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PT3 Oncology > Pharmacology > Flashcards

Flashcards in Pharmacology Deck (115):
1

classes that are alkylating agents

-nitrogen mustards
-nitrosoureas
-platinum compounds

2

alkylating agents general MoA

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

3

monofunctional alkylating agents cause

single strand DNA breaks

4

bifunctional alkylating agents cause

inhibition of DNA replication and transcription by crosslinking DNA

5

nitrogen mustards specific MoA

-get activated into a aziridine ring
-nucleophilic attack of unstable aziridine ring on DNA

6

nitrogen mustard drugs

-mechlorethamine
-cyclophosphamide (used more)
-procarbazine (atypical)
-dacarbazine (atypical)

7

mechlorethamine recovery rate

delayed, very slow

8

cyclophosphamide recovery rate

rapid

9

nitrogen mustards dose limiting toxicity

myelosuppression

10

nitrogen mustards common resistance pathway

increase in DNA repair

11

toxic metabolite of cyclophosphamide

acrolein

12

acrolein toxicity

-nephrotoxic and urotoxic
-causes severe hemorrhagic cystitis

13

drug to reduce acrolein toxicity

MESNA

14

procarbazine main action

methylator

15

dacarbazine is given with what

temozolomide

16

dacarbazine and temozolomide are metabolized to what

5-imidizole-4 caroxamide, the active alkylating species

17

platinum compounds

-cisplatin
-carboplatin
-oxaliplatin

18

cisplatin feature

non-cell cycle specific

19

carboplatin feature

less toxic than cisplatin, but less active

20

oxaliplatin feature

little cross resistance with other Pt compounds, less toxic too

21

notable ADME of platinum compounds

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

22

cisplatin DLT

nephrotoxicity
neurotoxicity
ototoxicity

23

carboplatin DLT

myelosuppression - thrombocytopenia

24

oxaliplatin DLT

peripheral neuropathy

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