Sulfamethoxazole, contributing to folate deficiency, indirect anticoagulants, lipid-lowering agents can enhance the toxic effect of Methotrexate.
• The clearance of the active substance is reduced when combined with cytostatics.
• The risk of tissue necrosis increases with the combination of drug treatment with radiotherapy.
• The drug reduces the immune response to vaccinations, with the introduction of live vaccines, severe antigenic reactions are possible.
• The risk of neurological complications increases with the simultaneous use of methotrexate intrathecally and acyclovir.

Side effects of Methotrexate

Therapy with the drug can provoke pathological reactions from various body systems. The instructions for use indicate the following side effects:

• thrombocytopenia, pancytopenia, anemia, leukopenia, bone marrow dysfunction high degree gravity;
• drowsiness, frequent mood swings, fatigue, depression, headache, insomnia, confusion, leukoencephalopathy, epileptic seizures, paralysis, paresthesia of the extremities, symptoms of meningism, metallic taste in the mouth;
• conjunctivitis, eye irritation;
• development of pneumonitis, alveolitis, pleural effusion, pulmonary fibrosis, bronchial asthma, pharyngitis, pulmonary edema, thickening of the pleural sheets;
• the appearance of inflammation and ulcers in oral cavity, nausea, dyspepsia, stomatitis, diarrhea, cirrhosis and fibrosis of the liver, anorexia, vomiting, increased transaminases, steatosis;
• pruritus, photosensitivity, herpes zoster, alopecia, vasculitis, herpetiform eruptions, epidermal necrosis, increased nail pigmentation, hidradenitis, acute paronychia, furunculosis;
• the appearance of ulcers, inflammation of the bladder, impaired functioning of the kidneys, electrolyte balance, failures in urination, anuria, oliguria;
• osteoporosis, joint and muscle pain;
• bleeding, pericardial effusion, cardiac tamponade;
• decrease in the immune defense of the body, anaphylactic reactions, an increase in the number of rheumatoid nodules, sepsis;
• inflammation, vaginal ulceration, menstrual irregularities, atypical vaginal discharge, decreased sex drive, impotence;
• fever, chills, general malaise, decreased wound healing;
• when administered intramuscularly, the formation of polyps, cysts, lymphomas, abscesses, tissue destruction at the injection site is possible;
• metabolic disorders, diabetes;
• with intrathecal administration: acute arachnoiditis, plegia, paresis, dysfunction of the cerebellum, leukoencephalopathy, death.

Overdose

If the dose of the drug specified according to the instructions or recommended by the doctor is exceeded, oppression of the hematopoietic system occurs. Calcium folinate is used as an antidote. The substance must be administered in the first hour after taking the medication, its dose must correspond to or exceed the amount of Methotrexate taken orally. In case of severe overdose, hydration of the body, alkalization of urine is used. If the amount of the drug is exceeded with intrathecol administration, it is necessary to use an antidote in combination with drainage cerebrospinal fluid.

Contraindications

• alcoholism;
• damage to the liver and kidneys of high severity;
• the presence of vaccinations with live vaccines;
• HIV infection, tuberculosis and other severe infectious diseases;
• a history of oral ulcers and gastrointestinal tract;
• taking drugs containing acetylsalicylic acid in large doses;
• violations of the hematopoietic system;
• individual intolerance to the active substance or other components of the drug;
• period of pregnancy and lactation.

In some cases, Methotrexate is prescribed with caution so as not to provoke the appearance of side effects. The drug should be taken under the supervision of a physician in the presence of certain pathologies, conditions:

• diseases of the liver, kidneys;
• diabetes;
• obesity;
• oppression of bone marrow circulation;
• infections of viral, fungal or bacterial origin;
• pleural and peritoneal effusion;
• dehydration;
• herpes zoster;
• measles, chicken pox;
• strongyloidiasis, amoebiasis;
• gout;
• inflammatory processes, infections of the oral mucosa;
• vomiting, ulcerative colitis, diarrhea, gastrointestinal obstruction;
• asthenia, aciduria;
• prior treatment with radiotherapy or chemotherapy.

Terms of sale and storage

According to the instructions for use, Methotrexate is a prescription drug. Keep the medication out of the reach of children, protected from light at a temperature of 15-25 degrees. The shelf life of the drug is 36 months.

