Term
| This category of chemotherapeutics form covalent bonds with DNA thus impeding replication: |
|
Definition
|
|
Term
| Alkylating Agents act by: |
|
Definition
| Forming covalent bonds with DNA thus impeding replication. |
|
|
Term
| This category of chemotherapeutic contain platinum: |
|
Definition
| Platinum-containing DNA-binding Drugs |
|
|
Term
| These are the two subcategories of DNA-binding agents: |
|
Definition
| Alkylating agents, platinum-containing DNA-binding drugs |
|
|
Term
|
Definition
| Blocking or subverting one or more of the metabolic pathways involved in DNA synthesis. |
|
|
Term
| This category of chemotherapeutics block or subvert one or more of the metabolic pathways involved in DNA synthesis: |
|
Definition
|
|
Term
| This category of chemotherapeutics have a microbial origin, which prevents mammalian cell division: |
|
Definition
|
|
Term
| Cytotoxic antibiotics are of microbial origin, which: |
|
Definition
| Prevent mammalian cell division |
|
|
Term
| This category of chemotherapeutics specifically affect microtubule function (i.e. interfere with formation of mitotic spindles): |
|
Definition
|
|
Term
| Microtubule inhibitors act by: |
|
Definition
| Interfering with the formation of mitotic spindles |
|
|
Term
| Microtuble inhibitors are of this origin: |
|
Definition
|
|
Term
| This category of chemotherapeutics suppresses hormone dependent tumor types: |
|
Definition
|
|
Term
| Hormones act as chemotherapeutics by: |
|
Definition
| Suppressing hormone dependent tumor types |
|
|
Term
| Alkylating agents are used to treat a wide variety of: |
|
Definition
| Lymphatic and solid cancers |
|
|
Term
| The most significant adverse effect of alkylating agents is: |
|
Definition
| They are mutagenic and carcinogenic (i.e. can lead to a secondary malignancy such as acute leukemia) |
|
|
Term
| Mechlorethamine is in this category of chemotherapeutics: |
|
Definition
|
|
Term
| Mechlorethamine was originally used as a______ during _______. |
|
Definition
|
|
Term
|
Definition
|
|
Term
| Mechlorethamine causes lymphocytopenia, which is: |
|
Definition
| A lower than normal level of lymphocytes |
|
|
Term
| Mechlorethamine is used to treat this type of cancers: |
|
Definition
|
|
Term
| Mechlorethamine is a bifunctional agent, meaning it: |
|
Definition
| Can bind and react with two separate sites |
|
|
Term
| Mechlorethamine is transported by: |
|
Definition
| Chloine Uptake Transporter |
|
|
Term
| Once mechlorethamine is transported by a choline uptake transporter, it: |
|
Definition
| Loses a chloride ion and forms a reactive intermediate that can alkylate N7-nitrogen of guanine residues in DNA --> leads to cross-linking between guanine residues and facilitates in DNA strand breakage. |
|
|
Term
| Resistance to mechlorethamine is associated with: |
|
Definition
| Decreased cellular permeability, increased conjugation w/ thiols (glutathione), and possible increase in DNA repair |
|
|
Term
| Mechlorethamine is a very _____ compound; thus, it must be made just prior to administration. |
|
Definition
|
|
Term
| Adverse effects of mechlorethamine include: |
|
Definition
| Severe nausea, vomiting, and bone marrow depression |
|
|
Term
| This drug is the most common alkylating agent: |
|
Definition
|
|
Term
| Cyclophosphamide are first: |
|
Definition
| Biotransformed to hydroxylated intermediates by hepatic P450 enzymes, which are then broken down to form active compounds. |
|
|
Term
| The cytotoxic step (i.e. alkylation of DNA) of cyclophosphamide is: |
