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57 Cards in this Set
- Front
- Back
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What is the mechanism of action of methotrexate?
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inhibits dihydrofolate reductase, decreased dTMP and decreased DNA
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What drugs are cell cycle specific?
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Antimetabs (MTX, 5-FU, 6-MP
etoposide bleomycin vinca alkaloids paclitaxel |
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What drugs are cell cycle nonspecific?
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alkylating agents
Abtics |
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What phase of the cell cycle do the vinca alkaloids and taxols work on?
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M
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What part of the cell cycle do the antimetabolites work on?
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S
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What part of the cell cycle does etoposide work on?
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S and G2
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What part of the cycle does Bleomycin work on?
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G2
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What is MTX used for clinically?
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Leukemias
lymphomas choriocarcinoma sarcomas abortion ectopic preggs RA psoriasis |
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What is the mechanism of action of 5-FU?
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Pyrimidine analog activated to 5F-dUMP- covalently complexes folic acid.
Inhibs thymidylate synthase. decreased dTMP |
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What are the SEs of MTX?
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myelosuppression- reversible with leucovorin
Macrovesicular fatty change in liver |
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What is the role of leucovorin?
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reverses MTX myelosuppression
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When is 5FU used clinically?
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colon cancer, other solid tumors
basal cell carcinoma- topical Synergy w/ MTX |
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What are the SEs of 5FU?
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Myelosuppression- not reversible
photosensitivity |
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What is the mechanism of action of 6-mercaptopurine?
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blocks de novo purine synthesis. Activated by HGPRTase
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What is 6-MP clinically used for?
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Leukemias, lymphomas (not CLL or hodgkins)
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What are the SEs of 6-MP?
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BM, GI, Liver
metabed by xanthine oxidase increased tox with allopurinol |
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What is the mechanism of action of Cytarabine?
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inhibs DNA polymerase
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What is cytarabine used for?
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AML
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What is the tox of Cytarabine?
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Leukopenia, Tpenia, Megaloblastic anemia
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What is the mechanism of action of alkylating agents?
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covalently x-link DNA at N-7
require bioactivation by the liver |
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What are the two major alkylating agents?
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Cyclophosphamide
Ifosfamide |
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What is the clinical use of Cyclophosphamide and Ifosfamide?
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Non-Hodgkin's lymphoma, breast and ovarian carcinomas. Immunosuppression
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What are the SEs of cyclophosphamide and ifosfamide?
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Myelosuppression; hemorrhagic cystitis, prevented with mesna
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What is the mechanism of action of the Nitrosureas?
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alkylate DNA, require bioactivation, cross BBB
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What is the clinical use for Nitrosureas?
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brain tumors (including glioblastoma multiforme)
crosses BBB |
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what are the SEs of Nitrosureas?
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CNS tox- dizzy, ataxia
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What are the Nitrosureas?
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carmustine
lomustine semustine streptozocin |
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What is the mechansim of action of Cisplatin and Carboplatin?
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alkylate DNA
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What is Cisplatin used for?
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Testicular, bladder, ovary and lung carcinoma
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What are the SEs of Cisplatin?
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Nephrotox, acoustic nerve damage
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What is the mechanism of action of Busulfan?
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alkylates DNA
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What is Busulfan clinically used for?
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CML
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What is the tox of Bulsulfan?
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Pulm fibrosis, hyperpigmentation.
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What is the mech of action of Doxorubicin (adriamycin) and daunorubicin?
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generates free radicals and noncovalently intercalates in DNA Creating breaks
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What is Adriamycin used for clinically?
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ABVD of Hodgkins
myelomas, sarcomas and solit tumors breast, ovary, lung |
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What are the SEs of adriamycin
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Cardiotox
myelosuppression marked alopecia toxic extravaasaion. |
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What is the mechanism of action of Dactinomycin (actinomycin D)?
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Intercalates in DNA.
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What is actinomycin used for clinically?
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ACTinomycin ACTS out, just like kids. Kids tumors
Wilm's Ewing's Rhabdomyosarcoma |
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What is the tox of actinomycin?
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Myelosuppression
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What is the mechanism of action of Bleomycin?
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Free radicals
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What is bleomycin used for clinically?
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testes
ABVD in hodgkins |
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What are the SEs of Bleomycin?
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plm fibrosis, skin changes
minimal myelosuppression |
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What is the mechanism of action of Etoposide?
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G2-phase-specific- inhibs topo II and increases DNA degredation
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What is Etoposide used for clinically?
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small cell carcinoma of lung and prostate, teste carcinoma
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What is prednisone used for in cancer treatment?
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CLL, Hodgkins
can trigger apoptosis |
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What is the mechanism of action of Tamoxifen?
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SERM
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What are the SEs of Tamoxifen?
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may increase risk of endometrial carcinoma
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What is the mechanism of action of trastuzumab?
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Herceptin
Monoclonal Ab against HER-2 (erb-B2) breast cancer |
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What are the SEs to Trastuzumab?
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Herceptin
Cardiotoxicity |
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What are the SEs of Imatinib?
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Fluid retention
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What is the mechanism of vincristine/vinblastine?
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M phase alkaloid that bind to tubulin and block polymerization of microtubules so that mitotic spindle cannot form
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What is vincristine used for clinically?
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mOpp for lymphoma
wilm's tumor choriocarcinoma |
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What are the SEs of vincristine?
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neurotox (areflexia, peripheral neuritis)
paralytic ileus |
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What are the SEs of vinblastine?
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BLAST's Bone Marrow
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What is the mechanism of action of Paclitaxel?
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M-phase specific agents that bind to tubulin and hyperstabalize it. No anaphase
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What is the clinical use of Paclitaxel?
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Ovarian and breast cancer
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What are the SEs of Paclitaxel
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myelosuppression
hypersensitivity |
