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Pharm > Antineoplastics > Flashcards

Antineoplastics Flashcards

1
Q

During what phase of the cell cycle are antimetabolites most effective?

A

S-phase

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2
Q

What event can increase the resistance to methotrexate?

A

gene duplications of DHFR

decreased affinity of DHFR for methotrexate

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3
Q

What drug is a prodrug 5FU? Why is this drug used?

A

capectibane

increased oral availability

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4
Q

What enzyme ACTIVATES cytarabine?

A

Deoxycytidine Kinase

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5
Q

What enzyme does cytarabine inhibit?

A

DNA polymerase

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6
Q

What cancer is most commonly treated with cytarabine?

A

AML

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7
Q

What enzyme does ara-C inhibit?

A

DNA polymerase

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8
Q

What drug causes cerebellar syndrome? Why?

A

cytarabine

cytadine deaminase levels are low in CNS

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9
Q

What enzyme inactivates cytarabine?

A

cytidine deaminase

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10
Q

What are the two enzymatic mechanisms by which resistance to cytarabine develops?

A

loss of deoxycytidine kinase

increase cytidine deaminase

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11
Q

What is gemcitabine an analogue of?

A

Difluorodeoxycytidine

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12
Q

What enzyme activates gemcitabine?

A

Deoxycytidine Kinase

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13
Q

What enzyme does deoxycytidine kinase inactivate?

A

Ribonucleotide Reductase

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14
Q

What are the two mechanisms by which tumor cells can increase resistance to gemcitabine?

A

decreased expression of deoxycytidine kinase

increase expression of deoxycytidine

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15
Q

What enzyme activates 6-MP and 6-TG?

A

HGPRTase

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16
Q

What is 6-MP converted to?

A

thio-IMP

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17
Q

What is 6-TG converted to?

A

thio-GMP

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18
Q

What can thio-IMP be converted into?

A

thio-GMP

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19
Q

What two products does IMP get converted into?

A

AMP and GMP

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20
Q

What can thio-GMP be converted into?

A

thio-dGTP

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21
Q

What is the main side effect of 6-MP and 6-TG?

A

myelosuppression

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22
Q

How do cells become resistant to 6-MP and 6-TG?

A

mutations in HGPRTase

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23
Q

Is fludarabine a purine or pyrimidine analogue?

A

purine

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24
Q

What enzyme activates fludarabine?

A

Deoxycytidine kinase

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25
Q

What two enzymes does fludarabine inhibit?

A

DNA polymerase and RNR

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26
Q

What cancer is most often treated with fludarabine?

A

CLL

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27
Q

What is the mechanism by which fludarabine resistance can develop?

A

decreased activity of deoxycytidine kinase

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28
Q

Is cladribine a purine or pyrimidine analogue?

A

purine

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29
Q

What enzyme activates cladrabine?

A

deoxycytidine kinase

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30
Q

What enzyme is inhibited by cladrabine ?

A

RNR

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31
Q

What disease is most often treated with cladrabine?

A

hairy cell leukemia

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32
Q

What are the two mechanisms by which a cell can become resistance to cladribine?

A

decreased activity of deoxycytidine kinase

increased expression of RNR

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33
Q

What is the most common site for alkylating agents to function?

A

Guanine N7

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34
Q

What disease often presents after treatment with an alkylating agent?

A

leukemia

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35
Q

What type of drug is Mechlorethamine?

A

alkylating agent

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36
Q

What type of drug is cyclophosphamide?

A

alkylating agent

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37
Q

What is the main side effect of cyclophosphamide?

A

hemorrhagic cystitis

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38
Q

What drug is used to treat the side effects of cyclophosphamide? What is the MOA of this drug?

A

Mesna

scavenges acroleid

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39
Q

What is the MOA of carmustine? What type of drug family does carmustine fall into?

A

alkylating agent

nitrosurea

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40
Q

What type of cancer is most often treated with carmustine?

A

brain tumors

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41
Q

What are the three non-classical alkylating agents ?