Analogues

Doctors may prescribe medications that are identical to Methotrexate in composition and action. The main analogues of the drug are:

• Vero-Methotrexate - is released in the form of ampoules with a solution for injection. The agent has an antitumor effect, is used for malignant neoplasms in organs, trophoblastic disease, severe psoriasis, rheumatoid arthritis. According to the instructions for use, Vero-Methotrexate is forbidden to use during pregnancy, leukopenia, thrombocytopenia, impaired functioning of the liver, kidneys, immune system. The dose and route of administration of the drug depend on the state of the hematopoietic system, concomitant antitumor therapy, and the stage of the disease. The cost of Vero-Methotrexate is about 120 rubles.
• Methodoject is an antitumor, immunosuppressive agent. It is released in the form of a solution placed inside special syringes. According to the instructions for use, Metoject is indicated for polyarthritis, severe psoriasis, juvenile rheumatoid arthritis. The medicine has a wide list of contraindications and side effects, so its use is recommended only when prescribed by a doctor. The solution is administered intramuscularly, subcutaneously or intravenously. The treatment regimen should be selected only by a specialist. You can buy Metoject at a price of 461 rubles.
• Methotrexate Teva is an injection solution that has an antitumor effect. According to the instructions for use, the drug is used to treat malignant neoplasms, severe forms of psoriasis, and rheumatoid arthritis. Taking the medicine is prohibited in case of hypersensitivity to the components, pregnancy, lactation, hepatic or kidney failure, thrombocytopenia, anemia, neutropenia, leukopenia. The method of application and dosage are established by the doctor, according to the instructions. The cost of Methotrexate Teva is from 250 rubles.
• Metotab - tablets, the active substance of which is methotrexate. Instructions for use prescribes taking pills for rheumatoid arthritis, chronic psoriasis, acute lymphocytic leukemia. Metotab has an extensive list of contraindications, side effects, and is used only by prescription. The drug is taken orally in the dosage prescribed by the doctor, instructions. The cost of Metotab is about 1400 rubles.

Metoject and Methotrexate - what is the difference

According to the composition and principle of impact on the patient's body, medicines do not have significant differences. Methodoject is released only in the form of a solution intended for intramuscular or intravenous injections. According to the reviews of doctors and patients, Methotrexate from the Austrian manufacturer Ebewe has less toxicity. The cost of drugs is about the same.

Video

Content

Drug therapy is an integral part of the treatment of many inflammatory diseases. Yes, to remove pain syndrome, reducing the area of ​​inflammation and stopping the progression of the disease, cytotoxic drugs are often prescribed. Methotrexate is a modern non-steroidal drug that is prescribed by a rheumatologist during an exacerbation of rheumatoid arthritis, for the treatment of psoriasis and in the diagnosis of other autoimmune diseases.

Instructions for use Methotrexate

An antitumor, cytostatic agent from the group of antimetabolites is used in the basic therapy of rheumatoid arthritis, to achieve remission in diseases of the bone marrow, for the treatment early stage psoriatic arthritis. The drug helps to reduce the intensity of the pain syndrome, stops the inflammatory process of joint destruction, prevents the division of cancer cells, and suppresses active inflammation. The drug can be prescribed even before an accurate diagnosis is made, to remove the first manifestations of the disease.

Composition and form of release

The drug is available in the form of tablets. round shape in vials of 50 pcs., in ampoules for intramuscular or subcutaneous injection 1.5 and 10 ml. Imported methotrexate-ebew is produced as a concentrate for preparing a solution for infusions of 5.10 or 50 ml. Detailed composition for each release form is indicated in the table:

pharmachologic effect

The antitumor and cytostatic effect of the drug is achieved by slowing down DNA repair, synthesis and cell division. Tissues that have a high ability to grow are sensitive to the composition: embryonic cells, bone marrow, mucous epithelium and tumor tissues. The maximum concentration of active substances in the blood plasma is fixed after 30-60 minutes.

The composition of the drug breaks down into metabolites in the liver. 90% is excreted by the kidneys with urine throughout the day, the remaining 10% is excreted with bile. The average elimination half-life is from 6 to 7 hours, when taking high doses - 17 hours. This process may be somewhat slowed down in patients with severe hepatic or renal impairment. Metabolites can accumulate in the liver, spleen, kidneys.

Indications for use

According to the instructions, taking the drug is advisable if the patient has processes accompanied by an increased division of immune cells. Methotrexate is prescribed for:

• acute lymphoblastic leukemia;
• non-Hodgkin's lymphoma;
• lymphosarcoma;
• severe forms of mycosis fungoides;
• psoriasis;
• osteogenic sarcoma;
• cancer of the skin, breast, digestive tract, urinary tract;
• psoriatic arthritis;
• rheumatoid arthritis;
• systemic lupus erythematosus;
• dermatomyositis;
• neuroleukemia;
• trophoblast tumors.

