Miscellaneous Chemotherapeutics Flashcards
What is the MOA of Anthracyclines?
They intercalate between base pairs in the DNA helix; Interfere with DNA chain elongation and nucleic acid synthesis.
Which enzyme is inhibited by anthracyclines?
Topoisomerase 2; Forms free radicals
Describe Anthracyclines cardiac toxicity.
ROS is toxic to cardiac myocytes through intracellular reductase enzymes action on cellular iron-anthracycline complex.
What role does Dexrazoxane play?
Chelates iron and prevents hydroxyl radical formation in the presence of anthracyclines; Prevents anthracyclines cardiac injury.
Differentiate Anthracenediones from Anthracyclines.
Anthracenediones dont produce oxygen derived free radical species. Same MOA. Delayed presentation of identical side effects
Name the Podophyllotoxins. Function?
Etoposide and Teniposide; Topoisomerase 2 poison that halts G2 phase
What are the side effects of podophyllotoxins?
GI toxicities and myelosuppresison.
What is the MOA of Camptothecins?
Inhibit Topoisomerase 1; Topotecan and Irinotecan
What is Irinotecan’s unique side effect?
Early onset acute diarrhea
Discuss Irinotecan
A selective reversible AChase inhibitor and direct ACh receptor agonist.
What is the MOA of Vinca Alkaloids?
Block mitotic cell division by binding to tubulin molecules and inhibiting their polymerisation to microtubules; Vincristine, Vinorelbine and Vinblastine.
What are the side effect of Vinca alkaloids?
Neurotoxicity; Microtubules are the primary structural element of axons.
What is the drug interaction problem involving Vinca alkaloids?
Substrates of CYP450 3A4 are off limits; Itraconazole
What is the MOA of Taxanes?
Mitotic spindle poisons; They stabilize microtubules against depolymerization. Opposite affect of vinca alkaloids.
What is the MOA of L-asparaginase?
Hydrolyzes Asparagine, an amino acid required for tumor cell growth
