Tamoxifen  |     Methotrexat  |     Doxorubicin  |     Calciumfolinate  |     5 Fluorouracil  |    Cisplatin  |    Etoposid
       Carboplatin  |     Epirubicin  |     Paclitaxel
 
    Methotrexante a derivative of folic acid, belongs to class of cytotoxic agents known as antimetabolites.   It acts principally during the >S< phase of cell division,  by the competitive inhibition  of  the enzyme  dihydrofolate reductase, thus preventing the reduction of dihydrofolate to tetrahydrofolate, a necessary step in the process of DNA synthesis and cellular replication.
 
Methotrexate is used :
 
  • Antirheumatic: active rheumatoid arthritis in adults.
  • Antipsoriatic: disseminated chronic psoriasis
  • Cytotoxic: maintenance therapy in acute lymphatic leukaemia, Non-Hodgkin’s Lymphoma, Breast cancer,Choriocarcinoma
  •  
    Posology&Method of administration Tablets
     
     
  • The tablets should be taken one hour before or 1.5-2 hours after a meal.
  • Rheumatoid arthritis and psoriasis: the product should be prescribed by specialists in dermatology, rheumatology an internal medicine.
  • Psoriasis: the recommended initial dose is 2.5 mg three times per week with 12 hours interval;alternatively, one single dose of 7.5 mg once a week.
  • Rheumatoid arthritis: Initial dose of 7.5 mg per week given as a single dose.
  • For both dose regimens, the therapeutic effect is obtained usually within six weeks with the condition of the patient  improving after another 12 weeks or more. If no response has been achieved after 6-8 weeks and no toxic symptoms are observed, the dose may be increased stepwise by 2.5 mg/week.
  • Usually the optimum dose per week is between 7.5-16 mg but should not exceed 20 mg/week.
  •  
    Cytotoxic
    oral administration of methotrexate in doses up to 30 mg/m2 is possible while higher doses should be given parenterally.  Oral treatment with doses up to 20 mg/m2 per week should be used together with intravenous administration and  intrathecal CNS prophylaxis as maintenance treatment in acute lymphatic leukaemia (ALL) in children.
    Ampoules & Vials

    Adults and Children:

  • Methotrexate may be given by intramuscular, intravenous (bolus injection or infusion), intrathecal, intra-arterial and  intraventricular routes of administration. Dosages are based on the patient’s body weight or body surface area except   in  the  case  of  intrathecal  or  intraventricular  administration  when a  maximum  dose  of 15 mg  and a  maximum concentration of 5 mg/ml is recommended. Doses should be reduced in cases of haematological deficiency and hepatic or renal impairment. Larger doses ( more than 100 mg.) are usually given by intravenous infusion over periods not exceeding 24 hours.
  • Particularly when more than 150 mg/m2 are administered, the regimens are followed by the administration of calcium folinate to rescue normal cells from toxic effects. Dosage regimens for calcium folinate rescue vary, depending upon the dose of methotrexate administered. In general,up to 150 mg are usually given in divided doses,over 12-24 hours,  by intramuscular injection, bolus intravenous injection or intravenous infusion or orally, followed by 12-25 mg
     
    intramuscularly, IV, or 15 mg orally (one capsule), every six hours for the next 48 hours. Rescue therapy is usually started 8 to 24 hours after the beginning of the methotrexate infusion. One capsule (15 mg) of calcium folinate every" six hours for 48-72 hours may be sufficient when lower doses (less than 100 mg) of methotrexate were given.   The following regimens are only examples.
  • Leukaemia
  • 3.3 mg/m2 in combination with other cytotoxic agents once daily for 4-6 weeks.
  • 2.5 mg/kg every two weeks.
  • 30 mg/m2/week maintenance therapy.
  • Hight-dose regimen between 1 and 12 g/m2 (IV 1-6 h) repeated every 1-3 weeks.
  • 20 mg/m2 in combination with other cytotoxic agents once weekly.
  • Non-Hodgkin’s Lymphoma:
  • Combination therapy varies between 500 mg/m2 and 2000 mg/m2 once weekly or in three week intervals.
  • Once weekly 7500 mg/m2 IV.
  • Breast Cancer:
  • 40 mg/m2 IV in combination with other cytotoxic agents on day 1, or 1 and 3, or 1 and 8, or 3x per year.
  • Choriocarcinoma:
  • 15-30 mg daily for five days in therapy intervals of one week or more.
  • Contraindications
  • Pregnancy and lactation.
  • Significant hepatic dysfunction including fibrosis, cirrhosis, or hepatitis.
  • Significant renal dysfunction.
  • Blood dyscrasias including hypoplasia of the bone marrow, leucopenia, thrombocytopenia, anaemia.
  • Active infectious disease, evidence of immunodeficiency syndrome.
  • Known hypersensitivity to methotrexate.
  • Poor general condition.
  • Side effects
  • The most frequently reported adverse reactions include ulcerative stomatitis, leukopenia, nausea, and abdominals distress.
  • Other frequently reported adverse effects are malaise, undue fatigue, chills and fever, dizziness and decreased resistance to infection.
  • Shelf life and special precaution for storage
  • Shelf-life:   36 months.
  • Documented 4 days stability after first opening of the vial or dilution.

  • Presentation&Pack :
    Form Packing
    Tablet
    Vial
    Vial
    2.5 mgx50’s
    50 mgx5 mlx1’s
    1000 mgx10 mlx1’s




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