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Heme/Onc > Chemo Drugs > Flashcards

Chemo Drugs Flashcards

1
Q

Which medications are folate antagonists?

A

MTX

Pemetrexed

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2
Q

What do we give with HD MTX?

A

Leucovorin

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3
Q

What do we give with pemetrexed?

A

Folic acid

B12

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4
Q

What is the MOA of folate antagonists?

A

Inhibits dihydrofolate reductase which results in blockage of thymidylate and purine synthesis
Pemetrexed is a multi-targeted antifolate

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5
Q

What are the AEs of folate antagonists?

A

Myelosuppression
Mucositis
Renal tubular necrosis with HD MTX

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6
Q

With which drug should supplemental steroid eye drops be given?

A

HD Cytarabine

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7
Q

What are the pyrimidine antagonists?

A

Fluorouracil
Capecitabine
Cytarabine
Gemcitabine

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8
Q

What is the MOA of pyrimidine antagonists?

A

Structural analogues of pyrimidines
Fluorouracil inhibits thymidylate synthase, which inhibits formation of thymidine (affects DNA and RNA)
Capecitabine is a fluorouracil prodrug

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9
Q

What are the AEs of pyrimidine antagonists?

A 
Myelosuppression
Mucositis, stomatitis
Diarrhea
"Hand-foot syndrome"
Neurologic
Cytarabine: rash and conjunctivitis
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10
Q

What AE is more common with capecitabine use?

A

Hand-foot syndrome

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11
Q

What neurologic AE does cytarabine cause?

A

Cerebellar toxicity

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12
Q

What are the purine antagonists?

A

Fludarabine
Thioguanine (6-TG)
Mercaptopurine (6-MP)

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13
Q

What is the MOA of purine antagonists?

A

Analogues of purines which get incorportated into DNA to prevent functional DNA synthesis

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14
Q

What are the AEs of purine antagonists?

A 
Myelosuppression
Liver toxicity (6-TG, 6-MP)
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15
Q

Which purine do we give prophylactic abx and antivirals with?

A

Fludarabine

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16
Q

What classes are the antimetaolites?

A

Folate antagonists
Pyrimidine antagonists
Purine antagonists

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17
Q

What classes are the alkylating agents?

A

Nitrogen mustard derivatives
Platinum analogs
Alkylsulfonates

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18
Q

Which drugs are the nitrogen mustard derivatives?

A

Cyclophosphamide
Ifosfamide
Bendamustine
Mechlorethamine

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19
Q

What is the MOA of nitrogen mustard derivatives?

A

Form DNA cross-links, resulting in inhibition of DNA synthesis and function

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20
Q

What are the AEs of nitrogen mustard derivatives?

A 
Myelosuppression
N/V
Alopecia
Sterility/Infertility
Hemorrhagic cystitis
Infections (bendamustine)
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21
Q

Which drugs cause hemorrhagic cystitis?

A

Ifosfomide

Cyclophosphamide

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22
Q

What medication is used to prevent hemorrhagic cystitis?

A

Mesna

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23
Q

Which drugs are platinum analogs?

A

Cisplatin
Carboplatin
Oxaliplatin

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24
Q

What is the MOA of the platinum analogs?

A

From intrastrand and interstrand DNA cross-links

Binds to nuclear and cytoplasmic proteins

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25
Q

What are the AEs of cisplatin?

A 
Nephrotoxicity
Severe N/V
Ototoxicity
Neuropathy
Electrolyte depletion (Mg, K)
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26
Q

What are the AEs of carboplatin?

A

Myelosuppression
Moderate-severe N/V
Hypersensitivity

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27
Q

What are the AEs of oxaliplatin?

A

Neuropathy
Moderate-severe N/V
Myelosuppression
Hypersensitivity

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28
Q

What drug additional therapy is given with cisplatin?

A

Fluids before and after for nephrotoxicity

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29
Q

What are the alkylsulfonates?

A

Busulfan

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30
Q

When is Busulfan used?

