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Irinotecan

    Brands

    DAE Class; Rx

    Common Brand Names; Camptosar

    • Antineoplastics, Topoisomerase Inhibitors; 
    • Antineoplastics, Camptothecin

    Synthetic form of prostaglandin E2; has oxytocic actions; use requires specialized care facilities and monitoring
    Vaginal suppositories used clinically to induce abortion or to evacuate uterine contents following intrauterine fetal death, missed abortion, or benign hydatidiform mole
    Endocervical gel or vaginal inserts are used for cervical ripening during labor in term pregnancies

    Indicated as first-line therapy (with 5-fluorouracil and leucovorin) for metastatic colorectal cancer (CRC); it is also indicated for CRC that has recurred or progressed following initial fluorouracil-based therapy
    For the treatment of metastatic colorectal cancer that has recurred or progressed after fluorouracil-based therapy, as monotherapy.
    For the treatment of KRAS wild-type, EGFR-expressing, metastatic colorectal cancer (mCRC) in combination with cetuximab in patients who are refractory to irinotecan-based chemotherapy.
    For the treatment of metastatic colorectal cancer, in combination with leucovorin and fluorouracil (FOLFIRI).
    For the treatment of BRAF mutation-positive, RAS wild-type, metastatic colorectal cancer, in combination with vemurafenib and cetuximab.

    Hypersensitivity to drug or excipients

    >10%

    Anemia (>90%)

    Leukopenia (>90%)

    Neutropenia (>90%)

    Thrombocytopenia (>90%)

    Elevated bilirubin (88%)

    Diarrhea (85%)

    Nausea (79%)

    Asthenia (70%)

    Abdominal pain (63%)

    Vomiting (60%)

    Alopecia (43%)

    Fever (42%)

    Constipation (41%)

    Anorexia (34%)

    Mucositis (32%)

    Pain (31%)

    Dyspnea (28%)

    Cough (27%)

    Dizziness (23%)

    Infection (22%)

    Rash (19%)

    1-10%

    Abdominal fullness (10%)

    AST increased (10%)

    Dyspepsia (10%),

    Edema (10%)

    Ascites/jaundice (9%)

    Vasodilation (9%)

    Thromboembolism (9%)

    Hypotension (6%)

    Neutropenic fever (2-6%)

    Frequency Not Defined

    Headache

    Insomnia

    Orthostatic hypotension

    Black Box Warnings

    Severe myelosuppression may occur

    Diarrhea

    • Early and late forms of diarrhea can occur
    • Early diarrhea may be accompanied by cholinergic symptoms which may be prevented or ameliorated by atropine
    • Late diarrhea can be life threatening and should be treated promptly with loperamide
    • Monitor and give fluid and electrolytes as needed
    • Institute antibiotic therapy if patients develop ileus, fever, or severe neutropenia
    • Interrupt irinotecan and reduce subsequent doses if severe diarrhea occurs

    Use caution in hyperbilirubinemia and elderly

    Outside of a clinical study, not for use in combination with a regimen of 5-FU/LV administered for 4-5 consecutive days every 4 weeks owing to increased toxicity, including toxic deaths

    Renal impairment and acute renal failure reported; usually in patients who became volume depleted from severe vomiting and/or diarrhea

    Drug is subject to photodegradation, especially in neutral and alkaline solutions

    Individuals who are homozygous for the UGT1A1*28 allele are at increased risk for neutropenia following initiation of therapy; consider dose reduction by at least 1 level for pts homozygous in the enzyme UDP-glucuronosyl transferase 1A1*28 (UGT1A1*28) variant

    Avoid pregnancy; can cause fetal harm

    Pregnancy

    Available postmarketing and published data reporting the use in pregnant women, are insufficient and confounded by concomitant use of other cytotoxic drugs, to evaluate for any drug-associated risk for major birth defects, miscarriage, or adverse maternal or fetal outcomes

    Lactation

    Irinotecan and its metabolites are present in human milk; there is no information regarding effects of drug on breastfed infant, or on milk production; because of potential for serious adverse reactions from drug in breastfed child, advise lactating women not to breastfeed during treatment and for 7 days after final dose

    Adults

    Single agent: 350 mg/m2 IV every 3 weeks or 125 mg/m2 IV weekly.
    In combination with fluorouracil and leucovorin: 180 mg/m2 IV every 2 weeks or 125 mg/m2 IV weekly.

    Geriatric

    Single agent: 350 mg/m2 IV (age greater than or equal to 70 years, 300 mg/m2) every 3 weeks or 125 mg/m2 IV weekly.
    In combination with fluorouracil and leucovorin: 180 mg/m2 IV every 2 weeks or 125 mg/m2 IV weekly.

    Adolescents

    Safety and efficacy have not been established.

    Children

    Safety and efficacy have not been established.

    Irinotecan

    injectable solution

    • 20mg/mL