Indications |
Intravenous Refractory colorectal malignancies Adult: 125 mg/m2 infused IV over 90 min once wkly for 4 wk followed by a 2 wk rest period. Or, 350 mg/m2 infused IV over 90 min repeated once every 3 wk. Hepatic impairment: Dose reduction may be necessary. Intravenous Metastatic colorectal cancer Adult: As 1st line treatment: 125 mg/m2 infused IV over 90 min on days 1,8,15 and 22 of a 6 wk cycle. Alternatively 180 mg/m2 infused IV over 90 min on days 1,15 and 29 of a 6 wk cycle. Hepatic impairment: Dose reduction may be necessary. Reconstitution: Dilute in 5% dextrose injection (preferred) or 0.9% sodium chloride injection to a final concentration of 0.12-2.8 mg/ml. |
Contraindications |
Inflammatory bowel disease, bowel obstruction, severe hepatic impairment. Pregnancy and lactation. |
Warnings / Precautions |
Previous pelvic/abdominal irradiation; elderly; Raised plasma-bilirubin concentration; severe myelosuppression. Avoid extravasation. |
Adverse Reactions |
Neutropenia, anaemia, thrombocytopenia; acute diarrhoea, sweating, hypersalivation, abdominal cramps, lachrymation, miosis, weakness; nausea, vomiting, alopecia and skin reactions; cardiovascular toxicity. Potentially Fatal: Fatal sepsis due to myelosuppression; severe, chronic diarrhoea. |
Drug Interactions |
Diuretics increase risks of dehydration secondary to vomiting/diarrhoea; prophylactic dexamethasone as an antiemetic may enhance lymphocytopenia; prochlorperazine may increase incidence of akathisia; antineoplastic agents (myelosuppression and diarrhoea). St John's wort, ketoconazole may reduce irinotecan exposure. See Below for More irinotecan Drug Interactions |
Mechanism of Actions |
Irinotecan, a derivative of camptothecin, works by inhibiting the enzyme topoisomerase I thereby interfering with the coiling and uncoiling of DNA during replication and causing irreparable damage. Distribution: Irinotecan is moderately bound to plasma albumin (approx 65%) and SN-38 is extensively bound (approx 95%). Metabolism: Converted to active metabolite SN-38 via hydrolysis in the liver. Excretion: Both biliary and urinary excretion. SN-38 primarily removed by glucuronidation. Elimination half life of 6-12 hr. |
ATC Classification |
L01XX19 - irinotecan ; Belongs to the class of other antineoplastic agents. Used in the treatment of cancer. |
Available As |
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Irinotecan
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Irinotecan Containing Brands
Irinotecan is used in following diseases
Drug - Drug Interactions of Irinotecan
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