Methotrexate

Description overdue on 05/29/2014

• Latin name: Methotrexate-Ebewe
• ATC code: L01BA01
• Active substance: Methotrexate (Methotrexate)
• Manufacturer: Ebewe Pharma, Austria

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• Composition
• Product form
• Pharmacological action
• Pharmacodynamics and pharmacokinetics
• Indications
• Contraindications
• Side effects
• Instructions for use of methotrexate (method and dosage)
• Overdose
• Cooperation
• Terms of sale
• Storage conditions
• Shelf life
• Cautions
• Analogs
• Babies
• With alcohol
• During pregnancy (and lactation)
• Reviews
• Price, where to buy

Composition

AT solution   contains Methotrexate   in an amount of 10 mg in 1 ml, in Injection Concentrate   100 mg per 1 ml; Additional components: sodium hydroxide, water for injection, sodium chloride.

Pills   contains   Methotrexate   in an amount of 2, 5 mg; 5 and 10 mg; in the form of additional materials - cellulose, corn starch, silicon dioxide, magnesium stearate, lactose monohydrate.

Product form

Pills   vials: 2, 5; 5 and 10 mg.

The ampules and vials of 1, 5 and 10 ml.

Concentrate   Patients in the 5, 10 and 50 ml.

Pharmacological action

The group of antimetabolites which analogue is folic acid . It shows an antitumor effect, and further has an immunosuppressive effect.

The drug slows down the repair of DNA and its synthesis, inhibits mitosis cells. By exposure methotrexate most sensitive fabric having a high proliferation ability: tumor tissue, fetal cells, bone marrow, mucosal epithelium.

When cell proliferation of malignant tissues, which normally advances per se, leads to Methotrexate dysplasia malignancies   without harming healthy tissue.

In therapy rheumatoid arthritis   effect presumably related to the mechanism of immunosuppression. Methotrexate for rheumatoid arthritis to reduce inflammation and the resulting symptoms - swelling, pain, stiffness.

When treating psoriasis   Methotrexate acts on keratinocytes plaques, which increased the rate of growth compared to the normal skin cell proliferation.

Pharmacodynamics and pharmacokinetics

The maximum concentration of methotrexate in the blood occurs within 30-60 minutes. In patients with leukemia may be fluctuations up to 3 hours.

The plasma is bound to albumin. In simultaneous reception with salicylates, chloramphenicol, sulfonamides, tetracyclines, phenytoin can be a competitive replacement.

Methotrexate blood-brain barrier does not penetrate, for that it should be administered intrathecally.

The half-life of about 6-7 hours methotrexate in the case of high dose - is increased to 17 hours.
It writes mainly (90%) by the kidneys during the day. About 10% is excreted in the bile.

In the case of severe renal impairment is prolonged excretion.

Methotrexate may accumulate in the liver, kidney and spleen in the form of metabolic products.

Indications

• trophoblastic tumor;
• neuroleukemia ;
• non-Hodgkin lymphoma , Including lymphosarcoma ;
• sharp leukemia   (myeloid and lymphocytic);
• osteogenic sarcoma   and soft tissues;
• skin cancer Cancer, lung mammary cancer , Squamous cancer, reproductive organs (male and female), bladder cancer, esophageal cancer, kidney cancer, medulloblastoma, retinoblastoma;
• severe stage of mushroom mycosis . psoriasis ;
• arthritis   psoriatic and rheumatoid, systemic lupus erythematosus, dermatomyositis, ankylosing spondylitis .

Contraindications

• severe kidney damage and liver;
• alcoholism ;
• severe infectious diseases ( tuberculosis . HIV infection );
• pathology of the hematopoietic system in history;
• vaccination with live vaccines;
• GI ulcers and oral history;
• taking high doses of acetylsalicylic acid;
• breastfeeding and pregnancy ;
• idiosyncrasy.

Methotrexate is administered cautiously in patients with lesions of the kidneys and liver, obesity , Inhibition of bone marrow hematopoiesis, diabetes , Use of pre-treatment of hepatotoxic drugs, infectious diseases of bacterial, viral, fungal origin, ascites, peritoneal and pleural effusion, dehydration, herpes zoster, previous contact with the patient herpes simplex, with Measles . varicella . strongiloidoze . amebiasis ; in the presence of gout   or urate nefrourolitiaza , Infections and inflammations of the mouth, ulcerative colitis, ulcers, vomiting, diarrhea, gastrointestinal tract obstruction, aciduria . asthenia , Chemotherapy or radiotherapy prior to treatment, elderly patients and children.

Side effects of methotrexate

Hematopoietic system: anemia . thrombocytopenia . leukopenia . pancytopenia ; very rarely - severe impairment of bone marrow function; megaloblastic anemia .