|
Definition
| Reaction of the phosphoramide mustard with DNA |
|
|
Term
| Resistance to cyclophosphamide is due to: |
|
Definition
| Either increased DNA repair or decreased drug permeability |
|
|
Term
| Cyclophosphamide is used to treat these cancers: |
|
Definition
| Burkitt's lymphoma, breast cancer, lung cancer, non-Hodgkins lymphomas, acute leukemia |
|
|
Term
| Cyclophosphamide is preferably administered: |
|
Definition
|
|
Term
| Cyclophosphamide may be administered by these routes: |
|
Definition
|
|
Term
| Adverse effects of cyclophosphamide include: |
|
Definition
| Bladder toxicity, myelosuppression, transient alopecia, emetic potential |
|
|
Term
| This metabolite of cyclophosphamide may accumulate and lead to bladder toxicity: |
|
Definition
|
|
Term
| Acrolein, a metabolite of cyclophosphamide, can accumulate and cause: |
|
Definition
| Chronic fibrosis and acute ulceration with bleeding. |
|
|
Term
| Bladder toxicity due to cyclophosphamide may be prevented by: |
|
Definition
| Hydration, high urine flow, frequent voiding, or GIVING A NUCLEOPHILIC THIOL SUCH AS SODIUM THIOLSULFATE OR MESNA TO CONJUGATE ACROLEIN. |
|
|
Term
| This sub-category of alkylating agents contains carmustine, lomustine, and streptozotocin: |
|
Definition
|
|
Term
| These closely related nitrosoureas can penetrate the CNS: |
|
Definition
|
|
Term
| This nitrosourea is used in the management of pancreatic islet cell carcinoma, carcinoid tumor, colorectal cancer, and pancreatic adenocarcinoma: |
|
Definition
|
|
Term
| Carmustine is administered via this route: |
|
Definition
|
|
Term
| Lomustine is administered via this route: |
|
Definition
|
|
Term
| Streptozocin is particularly toxic to the: |
|
Definition
| Insulin-producing beta cells of the pancreas in mammals |
|
|
Term
| Streptozocin can be used for treating specific cancers of these pancreatic cells: |
|
Definition
|
|
Term
| The cytotoxic effect of nitrosoureas is expressed only during this stage of the cell cycle: |
|
Definition
|
|
Term
| Nitrosoureas can alkylate during the resting phase of the cell cycle, but: |
|
Definition
| Cytotoxicity is only expressed during division, so non-dividing cells can escape death if DNA repair occurs. |
|
|
Term
| Resistance to nitrosoureas is thought to be: |
|
Definition
|
|
Term
| The primary use for nitrosoureas is: |
|
Definition
|
|
Term
| Nitrosoureas are highly _____, thus they distribute heavily to all tissues. |
|
Definition
|
|
Term
| Adverse effects of nitrosoureas include: |
|
Definition
| Profound myelosuppression, mutagenesis, carcinogenesis |
|
|
Term
| Streptozocin may be used to treat brain tumors and: |
|
Definition
|
|
Term
| This drug kills off beta-cells of the pancreas, thus it can be used to treat insulinomas: |
|
Definition
|
|
Term
| This drug is an inorganic planar coordinate complex of platinum, which binds to DNA nucleophiles following the loss of the chlorides in the intracellular mileau: |
|
Definition
|
|
Term
| Cisplatin enters the cell and binds to the ______ residues of DNA. |
|
Definition
|
|
Term
| Cisplatin binds to the guanine residues of DNA: |
|
Definition
| Forming intra and inter -strand cross-links --> Inhibits DNA and RNA synthesis |
|
|
Term
| Cisplatin is effective in any phase of the cell cycle, but is most effective during: |
|
Definition
|
|
Term
| Resistance to cisplatin is due to: |
|
Definition
| Increased DNA repair, cross-resistance between cisplatin and carboplatin |
|
|
Term
| Adverse effects of cisplatin include: |
|
Definition
