Methotrexate Tablets

width = Methotrexate is an antitumor agent, has an immunosuppressive, cytostatic and antitumor effect.

It is produced in ampoules for injection and in tablet form for oral administration.

Methotrexate-Ebwee acts on the cells of the epithelium of the bladder, malignant tumors, bone marrow, cells of the intestinal mucosa and oral cavity, embryonic cells.

Assign the drug in severe form of psoriasis, rheumatoid arthritis, trophoblastic tumors, lymphomas and leukemia, mushroom fungi in severe form.

Clinical and pharmacological group

Antitumor drug.

Conditions of leave from pharmacies

It is released on prescription.

Price list

How much does Methotrexate cost? The average price in pharmacies is at the level of190 rubles.

Form of issue and composition

Produced in several forms. One of these are pills Methotrexate, each containing, mg active ingredient and tablets Methotrexate-Ebweve with 10 mg of active substance.

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

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Pharmacological effect

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

It shows activity against rapidly growing cells. Produces some immunosuppressive effect.

Indications for use

What helps? Methotrexate is prescribed for the following diseases:

Trophoblastic disease.
Acute lymphatic leukemia.
Mushroomed mycosis in severe stages.
Rheumatoid arthritis (in case of ineffectiveness of other methods of treatment).
Heavy forms of psoriasis (if inadequate therapy is ineffective).
Soft-cell and osteogenic sarcoma, Ewing's sarcoma.
Germinogenic tumors of the ovaries and testes.
Medulloblastoma, retinoblastoma, lymphogranulomatosis.
Cancer of the skin, vulva and cervix, breast, cancer of the 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 while reducing the number of platelets;
immunodeficiency syndrome;
during vaccination with live vaccines;
hypersensitivity to the main active ingredient or ancillary components;
severe disturbances in kidney and liver function;
decrease in the number of leukocytes per unit volume of blood;
alcohol addiction.

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

oppression of bone marrow hematopoiesis;
diabetes;
ulcerative diseases of the digestive tract;
lactose intolerance.

The drug is not used in children's practice for up to 3 years.

Use in pregnancy and lactation

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

Methotrexate is excreted in breast milk, for the entire course of treatment breastfeeding should be discontinued.

Dosage and route of administration

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

Rheumatoid arthritis:

The initial dose is usually 7.5 mg once a week, which is taken at one time or divided into three doses at an interval of 12 hours. To achieve the optimal effect, a weekly dose can be increased, while it should not exceed 20 mg. When the optimal clinical effect is achieved, the dose should be reduced before reaching the lowest effective dose. The optimal duration of therapy is not known. In juvenile chronic arthritis, a dose of 10-30 mg / m2 / week (0.3-1 mg / kg) is effective for children.

Trophoblastic tumors:

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

Acute lymphoblastic leukemia (as part of complex therapy):

at 3.3 mg / m2 in combination with prednisolone until remission, 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 per reception 2 times a week;
7.5 mg / m2 daily for 5 days.

Mushroom mycosis:

25 mg twice a week. Dose reduction or withdrawal of drug administration is determined by the patient's reaction and hematological parameters.

Psoriasis:

Therapy with methotrexate is carried out at doses of 10 to 25 mg per week. The dose is usually increased gradually, when the optimal clinical effect is achieved, a dose reduction begins before the lowest effective dose is reached.

Side effects

The severity of side effects from taking Methotrexate in all people is different.

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

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

Overdose

For an overdose of Methotrexate, specific symptomatology is not characteristic, so it is determined by the level of the active substance of the drug in the blood plasma.

As a treatment, the introduction of a specific antidote - calcium folinate - is recommended 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 renal tubules, alkalinization of urine and hydration of the organism should be carried out, leading to an accelerated elimination of the drug.

To minimize the risk of developing nephropathy due to the formation of methotrexate precipitate or its metabolites in urine, an additional determine the pH of urine before each administration and every 6 hours during the entire period of calcium folinate, used as an antidote. The latter should be continued until the plasma methotrexate concentration drops to a value not exceeding 5 μmol / L and the pH is raised to more than 7.

special instructions

Before starting or recommending methotrexate therapy, a complete general blood test should be performed to determine platelet levels, a biochemical blood test with determination liver enzymes, bilirubin, serum albumin, chest x-ray, 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 appointed by a doctor who has experience with methotrexate and is familiar with its properties and the characteristics of the action. In view of the possible development of severe and even fatal adverse reactions, patients should be fully informed of the possible risks and recommended safety measures by the physician. Patients undergoing methotrexate therapy should be monitored appropriately, so that signs of possible toxic effects and adverse reactions are identified and evaluated in a timely manner.

To timely detect symptoms of intoxication, it is necessary to monitor the state of peripheral blood (the number of leukocytes and platelets: first a day, then every 3-5 days for the first month, then once every 7-10 days, in the period of remission - once every 1-2 weeks), the activity of "liver" transaminases, renal function (urea nitrogen, creatinine clearance and / or serum creatine), the concentration of uric acid in the blood serum, periodically perform chest X-ray, examination of the oral and pharyngeal mucosa for the presence of ulceration before each application. It is recommended to monitor the state of bone marrow hematopoiesis before treatment, 1 time during the treatment period and at the end of the course.

