Heme Chemo Flashcards

chemo

1
Q

Alkylating Agents Mechanism

A

alkylate DNA by interacting with nucleophilic groups which disrupts DNA and leads to apoptosis

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2
Q

Alkylating agents are phase specific or non specific

A

non- specific, but cells ahe to be cycling

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3
Q

what does the response curve look like for alkylating agents

A

linear dose response

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4
Q

alkylating agents side effects

A

nausea, marrow suppression, mutagenesis, secondary carcinogenesis

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5
Q

Mechlorethamine aka

A

nitrogen mustard

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6
Q

Mechlorethamine drug class/ mechanism

A

alkylating agent –interacts w/ N7 group of guanine which leads to crosslinking and depurination = bifunctional

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7
Q

how is Mechlorethamine metabolized

A

degraded by non-enyatic hydrolysis so does not require dose adjustment in renal/hepatic failure

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8
Q

What is dose limiting side effect of Mechlorethamine

A

myelo suppression

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9
Q

melphalan is what drug class and derivative of what drug

A

alkylating agent –mechlorethamine

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10
Q

ifosphamide is what drug class and derivative of what drug

A

alkylating agent –mechlorethamine

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11
Q

chlorambucil is what drug class and derivative of what drug

A

alkylating agent –mechlorethamine

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12
Q

Cyclophosphamide is a derivative of

A

mechlorethamine

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13
Q

what is the most widely used alkylating agent

A

cyclophosphamide

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14
Q

cyclophosphamide route

A

IV or oral

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15
Q

cyclophosphamide
(is parent drug active0

A

no has to be activated by p450 system

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16
Q

how is cyclophosphamide
elimiated

A

liver and kidney

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17
Q

cyclophosphamide
unique side effect

A

hemorrhagic cystitis from acrolein metabolite which is treated with MESNA ( 2-mercaptoethane sulphonate)

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18
Q

cyclophosphamide drug class

A

alkylating agent

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19
Q

Cisplatin drug class

A

alkylating agent

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20
Q

cisplatin widely used in which cancers

A

Head/neck, lung, breast, and ovarian

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21
Q

cisplatin side effects

A

renal insufficiency and neuropathy

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22
Q

most antimetabolites are specific for cells in which phase

A

S phase

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23
Q

antimetabolites are most effective when administered how

A

continuous infusion or hyperfractionated IV bolus

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24
Q

Methotrexate drug class

A

antimetabolite

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25
Q

methotrexate mechanism

A

analogue of folic acid and inhibits DHFR by competitive inhibition which stops dUMP to dTMP which stops DNA synthesis

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26
Q

function of leucovorin

A

given after methotrexate given to rescue pathway so that higher doses can be given

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27
Q

methotrexate common uses

A

lymphoma, breast, HN, and lung cancer

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28
Q

methotrexate severe side effect

A

renal failure from precipitation in renal tubules

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29
Q

3 mechanims that give tumor cells methotrexate resistance

A

decreased transport, gene amplification, and mutation of DHFR

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30
Q

5 fluoroucil mechanism

A

inhibits thymidalte synthase by suicide mechanism which stops DNA syntehsis

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31
Q

Leucovorin has what relationshiop w/ 5 fluoroucil

A

used to potentiate action of 5FU by stabiliziang fdUMP to thymidilate synthase

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32
Q

f5U drug class

A

antimetbolite

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33
Q

mechanism of Cytarbine

A

cytidine analogue that inhibits DNA polymerase and inhibits DNA replication. Also if it is incorporated into DNA it slows chain elongation and inhibits DNA ligation

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34
Q

Cytarbine is specific for what phase

A

S phase

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35
Q

Cytarbine indications

A

AML (7+3 regimen) and lymphoma

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36
Q

side effect of high dose Ara-C

A

acute cerebellar toxicity

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37
Q

cytarbine side effects (3)

A

marrow aplasia, GI toxicity, alopecia

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38
Q

Doxo/Dana/ Ida- Rubicine drug class and chemo class

A

anthracycline Abx, inhibitor of topoisomerase

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39
Q

Doxo/Dana/ Ida- Rubicine structure

A

tetracycline + sugar

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40
Q

Doxo/Dana/ Ida- Rubicine mechanism

A

intercalates into DNA and inhibits DNA replication and mRA synthesis and also inhibits Topo II which inhibits DNA which leads to DNA fragmentation and apoptosis

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41
Q

Anthracyclines used to treat

A

hematologic malignancies, breast, lung, GI and GU cancers

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42
Q

anthracycline metabolized where

A

liver, so have to decrease dose in liver failure

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43
Q

anthracycline side effects

A

cardiac, GI, marrow= vesicants if they infiltrate they cause damage

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44
Q

incidence of cardiomyopathy is relative low below cumulative dose of ___ At a dose of ____ the incidence increases to greater than 20%

A

400 mg/m2 , 550

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45
Q

t/f anthracycline induced cardiomyopathy is reversible

A

t

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46
Q

Odansetron drug class

A

serotonin receptor blocking agent

47
Q

odansetron therapeutic class

A

anti-emetic

48
Q

Aprepitant drug class

A

serotonin receptor blocking agent

49
Q

Aprepitant therapeutic class

A

anti-emetic

50
Q

Velcade is what drug class

A

proteosomal inhibitor

51
Q

velcade mechanism

A

inhibits degradation of proteins leading to unfolded protein stress response and apoptosis

