Methotrexate-Ebeve solution for in 10mg ml 2ml
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Active ingredients
Methotrexate
Release form
Solution
Composition
1 ml methotrexate 10 mg.
Pharmacological effect
An antitumor drug from the group of antimetabolites - folic acid analogues. Along with antitumor has an immunosuppressive effect. Inhibits dihydrofolate reductase involved in the reduction of dihydrofolic acid to tetrahydrofolic acid - a carrier of carbon fragments necessary for the synthesis of purine nucleotides and their derivatives. Inhibits synthesis, DNA repair and cell mitosis (during the synthesis phase). Particularly sensitive to the action of methotrexate tissue with high cell proliferation: tumor tissue, bone marrow, mucous membrane epithelium cells, embryonic cells. When cell proliferation of malignant tissue is greater than in most normal tissues, methotrexate can lead to an abnormal growth of malignant tumors without irreversible damage to normal tissue. The mechanism of action for rheumatoid arthritis is unknown, perhaps this action is due to the immunosuppressive properties of methotrexate. In patients with rheumatoid arthritis, the use of methotrexate reduces the symptoms of inflammation (pain, swelling, stiffness), but there is a limited number of studies with long-term use of methotrexate (regarding the ability to maintain remission in rheumatoid arthritis). In psoriasis, the growth rate of keratinocytes in psoriatic plaques increases compared with normal proliferation of skin cells. This difference in cell proliferation is the basis for the use of methotrexate for the treatment of psoriasis.
Indications
- trophoblastic tumors. - acute leukemia (especially lymphoblastic and myeloblastic variants). - neuroleukemia. - Non-Hodgkin lymphomas, including lymphosarcoma. - breast cancer, squamous cell 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. - osteogenic sarcoma and soft tissue sarcoma. - mushroom mycosis (advanced stages). - severe forms of psoriasis, psoriatic arthritis, rheumatoid arthritis, dermatomyositis, SLE, ankylosing spondylitis (with the ineffectiveness of standard therapy).
Contraindications
- severe renal failure (CC less than 20 ml / min) - severe liver failure - alcohol abuse - history of the hematopoietic system (in particular, bone marrow hypoplasia, leukopenia, thrombocytopenia, or clinically significant anemia) - severe acute and chronic infectious diseases , such as tuberculosis and HIV infection — concomitant vaccination with live vaccines — oral ulcers, gastrointestinal ulcers in the active phase — simultaneous use of methotrexate in a dose of 15 8805.15 mg / week. with acetylsalicylic acid - pregnancy - lactation period - hypersensitivity to methotrexate and / or any other component of the preparationWith caution, use the drug if patients have abnormal liver and kidney function, diabetes, obesity and previous exposure to hepatotoxic drugs, dehydration, ascites, bone marrow hemorrhage , pleural or peritoneal effusion, parasitic and infectious diseases of viral, fungal or bacterial nature - the risk is developed I have a severe generalized disease (currently or recently suffered, including recent contact with a patient — herpes simplex, herpes zoster (viraemic phase), chicken pox, measles, amebiasis, strongyloidiasis (established or suspected)) of gout (including anamnesis) or uratne nephrorurolithiasis (including a history), infections and inflammations of the oral mucosa, vomiting, diarrhea, gastric ulcer and duodenal ulcer, ulcerative colitis, obstructive gastrointestinal diseases, previous chemotherapy or radiation therapy and asthenia aciduria (pH less than 7 of urine) as well as in children and elderly patients.
Use during pregnancy and lactation
Acceptance of methotrexate during pregnancy can cause serious malformations of the fetus (an increase in the incidence of malformations of the skull, cardiovascular system and limbs 14 times), therefore Methotrexate-Ebeve is contraindicated during pregnancy. If pregnancy occurs during methotrexate treatment, you should consult with specialists about the risk of adverse effects of methotrexate on the fetus.Patients of reproductive age (both women and men) should use effective contraceptive methods during and at least 6 months after the end of treatment with Methotrexate-Ebev. Methotrexate passes into breast milk in concentrations that are dangerous to the infant. Therefore, during the period of treatment with methotrexate, breastfeeding should be stopped.
