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IC Part II > Antineoplastics > Flashcards

Antineoplastics Flashcards

1
Q
  • antimetabolites
  • topoisomerase II inhibitors
  • microtubule poisons
  • bleomycin
  • all drugs are cell cycle ______
A

specific

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2
Q
  • alkylating agents
  • antitumor antibiotics
  • topoisomerase I inhibitors
  • all drugs are cell cycle _______
A

nonspecific

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3
Q

bleomycin causes?

A

pulmonary fibrosis

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4
Q

cyclophosphamide adverse effect

A

cystitis

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5
Q

anthracyclines (daunorubicin, doxorubicin) adverse effects

A

cardiotoxicity

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6
Q

cisplatin adverse effects

A

nephrotoxicity

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7
Q

cepaceitabine, pemetrexed effects

A

hand and foot syndrome

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8
Q

vincristine, docetaxel, paclitaxel adverse effects

A

neurotoxicity

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9
Q

irinotecan adverse effects

A

intestinal toxicity (diarrhea)

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10
Q
  • tumor cells initially not sensitive to a given drug

- test by in vitro sensitivity by cell conolony assays or genotyping

A

primary resistance

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11
Q
  • tumor cells develop resistance during drug therapy

- changes in permeability, amplification/alteration of targets, enhanced repair

A

secondary resistance

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12
Q
  • MDR protein

- can export multiple classes of anti cancer drugs (antimetabolites, antibiotics, alkaloids)

A

p-glycoprotein

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13
Q
  • impermeable to drug or pump drug out
  • alternate targets for drug (glutathione)
  • no apoptosis
  • mechanism of restistance to what class?
A

alkylating agents

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14
Q
  • bifunctional nitrogen mustard
  • vesicant, caustic to skin and mucus membranes
  • IV only (sQ causes necrosis), often in arterial supply to tumor
  • half life minutes
  • n/v, decreased blood counts w/ recovery in 3-6 wks
  • use for Hodgkin’s (part of MOPP)
A

mechlorethamine

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15
Q
  • oral or IV
  • bioactivated by host metabolism (liver)
  • adverse: n/v, bone marrow depression, alopecia
  • sterile hemorrhagic cystitis
A

cyclophosphamide

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16
Q

_____ is the major cause of cyclophosphamide cystitis, protect by forced hydration and Mesna

A

acrolein

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17
Q
  • activated non enzymatically
  • lipid soluble, cross BBB
  • Lymphomas and brain tumors
  • IV or direct brain implant
  • GI, myelosuppression
A

nitrosoureas (carmustine, lomustine, beadamustine)

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18
Q
  • sugar molecule attached to nitrosourea structure

- malignant pancreatic insulinoma, malignant carcinoid

A

streptozocin

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19
Q

alkylating agent used for multiple myeloma and myeloablative therapy?

A

melphalan

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20
Q

alkylating agent used for CLL?

A

chlorambucil

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21
Q

alkylating agent used for CML? seldom used after imatinib, sulfur mustard not nitrogen

A

busulfan

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22
Q
  • superficial papillary bladder cancer
  • palliative for adenocarcinoma of breast or ovary
  • controlling intracavity effusions caused by metastatic tumors
A

thiotepa

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23
Q

metastatic islet cell carcinoma of pancreas

A

streptozocin

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24
Q
  • bifunctional platinating agent, cross links DNA
  • blocks DNA synthesis
  • IV, cleared in urine
  • non toxic to bone marrow
  • n/v (use ondansetron)
  • renal toxicity, dose limiting
A

cisplatin

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25
Q
  • causes more myelosuppression than cisplatin, less nausea and renal
  • solid tumor treatment
A

carboplatin

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26
Q
  • less renal than cisplatin, but neurotoxic
  • advanced colorectal cancer
  • solid tumors
A

oxaliplatin

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27
Q
  • alkylating agent, also causes strand cission
  • bioactivated, blocks DNA and RNA synthesis
  • standard toxicities: n/v/bone marrow suppression
  • strongly leukemogenic and teratogenic
A

procarbazine

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28
Q
  • IV, converted to active methylating metabolite MTIC by CYP enzyme
  • treat malignant melanoma, hodgkin’s
A

