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Skin Lymph Blood Exam 2 > Cancer Pharmocology - Dr. Kruse > Flashcards

Cancer Pharmocology - Dr. Kruse Flashcards

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1
Q

p-Glycoprotein (PGP) (MDR1)

A

linked to resistance if a cell type has this expressed

  • primary or natural resistance if expressed
  • acquired resistance if overexpressed
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2
Q

tumor supressors act on

A

G2

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3
Q

oncogenes act on

A

G1

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4
Q

as tumor spreads more reason its harder to cure

A

it takes up more of the organs
it slows its division rate because there are less BVs available to take over for nutrients
= chemotherapy drugs cant effectively target the cancer calls now since they arent as fast replicating

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5
Q

how to over come the BBB

A

intrathecal, intracavity, intra….

IMPLANTABLE WAFER coated with Carmustine = radiation constant in high grade malignant glioma

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6
Q

Alkalizing drugs can be toxic and cause what new cancers

A

ALL and AML

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7
Q

chemotherapy usually caues what common side effects

A 
hair loss
oral mucosa destruction
sperm forming cell destruction 
GI cell destruction 
BM destruction
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8
Q

Hematopoietic agents

A

prevents or decreases the neutropenia, thrombocytopenia, and anemia

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9
Q

Seratonin receptor agonist

A

prevents or decreases the Nausea Vomiting (Zophran)

also called Ondansetron

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10
Q

Bioohosphates

A

delay skeletal complications

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11
Q

Akylating agents do what

A

bind to DNA esp Guanines and cause cross linking between then to prevent DNA uncoiling = no DNA replication or check points

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12
Q

Cyclophosphamide side effects and what class of drugs

A

most used akylating agent and causes the most N/V

** Hemorrhagic cystits** = from Acrolein side product

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13
Q

Akylating agents include what 6 drugs and cell cycle

A
  1. Cyclophosphamide
  2. Carmustine
  3. Busulfan
  4. Procarbazine
  5. Dacarbazine
  6. Cisplatin

Cell cycle : nonspecific

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14
Q

How to activate Cyclophosphamide

A

CYP450 2B

this makes Acrolein + Phosphate mustard

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15
Q

how to elliminate Side effects of cyclophosphamide

A

MESNA : inhibits Acrolein to avoid hemorrhagic cystitis

SERATONIN : to prevent N/V

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16
Q

Cisplatin side effect

A

renal tubular damage, ototoxicity

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17
Q

Busulfan side effects

A

pulmonary fibrosis

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18
Q

Antimetabolites do what

A

block metabolited for DNA replication

- effects S phase

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19
Q

Antimetabolites 3 drugs and cell cycle

A
  1. Folic acid analog : methotraxate + Leucovorin
  2. Pyrimidine analog : 5-fluorouracil
  3. Purine analog : 6- mercaptopurine (6-MP)

Cell cycle : S-phase specific

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20
Q

Methotrexate needs what and for what reason

A
  1. low dose Leucovorin rescue
    = rescues the normal cells that absorb it at low levels (not cancer cells that dont absorb anything at low levels
    = high dose methotrexate (cancer cells absorb it even the more resistant ones, so they die)
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21
Q

