IC Part II > Antineoplastics > Flashcards

Antineoplastics Flashcards

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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
- causes more myelosuppression than cisplatin, less nausea and renal - solid tumor treatment
carboplatin
26
- less renal than cisplatin, but neurotoxic - advanced colorectal cancer - solid tumors
oxaliplatin
27
- alkylating agent, also causes strand cission - bioactivated, blocks DNA and RNA synthesis - standard toxicities: n/v/bone marrow suppression - strongly leukemogenic and teratogenic
procarbazine
28
- IV, converted to active methylating metabolite MTIC by CYP enzyme - treat malignant melanoma, hodgkin's
dacarbazine
29
- oral prodrug - crosses BBB - anaplastic astrocytoma, glioblastoma multiforme
temozolomide
30
- analogs of normal components that target the cells - enters normal path then blocks - folate analogs, purine and pyrimidine analogs
antimetabolites
31
- DHFR inhibitor, depletion of tetrhydrofolate shuts down biosynthetic paths - greater accumulation in tumor cells - blocks produciton of bases required for DNA synthesis
methotrexate
32
- oral, IV, intrathecal - excreted in urine - high dose followed by rescue with folinic acid - anti folate effects - resistance: aplified DHFR, decreased accumulation of polyglutamates
methotrexate
33
- 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
purine analogs
34
- active metabolite, inactivates thymidylate synthase - folinic acid required for inactivation of thymidylate synthase - treat many carcinomas - bone marrow toxicity, GI
5-flurouracil
35
- cytosine analog, chain terminator - CCS: active during S phase - treat AML, ALL, CLL, high grade lymphomas
cytarabine
36
- inhibits tubulin polymerization, disrupts mitotic spindles - metaphase arrest - IV admin - biliary excretion
vinca alkaloids (vincristine, vinblastine)
37
-vinca alkaloid that causes alopecia, bone marrow depression
vinblastine
38
-vinca alkaloid that causes peripheral neuropathy
vincristine
39
- 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
paclitaxel, docetaxel
40
- topoisomerase II inhibitors, double strand breaks, DNa degradation - induces apoptosis - oral and IV - bone marrow suppression, alopecia
etoposide, teniposide
41
etoposide and teniposide arrest cell in _____ stage
S-G2
42
- topoisomerase I inhibitors (ss DNA breaks) - myelosuppressive - dose limiting toxicity is severe diarrhea
topotecan, irinotecan
43
______ in combo with 5-FU and leucovorin is first line for metastatic colorectal cancer
irinotecan
44
prodrug metabolized to SN-38, metabolized by UGT1A1 so do genetic testing
irinotecan
45
- block access to/function of DNA or RNA - all IV - unique toxicities - most produced by microbes
antitumor antibiotics
46
- intercalate into DNA - blocks topoisomerase II, cause strand breaks - generate free radicals - IV, hepatic clearance
anthracyclines (dox/daunorubicin)
47
- bone marrow suppression, GI distress, severe alopecia - signature adverse is cardiotoxicity (arryhtmias, cardiomyopathy, CHF) - free radicals minimized by dexrazoxance (iron chelator)
anthracyclines (doxo/daunorubicin)
48
- mix of glycopeptides - binds DNA, generates free radicals --> strand breaks, active in G2 - hypersensitivity, cutaneous rxns - pulm toxicity, fibrosis
bleomycin
49
- effective against solid tumors - activation favored by hypoxia, alkylates DNA - given IV or by bladder instillation - very toxic: severe bone marrow suppression, GI, renal
mitomycin C (antitumor antibiotic)
50
- intercalates, blocks RNA and DNA synthesis | - radiation recall: inflammation at sites of prior radiaiton
dactinomycin (actinomycin D)
51
- depletes serum asparagine needed by some tumors - parenteral - hypersensitivity - use in ALL
asparaginase
52
- inhibits ribonucleotide reductase - oral therapy for leukemias, some head and neck - mucositis, rash, bone marrow suppression
hydroxyurea
53
- monoclonal antibody, blocks CD20 B cell antigen - IV, half life 22 days - for B cell lymphomas, CLL, non hodgkins - hypogammaglobulinemia, autoimmune disorders
rituximab
54
- suppress proliferation of immune cells (leukocytes, lymphocytes) - oral - delayed: fluid retention, immunosuppression, diabetes
prednisone, hydrocortisone
55
- block conversion of androgens to estrogens | - specific for estrogen production
selective aromatase inhibitors
56
- azole, similar to antifungals - more effective against peripheral aromatase - for ER+ primary and metastatic breast cancer
anastrazole, letrozole
57
- steroidal irreversible aromatase inhibitor - no cross resistance w/ azoles - fatigue, hot flashes
exemestane
58
- competing ligands for estrogen receptor | - more effective in post menopausal women
SERMs
59
- ER antagonist in breast, ER agonist in endometrium - converted by CYP2D6 - chemopreventive for breast cancer - ER+ primary and metastatic
tamoxifen, toremifine
60
- ER antagonist in breast, ER agonist in bone - chemoprevention for breast cancer, treatment and prevention of osteoporosis - hot flashes, vaginal bleeding
raloxifene
61
- use with leuprolide and/or radiation for prostate cancer | - hot flashes, transient hepatic effects
flutamide, bicalutamide
62
- 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
interferon- alpha
63
- monoclonal antibody against Her2neu oncogene (epidermal growth factor) - receptor amplified in 25% of breast cancers - IV - hypersensitivity, cardiomyopathy
trastuzamab (herceptin)
64
- 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
imatinib (gleevec)
65
- newer receptor tyrosine kinase inhibitors, broad spectrum | - use in imatinib resistance
dastinib, nilotinib
66
- 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
ibrutinib
67
- 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
idelalisib
68
- inhibits 26S proteasome, disrupts signal cascades, apoptosis - multiple myeloma, mantle cell lymphoma - causes thrombocytopenia, fatigue, peripheral neuropathy - hypotension upon infusion
bortezimib
69
- 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
all trans retinoic acid
70
- inhibits thioredoxin reductase, enhancing oxidative stress - modification and degradation of APL fusion protein - cytotoxic, promotes differentiation
arsenic trioxide (As2O3)
71
- thalidomide derivative - CLL, multiple myeloma - lacks sedative effects and teratogenic of thalidomide - inhibits rituximab
lenalidomide
IC Part II
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