Cancer Pharmacology Flashcards
Antimetabolites: ___, ___ and ___
Antifolates, Purine, and Pyrimidine Analogs
Microtubule inhibitors: ___ and ___
Vinca alkaloids and taxanes
Topoisomerase inhibitors: ___ and ___/___
“Tecans”, and Anthracyclins/Etoposide
Topoisomerase I Inhibitor: ___
Tecans
Topoisomerase II Inhibitor: ___, ___
Anthracyclins, Etoposide
Cyclophosphamide is a ___.
DNA alkylating agent.
Cyclophosphamide is used for
Breast cancer and lymphoma
Resistance to cyclophosphamide arises through
detoxification by thiols, increased DNA damage repair, and increased drug metabolism.
Cyclophosphamide toxicities of note
Intertility/mutagenesis
Hemorrhagic cystitis
How do you prevent hemorrhagic cystitis with alkylator treatment?
Thiols
Cisplatin and Oxaliplatin are
DNA Damaging Agents (Platinum compounds)
Cisplatin is used for
Lung and testicular cancer, among others.
Oxaliplatin is used for
Colorectal cancers.
___ can be used as radiosensitizers.
Platinum compounds.
Platinum compound toxicities for:
- cisplatin
- oxaliplatin
- cisplatin: neuro and renal
- oxaliplatin: neuro (low renal tox)
Methotrexate is an
Anti-metabolite (folic acid analog).
Ara-C, 5’FU, and Gemcitabine are
Pyrimidne analogs.
Methotrexate is used for for
Leukemia, lymphoma, and immunosuppression.
Methotrexate toxicities of note
liver toxicity (hepatitis may develop)
pulmonary toxicity
toxic in utero
Effects of methotrexate can be reversed with
Leukovorin/tetrahydrofolate
Resistance arises to methotrexate through
1) Mutation/amplification of DHFR
2) Altered drug transport
3) Decreased polyglutamates
Cytosine arabinoside (Ara-C) is an
Antimetabolite (pyrimidine analog).
Resistance to Ara-C arises by
1) Delete activating enzyme
2) over-express metabolic enzymes
Ara-C is used for
Leukemia and lymphoma
Gemcitabine is a
antimetabolite (pyrimidine analog).
Resistance togemcitabine arises through
Deletion of the activating enzyme.
Notable toxicities of gemcitiabine
Flu-like syndrome
Edema
Gemcitabine is used for
Pancreatic cancer
5’FU is an
Anti-metabolite(blocks thymidylate synthase)
Resistance to 5’FU arises through
mutations of thymidylate synthase
loss of reduced folates (laukovorin improves)
Notable toxicities of 5’FU
Hand-foot syndrome
Diarrhea
5’FU is used for
GI malignancies (also esophageal cancer with radiosensitizer)
Vincristine is
microtubule inhibitors (block polymerization, vinca alkaloid).
Docetaxel is
microtubule inhibitors (stabilizers, taxanes).
Resistance to MT inhibitors arises though
MDR overexpression
tubulin mutations
Notable toxicities of vincristine:
Neurotoxicity
Vincristine is used for
leukemia, lymphoma
Notable toxicities of docetaxel
Neurotoxicity Hypersensitivity reactions (to the drug vehicle)
Docetaxel is used for
Lung, OvCa, Br, Pr
Irinotecan is a
Topo I inhibitor (“Tecans”, causes SSB)