Irinotecan

Irinotecan Brand Name– Camptosar

What is Irinotecan

Irinotecan is an intravenous antineoplastic agent. Irinotecan is one of many water-soluble derivatives of camptothecin (CPT), a cytotoxic plant alkaloid isolated from the Chinese tree Camptotheca acuminata.

The activity of irinotecan is due to the parent compound and the more potent active metabolite, SN-38.

Irinotecan is approved by the FDA for the treatment of metastatic colorectal cancer, both as monotherapy and in combination with 5-fluorouracil and leucovorin, along with several off-label indications.

Irinotecan can cause severe myelosuppression and may necessitate interruptions of therapy or dose adjustments; complete blood counts should be monitored throughout treatment.

Additionally, severe diarrhea is common with irinotecan therapy. Early diarrhea, within the first 24 hours of treatment, may be associated with cholinergic effects and should be treated with atropine.

Loperamide should be initiated for the first signs of loose stool or diarrhea occurring more than 24 hours after administration of irinotecan; late diarrhea may also require an interruption of therapy or dose adjustment.

Indications

1. colorectal cancer
2. gastric cancer
3. glioblastoma multiforme
4. malignant glioma
5. non-small cell lung cancer (NSCLC)
6. pancreatic cancer
7. rhabdomyosarcoma
8. small cell lung cancer (SCLC)

For the treatment of metastatic colorectal cancer

Side Effects

1. abdominal pain
2. abdominal pain
3. akathisia
4. alopecia
5. anaphylactoid reactions
6. anemia
7. anemia
8. angina
9. anorexia
10. anorexia
11. ascites
12. asthenia
13. asthenia
14. back pain
15. back pain
16. bleeding
17. bone marrow suppression
18. bradycardia
19. cardiac arrest
20. chills
21. colitis
22. confusion
23. confusion
24. constipation
25. constipation
26. cough
27. cough
28. dehydration
29. dehydration
30. diaphoresis
31. diarrhea
32. diarrhea
33. dizziness
34. dizziness
35. drowsiness
36. drowsiness
37. dysarthria
38. dyspepsia
39. dyspnea
40. dyspnea
41. edema
42. edema
43. elevated hepatic enzymes
44. elevated hepatic enzymes
45. exfoliative dermatitis
46. fever
47. fever
48. flatulence
49. flushing
50. flushing
51. GI bleeding
52. GI obstruction
53. GI perforation
54. headache
55. headache
56. hepatomegaly
57. hyperamylasemia
58. hyperbilirubinemia
59. hyperbilirubinemia
60. hypersalivation
61. hypokalemia
62. hyponatremia
63. hypotension
64. hypotension
65. hypovolemia
66. ileus
67. infection
68. infection
69. insomnia
70. interstitial lung disease
71. jaundice
72. lacrimation
73. leukopenia
74. leukopenia
75. miosis
76. myocardial infarction
77. nausea
78. nausea
79. neutropenia
80. neutropenia
81. oral ulceration
82. palmar-plantar erythrodysesthesia (hand and foot syndrome)
83. pancreatitis
84. phlebitis
85. pneumonitis
86. pulmonary embolism
87. rash
88. renal failure (unspecified)
89. rhinitis
90. stomatitis
91. stomatitis
92. stroke
93. syncope
94. thrombocytopenia
95. thrombocytopenia
96. thromboembolism
97. thrombosis
98. toxic megacolon
99. vertigo
100. vomiting
101. vomiting
102. weight loss
103. weight loss

Monitoring Parameters

• CBC with differential
• LFTs
• pregnancy testing

Contraindications

• accidental exposure
• anemia
• biliary tract disease
• bone marrow suppression
• breast-feeding
• children
• chronic lung disease (CLD)
• contraception requirements
• dehydration
• diarrhea
• extravasation
• geriatric
• GI obstruction
• hepatic disease
• infertility
• male-mediated teratogenicity
• neutropenia
• pneumonitis
• poor metabolizers
• pregnancy
• pregnancy testing
• radiation therapy
• reproductive risk
• thrombocytopenia

Interactions

• Acalabrutinib
• Amoxicillin; Clarithromycin; Lansoprazole
• Amoxicillin; Clarithromycin; Omeprazole
• Apalutamide
• Atazanavir
• Atazanavir; Cobicistat
• Atracurium
• Atropine; Hyoscyamine; Phenobarbital; Scopolamine
• Belladonna Alkaloids; Ergotamine; Phenobarbital
• Bosentan
• Brigatinib
• Cabozantinib
• Carbamazepine
• Carvedilol
• Ceritinib
• Chloramphenicol
• Cisatracurium
• Clarithromycin
• Cobicistat
• Conivaptan
• Darolutamide
• Darunavir
• Darunavir; Cobicistat
• Darunavir; Cobicistat; Emtricitabine; Tenofovir alafenamide
• Dasabuvir; Ombitasvir; Paritaprevir; Ritonavir
• Delavirdine
• Dextromethorphan; Quinidine
• Elvitegravir; Cobicistat; Emtricitabine; Tenofovir Alafenamide
• Elvitegravir; Cobicistat; Emtricitabine; Tenofovir Disoproxil Fumarate
• Enzalutamide
• Flibanserin
• Fosamprenavir
• Fosphenytoin
• Fostamatinib
• Gemfibrozil
• Glecaprevir; Pibrentasvir
• grapefruit juice
• Idelalisib
• Indinavir
• Isoniazid, INH; Pyrazinamide, PZA; Rifampin
• Isoniazid, INH; Rifampin
• Itraconazole
• Ketoconazole
• Letermovir
• Lomitapide
• Lopinavir; Ritonavir
• Lumacaftor; Ivacaftor
• Mefloquine
• Mephobarbital
• Mifepristone
• Mitotane
• Mivacurium
• Nefazodone
• Nelfinavir
• Neratinib
• Ombitasvir; Paritaprevir; Ritonavir
• Osimertinib
• Palifermin
• Pancuronium
• Penicillamine
• Phenobarbital
• Phenytoin
• Posaconazole
• Primidone
• Prochlorperazine
• Propafenone
• Quinidine
• Regorafenib
• Ribociclib
• Ribociclib; Letrozole
• Rifampin
• Ritonavir
• Rocuronium
• Saquinavir
• Sofosbuvir; Velpatasvir
• Sofosbuvir; Velpatasvir; Voxilaprevir
• Sorafenib
• St. John’s Wort, Hypericum perforatum
• Succinylcholine
• Tafamidis
• Telithromycin
• Temsirolimus
• Tipranavir
• Tuberculin Purified Protein Derivative, PPD
• Tucatinib
• Vecuronium
• Voriconazole