Absorption: IV administration results in complete bioavailability.
Distribution: Unknown.
Protein Binding: Irinotecan 3068%; SN38 (active metabolite) 95%.
Metabolism/Excretion: Converted by the liver to SN38, its active metabolite, which is metabolized by the liver by UDP-glucuronosyl 111 transferase 1A1 (UGT1A1) and CYP3A4. Small amounts excreted by kidneys.
Half-life: 6 hr.
Contraindicated in:
Use Cautiously in:
65 yr (↑ risk of myelosuppression)CV: edema, vasodilation.
Derm: alopecia, rash, sweating.
EENT: rhinitis.
F and E: dehydration.
GI: DIARRHEA, ↑LIVER ENZYMES, abdominal pain/cramping, anorexia, constipation, dyspepsia, flatulence, nausea, stomatitis, vomiting, abdominal enlargement, colonic ulceration.
GU: ↓fertility, menstrual abnormalities.
Hemat: neutropenia, anemia, leukopenia, thrombocytopenia.
Local: injection site reactions.
Metab: weight loss.
Neuro: dizziness, headache, insomnia, weakness.
Resp: INTERSTITIAL LUNG DISEASE, coughing, dyspnea.
Drug-Drug:
1 wk before initiating irinotecan.Drug-Natural Products:
Single Agent
Hepatic Impairment
As Part of Combination Therapy with Leucovorin and 5-Fluorouracil
IV Administration:
grade 2, then ↓ by 25 mg/m2. If diarrhea of 79 stools/day pretreatment occurs at the beginning of a weekly cycle,↓ by 25 mg/m2. If diarrhea of 79 stools/day pretreatment occurs at the beginning of a once every 3 wk cycle,↓ by 50 mg/m2. If diarrhea
10 stools/day pretreatment occurs during a cycle, hold dose until resolved to
grade 2, then ↓ by 50 mg/m2. If diarrhea
10 stools/day pretreatment occurs at the beginning of a weekly cycle or at the beginning of a once every 3 wk cycle,↓ by 50 mg/m2.
grade 2, then ↓ by 25 mg/m2. If ANC 500999/mm3 occurs at the beginning of a weekly cycle, ↓dose by 25 mg/m2. If ANC 500999/mm3 occurs at the beginning of a once every 3 wk cycle, ↓dose by 50 mg/m2. If ANC <500/mm3 occurs during a cycle, hold dose until resolved to
grade 2, then ↓ by 50 mg/m2. If ANC 500999/mm3 occurs at the beginning of a weekly cycle or at the beginning of a once every 3 wk cycle, ↓dose by 50 mg/m2. If neutropenic fever occurs during a cycle, hold dose until resolved, then ↓ by 50 mg/m2 when resolved. If neutropenic fever occurs at the beginning of a weekly cycle or at the beginning of a once every 3 wk cycle, ↓by 50 mg/m2. Administration of a colony-stimulating factor may be considered if clinically significant decreases in WBC (<2000/mm3), neutrophil count (<1000/mm3), hemoglobin (<9 g/dL), or platelet count (<100,000 cells/mm3) occur.NDC Code*