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PT3 Oncology > Pharmacology > Flashcards

Pharmacology Flashcards

(115 cards)

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1
Q

classes that are alkylating agents

A
  • nitrogen mustards
  • nitrosoureas
  • platinum compounds
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2
Q

alkylating agents general MoA

A

-electrophilic molecules that covalently modify nucleophilic molecules in cell, particularly DNA

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3
Q

monofunctional alkylating agents cause

A

single strand DNA breaks

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4
Q

bifunctional alkylating agents cause

A

inhibition of DNA replication and transcription by crosslinking DNA

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5
Q

nitrogen mustards specific MoA

A
  • get activated into a aziridine ring

- nucleophilic attack of unstable aziridine ring on DNA

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6
Q

nitrogen mustard drugs

A
  • mechlorethamine
  • cyclophosphamide (used more)
  • procarbazine (atypical)
  • dacarbazine (atypical)
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7
Q

mechlorethamine recovery rate

A

delayed, very slow

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8
Q

cyclophosphamide recovery rate

A

rapid

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9
Q

nitrogen mustards dose limiting toxicity

A

myelosuppression

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10
Q

nitrogen mustards common resistance pathway

A

increase in DNA repair

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11
Q

toxic metabolite of cyclophosphamide

A

acrolein

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12
Q

acrolein toxicity

A
  • nephrotoxic and urotoxic

- causes severe hemorrhagic cystitis

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13
Q

drug to reduce acrolein toxicity

A

MESNA

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14
Q

procarbazine main action

A

methylator

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15
Q

dacarbazine is given with what

A

temozolomide

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16
Q

dacarbazine and temozolomide are metabolized to what

A

5-imidizole-4 caroxamide, the active alkylating species

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17
Q

platinum compounds

A
  • cisplatin
  • carboplatin
  • oxaliplatin
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18
Q

cisplatin feature

A

non-cell cycle specific

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19
Q

carboplatin feature

A

less toxic than cisplatin, but less active

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20
Q

oxaliplatin feature

A

little cross resistance with other Pt compounds, less toxic too

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21
Q

notable ADME of platinum compounds

A

Cl diuresis reduces toxicity so the drug doesn’t get activated until it is in the cell