Central nervous system: fatigue, drowsiness, mood changes, headache, depression . insomnia , Confusion; rarely - cognitive impairment, paresthesia and pain in the limbs, metal taste in the mouth, paralysis and seizures, symptoms meningism .

Bodies of irritation, conjunctivitis .

Respiratory system: pneumonitis   (symptoms are cough, dry, short of breath, fever), pleural effusion, alveolitis ; rarely - bronchial asthma   or fibrotic lung disease , Thickening of the pleural sheets, pulmonary edema.

Digestive system: nausea, inflammation and ulceration of the mouth, stomatitis . dyspepsia . vomiting . anorexia , Increased transaminases, diarrhea, fibrosis and cirrhosis of the liver . steatosis .

The urinary system: inflammation and ulceration of the bladder, a violation of urination and renal function, oliguria and anuria, electrolyte imbalance.

Skin: itching, erythema . alopecia , Photosensitivity, vasculitis , Shingles, rash herpetiformis; rarely - epidermal necrolysis . Under the influence of ultraviolet radiation may increase pigmentation of nails, furunculosis . hydradenitis , Acute paronychia .

Musculoskeletal system: pain in the muscles and joints, osteoporosis .

Heart and vascular system: bleeding, vasculitis, pericardial effusion in the cavity; rarely - cardiac tamponade.

The immune system: pharyngitis , Low immunity; rarely - sepsis Increasing the number of rheumatoid nodules, anaphylactic reactions.

Reproductive system: inflammation and ulceration of the vagina; rarely - impotence , Menstrual disorders, vaginal discharge, decreased desire.

Other side effects that may occur: fever , Malaise, fever, rarely - bad zazhivlyaemost wounds. In the case of intramuscular administration can be tissue damage at the injection site ( abscess . destruction ) cyst and Polyps . lymphoma . With unknown frequency may experience metabolic disorders, diabetes.

In the case of intrathecal methotrexate may occur acutely arachnoiditis   (headache, stiff neck, fever ). In the future, there may be paresis and plegia , Violation of cerebellar functions. Chronic reactions to the intrathecal administration may be leukoencephalopathy manifested confusion, convulsions, dementia, coma, rarely - death.

Instructions for use of methotrexate (method and dosage)

Perhaps the introduction of methotrexate - Ebewe intramuscularly, intraarterially, intravenously or intrathecally. Pills   do not chew, reception before the meal.

Instructions on Methotrexate warns that the selection of dose and treatment regimens at each specific disease should be carried out strictly in accordance with the special literature.

When trophoblastic disease   administered daily to 30 mg intramuscular injection rate is 5 days. Courses repeated after 1 week, until you reach the dose of 400 mg.

Lymphomas   and leukemia   involve intravenous administration at 200-500 mg per 1 m2 once a month.

Neuroleukemia : Intrathecally administered 1 - 2 times a day, 7 days a dose of 12 mg per m2.

Children appoint the following doses:

• under 1 year to 6 mg;
• age 1 year - 8 mg;
• up to 2 years of use 10 mg;
• older than 3 years are administered 12 mg.

Methotrexate at rheumatoid arthritis   administered from the dose 7. 5 mg, 1 time per week. By indications dose increased, but no more than 20 mg per week.

With psoriasis   administered dose to 25 mg per week, intramuscularly or intravenously.

With mushroom avium   50 mg administered once a week or 2 doses intramuscularly.

Overdose

The main symptoms of overdose are signs of oppression of the hematopoietic system. An antidote is a calcium folinate Which is introduced not later than 60 minutes, but the dosage should be equal to or higher doses of methotrexate. In severe cases, use of urine alkalization and hydration.

In case of excess doses of intrathecal, along with the introduction of an antidote, provide rapid drainage of cerebrospinal fluid.

Cooperation

When alcohol abuse and taking hepatotoxic agents increases the toxic effects of methotrexate on the liver.

Simultaneous treatment with leflunamidom upconverts pancytopenia and cases hepatotoxicity .

Chloramphenicol . tetracycline   when administered orally reduce the absorption of methotrexate.

Ciprofloxacin . glycopeptides . penicillins , Loop diuretics . phenylbutazone reduced renal clearance of the drug, which increases its concentration in blood and increases the toxicity of hematopoiesis.

Also, the toxicity of methotrexate is increased by simultaneous use of salicylates and nonsteroidal anti-inflammatory drugs.

Chloramphenicol . sulfonamides . pyrimethamine have a negative effect on the bone marrow, so the combined reception with methotrexate worsens haematological disorders.

Trimethoprim   and sulfamethoxazole Which cause folate deficiency, as well as lipid-lowering agents and indirect anticoagulants may increase the toxicity of methotrexate.

