Naprod Life Sciences


Atlanta Medicare
Full Prescribing Info
Each mL contains Methotrexate BP 100 mg, water for injection BP q.s.
Methotrexate, chemically designated as N-(4-{(2,4-Diaminopteridin 6-methyl) methylamino] Benzoyl}-L(+)-glutamic acid, is an antimetabolite used in the treatment of certain neoplastic diseases and severe psoriasis.
Pharmacology: Methorexate inhibits dihydrofolic add reductase and interferes with DNA synthesis and cellular replication. Actively proliferating tissues such as malignant cells, bone marrow, fetal cells, buccal and intestinal mucosa and cells of the urinary bladder are generally more sensitive to this effect of Methotrexate. Thus Methotrexate may impair malignant growth without irreversible without damage to normal tissues.
Antineoplastic chemotherapy: Treatment of gestation choriocarcinoma, chorioadenomadestruens, hydatidiform mole and acute lymphocytic leukemia in alone or combination with other chemotherapeutic agents.
Psoriasis: In the symptomatic control of severe, recalcitrant, disabling psoriasis that is not responsive to other forms of therapy after diagnosis has been established by biopsy and/or dermatological consultation.
Dosage/Direction for Use
Neoplastic Diseases: Methotrexate Injection B.P. (Preservative free) may be given by the intramuscular, intravenous, intra-arterial or intrathecal route.
Chorlocarcinoma and similar Trophoblastic diseases: 15 to 30 mg daily IM for 5 days, with rest periods of more than 1 weeks interposed between courses, until any manifesting toxic symptoms subside. Three to five courses usually required.
Leukemia: Methotrexate in combination with steroids is used for induction of remission of leukemias. Methotrexate in doses of 3.3 mg/m2 IV in combination with prednisone 60 mg/m2 FV7 daily has been used. When remission has been obtained, a maintenance doses of Methotrexate 30 mg/ms orally or IM twice weekly, or alternatively 2.5 mg/kg IV every 14 days may be given. The induction regime may be repeated if and when relapse occur. Acute granulocytic leukemias responds poorly to chemotherapy. Remissions are of short duration, relapses are common and resistance to treatment develops rapidly.
Meningeal Leukemia:
For the treatment of meningeal leukemia, administer 12 mg/m2 intrathecally. Dilute preservative-free Methotrexate to a concentration of 1 mg/mL with a sterile preservative-free 0.9% Sodium Chloride Inj. At intervals of 2 to 5 days and repeat until the cell count of the CSF returns to normal, may be given with close monitoring for toxicity. However, caution needs to be exercised as large doses may cause convulsions. Mainly neurological in character may occurs. The cerebrospinal fluid volume (CSF) is dependent on age and not on body surfaces area. The CSF is at 40% of the adult volume at birth and reaches the adult volume in several years. The following dose regimen is recommended for intrathecal administration of Methotrexate based on age instead of body surface area and appears to result in more consistent CSF Methotrexate concentrations and less neurotoxicity: see Table.

