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Indication & Dosage |
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| Oral |
| ACUTE NON-LYMPHOCYTIC (MYELOID) LEUKAEMIA, ACUTE LYMPHOBLASTIC LEUKAEMIA AND CHRONIC MYELOID LEUKAEMIA |
Child:
As a single agent chemotherapy: Initially 2 mg/kg/day, increased to 3 mg/kg/day after 4 wk if no improvement and no leukocyte or platelet depression. Alternatively, induction therapy: 60-200 mg/m2/day in 1-2 divided doses over a period of 5-20 days. Maintenance therapy: Intermittent or continuous daily doses between 60-200 mg/m2. In combination with other cytotoxic drugs: Refer to currently published protocols for dose, method and sequence of admin. Dose and duration depends on the combination of cytotoxic drug used.
Inherited deficiency of the enzyme thiopurine methyltransferase: Dose reductions needed. |
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| Oral |
| ACUTE NON-LYMPHOCYTIC (MYELOID) LEUKAEMIA, ACUTE LYMPHOBLASTIC LEUKAEMIA AND CHRONIC MYELOID LEUKAEMIA |
| Adult:
As a single agent chemotherapy: Initially 2 mg/kg/day, increased to 3 mg/kg/day after 4 wk if no improvement and no leukocyte or platelet depression. Alternatively, induction therapy: 100-200 mg/m2/day in 1-2 divided doses over a period of 5-20 days. Maintenance therapy: Intermittent or continuous daily doses between 60-200 mg/m2. In combination with other cytotoxic drugs: Refer to currently published protocols for dose, method and sequence of admin. Dose and duration depends on the combination of cytotoxic drug used. |
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| Administration |
Should be taken on an empty stomach (i.e. At least one hour before food or four hours after food). |
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| Precautions |
Renal or hepatic impairment. Inherited deficiency of thiopurine methyltransferase. Resistance to tioguanine therapy in Lesch-Nyhan syndrome. Monitor haemoglobin concentration, haematocrit, total WBC count, differential count and platelet count at least once a wk or more frequently during therapy. Discontinue treatment temporarily at first signs of unusually large decrease in leukocytes, platelets or haemoglobin. Resume therapy if leukocyte or platelet count increases or stays at an acceptable level for 2-3 days. Withhold therapy if there is worsening of LFT, jaundice, hepatomegaly, anorexia with tenderness in the right hypochondrium, or if there is evidence of toxic hepatitis, biliary stasis or severe bone marrow depression. Not recommended for maintenance therapy or long-term continuous treatments due to hepatotoxicity. |
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Potentially Life-threatening
Adverse Drug Reactions |
Myelosuppression especially leukopenia, thrombocytopenia, anaemia; hyperuricaemia; nausea; vomiting; diarrhoea; anorexia and stomatitis; rash; dermatitis; jaundice; increased risk of infections. |
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| Adverse Drug Reactions |
Hepatotoxicity, life-threatening infections due to myelosupression. |
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| Interactions |
Increased risk of heptotoxicity, portal hypertension and oesophageal varices during long-term continuous therapy with busulfan. Increased haematological toxicity with aminosalicylate derivatives (e.g. olsalazine, mesalazine or sulfasalazine), which may inhibit the thiopurine methyltransferase enzyme. May decrease phenytoin or carbamazepine levels. |
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