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Heme/Onc > Chemo Drugs > Flashcards

Chemo Drugs Flashcards

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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
What are the AEs of cisplatin?
``` Nephrotoxicity Severe N/V Ototoxicity Neuropathy Electrolyte depletion (Mg, K) ```
26
What are the AEs of carboplatin?
Myelosuppression Moderate-severe N/V Hypersensitivity
27
What are the AEs of oxaliplatin?
Neuropathy Moderate-severe N/V Myelosuppression Hypersensitivity
28
What drug additional therapy is given with cisplatin?
Fluids before and after for nephrotoxicity
29
What are the alkylsulfonates?
Busulfan
30
When is Busulfan used?
Bone marrow/stem cell transplant
31
What is the MOA of Alkylsulfonates?
Cleavage of alkyl oxygen bond and formation of a butyl compound that forms crosslinks with DNA
32
What are the AEs of alkylsulfonates?
Myelosuppression Pulmonary toxicity Skin pigmentation
33
What are miscellaneous alkylating agents?
Bleomycin | Dacarbazine
34
What is the MOA of Bleomycin?
Mixture of peptides from fungal streptomyces species | Binds to DNA and produces single and double stranded DNA breaks following free radical formation
35
What are bleomycin AEs?
Pulmonary toxicity Hyperpigmentation Febrile reaction
36
What are the dacarbazine AEs?
Myelosuppression | N/V
37
What are the classes of enzyme inhibitors?
Anthracyclines Epipodophyllotoxins Captothecans
38
What drugs are anthracyclines?
Daunorubicin Doxorubicin Idarubicin Epirubicin
39
What is the MOA of anthracyclines?
Topoisomerase II inhibition Intercalation of DNA Formation of free radicals
40
What are the AEs of anthracyclines?
``` Myelosuppression Cardiomyopathy Moderate-severe N/V Extravasation Red urine ```
41
What do we monitor in anthracyclines?
CBC LFTs EF
42
What drugs are epipodophyllotoxins?
Etoposide | Tenoposide
43
What is the MOA of epipodophyllotoxins?
Topoisomerase II inhibition
44
What are the AEs of epipodophyllotoxins?
Myelosuppression Hypotension (IV etoposide) Alopecia
45
What are the camptothecans?
Irinotecan | Topotecan
46
What is the MOA of camptothecans?
Topoisomerase I inhibition
47
What are the AEs of camptothecans?
Myelosuppression Alopecia Diarrhea (dose-limiting for irinotecan)
48
If a patient on a camptothecan experiences diarrhea, how do we treat it?
w/in 24 hours = atropine | after = loperamide
49
What classes are microtubule-targeting drugs?
Taxanes | Vinca alkaloids
50
Which medications are taxanes?
Paclitaxel Docetaxel Albumin-bound paclitaxel Cabazitaxel
51
What is the MOA of taxanes?
``` Bind tubulin and stabilize microtubules Prevent depolymerization (freeze cell in anaphase/telophase) ```
52
What are the AEs of Taxanes?
Hypersensitivity** Peripheral neuropathy** Myelosuppression Alopecia
53
What medications do we administer with docetaxel and why?
Dexamethason to lower risk of fluid retention
54
What medications do we adminsiter with Paclitaxel?
Steroid, H1RA (benadryl) and H2RA (ranitidine)
55
What are vinca alkaloids?
Vinblastine Vincristine Vinorelbine
56
What is the MOA of vinca alkaloids?
Bind tubulin and interfere with microtubule assembly (depolymerize microtubule) preventing spindle formation
57
What are the AEs of Vinca alkaloids?
Myelosuppression (vinblastine/vinorelbine) Neurologic toxicity (vincristine) Constipation Extravasation
58
Which vinca alakloid do we not administer intrathecally?
Vincristine | ISMP recommends against syringe use
59
What is the MOA of target agents-ABs?
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
60
What are the 4 ways that target agents-AB work?
Binding of ab to surface protein Stimulation of ADCC (Antibody-dependent cellular toxicity) Stimulation of CDC (complement-dependent cytotoxicity) Angiogenesis
61
What are AEs of target agents-ABs?
Hypersensitivity/infusion related reactions (get better with subsequent treatment)
62
How do we premedicate for target agent-ABs?
Antihistamines AND APAP/dexamethasone
63
What medications target antibodies?
``` Trastuzumab Pertuzumab Rituxumab Ofatumumab Obinutuzumab Alemtuzumab Cetuximab Panitumumab Blinatumomab Bevacizumab ```
64
What AB does trastuzumab target?
HER-2
65
What is the AE for trastuzumab?
Cardiomyopathy
66
What is the target for Pertuzumab?
HER-2 extracellular domain | Works complementary with trastuzumab
67
What are the AEs for pertuzumab?
