Metarthritis solution for injection 10mg/ml syringe 1.5ml with hypodermic needle

Composition

The solution for injection is yellow, transparent.

1 ml: disodium methotrexate 10.97 mg, which corresponds to a methotrexate content of 10 mg

Auxiliary substances:

sodium chloride-7 mg,

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

sodium benzoate solution 1 M-up to pH-8.5±0.1,

d/i water – up to 1 ml

Pharmacological action

Antitumor drug.

Indications

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

Severe forms of psoriasis (if standard therapy is ineffective).

Severe form of rheumatoid arthritis (if standard therapy is ineffective).

Contraindications

Severe liver and/or kidney dysfunction, leukopenia, thrombocytopenia, pregnancy. Methotrexate should not be used in immunodeficiency conditions.

Side effects

From the digestive system:  ulcerative stomatitis, anorexia, gingivitis, pharyngitis, nausea are possible; rarely-diarrhea, melena, enteritis, pancreatitis; in some cases (with prolonged daily use) – liver necrosis, cirrhosis, fatty atrophy, periportal fibrosis of the liver.

From the hematopoietic system:  leukopenia, anemia, and thrombocytopenia.

From the central nervous system:  fatigue, dizziness; rarely-headache, aphasia, drowsiness, convulsions.

From the side of the reproductive system:  disorders of oogenesis and spermatogenesis, oligospermia, menstrual disorders, decreased libido, impotence.

From the urinary system:  hematuria, cystitis, severe 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.

Interaction

When used concomitantly with vitamin preparations containing folic acid or its derivatives, the effectiveness of methotrexate may decrease.

Concomitant use of NSAIDs in high doses can lead to an increase in the concentration of methotrexate in plasma and to a prolonged period of its elimination, as well as to an increase in the concentration of methotrexate that is not associated with plasma albumins, which in turn increases the toxic effects of methotrexate (primarily on the gastrointestinal tract and hematopoietic system).

When methotrexate is used simultaneously with penicillins (even in low doses), its toxic effects may increase.

When used concomitantly with sulfonamides, especially co-trimoxazole, there is a risk of increasing the myelodepressive effect.

When nitrous oxide is used in patients receiving methotrexate, severe unpredictable myelodepression and stomatitis may develop.

When valproic acid is used simultaneously with methotrexate, its concentration in blood plasma may decrease.

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

When used concomitantly with mercaptopurine, its bioavailability may increase due to metabolic disorders during the “first pass” through the liver.

Neomycin and paromomycin reduce the absorption of methotrexate from the gastrointestinal tract.

In patients receiving omeprazole, an increase in the concentration of methotrexate in blood plasma may occur.

When used concomitantly with probenecid, a 3-4-fold increase in the concentration of methotrexate in blood plasma is possible due to a decrease in its renal excretion.

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

Salicylates potentiate the effect of methotrexate due to a decrease in its renal excretion.

After a course of treatment with tetracycline, methotrexate, used even in low doses, can have a toxic effect.

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

Cisplatin has a nephrotoxic effect and therefore can reduce the renal excretion of methotrexate, which leads to an increase in its toxicity.

Increased toxicity may occur with cyclosporine in patients treated with methotrexate.

How to take, course of use and dosage

Taken orally, administered intravenously, intralumbally.

Set individually, depending on the indications and stage of the disease, the state of the hematopoietic system, the scheme of antitumor therapy.

Special instructions

Use in patients with liver function disorders

It is contraindicated in patients with severe liver function disorders.

Use in patients with impaired renal function

It is contraindicated in patients with severe renal impairment.

Methotrexate should not be used for ascites, pleural effusion, gastric and duodenal ulcers, ulcerative colitis, gout, or nephropathy (including in the anamnesis).

It is not recommended to use in patients with chickenpox (including recently transferred or after contact with sick people), herpes zoster and other acute infectious diseases.

Before starting therapy and against the background of ongoing treatment, the picture of peripheral blood, liver and kidney function, and chest radiography should be monitored.

In the treatment of 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 should be performed 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).

When conducting combined antitumor therapy, special care should be taken when concomitant use of methotrexate in high doses with drugs that have a nephrotoxic effect (for example, with cisplatin).

It is not recommended to vaccinate patients and their families.

Caution should be exercised when combining methotrexate (even in low doses) with acetylsalicylic acid.

Experimental studies have established the carcinogenic and mutagenic effects of methotrexate.

Active ingredient

Methotrexate

Conditions of release from pharmacies

By prescription

Dosage form

solution for injection