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57 Cards in this Set
- Front
- Back
which cancer drugs are cell cycle specific (5)
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antimetabolites (MTX, 5-FU, 6-MP), etoposide, bleomycin, vinca alkaloids, paclitaxel
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which cancer drugs are cell cycle nonspeficic (2)
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alkylating agents, antibiotics
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MOA of MTX
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S-phase specific antimetabolite. Inhibits duhydrofolate reductase (b/c is folate acid analog)
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Clinical uses of MTX
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leukemias, lymphomas, choriocarcinomas, sarcomas, abortion, ectopic preggers, RA, psoriasis
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toxicities of MTX
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myelosuppression (use leucovorin for "rescue"), macrovesicular fatty change in liver
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MOA 5-FU
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S-phase specific antimetabolite. Bioactivated form (5F-dUMP complexes with folic acid and inhits thymidylate synthase
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Clinical use of 5-FU
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colon cancer and other solid tumors, basal cell carcinoma (topical). Synergy with MTX
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toxicity of 5-FU
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myelosuppression which is NOT reversible with leucovorin (vs MTX); photosensitivity
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MOA 6-MP
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blocks de novo purine synthesis
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what activates 6-MP?
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HGPRTase
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Toxicities of 6-MP
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done marrow, GI, liver; metabolized by xanthine oxidase so increased toxicity with allopurinol
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MOA cytarabine (ara-C)
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inhibits DNA polymerase
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Clinical use of ara-C?
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AML
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toxicities of ara-C
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leukopenia, thrombocytopenia, megaloblastic anemia
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MOA of cyclophosphamide/ifosfamide
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(alkylaying agts) covalently x-link DNA at guanine N-7; require bioactivation by liver
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Clinical use of cyclophosphamide/ifosfamide
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non-Hodgkin's lymphoma, breast and ovarian carcinomas
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toxicities of cyclophosphamide
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myelosuppressin, hemorrhagic cystitis (use mesna!!)
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4 nitrosoureas
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carmustine, lomustine, semustine, streptozocin
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MOA of nitrosoureas
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(e.g. carmustine, steptozocin). Alkylate DNA; require bioactivation; CROSS BBB!!
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toxicities of nitrosoureas
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CNS (dizziness, ataxia)
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MOA of cisplatin, carboplatin
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act like alkylating agents
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clinical uses of cisplatin?
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testicular, bladder, ovary, and lung carcinomas
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toxicity of cisplatin?
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nephrotoxicity and acoustic nerve damage
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MOA of busulfan
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alkylates DNA
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clinical use of busulfan
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CML
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toxicities of busulfan
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pulmonary fibrosis, hyperpigmentation
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MOA of doxorubucin, daunurubicin
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generate free radicals and noncovalently intercalate into DNA
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Clinical uses of doxorubucin, daunorubicin
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part of ABVD treatment for Hodgkin's; also for myelomas, sarcomas, solid tumors
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toxicities of doxorubicin, daunorubicin
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cardiotoxic; myelosuppression, marked alopecia; toxic extravasation
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MOA dactinomycin
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DNA intercalater
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clinical uses of dactinomycin
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Wilm's tumor, Ewing's sarcoma, rhabdomyosarcoma (for childhood tumors!)
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toxicity of dactinomycin
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myelosuppression
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MOA of bleomycin
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induces formation of free radicals-->DNA strand breaks
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Clinical uses of bleomycin
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testicular cancer; part of ABVD for Hodgkin's (along with doxorubicin/daunorubicin)
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toxicities of bleomycin
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PULMONARY FIBROSIS, skin changes, MINIMAL myelosuppression
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MOA of etoposide
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G2 phase specific agt, inhibits topoisomerase II
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Clinical uses of etoposide
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small cell carcinoma of lung and prostate, testicular carcinoma
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Toxicities of etoposide
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myelosuppression, GI irritation, alopecia
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MOA of prednisone
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steroid; may trigger apoptosis?
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Clinical uses of prednisone
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lots but spefically part of MOPP regimen for Hodgkin's , CLL
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Toxicities of prednisone
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Cushing-like sxs; immunosuppression, CATARACTS, acne, OSTEOPOROSIS, HTN, peptic ulcers, hyperglycemia, psychosis
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MOA of tamoxifen, raloxifene
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estrogen R antagonits in breasts, agonists in bone
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tamoxifen vs raloxifene
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tamoxifen may increase risk of endometrial cancer but raloxifene is an endometrial ANTAGonist
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MOA of trastuzumab (herceptin)
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monoclonal Ab against HER-2; helps kill breast cancer cells that overexpress HER-2
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Clinical use of trastuzumab
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(herceptin) metastatic breast cancer
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toxicity of trastuzumab
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cardiotoxicity
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MOA of imatinib?
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(Gleevec) Phl chromosome bcr-abl tyrosine kinase inhibitor
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Clinical uses of imatinib
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(gleevec) CML, GI stromal tumors
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toxicity of imatinib
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(gleevec) fluid retention
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MOA of vincristine, vinblastine
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(vinca alkaloids) M phase specifics, bind tubulin and block polymerization of microtubules
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Clinical uses of vincristine, vinblastine
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part of MOPP regimen (as is prednisone) for lymphoma, Wilms' tumor, choriocarcinoma
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toxicity of vincristine
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neurotoxicity, paralytic ileus
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toxicity of vinblastine
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myelosuppression (vinBLASTine BLASTS bone marrow)
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MOA of taxols
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(e.g. paclitaxel) M phase specific agents to bind tubulin and disallow microtubule breakdown
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clinical uses of taxols
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ovarian and breast carcinomas
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toxicities of taxols
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myelosuppression and hypersensitivity
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Which cancer drugs are M-phase specific?
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taxols and vinca alkaloids
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