Zexate Tablet

Methotrexate
2.5mg
Fresenius Kabi pharmaceuticals
Pack size 10's
Dispensing mode
Source
Agent
Retail Price 5.61 NPR

Indications

Zexate Tablet is used for: Burkitt's lymphoma, Choriocarcinoma, Mycosis fungoides, Crohn's disease, Psoriasis, Osteosarcoma, Breast cancer, lymphosarcoma, Acute lymphoblastic leukaemia, Rheumatoid arthritis

Adult Dose

Adult: PO Burkitt's lymphoma 10-25 mg/day for 4-8 days, repeat after 7-10 days. Choriocarcinoma 15-30 mg/day for 5 days, repeat after an interval of at least 1 wk for 3-5 courses. Mycosis fungoides 2.5-10 mg/day to induce remission. Rheumatoid arthritis 7.5 mg once wkly, adjust if needed. Up to 20 mg/wk. Crohn's disease 12.5-22.5 mg once wkly for up to 1 yr. PO/IV/IM Psoriasis 10-25 mg once wkly, adjust subsequent doses if needed. IV Osteosarcoma 12-15 g/m2 as infusion, followed by folinic acid. Breast cancer 10-60 mg/m2 often w/ cyclophosphamide and fluorouracil. Advanced lymphosarcoma Up to 30 mg/kg, followed by folinic acid rescue. Acute lymphoblastic leukaemia Maintenance: 2.5 mg/kg every 14 days. PO/IM Acute lymphoblastic leukaemia Maintenance: 15 mg/m2 1-2 times/wk w/ other agents. IM Choriocarcinoma 15-30 mg/day for 5 days. Repeat after at least 1 wk for 3-5 courses. Mycosis fungoides 50 mg/wk in 1-2 divided doses. Crohn's disease 25 mg once wkly for 16 wk. Maintenance: 15 mg/wk. Intrathecal Meningeal leukaemia 12 mg/m2 (Max: 15 mg) once wkly for 2-3 wk, then once mthly. Hepatic impairment Bilirubin 3.1-5.0 mg/dL or AST > 3 times ULN: Give 75% of dose Bilirubin >5.0 mg/dL: Avoid use

Child Dose

Polyarticular Juvenile Idiopathic Arthritis Initial: 10 mg/m² PO/IM/SC qWeek Meningeal Leukemia <1 year: 6 mg intrathecally (IT) every 2-5 days 1-2 years: 8 mg IT every 2-5 days 2-3 years: 10 mg IT every 2-5 days >3 years: 12 mg IT every 2-5 days

Renal Dose

Renal impairment: CrCl (ml/min) Dosage Recommendation 61-80 75% of dose 51-60 70% of dose 10-50 30-50% of dose <10 Avoid use Intermittent hemodialysis: 50% of dose at normal dosing interval Continuous renal replacement therapy: 50% of dose at normal dosing interval

Administration

Should be taken on an empty stomach. Best taken on an empty stomach. May be taken w/ meals to reduce GI discomfort. Avoid taking w/ milk-rich products. IV/IM Preparation Reconstitute with D5W or NS: 20-mg vial, up to 25 mg/mL; 1-g vial, up to 50 mg/mL May dilute further for IV infusion IV/IM Administration Administer by IM, IV push, or IV infusion Regular IV given with no more than 25 mg/mL IV push: Administered at 10 mg/min IV infusion (usually >100 mg): Administered over 30 minutes to 4 hours, or according to institutional protocol High-dose therapy (uses 1-g vial): Administered over 4 hours Specific dosing schemes vary, but high doses should be followed by leucovorin 24 hours after initiation of therapy to prevent toxicity

Contra Indications

Severe renal or hepatic impairment, pre-existing profound bone marrow suppression in patients with psoriasis or rheumatoid arthritis, alcoholic liver disease, AIDS, pre-existing blood dyscrasias, pregnancy (in patients with psoriasis or rheumatoid arthritis), breast-feeding.

Precautions

Hepatic or renal impairment, bone marrow depression, elderly, neonates. Ulcerative disorders of the GI tract. Monitor haematological, renal and hepatic function, and GI toxicity regularly. Lactation: Drug excreted in breast milk; do not nurse

Pregnancy-Lactation

Interactions

Decreased effectiveness with folic acid and its derivatives. Potentially Fatal: Increased toxicity with NSAIDs and salicylates; probenecid; some penicillins; aminoglycosides neomycin and paromomycin; sulfonamides such as sulfafurazole and sulfamethoxazole; co-trimoxazole or trimethoprim; nephrotoxic agents (e.g. cisplatin); ciclosporin; etretinate. Synergistic enhancement of effects with fluorouracil. Increased bioavailability of mercaptopurine. Reduces serum-valproate concentrations. Reduced serum concentrations with colestyramine. Increased serum concentrations with omeprazole.

Adverse Effects

Side effects of Methotrexate : >10% Arachnoiditis with intrathecal administration,Subacute toxicity with intrathecal administration (paralysis of extremities, cranial nerve palsy, seizure or coma),Demyelinating encephalopathy with cranial irradiation or other systemic chemotherapy,Reddening of skin,Hyperuricemia,Ulcerative stomatitis,Glossitis,Gingivitis,Nausea and vomiting,Diarrhea,Anorexia,Intestinal perforation,Mucositis (dose-dependent),Leukopenia,Thrombocytopenia,Renal failure,Azotemia,Nephropathy,Pharyngitis 1-10% Alopecia,Photosensitivity,Rash,Abdominal distress,Malaise,Fatigue,Chills, fever,Decreased resistance to infection,Gastrointestinal hemorrhage,Myelosuppression,Disorders of lung, interstitial pneumonia (acute, chronic),Atrophy of liver, cirrhosis, hepatic fibrosis or necrosis, elevated liver function tests, hepatic failure Potentially Fatal: Pulmonary reactions (e.g. interstitial lung disease); neurotoxicity (e.g. leukoencephalopathy, paresis, demyelination) with intrathecal use; foetal deaths.

Mechanism of Action

Methotrexate is a folic acid antagonist that inhibits DNA synthesis. It irreversibly binds to dihydrofolate reductase, inhibiting the formation of reduced folates, and thymidylate synthetase, resulting in inhibition of purine and thymidylic acid synthesis.

Note

Zexate 2.5mg Tablet manufactured by Fresenius Kabi pharmaceuticals. Its generic name is Methotrexate. Zexate is availble in Nepal. Farmaco Nepal drug index information on Zexate Tablet is not intended for diagnosis, medical advice or treatment; neither intended to be a substitute for the exercise of professional judgment.

Some other brands of Methotrexate :