Method of application and dosage

This drug is included in many drug treatment regimens, and therefore the route of administration, the course of therapy and dosage are selected individually by the attending physician. Methotrexate in ampoules is administered intramuscularly, intravenously, intrathecally (under the shell spinal cord) or intraarterially. Unused solutions, injection instruments that have been in contact with this medicinal substance are destroyed by incineration.

The medicine in the form of tablets should be taken orally as a whole, without chewing and washing down the capsule with a sufficient amount of non-carbonated water. To achieve optimal results and speedy absorption of the tablet, it is recommended to drink one hour before meals or one and a half to two hours after meals. Dosages are selected according to the patient's performance. The instruction recommends using the dosage of the drug from 7.5 to 16 mg per day at the initial stages of treatment. In severe cases, standard daily dose can be immediately increased.

Droppers

High doses of the drug, usually more than 100 mg, are administered by intravenous infusion lasting no more than 24 hours. To speed up the process, part of the dose prescribed by the doctor can be administered as an emergency intravenous injection. When choosing this method of treatment, patients are additionally prescribed calcium folinate to protect normal tissues from the toxic effects of Methotrexate-Ebewe.

Protective therapy begins 8-24 hours before the start of the introduction of the main drug. Doses of calcium folinate are determined depending on the volume of the dropper:

• When receiving 100-150 mg within 12-24 hours, 150 mg of folinate are administered, then another 12-25 mg of calcium in injections or 15 mg orally every 6 hours for 2 days.
• When treating with doses below 100 mg, take 1 capsule of folinate every 6 hours for 2-3 days.

Injections Methotrexate

Intravenous, intramuscular or intra-arterial injections are prescribed for trophoblastic tumors, leukemia, rheumatoid arthritis. Before the administration of the drug, a part of the cerebrospinal fluid is removed in the volume in which the drug will be administered. After opening the ampoule, the drug remains stable for 24 hours, after which the drug should be disposed of. Injections for rheumatoid arthritis are prescribed once a week, while the drug is administered on the same day and time.

How to take methotrexate for rheumatoid arthritis

The effect of the drug in the treatment of chronic inflammation of the joints is presumably associated with its ability to suppress the immune system. The use of this medicine allows you to restore the function of the joints, reduce inflammation and the symptoms associated with arthrosis - swelling, stiffness of the joints, severe pain. There is no single scheme for the use of the drug.

To cure arthritis, doctors prescribe a minimum dosage of 6.5 mg. Then, after two to three weeks of therapy, the dose is gradually increased, bringing it up to 26 mg. The recommended dosage is adhered to throughout the treatment, and the regimen medicinal product in tablets remains the same as for the drug in injections - 1 time per week. Sometimes the daily dosage is divided into two or three doses, which must be carried out with an interval of 12 hours.

The effect of treatment for arthritis and arthrosis is not achieved immediately, but 5-6 months after the start of therapy. If the clinical effect occurs too slowly, the drug is combined with other drugs. Rheumatoid arthritis is treated with methotrexate and folic acid or medication:

• cyclosporine;
• leflunomide;
• hydroxychloroquine;
• sulfasalazine.

Treatment of lymphoma and leukemia

The drug is administered intravenously, intramuscularly, intralumbally. For children diagnosed with leukemia, it is preferable to give the medication inside with water. For adults, the optimal dosage for injection is 200-500 mg per m2 (body surface area). An injection is made 1 time per week, as in case of arthrosis or arthritis. Sometimes prescribed 2.5-5-10 mg daily for 5 days. Active ingredients affect the division of malignant tissues without harming healthy cells. The use of the drug helps to achieve a long-term remission.

For psoriasis and mycosis

To prescribe the drug in the treatment of psoriasis or mycosis in chronic stage the patient should have a skin lesion of at least 20% and a decrease in the sensitivity of the pathogenic flora to other medicines local action or photochemistry. For psoriasis, tablets are prescribed in dosages up to 25 mg per week. For fungal mycosis of the skin or nails, solutions are used that are administered 50 mg once intramuscularly.