| Severe emesis, nephrotoxicity (need concurrent hydration Tx), and myelosuppression |
|
|
Term
| This drug acts similarly to cisplatin, but is more slowly activated, not nephrotoxic, but will cause myelosuppression: |
|
Definition
|
|
Term
| This platinum-containing DNA-binding drug is often employed when patients cannot be vigorously hydrated or if they suffer kidney dysfunction: |
|
Definition
|
|
Term
| This is a new member of the platinum-containing DNA-binding drugs, which has shown significant effect against advanced colorectal cancer: |
|
Definition
|
|
Term
| These chemotherapeutic agents interfere with the availability of normal purine and pyrimidine nucleotide precursors by inhibiting their synthesis or by competing with them in DNA and RNA synthesis: |
|
Definition
|
|
Term
| This class of chemotherapeutic agents have close structural similarity to DNA and RNA bases: |
|
Definition
|
|
Term
| These chemotherapeutic agents oftem require metabolic activation within target tumor cells: |
|
Definition
|
|
Term
| These chemotherapeutic agents are schedule dependent and their action is enhanced by repetitive or prolonged administration: |
|
Definition
|
|
Term
| Antimetabolites exhibit this dose-limiting toxicity: |
|
Definition
|
|
Term
| Methotrexate is structurally related to: |
|
Definition
|
|
Term
| This drug is structurally related to folic acid: |
|
Definition
|
|
Term
| Methotrexate acts as a(n)_______ to folic acid. |
|
Definition
|
|
Term
| Methotrexate antagonizes folic acid by inhibiting: |
|
Definition
|
|
Term
| This enzyme which converts folic acid to its active coenzyme is antagonized by Methotrexate: |
|
Definition
|
|
Term
| This drug decreases FH4, which depresses DNA, RNA, and protein synthesis: |
|
Definition
|
|
Term
| Methotrexate decreases FH4, which: |
|
Definition
| Decreases biosynthesis of thymidylic acid, methionine, serine and purines (adenine and guanine); depresses DNA and RNA and protein synthesis |
|
|
Term
| This drug can be used to rescue bone marrow via reversal of a folate deficiency: |
|
Definition
|
|
Term
| This drug bypasses the inhibition of DHFR and replenishes the concentration of folic acid: |
|
Definition
|
|
Term
| High doses of this drug can be curative for osteogenic sarcoma and choiocarcinoma, but the high doses result in significant myelosuppression: |
|
Definition
|
|
Term
| Leucovorin may be used to rescue _________ because of a __________. |
|
Definition
| Bone marrow; folate deficiency |
|
|
Term
| MTX is not effective in these cells: |
|
Definition
|
|
Term
| MTX is clinically used to treat these types of cancers: |
|
Definition
Acute lymphocytic leukemia, Burkitt's lymphoma in children, breast cancer, choriocarcinoma, OSTEOGENIC SARCOMA;
Other uses: inflammatory diseases such as rheumatoid arthritis |
|
|
Term
| This drug is an oral, cell cycle-phase specific antineoplastic agent used chiefly in the treatment of acute lymphoblastic leukemia: |
|
Definition
|
|
Term
| 6-Mercaptopurine is a chemical analog of: |
|
Definition
|
|
Term
| 6-Mercaptopurine functions as this class of chemotherapeutic agent: |
|
Definition
|
|
Term
| 6-Mercaptopurine substitutes for this purine base in RNA and DNA: |
|
Definition
|
|
Term
| Substitution of 6-Mercaptopurine for guanine results in: |
|
Definition
|
|
Term
| The end result of 6-Mercaptopurine is that it: |
|
Definition
| Blocks biosynthesis (blocks conversion of inosinate to AMP and GMP). |
|
|
Term
| 5-Fluorouracil is a chemical analog to: |
|
Definition
|
|
Term