A

Bone marrow/stem cell transplant

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31
Q

What is the MOA of Alkylsulfonates?

A

Cleavage of alkyl oxygen bond and formation of a butyl compound that forms crosslinks with DNA

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32
Q

What are the AEs of alkylsulfonates?

A

Myelosuppression
Pulmonary toxicity
Skin pigmentation

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33
Q

What are miscellaneous alkylating agents?

A

Bleomycin

Dacarbazine

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34
Q

What is the MOA of Bleomycin?

A

Mixture of peptides from fungal streptomyces species

Binds to DNA and produces single and double stranded DNA breaks following free radical formation

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35
Q

What are bleomycin AEs?

A

Pulmonary toxicity
Hyperpigmentation
Febrile reaction

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36
Q

What are the dacarbazine AEs?

A

Myelosuppression

N/V

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37
Q

What are the classes of enzyme inhibitors?

A

Anthracyclines
Epipodophyllotoxins
Captothecans

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38
Q

What drugs are anthracyclines?

A

Daunorubicin
Doxorubicin
Idarubicin
Epirubicin

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39
Q

What is the MOA of anthracyclines?

A

Topoisomerase II inhibition
Intercalation of DNA
Formation of free radicals

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40
Q

What are the AEs of anthracyclines?

A 
Myelosuppression
Cardiomyopathy
Moderate-severe N/V
Extravasation
Red urine
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41
Q

What do we monitor in anthracyclines?

A

CBC
LFTs
EF

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42
Q

What drugs are epipodophyllotoxins?

A

Etoposide

Tenoposide

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43
Q

What is the MOA of epipodophyllotoxins?

A

Topoisomerase II inhibition

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44
Q

What are the AEs of epipodophyllotoxins?

A

Myelosuppression
Hypotension (IV etoposide)
Alopecia

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45
Q

What are the camptothecans?

A

Irinotecan

Topotecan

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46
Q

What is the MOA of camptothecans?

A

Topoisomerase I inhibition

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47
Q

What are the AEs of camptothecans?

A

Myelosuppression
Alopecia
Diarrhea (dose-limiting for irinotecan)

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48
Q

If a patient on a camptothecan experiences diarrhea, how do we treat it?

A

w/in 24 hours = atropine

after = loperamide

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49
Q

What classes are microtubule-targeting drugs?

A

Taxanes

Vinca alkaloids

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50
Q

Which medications are taxanes?

A

Paclitaxel
Docetaxel
Albumin-bound paclitaxel
Cabazitaxel

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51
Q

What is the MOA of taxanes?

A 
Bind tubulin and stabilize microtubules
Prevent depolymerization (freeze cell in anaphase/telophase)
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52
Q

What are the AEs of Taxanes?

A

Hypersensitivity**
Peripheral neuropathy**
Myelosuppression
Alopecia

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53
Q

What medications do we administer with docetaxel and why?

A

Dexamethason to lower risk of fluid retention

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54
Q

What medications do we adminsiter with Paclitaxel?

A

Steroid, H1RA (benadryl) and H2RA (ranitidine)

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55
Q

What are vinca alkaloids?

A

Vinblastine
Vincristine
Vinorelbine

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56
Q

What is the MOA of vinca alkaloids?

A

Bind tubulin and interfere with microtubule assembly (depolymerize microtubule) preventing spindle formation

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57
Q

What are the AEs of Vinca alkaloids?

A

Myelosuppression (vinblastine/vinorelbine)
Neurologic toxicity (vincristine)
Constipation
Extravasation

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58
Q

Which vinca alakloid do we not administer intrathecally?

A

Vincristine

ISMP recommends against syringe use

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59
Q

What is the MOA of target agents-ABs?

A

Block cell surface receptor function and/or recruit immune cells and complement for tumor cell apoptosis
May be linked to chemotherapy agents or radioactive particles

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60
Q

What are the 4 ways that target agents-AB work?

