Pharm II(Chemo Ic)

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Pharm II(Chemo Ic)
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2011-01-06 10:07:45
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Pharm II Chemo Ic
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Pharm II(Chemo Ic)
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  1. What are the 5 different Antibiotics ?
    • Major types:
    • 1. anthracyclines
    • - doxorubin
    • - daunorubicin
    • - idarubicin
    • - epirubicin
    • 2. anthracenedione
    • - mitoxantrone
    • 3. dactinomycin
    • 4. mitomycin
    • 5. bleomycin
  2. What is the Mech of action of the Anthracyclines?
    • 1. Inserts between the base pairs--> Blocks DNA and RNA synthesis
    • 2. Inhibits Topo-2
    • 3. Generates Oxygen/ Hydroxyl radicals
  3. How is resistance generated to Anthracyclins?
    The cancer cell developes MDR due to increase in Efflux.
  4. What is the Toxicity of Anthracyclins?
    What color is it?
    • 1. CARDIAC - free radical generated has affinity for cardiac muscle--> leads to Cardiomyopathy (note prevented with Dexrazoxane (Iron Chelating agent)
    • 2. bone marrow suppression
    • 3. alopecia
    • 4. severe nausea and vomiting
    • 5. secondary malignancies
    • *** The RED DEVIL !!!
  5. Anthracinediones

    Name one in the group
    When is it used?
    Color?
    Mitoxantrone

    • Similar Action and toxicity to Anthracyclins
    • Used in frail patient
    • BLUE
  6. Dactinomycin
    Mech of action?
    Uses?
    Toxicity?
    Color?
    • Insertion inbetween bases
    • Used in pediatric tumors (WILMS TUMOR)
    • Myelosupression, Vesican

    GOLD
  7. Mitomycin-C
    Mech of action?
    Mech of resistance?
    Uses?
    Toxicity?
    Color?
    • -Acts like an Alkylator (cross linking)
    • -MDR
    • -Used in Anal cancer. Used with 5-FU and radiation to preserve the anal function
    • - Associated with TTP
    • -PURPLE
  8. What is the Mech of action of Bleomycin?
    Resistance?
    Uses?
    Toxicity?
    • 1. Inserts into DNA
    • 2. Produces single and double strand breaks
    • 3. Most activity in G2

    • -MDR
    • - Several uses, Stops Pleural effusions
    • - Its creates Free radicals that are Toxic to the LUNG
    • and my cause acute anaphylactic reaction
  9. What are the 4 plant alkaloid groups? Where are they from?
    • 1. Vinca Alkaloids (periwinkle plant)
    • 2. Alkaloid Esters (Yew tree)
    • 3. Podophyllotoxin (Mandrake plant)
    • 4. Quinoline alkaloids (Happy tree)
  10. What is the Mech of action of the Vinca Alkaloids?
    • - bind to microtubular protein ( tubulin)
    • - cause depolymerization of microtubules
    • - prevents spindle formation
    • (leads to mitotic arrest)
  11. Name the Spindle Inhibitors
    • Vinca Alkaloids
    • Paclitaxel (Taxol)
    • Docetaxel (Taxotere)
  12. What is the Toxicity of Vinca Alkaloids?
    • -peripheral neuropathies- Because tubular proteins have
    • similarities to neural sheath proteins

    (note: sensory neuropathy usually reversible while motor often not).
  13. What are the uses for Vinca Alkaloids?
    • - Hodgkin’s disease
    • - NHL
    • - lung cancer
    • - gliomas
    • - breast cancer (via analogue)
  14. What is the Mech of action of the Taxanes?
    what is it used for?
    • - binds to tubulin
    • - enhances tubulin polymerization
    • - prevents spindle disassociation causing
    • mitotic arrest
    • ______________________________
    • Ovarian *, Breast and lung cancer
  15. What are some Toxicities of the Taxanes?
    • - bone marrow
    • - allergies
    • - myalgias and arthralgias
    • - neurologic
    • - skin (particularly nails)
  16. What is the Mech of action of the podophyllotoxins?
    What is it used for?
    - inhibits DNA topoisomerase-2 --> inhibition of DNA / RNA synthesis

    • Uses:
    • - testicular cancer
    • - lung cancer (especially small cell)
    • - NHL
    • - minor activity in a variety of cancers
  17. What is the Mechanism of action of the Camptothecins?
    What are the Two Clinically active agents?
    • Inhibit topoisomerase 1--> leads to arrest of DNA
    • replication --> cell death

    • - Irinotecan -- used for Colon cancer. Can cause excessive diarrhea (treat with Atropine)
    • -topotecan - small cell lung cancer and
    • ovarian cancer. Can cause BM supression
  18. What are the MAJOR toxicities of the Antibiotics (note: all make free radicals)
    - anthracyclines
    - anthracenediones
    - dactinomycin
    - mitomycin
    - bleomycin
    • - Cardiac
    • - Cardiac
    • - Myelosuppression
    • - TTP (renal, cns and micro angiopathic hemolitic anemia)
    • - Pulmonary
  19. What are the Major Toxicities of the Plant alkaloids?
    -Vincas
    -Taxanes
    -Podophyllotoxins
    -Camptothecins
    • -Neurologic
    • -Neurologic
    • -Myelosuppression
    • -Gastrointestinal
  20. What Antibiotic is the only cell cycle specific one?
    Bleomycin (G2)
  21. Name the Vinca Alkaloids
    • - vincristine
    • - vinblastine
    • - vindesine
    • - vinorelbine
  22. Name the Alkaloid Esters (Taxanes)
    • - paclitaxel
    • - docetaxel
  23. Name the Podophyllotoxins
    • - etoposide
    • - teniposide
  24. Name the Quinoline alkaloids (Camptothecins)
    • - irinotecan
    • - topotecan
  25. What are the General properties of the Miscellaneous agents?

    Name Them and their specific Toxicities.
    • 1. Heavy metals
    • 2. Act as alkylators
    • 3. The major toxicity is neurologic (permanent)
    • __________________________________
    • Cisplatinum--nephrotoxicity
    • Carboplatinum --myelosuppression
    • Oxaliplatinum--cold intolerance
  26. What are the uses for the Miscellaneous agents?
    • •Cisplatinum-- Lung, Ovarian cancers (most germ cells).
    • •Carboplatinum-- Breast, Ovarian, Lung
    • •Oxaliplatinum-- Colon
  27. How do you pervent Nephrotoxicity, Neurotoxicity, and cold induced neuropathy of the Platinum Compounds?
    • Nephro--
    • -parenteral and oral hydration
    • -replace both potassium and magnesium
    • -use of amifostine (scavanges for cisplatin)

    • Neuro--
    • -calcium and magnesium infusions
    • Cold--
    • -avoidance of cold air and drink

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