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22
Q

cisplatin DLT

A

nephrotoxicity
neurotoxicity
ototoxicity

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23
Q

carboplatin DLT

A

myelosuppression - thrombocytopenia

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24
Q

oxaliplatin DLT

A

peripheral neuropathy

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25
bifunctional alkylating agents
nitrogen mustards | platinums
26
monofuctional alkylating aget
nitrosoureas
27
general metabolite/antimetabolite MoA
interfere with DNA synthesis or synthesis of precursors
28
the classical cell cycle specific drugs
metabolites/antimetabolites
29
folate antimetabolite drugs
methotrexate | amethopterin
30
folate antimetabolite MoA
inhibit dihydrofolate reductase and dTMP synthesis
31
unique ADME of methotrexate
polyglutamation concentrates drug in the cell
32
folate antimetabolite toxicity
bone marrow GI renal teratogen
33
folate antimetabolite resistance
increased/altered DHFR | decreased uptake
34
nucleotide analog (antimetabolite) drug
5-FU
35
5-FU MoA
irreversible inhibition of thymidylate synthase and incorporation into DNA/RNA
36
phsases of cell cycle 5-FU can kill cells
G1 and S
37
5-FU DLT
bone marrow suppression
38
5-FU resistance
increased/altered thymidylate synthase
39
pharmacogenetic issue with 5-FU
dihydropyrimidine dehydrogenase deficiency | -could lead to extreme toxicity
40
leucovorin use
- rescues cells exposed to folate antagonists | - given with high dose methotrexate
41
antimetabolite resistance
most are prodrugs so alterations in metabolic pathway alterations
42
antibiotic anticancer drugs
doxorubicin | bleomycin
43
doxorubicin MoA
DNA intercalator and topoisomerase-II interference
44
bleomycin MoA
DNA & metal binding via free radical damage in *G2 stage*
45
doxorubicin DLT
cardiotoxicity | myelosuppresison
46
bleomycin DLT
lung and skin fibrosis
47
etoposide MoA
stabilized topo-II DNA complex to cause double strand breaks | prevents religation
48
etoposide DLT
bone marrow
49
etoposide resistance
P-glycoprotein activity which decreases accumulation
50
irinotecan MoA
topoisomerase I inhibition
51
irinotecan DLT
bone marrow suppression
52
other side effects of note in irinotecan
severe diarrhea, which lets you know its working
53
two groups of antimitotic agents
stabilizers | destabilizers
54
stabilizing antimitotic drug groups
taxanes | epothilones
55
destabilizing antimitotic drug groups
vinca alkaloids
56
vinca alkaloid drugs
vincristine | vinblastin
57
vinca alkaloids MoA
destabilize microtuble assembly so sister chromatids can't be pulled apart, causing too much DNA to accumulate and cell dies
58
vincristine DLT
peripheral neuropathy
59
vinblastin DLT
bone marrow suppression
60
Taxane drug
paclitaxel
61
paclitaxel MoA
stabilizes microtubule assembly, preventing the spindle from being broken down
62
paclitaxel DLT
myelosuppression | peripheral neuropathy
63
Epothilone drug
ixabepilone
64
ixabepilone mechanism
stabilizes microtubule assembly, preventing the spindle from being broken down
65
L-asparaginase MoA
hydrolyzes L-asparagine to deplete it, inhibiting protein synthesis
66
L-asparaginase use
treatment of ALL
67
hormonal agent drugs
``` tamoxifen anastrozole degarelix bicalutamide prednisone ```
68
tamoxifen MoA
- blocks estrogen response - inhibits G1 to S transition - antiestrogen SERM
69
tamoxifen toxicity
- rarely severe - n/v - hot flashes - vaginal bleeding
70
tamoxifen cancer risk
2-3 fold increase in endometrial cancer risk
71
anastrozole MoA
- significantly suppress serum estradiol levels | - inhibits aromatase, which catalyzes the final step in estrogen production
72
anastrozole toxicity
- rare severe | - some musculoskeletal
73
anastrozole use
ER positive breast cancer
74
tamoxifen use
breast cancer
75
leuprolide MoA
acts on pituitary to inhibit FSH and LH release (via negative feed back because it is an AGONIST)
76
Degarelix MoA
GnRH antagonist
77
leuprolide and degarelix use
prostate cancer | leuprolide needs antiandrogens with it
78
benefit of degarelix over leuprolide
no initial testosterone surge
79
bicalutamide MoA
inhibits uptake and/or binding of testosterone by prostate tissue (antiandrogen)
80
bicalutamide use
- metastatic prostatic carcinoma | - combined with LHRH agonists
81
bicalutmide toxicity
rarely severe adverse reactions
82
prednisone use
- hodgkins - acute lymphocytic leukemia - lymphoma
83
trastuzumab target and use
- HER2/neu | - breast cancer
84
cetuximab target and use
- EGFR | - colon cancer
85
rituximab target and use
- CD20 | - B cell lymphoma
86
bevacizumab target and use
- VEGF | - colon and breast
87
ipilimumab target and use
- CTLA-4 | - melanoma and lung
88
anti cancer antibody that targets the immune system
ipilimumab
89
potential mechanisms for how antibodies work in breast cancer
- prevent cleavage of HER2 - prevent dimerization - activate immune response - endocytosis
90
imatinib main target
Bcr-Abl
91
imatinib toxicity
usually mild N/V edema some bone marrow
92
signal transduction inhibitors
``` imatinib nilotinib dasatinib bosutinib ponatinib sorafenib tosylate vemurafenib *all kinases* ```
93
sunitinib features
broad spectrum kinase inhibitor that is used after others have failed
94
sorafenib tosylate MoA
inhibits raf/MEK/ERK and VEGFR pathways
95
sorafenib tosylate uses
carcinomas | melanoma
96
sorafenib tosylate ADME
metabolized by 3A4 | inhibits other cyps
97
sorafenib tosylate DLT
bone marrow suppression | *skin rash most common
98
vemurafenib MoA
inhibits Raf/MEK/ERK
99
vemurafenib use
metastatic melanoma | some lung cancers
100
vemurafenib toxicity
30% develop cutaneous squamous sell carcinoma
101
bortezomib MoA
- 26S proteasome inhibitor in mammalian cells | - inhibits NFkB
102
bortezomib uses
multiple myeloma
103
bortezomib toxicity
GI peripheral neuropathy hematological toxicities
104
tretinoin use
acute promyelocytic leukemia
105
arsenic trioxide use
acute promyelocytic leukemia
106
arsenic trioxide mechanism
damages PML/RAR fusion protein
107
arsenic trioxide toxicity
tachycardia | prolonged QT
108
thalidomide use
multiple myeloma
109
thalidomide mechanism
- angiogenesis inhibitor | - TNF blocking
110
thalidomide toxicity
- CV events - neuropathy - teratogen
111
vorinostat MoA
histone deacetylase inhibitor
112
vorinostat use
cutaneous t-cell lymphoma
113
biologics used to bolster immune system
IL-2 | interferons
114
IL-2 use
metastatic melanoma
115
Interferons use
hairy cell leukemia

PT3 Oncology (9 decks)

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