Heme Chemo Flashcards

chemo (114 cards)

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
methotrexate mechanism
analogue of folic acid and inhibits DHFR by competitive inhibition which stops dUMP to dTMP which stops DNA synthesis
26
function of leucovorin
given after methotrexate given to rescue pathway so that higher doses can be given
27
methotrexate common uses
lymphoma, breast, HN, and lung cancer
28
methotrexate severe side effect
renal failure from precipitation in renal tubules
29
3 mechanims that give tumor cells methotrexate resistance
decreased transport, gene amplification, and mutation of DHFR
30
5 fluoroucil mechanism
inhibits thymidalte synthase by suicide mechanism which stops DNA syntehsis
31
Leucovorin has what relationshiop w/ 5 fluoroucil
used to potentiate action of 5FU by stabiliziang fdUMP to thymidilate synthase
32
f5U drug class
antimetbolite
33
mechanism of Cytarbine
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
34
Cytarbine is specific for what phase
S phase
35
Cytarbine indications
AML (7+3 regimen) and lymphoma
36
side effect of high dose Ara-C
acute cerebellar toxicity
37
cytarbine side effects (3)
marrow aplasia, GI toxicity, alopecia
38
Doxo/Dana/ Ida- Rubicine drug class and chemo class
anthracycline Abx, inhibitor of topoisomerase
39
Doxo/Dana/ Ida- Rubicine structure
tetracycline + sugar
40
Doxo/Dana/ Ida- Rubicine mechanism
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
41
Anthracyclines used to treat
hematologic malignancies, breast, lung, GI and GU cancers
42
anthracycline metabolized where
liver, so have to decrease dose in liver failure
43
anthracycline side effects
cardiac, GI, marrow= vesicants if they infiltrate they cause damage
44
incidence of cardiomyopathy is relative low below cumulative dose of ___ At a dose of ____ the incidence increases to greater than 20%
400 mg/m2 , 550
45
t/f anthracycline induced cardiomyopathy is reversible
t
46
Odansetron drug class
serotonin receptor blocking agent
47
odansetron therapeutic class
anti-emetic
48
Aprepitant drug class
serotonin receptor blocking agent
49
Aprepitant therapeutic class
anti-emetic
50
Velcade is what drug class
proteosomal inhibitor
51
velcade mechanism
inhibits degradation of proteins leading to unfolded protein stress response and apoptosis
52
velcade indications
multiple myeloma and mantle cell lymphoma
53
carfilzomib drug class
proteosomal inhibitor
54
Erythopoiesis Stimulating Agents (ESA) use
decrease need for transfusion in patients with MDS after marrow suppression
55
G-CSF
enhanced recovery of neutrophils after cytotoxic chemo and allows increased maximum tolerated dose of chemo
56
romiplostin drug calss
platelet stimulating drug
57
eltrombopag drug class
platelet stimulating drug
58
platelet stimulating drugs indication
MDS, immune thrombocytopenia, aplastic anemia
59
Aranesp and Neulasta are what
EPO and GCSF that are modified by glycosylation
60
t/f ESAs are indicated for patients receiving myelosuppressivetherappy when anticipated outcome is cure
false
61
What was the first humanized mAb approved for human use
Rutiximab
62
Rituximab mechanism
targets CD20 on pre-B and B lymphocytes and most B-cell NHLs
63
Rituximab mechanisms (3)
Fc mediated phagocytosis complement-mediated cytotoxicity apoptosis induction
64
Rituximab use
lymphoma
65
Gemtuzumab target
CD33 of immature myeloid cells
66
Gemtuzumab used to treat
AML
67
Tiuxetan target
CD20
68
Tiuxetan used to treat
NHL
69
Cetuximab target
EGFR
70
Cetuximab used to treat
colorectal and H/N
71
Bevacizumab target
VEGF
72
Bevacizumab used to treat
colorectal, lung, breast, kidney, gliobastoma
73
Imid (ie Thalidomide, Lenalidomide, Pomalidomide) drug class
immunomodulatory drugs
74
immunomodulatory mechanism
no one knows, but they are highly effective and have several mechanisms of action
75
thalidomide use
leprosy, GVHD, MM
76
lenalidomide use
MM, mantle cell NHL, MDS
77
lenalidomide side effects
fatigue, GI distress, peripheral neuropathy
78
pomalidomide use
resistant MM
79
Ipilumumab target
CTLA-4
80
Ipilumumab use
melanoma
81
Pembrolizumab target
PD-1
82
Pembrolizumab use
melanoma w or w/o BRAF inhibitor
83
Nivolumab target
PD-1
84
Nivolumab use
melanoma and Non small cell lung cancer
85
side effect of immune targeted Abs
autoimmune organ damage ie Graft vs Host which is treated w/ steroids and can be severe
86
Imatinib Meseylate primary target
bcr-abl translocation
87
Imatinib used in what kind of cancer
CML and GI stromal tumors
88
Erlotinib target
EGFR
89
Erlotinib used for what kind of cancer
NSCLC, colorectal retastatic disease
90
Trastuzumab target
Her2/neu overexpression
91
Trastuzumab used for what kind of cancer
Breast
92
Imatinib secondary targets
PDGFR, stem cell factor, and c-kit
93
Imatinib mechanism
inhibits tyrosine kinase domain of Bcr-abl oncoprotein, so steops signaling
94
2nd generation bcr-abl TKIs
noltinib and dasatinib
95
Imatinib drug class
TKI , c-kit and PDGF inhibitor
96
qualitatively what is Imatinibs oral absorption
good
97
Imatinib's side effects
cardiac toxicity
98
Trastuzumab mechanism
block Her2/Neu receptor, so stops growth factor binding
99
Trastuzumab half life
5.8 days
100
Erlotinib class
small molecule EGFR inhibitor
101
Erlotinib mechanism
inhibits kianse activity of EGFR
102
qualitatively what is Erlotinib's oral absorption
good
103
Erlotinib kinetics
36 hours
104
Erlotinib side effects
rash, diarrhea, dyspnea
105
Erlotinib used for which kinds of cancer
lung and pancreatic
106
Vemurafenib target
BRAF serine-threonine kinase oncogene inhibitor
107
Vemurafenib used for which kind of cancer
melanoma
108
vemurafenib side effects
arthralgia, skin rash, photosensitivity
109
benefits of targeting angiogenesis
resistance is infrequent, activity doesn't depend on tumor cell targeting, could prevent vascularization of tumors
110
Bevacizumab class
VEGF inhibitor so blocks angiogenic activity
111
Bevacizumab used for which cancers
colon, lung, macular degeneration, retinal disease
112
Bevacizumab side effects
bleeding, allergic rxns, wound healing, Gi perforation
113
P-glycoprotein causes resistance in which drugs
vinca alkaloids, antracyclines,taxanes, etoposide, imatinib mesylate)
114
Glutathione-S transferase induction causes resistance in which
(cisplatin, antracycline,aklylating agents)