| 5-Fluorouracil in its parent form is: |
|
Definition
| Devoid of anti-cancer activity |
|
|
Term
| 5-Fluorouracil must be converted to this deoxynucleotide: |
|
Definition
|
|
Term
| 5-Fluorouracil is converted to 5-FdUMP, which competes with: |
|
Definition
| Deoxyuridine monophosphate (dUMP) |
|
|
Term
| This molecule is required for thymidylate synthase: |
|
Definition
| Deoxyuridine monophosphate (dUMP) |
|
|
Term
| 5-Fluorouracil results in a decrease in ___________ due to a lack of ____. |
|
Definition
|
|
Term
| 5-Fluorouracil is primarily used to treat these types of cancers: |
|
Definition
| Slow growing cancers, such as: breast, colon, ovarian, and pancreatic cancers. Also penetrates the CNS. |
|
|
Term
| Adverse effects of 5-Fluorouracil include: |
|
Definition
| Severe ulceration of oral and GI mucosa and bone marrow depression. Because of GI effects, it is given I. V. |
|
|
Term
| Doxorubicin is in this category of chemotherapeutic agents: |
|
Definition
|
|
Term
| Daunorubicin is in this category of chemotherapeutic agents: |
|
Definition
|
|
Term
| Cytotoxic antibiotics owe their cytotoxic action to: |
|
Definition
| Their interactions with DNA |
|
|
Term
| Doxorubicin and daunorubicin are classified as this type of cytotoxic antibiotics: |
|
Definition
| Anthracycline antibiotics |
|
|
Term
| Doxorubicin and daunorubicin act by inserting ____ between _______ to ______ backbones of DNA. |
|
Definition
| Doxorubicin and daunorubicin act by inserting NON-SPECIFICALLY between BASE-PAIRS to SUGAR PHOSPHATE backbones of DNA. |
|
|
Term
| Intercalation of doxorubicin/daunorubicin causes: |
|
Definition
| Local uncoiling of DNA, thus blocking DNA and RNA synthesis |
|
|
Term
| DNA breaks by interfering with _____ forming a stable complex, thus preventing__________ of DNA strands. |
|
Definition
| DNA breaks by interfering with TOPOISOMERASE II forming a stable complex, thus preventing REUNION of DNA strands. |
|
|
Term
| Generation of ____ also contributes to DNA strand breakage. |
|
Definition
| Oxygen radicals (superoxide ions and H2O2) |
|
|
Term
| When are cells most sensitive to doxorubicin/daunorubicin? |
|
Definition
| Near the end of G1-phase and S-phase |
|
|
Term
| Resistance to doxorubicin/daunorubicin may be due to: |
|
Definition
| Decreased topoisomerase II, decreased drug accumulation due to increased efflux (via PGP), and increased glutathione peroxidase activity |
|
|
Term
| Doxorubicin is clinically used: |
|
Definition
| For a wide range of clinical activity for solid tumors and leukemia. |
|
|
Term
| Daunorubicin is limited to clinically treat: |
|
Definition
| Acute myelogenous leukemias |
|
|
Term
| Doxorubicin and daunorubicin have poor oral absorption, so they are administered: |
|
Definition
|
|
Term
| Doxorubicin is associated with ______ at high doses. |
|
Definition
| Cardiac toxicity: Necrosis of myocytes and irreversible cardoimyopathy and congestive heart failure! |
|
|
Term
| Adverse effects of doxarubicin include: |
|
Definition
| Cardiac toxicity (!!!), myelosuppression, total hair loss, N/V |
|
|
Term
| Irreversible, dose-dependent cardiotoxicity of doxorubicin is a result of: |
|
Definition
| The generation of free radicals and lipid peroxidation. |
|
|
Term
| This cytotoxic antibiotic intercalates in the minor groove of DNA between adjacent guanosine-cytosine pairs: |
|
Definition
|
|
Term
| A stable dactinomycin-DNA complex is formed by: |
|
Definition
| The intercalation of dactinomycin in the minor groove of DNA between adjacent guanosine-cytosine pairs. |