A

Binding of ab to surface protein
Stimulation of ADCC (Antibody-dependent cellular toxicity)
Stimulation of CDC (complement-dependent cytotoxicity)
Angiogenesis

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61
Q

What are AEs of target agents-ABs?

A

Hypersensitivity/infusion related reactions (get better with subsequent treatment)

62
Q

How do we premedicate for target agent-ABs?

A

Antihistamines
AND
APAP/dexamethasone

63
Q

What medications target antibodies?

A 
Trastuzumab
Pertuzumab
Rituxumab
Ofatumumab
Obinutuzumab
Alemtuzumab
Cetuximab
Panitumumab
Blinatumomab
Bevacizumab
64
Q

What AB does trastuzumab target?

A

HER-2

65
Q

What is the AE for trastuzumab?

A

Cardiomyopathy

66
Q

What is the target for Pertuzumab?

A

HER-2 extracellular domain

Works complementary with trastuzumab

67
Q

What are the AEs for pertuzumab?

A

Cytopenias
Fetal toxicity
LV dysfunction

68
Q

What are the AEs of Rituximab?

A

HepB/Tb reactivation

Severe SJS

69
Q

What does ofatumumab/ obinutuzumab/ rituximab target?

A

CD20 surface antigen on B-lymphocyte

70
Q

What are the AEs of ofatumumab/obinutuzumab?

A

HepB/Tb reactivation
Cytopenias
Progressive multifocal leukoencephalopathy (PML)

71
Q

What does alemtuzumab target?

A

CD52 antigen on leukemic lymphocytes

72
Q

What are the AEs for alemtuzumab?

A

Cytopenias

Infections

73
Q

What is the target of cetuximab/ panitumumab?

A

Cell surface EGFR-2

74
Q

When are cetuximab/ panitumumab not effective?

A

KRAS mutations

75
Q

What are the AEs of Cetuximab/ panitumumab?

A

Acniform rash

Hypomagnesemia (monitor Mg, K, Ca)

76
Q

What does blinatumomab a target?

A

Bispecific T-cell egager (BiTE): helps connect T cell to cancer cell

77
Q

What are the AEs of blinatumomab?

A

Cytopenias
Infections
Cytokine release syndrome

78
Q

What de we premedicate blinatumomab with?

A

Dexamethasone

79
Q

What does bevacizumab target?

A

VEGF ligand to prevent angiogenesis

80
Q

Which targeted agents-AB cannot be administered within 28 days of surgery?

A

Bevacizumab

81
Q

What are AEs for Bevacizumab?

A

GI perforation
Hemorrhage/thrombotic nephrotic syndrome
HTN

82
Q

What agents target Tyrosine Kinase inhibitors?

A 
Imatinib
Nilotinib
Dasatinib
Erlotinib
Afatinib
Alectinib
Dabrafenib
Vemurafenib
Trametinib
Cobimetinib
83
Q

What drugs do tyrosine kinase inhibitors interact with?

A

3A4
Azoles (inhibitors)
Rifampin/phenytoin (inducers)

84
Q

What is the MOA of imatinib?

A

Inhibits BCR-ABL tyrosine kinase caused by Philadelphia chromosome translocation

85
Q

What is the DDI for imatinib?

A

3A4 substrate

86
Q

What are the AEs for imatinib?

A

Myelosuppression
Fluid retention
Myalgias
CHF

87
Q

What is the MOA of nilotinib?

A 
Inhibits BCR-ABL tyrosine kinases, including those resistant to imatinib
Multiple receptor (mrTKI)
88
Q

What are the DDIs of nilotinib?

A

3A4, 2C8, 2C9, 2D6 inhibitor

Inducer of other enzymes

89
Q

What are the AEs of nilotinib?

A

QT prolongation**
Rash
Myelosuppression
Hepatotoxicity

90
Q

What is the MOA of dasatinib?

A

Inhibits BCR-ABL tyrosine kinases, including those resistant to imatinib
mrTKI

91
Q

What are the DDIs of dasatinib?

A

3A4 substrate

92
Q

What are the AEs of dasatinib?