A

carboplatin

cisplatin

oxaliplatin

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42
Q

What are the three main adverse effects of cisplatin?

A

nephrotoxicity

peripheral neuropathy

ototoxicity

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43
Q

What is the main difference between cisplatin and carboplatin?

A

carboplatin does not cause nephrotoxicity or neuropathy

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44
Q

What is used to mitigate the deleterious effects of cisplatin?

A

co-administration with IV saline

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45
Q

What is the MOA of vinblastine?

A

prevents formation of microtubules

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46
Q

What is the MOA of vincristine?

A

prevents formation of microtubules

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47
Q

What is the main side effect of cytarabine?

A

pancytopenia

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48
Q

What is the main side effect of Carboplatin?

A

myelosuppression

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49
Q

What is the main side effect of vinblastine?

A

myelosuppression (BLASTs bone marrow)

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50
Q

What is the main side effect of vincristine?

A

neurotoxicity

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51
Q

What subunit of microtubules does paclitaxel bind? What does this prevent?

A

β-tubulin

disassembly of microtubules

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52
Q

What are the two main side effects of paclitaxel?

A

PERIPHERAL NEUROPATHY and myelosuppression

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53
Q

What drug is used to ameliorate the myelosuppressive side effects of paclitaxel? What is the MOA of this drug?

A

Filgrastim

acts as G-CSF

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54
Q

What drug has the identical MOA of paclitaxel?

A

Docetaxel

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55
Q

Paclitaxel and docetaxel requires the pretreatment with what two drugs? Why?

A

Dexamethosone or anti-histamine

prevent hypersensitivity

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56
Q

Topoisomerase I is inhibited by what two drugs? What phase of the cell cycle do these two drugs work?

A

irinotecan and topotecan

S-phase

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57
Q

What enzyme does etoposide inhibit?

A

topoisomerase II

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58
Q

What are the three MOAs of doxorubicin?

A

intercalates DNA

inhibit DNA polymerase

inhibits topoisomerase II

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59
Q

What is the main adverse effect of doxorubicin?

A

cardiomyopathy

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60
Q

What drug functions similar to doxorubicin but has a lower liklihood of developing cardiomyopathy?

A

Epirubicin

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61
Q

Iron and copper can be chelated by what drug?

A

Bleomycin

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62
Q

What is the MOA of bleomycin?

A

causes single and double stranded DNA breaks

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63
Q

What is the main side effect of bleomycin?

A

pulmonary fibrosis

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64
Q

What type of cancer would prednisone be useful for? Why?

A

lymphocytic leukemias

causes apoptosis of lymphocytes

65
Q

What cancer is dexamethasone used to treat?

A

multiple myeloma

66
Q

Other than endometrial issues, what can tamoxifen cause?

A

thromboembolism

67
Q

How does a cell develop a resistance to tamoxifen?

A

decreased affintity for the estrogen receptor

68
Q

What is the MOA of anastrazole? What patient group?

A

aromatase inhibitor

post-menopausal women

69
Q

What specific type of cancer is anastrazole used to treat?

A

estrogen sensitive breast cancer

70
Q

What two drugs are androgen receptor antagonists?

A

Flutamide and bicalutamide

71
Q

What specific type of cancer are flutamide and bicalutamide used to treat?

A

prostate

72
Q

What two drugs affect GnRH release? Are they agonists or antagonists?

A

Leuprolide and Goserelin

Agonists

73
Q

Leuprolide and Goserelin are used to decrease the secretion of what? How do they do this?

A

LH and FSH

desensitizing GnRH receptors

74
Q

What is the GnRH antagonist?

A

Degarelix

75
Q

What is another name for trastuzumab?

A

Herceptin

76
Q

What family does HER2/Neu belong?

A

EGFR

77
Q

What is the main side effect of trastuzumab?

A

cardiotoxicity

78
Q

What type of antibody is Cetuximab? What does Cetuximab target? What cancer?

A

monoclonal

EGFR

colorectal

79
Q

How does resistance to cetuximab develop?