dacarbazine

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29
Q
  • oral prodrug
  • crosses BBB
  • anaplastic astrocytoma, glioblastoma multiforme
A

temozolomide

30
Q
  • analogs of normal components that target the cells
  • enters normal path then blocks
  • folate analogs, purine and pyrimidine analogs
A

antimetabolites

31
Q
  • DHFR inhibitor, depletion of tetrhydrofolate shuts down biosynthetic paths
  • greater accumulation in tumor cells
  • blocks produciton of bases required for DNA synthesis
A

methotrexate

32
Q
  • oral, IV, intrathecal
  • excreted in urine
  • high dose followed by rescue with folinic acid
  • anti folate effects
  • resistance: aplified DHFR, decreased accumulation of polyglutamates
A

methotrexate

33
Q
  • oral, well toelrated, bone marrow depression only at high doses
  • bioactivated by salvage path (HGPRT)
  • blocks DNA and RNA synthesis, inhibits AMP and GMP, or incorporated into DNA altering function
  • used for leukemias and lymphomas
  • resistance from decrease in hgprt activity, or increase in alk phos
A

purine analogs

34
Q
  • active metabolite, inactivates thymidylate synthase
  • folinic acid required for inactivation of thymidylate synthase
  • treat many carcinomas
  • bone marrow toxicity, GI
A

5-flurouracil

35
Q
  • cytosine analog, chain terminator
  • CCS: active during S phase
  • treat AML, ALL, CLL, high grade lymphomas
A

cytarabine

36
Q
  • inhibits tubulin polymerization, disrupts mitotic spindles
  • metaphase arrest
  • IV admin
  • biliary excretion
A

vinca alkaloids (vincristine, vinblastine)

37
Q

-vinca alkaloid that causes alopecia, bone marrow depression

A

vinblastine

38
Q

-vinca alkaloid that causes peripheral neuropathy

A

vincristine

39
Q
  • affects microtubules by stabilization
  • blocks progression through M phase
  • effective in solid tumors
  • IV in cremaphor –> hypersensitivity
  • acute hypersensitivity, nausea
  • delayed bone marrow suppression, neuropathy
A

paclitaxel, docetaxel

40
Q
  • topoisomerase II inhibitors, double strand breaks, DNa degradation
  • induces apoptosis
  • oral and IV
  • bone marrow suppression, alopecia
A

etoposide, teniposide

41
Q

etoposide and teniposide arrest cell in _____ stage

A

S-G2

42
Q
  • topoisomerase I inhibitors (ss DNA breaks)
  • myelosuppressive
  • dose limiting toxicity is severe diarrhea
A

topotecan, irinotecan

43
Q

______ in combo with 5-FU and leucovorin is first line for metastatic colorectal cancer

A

irinotecan

44
Q

prodrug metabolized to SN-38, metabolized by UGT1A1 so do genetic testing

A

irinotecan

45
Q
  • block access to/function of DNA or RNA
  • all IV
  • unique toxicities
  • most produced by microbes
A

antitumor antibiotics

46
Q
  • intercalate into DNA
  • blocks topoisomerase II, cause strand breaks
  • generate free radicals
  • IV, hepatic clearance
A

anthracyclines (dox/daunorubicin)

47
Q
  • bone marrow suppression, GI distress, severe alopecia
  • signature adverse is cardiotoxicity (arryhtmias, cardiomyopathy, CHF)
  • free radicals minimized by dexrazoxance (iron chelator)
A

anthracyclines (doxo/daunorubicin)

48
Q
  • mix of glycopeptides
  • binds DNA, generates free radicals –> strand breaks, active in G2
  • hypersensitivity, cutaneous rxns
  • pulm toxicity, fibrosis
A

bleomycin

49
Q
  • effective against solid tumors
  • activation favored by hypoxia, alkylates DNA
  • given IV or by bladder instillation
  • very toxic: severe bone marrow suppression, GI, renal
A

mitomycin C (antitumor antibiotic)

50
Q
  • intercalates, blocks RNA and DNA synthesis

- radiation recall: inflammation at sites of prior radiaiton

A

dactinomycin (actinomycin D)