|
|
Term
| The dactinomycin-DNA complex interferes with the movement of: |
|
Definition
|
|
Term
| The movement of RNA polymerase along the gene is inhibited by _________, thus preventing transcription. |
|
Definition
|
|
Term
| Resistance to dactinomycin is due to: |
|
Definition
| Enhanced DNA repair or decreased drug accumulation due to increased efflux (via PGP) |
|
|
Term
| Dactinomycin is used clinically: |
|
Definition
| In combination with vincristine for Wilm's tumors (childhood associated kidney tumors) |
|
|
Term
| This drug, like the anthracylin antibiotics, causes breaks in the DNA by oxidative processes: |
|
Definition
|
|
Term
| When DNA-Bleomycin-Fe++ is oxidized to Fe+++, the following result: |
|
Definition
|
|
Term
| Bleomycin is most selective in this phase of the cell cycle: |
|
Definition
| G2 and mitosis (but is also effective in cells in non-dividing cells, i.e. Go) |
|
|
Term
| Bleomycin is used to treat: |
|
Definition
| Hodgkin's Lymphoma and testicular tumors (with vinblastine or etoposide) |
|
|
Term
| The dose-limiting adverse effect of bleomycin is: |
|
Definition
|
|
Term
| Bleomycin is unusual in that it rarely causes this adverse effect: |
|
Definition
|
|
Term
| Vincristine and vinblastine are examples of this category of chemotherapeutic agents: |
|
Definition
|
|
Term
| Vincristine and vinblastine block mitosis in this phase, and bind maximally in this phase of the cell cycle: |
|
Definition
|
|
Term
| Vincristine and vinblastine act by binding ______ and inhibiting its polymerization into microtubules. This eventually causes an arrest at metaphase. |
|
Definition
|
|
Term
| The dose-limiting toxicity of vincristine is: |
|
Definition
|
|
Term
| The dose limiting toxicity of vinblastine is: |
|
Definition
|
|
Term
| Vincristine and vinblastine are often used in _________ with other chemo drugs. |
|
Definition
|
|
Term
| Taxol is an example of this category of chemotherapeutic agent: |
|
Definition
|
|
Term
| Taxol binds _____ to tubulin. |
|
Definition
|
|
Term
| Taxol _____ polymerization and stabilization of microtubules. |
|
Definition
|
|
Term
| Why does taxol promote the stablization of polymerization and stabilization of microtubules? |
|
Definition
| This results in super stable microtubules that don't dissociate during anaphase and results in cell death. |
|
|
Term
| Taxol resistance is most notably due to: |
|
Definition
|
|
Term
|
Definition
| Ovarian and metastatic breast cancer |
|
|
Term
| The dose limiting toxicity of taxol is: |
|
Definition
| Neutropenia (loss of neutrophils) |
|
|
Term
| This drug can be coadministered with taxol to prevent problems associated with neutropenia: |
|
Definition
|
|
Term
| Filgrastim is used with taxol to: |
|
Definition
| Treat neutropenia by stimulating neutrophil production |
|
|
Term
| Tamoxifen is an example of this category of chemotherapeutic agents: |
|
Definition
|
|
Term
| Tamoxifen acts as an estrogen ______ used to treat estrogen dependent breast cancers. |
|
Definition
|
|
Term
|
Definition
| COMPETITIVE estrogen receptor antagonist |
|
|
Term
| Tamoxifen binds _____ to estrogen receptors and ____ the receptors. |
|
Definition
| Competitively; antagonizes --> Estrogen-responsive genes and RNA synthesis does NOT occur. |
|
|
Term
| Tamoxifen is [cell cycle specific/cell cycle non-specific] |
|
Definition
| Cell cycle non-specific (i.e. Tamoxifen's action is not related to any specific phase of the cell cycle) |
|
|
Term