Should be avoided in the treatment of high consumption of coffee, tea and sugary drinks with caffeine because it can decrease theophylline clearance .

At simultaneous reception with cytostatics decreased clearance of methotrexate.

Combination with radiotherapy   It increases the chance of tissue necrosis.

Methotrexate inhibits the immune response to vaccination And in case of administration of live vaccines probable severe reactions antigenic character.

Receiving Amiodarone   It contributes to the appearance of skin ulcers.

When administered acyclovir   and the simultaneous use of intrathecal methotrexate increased risk of neurological lesions.

Terms of sale

Prescription.

Storage conditions

The preparation is stored, keeping the temperature regime of 15-25 ° C, in a closed and dark place away from children.

Shelf life

3 years.

Cautions

The drug is prescribed only oncologist with experience Chemotherapy .

The patient must be advised of the risk of developing severe adverse reactions in the form of toxic lesions, which can lead to death.

In the case of a patient of the liquid in the cavities (pleural and peritoneal) is necessary before the treatment liquid is removed.

If symptoms stomatitis Indicating toxic shock syndrome, it is necessary to temporarily discontinue treatment with methotrexate, since the risk of ulceration and perforation of the intestine.

Before initiation of therapy requires careful study of laboratory blood parameters (detailed clinical and biochemical analysis), kidney function tests, X-rays of the chest cavity.

When methotrexate patient be kept under medical supervision for the early detection of complications.

During treatment the patient is carried out monthly surveys, which include:

• oral examination;
• full blood count;
• liver function tests;
• urine and renal function;
• the study of the respiratory system.

1 week before surgery methotrexate therapy should be canceled and re-assign 2 weeks.

The drug increases the risk of cancer lymphomas Including when taken in low doses.

Prior to treatment to exclude pregnancy.

Patients of reproductive age must be notified about the negative effects of methotrexate on the reproductive system and to recommend the use of contraception during treatment.

Intrathecal methotrexate possible complications, life-threatening, so at the first sign of side effects require removal of the drug.

The drug should not be mixed with other substances in one bottle.

In the case of contact with skin or mucous membranes must be washed off immediately with water.

At the time of treatment need to be careful when playing in which you need attention and quick reactions.

Analogs Methotrexate

Match code ATC 4th level:

• Metodzhekt
• Vero Methotrexate

The main counterparts: Vero Methotrexate . Methotrexate Teva . Metodzhekt . Metotab .

Which is better: Methotrexate or Metodzhekt?

When compared with the conventional methotrexate Metodzhekt some call it more effective, but if Methotrexate Ebewe Austria - Austrian drug is characterized by a good effect and purity, ie with fewer side effects. For the price of drugs are virtually identical.

Babies

Apply with caution.

With alcohol

Alcohol can aggravate the hepatotoxic effects of methotrexate, so use during treatment is contraindicated.

During pregnancy and lactation

Methotrexate has fetotoxic effects (causing malformations of the fetus), use during pregnancy is contraindicated.

The drug passes into breast milk in dangerous concentrations. In this connection, in the treatment of breast-feeding period is terminated.

Reviews of methotrexate

There are multiple reviews of the preparation. Almost all of the reviews at ectopic pregnancy talk about the side effects such as severe nausea, abdominal pain, sore liver. There must be sufficient monitoring of the effectiveness of getting rid of ectopic pregnancy human chorionic gonadotropin .

Reviews at psoriasis   most of them are not very good, many people prefer to do without methotrexate. Patients report that the aggravation of the drug greatly facilitates the state, but with the abolition of degradation occurs. There are references to cases toxic hepatitis .

Reviews at rheumatoid arthritis   about the effect of mostly positive. Mark on the drug-resistant remission, but at the same time and frequent side effects such as nausea. The advantage is that the cancellation condition does not deteriorate. It is important to observe the gradual increase in dosage at the start of therapy. There are also individual reviews of the low effectiveness of the drug.

Price methotrexate, where to buy

Buy Methotrexate Ebewe Austria in Moscow can be the average for 1141 rubles. in ampoules. Price tablets
It is about 415 rubles. 50 Tab. dose of 5 mg and 480 rubles. 10 mg.

Where to buy pills   in Moscow? You can buy it in pharmacies at a price from 82 to 195 rubles. depending on the dose.

The price of the drug in Ukraine is dependent on the size and number in the package and varies from 445 UAH. up to 814 UAH.

Where to buy Austrian Methotrexate in Rostov - on - Don? It has the opportunity to buy in pharmacies at an average price of 1205 rubles.

Buy in St. Petersburg, you can at a price of 106 to 269 rubles. for 1 ampoule or vial.

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