Antineoplastics

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Author:
lazzsant
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112369
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Antineoplastics
Updated:
2011-10-26 20:31:14
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Antineoplastics
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Antineoplastics
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  1. S phase drugs
    • Antimetabolites:
    • Methotrexate
    • 5-FU
    • Cytarabine
    • Mercaptopurine
    • Hydroxyurea
    • Pentstatin
  2. G2 phase drugs
    Bleomycin
  3. M phase
    • Vincristine
    • Vinblastine
    • Paclitaxel
  4. G1 phase
    • Dactinomycin
    • Tamoxifen
  5. Between S & G2
    • Etoposide
    • dactinomycin
  6. CCS
    Cell Cycle Specific - act at specific phases of cell cycle
  7. CCNS
    • Cell cycle not specific
    • Act on both dividing and non-dividing cells
  8. Doxorubicin
    Both CCS and CCNS
  9. Drugs that need to be activated before they act.
    • Cytarabine (pyrimidine antagonist(Sphase )
    • Fluorouracil(pyrimidine antagonist)(S phase)
    • Mercatpopurine (purine antagonist)(S phase)
    • Methotrexate (antimetabolite) (S phase)
    • Thioguanine (Purine antagonist) (S phase)
  10. Akylating agents
    CCNS
    • Cyclophosphamide
    • busulphan
    • chlorambucil
    • cisplatin/carboplatin
    • oxaliplatin
    • Lomustine
  11. Antitumor Antibiotics
    CCNS
    • doxorubicin
    • daunorubicin
    • dactinomycin
  12. Log-kill concept
    • Drugs or irradiation that kills a constant population of cells in a population.
    • Pulses of treatment separated by recovery intervals of fixed duration.
  13. Drugs that are cumulatively toxic
    Bone marrow
    kidney
    heart
    nervous tissue
    • Bone marrow: methotrexate
    • kidney: cisplatin
    • heart: doxorubicin
    • nervous tissue: vincristine
  14. Mechanisms of resistance
    • Change in senestivity of gene product
    • change in target receptor affinity characteristics
    • change in expression of drug transporter glycoprotein(Pgp or MDR-1)
    • modification in the prodction of drug inactivating enzymes
    • Inc DNA repair reducing damage
    • red activation of drugs
    • alteration in the P53 pathway
  15. Breast cancer
    28 day cycle
    • CMF
    • Cyclophosphamide (1-14)
    • Methotrexate (1&8)
    • 5-Fluorouracil (1 & 8)
  16. Colorectal cancer
    every 2 weeks
    • FOLFOX
    • Fluorouracil
    • leucovorin
    • oxaliplatin
  17. Ovarian Cancer
    cisplatin and paclitaxel
  18. Testicular cancer
    21 day cycle
    • PVB
    • cisplatin
    • Vinblastine
    • Bleomycin
  19. Non Hodgkins Lymphoma
    21 day cycle
    • CHOP
    • cyclophosphamide
    • doxorubicin(hydroxyldaunorubicin)
    • Vincristine (Oncovorin)
    • Prednisone
  20. Hodgkins Disease
    28 days
    2 regimens
    • MOPP
    • Mechlorethamine
    • vincristine(Oncovorine)
    • Prednisone
    • Procrbazine