For the objectivization of liver function, along with biochemical parameters, it is recommended that a liver biopsy be performed before beginning 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 of mild form it is usually recommended to repeat biopsy after 6 months. During initial therapy, minor histological changes in the liver are possible (minor portal inflammation and fatty changes), which is not grounds for refusal or termination of treatment, but indicates the need for caution when applying preparation.

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 of methotrexate (usually within 2 or more years) or achieving a total cumulative dose of at least 1.5 g and may lead to adverse outcome. Hepatotoxic effect can also be caused by a burdensome concomitant anamnesis (alcoholism, obesity, diabetes) and senile age. Due to the toxic effect of the drug on the liver during treatment, one should refrain from prescribing to patients other hepatotoxic drugs, except in cases of obvious need. Patients taking other hepatotoxic drugs (eg leflunomide) should be closely monitored.

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

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

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

Since methotrexate is able to influence the central nervous system (feeling tired, dizzy), patients taking the drug should refrain from driving vehicles or potentially dangerous mechanisms.

Drug Interactions

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

Simultaneous reception with leflunamide increases the incidence of pancytopenia and cases of hepatotoxicity.
With alcohol abuse and the use of hepatotoxic drugs, the toxic effect of methotrexate on the liver is increasing.
Ciprofloxacin, glycopeptides, penicillins, loop diuretics, phenylbutazone reduce the clearance of the drug in the kidneys, which increases its concentration in the blood and increases toxicity on the hematopoiesis.
Chloramphenicol, tetracycline for oral administration reduces the absorption of methotrexate.
Also the toxicity of Methotrexate is increased when used simultaneously with salicylates and non-steroidal anti-inflammatory drugs.
Trimethoprim and sulfamethoxazole, which cause folate deficiency, as well as hypolipidemic drugs and indirect anticoagulants, can increase the toxic effect of Methotrexate.
Chloramphenicol, sulfonamides, pyrimethamine have a negative effect on the bone marrow, so the combination with methotrexate exacerbates hematologic disorders.
Methotrexate inhibits the immune response to vaccination, and in the case of administration of live vaccines, severe antigenic reactions are likely.
With simultaneous admission with cytostatics, the clearance of methotrexate is reduced.
Combination with radiotherapy increases the likelihood of tissue necrosis.
The use of amiodarone contributes to the appearance of skin ulcers.
With the introduction of acyclovir and simultaneous use of methotrexate, the risk of neurologic damage is intrathecal.

It is necessary to avoid during the treatment of increased consumption of coffee, tea and sugary drinks with caffeine, as the clearance of theophylline can decrease.

Reviews

We picked up some reviews of people taking the drug Methotrexate:

Marina. She took Methotrexate for 8 months in ampoules (she pricked her prick, so she did not spoil her stomach again). First, 1 cube, e helped, by 1.5 and then 2 cubes. There were no pills, but there was no sense. While you are at home, nothing bothers you. And how will you get to work-swollen joints. And every day I drank anti-inflammatory drugs. But nothing helped, the OE creeps every month, and from 30 it increased to 41. From today on it has passed to the Harav, ochen ochen, oh look, it will be.
Larissa. I have the third stage. Methotrexate has been treated for almost a year. Now the tests are almost normal, except for ESR, which decreased by half compared to what was before the treatment. I feel quite decent, only now if I drink tablets, then my stomach hurts from them and there is absolutely no desire. Therefore I try to use only in the form of injections. The doctor says that we will soon pass to the maintenance dosage.
Ilona. My mother had a revm.ar, the first one was put on the metipred from which she could not go away = a slight improvement, a lowering of immunity, in an attempt to stop taking the fever began to boom, and doctors also prescribed methotrexate for the elderly person 20m, and the background of taking these drugs immunity fell intoxication of the body and the side effect of methotrexate thromboembolism of the pulmonary arteries from which my best mother has not come to light, check all appointments of "doctors" and weigh all pro and contra.
Lyudmila. I fell ill at the age of 29. The diagnosis was made only after two years - I drink methotrexate 15 mg once a week. I have been drinking for 10 years. Tried to cancel-joints have inflamed, iridocyclitis has begun. Methotrexate was returned and sulfasalazine was added. Against the background of taking methotrexate, anemia began. They were able to raise iron only with the help of intravenous infusion (in three years it was necessary to repeat again as iron constantly falls). I stop drinking methotrexate with sulfasalazine-joints swelling, pain infernal. Rheumatologist asked what it is possible to replace, but there seems to be no alternative. For me it's better so than to howl from the ball, it's still not life, but it also needs to go to work and the burden of being reluctant to anyone.

Analogues

Structural analogs for the active substance:

Vero Methotrexate;
Zexate;
The methodical;
Methotrexate (Emtexate);
Methotrexate for injection;
Lathema Methotrexate;
Methotrexate sodium;
Methotrexate LENS;
Methotrexate Teva;
Methotrexate Ebewe;
Treksan;
Evetrex.

Before using analogues, consult your doctor.

Storage conditions and shelf life

Shelf life of tablets Methotrexate is 3 years from the time of their manufacture. The drug should be stored in a protected light and moisture location at an air temperature of not more than + 25 ° C.