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43 Cards in this Set
- Front
- Back
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Acquired resistance developos during therapy. One method is through amplification of target genes. Gene amplification occurs in what phenotype? How?
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Multidrug resistance phenotype (MDR1 gene). Cells overproduce cell surface glycoproteins (P-glycoprotein) which actively transports agents out of the cell. Cell fails to accumulate toxic concentrations of drugs.
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Whats the MOA of cancer chemotheraputic alkylating agent?
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They contain an electrophiliic center which covalently links nucleophilic centers on target molecules (N-7 of guanine and O of purines/pyrimidines in DNA). This causes abnormal base pairing, depurination, cleavage, crosslinking. Act in all stages of the cell cycyle.
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Name the nitrogen mustard derivatives (part of the alkylating agents) that are used in chemotherapy.
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Mechlorethamine
Cyclophosphamide Ifosfamide Melphalan Chlorambucil Busulfan |
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Patient with non-Hodgkin's leukemia is put on the CHOP regimen. One of the drugs causes hemorrhagic cystitis. Which one and how do you treat it?
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The metabolite acrolein of cyclophosphamide causes this side effect which can be prevented by coadministration of MESNA. MESNA neutralizes acrolein at acidic pH in urine.
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What receptor does Ondansetron (as well as other -setrons) act on?
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5-HT3 receptor antagonists, which are used to treat nausea and vomiting associated with chemotherapy.
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Which alkylating agent has the potential to produce a fatal pulmonary fibrosis?
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Busulfan lung.
Busulfan is used to treat myeloproliferative disorders (CML). |
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Nitrosoureas, part of the alkylating agents, are unique because they can ____________. Name the nitrosoureas.
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Cross the blood brain barrier. They are lipophilic. They carbamylate intracellular molecules.
Carmustine, lomustine, streptozocin. |
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What is dacarbazine used to treat and how does it work?
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It is used to treat malignant melanoma. Its proposed that it is an alkylating agent, but it is unknown. It ultimately inhibits DNA, RNA, and protein synthesis.
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What are anti-metabolites (as chemotherapeutic drugs) and where do they act in the cell cycle?
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Antimetabolites are S-phase specific drugs that are structural analogues of essential metabolites that interfere with DNA synthesis. Myelosuppresion is the does-limiting toxicity.
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Name the metabolite that these drugs inhibit:
1) Methotrexate 2) Cytarabine 3) Mercaptopurine 4) Fluorouracil 5) Thioguanine 6) Capecitabine 7) Gemcitabine 8) Cladribine |
1) Folic acid analogue
2) Pyrimidine antagonist 3) Purine analogue 4) Pyrimidine antagonist 5) Purine analogue 6) Converted to 5-FU (pyrimidine antagonist) 7) Nucleotide analogue 8) Purine analog |
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Cytarabine is a pyrimidine antagonist. One of its metabolites inhibits _______.
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DNA polymerases. Cytarabine is commonly used in AML treatments.
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Methotrexate is a folic acid analogue that inhibits ______, thus inhibiting DNA synthesis.
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Methotrexate inhibits dihydrofolate reductase, therefore there is limited amounts of tetrahydrofolate that is required for the conversion of dUMP to dTMP.
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What drug is used as an adjunct with methotrexate in order to rescue folate?
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Leucovorin.
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In addition to cancer therapy, what is methotrexate used for?
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Therapeutic abortion, immune disorders, and psoriasis.
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What antimetabolite drug inhibits thymidylate synthetase?
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Fluorouracil (5-FU). Also, capecitabine is a prodrug that is converted to 5-FU.
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What anti-metabolite is used for hairy cell leukemia?
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Cladribine, which is a purine analogue.
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What anti-metabolite is used to treat acute promyelocytic leukemia (M3)?
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Tretinoin, a vitamin A derivative.
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What is the mechanism of the vinca alkaloid cancer drugs? Name them.
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Vinblastine, vincristine, vinorelbine.
Vinca alkaloids are derived from periwinkle plants and bind to tubilin disrupting microtubule assemply and the formation of the mitotic spindle. Active during mitosis at metaphase. |
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What is the dose-limiting toxicity of:
vinblastine vincristine |
Vinblastine: bone marrow suppression with leukopenia (other side effects: neurologic toxicity, alopecia, nausea, vomiting).
Vincristine: peripheral neuropathies (other side effects: severe constipation and alopecia). |
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Paclitaxel and doetaxel act in _____ phase of the cell cycle. What are there main side effects?
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These drugs stabilize microtubules and arrest the cell cycle in mitosis. Myelosuppression and peripheral neuropatheis are the does-limiting toxicities.