Methotrexate side effects

A

mucosal ulceration

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22
Q

Methotrexate does what MOA

A

Blocks dihydrofolate reductase = no dTMP —-> dTTP made

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23
Q

what does leucovorin do specifically

A

gives N5N10 methylene FH4 that allows call to still make dTMP —-> dTTP

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24
Q

Methotrexate is used for what

A

psoriasis - immune supressor
RA - immune supressor
Cancer treatment

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25
Fluorouracil is what active compund and what is the MOA
FdUMP = active compound | it binds to thymidylate synthase and blocks dTMP being made which later becomes dTTP
26
Fluorouracil does what to DNA
alters the Uracil and how it is made
27
Mercaptopurine (6-MP) active form and metabolized form
HGPRT : makes monophosphate nucleotide 6-thioinsinic acid | Xanthinie oxidase : makes 6-thiouric acid
28
Mercaptopurine (6-MP) used for what and side effect
acute leukemias | Tumor Lysis Syndrome causing hyperuricemia
29
Drug to prevent Mercaptopurine (6-MP) side effects
Allopurinol : inhibits xanthine oxidase | **** can cause build up of 6-Thiouric acid toxic so must be given with small amounts of 6MP to control this****
30
allopurinol tx what
gout | toxic lysis syndrome hyperuricemia
31
Antineoplastic agents are from what
bacteria or plants agents
32
Antineoplastic agents 6 drugs
1. Vinca alkaloids : Vinblastine + Veincristine 2. Taxanes : Pacitaxel 3. Epipodophyllotoxins : Etoposide 4. Antibiotics : Doxorubicin 5. Anthracenedione : Bleomycin 6. Enzymes : L-Asparaginase
33
Vinblastine + Veincristine MOA cell cycle
binds to B-tubulin and inhibits microtubule assembly or deporlaization (casues aggregation of the tubulin dimers) M-phase only
34
Vinblastine + Veincristine side effects which one has more of what
Vinblastine : more BM myelosuppression Veincristine : more neurologic toxicites (numbness and tingling, XDTR, motor weakness) COMMON TO BOTH : alopecia, BM depression
35
Taxanes MOA cell cycle
Binds to B-tubulin to inhibit shortening of it by stabilizing microtubules, no divisions in cells M-phase
36
Paclitaxel side effects
Hypersensitivity hands toes, change in taste
37
Docetaxel side effects and difference compared to Pacitaxel
smaller dose needed and less side effects, longer half-life | hypersensitivity, neutropenia, hair loss
38
Paclitaxel and Docetaxel is made for what
breast cancer
39
Topoisomerase 1 Topoisomerase 2 MOA
1. cuts 1 strand of the DNA , relax strand, reattach it 2. cutes both strands of DNA and coils and uncoils and supercoils X topoisomerases = cell death
40
Camptothecins
topotecan, irinotecan = inhibits topisomerase 1
41
Epipodophyllotoxins
etoposide, teniposide = inhibits topoisomerase 2
42
Camptothecins and Epipodophyllotoxins | cell cycle
mainly phase S, some G1/G2
43
Antitumor antibiotics 3 drugs
1. Anthracyclines (doxorubicin) 2. Bleomycin 3. Dactinomycin
44
Anthracyclines (doxorubicin) MOA cell cycle
inhibits topoisomease 2 + DNA intercalaltion | nonspecific cell cycle + specific
45
Anthracyclines (doxorubicin) side effects
accumulation of free radicals | = dysrhythmias and heart failure
46
Bleomycin | MOA
single and double strand DNA breaks
47
Bleomycin side effects
some myelosuppression | ** Pulmonary toxcicity (pneumonitis sx, cough, dyspnea, dry crackels)
48
Dactinomycin MOA
DNA intercalation
49
Asparaginase and pegaspargase | is used for what
ALL , targeted therapy by X asparagine to ALL cells which dont have asparaginie synthase enzyme
50
Asparaginase and pegaspargase MOA cell cycle
hydrolyze L-asparagine ----> aspartic acid + ammonia = inhibit protein synthesis Cell Cycle : G1 phase
51
Asparaginase and pegaspargase | side effects
acute hypersensitivity*, fevers, chills, N/V, skin rash , urticaria (clotting and bleeding problems, pancreatitis, CNA toxic)
52
imatinib | for what and does what
9:22 CML | inhibits the ABL TK, RTK, PDGFR, KIT
53
Erlotinib and Gefitinib does what and for what
TK ibhibitor of the EGFR | non-small cell lung cancer, pancreatic cancer
54
Erlotinib and Gefitinib side effects
dermatologic toxicites : skin rash that looks like roscea or acne
55
Ziv -aflibercept does what and MOA
TK + GF receptor inhibitor = VEGFR 1 VEGFR 2 bind to IgG1 (Fc part) = no VEGFR signaling
56
VEGFR signaling pathways is for what
VEGF-A VEGF-B, PIGF (placental GF)
57
Ziv -aflibercept resistance can for how side effects
Point mutations on the drug binding site | N/V, Acneform skin rash + hypersensitivity (allergic reaction)
58
IL 2 INF-a2a, INF-a2b WHAT and side effects
IL2 : increase CTL, NK cells (can cause capillary leak syndrome) INF-2 : inhibits cell growth, M, Lymphocytes, (can cause BM depression, Neutropenia, anemia, renal toxic, edema, arrhythmia)
59
Rituximab
CD20 Non-Hodgkins X proloferation and differentiation
60
Alemtuzumab
CD52 | CLL
61
Gemtuzumab
CD33 | AML
62
Trastuzumab
HER2/neu breast Tyrosine Kinase
63
Cetuximab
EGFR (ErbB-1) Colorectal, lung, pancreatic, breast Tyrosine Kinase
64
Bevacizumab
VEGF colorectal, lung Angiogenesis
65
Ibritumomab + Tositumomab
CD20 Non-Hodgkins Proliferation and Differentiation
66
Melanoma 3 most active cytotoxic agents to give for it and response
Dacarbazine Temozolomide cisplatin = slow response rare
67
Melanoma is most effectively tx by and this is not a widely used thing that is approved
immunostimulation (IL2, INF2) higher response rate
68
Melanoma TX most effective approved
Nivolumab + pembrolizumab = when melanoma is not resectable and metastatic
69
mutation in most melanomas and 3 drugs against it
BRAF V600E (BARK kinase) 1. Vemurafenib 2. dabrafenib 3. encorafenib
70
Side effect one word : Methotrexate, melphalan
Mucositis
71
Side effect one word : Bleomycin, busulfan
Pulmonary fibrosis
72
Side effect one word : Vincristine
Peripheral neuropathy
73
Side effect one word : Cisplatin
Ototoxicity
74
Side effect one word : Doxorubincin, daunorubicin
Cardiotoxicity
75
Side effect one word : Cisplatin, cyclophosphamide
Nephrotoxicity
76
Side effect one word : Cyclophosphamide, ifosfamide
Hemmorrhagic cyctitis

Skin Lymph Blood Exam 2 (9 decks)

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