Irinotecan Hcl Aqvida (Irinotecan Hydrochloride Trihydrate)

• Irinotecan is a topoisomerase I inhibitor used in colorectal cancer therapy.
• Metastatic colorectal cancer: used as part of combination chemotherapy to extend overall survival.
• Advanced colorectal cancer: administered to control disease progression and improve response rates.
• Colorectal cancer (first‑line or second‑line): incorporated into treatment regimens to increase tumor response and delay progression.

• Irinotecan is converted intracellularly to its active metabolite SN‑38, which binds to the DNA‑topoisomerase I complex, stabilizing it and preventing relegation of single‑strand breaks. This results in accumulation of DNA damage, inhibition of DNA replication and transcription, ultimately leading to tumor cell apoptosis. The effect is selective for rapidly dividing cells and is enhanced in tumors with high topoisomerase I expression.

Irinotecan may cause a range of adverse reactions, varying from mild to severe.

Common Side Effects

• Diarrhea: often severe, may require antidiarrheal therapy.
• Nausea and vomiting: typical chemotherapy‑related symptoms.
• Neutropenia: reduced white blood cell count increasing infection risk.
• Alopecia: hair loss during treatment.
• Fatigue: persistent tiredness.
• Elevated liver enzymes: indicating hepatic stress.

Serious or Rare Side Effects

• Febrile neutropenia: fever with low neutrophils requiring hospitalization.
• Severe abdominal cramping and colitis: can lead to dehydration.
• Hypersensitivity reactions: including rash, dyspnea, or anaphylaxis.

When using Irinotecan, several precautions should be observed to minimize risks.

• Baseline blood counts: obtain CBC before each cycle to monitor neutropenia.
• Liver function monitoring: assess hepatic enzymes regularly due to metabolism.
• Hydration status: ensure adequate fluids to reduce risk of severe diarrhea.
• Drug interactions: review concomitant medications, especially enzyme inhibitors.
• Pregnancy and lactation: avoid use unless benefits outweigh potential fetal risks.
• Store at ambient temperature: keep vials in original packaging, protect from light and moisture.

Irinotecan can interact with other medicines, affecting its efficacy or safety.

Major Interactions (Avoid)

• Strong CYP3A4 inhibitors (e.g., ketoconazole, clarithromycin): may increase SN‑38 exposure and toxicity.
• UGT1A1 inhibitors (e.g., atazanavir): raise risk of neutropenia and diarrhea.

Moderate Interactions (Monitor Closely)

• Anticoagulants (e.g., warfarin): monitor INR as Irinotecan may alter bleeding risk.
• Other myelosuppressive agents: increase risk of severe neutropenia.
• Antiemetics containing corticosteroids: may affect metabolism; adjust dosing if needed.