51
Q
  • depletes serum asparagine needed by some tumors
  • parenteral
  • hypersensitivity
  • use in ALL
A

asparaginase

52
Q
  • inhibits ribonucleotide reductase
  • oral therapy for leukemias, some head and neck
  • mucositis, rash, bone marrow suppression
A

hydroxyurea

53
Q
  • monoclonal antibody, blocks CD20 B cell antigen
  • IV, half life 22 days
  • for B cell lymphomas, CLL, non hodgkins
  • hypogammaglobulinemia, autoimmune disorders
A

rituximab

54
Q
  • suppress proliferation of immune cells (leukocytes, lymphocytes)
  • oral
  • delayed: fluid retention, immunosuppression, diabetes
A

prednisone, hydrocortisone

55
Q
  • block conversion of androgens to estrogens

- specific for estrogen production

A

selective aromatase inhibitors

56
Q
  • azole, similar to antifungals
  • more effective against peripheral aromatase
  • for ER+ primary and metastatic breast cancer
A

anastrazole, letrozole

57
Q
  • steroidal irreversible aromatase inhibitor
  • no cross resistance w/ azoles
  • fatigue, hot flashes
A

exemestane

58
Q
  • competing ligands for estrogen receptor

- more effective in post menopausal women

A

SERMs

59
Q
  • ER antagonist in breast, ER agonist in endometrium
  • converted by CYP2D6
  • chemopreventive for breast cancer
  • ER+ primary and metastatic
A

tamoxifen, toremifine

60
Q
  • ER antagonist in breast, ER agonist in bone
  • chemoprevention for breast cancer, treatment and prevention of osteoporosis
  • hot flashes, vaginal bleeding
A

raloxifene

61
Q
  • use with leuprolide and/or radiation for prostate cancer

- hot flashes, transient hepatic effects

A

flutamide, bicalutamide

62
Q
  • cytokine produced by WBCs
  • parenteral
  • alters gene expression, antiviral and immunomodulatory
  • used against hematologic malignancies, metastatic melanoma, renal cell carcinoma
  • fever and chills, anorexia, weakness
A

interferon- alpha

63
Q
  • monoclonal antibody against Her2neu oncogene (epidermal growth factor)
  • receptor amplified in 25% of breast cancers
  • IV
  • hypersensitivity, cardiomyopathy
A

trastuzamab (herceptin)

64
Q
  • inhibits Bcr-Abl and c-kit (GI stromal tumors) tyrosine kinases
  • used in CML
  • any hematologic malignancy with Philadelphia chromosome
  • myelosuppressive
  • edema, fluid retention, hepatotoxic
A

imatinib (gleevec)

65
Q
  • newer receptor tyrosine kinase inhibitors, broad spectrum

- use in imatinib resistance

A

dastinib, nilotinib

66
Q
  • inhibits bruton’s tyrosine kinase, essential for B cell receptor signaling
  • oral
  • metabolized by CYP3A4
  • for mantle cell lymphoma, refractory CLL
  • adverse: GI, thrombocytopenia, neutropenia, infections, fatigue
A

ibrutinib

67
Q
  • PI3K inhibitor
  • metabolized by aldehyde oxidase and CYP3A4 (Strong inhibitor)
  • relapsed CLL and SLL, relapsed follicular B cell lymphoma
  • hepatotox, diarrhea, colitis, pneumonitis, intestinal perf
A

idelalisib

68
Q
  • inhibits 26S proteasome, disrupts signal cascades, apoptosis
  • multiple myeloma, mantle cell lymphoma
  • causes thrombocytopenia, fatigue, peripheral neuropathy
  • hypotension upon infusion
A

bortezimib

69
Q
  • monotherapy or w/ anthracycline or arsenic for APL
  • binds to RAR-alpha receptor, promotes differentiation
  • promotes degradation of PML RAR-alpha fusion protein
  • resistance through enhanced clearance (CyP25A1) or loss of expresion of fusion gene
A

all trans retinoic acid

70
Q
  • inhibits thioredoxin reductase, enhancing oxidative stress
  • modification and degradation of APL fusion protein
  • cytotoxic, promotes differentiation
A

arsenic trioxide (As2O3)

71
Q
  • thalidomide derivative
  • CLL, multiple myeloma
  • lacks sedative effects and teratogenic of thalidomide
  • inhibits rituximab
A

lenalidomide

IC Part II (29 decks)

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