Methotrexate for injection

Tetrahydrofolate is an important coenzyme for synthesizing purine nucleotides and pyrimidine deoxynucleotides in the body. As a folate reductase inhibitor, this product mainly inhibits dihydrofolate reductase and prevents dihydrofolate from being reduced to physiologically active tetrahydrofolate, thereby hindering the transfer of one-carbon groups in the biosynthesis of purine nucleotides and pyrimidine nucleotides, resulting in the inhibition of DNA biosynthesis. In addition, this product also has an inhibitory effect on thymic nucleotide synthetase, but its effect on inhibiting RNA and protein synthesis is weaker. This product mainly acts on the S phase of the cell cycle and is a cell cycle-specific drug. It also has a delaying effect on cells in the G1/S phase, but its effect on G1 phase cells is weaker.

The main ingredient of this product is methotrexate. Its chemical name is L-()-N-［4-［［(2,4-diamino-6-pterygium]methyl］methylamino］benzoyl）glutamic acid.

1. All types of acute leukemia, especially acute lymphocytic leukemia; malignant lymphoma, non-Hodgkin's lymphoma and mycosis fungoides, multiple myelopathy. 2. Malignant hydatidiform mole, choriocarcinoma, breast cancer, ovarian cancer, cervical cancer, testicular cancer. 3. Head and neck cancer, bronchial lung cancer, various soft tissue sarcomas. 4. High doses are used for osteosarcoma, intrathecal injection can be used to prevent and treat meningeal leukemia and nerve invasion of malignant lymphoma, this product also has a certain effect on psoriasis.

1 This product is dissolved in 2 ml of water for injection and can be used for intravenous, intramuscular, arterial, and intrathecal injection. 2 For acute leukemia: intramuscular or intravenous injection, 10-30 mg each time, 1-2 times a week; children 20-30 mg/m2 per day, once a week, or depending on the bone marrow condition. 3 For choriocarcinoma or malignant hydatidiform mole: 10-20 mg per day, or dissolved in 500 ml of 5% or 10% glucose injection solution for intravenous drip, once a day, 5-10 times as a course of treatment. Total amount 80mg-100mg. 4 For meningeal leukemia: intrathecal injection of methotrexate is generally 6 mg/m2 each time, 5-12 mg is commonly used for adults, and the maximum is not 12 mg, once a day, 5 days as a course of treatment. When used to prevent meningeal leukemia, 10-15 mg per day, once a day, once every 6-8 weeks. 5 For solid tumors (1) Intravenous generally 20 mg/m2/time. (2) Interventional therapy is also possible. (3) High-dose folic acid is used to treat certain tumors. The treatment plan is determined by the physician based on the tumor, such as osteosarcoma.

1. Bone marrow suppression: leukopenia, thrombocytopenia, anemia, decreased immunoglobulin, multiple bleeding, sepsis. These side effects are related to the dose and duration of use. 2. Skin system: erythema, itching, urticaria, photosensitivity, depigmentation, ecchymosis, capillary dilation, acne and furunculosis. At the same time, the skin lesions of psoriasis may be aggravated after ultraviolet irradiation. Hair loss may also occur, but it can usually regenerate. 3. Digestive system: gingivitis, pharyngitis, gastritis, nausea, anorexia, vomiting, diarrhea, hematemesis, black stools, gastrointestinal ulcers and bleeding, enteritis. Liver toxicity can manifest as acute liver atrophy and necrosis, fatty degeneration, portal vein fibrosis or cirrhosis. 4. Urinary system: renal failure, azotemia, cystitis, hematuria, reduced eggs or sperm, short-term semen reduction, irregular menstruation, infertility, miscarriage, fetal congenital defects and severe kidney disease. 5. Central nervous system: headache, dizziness, blurred vision, aphasia, mild hemiplegia and convulsions may occur. 6. Other pneumonia, metabolic changes, aggravation of diabetes, osteoporosis, abnormal changes in tissue cells, and even sudden death have been reported.

Methotrexate is contraindicated in the following cases: patients with impaired renal function, pregnant women, malnutrition, poor liver and kidney function, or those with blood diseases such as leukopenia, thrombocytopenia, anemia and bone marrow suppression.

When methotrexate is displaced from protein binding sites by other drugs, potential drug-toxic interactions may occur, including salicylates, nonsteroidal anti-inflammatory drugs, sulfonamides, and phenytoin. Oral antibiotics, such as tetracycline, chloramphenicol, and nonabsorbable broad-spectrum antibiotics, may reduce intestinal absorption of methotrexate or interfere with enterohepatic circulation by inhibiting intestinal flora or inhibiting drug metabolism by bacteria. It has been reported that the combination of methotrexate and some drugs can change the cellular uptake rate of methotrexate, so patients can only use other drugs approved by their oncologists while receiving methotrexate. These drugs include hydrocortisone succinate, cephalosporin I, methylprednisolone, asparaginase, bleomycin, penicillin, kanamycin, vincristine, and vinblastine. Probenecid can reduce renal tubular transport function, so careful monitoring should be performed when methotrexate is used in combination with probenecid. When lipid-lowering compounds (e.g., cholestyramine) are used in combination with methotrexate, their ability to bind methotrexate is greater than that of serum proteins. Penicillins and sulfonamides may reduce the renal clearance of methotrexate. Increased serum concentrations of methotrexate have been observed with associated hematologic and gastrointestinal toxicity. Close observation should be made when methotrexate is used in combination with penicillins or sulfonamides.

Keep away from light, tightly closed, in a cool place.

0.1g

Guangdong Lingnan Pharmaceutical Co., Ltd.

• Founded in:

  1991-04-12

• Address:

  No. 5, Muxi 8th Road, Xilian Town, Wujiang District, Shaoguan City

• Tax NO.:

  91440000190333956C

• Registered Funds:

  11.38 million yuan

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