Irinotecán Aurovitas (Irinotecan Hydrochloride Trihydrate)

Irinotecan is used in oncology to target DNA replication in rapidly dividing cancer cells.

• Metastatic colorectal cancer: improves overall survival and disease control when combined with fluoropyrimidine therapy.
• Other solid tumours: incorporated into combination regimens to reduce tumor burden in selected patients.
• Colorectal cancer (adjuvant setting): may be administered as part of postoperative chemotherapy to lower recurrence risk.

• Irinotecan is a prodrug that is converted intracellularly to SN‑38, a potent inhibitor of topoisomerase I. By stabilizing the DNA‑topoisomerase I complex, it prevents relegation of single‑strand DNA breaks, leading to accumulation of DNA damage, inhibition of DNA synthesis, and ultimately apoptotic cell death in proliferating cancer cells.

Irinotecan may cause a range of adverse reactions, from mild to life‑threatening.

Common Side Effects

• Diarrhea: often severe and may require antidiarrheal therapy.
• Nausea and vomiting: managed with antiemetics.
• Fatigue: common during treatment cycles.
• Neutropenia: reduced white blood cell count increasing infection risk.
• Alopecia: hair loss may occur.
• Abdominal pain: can accompany gastrointestinal toxicity.

Serious or Rare Side Effects

• Febrile neutropenia: fever with low neutrophil count requiring urgent care.
• Severe colitis or intestinal perforation.
• Hepatotoxicity: marked elevation of liver enzymes.
• Allergic reactions: rash, bronchospasm, or anaphylaxis.
• Cardiac toxicity: rare arrhythmias or myocardial ischemia.
• Secondary malignancies: very rare long‑term risk.

Prior to initiating Irinotecan therapy, several safety considerations are recommended.

• Monitor blood counts: perform regular CBC to detect neutropenia.
• Assess liver function: adjust dose in hepatic impairment.
• Evaluate renal function: consider dose modification in severe renal failure.
• Avoid in patients with bowel obstruction: risk of perforation.
• Use prophylactic antiemetics: to reduce nausea and vomiting.
• Adjust dose for hepatic impairment: follow prescribing information.
• Store at 2-8°C: keep refrigerated, protect from light, do not freeze or shake.

Irinotecan interacts with several drug classes that may alter its efficacy or safety.

Major Interactions (Avoid)

• Strong CYP3A4 inhibitors (e.g., ketoconazole): increase SN‑38 exposure.
• Strong CYP3A4 inducers (e.g., rifampin): decrease efficacy.
• Live vaccines: risk of infection due to immunosuppression.
• Anticoagulants (e.g., warfarin): heightened bleeding risk.
• High‑dose aspirin: may exacerbate gastrointestinal toxicity.

Moderate Interactions (Monitor Closely)

• Other myelosuppressive agents (e.g., carboplatin): additive bone‑marrow suppression.
• Antidiarrheal agents (e.g., loperamide): may mask severity of diarrhea.
• Proton pump inhibitors: potential effect on gastric pH and absorption.
• Herbal supplements (e.g., St. John’s wort): possible CYP induction.
• Electrolyte‑altering drugs: monitor for electrolyte imbalance during diarrhea.