Dosage and administration
Methotrexate is a part of many chemotherapeutic treatment regimens, and therefore in choosing the route of administration, regimen and doses in each individual case, one should be guided by the data of special literature. Methotrexate-Ebeve for injection can be injected in a / m, in / in, in / a or intrathecal. When trophoblastic tumors - 15-30 mg / m, daily for 5 days with an interval of & # 8805 .1 week (depending on signs of toxicity). Or 50 mg 1 time in 5 days with an interval of at least 1 month. The course of treatment is usually repeated from 3 to 5 times to a total dose of 300-400 mg. For solid tumors in combination with other anticancer drugs - 30-40 mg / m2 w / w jet once a week. For leukemia or lymphomas, 200-500 mg / m2 by IV infusion every 2-4 weeks. With neuroleukemia, 12 mg / m2 intrathecally for 15-30 seconds, 1 or 2 times a week. When treating children, the dose is selected depending on age: children under the age of 1 year are prescribed 6 mg, children at the age of 1 year - 8 mg, children at the age of 2 years - 10 mg, children over 3 years old - 12 mg. Before the administration, the cerebrospinal fluid should be removed in a volume approximately equal to the volume of the medicinal product to be introduced. When using high-dose therapy, from 2 to 15 g / m2 in the form of a 4-6 hour intravenous infusion with an interval of 1-5 weeks with a mandatory subsequent administration of calcium folinate, which usually starts 24 hours after the start of the infusion of methotrexate and is administered every 6 hours at a dose of 3-40 mg / m2 (usually 15 mg / m2) and higher, depending on the serum concentration of methotrexate for 48-72 hours. In rheumatoid arthritis, the initial dose is usually 7.5 mg once a week, which is administered simultaneously in / in, in / m 2.5 mg every 12 hours (only 3 doses). To achieve an optimal effect, the weekly dose may be increased, but it should not exceed 20 mg. When the optimal clinical effect is achieved, the dose should be reduced to the lowest effective dose. The optimal duration of treatment is unknown. With psoriasis in the / m or / in the jet in doses of 10 to 25 mg per week.The dose is usually increased gradually, when the optimal clinical effect is reached, the dose reduction begins until the lowest effective dose is reached. For fungal mycosis i / m, 50 mg once a week or 25 mg 2 times a week for several weeks or months. Dose reduction or withdrawal of the drug is determined by the patient's response and hematological parameters.
Side effects
According to WHO, undesirable effects are classified according to their frequency of development as follows: very often (& # 8805 .1 / 10), often (from & # 8805 .1 / 100 to less than 1/10), infrequently (from & # 8805 .1 / 1000 to less than 1/100), rarely (from & # 8805 .1 / 10 000 to less than 1/1000), very rarely (less than 1/10 000). frequency is unknown - according to the available data it was not possible to establish the frequency of occurrence. On the part of the blood system: often - inhibition of bone marrow function (leukopenia, thrombocytopenia, anemia). infrequently - pancytopenia. very rarely - severe progressive depression of bone marrow function, agranulocytosis. frequency unknown - megaloblastic anemia. From the side of the central nervous system: often - drowsiness, headache, fatigue. infrequently - depression, confusion, mood changes. rarely - with the use of low-dose methotrexate - transient small cognitive impairment, unusual sensations in the skull. very rarely - pain, myasthenia gravis or paresthesias in the limbs, taste perversion (metallic taste in the mouth), seizures, meningism, paralysis, insomnia. From the senses: often - visual impairment. infrequently - eye irritation. rarely - conjunctivitis. On the part of the respiratory system: often - chronic interstitial pneumonitis (symptoms indicative of potentially serious lung damage in interstitial pneumonitis: dry, nonproductive cough, shortening of the breath, fever). infrequently - alveolitis, pleural effusion. rarely - pulmonary fibrosis, pneumocystic pneumonia, bronchial asthma. very rarely - pleural pain and thickening of the pleura (with high-dose methotrexate treatment), acute pulmonary edema. On the part of the digestive system: very often - stomatitis, nausea, inflammation of the mucous membranes, loss of appetite, dyspepsia, anorexia, a significant increase in the activity of hepatic transaminases. often - diarrhea, ulceration of the oral mucosa. infrequently - enteritis, vomiting, liver cirrhosis, liver fibrosis, liver steatosis. rarely - ulceration of the gastrointestinal mucosa. very rarely - malabsorption syndrome, toxic megacolon.On the part of the urinary system: infrequently - inflammation and ulceration of the bladder, renal dysfunction, urinary disorders. rarely - renal failure, oliguria, anuria, electrolyte imbalance. For the skin: often - rash, erythema, itching. infrequently - photosensitivity, alopecia, shingles, vasculitis, herpetiform skin rash, urticaria. rarely - increased pigmentation. very rarely - Stevens-Johnson syndrome, epidermal necrolysis (Lyell's syndrome). When exposed to ultraviolet radiation, increased psoriatic skin lesions, increased nail pigmentation, acute paronychia, furunculosis and hydradenitis. From the musculoskeletal system: infrequently - arthralgia, myalgia, osteoporosis. Since the cardiovascular system: often - vasculitis, bleeding of different localization. infrequently, effusion into the pericardial cavity. rarely - cardiac tamponade, nasal bleeding. On the part of the immune system: very often - reduction of resistance to infections, pharyngitis. infrequently - hypogammaglobulinemia. rarely sepsis. very rarely - anaphylactic reactions, an increase in the number of rheumatoid nodules. Reproductive system: Infrequent: ulceration and inflammation of the vagina. very rarely - loss of libido, impotence, oligospermia, menstrual disorders, vaginal discharge. Other: often - chills, malaise, fever, necrosis. rarely, impaired wound healing. With the / m injection - a burning sensation or tissue damage (the formation of a sterile abscess, the destruction of adipose tissue) at the injection site. very rarely, benign, malignant and non-specific neoplasms (including cysts and polyps), lymphomas, which in some cases regress after discontinuation of methotrexate. frequency is unknown - diabetes, other metabolic disorders, sudden death. Adverse reactions with intrathecal administration of methotrexate Acute: a chemical arachnoiditis, manifested by headache, pain in the back or shoulders, stiffness of the muscles of the back of the neck and fever. Subacute: paresis (usually transient), paraplegia, cerebellar dysfunction. Chronic: leukoencephalopathy, manifested by irritability, confusion, ataxia, muscle plasticity, sometimes convulsions, dementia, drowsiness, coma,in rare cases with a fatal outcome. When combining radiation therapy to the region of the skull and intrathecal administration of methotrexate, the incidence of leukoencephalopathy increases.
