Irinotecanhydrochlorid 3 H2o Phares (Irinotecan Hydrochloride Trihydrate)

Irinotecan is a topoisomerase I inhibitor used in chemotherapy regimens for gastrointestinal and other solid tumors.

• Metastatic colorectal cancer: improves progression‑free survival when combined with fluoropyrimidine‑based regimens.
• Advanced small cell lung cancer: contributes to tumor response as part of multi‑agent therapy.
• Gastric cancer: used in combination protocols to enhance antitumor activity in unresectable disease.

• Irinotecan is a prodrug that is converted intracellularly to SN‑38, a potent inhibitor of DNA topoisomerase I. By stabilizing the topoisomerase‑DNA complex, SN‑38 prevents the religation of single‑strand DNA breaks during replication, leading to accumulation of DNA damage, cell‑cycle arrest and apoptosis of rapidly dividing cancer cells.

Irinotecan may cause a range of adverse reactions, varying in frequency and severity.

Common Side Effects

• Diarrhea: often severe and may require antidiarrheal therapy.
• Neutropenia: reduced white blood cell count increasing infection risk.
• Nausea and vomiting: gastrointestinal upset commonly reported.
• Alopecia: hair loss may occur during treatment.

Serious or Rare Side Effects

• Febrile neutropenia: fever with low neutrophils requiring urgent medical care.
• Severe colitis: inflammation of the colon that can be life‑threatening.
• Hypersensitivity reactions: rash, bronchospasm or anaphylaxis.
• Hepatotoxicity: elevated liver enzymes indicating liver injury.

When using irinotecan, clinicians should observe several safety measures to minimize risks.

• Baseline blood counts: obtain complete blood count before each cycle to monitor neutropenia.
• Liver function: assess hepatic enzymes as impaired metabolism can increase toxicity.
• Diarrhea prophylaxis: initiate antidiarrheal agents and educate patients on early signs.
• Drug interactions: review concomitant medications that affect CYP3A4 or UGT1A1.
• Pregnancy and lactation: avoid use; safety not established.
• Store at 2-8°C: keep refrigerated, protect from light, do not freeze or shake.

Irinotecan interacts with several medicines that can alter its efficacy or toxicity.

Major Interactions (Avoid)

• Strong CYP3A4 inducers (e.g., rifampin, carbamazepine): may reduce SN‑38 formation and therapeutic effect.
• UGT1A1 inhibitors (e.g., atazanavir, indinavir): can increase SN‑38 exposure, raising risk of severe neutropenia and diarrhea.
• Concurrent use with other myelosuppressive agents: may potentiate bone‑marrow suppression.

Moderate Interactions (Monitor Closely)

• Anticholinergic agents: may exacerbate constipation and ileus.
• Anticoagulants (warfarin, DOACs): monitor for bleeding as irinotecan can affect platelet function.
• Proton pump inhibitors: may modestly affect gastric pH and absorption of oral formulations.