[3RD YEAR] PH 119 - Pharmacology 2 (Lec) > FINAL 07 - Anticancer Agents > Flashcards

FINAL 07 - Anticancer Agents Flashcards

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1
Q

inCovalently bind to DNA → cross-linking → inhibition of replication and transcription; non-cell-cycle specific (Anticancer agents)

A

Alkylating agents

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2
Q

Cyclophosphamide, Ifosfamide, Busulfan, Carmustine (nitrosoureas), Temozolomide (Anticancer agents)

A

Alkylating agents

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2
Q

Cyclophosphamide, Ifosfamide, Busulfan, Carmustine (nitrosoureas), Temozolomide (Anticancer agents)

A

Alkylating agents

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3
Q

____________ requires activation in liver (prodrug) (Alkylating agents)

A

Cyclophosphamide

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3
Q

__________ cross the blood-brain barrier (Alkylating agents)

A

Nitrosoureas

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4
Q

Cornerstone in breast cancer, lymphoma (Alkylating agents)

A

Cyclophosphamide

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5
Q

For sarcoma, testicular cancer (Alkylating agents)

A

Ifosfamide

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6
Q

First line for glioblastoma (Alkylating agents)

A

Temozolomide

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7
Q

Conditioning before stem cell transplant (hematologic malignancies) (Alkylating agents)

A

Busulfan

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8
Q

S/E is __________ (cyclophosphamide/ifosfamide) (Alkylating agents)

A

Hemorrhagic cystitis

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9
Q

Drug for hemorrhagic cystitis caused by cyclophosphamide/ifosfamide (Alkylating agents)

A

Mesna (Sodium 2-mercapto ethane sulfonate)

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10
Q

Cross-link DNA (similar to alkylators) (Anticancer agents)

A

Platinum compounds

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11
Q

Cisplatin, carboplatin, oxaliplatin (Anticancer agents)

A

Platinum compounds

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12
Q

____________, __________, and __________ are used for solid tumors (lung, ovarian, colon) (Platinum compounds) (CCO)

A

Cisplatin, Carboplatin, Oxaliplatin

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13
Q

Highly emetogenic (Platinum compounds)

A

Cisplatin

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14
Q

Peripheral neuropathy exacerbated by cold (Platinum compounds)

A

Oxaliplatin

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15
Q

Ifosfamide and nitrosoureas cause __________ as S/E (Alkylating agents)

A

CNS toxicity

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16
Q

S/E of cisplatin is nephrotoxicity (use __________ and __________) and ototoxicity (Platinum compounds) (HA)

A

Hydration, Amifostine

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17
Q

Less nephrotoxic (Platinum compounds)

A

Carboplatin

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18
Q

Interfere with nucleotide synthesis; S-phase specific (Anticancer agents)

A

Antimetabolites

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19
Q

Methotrexate is a __________ (Antimetabolites)

A

Folate antagonist

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20
Q

5-fluorouracil (5-FU) and capecitabine are __________ (Antimetabolites)

A

Pyrimidine analogs

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21
Q

6-mercaptopurine and 6-thioguanine are __________ (Antimetabolites)

A

Purine analogs

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22
Q

Used for breast cancer, lymphoma, osteosarcoma (Antimetabolites)