special instructions
According to WHO, undesirable effects are classified according to their frequency of development as follows: very often (& # 8805 .1 / 10), often (from & # 8805 .1 / 100 to less than 1/10), infrequently (from & # 8805 .1 / 1000 to less than 1/100), rarely (from & # 8805 .1 / 10 000 to less than 1/1000), very rarely (less than 1/10 000). frequency is unknown - according to the available data it was not possible to establish the frequency of occurrence. On the part of the blood system: often - inhibition of bone marrow function (leukopenia, thrombocytopenia, anemia). infrequently - pancytopenia. very rarely - severe progressive depression of bone marrow function, agranulocytosis. frequency unknown - megaloblastic anemia. From the side of the central nervous system: often - drowsiness, headache, fatigue. infrequently - depression, confusion, mood changes. rarely - with the use of low-dose methotrexate - transient small cognitive impairment, unusual sensations in the skull. very rarely - pain, myasthenia gravis or paresthesias in the limbs, taste perversion (metallic taste in the mouth), seizures, meningism, paralysis, insomnia. From the senses: often - visual impairment. infrequently - eye irritation. rarely - conjunctivitis. On the part of the respiratory system: often - chronic interstitial pneumonitis (symptoms indicative of potentially serious lung damage in interstitial pneumonitis: dry, nonproductive cough, shortening of the breath, fever). infrequently - alveolitis, pleural effusion. rarely - pulmonary fibrosis, pneumocystic pneumonia, bronchial asthma. very rarely - pleural pain and thickening of the pleura (with high-dose methotrexate treatment), acute pulmonary edema. On the part of the digestive system: very often - stomatitis, nausea, inflammation of the mucous membranes, loss of appetite, dyspepsia, anorexia, a significant increase in the activity of hepatic transaminases. often - diarrhea, ulceration of the oral mucosa. infrequently - enteritis, vomiting, liver cirrhosis, liver fibrosis, liver steatosis. rarely - ulceration of the gastrointestinal mucosa. very rarely - malabsorption syndrome, toxic megacolon.On the part of the urinary system: infrequently - inflammation and ulceration of the bladder, renal dysfunction, urinary disorders. rarely - renal failure, oliguria, anuria, electrolyte imbalance. For the skin: often - rash, erythema, itching. infrequently - photosensitivity, alopecia, shingles, vasculitis, herpetiform skin rash, urticaria. rarely - increased pigmentation. very rarely - Stevens-Johnson syndrome, epidermal necrolysis (Lyell's syndrome). When exposed to ultraviolet radiation, increased psoriatic skin lesions, increased nail pigmentation, acute paronychia, furunculosis and hydradenitis. From the musculoskeletal system: infrequently - arthralgia, myalgia, osteoporosis. Since the cardiovascular system: often - vasculitis, bleeding of different localization. infrequently, effusion into the pericardial cavity. rarely - cardiac tamponade, nasal bleeding. On the part of the immune system: very often - reduction of resistance to infections, pharyngitis. infrequently - hypogammaglobulinemia. rarely sepsis. very rarely - anaphylactic reactions, an increase in the number of rheumatoid nodules. Reproductive system: Infrequent: ulceration and inflammation of the vagina. very rarely - loss of libido, impotence, oligospermia, menstrual disorders, vaginal discharge. Other: often - chills, malaise, fever, necrosis. rarely, impaired wound healing. With the / m injection - a burning sensation or tissue damage (the formation of a sterile abscess, the destruction of adipose tissue) at the injection site. very rarely, benign, malignant and non-specific neoplasms (including cysts and polyps), lymphomas, which in some cases regress after discontinuation of methotrexate. frequency is unknown - diabetes, other metabolic disorders, sudden death. Adverse reactions with intrathecal administration of methotrexate Acute: a chemical arachnoiditis, manifested by headache, pain in the back or shoulders, stiffness of the muscles of the back of the neck and fever. Subacute: paresis (usually transient), paraplegia, cerebellar dysfunction. Chronic: leukoencephalopathy, manifested by irritability, confusion, ataxia, muscle plasticity, sometimes convulsions, dementia, drowsiness,coma, in rare cases with a fatal outcome. When combining radiation therapy to the region of the skull and intrathecal administration of methotrexate, the incidence of leukoencephalopathy increases.