A 
Myelosuppression
Fluid retention
Pleural effusion
QT prolongation
Pulmonary arterial HTN
93
Q

What is the MOA of erlotinib?

A

EGFR tyrosine kinase inhibitor

94
Q

What are the DDIs of erlotinib?

A

3A4 substrate

95
Q

What are the AEs of erlotinib?

A

Diarrhea
Rash
Hepatotoxicity
Interstitial lung disease

96
Q

What is the MOA of afatinib?

A

EGFR tyrosine kinase inhibitor

May have some HER-2 activity

97
Q

What are the DDIs of afatinib?

A

P-gp substrate and inhibitor

98
Q

What are the AEs of afatinib?

A

Severe diarrhea
Skin disorders
Hepatotoxicity

99
Q

What is the MOA alectinib?

A

Inhibits multiple tyrosine kinases including anaplastic lymphoma kinase (ALK)

100
Q

What are the DDIs of alectinib?

A

3A4 substrate

No clinically relevant drug interactions

101
Q

What are the AEs of alectinib?

A

Constipation
Fatigue
Peripheral edema
Bradycardia

102
Q

What are the MOAs of dabrafenib/ vemurafenib?

A

BRAF serine-threonine kinase inhibitor

Indicated for metastatic melanoma with BRAF V600E mutation (not indicated for wild type)

103
Q

What does BRAF stand for?

A

b-Rapidly Accelerated Fibrosarcoma

104
Q

What are the DDIs of dabrafenib/ vemurafenib?

A

3A4 substrate

Avoid strong 3A4 inducers and inhibitors

105
Q

What are the AEs of dabrafenib/ vemurafenib?

A

New malignancies

QT prolongation

106
Q

What is the MOA of trametinib/ cobimetinib?

A

Kinase inhibitor
Indicated for metastatic melanoma with BRAF V600E or V600K mutations
NOT indicated for patients who have received prior BRAF-inhibitor therapy

107
Q

What are the DDIs for cobimetinib?

A

3A4 substrate

108
Q

What are the AEs for trametinib/ cobimetinib?

A 
Cardiomyopathy
Retinal pigment
Epithelial detachment
Rash
Diarrhea
Lymphedema
109
Q

What drug targets b-cell receptor agents?

A

Ibrutinib

110
Q

What is the MOA for ibrutinib?

A

Selective and irreversible inhibitor of Bruton’s tyrosine kinase (BtK)

111
Q

What are the DDIs for ibrutinib?

A

3A4 substrate

112
Q

What are the AEs for ibrutinib?

A

Diarrhea
Rash
Bruising/bleeding
Neutropenia

113
Q

What drugs block the immune systems checkpoints?

A

Ipilimumab
Pembrolizumab
Nivolumab

114
Q

What does ipilimumab target?

A

Cytotoxic T-lymphocyte antigen (CTLA-4) with effect of increasing T-cell activation and proliferation

115
Q

What is a CTLA-4?

A

Negative regulator of T-cell activation

116
Q

What does pembrolizumab/ nivolumab target?

A

Programmed death-1 receptor

  • Bind to the PD-1 receptor, and block interaction between PD-1 and PD-L1
  • Blocking this inhibitory activity can reactivate the T-cell tumor response
117
Q

What are the AEs of ipilimumab?

A

Infusion reactions
Diarrhea
Pruritis
Rash

118
Q

What are the AEs for pembrolizumab/ nivolumab?

A 
Rash
Pneumonitis
Colitis
Hepatitis
Nephritis
Renal dysfunction
Hypo/hyperthyroidism
119
Q

What is the MOA of interferon alpha-2b?

A

Activities include:

  • Inhibition of cell proliferation
  • Enhanced phagocytic activity of macrophages
  • Increased cytotoxicity of NKCs
120
Q

What are the AEs of interferon alpha-2b?

A 
Flu-like syndrome (fever, HA, myalgia, weakness)
Bone marrow suppression 
CNS & neurological effects
Thyroid changes
Hepatotoxicity
121
Q

What is the BBW of interferon alpha-2b?