    • ABVD
    • Doxorubicin (Adriamycin)
    • Bleomycin
    • Vinblastine
    • Dacarbazine
  21. Side effect of antineoplastics
    • 1) BM- pancytopenia
    • 2) Gonads - red in # of germ line cells
    • 3) GIT- red in rate of renewal
    • 4) Skin- bases of hair follicles --> alopecia
    • 5) Renal- hyperuricemia, hypercalcemia, hyperkalemia, & destruction of renal tissue
    • 6) CRTZ & VC - severe vomiting may occur
    • 7) Nerve damage
  22. Level 5 antiemetics (>90%)
    • aprepitant
    • dexamethzaone
    • ondansetron
  23. Level 3 & 4
    30-60%
    • dexamethazone
    • ondansetron
  24. Level 2 & 1
    <30%
    • dexamethazone
    • metochlopramide
    • prochlorperazine
  25. Antimetabolites
    • methotrexate
    • 5-fluorouracil
  26. Alkylating agents
    • cyclophosphamide
    • cisplatin
  27. cytotoxic antibiotics
    • doxorubicin
    • daunorubicin
    • bleomycin
  28. Natural products
    • vincristine
    • vinblastine
    • paclitaxel
  29. Hormones/ antihormones
    • tamoxifen
    • anastrozole
    • trastuzumab
    • prednisone
  30. Other enzymes
    asparaginase
  31. Bio response modifiers
    Monoclonal antibodies
    trastuzumab
  32. platinum coordinaton complexes
    cisplatin
  33. substituted ureas
    Imatinab mesylate aka (tyrosine kinase inhibitor)
  34. cytarabine
    • Antimetabolite
    • Used: AML
    • MOA: DNA strand elongation
    • A/E neurotoxic
  35. capecitabine
    • Oral prodrug -> 5-fluorouracil
    • MOA: inhibits thymidylate synthase
    • USED: paclitaxel and doxorubicin- resistant patients with colorectal or metastatic breast cancer.
  36. carmustine
    • Aklylating agent
    • A/E: toxic to the CNS
    • USED- CNS cancer
  37. etoposide
    • MOA: stabilizes the topoisomerase II- DNA complex causing double strand DNA breaks during DNA replication.
    • DOSE LIMITING LEUKOPENIA
  38. topotecan
    fulvestrant
    • MOA: Topoisomerase 1 inhibitor, preventing religation of bits helices; causes accumulation of single stranded breaks in DNA.
    • DOSE LIMITING NEUTROPENIA
    • antiestrogen for hormone-sensitive tumors.
  39. flutamide
    finasteride
    Nonsteroidal androgen antagonist - inhibits the translocation of steroid receptors to the nucleus.

    • 5-alpha reducatase inhibitor that inhibits synthesis of dihydrotestosterone.
    • Both used to treat prostate cancer.
  40. Leuprolide
    • GnRH analogues- act as a partial agonist at GnRH receptors. At constant doses inhibits the release of LH and FSH.
    • USED: treatment of prostate cancer
  41. Rituximab
    • unconjugated chimeric antiCD20 monoclonal antibody which binds to the CD20 antigen on follicular B cells in Non Hodgkins lymphoma.
    • USED: severe Crohn's disease especially with fistulation.
  42. imatinib
    mesylate
    MOA: inhibits bcr-abl tyrosin kinase found in chronic myelocytic leukemia.
  43. Methotrexate
    • Class: Antimalignant/ antimetabolite
    • USE: Solid Tumors
    • ALL
    • immunosuppressive
    • RA// SLE
    • abortifacient
    • Psoriasis
    • MOA: Inhibits DHFR -> no folate-> no DNA or RNA synthesis

    • TOXIC: Nephrotoxic
    • Myelotoxic (dose-limiting)
    • Pulmonary & liver toxicities
    • GIT (mucositis)

    • NORMAL CELL RESCUE: Leucovorin
    • BM RESCUE: G-CSF-Filgrastim

    Antidote: Folinic acid - displaces methotrexate and provides carbon for purine synthesis.
  44. 5-Fluorouracil (pyrimidine base)
    Floxuridine (pyrimidine base-sugar)
    Capecitabine (pyrimidine base sugar phosphate)
    • USE: metastatic carcinoma of breast, GIT, esophagus.(with folinic acid = more stable. VS methotrexate)
    • Carcinoma of the ovary, bladder, prostate, pancreas

    MOA: inhibits thymidylate synthase -> DNA synthesis is blocked

    • Toxicity: delayed: anorexia, N, alopecia, stomatitis, mucosal ulceration -> fulminant D-> shock and death.
    • Myelosuppression
    • Cardiotoxicity

    • Resistance: Insufficient activation of 5-FU
    • change in sensitivity of TS to the drug.