A

mutations in Ras signaling

80
Q

What three proteins can imatinib inhibit?

A

BCR-ABL

c-Kit

PDGF

81
Q

How does resistance against imatinib develop?

A

point mutations in ABL

82
Q

What receptor is inhibited by Erlotinib? What is the MOA of erlotinib?

A

EGFR inhibitor

prevent ATP from binding

83
Q

What rxn does asparaginase catalyze?

A

asparagine into aspartate

84
Q

What cancer is most often treated with asparaginase?

A

ALL

85
Q

What is the primary side effect of asparaginase?

A

allergic rxn

86
Q

What is the MOA of bortezomib? The txn of what gene can be inhibited by Bortezomib?

A

inhibitor of proteasome

NFKB

87
Q

What is the mechanism by which bortezomib can inhibit neoplasia?

A

inhibition of apoptosis during hypoxic conditions

88
Q

What specific important protein can Bortezemib inhibit the activity of ?

A

p53

89
Q

What is the most common side effect of bortezemib?

A

peripheral neuropathy

90
Q

Temsirolimus is an analogue of what drug? What complex is inhibited? What does this lead to?

A

rapamycin

mTOR

apoptosis

91
Q

What cancer is temsirolimus currently in approval for treatment of?

A

renal cell carcinoma

92
Q

What are the two specific toxicities of methotrexate?

A

interstitial pneumonitis

nephrotoxic

93
Q

Cytarabine is an incredibly important drug in treating what cancer?

A

AML

94
Q

When cell cycle phase is cytarabine most effective ?

A

S-phase

95
Q

What is the primary mode of resistance in AML?

A

loss of deoxycytidine kinase activity

96
Q

What enzyme does gemcitabine inhibit?

A

ribonucleotide reductase

97
Q

What is the main treatment of ALL?

A

6-MU/Azathioprine

98
Q

What organ is acrolein most toxic to?

A

bladder

99
Q

What is the important functional group of mesna?

A

sulfhydryl

100
Q

What molecule can a cell produce in order to increase resistance to an alkylating agent?

A

glutathione

101
Q

What enzyme can cells increase to provide resistance against alkylting agents? What is the MOA of this enzyme?

A

MGMT

quickly removes alkyl group from DNA

102
Q

What transporter is used to get platinum containing drugs into the cell?

A

copper transporter

103
Q

What is a shared toxicity between cisplatin and carboplatin?

A

anaphylaxis reactions

104
Q

What cancer is procarbazine used to treat?

A

Hodgkin’s lymphoma

105
Q

What three cancers can dacarbazine treat?

A

HL, Melanoma, Sarcoma

106
Q

What two cancers can temozolomide treat?

A

gliablastoma and metastatic melanoma

107
Q

What drug is often co-administered with doxorubicin? What is the MOA of this drug?

A

Dexrazoxane

to chelate iron

108
Q

What cell cycle phase is interrupted by bleomycin?

A

G2

109
Q

What is a notable characteristic about bleomycin concerning its administration with other drugs?

A

minimally myelosuppressive

110
Q

What family of drugs are used to reduce intracranial pressure?

A

glucocorticoids

111
Q

What is the most common side effect of bevacizumab?

A

hypertension

112
Q

Which two receptors does Lapatinib inhibit? What is the MOA of this drug?

A

EGFR and HER-2

inhibits tyrosine kinase activity of HER2 and EGFR

113
Q

Does imatinib inhibit BCR or ABL? By what mechanism?

A

ABL

competitive inhibitor of ABL ATP binding site

114
Q

What cancer is asparaginase used to treat? Why?

A

ALL

tumor cells cant produce enough asparagine

115
Q

What cancer is bortezemib used to treat?

A

refractory multiple myeloma

116
Q

What drug is used in combat the negative effects of methotrexate? What is the MOA of this drug?

A

Leucovorin

folinic acid

117
Q

Methotrexate causes can kill which two types of cell?

A

bone marrow and intestinal epithelial

118
Q

How does hemorrhagic cystitis manifest?