A

Methotrexate

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23
Used for GI cancers (colorectal, pancreatic) (Antimetabolites) (5C)
5-FU, Capecitabine
24
Used for acute leukemias (Antimetabolites) (C66)
Cytarabine, 6-MP, 6-TG
25
Methotrexate toxicity is reversible with __________ (Antimetabolites)
Leucovorin rescue
26
5-FU is potentiated by ___________ (Antimetabolites)
Leucovorin
27
High-dose __________ requires hydration and urine alkalization (Antimetabolites)
Methotrexate
28
__________ testing is done before 6-MP (Antimetabolites)
TPMT
29
Disrupt microtubules → mitotic arrest (M phase) (Anticancer agents)
Antimicrotubule agents
30
Prevent formation (Antimicrotubule agents) (VV)
Vincristine, Vinblastine
31
Vincristine and vinblastine are __________ (Antimicrotubule agents)
Vinca alkaloids
32
Paclitaxel and docetaxel are __________ (Antimicrotubule agents)
Taxanes
33
Prevent disassembly (Antimicrotubule agents) (PD)
Paclitaxel, Docetaxel
34
Used for lymphoma and leukemia (Antimicrotubule agents) (VV)
Vincristine, Vinblastine
35
Used for ovarian and lung cancers (Antimicrotubule agents) (PD)
Paclitaxel, Docetaxel
36
Is neurotoxic (Antimicrotubule agents)
Vincristine
37
Is more myelosuppressive (Antimicrotubule agents)
Vinblastine
38
Has hypersensitivity reactions (Antimicrotubule agents)
Paclitaxel
39
__________ can cause peripheral neuropathy (Antimicrotubule agents)
Vincristine
40
Give __________ premedication for taxanes (Antimicrotubule agents)
Dexamethasone
41
Avoid intrathecal __________ because it can be fatal (Antimicrotubule agents)
Vincristine
42
Interfere with topoisomerase enzymes → DNA damage (Anticancer agents)
Topoisomerase inhibitors
43
Topotecan and irinotecan inhibits __________ (Topoisomerase inhibitors)
Topoisomerase I
44
Etoposide inhibits __________ (Topoisomerase inhibitors)
Topoisomerase II
45
__________ can cause diarrhea (use loperamide or atropine) (Topoisomerase inhibitors)
Irinotecan
46
__________ and __________ can cause colorectal and lung cancer, and lymphoma (Topoisomerase inhibitors) (IE)
Irinotecan, Etoposide
47
Intercalate DNA, inhibit topoisomerase II, generate ROS (Anticancer agents)
Anthracyclines
48
Cardiotoxicity is dose-limiting; red urine (benign) (Anticancer agents)
Anthracyclines
49
Doxorubicin, Daunorubicin, Epirubicin (Anticancer agents)
Anthracyclines
50
Use __________ as cardioprotection (Anthracyclines)
Dexrazoxane
51
__________ and __________ are used for breast cancer and lymphoma (Anthracyclines) (DE)
Doxorubicin, Epirubicin
52
Inhibit intracellular signaling (Anticancer agents)
Tyrosine kinase inhibitors (TKIs)
53
Imatinib (CML-BCR-ABL), Erlotinib, Gefitinib (EGFR), Sunitinib, Sorafenib (VEGFR) (Anticancer agents)
Tyrosine kinase inhibitors (TKIs)
54
S/Es include CYP3A4 interactions, hepatotoxicity, rash, and QT prolongation (Anticancer agents)
Tyrosine kinase inhibitors (TKIs)
55
Enzymes that transfer a phosphate group (from ATP) to the tyrosine resides of proteins
Tyrosine kinases (TKs)
56
Enzymes responsible for cell signaling (cell growth, proliferation, differentiation, angiogenesis, apoptosis/inhibition)
Tyrosine kinases (TKs)
57
Are engineered proteins that bind specific antigens, often on tumor cells or in the tumor microenvironment, to kill or suppress cancer by various mechanisms (Anticancer agents)
Monoclonal antibodies (mAbs)
58
Trastuzumab (HER2), Rituximab (CD20), Bevacizumab (VEGF) (Anticancer agents)
Monoclonal antibodies (mAbs)
59
S/Es include infusion reactions (Anticancer agents)
Monoclonal antibodies (mAbs)
60
Risk of HBV reactivation (Monoclonal antibodies)
Rituximab (CD20)
61
Risk of cardiotoxicity (Monoclonal antibodies)
Trastuzumab
62
Risk of bleeding, GI perforation, HTN (Monoclonal antibodies)
Bevacizumab
63
Risk of hypomagnesemia (Monoclonal antibodies)
Cetuximab
64
Block inhibitory pathways that normally dampen T-cell responses, thereby enhancing the immune system's ability to recognize and destroy tumor cells (Anticancer agents)
Immune checkpoint inhibitors
65
Nivolumab, Pembrolizumab (PD-1), Atezolizumab (PD-L1), Ipilimumab (Monoclonal antibodies)
Immune checkpoint inhibitors
66
S/Es include immune-related adverse events: colitis, hepatitis, endocrinopathies (Anticancer agents)
