Term
Antimetabolites act during the ___ phase |
|
Definition
|
|
Term
Podophyllotoxins act during which cell cycle phases? |
|
Definition
|
|
Term
Bleomycin acts during the ____ phase |
|
Definition
|
|
Term
Vinca alkaloids act during the __ phase |
|
Definition
|
|
Term
Which drugs act during the S phase? |
|
Definition
antimetabolites and podophyllotoxins |
|
|
Term
which drugs act during the G2 phase? |
|
Definition
podophyllotoxins and bleomycin |
|
|
Term
which drug acts only during G2? |
|
Definition
|
|
Term
which drugs act during M phase? |
|
Definition
|
|
Term
Increased DNA repair can be responsible for resistance, especially for which drugs? |
|
Definition
alkylating agents and cisplatin |
|
|
Term
alkylating agents and cisplatin -- method of resistance? |
|
Definition
|
|
Term
Formation of thiol trapping agents - resistance to which drugs? |
|
Definition
bleomycin, cisplatin, anthracyclines |
|
|
Term
bleomycin, cisplatin, anthracyclines -- resistance mechanism? |
|
Definition
formation of thiol trapping agents |
|
|
Term
changes in dihydrofolate reductase and increased synthesis of the enzyme are methods of resistance to which drug? |
|
Definition
|
|
Term
method of resistance to methotrexate? |
|
Definition
increased synthesis of or change in dihydrofolate reducatase |
|
|
Term
resistance to purine and pyrimidine antimetabolites can result from... |
|
Definition
decrease in activity of enzymes needed to convert them to cytotoxic metabolites |
|
|
Term
Decreasing the activity of enzymes needed to convert prodrugs to active cytotoxic metabolites is a method of resistance against which drugs? |
|
Definition
purine and pyrimidine antimetabolites |
|
|
Term
increased activity of enzymes capable of inactivating cancer drugs is a method of resistance to most of the... |
|
Definition
purine and pyrimidine antimetabolites |
|
|
Term
How do cancer cells produce an accelerated efflux of many drugs? |
|
Definition
increased expression of a normal gene (MDR1) for a cell surface glycoprotein |
|
|
Term
increased expression of a normal gene (MDR1) for a cell surface glycoprotein results in... |
|
Definition
accelerated efflux of many drugs |
|
|
Term
the alkylating agents include which broad groups? |
|
Definition
nitrogen mustards, nitrosoureas, alkylsulfonates |
|
|
Term
nitrogen mustards, nitrosoureas, alkylsulfonates - what type of drugs are these? |
|
Definition
|
|
Term
Which drugs act in PART as alkylating agents? |
|
Definition
cisplatin, dacarbazine, procarbazine |
|
|
Term
cisplatin, dacarbazine, procarbazine - these act in PART as ... |
|
Definition
|
|
Term
name the nitrogen mustards |
|
Definition
chlorambucil, cyclophosphamide, mechlorethamine |
|
|
Term
chlorambucil, cyclophosphamide, mechlorethamine - what are these? |
|
Definition
|
|
Term
|
Definition
|
|
Term
carmustine, lomustine - what are these? |
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
Are the alkylating agents CCS or CCNS? |
|
Definition
|
|
Term
Alkylating agents act on nucleophilic groups on DNA bases, particularly... |
|
Definition
|
|
Term
Which drugs act on N-7 of guanine and other nucleophilic groups on DNA bases? |
|
Definition
|
|
Term
What does alkylating bases do? |
|
Definition
leads to cross-linking, abn base-pairing, DNA strand breakage |
|
|
Term
What enzyme is needed for antitumor activity of cyclophosphamide? |
|
Definition
|
|
Term
p450 enzymes are needed for antitumor activity of... |
|
Definition
|
|
Term
one of the breakdown products of the biotransformation of cyclophosphamide is... |
|
Definition
|
|
Term
|
Definition
a breakdown product of the biotransformation of cyclophosphamide |
|
|
Term
|
Definition