Click on icon to see table/diagram/image

Mycosis fungoides: Methotrexate IM doses of 50 mg once weekly or 25 mg two times weekly.
Osteosarcoma: The starting dose of Methotrexate for night dose therapy is 12 mg/m2 and may be escalated to 15 mg/m2 and given IV or IM Starting at 24 hrs after start of Methotrexate infusion, 15 mg leucovorin orally every 6 hrs for 10 doses is recommended.
Psoriasis: Weekly single IM or IV dose schedule of 10 to 25 mg per week until adequate response is achieved. Dose regimens used to treat psoriasis depending on the nature and severity of the condition. Severe uncontrolled psoriasis may respond to Methotrexate 10-25 mg per week by IM or IV.
Symptom of fatal intoxication are anorexia progressive weight loss, bloody diarrhoea, leucopenia depression and coma.
Leucovorin is indicated to diminish the toxicity and counteract the effect of inadvertently administered over dosages of methotrexate. The dose of leucovorin should be equal to or higher than the offending dose of methotrexate and should be given as soon as possible preferably within the first hours after which time it is much less effective. Leucovorin may be administered by IV infusion in doses of up to 75 mg within 12 hours. Follow by 12 mg IM every six hours for four doses.
Methotrexate can cause teratogenicity or fetal death during pregnancy and is contraindicated in pregnant women and nursing mothers as it is excreted in milk. Methotrexate is contraindicated in patients with serious renal or liver disorders, blood dyscrasias like bone marrow hypoplasia, leukopenia, thrombocytopenia or significant anemia. Patients with known hypersensitivity to Methotrexate should not receive the drug.
Special Precautions
Methotrexate should be used only by experienced physicians. Metriculous care is required in high dose regimens recommended for osteosarcoma and other neoplastic diseases and patients should be closely monitored for possible toxic reactions.
Methotrexate should be used with extreme care in patients with infection, peptic ulcer, ulcerative colitis, debility and in the very young or aged.
During the used of Methotrexate the following laboratory tests are generally advised: Hemograms and hematocrit, renal function test and urine analysis, measurements of liver enzymes and x-ray is recommended.
During methotrexate therapy and until at least three months after treatment with methotrexate, contraceptive precautions should be taken by female as well as male patients.
In the treatment of psoriasis Methotrexate restricted to patients with severe, recalcitrant disabling disease unresponsive to other forms of therapy, intoxication and death may occur.
During treatment severe leucopenia bacterial infections and bone marrow depression may occurs. When infections occurs, discontinuation of methotrexate and adequate antibacterial therapy is indicated. In case of severe bone marrow depression blood or thrombocytes transfusion may be necessary.
Use In Pregnancy & Lactation
Methotrexate can cause teratogenicity or fetal death during pregnancy and is contraindicated in pregnant women and nursing mothers as it is excreted in milk.
Adverse Reactions
The most frequently reported adverse reactions include ulcerative stomatitis, leukopenia nausea and abdominal distress. Other frequently reported adverse effects are malaise, undue fatigue, chills and fever, dizziness and decreased resistance to infection.
Other adverse reactions include: Alimentary system: Gingivitis, pharyngitis, stomatitis, anorexia, nausea, vomiting, diarrhoea, hematemesis, melena, gastrointestinal ulceration and bleeding enteritis.
CNS: Headache, drowsiness, blurred vision, aphasia hemiparesis, paresis, convulsions have been reported.
Skin: Erythematous rashes, pruritis, urticaria photosensitivity, pigmentary changes, alopecia, ecchymosis, telangiectasia, acne, furunculosis.
Urinogenital system: Renal failure, azotemia, cystitis, hematuria, menstrual dysfunction, infertility, abortion, fetal defects.
Blood: Bone marrow depression, leucopenia, thrombocytopenia, anaemia and septicaemia.
Other: Pneumonitis, arthralgia, myalgia, impotence, diabetes, osteoporosis, sudden death and anaphylaxis.
Drug Interactions
Concomitant therapy with NSAIDS and/or salicylates results in elevated and prolonged serum Methotrexate levels, resulting in deaths from severe hematologic and gastrointestinal toxicity.
Methotrexate is partially bound to serum albumin and toxicity may be increased due to displacement by salicylates, phenylbutazone, phenytoin and sulfonamides. Allopurinol may increase the incidence of cytotoxic induced bone marrow depression.
Caution For Usage
Handling and Preparation: Caution should be exercised in handling and preparing Methotrexate solutions. Should be worn two pairs of gloves and performed in a designated area (laminar flow hood). Protective gown, mask and appropriate eye protection should be worn while handling and preparing Methotrexate. If Methotrexate solution contacts the skin or mucosa, immediately wash the skin thoroughly with soap and water or rinse the mucosa with copious of water.
Disposal: Remnants of the medicinal product as well as all materials the that have been used for dilution and administration must be destroyed according to hospital standard procedures applicable to cytotoxic agents and with due regard to current laws related to the disposal of hazardous waste.
Store below 25°C.
Protect from light.
ATC Classification
L01BA01 - methotrexate ; Belongs to the class of antimetabolites, folic acid analogues. Used in the treatment of cancer.
Inj (vial) 100 mg/mL x 1's.
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