Buy Generic Methotrexate (Methotrexate) 2,5 mg online

Last Updated on February 19, 2017 by Dr.Derek Fhisher

Most popular brand: Methotrexate
Active ingredient: Methotrexate
Available dosage forms: 2,5 mg

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Methotrexate – instructions for use, analogs, reviews and release form (tablets 2.5 mg, 5 mg and 10 mg injections in vials for injection Ebewe) medicament for the treatment of rheumatoid arthritis, psoriasis in adults, children and in pregnancy

In this article, you can read the instructions for use of the drug Methotrexate. Presents reviews of visitors – users of the drug, as well as the opinion of medical specialists on the use of methotrexate in their practice. Most requested actively add their own reviews of the preparation: helped or did not help to get rid of the medicine from the disease, which were observed complications and side effects may not be claimed by the manufacturer in the summary. Analogues of methotrexate in the presence of the available structural analogues. Use for the treatment of rheumatoid arthritis, psoriasis, lymphoblastic leukemia in adults, children, and during pregnancy and breastfeeding.

Methotrexate – antineoplastic, cytostatic agent group antimetabolite, inhibits dihydrofolate reductase, participating in the restoration of dihydrofolate acid to tetrahydrofolic acid (transporter of carbon fragments necessary for the synthesis of purine nucleotides and their derivatives).

It inhibits the synthesis, DNA repair and cell mitosis. Particularly sensitive to bystroproliferiruyuschie tissues: malignant tumor cells, bone marrow, embryonic cells, epithelial cells of the intestinal mucosa, urinary bladder, oral cavity. Along with antitumor possesses immunosuppressive effect.

Methotrexate + auxiliaries.

The absorption from the digestive tract when administered dose dependent: when receiving 30 mg / m2 is well absorbed, the bioavailability of the average – 50%. Absorption is reduced when receiving at doses> 80 mg / m2 (probably due to saturation). Food slows the absorption of methotrexate. When receiving therapeutic doses, regardless of the route of administration, methotrexate does not penetrate the blood-brain barrier (BBB) ​​(after intrathecal cerebrospinal fluid in high concentrations achieved). Provided with breast milk. After oral methotrexate partially metabolised by intestinal flora, the majority – in the liver (regardless of the route of administration) to form a pharmacologically active form of polyglutamic inhibiting digidrofolatreduktaeu and thymidine synthesis. Excreted unchanged in the urine mainly by glomerular filtration and tubular secretion (by intravenous administration of 80 – 90% is excreted within 24 hours), with bile output up to 10% (with a subsequent reabsorption in the intestine). For repeated administrations accumulate in tissues of metabolites.

• trophoblastic tumor;
• acute lymphoblastic and myeloid leukemia;
• neuroleukemia;
• Non-Hodgkin lkmfomy including lymphosarcoma;
• breast cancer, squamous cell carcinoma of head and neck cancer, lung cancer, skin cancer, cervical cancer, vulvar cancer, esophageal cancer, kidney cancer, bladder cancer, testicular cancer, ovarian cancer, penile cancer, retinoblastoma, medulloblastoma;
• osteosarcoma and soft tissue sarcoma;
• mycosis fungoides (advanced stage);
• severe forms of psoriasis, psoriatic arthritis, rheumatoid arthritis, dermatomyositis, lupus, ankylosing spondylitis (after failure of standard therapy).

The tablets of 2.5 mg, 5 mg and 10 mg.

The solution for injection 10 mg (injections in vials for injection).

Concentrate for solution for infusion (import firm Ebewe production Austria).

Instructions for use and dosage

Methotrexate is part of many chemotherapy regimens, and therefore when choosing the route of administration, dosage and mode of each individual case should be guided by the data of literature.

Methotrexate for Injection may be administered intramuscularly, intravenously, or intrathecally vnturiarterialno. Methotrexate tablets should be taken orally before meals, not liquid.

When trophoblastic tumors – 15 – 30 mg orally or / m daily for 5 days with an interval of more than 1 week (depending on the signs of toxicity). Either one 50 mg every 5 days with an interval longer than 1 month. Course of treatment is usually repeated 3 to 5 times to a total dose of 300 – 400 mg.

When solid tumors in combination with other anticancer drugs – 30 – 40 mg / m2 / jet 1 time per week.