GI distress, myelosuppression, alopecia, hemorrhagic cystitis (acrolein), cardiac dysfunct, pulm tox, SIADH |
|
|
Term
What can be used to decrease hemorrhagic cystitis from cyclophosphamide? |
|
Definition
|
|
Term
|
Definition
decreasing hemorrhagic cystitis from cyclophosphamide |
|
|
Term
Name the drug - Tox: GI distress, myelosuppression, alopecia, hemorrhagic cystitis (acrolein), cardiac dysfunct, pulm tox, SIADH |
|
Definition
|
|
Term
|
Definition
spontaneously converts to cytotoxic product |
|
|
Term
which drug spontaneously converts to cytotoxic product? |
|
Definition
|
|
Term
mechlorethamine - used for what? |
|
Definition
|
|
Term
which drug is best known for use in Hodgkin's lymphoma? |
|
Definition
|
|
Term
|
Definition
GI distress, myelosuppression, alopecia, sterility. Marked vesicant actions. |
|
|
Term
Name the drug - Tox: GI distress, myelosuppression, alopecia, sterility. Marked vesicant actions. |
|
Definition
|
|
Term
cisplatin, carboplatin, oxaliplatin are what? |
|
Definition
|
|
Term
Cisplatin is used IV, distributes to most tissues and is cleared... |
|
Definition
in unchanged form by kidney |
|
|
Term
what is oxaliplatin used for? |
|
Definition
|
|
Term
|
Definition
GI, mild hematotoxicity, neurotoxic, nephrotoxic (can be reduced with mannitol and forced hydration). |
|
|
Term
Name the drug - Tox: GI, mild hematotoxicity, neurotoxic, nephrotoxic (can be reduced with mannitol and forced hydration). |
|
Definition
|
|
Term
How does toxicity of carboplatin compare to cisplatin? |
|
Definition
less nephrotoxic, less likely to cause tinnitus and hearing loss, more likely to cause myelosuppression |
|
|
Term
Compares to cisplatin, which drug is less nephrotoxic, less likely to cause tinnitus and hearing loss, but more likely to cause myelosuppression? |
|
Definition
|
|
Term
Oxaliplatin causes dose-limiting... |
|
Definition
|
|
Term
which platinum analog causes dose-limiting neurotoxicity? |
|
Definition
|
|
Term
|
Definition
forms hydrogen peroxide, generates free radicals, causes DNA strand scisson |
|
|
Term
Which drug forms hydrogen peroxide, generates free radicals, causes DNA strand scisson? |
|
Definition
|
|
Term
procarbazine is orally active, penetrates into most tissues, including CSF, and is eliminates via... |
|
Definition
|
|
Term
What is the primary use of procarbazine? |
|
Definition
|
|
Term
|
Definition
myelosuppressant, GI, CNS dysfunct, peripheral neuropathy, skin rxns, inhibits MAO and hepatic enzymes, causes disulfiram-like rxns with ethanol, it's leukemogenic |
|
|
Term
Name the drug - tox: myelosuppressant, GI, CNS dysfunct, peripheral neuropathy, skin rxns, inhibits MAO and hepatic enzymes, causes disulfiram-like rxns with ethanol, it's leukemogenic |
|
Definition
|
|
Term
Busulfan is sometimes used in... |
|
Definition
|
|
Term
|
Definition
adrenal insufficiency, pulm fibrosis, skin pigmentation |
|
|
Term
Which drug causes adrenal insufficiency, pulm fibrosis, skin pigmentation? |
|
Definition
|
|
Term
Carmustine and lomustine are highly ___-soluble drugs used in _____ tumors. |
|
Definition
|
|
Term
Which drugs are highly lipid-soluble drugs used in management of brain tumors? |
|
Definition
|
|
Term
dacarbazine is used in regimens for... |
|
Definition
|
|
Term
|
Definition
alopecia, rash, GI, myelosuppression, phototoxicity, flulike syndrome |
|
|
Term
Name the drug - tox: alopecia, rash, GI, myelosuppression, phototoxicity, flulike syndrome |
|
Definition
|
|
Term
Name 2 antagonists of purines |
|
Definition
mercaptopurine, thioguanine |
|
|
Term
mercaptopurine and thioguanine are... |
|
Definition
|
|
Term
Name 3 pyrimidine antagonists |
|
Definition
FU, cytarabine, gemcitabine |
|
|
Term
FU, cytarabine, gemcitabine- what are these? |