| Tamoxifen is given with this drug in pre-menopausal women to lower estrogen: |
|
Definition
|
|
Term
| This gonadotropin-releasing hormone analog is given with tamoxifen in pre-menopausal women: |
|
Definition
|
|
Term
| The dose limiting toxicity of tamoxifen is: |
|
Definition
|
|
Term
| These drugs are synthetic analogs of naturally-occurring gonadotropin-releasing hormone. |
|
Definition
|
|
Term
| Leuprolide is used as a ______ in the treatment of advanced prostatic cancer, and as a hormonal therapy in the treatment of ______. |
|
Definition
| Hormonal antagonist; endometriosis |
|
|
Term
| Leuprolide and goserelin provide a pharmaceutical ______ for the patient and deprives ____________-__________ ______ of testosterone and estrogen. |
|
Definition
| Castration; hormonally-dependent tumors. |
|
|
Term
| Leuprolide and goserelin MOA: |
|
Definition
| Occupy the GnRH receptor, leading to desensitization and inhibition in the release of FSH and LH. |
|
|
Term
|
Definition
| Synthetic anti-inflammatory corticosteroid |
|
|
Term
| Presnisone must first be reduced to _____ by 11-B-hydroxysteroid dehydrogenase. |
|
Definition
|
|
Term
| Prednisone binds to a receptor that triggers the production of specific proteins to induce ____ in lymphocytes. |
|
Definition
|
|
Term
| Prednisone is used to treat these cancers: |
|
Definition
| Acute lymphocytic leukemia, Hodgkin's and non-Hodgkin's lymphomas |
|
|
Term
| Trastuzumab and rituximab are classified as this category of chemotherapeutic agents: |
|
Definition
| Biological agents (more specifically monoclonal antibodies) |
|
|
Term
| Monoclonal antibodies are proteins produced by: |
|
Definition
|
|
Term
| Monoclonal antibodies bind to an antigen and: |
|
Definition
| Mark the target cell or foreign object for destruction and removal. |
|
|
Term
| Trastuzumab binds to this protein, which is a member of the epidermal growth factor receptor family (receptors with integral tyrosine kinase activity) |
|
Definition
|
|
Term
| Trastuzumab binds to Her2/neu inducing: |
|
Definition
| Antibody dependent cellular cytotoxicity |
|
|
Term
| Trastuzumab is used to treat: |
|
Definition
| Ovarian and breast cancers |
|
|
Term
| The dose limiting toxicity of trastuzumab is: |
|
Definition
|
|
Term
| Rituximab attaches to the _____ protein on ______ B cells. |
|
Definition
|
|
Term
| Rituximab attaches to CD20 protein on mature B cells and: |
|
Definition
| Blocks normal proliferation, induction of apoptosis, and targets cells for lysis. |
|
|
Term
| The Fab domain of rituximab binds to: |
|
Definition
| The CD20 antigen on B-cells |
|
|
Term
| The Fc domain of rituximab recruits ________, inducing complement and antibody dependent, cell-mediated ____ of the B cells. |
|
Definition
| Immune effector functions; Cytotoxicity |
|
|
Term
| This drug antagonizes serotonin at the 5-HT3 receptor: |
|
Definition
|
|
Term
| Ondansetron is used clinically as an: |
|
Definition
|
|
Term
| This dopamine receptor antagonist is used as an antiemetic: |
|
Definition
|
|
Term
| Prochloroperazine is effective against what kind of emetogenic chemotherapeutic agents? |
|
Definition
| Low or moderately emetogenic chemotherapeutics (e.g. fluorouracil and doxorubicin) |
|
|
Term
| This dopamine receptor antagonist has highly efficacious anti-emetic activity at high doses: |
|
Definition
|
|
Term
| This drug is used to treat anemia caused by chemotherapy, as well as anemia from other conditions (e.g. chronic renal failure): |
|
Definition
|
|
Term
| Epoietin Alfa stimulates: |
|
Definition
|
|