Treatment of neuroleukemia

The method of administration of Methotrexate in neuroleukemia is intralumbar injections and head irradiation in doses up to 2400 rad. The drug is administered 1-2 times every 7 days in dosages of 12 mg per m2 of body area. In the presence of extraosseous foci of autoimmune inflammation, which provoke the appearance of a severe pain syndrome and compress nearby organs, local radiation therapy is additionally performed with dosages of 500-2500 rad.

special instructions

The drug can only be prescribed by an oncologist who has experience in chemotherapy. The patient must be informed in advance of the risk of developing severe adverse reactions that can lead to disability and death. If a patient has fluid in the abdominal or pleural cavity it must be removed before starting treatment. If symptoms of stomatitis appear, the use of this medication should be discontinued. Before you prescribe Methotrexate, you need to do blood tests.

If an operation is necessary, the drug should be canceled 1 week before the scheduled date of surgical interventions and resumed after 14 days. Women of reproductive age should be informed about the negative impact of the components of the drug on the fetus and recommended effective means contraception. During treatment, it is necessary to approach with caution the performance of work that requires increased concentration.

During pregnancy

This medication has toxic properties, can adversely affect the course of pregnancy, cause congenital deformities in a child or fetal death. In situations where a woman becomes pregnant while taking medication, the question of terminating the pregnancy should be raised. The components of the drug can accumulate in the body and pass into breast milk, so for the duration of treatment it is worth stopping breastfeeding.

In childhood

In pediatrics, this medication is prescribed with caution when the risks of complications without treatment exceed the chance of side effects. The dosage of the drug is selected individually, based on the age of the sick child:

• newborns and infants up to 12 months - up to 6 mg;
• children 1-2 years old are prescribed up to 8 mg;
• a child of 2-3 years old is recommended to give up to 10 mg;
• the optimal dosage for children older than three years of age is 12 mg.

methotrexate and alcohol

To reduce the risk of liver damage, it is not recommended to use Methotrexate, alcohol, and those drugs that have increased hepatotoxicity at the same time. Neglect of this rule can lead to liver damage and unexpected immune reactions. In addition, at the time of treatment, it is worth abandoning the funds. traditional medicine that use alcohol or its derivatives.

drug interaction

On the day of taking Methotrexate, experts recommend abandoning those drugs that relieve autoimmune inflammation. You can take NSAIDs on all other days of the week. The instructions for use of the drug also indicate the following drug combinations and their consequences:

• oral administration of Tetracycline, Chloramphenicol reduces absorption;
• Phenylbutazone, loop diuretics, penicillins - increase the toxicity of the drug;
• Chloramphenicol, Pyrimethamine - negatively affect the bone marrow, disrupt the function of hematopoiesis;
• drugs that cause calcium folate deficiency, some lipid-lowering drugs and anticoagulants can increase toxicity;
• the appointment of a medication in conjunction with radiotherapy increases the risk of soft tissue necrosis;
• Amiodarone - increases the risk of ulcerative skin lesions;
• the introduction of Acyclovir - contributes to neurological lesions.

Side effects of Methotrexate

The use of the drug causes multiple negative reactions from different organs and systems:

• hematopoiesis - anemia, a decrease in the number of leukocytes, platelets;
• nervous system - fatigue, mood swings, headache, sleep disturbance, confusion, depression, metallic taste in the mouth, paralysis;
• organs of vision - conjunctivitis, irritation of the mucous membrane;
• respiratory organs - pulmonary fibrosis, bronchial asthma, pulmonary edema, dry cough;
• digestive tract - stomatitis, vomiting, anorexia, diarrhea;
• urinary system - inflammation of the bladder, impaired renal function, anuria or oliguria;
• skin - itching, vasculitis, tissue necrosis, ulcers, herpes zoster, increased skin sensitivity to sunlight, furunculosis;
• cardiovascular system - bleeding, cardiac tamponade, vasculitis;
• reproductive system - impotence, inflammation of the vagina, ulcers, menstrual irregularities, decreased libido, vaginal discharge;
• other manifestations are muscle pain, fever, diabetes, cerebellar dysfunction, exacerbation of chronic infections.

Overdose

In case of accidental or intentional administration of an overdose of the drug, the main symptom of an overdose is a violation of the function of hematopoiesis. In such situations, an antidote, calcium folinate, is urgently administered. In this case, the injection must be made no later than an hour later. The dosage of the antidote should be equal to or greater than the administered dose. In severe cases, it is necessary to carry out the procedure of hydration of the body, to drain the cerebrospinal fluid.