|
Definition
|
|
Term
Two agents act in the pathway from ribonucleotides to deoxynucleotides. What are they? |
|
Definition
|
|
Term
4 agents act in the pathway from deoxynucleotides to DNA. What are they? |
|
Definition
methotrexate, gemcitabine, FU, cytarabine |
|
|
Term
methotrexate causes a decrease in the synthesis of... |
|
Definition
thymidylate, purine nucleotides and amino acids |
|
|
Term
which drug causes a decrease in the synthesis of thymidylate, purine nucleotides and amino acids? |
|
Definition
|
|
Term
the formation of _____ derivates of methotrexate are important for cytotoxic action |
|
Definition
|
|
Term
Methotrexate is given orally and IV and has good tissue distribution except to.. |
|
Definition
|
|
Term
Describe the metabolism/clearance of methotrexate |
|
Definition
not metabolized, clearance is dependent on renal function |
|
|
Term
why do you need adequate hydration with methotrexate? |
|
Definition
to prevent crystallization in renal tubules |
|
|
Term
|
Definition
bone marrow spupression, mucositis, hepatotoxicity, pulm infiltrates and fibrosis - enhanced by salicylates, NSAIDs, sulfonamides, sulfonylureas |
|
|
Term
Name the drug- tox: bone marrow spupression, mucositis, hepatotoxicity, pulm infiltrates and fibrosis - enhanced by salicylates, NSAIDs, sulfonamides, sulfonylureas |
|
Definition
|
|
Term
the toxic effects of methotrexate on normal cells may be reduced by administration of... |
|
Definition
leucovorin (folinic acid) |
|
|
Term
6-MP and 6-TG are activated by... |
|
Definition
|
|
Term
HGPRTases activate which drugs? |
|
Definition
|
|
Term
how can tumor cells be resistant to 6-MP or 6-TG? |
|
Definition
decreased HGPRTases, increased alkaline phosphatases that inactivate the toxic nucleotides |
|
|
Term
describe the oral bioavailability of 6-MP and 6-TG |
|
Definition
|
|
Term
The metabolism of ______ by xanthine oxidase is inhibited by allopurinol |
|
Definition
|
|
Term
allopurinol inhibits the metabolism of... |
|
Definition
6-MP, by xanthine oxidase |
|
|
Term
purine antimetabolites are used mainly in the ... |
|
Definition
|
|
Term
which drugs are used mainly in the acute leukemias and CML? |
|
Definition
|
|
Term
|
Definition
converted to 5-FdUMP -> inhibits thymidylate synthase, leads to thymineless death of cells |
|
|
Term
which drug inhibits thymidylate synthase? |
|
Definition
|
|
Term
Does 5-FU get into the CSF? |
|
Definition
|
|
Term
elimination of 5-FU is mainly via... |
|
Definition
|
|
Term
Name a drug used for cancers of bladder, breast, colon, head and neck, liver, ovarian, topically for keratoses and BCC |
|
Definition
|
|
Term
|
Definition
GI distress, myelosuppression, alopecia |
|
|
Term
|
Definition
a pyrimidine antimetabolite |
|
|
Term
|
Definition
it's activated by kinases to AraCTP, an inhibitor of DNA polymerases. |
|
|
Term
which drug is activated by kinases to AraCTP, an inhibitor of DNA polymerases? |
|
Definition
|
|
Term
Cytarabine is the drug most specific for the ___ phase |
|
Definition
|
|
Term
Which drug is MOST specific for the S phase? |
|
Definition
|
|
Term
|
Definition
|
|
Term
which drug is a deoxycytadine analog? |
|
Definition
|
|
Term
|
Definition
it is converted into active diphosphate and triphosphate nucleotide forms and inhibits ribonucleotide reductase. It can also be incorporated into DNA and cause chain termination. |
|
|
Term
Which drug is converted into active di-and triphosphate nucleotide forms, inhibits ribonucleotide reductase and is incorporated into DNA, causing chain termination? |
|
Definition
|
|
Term
elimination of gemcitabine is mainly by ______ |
|
Definition
|
|
Term
|
Definition
primarily myelosuppression, mainly as neutropenia. pulm tox has been observed |