Cytopenias Fetal toxicity LV dysfunction
68
What are the AEs of Rituximab?
HepB/Tb reactivation | Severe SJS
69
What does ofatumumab/ obinutuzumab/ rituximab target?
CD20 surface antigen on B-lymphocyte
70
What are the AEs of ofatumumab/obinutuzumab?
HepB/Tb reactivation Cytopenias Progressive multifocal leukoencephalopathy (PML)
71
What does alemtuzumab target?
CD52 antigen on leukemic lymphocytes
72
What are the AEs for alemtuzumab?
Cytopenias | Infections
73
What is the target of cetuximab/ panitumumab?
Cell surface EGFR-2
74
When are cetuximab/ panitumumab not effective?
KRAS mutations
75
What are the AEs of Cetuximab/ panitumumab?
Acniform rash | Hypomagnesemia (monitor Mg, K, Ca)
76
What does blinatumomab a target?
Bispecific T-cell egager (BiTE): helps connect T cell to cancer cell
77
What are the AEs of blinatumomab?
Cytopenias Infections Cytokine release syndrome
78
What de we premedicate blinatumomab with?
Dexamethasone
79
What does bevacizumab target?
VEGF ligand to prevent angiogenesis
80
Which targeted agents-AB cannot be administered within 28 days of surgery?
Bevacizumab
81
What are AEs for Bevacizumab?
GI perforation Hemorrhage/thrombotic nephrotic syndrome HTN
82
What agents target Tyrosine Kinase inhibitors?
``` Imatinib Nilotinib Dasatinib Erlotinib Afatinib Alectinib Dabrafenib Vemurafenib Trametinib Cobimetinib ```
83
What drugs do tyrosine kinase inhibitors interact with?
3A4 Azoles (inhibitors) Rifampin/phenytoin (inducers)
84
What is the MOA of imatinib?
Inhibits BCR-ABL tyrosine kinase caused by Philadelphia chromosome translocation
85
What is the DDI for imatinib?
3A4 substrate
86
What are the AEs for imatinib?
Myelosuppression Fluid retention Myalgias CHF
87
What is the MOA of nilotinib?
``` Inhibits BCR-ABL tyrosine kinases, including those resistant to imatinib Multiple receptor (mrTKI) ```
88
What are the DDIs of nilotinib?
3A4, 2C8, 2C9, 2D6 inhibitor | Inducer of other enzymes
89
What are the AEs of nilotinib?
QT prolongation** Rash Myelosuppression Hepatotoxicity
90
What is the MOA of dasatinib?
Inhibits BCR-ABL tyrosine kinases, including those resistant to imatinib mrTKI
91
What are the DDIs of dasatinib?
3A4 substrate
92
What are the AEs of dasatinib?
``` Myelosuppression Fluid retention Pleural effusion QT prolongation Pulmonary arterial HTN ```
93
What is the MOA of erlotinib?
EGFR tyrosine kinase inhibitor
94
What are the DDIs of erlotinib?
3A4 substrate
95
What are the AEs of erlotinib?
Diarrhea Rash Hepatotoxicity Interstitial lung disease
96
What is the MOA of afatinib?
EGFR tyrosine kinase inhibitor | May have some HER-2 activity
97
What are the DDIs of afatinib?
P-gp substrate and inhibitor
98
What are the AEs of afatinib?
Severe diarrhea Skin disorders Hepatotoxicity
99
What is the MOA alectinib?
Inhibits multiple tyrosine kinases including anaplastic lymphoma kinase (ALK)
100
What are the DDIs of alectinib?
3A4 substrate | No clinically relevant drug interactions
101
What are the AEs of alectinib?
Constipation Fatigue Peripheral edema Bradycardia
102
What are the MOAs of dabrafenib/ vemurafenib?
BRAF serine-threonine kinase inhibitor | Indicated for metastatic melanoma with BRAF V600E mutation (not indicated for wild type)
103
What does BRAF stand for?
b-Rapidly Accelerated Fibrosarcoma
104
What are the DDIs of dabrafenib/ vemurafenib?
3A4 substrate | Avoid strong 3A4 inducers and inhibitors
105
What are the AEs of dabrafenib/ vemurafenib?
New malignancies | QT prolongation
106
What is the MOA of trametinib/ cobimetinib?
Kinase inhibitor Indicated for metastatic melanoma with BRAF V600E or V600K mutations NOT indicated for patients who have received prior BRAF-inhibitor therapy
107
What are the DDIs for cobimetinib?
3A4 substrate
108
What are the AEs for trametinib/ cobimetinib?
``` Cardiomyopathy Retinal pigment Epithelial detachment Rash Diarrhea Lymphedema ```
109
What drug targets b-cell receptor agents?
Ibrutinib
110
What is the MOA for ibrutinib?