Immune checkpoint inhibitors
67
Immune checkpoint inhibitors require __________ for severe reactions (Monoclonal antibodies)
Corticosteroids
68
-nib (e.g., imatinib, erlotinib) (Small molecule inhibitors or monoclonal antibodies)
Small molecule inhibitors
69
Small molecule type (Small molecule inhibitors or monoclonal antibodies)
Small molecule inhibitors
70
Inhibits intracellular enzymes (mainly kinases) (Small molecule inhibitors or monoclonal antibodies)
Small molecule inhibitors
71
Target location is inside the cell (cytoplasmic/nuclear) (Small molecule inhibitors or monoclonal antibodies)
Small molecule inhibtors
72
Example targets include tyrosine kinases (EGFR, BCR-ABL, VEGFR) (Small molecule inhibitors or monoclonal antibodies)
Small molecule inhibitors
73
Oral route (Small molecule inhibitors or monoclonal antibodies)
Small molecule inhibitors
74
Fast onset of action (short half-life) (Small molecule inhibitors or monoclonal antibodies)
Small molecule inhibitors
75
Daily dosing frequency (Small molecule inhibitors or monoclonal antibodies)
Small molecule inhibitors
76
S/Es include skin rash, diarrhea, hepatotoxicity (Small molecule inhibitors or monoclonal antibodies)
Small molecular inhibitors
77
Hepatic/renal clearance (Small molecule inhibitors or monoclonal antibodies)
Small molecule inhibitors
78
Ends in -nib = "inibitor" (Small molecule inhibitors or monoclonal antibodies)
Small molecular inhibitors
79
-mab (e.g., trastuzumab, rituximab) (Small molecule inhibitors or monoclonal antibodies)
Monoclonal antibodies
80
Large protein type (antibody) (Small molecule inhibitors or monoclonal antibodies)
Monoclonal antibodies
81
Binds to extracellular targets (receptors or antigens) (Small molecule inhibitors or monoclonal antibodies)
Monoclonal antibodies
82
Target location is outside the cell or on cell surface (Small molecule inhibitors or monoclonal antibodies)
Monoclonal antibodies
83
Example targets include EGFR, HER2, CD20, PD-1, VEGF (Small molecule inhibitors or monoclonal antibodies)
Monoclonal antibodies
84
IV/SC (parenteral) route (Small molecule inhibitors or monoclonal antibodies)
Monoclonal antibodies
85
Slower onset of action (longer half-life) (Small molecule inhibitors or monoclonal antibodies)
Monoclonal antibodies
86
Weekly dosing or every 2-4 weeks (Small molecule inhibitors or monoclonal antibodies)
Monoclonal antibodies
87
S/Es include infusion reactions, immune-mediated AEs (Small molecule inhibitors or monoclonal antibodies)
Monoclonal antibodies
88
Reticuloendothelial system (RES) clearance (Small molecule inhibitors or monoclonal antibodies)
Monoclonal antibodies
89
Ends in -mab = "monoclonal antibody" (Small molecule inhibitors or monoclonal antibodies)
Monoclonal antibodies
90
Blocks hormone production or receptors in hormone-sensitive tumors (Anticancer agents)
Hormonal agents
91
ER modulator-breast (Hormonal agents)
Tamoxifen
92
Aromatase inhibitor (Hormonal agents)
Anastrozole
93
Androgen receptor blocker (Hormonal agents) (FB)
Flutamide, Bicalutamide
94
GnRH agonist (Hormonal agents)
Leuprolide
95
Risk of endometrial cancer, DVT (Hormonal agents)
Tamoxifen
96
Risk of osteoporosis (Hormonal agents)
Aromatase inhibitors
97
Risk of tumor flare initially (Hormonal agents)
Leuprolide
98
Generates free radicals → DNA strand breaks; pulmonary fibrosis risk (Miscellaneous anticancer agents)
Bleomycin
99
Depletes asparagine → leukemic cells die; risk of hypersensitivity, pancreatitis, coagulopathy (Miscellaneous anticancer agents)
Asparaginase
100
Risk of pulmonary fibrosis (Chemo man) (BB)
Bleomcyin, Busulfan
101
Risk of nephrotoxicity and ototoxicity (Chemo man) (CC)
Cisplatin, Carboplatin
102
Risk of cardiotoxicity (Chemo man)
Doxorubicin
103
Risk of myelosuppression (Chemo man) (M5)
Methotrexate, 5-fluorouracil
104
Risk of neurotoxicity (crosses BBB) (Chemo man)
Nitrosoureas (Lomustine, Carmustin)
105
Risk of hemorrhagic cystitis (Chemo man)
Cyclophosphamide
106
Risk of peripheral neuropathy (Chemo man) (TV)
Taxanes (Paclitaxel, Docetaxel), Vinca alkaloids (Vincristine > Vinblastine)
[3RD YEAR] PH 119 - Pharmacology 2 (Lec)
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