|
|
Term
Name the drug - tox: primarily myelosuppression, mainly as neutropenia. pulm tox has been observed |
|
Definition
|
|
Term
plant alkaloids include which groups of drugs? |
|
Definition
vinca alkaloids, podophyllotoxins, camptothecins, taxanes |
|
|
Term
vinca alkaloids, podophyllotoxins, camptothecins, taxanes -- these are all under which classification? |
|
Definition
|
|
Term
|
Definition
vinblastine, vincristine, vinorelbine |
|
|
Term
vinblastine, vincristine, vinorelbine - what type of drug are these? |
|
Definition
|
|
Term
|
Definition
|
|
Term
etoposide, teniposide - what type of drug are these? |
|
Definition
|
|
Term
|
Definition
|
|
Term
topotecan, irinotecan - what are these? |
|
Definition
|
|
Term
|
Definition
|
|
Term
paclitaxel, docetaxel - what are these? |
|
Definition
|
|
Term
|
Definition
block formation of mitotic spindle by preventing assembly of tubulin dimers into microtubules. |
|
|
Term
Which drugs block formation of mitotic spindle by preventing assembly of tubulin dimers into microtubules? |
|
Definition
|
|
Term
Vinca alkaloids act primary during the __ phase |
|
Definition
|
|
Term
Vinca alkaloids must be given _____ |
|
Definition
|
|
Term
Do vinca alkaloids penetrate the CSF? |
|
Definition
|
|
Term
How are vinca alkaloids cleared? |
|
Definition
|
|
Term
What is vinorelbine used for? |
|
Definition
non-small cell lung CA, breast CA |
|
|
Term
Toxicity of vinblastine and vinorelbine? |
|
Definition
GI distress, alopecia, BM suppression |
|
|
Term
Vincristine does not cause serious ______ but has ______ actions |
|
Definition
myelosuppression, neurotoxic actions |
|
|
Term
What are the neurotoxic actions of vincristine? |
|
Definition
areflexia, peripheral neuritis, paralytic ileus |
|
|
Term
|
Definition
increase degradation of DNA, possibly via interaction with topisomerase II, also inhibits mitochondrial electron transport |
|
|
Term
Name the drug- MOA: increase degradation of DNA, possibly via interaction with topisomerase II, also inhibits mitochondrial electron transport |
|
Definition
|
|
Term
In which phases is etopiside most active? |
|
Definition
|
|
Term
Which drug is most active in late S and early G2? |
|
Definition
|
|
Term
Which drug is an analog of etopiside with similar characteristics? |
|
Definition
|
|
Term
|
Definition
analog of etoposide with similar characteristics |
|
|
Term
Is etoposide absorbed after oral admin? How is it eliminated? |
|
Definition
|
|
Term
|
Definition
GI irritant, alopecia, BM suppression |
|
|
Term
topotecan and irinotecan - MOA? |
|
Definition
inhibit topoisomerase I: they damage DNA by inhibiting an enzyme that cuts and relegates single DNA strands during normal DNA repair processes |
|
|
Term
Name the drugs - MOA: inhibit topoisomerase I: they damage DNA by inhibiting an enzyme that cuts and relegates single DNA strands during normal DNA repair processes |
|
Definition
|
|
Term
irinotecan is a prodrug that is converted into its active metabolite in the... |
|
Definition
|
|
Term
elimination of topotecan and irinotecan? |
|
Definition
topo - renally, irino - bile and feces |
|
|
Term
what is topotecan used for? |
|
Definition
second line therapy for advanced ovarian CA, small cell lung CA |
|
|
Term
what is irinotecan used for? |
|
Definition
|
|
Term
what are the 2 most common toxicities of topotecan and irinotecan? |
|
Definition
myelosuppression and diarrhea |
|
|
Term
paclitaxel and docetaxel - MOA? |
|
Definition
interfere with the mitotic spindle, prevent microtubule DISASSEMBLY into tubulin monomers |
|
|
Term
Name the drug: MOA- interfere with the mitotic spindle, prevent microtubule DISASSEMBLY into tubulin monomers |
|
Definition
|
|
Term
How are paclitaxel and docetaxel given? |
|
Definition
|
|
Term
the taxanes are used in... |
|
Definition
advanced breast and ovarian CA |
|
|
Term
|
Definition
neutropenia, thrombocytopenia, peripheral neuropathy, hypersensitivity rxns during infusion |
|
|
Term
Name the drug - tox: interfere with the mitotic spindle, prevent microtubule DISASSEMBLY into tubulin monomers |
|
Definition
|
|
Term
|
Definition
neurotoxicity and BM suppression |
|
|
Term
|
Definition
neurotoxicity and BM suppression |
|
|
Term
doxorubicin, daunorubicin, bleomycin, dactinomycin, mitomycin - what class are these? |
|
Definition
|
|
Term
doxorubicin and daunorubicin are_____ |
|
Definition
|
|
Term
|
Definition
doxorubicin and daunorubicin |
|
|
Term
doxorubicin and daunorubicin - MOA? |
|
Definition
intercalate btw base pairs, inhibit topisomerase II, generate free radicals, block synthesis of DNA and RNA, cause DNA strand scission, cause membrane disruption |
|
|
Term
name the drugs: MOA- intercalate btw base pairs, inhibit topisomerase II, generate free radicals, block synthesis of DNA and RNA, cause DNA strand scission, cause membrane disruption |
|
Definition
doxorubicin and daunorubicin |
|
|
Term
anthracyclines are CCNS or CCS? |
|
Definition
|
|
Term
doxorubicin and daunorubicin must be given... |
|
Definition
|
|
Term
how are the anthracyclines metabolized/excreted? |
|
Definition
metab in liver, products excreted in bile and urine |
|
|
Term
The main use of daunorubicin is in the treatment of... |
|
Definition
|
|
Term
idarubicin is approved for use in... |
|
Definition
|
|
Term
|
Definition
BM suppression, GI distress, severe alopecia, CARDIOTOXICITY |
|
|
Term
What may protect against cardiotoxicity from anthracyclines? |
|
Definition
|
|
Term
What does dexrazoxane do? |
|
Definition
it's an inhibitor of iron-mediated free radical formation, may protect against cardiotoxicity of anthracyclines |
|
|
Term
______ formulations of doxorubicin may be less cardiotoxic |
|
Definition
|
|
Term
|
Definition
generates free radicals, bind to DNA and cause strand breaks, inhibit DNA syn |
|
|
Term
Name the drug - MOA: generates free radicals, bind to DNA and cause strand breaks, inhibit DNA syn |
|
Definition
|
|
Term
Is bleomycin CCS or CCNS? |
|
Definition
|
|
Term
|
Definition
|
|
Term
Bleomycin is inactivated by tissue ______, but some renal clearance of intact drug also occurs |
|
Definition
|
|
Term
|
Definition
pulm dysfunction, hypersensitivity reactions, mucocutaneous rxns |
|
|
Term
|
Definition
binds dsDNA and inhibits DNA-dep RNA synthesis |
|
|
Term
name the drug - MOA: generates free radicals, bind to DNA and cause strand breaks, inhibit DNA syn |
|
Definition
|
|
Term
dactinomycin must be given _____, and intact drug and metabolites are excreted in ____ |
|
Definition
|
|
Term
dactinomycin is used in... |
|
Definition
|
|
Term
|
Definition
BM suppression, skin rxns, GI irritation |
|
|
Term
|
Definition
metabolized by liver enzymes to form alkylating agent that cross-links DNA |
|
|
Term
Mitomycin is given ____ and is rapidly cleared via _____ |
|
Definition
|
|
Term
Clinical use of mitomycin? |
|
Definition
acts against hypoxic tumor cells, used for adenocarcinoma of cervix, stomach, pancreas, lung |
|
|
Term
Name the drug - acts against hypoxic tumor cells, used for adenocarcinoma of cervix, stomach, pancreas, lung |
|
Definition
|
|
Term
|
Definition
causes severe myelosuppression, toxic to heart, liver, lung, kidney |
|
|
Term
What is the most commonly used glucocorticoid in cancer chemotherapy? What is it used for? |
|
Definition
prednisone, leukemias and lymphomas |
|
|
Term
What is tamoxifen? What is the effect on endometrium? |
