Methotrite, 10 mg/ml 0.75 ml

Psoriasis, Rheumatoid arthritis

Acute lymph leukemia, trophoblastic disease, skin cancer, cervical and vulvar cancer, esophageal cancer, squamous cell head and neck cancer, renal pelvis and urothelial cancer, osteogenic and soft cell sarcoma, Ewing’s sarcoma, lung cancer, breast cancer, testicular and ovarian germ cell tumors, liver cancer, kidney cancer, retinoblastoma, medulloblastoma, penile cancer, and lymphogranulematosis.

Severe forms of psoriasis (in case of ineffectiveness of standard therapy).

The severe form of rheumatoid arthritis (in case of ineffectiveness of standard therapy).

Active ingredient

Composition

The solution for injection is yellow, clear.

1 ml: methotrexate dinatrium 10.97 mg, which corresponds to the content of methotrexate10 mg

Ancillary substances:

sodium chloride – 7 mg,

sodium hydroxide solution 2M – 1.76 mg (22 µl),

Sodium benzoate solution 1M – to pH – 8.5±0.1,

water d/i – to 1 ml.

How to take, the dosage

It is taken orally, administered intravenously, intravenously, intralumbarly. It is established individually, depending on the indication and stage of the disease, the state of the hematopoiesis system, the scheme of anti-tumor therapy.

Interaction

Concomitant use with vitamin preparations containing folic acid or its derivatives may decrease the effectiveness of methotrexate.

Concomitant use of NSAIDs in high doses may lead to increased plasma concentrations of methotrexate and prolongation of its elimination period, as well as increased concentration of methotrexate not bound to plasma albumin, which in turn increases the toxic effects of methotrexate (especially on the GI and hematopoietic system).

In concomitant use with penicillins of methotrexate (even in low doses) it is possible to increase its toxic effects.

In concomitant use with sulfonamides, especially with co-trimoxazole, there is a risk of increased myelodepressive effects.

The use of nitrous oxide in patients receiving methotrexate may result in severe unpredictable myelodepression, stomatitis.

When concomitant use of valproic acid with methotrexate, its plasma concentrations may decrease.

Colestyramine binds methotrexate, reduces its enterohepatic recirculation, which leads to a decrease in its plasma concentrations.

Concomitant use with mercaptopurine may increase its bioavailability due to impaired metabolism during “first passage” through the liver.

Neomycin and paramomycin decrease absorption of methotrexate from the gastrointestinal tract.

In patients receiving omeprazole, increased plasma concentrations of methotrexate may occur.

In concomitant use with probenecid there may be 3-4 times increased plasma concentration of methotrexate due to decreased renal excretion.

Concomitant use of methotrexate with retinoids may increase the risk of hepatotoxic effects.

Salicylates potentiate the effects of methotrexate due to decreased renal excretion.

Methotrexate, even at low doses, may have toxic effects after tetracycline treatment.

When methotrexate and fluorouracil are administered sequentially, synergism is possible; fluorouracil administered before methotrexate may reduce its toxicity.

Cisplatin has a nephrotoxic effect and therefore may decrease renal excretion of methotrexate, resulting in increased toxicity.

There may be increased toxicity when using cyclosporine in patients who have received methotrexate.

Special Instructions

Use in liver disorders

Contraindicated in severe liver function disorders.

Performance with impaired renal function

Contraindicated in severe renal impairment.

Methotrexate should not be used in ascites, pleural effusion, gastric and duodenal ulcer, ulcerative colitis, gout or nephropathy (including history).

The use is not recommended in patients with varicella zoster (including those who have recently had it or have had exposure to it), herpes zoster and other acute infectious diseases.

Peripheral blood count, liver and kidney function and chest x-rays should be monitored before and during therapy.

When treating rheumatoid arthritis or psoriasis a detailed general blood test should be performed at least once a month, and laboratory tests of liver or kidney function at least once every 1-2 months.

When used for psoriasis, local treatment of the disease should not be interrupted. In case of overdose, the use of calcium folinate is recommended (but not later than 4 hours).

Particular caution should be exercised when concomitant use of methotrexate in high doses with drugs that have nephrotoxic effects (e.g., cisplatin) in combination antitumor therapy.

Vaccination of patients and family members is not recommended.

With caution, methotrexate should be combined (even in low doses) with acetylsalicylic acid.

The carcinogenic and mutagenic effects of methotrexate have been established in experimental studies.

Contraindications

Developed liver and/or kidney function abnormalities, leukopenia, thrombocytopenia, pregnancy. Methotrexate should not be used in immunodeficiency states.

Side effects

The digestive system: ulcerative stomatitis, anorexia, gingivitis, pharyngitis, nausea; rarely – diarrhea, melena, enteritis, pancreatitis; in individual cases (with long-term daily use) – liver necrosis, cirrhosis, fatty atrophy, periportal liver fibrosis.

Hematopoietic system disorders: leukopenia, anemia, thrombocytopenia.

CNS disorders: fatigue, dizziness; rarely – headache, aphasia, somnolence, seizures.

Reproductive system disorders: disorders of oogenesis and spermatogenesis, oligospermia, menstrual cycle disorders, decreased libido, impotence.

Urinary system disorders: hematuria, cystitis, marked renal dysfunction.

Allergic reactions: chills, decreased resistance to infection; rarely – urticaria, toxic epidermal necrolysis, Stevens-Johnson syndrome.

Dermatological reactions: skin rash, photosensitization, pigmentation disorders, telangiectasia, acne, furunculosis.

Similarities