52
Q

velcade indications

A

multiple myeloma and mantle cell lymphoma

53
Q

carfilzomib drug class

A

proteosomal inhibitor

54
Q

Erythopoiesis Stimulating Agents (ESA) use

A

decrease need for transfusion in patients with MDS after marrow suppression

55
Q

G-CSF

A

enhanced recovery of neutrophils after cytotoxic chemo and allows increased maximum tolerated dose of chemo

56
Q

romiplostin drug calss

A

platelet stimulating drug

57
Q

eltrombopag drug class

A

platelet stimulating drug

58
Q

platelet stimulating drugs indication

A

MDS, immune thrombocytopenia, aplastic anemia

59
Q

Aranesp and Neulasta are what

A

EPO and GCSF that are modified by glycosylation

60
Q

t/f ESAs are indicated for patients receiving myelosuppressivetherappy when anticipated outcome is cure

A

false

61
Q

What was the first humanized mAb approved for human use

A

Rutiximab

62
Q

Rituximab mechanism

A

targets CD20 on pre-B and B lymphocytes and most B-cell NHLs

63
Q

Rituximab mechanisms (3)

A

Fc mediated phagocytosis
complement-mediated cytotoxicity
apoptosis induction

64
Q

Rituximab use

A

lymphoma

65
Q

Gemtuzumab target

A

CD33 of immature myeloid cells

66
Q

Gemtuzumab used to treat

A

AML

67
Q

Tiuxetan target

A

CD20

68
Q

Tiuxetan used to treat

A

NHL

69
Q

Cetuximab target

A

EGFR

70
Q

Cetuximab used to treat

A

colorectal and H/N

71
Q

Bevacizumab target

A

VEGF

72
Q

Bevacizumab used to treat

A

colorectal, lung, breast, kidney, gliobastoma

73
Q

Imid (ie Thalidomide, Lenalidomide, Pomalidomide) drug class

A

immunomodulatory drugs

74
Q

immunomodulatory mechanism

A

no one knows, but they are highly effective and have several mechanisms of action

75
Q

thalidomide use

A

leprosy, GVHD, MM

76
Q

lenalidomide use

A

MM, mantle cell NHL, MDS

77
Q

lenalidomide side effects

A

fatigue, GI distress, peripheral neuropathy

78
Q

pomalidomide use

A

resistant MM

79
Q

Ipilumumab target

A

CTLA-4

80
Q

Ipilumumab use

A

melanoma

81
Q

Pembrolizumab target

A

PD-1

82
Q

Pembrolizumab use

A

melanoma w or w/o BRAF inhibitor

83
Q

Nivolumab target

A

PD-1

84
Q

Nivolumab use

A

melanoma and Non small cell lung cancer

85
Q

side effect of immune targeted Abs

A

autoimmune organ damage ie Graft vs Host which is treated w/ steroids and can be severe

86
Q

Imatinib Meseylate primary target

A

bcr-abl translocation

87
Q

Imatinib used in what kind of cancer

A

CML and GI stromal tumors

88
Q

Erlotinib target

A

EGFR

89
Q

Erlotinib used for what kind of cancer

A

NSCLC, colorectal retastatic disease

90
Q

Trastuzumab target

A

Her2/neu overexpression

91
Q

Trastuzumab used for what kind of cancer

A

Breast

92
Q

Imatinib secondary targets

A

PDGFR, stem cell factor, and c-kit

93
Q

Imatinib mechanism

A

inhibits tyrosine kinase domain of Bcr-abl oncoprotein, so steops signaling

94
Q

2nd generation bcr-abl TKIs

A

noltinib and dasatinib

95
Q

Imatinib drug class

A

TKI , c-kit and PDGF inhibitor

96
Q

qualitatively what is Imatinibs oral absorption

A

good

97
Q

Imatinib’s side effects

A

cardiac toxicity

98
Q

Trastuzumab mechanism

A

block Her2/Neu receptor, so stops growth factor binding

99
Q

Trastuzumab half life

A

5.8 days

100
Q

Erlotinib class

A

small molecule EGFR inhibitor

101
Q

Erlotinib mechanism

A

inhibits kianse activity of EGFR

102
Q

qualitatively what is Erlotinib’s oral absorption

A

good

103
Q

Erlotinib kinetics

A

36 hours

104
Q

Erlotinib side effects

A

rash, diarrhea, dyspnea

105
Q

Erlotinib used for which kinds of cancer

A

lung and pancreatic

106
Q

Vemurafenib target

A

BRAF serine-threonine kinase oncogene inhibitor

107
Q

Vemurafenib used for which kind of cancer

A

melanoma

108
Q

vemurafenib side effects

A

arthralgia, skin rash, photosensitivity

109
Q

benefits of targeting angiogenesis

A

resistance is infrequent, activity doesn’t depend on tumor cell targeting, could prevent vascularization of tumors

110
Q

Bevacizumab class

A

VEGF inhibitor so blocks angiogenic activity

111
Q

Bevacizumab used for which cancers

A

colon, lung, macular degeneration, retinal disease

112
Q

Bevacizumab side effects

A

bleeding, allergic rxns, wound healing, Gi perforation

113
Q

P-glycoprotein causes resistance in which drugs

A

vinca alkaloids, antracyclines,taxanes, etoposide, imatinib mesylate)

114
Q

Glutathione-S transferase induction causes resistance in which

A

(cisplatin, antracycline,aklylating agents)