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irinotecan/iri·no·te·can/ (i″rĭ-no-te´kan) a DNA topoisomerase inhibitor used as the hydrochloride salt as an antineoplastic in the treatment of colorectal carcinoma.
an antineoplastic hormone.
indication It is used to treat metastatic carcinoma of the colon or rectum.
contraindications Pregnancy and known hypersensitivity to this drug prohibit its use.
adverse effects Life-threatening effects include leukopenia, anemia, and neutropenia. Other adverse effects include fever, headache, chills, dizziness, diarrhea, nausea, vomiting, anorexia, constipation, cramps, flatus, stomatitis, dyspepsia, site irritation, rash, sweating, dyspnea, increased cough, rhinitis, vasodilation, edema, asthenia, and weight loss.
irinotecanA topoisomerase-1 inhibitor and semisynthetic analogue of the natural alkaloid camptothecin, which is activated by hydrolysis in vivo to an active metabolit, SN-38, and inactivated by glucuronidation with uridine diphosphate glucoronosyltransferase 1A1 (UGT1A1). It was FDA-approved for managing colorectal carcinoma in 1994.
Severe diarrhoea, possibly leading to dehydration, requiring aggressive antidiarrhoeal management with loperamide or Lomotil; immunosuppression with severe neutropaenia; functional overdose in patients who under-express UGT1A1 and cannot clear irinotecan as quickly (e.g., those with Gilbert syndrome as normal patients).