Contraindications

Do not take the drug to patients with severe liver / kidney damage, people diagnosed with tuberculosis or HIV infection, with ulcers of the gastrointestinal tract. It is forbidden to take the medication together with large doses of acetylsalicylic acid, after vaccination with live vaccines. Be wary appoint when:

• obesity
• diabetes;
• infectious diseases of a viral or bacterial nature;
• herpes zoster;
• ascites;
• measles;
• amoebiasis;
• chicken pox;
• gout;
• inflammatory processes oral mucosa or gastrointestinal tract;
• strongyloidiasis.

Terms of sale and storage

The drug is dispensed from pharmacies only by prescription from a doctor. Store the medication at a temperature of 15 to 25 degrees in a place closed from direct sunlight and moisture. Shelf life - 3 years.

Analogues

In the absence of a medicine in a pharmacy or intolerance to one of its components, the doctor may prescribe analogues. These may be drugs that are similar in structural structure or medicinal effect. The list of analogue drugs includes the following medicines:

• Evetrex;
• Zeksat;
• Vero Methotrexate;
• Emteksat;
• Trexan;
• Methodject;
• Metatab.

What is the difference between Methoject and Methotrexate

If we compare these two drugs in terms of composition and principle of action on the human body, then there is no significant difference between the drugs. However, judging by the feedback from patients, Methotrexate from the Austrian company Ebewe has less toxicity and side effects. In addition, there is a slight difference in the form of release of these drugs. So, Metoject is produced only in the form of a clear solution and is intended for injection under the skin, muscle or vein. Medicines are priced the same.

Methotrexate price

You can buy this drug at any public or private pharmacy. The cost of the drug varies depending on the region of sale, the manufacturer's company and the form of release. Approximate prices for the drug in Moscow are shown in the table.

If translated literally from Greek, it means a state of inflammation. The question of what factors provoke the development of this disease is still not clear. Indirect information that the number of leukocytes in the blood increases and increases makes it possible to conclude that the process of disease development is of an infectious nature. It is believed that the impetus for the development of the disease is an infection that provokes disturbances in the functioning of the immune system. However, not everyone is subject to this, but only those who have a hereditary predisposition. The result of the introduction of this infection into the human body is the formation of immune complexes (from viruses, antibodies, etc.), which accumulate in tissues and lead to joint damage.

In most cases, the treatment of this formidable disease is to alleviate pain, slowing down the course of the disease and in restoring damage (as far as possible in each case) using surgical methods.

There are a lot of them at the moment. One of these is methotrexate. With rheumatoid arthritis (reviews from health workers and patients confirm this information), the mentioned medication is quite effective, the results of its influence will be felt for quite a long time.

Composition and principle of action

The main active ingredient of the drug is methotrexate. This is a nitostatic, antagonist. Currently, to slow down the development of rheumatoid arthritis, treatment with methotrexate is used more often than other methods. In essence, this medication is an antitumor, cytostatic agent, inhibits mitosis (indirect cell division), slows down the growth of actively proliferating tissues, and inhibits the development of tumors.

According to statistics, the effectiveness of the drug is observed in 80% of patients, a positive trend becomes noticeable 2-6 weeks after the start of the course of therapy. After a long time of treatment (up to 5 years), methotraxate therapy is canceled much less frequently than any other medications used to slow the development of rheumatoid arthritis.

Forms of release of the drug

The medication itself is the Russian analogue of the Austrian Methotrexate Ebewe. The manufacturer offers the original drug to its customers in several forms of release. Tablets go on sale in three dosages: 2.5 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 - 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 medicine 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

Indications for the use of the drug are quite specific, since its main purpose is the 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, mycosis fungoides and psoriasis (in severe stages).

Also, if other treatments and drugs do not have a noticeable effect, Methotrexate is used for rheumatoid arthritis. Reviews of rheumatologists about the drug are quite positive.

Indications for taking "Methotrexate Ebeve" are somewhat more extensive. Specialists prescribe it if the patient has malignant neoplasms of various systems and organs: lung and breast cancer, osteosarcomas and soft tissue sarcomas, ovarian and testicular tumors, Young's sarcoma, retinoblastomas and autoimmune diseases.

Who should not take medication?

It is unacceptable to take the drug to people with hypersensitivity to the main active ingredient. Methotrexate is contraindicated for pregnant women and nursing mothers. Do not prescribe the drug for existing abnormalities in the liver and kidneys, with hematological disorders (anemia, thrombocytopenia, leukopenia). You can not start treatment with medication for patients who are in the acute stage of any infectious diseases suffering from immunodeficiency syndrome. How Russian analogue, and the original "Methotrexate" (Austria) is unacceptable to give to children under three years of age.