When leukemia or lymphoma – 200 – 500 mg / m2 by intravenous infusion of 1 every 2 – 4 weeks.

When neuroleukemia – 12 mg / m2 intrathecally for 15 – 30 seconds 1 or 2 times per week.

In the treatment of children, the dose is adjusted depending on the age: for children up to 1 year administered 6 mg for children aged 1 year – 8 mg for children aged 2 – 10 mg, children older than 3 years – 12 mg

Before introduction should proceed with the removal of the cerebrospinal fluid in volume about equal to the volume of drug that is supposed to enter.

In the application of high-dose therapy – from 2 to 15 g / m2 in 4 – 6 – clockwise / in infusion at intervals of 1 – 5 weeks required subsequent introduction of calcium folinate which typically begin 24 hours after initiation of the infusion of methotrexate and administered every 6 hours at a dose of 3 – 40 mg / m2 (typically 15 mg / m2) or higher depending on the concentration of methotrexate in serum for 48 – 72 h.

In rheumatoid arthritis, the initial dose is usually 7.5 mg 1 time per week, which is introduced simultaneously intravenously, in / m or inside – by 2.5 mg every 12 hours (a total of 3 doses). Day optimum effect weekly dose may be increased, but it should not exceed 20 mg. When an optimal clinical effect, a dose reduction should be initiated to achieve the lowest effective dose. The optimal duration of therapy is not known.

In psoriasis inside, intramuscularly or intravenously in doses of 10 to 25 mg per week. The dose is usually build up gradually, while achieving optimal clinical effect begin to decrease the dose to achieve the lowest effective dose.

When mushroom avium / m to 50 mg 1 per week or 25 mg 2 times a week, or inside of 2.5 mg per day for several weeks or months. Dose reduction or cancellation of the administration determined the patient’s response and hematological parameters.

• leukopenia, neutropenia, lymphopenia (especially T – cells), thrombocytopenia, anemia;
• anorexia;
• nausea, vomiting;
• stomatitis;
• gingivitis;
• glossitis;
• pharyngitis;
• enteritis;
• diarrhea;
• zrozivno – ulcerative gastrointestinal lesions;
• gastro – intestinal bleeding;
• periportal fibrosis and cirrhosis of the liver;
• hepatic necrosis;
• fatty liver;
• encephalopathy (when administered multiple doses of intrathecal, radiotherapy in the skull);
• fatigue;
• weakness;
• confusion;
• tremor;
• irritability;
• cramps;
• coma;
• pain in the back;
• stiff neck;
• paralysis;
• interstitial pneumonitis;
• pulmonary fibrosis;
• aggravation of lung infections;
• cystitis;
• nephropathy;
• violation of oogenesis process of spermatogenesis;
• libido;
• impotence;
• change fertility;
• teratogenic effects;
• conjunctivitis;
• excessive lacrimation;
• cataracts;
• photophobia;
• skin erythema and / or rash;
• itching;
• abrasions;
• depigmentation or hyperpigmentation;
• acne (pimples);
• peeling skin;
• folliculitis;
• alopecia (rarely);
• rash;
• urticaria;
• anaphylaxis;
• malignant exudative erythema (Stevens – Johnson);
• toxic epidermal necrolysis (Lyell’s syndrome);
• photosensitivity;
• immunosuppression (reduced resistance to infections);
• osteoporosis;
• vasculitis.

• expressed anemia, leukopenia, neutropenia, thrombocytopenia.
• renal failure;
• liver failure;
• pregnancy;
• during breastfeeding;
• hypersensitivity to methotrexate and / or any other component of the drug.

Application of pregnancy and breastfeeding

Do not use this drug during pregnancy and breastfeeding.

Men and women of childbearing age during treatment with methotrexate and at least for 3 months should use reliable methods of contraception.

Caution should be exercised when using methotrexate.

Formulations containing preservatives (benzyl alcohol), should not be used for intrathecal and high-dose.

When high doses of methotrexate requires careful monitoring of the patient for early detection of the first signs of toxic reactions.

high-dose therapy should be performed only by experienced chemotherapist that can monitor the concentration of methotrexate in the blood plasma in a hospital under the guise of calcium folinate.

