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96 Cards in this Set
- Front
- Back
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MoA of Actinomycin D
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intercalates into DNA and blocks RNA and DNA synthesis
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MoA of Anastrozole
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CYP19 aromatase inhibitor
=> prevents conversion of androgens to estrogens |
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MoA of Asparaginase (L-asparaginase)
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degrades asparagine in the circulation and starves tumor cells for this amino acid
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MoA of Bevacizumab
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antibody against VEGF
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MoA of Bleomycin
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interacts with DNA and catalyzes free radical formation and DNA destruction
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MoA of Cisplatin
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Cross-liinking of DNA
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MoA of Cyclophosphamide
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Alkylation and cross-liinking of DNA
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MoA of Cytosine arabinoside
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inhibitor of DNA polymerase, misincorporation into DNA
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MoA of Doxorubicin
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inhibitor of the topoisomerase II/DNA complex
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MoA of Etoposide
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inhibitor of the topoisomerase II/DNA complex
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MoA of Fluorouracil (5-Fluorouracil)
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inhibitor of thymidylate synthetase, misincorporation into RNA
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MoA of Gefitnib
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EGFR inhibitor
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MoA of Hydroxyurea
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inhibitor of ribonucleotide reductase
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MoA of Imatinib
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inhibitor of ABL tyrosine kinase
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MoA of Irinotecan
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inhibitor of topoisomerase I/DNA complex
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MoA of Leuprolide
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GnRH analog that causes GnRH receptor down regulation
=> targets endocrine system to reduce steroid synthesis |
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MoA of Mechlorethamine
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Alkylation and cross-liinking of DNA
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MoA of Methotrexate
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DHFR inhibitor
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MoA of Paclitaxel
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binds tubulin and stabilizes microtubules (prevents depolymerization)
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MoA of Tamoxifen
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estrogen receptor antagonist
=> down regulates stimulator growth factors (IGF-1, TGF-alpha, etc.) & upregulates inhibitor growth factors (TGF-beta) |
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MoA of 6-Thioguanine
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inhibitor of purine biosynthesis
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MoA of Trastuzumab
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binds to Her2 on cancer cells and stimulates antibody-dependent cellular cytotoxicity
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MoA of Vinblastine
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interacts with tubulin and prevents microtubule polymerization
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MoA of Vincristine
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interacts with tubulin and prevents microtubule polymerization
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MoA of allopurinol
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xanthine oxidase inhibitor
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MoA of leucovorin
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leucovorin is 5-formyl-tetrahydrofolate and it can rescue cells from methotrexate toxicity
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MoA of filgrastim (G-CSF)
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hematopoietic agent that stimulates neutrophil production
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Toxicities of Actinomycin D
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Major: bone marrow depression
Other: Nausea, vomiting, radiation recall, toxicity to skin and other tissues |
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Toxicities of Anastrozole
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Other: effects related to estrogen deficiency
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Toxicities of Asparaginase (L-asparaginase)
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Major: Liver damage, acute pancreatitis
Other: Hypersensitivity, central nervous system damage |
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Toxicities of Bevacizumab
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Other: hypertension, GI perforation
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Toxicities of Bleomycin
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Major: Pulmonary Fibrosis
Other: Skin changes, alopecia, acute febrile reaction, rarely anaphylaxis, radiation recall |
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Toxicities of Cisplatin
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Major: bone marrow depression
Other: Renal tubular damage, nausea, vomiting |
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Toxicities of Cyclophosphamide
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Major: bone marrow depression
Other: Nausea, vomiting, male sterility, amenorrhea, cystitis, alopecia |
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Toxicities of Cytosine arabinoside
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Major: bone marrow depression
Other: Nausea, vomiting, alopecia |
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Toxicities of Doxorubicin
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Major: bone marrow depression, cardiomyopathy
Other: Alopecia, nausea, vomiting, radiation recall |
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Toxicities of Etoposide