In a number of diseases, the drug is prescribed with great care. These problems include duodenal ulcers, ulcerative colitis, with viral, fungal and bacterial infections you also need to be very careful. This group of problems also includes previous 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 hematopoietic system (leukopenia, thrombocytopenia, etc.) and the gastrointestinal tract (dyspepsia, anorexia, hepatotoxicity, pancreatitis). The nervous system can react with headaches, drowsiness, paresis, convulsions. High doses of the drug can provoke the development of encephalopathy. Possible deviations from the organs of vision and of cardio-vascular system(hypotension, pericarditis, thromboembolism).

Respiratory failure, shortness of breath, dry non-productive cough, fever may develop. On the part of the genitourinary system, there is a possibility of severe forms of nephropathy or renal failure. Possible violation of spermatogenesis and ovogenesis, decreased libido, development of infertility, impotence.

If a woman is pregnant, Methotrexate (shots, tablets, droppers) can cause miscarriage, developmental defects, or death of the fetus.

Dosing regimen of tablets

In the treatment of malignant neoplasms, the pill regimen is developed individually and depends on the scheme of chemotherapy sessions. If we are talking about the use of the drug "Methotrexate" for rheumatoid arthritis (patient reviews have positive character), then the initial dose is usually 7.5 mg once a week. You can take the entire dose at once, or you can divide it into 3 doses with a 12-hour interval.

In some cases (achieving the optimal effect), the weekly dose may be increased. However, it should not exceed 20 mg. When the desired clinical effect is achieved, the dosage should be gradually reduced to a minimum. The optimal period for the course of therapy has not been clinically identified.

Methotrexate injections

And how do injections with the drug "Methotrexate"? Injections for rheumatoid arthritis begin with a dosage of 7.5 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 by 2.5 mg, but not more than 25 mg. When therapeutic effect will be reached (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, the dosage may be gradually adjusted to maintain the optimal effect of the treatment. Clinical researches showed that Methotrexate is better absorbed and gives a minimum number of adverse responses if injections are made subcutaneously or intramuscularly.

With continuous use of Methotrexate, the initial positive therapeutic effect persists for two years. With the abolition of the drug, rheumatoid arthritis makes itself felt after 3-6 weeks.

Exceeding the permissible dose

Exceeding the permissible dose of the Russian medicine or Methotrexate Ebeve (tablets, injections, infusions) is not manifested by any specific symptoms. The fact of an overdose can be established by the level of methotrexate concentration in the blood plasma.

Treatment consists of immediate (preferably within the first hour) administration of an antidote, which is calcium folinate. The volume of the injected substance must be equal to or greater than the dose of methotrexate taken. Additional doses of calcium folinate may be prescribed by your doctor as needed. Before introducing each subsequent dose, and then every 6 hours throughout the process of eliminating the symptoms of an overdose with an antidote, the pH of the urine should be determined. Such activities will minimize the likelihood of developing nephropathy.

Also, the necessary set of measures to eliminate the consequences of an overdose of medication includes hydration of the body and alkalization of urine. These procedures will speed up the elimination of methotrexate.

Interaction with other substances and drugs

If the patient has gout and is prescribed Methotrexate or Methotrexate Ebewe, the dose of anti-gout drugs should be adjusted. The parallel use of salicylates, phenylbutazone, phenytoion, sulfonamides, a number of certain antibiotics (tetracycline, penicillin, chloramphenicol), indirect anticoagulants and lipid-lowering drugs can lead to severe intoxication, even death.

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

Hepatotoxic drugs (based on sulfasalazine, azathioprine, ethanol) increase the risk of developing hepatotoxicity, hematotoxic - hematotoxicity "Methotrexate". The parallel use of the drug and the conduct of radiation therapy procedures can provoke bone marrow suppression.

Special Instructions

Before starting treatment with Methotrexate (injections, whether tablets are used - it doesn’t matter), it is necessary to conduct a general blood test (to find out the level of platelets), biochemistry (to determine the values ​​of liver enzymes, albumin, bilirubin), make a chest x-ray. In addition, it is necessary to examine 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 development of intoxication, it is necessary to control the composition of the peripheral blood (the number of platelets and leukocytes), the functioning of the kidneys, the activity of hepatic transaminases, the level of uric acid in the blood serum. Before each use of Methotrexate, the mucous membrane of the mouth and pharynx should be checked for ulcers. The process of bone marrow hematopoiesis should be monitored at the beginning of therapy, once during the course of treatment and after its completion.

Price range

Release form (tablets, injections) and dosage are the main factors affecting the cost of Methotrexate.

