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At a glance

Irinotecan Hydrochloride Trihydrate is used for the treatment of colon and rectal cancer, as first-line therapy in combination with 5-fluorouracil and leucovorin, or as second-line therapy after failure of fluorouracil-based therapy.

Indications
  • Metastatic colorectal cancer (first-line with 5-fluorouracil and leucovorin)
  • Metastatic colorectal cancer after failure of fluorouracil-based therapy
Pharmacology

Irinotecan is a derivative of Camptothecin. Camptothecins interact specifically with the enzyme topoisomerase I, which relieves torsional strain in DNA by inducing reversible single-strand breaks. Irinotecan and its active metabolite SN-38 bind to the topoisomerase I-DNA complex and prevent religation of these single-strand breaks, disrupting DNA replication and causing cell death.

Dosage

Adult Dose (IV Infusion):

  • Combination Therapy (Weekly): 125 mg/m2 (90 min infusion) on days 1, 8, 15, 22; then 2 weeks off
  • Combination Therapy (Every 3 Weeks): 350 mg/m2 (30-90 min infusion) every 3 weeks
  • Combination Therapy (6-week cycle, infusional 5-FU/LV): 180 mg/m2 on days 1, 15, 29
  • Combination Therapy (6-week cycle, bolus 5-FU/LV): 125 mg/m2 on days 1, 8, 15, 22

Child Dose: Not recommended

Side effects

Common Side Effects (>30%):

  • Nausea, vomiting
  • Abdominal pain
  • Diarrhea (early and late)
  • Constipation
  • Anorexia
  • Mucositis
  • Neutropenia, leukopenia
  • Anemia, thrombocytopenia
  • Asthenia, pain, fever, infection
  • Alopecia

Serious: Grade 3-4 late diarrhea (23-31%), neutropenic fever (3%), sepsis

Use in pregnancy

Use in Pregnancy: Category D; can cause fetal harm; unsafe during pregnancy; may be used in life-threatening situations if benefits outweigh risks.

Pregnancy Category: D — always consult a doctor before taking during pregnancy.

Precautions & warnings

Precautions:

  • Irinotecan may decrease alertness, affect vision or make you feel sleepy and dizzy; do not drive if symptoms occur
  • Early diarrhea (during or shortly after infusion): transient; prevent/treat with atropine
  • Late diarrhea (>24 hours): can be life-threatening; may lead to dehydration, electrolyte imbalance, or sepsis
  • Myelosuppression: deaths due to sepsis following severe neutropenia reported
  • Patients homozygous for UGT1A1*28 allele are at increased risk for neutropenia
Overdose effects

Overdose: Overdose effects mainly myelosuppression and severe diarrhea; provide symptomatic supportive treatment; no specific antidote.

Storage conditions

Store at controlled room temperature 15° to 30°C; protect from light; keep vial in carton until time of use.

Irinotecan Hydrochloride Trihydrate — see the full informationPharmacology, precautions, pregnancy, overdose and the rest on the generic page
⚠️ This information is for educational purposes only — not a substitute for medical advice. Consult a registered physician before taking any medicine.