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Major: bone marrow depression
Other: Nausea, alopecia, 2nd cancers |
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Toxicities of Fluorouracil (5-Fluorouracil)
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Major: bone marrow depression
Other: Nausea, vomiting, alopecia, GI mucositis |
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Toxicities of Gefitnib
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Other: skin problems, rashes
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Toxicities of Hydroxyurea
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Major: bone marrow depression
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Toxicities of Imatinib
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Other: hepatotoxicity, nause, GI upset, fluid retention
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Toxicities of Irinotecan
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Major: bone marrow depression/neutropenia
Other: alopecia |
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Toxicities of Leuprolide
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Other: hormone withdrawl effects
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Toxicities of Mechlorethamine
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Major: bone marrow depression
Other: Nausea, vomiting, phlebitis, skin vesicant, male sterility, amenorrhea |
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Toxicities of Methotrexate
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Major: bone marrow depression
Other: Alopecia, liver damage, lung |
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Toxicities of Paclitaxel
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Major: bone marrow depression
Other: Bradycardia, sensory neuropathy, hypotention |
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Toxicities of Tamoxifen
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Other: Hot flashes, risk increase for endometrial CA, thromboembolic events
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Toxicities of 6-Thioguanine
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Major: bone marrow depression
Other: Nausea, vomiting |
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Toxicities of Trastuzumab
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Other: Cardiac toxicity may be a problem
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Toxicities of Vinblastine
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Major: bone marrow depression, Granulocytopenia
Other: Mild peripheral neuropathy |
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Toxicities of Vincristine
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Major: Peripheral Neuropathy
Other: Alopecia, constipation |
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Toxicities of allopurinol
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Major: bone marrow depression
Other: sensitivity reactions |
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Toxicities of leucovorin
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Major: bone marrow depression
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Toxicities of filgrastim (G-CSF)
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Major: bone marrow depression
Other: mild to moderate bone pain, skin rxn |
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Which chemo drugs are usually administered by IV?
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Actinomycin D
Asparaginase (L-asparaginase) Bevacizumab Cisplatin Cytosine arabinoside Doxorubicin Fluorouracil (5-Fluorouracil) Paclitaxel Trastuzumab Vinblastine Vincristine |
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Which chemo drugs are usually administered orally only?
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Anastrozole
Gefitnib Hydroxyurea Imatinib Tamoxifen 6-Thioguanine allopurinol |
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Which chemo drugs can be administered by IV or orally?
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Cyclophosphamide
Etoposide Irinotecan |
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Leuprolide?
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Sub-cutaneous
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Mechlorethamine?
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IV
Intracavitary |
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Methotrexate?
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PO
IV Intrathecal |
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filgrastim (G-CSF)?
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IV
Sub-cutaneous |
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leucovorin?
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PO
IV IM |
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bleomycine?
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IV
IM |
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Which chemo drugs are cell cycle specific?
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fluorouracil
mercaptopurine methotrexate L-asparaginase paclitaxel vincristine/vinblastine |
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Which chemo drugs are not cell cycle specific?
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alkylating agents (cyclophosphamide, mechlorethamine, nitrosoureas)
actinomycin D daunorubicin, doxorubicin etoposide, irinotecan cisplatin bleomycin |
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Which chemo drugs target DNA?
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Bondage: alkylating agents (mechlorethamine, cyclophosphamide), cisplatin
Vaporization: bleomycin Confusion: actinomycin D, doxorubicin, etoposide, irinotecan Starvation: methotrexate, 5-fluorouracil, cytosine arabinoside, hydroxyurea Regulation: tamoxifen, anastrozole, leuprolide |
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Which chemo drugs target protein synthesis?
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L-asparaginase
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Which chemo drugs are mitotic poisons?
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vincristine
vinblastine paclitaxel |
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Which chemo drugs are protein kinase inhibitors?
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Imatinib (Gleevec)
Gefitnib |
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Which chemo drugs target specific antigens?
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Bevacizumab (Avastin)
Trastuzumab (Herceptin) |
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What are the topoisomerase inhibitors?
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Topo I inhibitors: camptothecins (irinotecan)
Topo II inhibitors: doxorubicin, etoposide |
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What is the significance of the UGT1A1 mutation?
