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60 Cards in this Set
- Front
- Back
methotrexate mechanism
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- S-phase specific antimetabolite
- folic acid analog that inhigits DHFR -> decreased dTMP -> decreased DNA and protein synthesis |
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methotrexate clinical use
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- leukemia, lymohoma, choriocarconima, sarcomas
- abortion, actopic pregnancy, rhemuatoid arthritis, psoriasis |
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methotrexate toxicity
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- myelosuppression, reversibe w/ leucovorin (folinic acid) rescue
- macrovasicular fatty change in liver |
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5-FU mechanism
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- S-phase specific antimetabolite
- pyrimidine analog bioactivated to 5F-dUMP - covalently complexes folic acid which inhibits thymidylate synthase -> decrease dTMP |
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5-FU use
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leukemias, lymphomas (not CLL or hodgkins)
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5-FU toxicity
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- BM, GI, liver
- metabolized to xanthine oxidase, so toxicity icreases w/ allopurinol |
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busulfan - everything
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- alkylates DNA
- used for CML - can cause pulmonar fibrosis or hyperpigmentation |
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Cytrabine - everything
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- inhibits DNA polymerase
- used for AML - can cause leukopenia, thrombocytopenia, and megaloblastic anemia |
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Cyclophosphamide, ifosfamide mechanism
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- alkylating agent
- covalently link interstand DNA at G N-7 - requires bioactivation by the liver |
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Cyclophosphamide, ifosfamide use
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- NH lymphoma, breast and ovarian carcinomas
- acts as immunosuppressent |
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Cyclophosphamide, ifosfamide toxicity
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- myelosuppression
- hemorrhagic cystitis which can be prevented w/ mensa |
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Nitosurases types
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carmustine, lomustine, semustine, streptozocin
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Nitosurases mechanism
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- alkylates DNA
- requires bioactivation - can cross BBB |
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Nitosurases use
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brain tumors (including glioblastona multiform)
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Nitosurases toxicity
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CNS
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Cisplatian, carboplatin mechanism
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- alkylating agents
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Cisplatian, carboplatin use
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testicular, bladder, ovary, and lung carcinomas
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Cisplatian, carboplatin toxicity
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nephrotoxicity an acoustic nerve damage
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doxorubicin (adriamycin) mechanism
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- noncovalently intercalates in DNA
- creates breaks in CNA strands to decrease replication - generated free radicals |
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doxorubicin (adriamycin) use
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- part of ABVD combo regimin for hodgkins
- for myelomas, sarcomas, and solid tumors (breast, lung, ovary) |
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doxorubicin (adriamycin) toxicity
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- cardiotoxicity
- myelosuppression and marked alopecia - toxic sctravasation |
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bleomycin, dactinomycin mechanism
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formation of free radicals which can brek DNA
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bleomycin, dactinomycin use
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testicular cancer and lymphomas
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bleomycin, dactinomycin toxicity
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- pulmonary fibrosis
- skin changes - minimal myelosuppression (bleomycin) |
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etopside mechanism
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G2-phase agent that inhibits topoisomerase II adn increases DNA degradation
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etopside use
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- oat cell carcinomas of the lung
- prostate, testicular cancer |
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etopside toxicity
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- myelosuppression
- GI irritation - alopecia |
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prednisone mechanism
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- may trigger apoptosis
- may even work on nondividing cells |
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prednisone use
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- most commonly used glucocorticoid in chemo
- CLL, hodgkins (part of MOPP) - immunosuppressant |
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prednisone toxicity
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- cushing-like syndrome
- immunosup, cataracts, acne, osteoporosis, hypertension, peptic ulcers, hyperglycemia, pshcyosis |
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Tamoxifen, raloxifene mechamism
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- estrogen receptor mixed agonist/antoagonist
- blocks the binding of estrogen to estrogen receptor positive cells |
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Tamoxifen, raloxifene use
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breast cancer, good to prevent osteoporosis
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Tamoxivfn, raloxifene toxicity
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- may increase risk of endometial carcinoma
- hot flashes |
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trastuzumab (herceptin) mechanism
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- momoclonal Ab against HER-2 (erb_B2)
- helps kill breast cnacer cells that overexpress it (Ab dependent cytotoxicity) |
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trastuzumab (herceptin) use
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metastatic breast cancer
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trastuzumab (herceptin) toxicity
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cardiotoxicity
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vincristine, vinblastine mechanism
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- M-phase alkaloid
- binds tubulin to block poly of microtubules - mitotic spindle cant form |
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vincristine, vinblastine use
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- lymphoma (MOPP) "Oncovin"
- wilms' tumor - choriocarcinoma |
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vincristine, vinblastine toxicity
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- vincristine has neurotoxicity, paralytic ileus
- vinBLASTin basts BM |
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paclitaxel mechanism
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- M-phase
- binds tubulin to hyperstabilize poly of microtubules - mitotic spindle cannot break down (no anaphase) |
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paclitaxel use
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ovarian and breast carcinoma
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paclitaxel toxicity
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myelosuppression and hypersensitivity
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drugs that interfere w/ nuclutide synthesis to DNA
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- methotrexate
- 5-FU - 6-MP |
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drugs that interfere w/ DNA to mRNA
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- alkylating agents and cisplatin - cross linkage
- dactomycin and doxorubicin - intercalte strands - bleomycin - etopside - strand breaks - steriods - tamoxifen |
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drugs that interfere w/ protein
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- vinca alkyloids - inhibit mucrotubule formation
- paclitaxel - inhibitmicrotubule disassembly |
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drugs that get the M pahse
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vinca alkaloids and taxols
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drugs that get the G2 pahse
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bleomycin
podophyllotoxins |
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drugs that get the S pahse
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podophyllotoxins
antimetabolites |
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cell cycle specific
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- antimetabolites
- plant alkyloids - steroid hormones - bleomycin - paxlataxel - etoposide |
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cell cycle nonspecific
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- alkylating agents
- antibiotics |
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paclitaxel use
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ovarian and breast carcinoma
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paclitaxel toxicity
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myelosuppression and hypersensitivity
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drugs that interfere w/ nuclutide synthesis to DNA
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- methotrexate
- 5-FU - 6-MP |
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drugs that interfere w/ DNA to mRNA
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- alkylating agents and cisplatin - cross linkage
- dactomycin and doxorubicin - intercalte strands - bleomycin - etopside - strand breaks - steriods - tamoxifen |
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drugs that interfere w/ protein
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- vinca alkyloids - inhibit mucrotubule formation
- paclitaxel - inhibitmicrotubule disassembly |
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drugs that get the M pahse
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vinca alkaloids and taxols
|
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drugs that get the G2 pahse
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bleomycin
podophyllotoxins |
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drugs that get the S pahse
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podophyllotoxins
antimetabolites |
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cell cycle specific
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- antimetabolites
- plant alkyloids - steroid hormones - bleomycin - paxlataxel - etoposide |
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cell cycle nonspecific
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- alkylating agents
- antibiotics |