Irinotecan

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
  • Irinotecan 100 mg
  • Irinotecan 40 mg
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