Selective and irreversible inhibitor of Bruton's tyrosine kinase (BtK)
111
What are the DDIs for ibrutinib?
3A4 substrate
112
What are the AEs for ibrutinib?
Diarrhea Rash Bruising/bleeding Neutropenia
113
What drugs block the immune systems checkpoints?
Ipilimumab Pembrolizumab Nivolumab
114
What does ipilimumab target?
Cytotoxic T-lymphocyte antigen (CTLA-4) with effect of increasing T-cell activation and proliferation
115
What is a CTLA-4?
Negative regulator of T-cell activation
116
What does pembrolizumab/ nivolumab target?
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
What are the AEs of ipilimumab?
Infusion reactions Diarrhea Pruritis Rash
118
What are the AEs for pembrolizumab/ nivolumab?
``` Rash Pneumonitis Colitis Hepatitis Nephritis Renal dysfunction Hypo/hyperthyroidism ```
119
What is the MOA of interferon alpha-2b?
Activities include: - Inhibition of cell proliferation - Enhanced phagocytic activity of macrophages - Increased cytotoxicity of NKCs
120
What are the AEs of interferon alpha-2b?
``` Flu-like syndrome (fever, HA, myalgia, weakness) Bone marrow suppression CNS & neurological effects Thyroid changes Hepatotoxicity ```
121
What is the BBW of interferon alpha-2b?
May cause or exacerbate fatal or life-threatening neuropsychiatric, autoimmune, ischemic, or infectious disorders
122
How do we pretreat interferon alpha-2b?
NSAIDs or APAP
123
What are the AEs for interleukin-2?
``` Flu-like syndrome Capillary leak syndrome (flu-like symptoms, low BP) N/V/D Impaired neutrophil function CNS effects ```
124
What is the BBW for interleukin-2?
Patients should have normal cardiac and pulmonary function
125
What drugs classes work on the endocrine system?
Antiestrogens Aromatase inhibitors GnRH Agonists/LHRH agonists Antiandrogens
126
What are the antiestrogens?
Tamoxifen Toremifene Raloxifene
127
What are the aromatase inhibitors?
Anastrozole Letrozole Exemestane
128
What are the GnRH/LHRH agonists?
Leuprolide Gosereline Triptorelen
129
What are the antiandrogens?
Flutamide Nilutamide Bicalutamide Enzalutamide
130
What is the MOA of antiestrogens?
Blocks estrogen receptor Blocking estrogen stimulation of hormone sensitive tumors Raloxifene with some proestrogenic effects
131
What are the AEs of antiestrogens?
Hot flashes N/V Thromboembolic events
132
What is the MOA of aromatase inhibitors?
Inhibits enzyme that converts androgen to estrogens
133
What are the AEs of aromatase inhibitors?
Hot flashes Fatigue Bone/joint pain Decreased bone density
134
What is the MOA of GnRH/LHRH agonists?
Feed back to pituitary to decrease release of FSH and LH
135
What are the AEs of GnRH/LHRH agonists?
``` Tumor flare (initially) Hot flashes Gynecomastia Decreased bone density Injection site pain Decreased libido ```
136
What is the MOA of antiandrogens?
Testosterone receptor blocker
137
What are the AEs of antiandrogens?
Hot flashes Gynecomastia Increased LFTs Blurred vision (nilutamide)
138
What is the MOA of hydroxyurea?
Ribonucleoside diphosphate reductase inhibitor
139
What is the MOA of L-Asparaginase pegasparaginase?
Inhibits protein synthesis by hydrolyzing asparagine to aspartic acid and ammonia
140
What is the MOA of arsenic trioxide?
Damages/degrades the PML-RAR alpha fusion protein
141
What is PML-RAR?
Promyelocytic leukemia-retinoin acid receptor
142
What is the MOA of tretinoin (ATRA)
Induces differentiation of acute promyelocytic leukemia cells
143
What are the AEs of hydroxyurea?
Myelosuppression Mucositis Hepatotoxicity Renal toxicity
144
What are the AEs of L-asparaginase pegasparaginase?
Hypersensitivity Hyperglycemia Pancreatitis
145
What are the AEs of arsenic trioxide?
``` QT prolongation Peripheral neuropathy Hyperglycemia Musculoskeletal pain "Retinoic acid syndrome" ```
146
What are the AEs of tretinoin (ATRA)?
``` Peripheral edema Edema Skin dryness RAsh Leukocytosis "Retinoic acid syndrome" ```
147
How is hydroxyurea used in sickle cell anemia?
Reduces painful crises
148
How is hydroxyurea used in leukemias?
Reduces malignant cell counts
149
What baseline labs should be taken prior to start of arsenic trioxide?
EKG | Electrolytes
150
What vitamin is tretinoin an analogue of?
Vitamin A

Heme/Onc (20 decks)

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