The price of a pack of tablets (50 pcs.) With a dosage of 2.5 mg can range from 240 to 250 rubles. The same number of tablets with a dose of 5 mg can be purchased for an amount of 390 to 420 rubles. The packaging of the drug with the largest dosage (10 mg) will cost the buyer 530-550 rubles.

The solution for injection is much more expensive, and the price range is much wider. For example, 5 ampoules of a drug with a dosage of 50 mg / 5 ml in some pharmacies can cost about 1200-1300 rubles, in others - 4900 rubles.

Consumer opinion

There are both positive and negative opinions of patients about the drug "Methotrexate". In rheumatoid arthritis, the reviews were mostly positive (about 80% of patients felt the effectiveness in the first 1-1.5 months from the start of treatment). However, you can often hear about the negative effect of the drug on the patient's body, the development of side effects of varying severity and from different systems and organs.

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

Anticancer drug. It is used in the treatment of benign and malignant tumors.

Instructions for use:

Methotrexate is a cytostatic drug from the group of antimetabolites, folic acid antagonists. It has a pronounced immunosuppressive effect even at relatively low doses that do not have noticeable hematological toxicity. Due to this, methotrexate is more widely used as an immunosuppressive drug than other cytostatics with immunosuppressive activity.

Description of the drug Methotrexate is not intended for prescribing treatment without the participation of a doctor.

Release form and composition

Tablets

Injection

Pharmacological properties

It has antitumor and immunosuppressive effects. Particularly sensitive to the action of methotrexate are actively dividing cells of malignant tumors, as well as those of the bone marrow, embryo, mucous membranes of the oral cavity, intestines, and bladder.

After intravenous administration, it is rapidly distributed within a volume equivalent to the total volume of body fluids. The initial volume of distribution is 0.18 l / kg (18% of body weight), the equilibrium volume of distribution is 0.4-0.8 l / kg (40-80% of body weight). Communication with plasma proteins is about 50%.

When taken in therapeutic doses, regardless of the route of administration, it practically does not penetrate the blood-brain barrier (after intrathecal administration, high concentrations). It is secreted into breast milk, passes through the placenta (has a teratogenic effect on the fetus).

It is metabolized mainly in liver cells with the formation of polyglutamates (inhibitors of DHF and thymidylate synthetase), which can be converted to methotrexate under the action of hydrolases.

A small amount of polyglutaminated derivatives is retained in tissues for a long time. The retention time and duration of action of these active metabolites depends on the cell type, tissue and type of tumor.

It is slightly metabolized (with the introduction of normal doses) to 7-hydroxymethotrexate (solubility in water is 3-5 times lower than that of methotrexate). The accumulation of this metabolite occurs with the introduction of high doses of methotrexate, prescribed for the treatment of osteosarcoma.

The half-life in patients receiving less than 30 mg / m2 of the drug in the initial phase is 2-4 hours. The final Tsh is dose-dependent and is 3-10 hours with the introduction of low (less than 30 mg / m2) and 8-15 hours - high doses of methotrexate (80 mg / m2 or more).

Excreted mainly by the kidneys by glomerular filtration and tubular secretion within 24 hours, less than 10% is excreted in the bile. The clearance of methotrexate varies widely, decreasing at high doses.

Excretion of the drug in patients with severe ascites or effusion into the pleural fluid is slow. At reintroduction accumulates in tissues as metabolites. In chronic renal failure, the elimination of the drug can be significantly prolonged.

Indications for the use of Methotrexate

• lympho- and myeloblastic leukemia;
• neuroleukemia;
• myeloma;
• trophoblastic tumors;
• esophageal carcinoma;
• squamous cell carcinoma of the head and neck;
• bladder cancer;
• lung cancer;
• liver cancer;
• mammary cancer;
• kidney cancer;
• cancer of the ureters;
• prostate cancer;
• cervical cancer;
• vulvar cancer;
• ovarian cancer;
• testicular cancer;
• penile cancer;
• Hodgkin's and non-Hodgkin's lymphomas (including Burkitt's lymphoma);
• mycosis fungoides (local treatment);
• non-metastatic osteogenic sarcoma.

Besides:

• rheumatoid arthritis (including Felty's syndrome);
• steroid-dependent bronchial asthma;
• Crohn's disease;
• chronic nonspecific ulcerative colitis;
• lichen planus;
• psoriasis;
• psoriatic arthritis;
• Reiter's syndrome;
• Cesari's syndrome;
• multiple sclerosis.

