Clinical Pharmacology Details


Methotrexate


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Indications & Dose:

Moderate to severe active rheumatoid arthritis;



7.5mg once weekly ( as a single dose or divided into three of 2.5mg given at intervals of 12 hours), adjusted according to response; max. total weekly dose 20mg.

Contraindications:

 Pleural effusion, ascites, hypersensitivity. Severe hepatic or renal impairment, severe anaemia, thrombocytopenia or leucopenia. Pregnancy. Blood count should be monitored.

Side Effects:

 Nausea, vomiting, diarrhea, anaphylaxis, hepatic necrosis, fever, bone marrow depression, osteoporosis, menstrual dysfunction, cirrhosis, pulmonary infiltrates and fibrosis, renal toxicity.

Cautions:

Precautions:

Children, GI disorders, CNS disturbance, hepatic or renal impairment, bone marrow depression. Monitor hepatic, renal and haemato- logical functions.


Breast feeding & old age: Use with caution.

Interaction:

Drugs


Aminoglycosides: Decrease absorption and AUC of oral methotrexate.


Charcoal: Decreases serum level of both oral and i.v methotrexate.


Etretinate: Hepatotoxicity.


Folic acid or its derivatives: Decrease response to methotrexate.


NSAIDs: Increase plasma levels of methotrexate which may be fatal.


Phenytoin: Serum concentration of phenytoin decreased.


Probenecid, Salicylates & Sulfornamides (including Phenylbutazone, Tetracyclines, Chloramphenicol,PABA & TMP-SMZ): Increase in efficacy as well as toxic effects of methrotrexate.


Procarbazine: Increase AUC and plasma levels of thiopurines.


Asparaginase: Reduces toxicity. Food: Reduction in plasma concentration of methotrexate.

Warnings:

Adverse Effects:

Lactations:

Special Precautions:

Counselling:

Side Effects Or Adverse Reactions:

Patient And Carer Advice: