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132 Cards in this Set
- Front
- Back
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what is the "log kill" hypothesis of anticancer agents?
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states that cytotoxic anticancer agents kills a certain percentage of cells, rather than a fixed number.
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cell cycle specific drugs act on …?
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proliferating cells (usually also cycle phase specific)
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dose dependent anticancer drugs act on …?
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non proliferating cells, they are dose dependent and cell cycle independent.
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what most often determines the upper limit of chemo tolerability?
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bone marrow supression
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what ccs anticancer agent acts in G2?
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bleomycin
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what ccs anticancer agents act in M?
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vinblastine, vincristine, pacilitaxel
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what are the dose dependent anticancer agents?
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alkyating agents, antitumor antibiotics, nitrosoureas, dacarbazide, and cisplatin
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What ccs anticancer agents act in S?
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cytarabine, 6-mercaptopurine, 6-thioguanine, methotrexate, hydroxyurea
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where in the cell cycle does etopside act?
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in the transition from S to G2.
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what is the MOA of methotrexate?
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inhibits DHF reductase (folic acid synthesis) - S phase
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when is methotrexate used clinically?
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leukemia, lymphoma, breast ca, rhematoid arthritis, and psoriasis
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what are the sfx of methotrexate?
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BMS (leucovorin rescue)
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what is leucovorin?
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folinic acid, used for rescue from sulfas and methotrexate and dapsone
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what is the MOA of cyclophosphamide?
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alkylating agent, G0, nucelophillic attack on guanine N7 -> dysfunctional DNA
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what is the most commonly used alkylating agent?
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cyclophosphamide
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when is cyclopohsphamide used clinically?
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non-hodgkins, neuroblastoma, ovarian, breast ca, DOC for Wegeners granulomatosis
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what is the primary sfx of cyclophosphamide?
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BMS (also hemorrhagic cystitis)
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what drug is cyclophosphamamide given with and why?
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MESNA: b/c it traps the acrolein byproduct and decreases renal and bladder toxicity
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what is 4-hydroperoxychyclophosphamide?
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a common bone marrow purging agent
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what is the mechanisms of cisplatin?
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alkylating agent - cross links DNA strands (CCNS but most active in S phase)
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when is cisplatin used clinically?
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solid tumors, testicular tumors, ovarian carcinoma, bladder, head, neck, lung
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what is the most effective anticancer agent for solid tumors?
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cisplatin
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what are the sfx of cisplatin?
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neprhotoxicity and neurotoxicity
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how can you decrease the nephrotoxicity of cisplatin?
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give with fluids and mannitol.
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when can you use carboplatin (an agent similar to cisplatin?)
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in ovarian cancer if pt is unable to tolerate cisplastin.
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what is doxorubicin?
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an antineoplastic
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what is the moa of doxorubicin?
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CCNS intercalates DNA, forms free radicals, and inhibits topoisomerase
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when is doxorubicin used clinically?
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leukemia, lymphoma, mm, ewings, kaposi,
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what are the sfx of doxorubicin?
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cardiomyopathy, bms, and gi upset are dose limiting
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what is vincristine?
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and M phase specific antineoplastic
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what is the MOA of vincristine?
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binds tubulin and blocks mitosis
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when is vincristine used clinically?
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leukemia, lymphomas, wilms, brain, rhabdomyosarcoma, hodkins (MOPP)
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what is the dose limiting sfx of vincristine?
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peripheral neruopathy
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what is vinblastine?
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and M phase specific antineoplastic
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when is vinblastine used clinically?
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testicular ca, kaposis, and hodgkins (ABVD)
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what is the MOA of vinblastine?
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binds tubulin and blocks mitosis
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what is the dose limiting sfx of vinblastine?
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bms
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what is bleomycin
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a G2 specific antitumor antibiotic
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what is the MOA of bleomycin?
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complexes with Fe and O2 -> DNA strand cuts in G2
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when is bleomycin used clinically?
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lymphomas, ovarian, and testicular tumors
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what is the dose limiting toxicity of bleomycin?
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pulmonary fibrosis (10% pts have significant loss of function)
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what are the clinical uses of alkylating agnets?
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wide range of tumors, cytotoxic to dividing and non dividing cells, can be used against slow growing malignancies
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what is the usual dose limiting toxicity of alkylating agnets?
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bms
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are cisplatin, carboplatin, and mitomycin alkylating agents?
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NO. While they do cross link DNA, they do NOT cross link DNA via alkylation … however they are cytotoxic by the same mechanism
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mechlorethamine and cyclophosphamide are what?
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nitrogen mustard alkylating agents
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when is mechlorethamine used clinically?
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HL (MOPP), NHL
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when is thiotepa used clinically?
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alkylating agent used in BC, ovarian cancer (however largely replaced by nitrogen mustards)
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when is carmustine used clinically?
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alkylating agent that crosses the BBB, used in meningeal leukemia and brain tumors
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when is busulfan used clinically?
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an alkylating agent used for chornic granulocytic leukemia
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when is mitomycin C used clinically?
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used with x-ray to attack hypotoxic tumor cells, adenocarcinomas of stomach, pancrease, and lung
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what are the severe sfx of mitomycin c?
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severe bms, and the "worst vesicant known to man"
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what is 5-fluorouracil?
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a S-phase specific antineoplasitc
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what is the MOA of 5-flurouracil?
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converts 5FU to 5Fdump, prevents DNA synthesis -> thymineless death of the cell
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when is 5-flurouracil used clinically?
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solid tumors, topically for solar keratosis or bassal cell ca
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what are the dose limiting toxicitids of 5FU
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bms, gi upset, and alopecia
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what is tamoxifen?
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a nonsteroidal anti-estrogen that binds to nuclear chromatin and inhibits rna synthesis
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what is the clinical use of tamoxifen?
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DOC for management of estrogen receptor positive breast cancer
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what is cytarabine?
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an S-phase antineoplastic
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what is the MOA of cytarabine?
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inhibits DNA synthesis
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when is cytarabine used clinically
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acute leukemias
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what are the dose limiting toxicities of cytarabine?
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bms and gi mucositis
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what is hydroxyurea?
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and S-phase antineoplastic
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what is the moa of hydroxyurea/.
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inhibits ribonucleotide reductase -> impaired dna synthesis
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when is hydroxyurea used clinically?
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CML (historically to increase potency of HIV regimens)
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what is the dose limiting toxicity of hydroxyurea?
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bms
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what is mercaptopurine?
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an Sphase specific antineoplasitc
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what is the moa of mercaptopurine?
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inhibits purine ring sytnehsis, and nucleotide interconversion - > inhibits dna synthesis
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when is mercaptopurine used clinically?
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in some leukemias, and as an immunosupressant in IBD
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what is the typical dose limiting toxicity of mercaptopurine?
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bms
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how is prednisone used clinically to treat neoplasms?
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childhood ALL, undifferentiated childhood lymphomas - used with vincristine and antracycline +/- mtx to induce reminssion and then as continuous remission maintenance with mtx
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what is pentostatin?
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and S-phase antineoplastic
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what is the moa of pentostatin?
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dATP anolog prevents de novo pruine synthesis - >inhibit dna synthesis
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when is pentostatin used clinically?
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hairy cell leukemia and T cell lymphomas
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what is the dose limiting toxicity of pentostatin?
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bms
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what is dactinomycin?
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a ccns antineoplastic
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what is the moa of dactinomycin?
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intercalates dna and blocks rna synthesis
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when is dactinomycin used clinically?
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rhabdomyosarcoma and wilms in children, ewings, and choriocarcinomas
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what is the dose limiting toxicity of dactinomycin?
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bms and gi upset
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what is etopside?
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a ccs specific antineoplastic that acts in late S to G2 phase of cell cycle
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what is the moa of etopside?
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induce strange breakage via DNA topoisomerase inhibition
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when is etopside used clinically?
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testicular, ovarian, lung ca, lymphomoa, aml, kaposi, osteo, neuroblastomas
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what are the dose limiting sfx of etopside?
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leukopenia, gi upset, and an usually hig rate of secondary leukemias in chidlren treated with etopside
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what is 6-thioguianine?
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an S phase specific antineoplastic antimetabolite
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what is the moa of 6-thioguianine?
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prodrug that inhibits purine synthesis, cuases dysfunctional rna (the same as 6-MP but 6TG has fewer indications and fewer side effects)
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what is the clincal use of 6 thioguanine?
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aml
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what is the dose limiting sfx of 6 thioguianine?
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bms
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what is herceptin?
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an antitumor monoclonal AB that binds her/neu antigen present on 1/4 of bcs (usually more aggressive)
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what is the clinical use of herceptin?
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breast cancer if express her/neu
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what are the sfx of herceptin?
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hypersensitivity rxns, chf, increased cardiotoxicity of doxorubicin
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what is GM-CSF
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an antineoplastic signal that simulates PMNs, macrophages, and eosinophils
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when is GM-CSF used clinically?
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recovery from bmt
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what does G-CSF do?
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stimulates pmn production
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when is G-CSF used clinically?
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prevent chemo induced neutropenia
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how is IL-2 used in cancer treatment?
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stimulates T cell production leads to malignant cell cytolysis, in advanced malignant melanoma
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what antineoplastics cause marked renal toxicity?
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cisplatin, methotrexate
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what antineoplastics causemarked hepatic toxicity?
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6MP, busulfan, cyclophosphamide
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what antineoplastics cause marked pulmonary toxicity?
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busuflan, bleomycin, procarbazine
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what antineoplastics cause marked cardiotoxicity?
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doxorubicin, daunorubicin
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what antineoplastics cause marked neurologic toxicity?
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vincristine, cisplatin, paclitaxel
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what antineoplastics are immunosupressive
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cyclophosphamide, cytarabine, dactinomycin, methotrexate
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what antineoplastic causes hemorrhagic cystitis and how do you treat it
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cyclophosphamide
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what antineoplastic has leukemia as a potential sfx?
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procarbazine
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what antineoplastic may lead to pancreatitis?
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asparaginase
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which antineoplastics are bone marrow sparing?
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cisplatin, bleomycin, vincristine, asparaginase
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what is cyclosporine?
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an immunosuppressant
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what is the moa of cyclosporine?
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inhibit cmi by blocking IL2 dependent growth and differentiation of T cells
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when is cyclosporine used clinically?
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doc: for organ or tissue transplant, topically (tacromalis) to treat atopic dermatitis, and on stents (sirolimus) to minimize restenosis after angioplasty
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what are the sfx of cyclosporine?
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peripheral neruopathy, nephrotoxicity, gingival overgrowth
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what is azathioprine?
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an immunosuppressant
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what is the moa of azathioprine?
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converted to 6MP - inhibits dna synthesis
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what is the clincal use of azathrioprine?
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ra, immunosupression for renal transplant
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what is RhoGam
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human IgGxRBCRhd antigen - used to prevent hemolytic dz of newborn in subsequent pregnancy to an Rh- mom (also use during miscarriage for same reason)
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what is etanercept and when is it used?
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an immunomodulator that binds TNF and is used to treat RA, and psoriasis
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what is thalidomide and when is it used?
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an immunmodulator - suppresses TNFa production, used for the skin manifefstations of lupus and leprosy - DO NOT USE IN PREGNANCY
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what is ANTI-CD3 and when is it used?
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monoclonal AbxTcellCD3 - impairs antigen recognition and suprresses immune system: used to prevent allograft rejection.
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what is ALG and when is it used?
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antilymphocytic globluin - polyclonal AbxTcell: used to decrease cmi and treat allograft rejection, sfx include serum sickness and nephritis
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abciximab, daclixumab, infliximab, muromonab, palivizumab, rituximab, and trastuxumab are all examples of what?
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monoclonal antibodies
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what mab is used to as antiplatelet therapy?
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abciximab - AbxIIbIIIaR.
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what mabs are used in kidney transplant?
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daclixumab, muromonmab
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what mab is used in ra and chrons disease?
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infliximab - AbxTNF
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what mab is used to treat rsv?
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palivizumab - AbxRSV
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what mab is used to treat NHL?
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rituximab - AbxNHLsuface protein
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what mab is used to treat some aggressive breast cas?
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trastuzumab (herceptin) Abxher2/neuR.
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what is aldesleukin and when is it used?
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IL2: increase T differentiation and NK cells in renal cell ca and metastatic melanoma
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when is IL11 used clinically?
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in thrombocytopenia to induce platelet formation
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what is filgrastim?
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G-CSF for marrow recovery
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what is sargramostim?
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GM-CSF for marrow recovery
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when is erythropoeitin used?
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anemia, especially associated with renal failure
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when is thrombopoietin used?
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thrombocytopenia
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when is Ifa used?
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hep B, hep C, leukemia, and melanoma
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when is IF B used?
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MS
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when is IF y used?
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CGD to increase TNF
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