During therapy with methotrexate in high doses and high patient should be monitored pH of urine: the day of administration, and in the next 2 – 3 days the reaction of urine should be alkaline. This is accomplished in / drip in a mixture consisting of 40 mL of 4.2% sodium carbonate solution and 400 – 800 ml of isotonic sodium chloride solution, on the eve of the day of treatment, and in the next 2 – 3 days.

Treatment of elevated methotrexate and high doses should be combined with increased hydration – up to 2 liters per day.

Introduction of methotrexate at a dose of more than 2 g / m3 should be under the control of its concentration in the blood serum. The normal decline in serum methotrexate after 22 hours after administration at 2-fold compared with baseline. Increased creatinine level of more than 50% of the original content and / or an increase in bilirubin level require intensive detoxification therapy.

For the treatment of psoriasis Methotrexate is prescribed only to patients with a severe form of the disease that is refractory to other therapies.

To prevent toxicity during treatment with methotrexate should periodically blood analysis (1 per week), to determine the content of leukocytes and platelets, to carry out liver and renal function tests.

With the development of diarrhea and ulcerative stomatitis methotrexate therapy should be interrupted in order to avoid the development of hemorrhagic enteritis and death of the patient due to bowel perforation.

In patients with impaired liver function during excretion of methotrexate increased, so drug therapy should be done with extreme caution, with decreasing doses.

Impaired renal function is dose-dependent. The risk of violations increased in patients with reduced renal function or dehydration, as well as in patients receiving other nephrotoxic drugs.

Effects on ability to drive vehicles and management mechanisms

Some of the side effects of the drug may adversely affect driving ability and the performance of potentially hazardous activities that require high concentration and speed of psychomotor reactions.

With the simultaneous use of high-dose methotrexate with various nonsteroidal anti-inflammatory drugs (NSAIDs) (including aspirin and other salicylates, azapropazone, diclofenac, indomethacin, and ketoprofen) the toxicity of methotrexate can be amplified. In some cases, severe toxic effects, sometimes fatal. At observance of special precautions and appropriate monitoring of the use of methotrexate in low doses. (7.5 – 15 mg per week), particularly in the treatment of rheumatoid arthritis in combination with NSAIDs is not contraindicated

While the use of sulfonamides, sulfonylureas, phenytoin, phenylbutazone, benzoic acid, probenecid, pyrimethamine or trimethoprim, a number of antibiotics (including penicillin, tetracycline, chloramphenicol), indirect anticoagulants and lipid-lowering drugs (cholestyramine) enhanced toxicity methotrexate. The antibiotics are poorly absorbed from the gastrointestinal tract (including tetracyclines, chloramphenicol), reduce the absorption of methotrexate and disrupt its metabolism due to the suppression of normal intestinal microflora.

While the use of retinoids methotrexate, azathioprine, sulfasalazine increase the risk of hepatotoxicity. Parenteral administration of acyclovir on the background of intrathecal methotrexate increases the risk of neurological disorders.

With the simultaneous use of methotrexate with multivitamin preparations containing folic acid or its derivatives may decrease the effectiveness of methotrexate therapy.

L – asparaginase is an antagonist methotrexate.

anesthesia with the use of dinitrogen oxide during therapy with methotrexate can lead to severe unpredictable myelosuppression and stomatitis.

While the use of methotrexate, amiodarone can promote skin ulceration.

Methotrexate reduces the clearance of theophylline.

A few patients with psoriasis or mycosis fungoides treated with methotrexate in combination with PUVA – therapy (methoxsalen and ultraviolet irradiation) was identified skin cancer.

It is necessary to be careful at simultaneous application of packed red blood cells and methotrexate.

The combination of methotrexate therapy with radiotherapy may increase the risk of soft tissue necrosis.

Methotrexate may reduce the immunological response to the vaccine; while the introduction of the drug with a live vaccine may develop severe antigenic reaction.

Analogs Methotrexate drug

The structural analogs of active material:

• Vero Methotrexate;
• Zeksat;
• Metodzhekt;
• Methotrexate (Emteksat);
• Methotrexate for Injection;
• Methotrexate Lachema;
• methotrexate sodium;
• Methotrexate LENS;
• Methotrexate Teva;
• Methotrexate Ebewe;
• Treksan;
• Evetreks.

In the absence of drug analogs of active material, it is possible to follow the links below on the disease, which makes it an appropriate drug and see the existing analogues for therapeutic impact.