Chemo Drugs

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Author:
eschott
ID:
82256
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Chemo Drugs
Updated:
2011-04-27 11:18:55
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Pharm4
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  1. What's the characteristic of Class 1 Chemo Agents?
    Kill cells regardless of state of proliferation
  2. What's the characteristic of Class 2 chemo agents?
    Kill cells in a specific phase of cell cycle; plateau proportional to fraction not at stage
  3. What's the characteristic of Class 3 chemo drugs?
    • Non-cycle specific
    • More effective against proliferating cells
  4. What are chemo drugs' effectiveness dependent on?
    Concentration and time of exposure
  5. What chemo class are Alkylating agents?
    Class III (no specific phase)
  6. What's the mechanism of alkylating agents?
    Induce DNA damage or p53 mediated apoptosis
  7. What's the specific mechanism of action of Nitrogen Mustards?
    • Alkylation of DNA at N-7 position of guanine
    • Misreading of DNA replication
  8. What is Mechlorethamine?
    Nitrogen Mustard Alkylating Agent
  9. What is Melphalan?
    • Nitrogen Mustart Alylating agent
    • Oral stable
  10. What's Chlorambucil?
    Nitrogen Mustard Alkylating Agent
  11. What's Cyclophosphamide?
    • Nitrogen Mustard Alkylating Agent
    • CYP450 Activation
  12. What SE come from Cyclophosphamide?
    • Hepatotoxicity
    • Pulmonary Fibrosis
  13. What's Busulfran? (MoA & SE)
    • Alkylsulfonate Alkylating Agent
    • Granulocytopenia
  14. What's Carmustine? (MoA & SE)
    • Nitrosourea Alkylating Agent
    • Lipid soluble -> CNS & delayed/severe BM&pulmonary fibrosis
  15. What's Cisplatin? (MoA & SE)
    • Platinum Complex Alkylating Agent
    • MoA: Covalent bonds to plasma proteins
    • SE: Nephrotoxicity
  16. What's Oxaliplatin? (MoA & SE)
    • Cisplatin analogue (AA)
    • SE: not cross resistant
  17. What's Carboplatin? (MoA & SE)
    • Cisplatin Analogue (AA)
    • Less renal toxicity
  18. What's vincristine?
    • Vinca Alkaloid
    • MoA: inhibit spindle fiber mitosis/cytoskeletal movement
    • SE: Neurotoxicity
  19. What's vinblastine?
    • Vinca Alkaloid
    • MoA: inhibit spindle fiber mitosis/cytoskeletal movement
    • SE: less neurotoxicity; granulocytopenia
  20. What's Paclitaxel?
    • Taxane
    • MoA: inhibits dissasembly of microtubules during mitosis
    • SE: cardiotoxic
  21. What's Docetaxel?
    • Paclitaxel Analogue
    • MoA: inhibits dissasembly of microtubules during mitosis
    • SE: cardiotoxic
  22. What's etoposide?
    • Epipodophyllotoxin
    • Inhibition of topoisomerase II
  23. What's teniposide?
    • Epipodophyllotoxin
    • Inhibition of topoisomerase II
  24. What's Irinotecan?
    Inhibition of Topoisomerase I
  25. What's topotecan?
    Inhibition of Topoisomerase I
  26. What's Dactinomycin? (MoA & SE)
    • Antibiotic
    • Intercalates between G:C
    • Low conc: inhibit RNA synthesis
    • High conc: inhibit RNA & DNA synthesis
    • SE: radiation sensitization
  27. What's Daunorubicin?
    • MoA: DNA intercalation & single stratnded breaks
    • SE: Cumulative cardiotoxicity (lack of superoxide dismutase to fix ROS)
  28. What's Dexrazoxane?
    Inhibits ROS to reduce cardiotoxicity from Daunorubicin/doxorubicin
  29. What's doxorubicin?
    • MoA: DNA intercalation & single stratnded breaks
    • SE: Cumulative cardiotoxicity (lack of superoxide dismutase to fix ROS)
  30. What's Bleomycin? (MoA/SE)
    • MoA: DNA/Fe binding => single/double stranded breaks
    • SE: pneumonitis with oxygen reaction
  31. What's the mechanism of resistance for Bleomycin?
    Bleomycin hydrolase -> inactivation of drug
  32. What's Methotrexate (MoA)
    • Folic Acid analogue -> competative inhibition of DHFR
    • Block dUMP-> dTMP DNA synthesis
    • Block FH4 co-factor rxns
  33. What's the mechanism of resistance for Methotrexate?
    Increased DHFR activity
  34. What's the toxicity of Methotrexate?
    • Low: Myelosuppression
    • High: Mylosuppression, renal & liver toxicity
  35. What's Leucovorin?
    Abort MTX tocity by supplying already reduced folate to cells (bypass DHFR)
  36. What's 5-Fluorouracil?
    • Metabolized to 5-FdUMP in cell
    • Suicide inhibitor of thymidylate synthase
    • Defective RNA synthesis
  37. What's the mechanism of resistance to 5-Fluorouracil?
    Overexpression of TS
  38. What's capecitabine?
    5-FU prodrug selectively activated in target cell
  39. What's azacitidine?
    • Pyrimidine Analogue
    • Inhibit DNA methyltransferase; inhibited RNA
  40. What's 6-mercaptopurine? (MoA/Resistance)
    • MoA: inhibit de novo purine synthesis -> inhibit biosynthetic reactions
    • Resistance: HPRT mutations
  41. What's 6-thioguanine?
    • MoA: inhibit de novo purine synthesis -> inhibit biosynthetic reactions
    • Resistance: HPRT mutations
  42. What's asparaginase?
    • MoA: Deprivation of asparagine (-> aspartate)
    • SE: reduction on concentration of proteins (albumin, clotting, insulin); HS, hepatotoxicity
  43. What's imatinib mesylate? (MoA/SE)
    • Competatively blocks ATP binding site of c-abl kinase
    • SE: CHF
  44. What's erlotinib/gefitinib? (MoA/SE)
    • Inhibitors of EGF receptor associated tyrosine kinase
    • SE: CHF
  45. What's Cetuximab?
    Antibody against EGF receptor
  46. What's trantuzumab?
    • Ab against VGEF
    • Anti-angiogenesis
    • SE: increased Thromboembolic events
  47. What's rituximab?
    anti CD-20 against B-cells
  48. What's gemtuzumab/ozogamin?
    Ab against CD33
  49. What's vorinostat?
    histone deacetylase inhibitor
  50. What's bortezomib?
    proteasome inhibitor
  51. What's all-trans-retinoic acid?
    Vitamin a

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