A

blood in urine

119
Q

What is the most severe side effect of carmustine?

A

myelosuppression

120
Q

What three reasons is carbiplatin used in the place of cisplatin?

A

decrease ototoxicity

decreased nephropathy

decreased peripheral neuropathy

121
Q

What drug is used to mitigate the effects of paclitaxel? Why?

A

filgastrim

acts as GCSF

122
Q

What is another side effect of paclitaxel, other than myelosuppression and peripheral neuropathy?

A

Hypersensitivity rxn

123
Q

What are the two main side effects of irinotecan and topotecan?

A

myelosuppression and diarrhea

124
Q

Which antineoplastic can chelate iron and copper ?

A

bleomycin

125
Q

What is the MOA for how Degarelix is used to treat prostate cancer?

A

decreases FSH and LH secretion from anterior pituitary

126
Q

What drug is trastuzumab often used in combination with?

A

paclitaxel

127
Q

What type of symptoms do all monoclonal therapies produce?

A

B-cell symptoms

128
Q

What is the common side effect of avastin?

A

HTN

129
Q

Which component of BCR-ABL fusion has the kinase activity?

A

ABL

130
Q

How do cells develop resistance against imatinib?

A

point mutations in ABL

131
Q

Erlotinib is used to treat which type of cancer?

A

metastatic non-small cell lung carcinoma

132
Q

Bortezomib is used to treat what cancer?

A

multiple myeloma

133
Q

Does methotrexate inhibit DNA or RNA or synthesis of both?

A

both

134
Q

Does methotrexate inhibit purine or pyrimidie or synthesis of both?

A

both

135
Q

What drug is methotrexate often used in combination with?

A

Dactinomycin

136
Q

What enzyme does 5-FU inhibit?

A

thymidylate synthase

137
Q

What is 5-FU metabolized into?

A

FdUMP

138
Q

Does 5-FU cause damage to DNA or RNA or both?

A

both

139
Q

Which phase of the cell cycle is cytarabine effective in?

A

S-phase

140
Q

What is 6-MP converted into?

A

thio-IMP

141
Q

What is 6-TG converted into?

A

thio-GMP

142
Q

Thiopurine methyltransferase selectively inhibits which anti-neoplastic? What is the severe effect in individuals who have mutations in this enzyme?

A

6-MP

life-threatening bone marrow suppression

143
Q

Does thio-IMP inhibit the synthesis or salvage or both of purines?

A

both

144
Q

During what cell cycles are alkylating agents cytotoxic?

A

all cell cycles

145
Q

What is the main side effect of all alkylating agents?

A

myelosuppression

146
Q

What are the two mechanisms of resistance for all alkylating agents?

A

glutathione

MGMT (methylguanosine-methyl transferase)

147
Q

What nucleophile do non-classical alkylating agents target?

A

Guanine N7

148
Q

How do non-classical alkylating agents get into the cell?

A

copper transporter

149
Q

What electrolyte can cisplatin disturb?

A

magnesium

150
Q

Which two alkylating agent can cause hypersensitivity rxns?

A

Cisplatin and carboplatin

151
Q

What cancer is treated with procarbazine?

A

HL

152
Q

What two cancers are treated with dacarbazine?

A

melanoma and sarcoma

153
Q

What cell cycle phase does paclitaxel arrest cells in?

A

mitosis

154
Q

Lapitinib is a monoclonal antibody against which two receptors? Which cancer is lapitinab used to treat?

A

EGFR and HER2

refractory breast

155
Q

What are the two mechanisms by which a cancer may develop resistance to erlotinib?

A

mutation in EGFR

amplification of MET oncogene

156
Q

Tamoxifen can increase the risk for what cancer?

A

endometrial

157
Q

Flutamide and bicalutamide prevent what agonist from binding the androgen receptor?

A

dihydrotestosterone

158
Q

Which anti-neoplastics can cause blister and damage veins?

A

alkylating agents

159
Q

What is the main use of bevucizimab?

A

colorectal cancer

Pharm (12 decks)

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