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Mutation in UDP-glucuronosyltransferases 1A1
Makes pts. 5X more sensitive to irinotecan (Topo I inhibitor) |
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What are the effects of co-treatment w/methotrexate & 5-FU?
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5-FU first, then MTX => antagonism
MTX first, hrs, then 5-FU => synergism Give MTX then 5-FU |
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Which chemo drugs are sensitive to cancers that induce metallotioneins that quench their activity as a resistance mechanism?
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Alkylators (mechlorethamine, cyclophosphamide)
Cross-linkers (cisplatin) |
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Which chemo drugs are sensitive to cancers that induce DNA repair enzymes as a resistance mechanism?
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Any drug that damages DNA
Cisplatin Alkylators (mechlorethamine, cyclophosphamide) Bleomycin |
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Which chemo drugs are sensitive to cancers that induce glutathione transferase as a resistance mechanism?
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Alkylators (mechlorethamine, cyclophosphamide)
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Which chemo drugs are susceptible to enzymatic destruction as a resistance mechanism?
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Bleomysin
Cytosine arabinoside |
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Which chemo drugs are susceptible to increased efflux out of a cell by transporters (i.e. MDR transporter) as a resistance mechanism?
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actinomycin D
vincristine vinblastine etoposide doxorubicin paclitaxel |
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Which chemo drugs are susceptible to DHFR amplification as a resistance mechanism?
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methotrexate
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Which chemo drugs are susceptible to Abl-kinase mutations as a resistnace mechanism?
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imatinib (Gleevec)
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What drug can block the multi-druge resistance pump of MDR cells and can be used together w/chemo drugs?
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Verapamil
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What toxicities are common to many chemo drugs?
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myelosuppression w/leukopenia, thrombocytopenia, & anemia (bone marrow depression)
alopecia mucous membrane ulceration |
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Which chemo drugs cause severe alopecia?
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cyclophosphamide
doxorubicin vinblastine vincristine |
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Which chemo drugs cause nausea & vomiting?
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mechlorethamine
cisplatin cyclophosphamide (delaed by 8hr) |
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Which chemo drugs cause extravasation injury?
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oxorubicine
actinomycin D mechlorethamine -> NOT cyclophosphamide |
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Which chemo drugs cause radiation recall?
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free radical-forming drugs
actinomycin D doxorubicin bleomycin |
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What are the uses of allopurinol?
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Treat hyperuricemia, urica acid precipitates in kidney (given alongside chemo drugs to help w/side effects)
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Why might hydration/diuretics be given to certain cancer pts?
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reduce cisplatin nephrotoxicity
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What are the uses of leucovorin?
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limit toxicity of high dose methotrexate
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Why might hematopoietic growth factors (i.e. filgrastim) be given to cancer pts?
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restores bone marrow derived cells (RBCs, lymphocytes, granulocytes, platelets)
=> allows high dose chemo w/much less toxicity & reduces risk of infxn |
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Which transcription factors can estrogen bind to besides ERE (via indirect gene activation path)?
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fos/jun
Sp1 NF-kB |
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How does estrogen activate MAP kinase signalling?
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Src-dependent (ligand)
Rapid, non-nuclear interactions |
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What are the physiological effects of glucocorticoids?
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increased gluconeogenesis (liver)
increased release of amino acids (muscle) increased release of fatty acids-lipolysis (fat) increased plasma glucose increased insulin secretion (pancreas-in response to glucose) decreased glucose uptake (muscle) increased bone resorption decreased fibroblast proliferation decreased collagen synthesis changes in mood and excitability altered leukocyte functions (anti-inflammatory) |
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What are the anti-inflammatory mechanisms of glucocorticoids?
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alters leukocyte traffic control
inhibits leukocyte function inhibits the prostaglandin-leukotriene pathway |
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What are the toxic effects of glucocorticoids?
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hyperglycemia
weakness fat redistribution osteoporosis thin skin, bruising growth retardation masking underlying dz causing inflammation |
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What are LXR, FXR, & PXR?
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Nuclear receptors
LXR & FXR: regulation cholesterol & bile homeostasis PXR: regulates druge metabolic (CYP) genes |