|
Definition
SERM, agonist -> ^ risk of cancer |
|
|
Term
|
Definition
N/V, hot flashes, vaginal bleeding, venous thrombosis, ^risk endometrial hyperplasia/neoplasia |
|
|
Term
|
Definition
a newer estrogen recep antagonist used in advanced breast cancer |
|
|
Term
What is flutamide and what is it used for? |
|
Definition
androgen receptor antagonist used in prostatic carcinoma |
|
|
Term
Name an androgen receptor antagonist used in prostatic carcinoma |
|
Definition
|
|
Term
|
Definition
gynecomastia, hot flashes, hepatic dysfunction |
|
|
Term
|
Definition
leuprolide, gosrelin, nafarelin |
|
|
Term
leuprolide, gosrelin, nafarelin - what are these? |
|
Definition
|
|
Term
|
Definition
bone pain, gynecomastia, hematuria, impotence, testicular atrophy |
|
|
Term
Name the drug - tox: bone pain, gynecomastia, hematuria, impotence, testicular atrophy |
|
Definition
|
|
Term
Name 2 aromatase inhibitors |
|
Definition
|
|
Term
anastrozole, letrozole - what are these? |
|
Definition
|
|
Term
|
Definition
androstenedione -> estrone |
|
|
Term
aromatase inhibitors are used in... |
|
Definition
|
|
Term
aromatase inhibitors - tox? |
|
Definition
N/D, hot flashes, bone and back pain, dyspnea, peripheral edema |
|
|
Term
What does asparaginase do? What's it used for? |
|
Definition
depletes serum asparagine, used in treatment of T cell auxotrophic cancers (leukemia and lymphoma) |
|
|
Term
|
Definition
hypersensitivity, acute pancreatitis, bleeding |
|
|
Term
Name the drug - tox: hypersensitivity, acute pancreatitis, bleeding |
|
Definition
|
|
Term
|
Definition
inhibits the TKase activity of protein product of Bcr-Abl oncogene expressed in CML |
|
|
Term
In addition to CML, imatinib is used for... |
|
Definition
GIST (c-kit TKase is also inhibited) |
|
|
Term
|
Definition
diarrhea, myalgia, fluid retention |
|
|
Term
Name the drug- tox: diarrhea, myalgia, fluid retention |
|
Definition
|
|
Term
____-interferons are effective against hairy cell leukemia, early CML and t-cell lymphomas |
|
Definition
|
|
Term
|
Definition
myelosuppression and neuro dysfunction |
|
|
Term
What is rituximab and how does it work? |
|
Definition
monoclonal Ab that binds a surface protein in non-Hodgkin's lymphoma cells and induces complement-mediated lysis, direct cytotoxicity,induction of apoptosis |
|
|
Term
Name the drug - monoclonal Ab that binds a surface protein in non-Hodgkin's lymphoma cells and induces complement-mediated lysis, direct cytotoxicity,induction of apoptosis |
|
Definition
|
|
Term
|
Definition
|
|
Term
Rituximab use is associated with... |
|
Definition
hypersensitivity rxns and myelosuppression |
|
|
Term
|
Definition
monoclonal Ab against HER-2/neu receptor for epidermal growth factor |
|
|
Term
name a monoclonal Ab against HER-2/neu receptor for epidermal growth factor |
|
Definition
|
|
Term
|
Definition
nausea, vomiting, chills, fevers, HA. May cause cardiac dysfunction, CHF |
|
|
Term
Name the drug - tox: nausea, vomiting, chills, fevers, HA. May cause cardiac dysfunction, CHF |
|
Definition
|
|
Term
|
Definition
antibody against extracellular domain of EGFR |
|
|
Term
name an antibody against extracellular domain of EGFR |
|
Definition
|
|
Term
what are gefitinib and erlotinib? |
|
Definition
small molecule inhibitors of the EGFR TK domain |
|
|
Term
name the small molecule inhibitors of the EGFR TK domain |
|
Definition
|
|
Term
what are the main toxicities of gefitinib and erlotinib? |
|
Definition
|
|
Term
|
Definition
monoclonal Ab that binds VEGF |
|
|
Term
name a monoclonal Ab that binds VEGF |
|
Definition
|
|
Term
adverse effects of bevacizumab? |
|
Definition
HTN, arterial thrombosis, impaired wound healing, GI perforation, proteinuria |
|
|