Overview of Antineoplastics Flashcards
What ADR is associated with Cisplatin?
Nephrotoxicity
What are the clinical indications for the use of Trastuzumab?
Breast & gastric cancers expressing HER2
What anticancer drugs are associated with neurotoxic effects?
Paclitaxel (peripheral neuropathy), Vincristine, Cytarabine, Oxaliplatin (peripheral neuropathy)
What anticancer drugs act primarily on the M phase of the cell cycle?
Vincristine & Paclitaxel
What anticancer drug is known to have adverse effects on the heart and could lead to irreversible CHF?
Doxorubicin
Peripheral neuropathy is an ADR associated with what anticancer drug?
Oxaliplatin
True/False. Starting cancer treatment after symptoms present always results in death.
True. Treatment must be started early and before direct symptoms begin for effective treatment.
What unique ADRs are associated with Bleomycin?
Skin pigmentation on the hands, pulmonary pneumonitis
What is the MOA for the aromatse inhibitors used in the treatment of advanced breast cancer?
Letrozole & Anastrozole - inhibits estrogen formation from testosterone
What is the MOA of Doxorubicin?
Inhibits topoisomerase II and causes formation of free radicals
What common toxicities are associated with nearly all antineoplastics?
Bone marrow suppression, GI damage, skin damage, loss of hair, sterility, nausea/vomiting
What anticancer drug is used to treat prostate cancer and inhibits FSH/LH secretion?
Leuprolide
Bleomycin is a cell cycle-specific anticancer drug that causes DNA strand breaks. In what phase of the cell cycle does it act?
G2 phase
What strategy is utilized with Cyclophosphamide to prevent its unique ADR?
Pre-hydration with mensa disulfide to prevent hemorrhagic cystitis
To what class of anticancer drugs does Meclorethamine belong?
Alkylating Agent
What is the MOA of vincristine?
Acts during M phase of the cell cycle to prevent microtubule formation
What is the most common method of antineoplastic resistance?
Increased P-gp function and drug efflux
What is the MOA of Bortezomib?
Inhibits 26S proteasome degradation
What ADRs are associated with Paclitaxel?
Neutropenia, peripheral neuropathy
True/False. Chemotherapy should not be begun until after surgery to remove a solid tumor.
False. Neoadjuvant chemotherapy is begun before surgery to shrink the tumor and improve results.
What anticancer drugs inhibit topoisomerase II?
Etoposide & Teniposide
What anticancer drug inhibits the DNA polymerase and is known to cause neurotoxicity?
Cytarabine
What aromatase inhibitors are used in the treatment of advanced breast cancer?
Letrozole & Anastrozole
Hemorrhagic cystitis is a severe ADR associated with what antineoplastic drug?
Cyclophosphamide
What anticancer drug cross-links DNA strands and has wide use with solid tumors?
Cisplatin
What plant alkaloid anticancer drug is associated with neurotoxicity?
Vincristine & Paclitaxel (peripheral neuropathy)
What small organic molecule inhibits the ABL portion of the tyrosine kinase?
Imatinib mesylate
What is the MOA for the anticancer drug that may cause neutropenia and peripheral neuropathy as an ADR?
Paclitaxel - prevents polymerization of the mitotic spindle
What anticancer drug crosses the BBB and is used to treat CNS tumors and meningeal leukemia?
Carmustine
What is the MOA of Oxaliplatin?
Causes intrastrand crosslinks of DNA
What is the MOA of Methotrexate?
Inhibits the dihydrofolate reductase required to activate folic acid
What drug is administered to prevent the unique ADR of Doxorubicin?
Dexrazoxane chelates Fe to prevent free radical formation that causes cardiac toxicity with Doxorubicin use
True/False. Leucovorin prevents toxicity with both Methotrexate & 5-FU.
False. Leucovorin prevents Methotrexate nephrotoxicity, but enhances the anticancer effects of 5-FU.
Methotrexate and 5-FU both ultimately lead to the inhibition of the thymidylate synthase. What is the effect of this inhibition?
Inhibition of RNA & DNA synthesis
What is the function of Leucovirin?
Folate analog that acts as a rescue drug to prevent Methotrexate nephrotoxicity
Alkylating agents are (cell cycle specific/non-specific) anticancer drugs?
Cell cycle non-specific
Topoisomerase inhibitors are cell cycle-specific. At what phase of the cell cycle do they act?
S phase
What ADR is associated with Cytarabine?
Neurotoxicity
How do the MOAs of Methotrexate and 5-Fluorouracil differ?
Methotrexate inhibits the dihrydrofolate reductase. This ultimately leads to the inhibition of the thymidylate synthase. 5-FU directly inhibits the thymidylate synthase.
What Cyclophosphamide metabolite is responsible for causing hemorrhagic cystitis?
Acrolein