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What cancer drug binds to topoisomerase II causing DNA breaks?
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Etoposide.
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This phase nonspecific cancer drug acts by intercalating between guanosine-cytosine base pairs of DNA forming a stable complex, thus inhibiting RNA synthesis.
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Dactinomycin.
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What antibiotic drugs can produce both reversible acute and irreversible chronic cardiomyopathies?
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Doxorubicin, daunorubicin, and idarubicin. These drugs intercalate in DNA blocking DNA and RNA synthesis. They act in the S phase of the cell cycle.
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Bleomycin is produced by streptomyces and it causes DNA chain scission and fragmentation. Where does this drug accumulate to toxic levels? What other major side effect may occur when bleomycin is given to patients with lymphoma?
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Bleomycin hydrolase inactivates bleomycin and is found in many tissue except for lung and skin.
Anaphylactoid-like reactions. |
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The regimen of bleomycin, cisplatin, and etoposide are often used to treat _______.
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Testicular cancer.
Bleomycin - DNA scission Etoposide - complexes with topoisomerase II Cisplatin - DNA crosslinking |
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Name the antibiotic cancer drug that is often used to treat hypercalcemia or hypercalciuria associated with malignant disease by its action on osteoclasts.
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Plicamycin.
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The -tecan cancer drug (topotecan and ironotecan) act by inhibiting ______ resulting in DNA damage.
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Topoisomerase I.
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What is the dose-limiting toxicity of cisplatin? How is this prevented?
Can you name the other side effects of cisplatin? |
Damage to the renal tubules. Treat by hydration and diuresis.
Ototoxic, peripheral neuropathy, nausea, and vomiting. |
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Hydroxyurea. What is its MOA? What is its major adverse effect?
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Inhibits ribonucleoside diphophate reducatase which catalyzes the conversion of ribonucleotides to deoxyribonucleotides.
Adverse effect: hematopoietic depression. |
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What factor does thalidomide reduce?
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Tumor necrosis factor.
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Patient test results come back and show a positive BCR-ABL fusion gene. What drug should you use to treat?
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Imatinib is a tyrosine kinase inhibitor specific for the BCR-ABL oncoprotein.
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Both gefitinib and erlotinib inhibit the same receptor and can be used in non-small cell lung cancer. What receptor do they target?
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Epidermal growth factor receptor tyrosine kinase.
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What antigen is overexpressed on B cells of non-Hodgkin's lymphoma tissues and is used as a target for chemotherapy?
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CD20 antigen. Rituximab is a chimeric human/mouse IgG antibody that binds to CD20 antigens on B cells. The net effect of this interaction is cell lysis
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Rituximab is used for what hematological disorder?
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Thrombocytopenic purpura.
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What IgG antibody can be used to treat breast cancer ?
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Trastuzumab.
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Cetuximab is a monoclonal antibody chemotherapy drug. What cancer is this drug currently approved to treat?
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Metastatic colon cancer. It is an IgG antibody to epidermal growth factor receptor. It differs from imatinib in that cetuximab actually blocks the receptor and induces apoptosis.
Bevacizumab is another IgG approved for colon cancer, but this drug is directed against VEGF thus inhibiting angiogenesis. |
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Patient with breast cancer test positive for an estrogen receptor tumor? What drugs would be effective in this individual? If the patient is 40 years old, what additional drug would you also administer?
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Tamoxifen and toremifene (SERMs - selective estrogen receptor modulator). Premenopausal women also should receive a gonadotropin-releasing analog such as leuprolide.
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What sort of side effects may a 60 year old women on anastrozole (for her breast cancer) experience?
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Anastrozole is an aromatase inhibitor (no effect on steroid synthesis). It is used for postmenopausal women with breast cancer. Short-term effects: hot flashes. Long-term effects: osteopenia, thrombogenic, and risk of endometrial cancer.
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Filgrasti and pegfilgastim are used as prophylaxis and treatment against _________.
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Chemotherapy induced neutropenia. These drugs are granulocyte colony-stimulating hormones.
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Sargramostim is used to assist graft recovery in patients undergoing bone. What is sargramostim?
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Recombinant human granulocyte/macrophage colony-stimulating hormone (GM-CSF).
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What enzyme does allopurinol act on?
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Xanthine oxidase thus preventing severe uric acid build.
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Chemotherpay-induced thrombocytopenia can be treated prophylactically with....
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Oprelvekin: an interleukin.
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What advantage does fulvesatrant have over the SERMS (e.g. tamoxifen)?
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Fulvesatrant is associated with much lower risk of causing endometrial pathology, including cancer. It is a pure estrogen antagonist while SERMs have estrogenic agonist activity in some tissues.
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