    Inactivated by dihydropyrimidine. (def -> death)
  45. Cyclophosphamide
    • Alkylating agent (CCNS)
    • Antimalignant

    • USE: CLL
    • solid tumors
    • Non hodgkins lymphoma
    • Ovarian carcinomas
    • Neuroblastoma
    • immunosuppressive to prevent graft rejection
    • SLE

    MOA: Prodrug transcription and translation interference.

    oral or IV

    • Metabolism: CYP450, CYP2B6 ->
    • active phosphoramide mustard(nephrotoxic)
    • Acrolein (hemorrhagic)

    Given with high waterload -> alkaline urine prevents reabsorption

    • TOXIC: myelosuppression
    • permanent amenorrhea & azoospermia
    • Leukemogenic
    • cardiotoxic
    • renal & bladder toxicity

    Causes inappropriate secretion of ADH

    • ANTIDOTE:
    • Mesna - conjugates acrolein
    • demeclocycline- blocks effect of ADH

    • Resisitance: Inc DNA repair
    • MDR overexpressed -> kicks out drug
  46. Nitrosoureas
    Alkylating agent

    Lipophilic & cross BBB

    USE: malignant astrocytomas & metastatic tumors of the brain

    TOXIC: CNS toxicity

    MOA: disrupt transcription via reacting with guanine bases
  47. Doxorubicin
    • Cytotoxic (anthracycline) antibiotic
    • IV : severe local vesicant action if extravasation occurs

    • USE: Hodgkins Disease
    • Non Hodgkins lymphoma
    • osteosarcoma, Ewings Sarcoma

    • MOA: prevents topoisomerase from resealing helical breaks
    • free radical formation

    • ANTIDOTE: Dimethyl sulphoxide - counteract free radical produced ulcers
    • Dexrazoxane(iron chelator-> red cardiomyopathy)

    • Toxicity: cardiomyopathy
    • Myelosuppresion
    • stomatitis
    • (with azathioprine) cholestasis

    RESISTANCE: abn transport in and inc MDR

    pegylated liposomal doxorubicin -> AIDS- related Karposi's sarcoma
  48. Vincristine
    • Vinca alkaloid
    • Antimalignant, antimitotic

    neurotoxic

    USE: Hodgkins diseases, peds leukemia

    • S/E: peripheral nerve neuropathy
    • sensory & motor paresthesias

    RESISTANCE: inc MDR gene

    • MOA: spindle poisons
    • bind to tubulin and prevent assembly of microtubules
    • M phase
  49. Vinblastine
    • Vinca Alkaloid
    • Antimalignant, antimitotic

    • USE: Hodkins
    • Testicular carcinoma

    • MOA: spindle poisons
    • bind to tubulin and prevent assembly of microtubules
    • M phase

    • S/E: Reversible myelosuppression
    • leukopenia and alopecia

    RESISANCE: inc MDR gene
  50. Paclitaxel & Docetaxel
    Natural products

    • USE: 1st & 2nd advanced ovarian cancer
    • metastatic cnacers

    Given with corticosteroid, antihistamine, and histamine H2 receptor antagonist -> prevent severe hypersenstivity reactions

    MOA: inhibit microtubule disassembly -> microtubule accumulation

    • TOXIC: Hypersensitivity
    • Neutropenia
    • Cardiac conduction defects
    • Peripheral neuropathy
  51. Tamoxifen
    Selective estrogen receptor modulator

    • USE: breast cancer tx and prophylaxis
    • infertility
    • gynecomastia
    • older women with inoperable tumors

    Long use -> inc risk of endometrial cancer

    MOA: blocks estrogen binding

    TOXIC: N/V, hot flashes, vaginal bleeding, hypercalcemia, ocular dysfunction, peripheral edema
  52. Anastrozole
    Aromatase inhibitor

    MOA: prevent estrogen synthesis
  53. Asparaginase
    L- asparagine -> aspartic acid & ammonia -> apoptosis

    • Toxicity: Hypersensitivity
    • intracranial hemorrhage
  54. Platinum coordination complex
    Cisplatin

    USE: Urinogenital, testicular, ovarian, and bladder cancer

    MOA: Diffuses and Cl replace water -> inhibition of replication and transcription

    • TOXIC: nephrotoxicity
    • electrolyte disturbances
    • otoxicity

    ANTIDOTE: amifostine -> thiol metabolites which scavange free radicals
  55. Lymphocyte immune globulin
    Aplastic Anemia
  56. Rituximab
    • Monoclonal AB
    • anti CD 20
  57. Trastuzumab (Herceptin)
    specific breast cancer HER2 amplification

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