Dosage and administration

Doses and terms of treatment are set individually, depending on the chemotherapy regimen, indications, treatment regimen, patient's "response" and tolerability. Doses are calculated based on the body surface area or weight of the patient.

The doses used in accordance with the treatment regimens are divided:

• usual (low) doses ( single dose below 100 mg/m2);
• medium (single dose 100-1000 mg/m2);
• high (single dose above 1000 mg/m2).

Doses above 100 mg/m2 are administered only by intravenous drip and under the protection of calcium folinate. For intravenous administration the drug is diluted in a 5% dextrose solution to a concentration of 10 mg / ml.

The following dosing regimens are used:

Application features

Conception should be avoided during and after treatment with methotrexate (men - 3 months after treatment, women - at least one ovulation cycle). After a course of treatment with methotrexate, the use of calcium folinate is recommended to reduce the toxic effects of high doses of the drug. With the development of diarrhea and ulcerative stomatitis, methotrexate therapy should be interrupted and immediately consult a doctor.

Side effects

From the nervous system and sensory organs:

• encephalopathy;
• dizziness;
• headache;
• visual impairment;
• drowsiness;
• aphasia;
• back pain;
• stiffness of the muscles of the back of the neck;
• convulsions;
• paralysis;
• hemiparesis.

In some cases:

• fatigue;
• weakness;
• confusion;
• ataxia;
• tremor;
• irritability;
• coma;
• conjunctivitis;
• excessive lacrimation;
• cataract;
• photophobia;
• cortical blindness (at high doses).

From the side of the cardiovascular system:

• pericarditis;
• exudative pericarditis;
• hypotension.

Thromboembolic changes:

• arterial thrombosis;
• cerebral thrombosis;
• deep vein thrombosis;
• thrombosis of the renal vein;
• thrombophlebitis;
• pulmonary embolism.

From the side of the hematopoietic organs and the hemostasis system:

• anemia;
• leukopenia;
• thrombocytopenia;
• neutropenia;
• lymphopenia (especially T-lymphocytes);
• hypogamma globulinemia;
• hemorrhage;
• septicemia due to leukopenia.

From the respiratory system:

• interstitial pneumonitis;
• pulmonary fibrosis;
• exacerbation of lung infections.

From the digestive tract:

• gingivitis;
• pharyngitis;
• ulcerative stomatitis;
• anorexia;
• nausea;
• vomit;
• diarrhea;
• difficulty swallowing;
• melena;
• ulceration of the gastrointestinal mucosa;
• gastrointestinal bleeding;
• enteritis;
• liver damage;
• fibrosis and cirrhosis of the liver.

From the genitourinary system:

• cystitis;
• nephropathy;
• azotemia;
• hematuria;
• hyperuricemia or severe nephropathy;
• dysmenorrhea;
• unstable oligospermia;
• violation of the process of oogenesis and spermatogenesis;
• malformations of the fetus.

From the side of the skin:

• skin erythema;
• hair loss (rare);
• photosensitivity;
• ecchymosis;
• acne rash;
• furunculosis;
• peeling;
• de- or hyperpigmentation of the skin;
• blistering;
• folliculitis;
• telangiectasia;
• toxic epidermal necrolysis;
• Stevens-Johnson syndrome.

Allergic reactions:

• fever;
• chills;
• rash;
• hives;
• anaphylaxis.

Others:

• immunosuppression;
• opportunistic infection;
• osteoporosis;
• vasculitis.

Interaction with other drugs

Contraindications

• hypersensitivity;
• immunodeficiency;
• anemia (including hypo- and aplastic);
• leukopenia;
• thrombocytopenia;
• leukemia with hemorrhagic syndrome;
• liver or kidney failure;
• effusion in the pleural cavity;
• ascites;
• oppression of bone marrow function;
• chickenpox (including recently transferred);
• stomatitis;
• ulcerative colitis.

Contraindicated during pregnancy (may cause fetal death or cause congenital deformities). For the duration of treatment should stop breast-feeding.

Overdose

There are no specific symptoms of overdose. In case of intentional or accidental intake of doses exceeding the recommended ones, as well as in case of obvious symptoms of side effects, you should immediately consult a doctor.

Terms and conditions of storage

Terms of dispensing from pharmacies

Released by prescription.

Methotrexate analogs

Analogues are the following drugs:

• Vero-Methotrexate;
• Methotrexate Teva;
• Methotab;
• Methodject;
• Zeksat.

The price of Methotrexate

You can buy Methotrexate tablets and injection solution in pharmacies at a price of 169–597 rubles.