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Introduction
Illustrated mechanism of action
Examples of Medication Brand Names (with Images)
Indication
Side Effects
Precautions & Contraindications
Monographs
Reference
Introduction about Irinotecan:
Introduction about Irinotecan:
1-Discovery & Early Use: a, a camptothecin derivative and topoisomerase I inhibitor, was synthesized in 1983 and initially approved in Japan (1994) for lung, cervical, and ovarian cancers after demonstrating anti-tumor activity in early clinical trials. 2-Key Approvals & Combinations: It gained FDA approval for metastatic colorectal cancer in 1996 (initially for refractory cases) and was later incorporated into first-line regimens like FOLFIRI, significantly improving treatment outcomes for colorectal cancer patients. 3-Continued Development: The drug continues to evolve with the development of liposomal formulations (e.g., Onivyde for pancreatic cancer) and ongoing research focused on mitigating toxicities and expanding its use in combination therapies for various cancers.
Illustrated mechanism of action
Irinotecan's primary mechanism of action involves inhibiting topoisomerase I, an enzyme essential for DNA replication and transcription. Irinotecan is a prodrug that is converted to its active metabolite, SN-38, which binds to the topoisomerase I-DNA complex, preventing the religation of single-strand breaks. This leads to DNA damage, cell cycle arrest in the S-G2 phase, and ultimately, cancer cell death
Irinotecan's primary mechanism of action involves inhibiting topoisomerase I, an enzyme essential for DNA replication and transcription. Irinotecan is a prodrug that is converted to its active metabolite, SN-38, which binds to the topoisomerase I-DNA complex, preventing the religation of single-strand breaks. This leads to DNA damage, cell cycle arrest in the S-G2 phase, and ultimately, cancer cell death
Examples of Medication Brand Names (with Images)
Examples of Medication Brand Names (with Images)
Camptosar
Camptosar
generic name is :Irinotecan
Onivyde
Onivyde
Irinotecan MYLAN
Campto
Campto
IRINOTECAN
Indication
Topoisomerase inhibitors are drugs that block the action of topoisomerases, enzymes essential for DNA replication, transcription, and repair by managing DNA topology. They are mainly used as anti-cancer agents because they induce DNA damage leading to apoptosis in cancer cells.
Indications of Topoisomerase Inhibitors
They are primarily indicated for the treatment of various cancers, including:
Colorectal cancer
Pancreatic cancer
Breast cancer
Small cell lung cancer
Ovarian cancer
Gastric cancer
Cervical cancer
Urothelial cancer
Leukemias and lymphomas
Side Effect
Side Effect
Common side effects of irinotecan (Camptosar) may include nausea, vomiting, diarrhea (which can be severe and occur early or late after treatment), loss of appetite, and low blood cell counts. Other possible side effects are fever, pain, mouth sores, weakness, constipation, cough, drowsiness, or trouble sleeping. Severe side effects that require immediate medical attention include bloody stools, dehydration symptoms, and signs of infection
Precautions & Contraindications
Precautions & Contraindications
Precautions
Severe diarrhea: Can occur immediately (with cholinergic symptoms like sweating/flushing) or delayed (life-threatening dehydration). Report diarrhea immediately.
Bone marrow suppression: Increases infection/bleeding risk. Monitor blood counts and avoid infections.
Birth control: Required for both sexes (females: 6 months post-treatment; males: 3 months).
Liver/kidney/lung disease: Requires dose adjustments or avoidance.
Drug interactions: Avoid strong CYP3A4 inducers (e.g., St. John’s wort) and ketoconazole. Contraindicated with atazanavir.
Allergic reactions: May cause anaphylaxis (swelling, breathing issues). Discontinue permanently if severe.
Interstitial lung disease: Stop if new/worsening cough, fever, or dyspnea occurs
intolerance: Avoid due to sorbitol content
Contraindications
Hypersensitivity to irinotecan or sorbitol.
Bowel obstruction (risk of fatal diarrhea).
Pregnancy/breastfeeding: Harmful to fetus; avoid conception. Breastfeeding prohibited during treatment +7 days.
Concurrent use of atazanavir (increases toxicity).
Severe neutropenia/sepsis history (high risk of recurrence
DOC-20250321-WA0004..pdfDrug monograph.docx_20250424_201024_0000.pdfDrug monograph sara1[1] (5).pdfHabiba Younis 11.pdfDrug monograph.pdfTopotecan drug. pharma activity.pdfReference
Reference
* https://pubchem.ncbi.nlm.nih.gov/compound/Irinotecan
* https://www.cancernetwork.com/view/fda-approves-irinotecan-first-line-therapy-colorectal-cancer
* https://www.fda.gov/drugs/resources-information-approved-drugs/fda-approves-irinotecan-liposome-first-line-treatment-metastatic-pancreatic-adenocarcinoma
* https://www.pharmgkb.org/pathway/PA2029/pathway
* https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10609717/
* https://www.mayoclinic.org/drugs-supplements/irinotecan-intravenous-route/description/drg-20064383
* https://www.drugs.com/cons/irinotecan.html
* https://anesth.unboundmedicine.com/anesthesia/view/Davis-Drug-Guide/110546/all/irinotecan_liposoma
* https://images.app.goo.gl/aaxNgzhMeCKgndk17
* https://images.app.goo.gl/XMWb5roT5J9YaHk58
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