A

May cause or exacerbate fatal or life-threatening neuropsychiatric, autoimmune, ischemic, or infectious disorders

122
Q

How do we pretreat interferon alpha-2b?

A

NSAIDs or APAP

123
Q

What are the AEs for interleukin-2?

A 
Flu-like syndrome
Capillary leak syndrome (flu-like symptoms, low BP)
N/V/D
Impaired neutrophil function
CNS effects
124
Q

What is the BBW for interleukin-2?

A

Patients should have normal cardiac and pulmonary function

125
Q

What drugs classes work on the endocrine system?

A

Antiestrogens
Aromatase inhibitors
GnRH Agonists/LHRH agonists
Antiandrogens

126
Q

What are the antiestrogens?

A

Tamoxifen
Toremifene
Raloxifene

127
Q

What are the aromatase inhibitors?

A

Anastrozole
Letrozole
Exemestane

128
Q

What are the GnRH/LHRH agonists?

A

Leuprolide
Gosereline
Triptorelen

129
Q

What are the antiandrogens?

A

Flutamide
Nilutamide
Bicalutamide
Enzalutamide

130
Q

What is the MOA of antiestrogens?

A

Blocks estrogen receptor
Blocking estrogen stimulation of hormone sensitive tumors
Raloxifene with some proestrogenic effects

131
Q

What are the AEs of antiestrogens?

A

Hot flashes
N/V
Thromboembolic events

132
Q

What is the MOA of aromatase inhibitors?

A

Inhibits enzyme that converts androgen to estrogens

133
Q

What are the AEs of aromatase inhibitors?

A

Hot flashes
Fatigue
Bone/joint pain
Decreased bone density

134
Q

What is the MOA of GnRH/LHRH agonists?

A

Feed back to pituitary to decrease release of FSH and LH

135
Q

What are the AEs of GnRH/LHRH agonists?

A 
Tumor flare (initially)
Hot flashes
Gynecomastia
Decreased bone density
Injection site pain
Decreased libido
136
Q

What is the MOA of antiandrogens?

A

Testosterone receptor blocker

137
Q

What are the AEs of antiandrogens?

A

Hot flashes
Gynecomastia
Increased LFTs
Blurred vision (nilutamide)

138
Q

What is the MOA of hydroxyurea?

A

Ribonucleoside diphosphate reductase inhibitor

139
Q

What is the MOA of L-Asparaginase pegasparaginase?

A

Inhibits protein synthesis by hydrolyzing asparagine to aspartic acid and ammonia

140
Q

What is the MOA of arsenic trioxide?

A

Damages/degrades the PML-RAR alpha fusion protein

141
Q

What is PML-RAR?

A

Promyelocytic leukemia-retinoin acid receptor

142
Q

What is the MOA of tretinoin (ATRA)

A

Induces differentiation of acute promyelocytic leukemia cells

143
Q

What are the AEs of hydroxyurea?

A

Myelosuppression
Mucositis
Hepatotoxicity
Renal toxicity

144
Q

What are the AEs of L-asparaginase pegasparaginase?

A

Hypersensitivity
Hyperglycemia
Pancreatitis

145
Q

What are the AEs of arsenic trioxide?

A 
QT prolongation
Peripheral neuropathy
Hyperglycemia
Musculoskeletal pain
"Retinoic acid syndrome"
146
Q

What are the AEs of tretinoin (ATRA)?

A 
Peripheral edema
Edema
Skin dryness
RAsh
Leukocytosis
"Retinoic acid syndrome"
147
Q

How is hydroxyurea used in sickle cell anemia?

A

Reduces painful crises

148
Q

How is hydroxyurea used in leukemias?

A

Reduces malignant cell counts

149
Q

What baseline labs should be taken prior to start of arsenic trioxide?

A

EKG

Electrolytes

150
Q

What vitamin is tretinoin an analogue of?

A

Vitamin A

Heme/Onc (20 decks)

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