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57 Cards in this Set
- Front
- Back
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How many classes of Natural Products that are antineoplastics should I know?
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6
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What are the 6 classes of Natural Product antineoplastics?
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-Vinca alkaloids
-Taxanes -Epipodophyllotoxins -Monoclonal antibodes -Antibiotics -BRMs |
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What are the 2 vinca alkaloids?
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-Vincristine
-Vinblastine |
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What taxane should I know?
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Paclitaxel
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What is the Epipodophyllotoxin?
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Etoposide
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What monoclonal antibody?
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Trastuzumab
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What are 2 antibiotics that are antineoplastic drugs?
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-Doxorubicin
-Bleomycin |
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What is the BRM antineoplastic to know?
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G-CSF - granulocyte colony stimulating factor
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What are Vinca alkaloids derived from?
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The periwinkle plant!
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What is the mechanism of the Vinca Alkaloids?
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-Bind to Tubulin
-Inhibit proper formation of microtubules and the mitotic spindle |
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And what are the 2 vinca alkaloids?
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-Vincristine
-Vinblastine |
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How are Vincristine and Vinblastine similar?
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Structurally
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How are Vincristine/Vinblastin different?
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-Different side effects
-Different antitumor spectrums |
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What is the tumor spectrum of Vincristine?
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BLT
-Breast cancer -Lymphomas (HL/NHL) -Testicular cancer |
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What are 2 toxic side effects of Vincristine?
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-Strong myelosuppression
-Epithelial ulcerations |
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What is the tumor spectrum of Vincristine?
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-Lymphomas
-ALL -Wilm's tumor -Neuroblastoma |
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How does the toxicity of Vincristine compare to that of vinblastine?
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CRISTine is much LESS bone marrow suppressive than BLASTine
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So which vinca alkaloid blasts the bone marrow?
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Vinblastine
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And which vinca alkaloid has the tumor spectrum of BLT? LAWN?
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BLT = vinBlastine
Lawn = vinCristine |
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What is a toxic side effect unique to Vincristine?
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Neuromuscular abnormalities
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What class of Natural product antineoplastics is derived from Yew trees? What is the specific agent to know?
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Taxanes - Paclitaxel
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What is the mechanism of the Taxanes/Paclitaxel?
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By binding the B-subunit of Tubulin, they ENHANCE microtubule stability and assembly!
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Where does Paclitaxel block the cell cycle by enhancing MT assembly and stability?
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Late in G2, near the G2M interface
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What is the G2M interface similar to/how?
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Similar to the G1S interface - radiosensitive!
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So what are 2 drugs that may be used as radiosensitizing agents?
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-Methotrexate
-Paclitaxel |
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What are the 2 cancer indications of Paclitaxel?
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-Refractory ovarian cancer
-Breast cancer |
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What regimen is the standard therapy for ovarian cancer?
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Paclitaxel PLUS Cisplatin
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3 side effects of Paclitaxel:
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-Dose limiting leukopenia
-Peripheral neuropathy -Myalgia/arthralgia |
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What antibiotic is one of the most widely used antitumor drugs because it is so active?
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Doxorubicin
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What should Doxorubicin NOT be confused with?
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Doxycycline or Daptomycin
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What is Doxycycline?
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An antimalaria drug
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What is Daptomycin?
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An antibacterial cell membrane inhibitor (goes along with polymyxin B)
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What is Doxorubicin's other name?
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Adriamycin
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What are the 3 mechanisms of Doxorubicin?
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1. Intercalates btwn DNA base pairs and distorts the helix
2. Causes lipid peroxidation and generates free radicals 3. Binds DNA/topoisomerase II |
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What is the spectrum of Doxorubicin?
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Very BROAD
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What is a specific side effect of Doxorubicin?
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Cardiomyopathy
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What is another antibiotic anticancer drug to know in addition to Doxorubicin?
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Bleomycin
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What is Bleomycin made up of and what does it do in its mechanism?
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-Mixture of iron-containing glycopeptides that bind to DNA
-Causes oxidative damage to DNA leading to DNA strand breaks |
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What is the tumor spectrum of Bleomycin?
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BROAD
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What is the most feared side effect of Bleomycin? Why?
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Pulmonary toxicity - it is dose related and leads to irreversible fibrosis!
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What does Bleomycin do to skin?
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Causes skin vesiculation
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What is myelosuppression caused by Bleomycin like? Why care?
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Minimal - it can be added to another drug without adding to bone marrow suppression
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What natural product anticancer drug is an epipodophyllotoxin?
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Etoposide
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What is the mechanism by which Etoposide is an antineoplastic?
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It STABILIZES DNA-topoisomerase II complexes, resulting in dsDNA breaks that cannot be repaired.
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What is the tumor spectrum of Etoposide?
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Broad
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What kind of side effects does Etoposide cause?
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The typicals - BAD (bm, alopecia, damage to GI)
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What is the biological response modifier to know?
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Filgrastim
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What is Filgrastim?
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G-CSF
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What is the GOAL of Filgrastim, ie why is it given?
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To limit chemotherapy induced neutropenia
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So what is the mechanism of filgrastim?
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Stimulates granulocyte production by the marrow
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When is Filgrastim used? Why?
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After myelosuppressive agents to speed the white count recovery
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What is a bad side effect of Filgrastim?
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Bone pain
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What is the monoclonal antibody to know of as an antineoplastic drug?
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Trastuzumab
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What is Trastuzumab's other name?
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Herceptin
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What IS Trastuzumab?
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Monoclonal Ab to the Her2 receptor
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What is Trastuzumab used for treating?
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The 25-30% of breast cancers that overexpress Her2!!
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What are 3 side effects of Trastuzumab?
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-Cardiomyopathy
-Hypersensitivity -Infusion reactions |
