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Concepts in Pathology and Tissue Morphology > Antineoplastic pharmacology > Flashcards

Antineoplastic pharmacology Flashcards

1
Q

Mechanism of action of 5-FU

A

Inhibit thymidylate synthetase

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2
Q

Drug that causes acute hemorrhagic cystitis

A

Cyclophosphamide

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3
Q

Drug that is cell cycle specific, acting specifically in mitotic phase

A

Paclitaxel

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4
Q

Cardiotoxicity limits total administration of

A

Adriamycin

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5
Q

Drug that doesn’t suppress bone marrow

A

Bleomycin

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6
Q

Kinase inhibitors

A

Imatinib (gleevec)
Nilotinib
Dasatinib

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7
Q

Antibody against EGFR-HER2 receptor

A

Trastuzuma (herceptin)

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8
Q

Antibody against VEGF

A

Bevacizumab (avastin)

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9
Q

Checkpoint inhibitors

A

Ipilimumab (yervoy)

Nivolumab (opdivo)

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10
Q

Inhibit angiogenesis by blockin VEGF and bFGF

A

Thalidomide

Lenalidomid

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11
Q

Proteosome inhibitors

A

Bortezamib (velcade)

Carfilzomib

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12
Q

Alkylating agents

A 
Mechlorethamine
Cyclophosphamide
Busulfan
Carmustin
Cisplatin
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13
Q

Binds dsDNA containing guanosine, intercalates, and generates free radicals

A

Actinomycin D

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14
Q

Intercalated quinone redox center that binds Fe++ and oxidized to Fe+++ ->superoxides

A

Adriamycin

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15
Q

Glycopeptide that intercalates and generates free radicals

A

Bleomycin

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16
Q

Inhibitors of topoisomerase II

A

Etoposide

Teniposide

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17
Q

Inhibitor of topoisomerase I

A

Irinotecan

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18
Q

Imatinib (gleevec) is used frequently for

A

Ph+ CML and AML

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19
Q

Metabolism of imatinib (gleevec)

A

CYP3A4

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20
Q

Drugs that Compete with imatinib for CYP3A4 metabolism

A

Warfarin

Grapefruit juice

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21
Q

Drugs that induce CYP3A4 metabolism and affect imatinib administration

A

Phenytoin

St. John’s wort

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22
Q

Side effects of imatinib

A 
Nvd
Skin rxns
Hepatotoxicity
Htn
Myelosuppression
Edema
CHF
Musculoskeletal pain
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23
Q

Side effects of trastuzumab (herceptin)

A 
Nvd
Rigors
Infusion rxns
Cardiac dysfunction
CHF
Hypotension
Edema
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24
Q

Uses for bevacizumab (avastin)

A

Colon cancer, vasculopathy

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25
Checkpoint inhibitor that is an MAB against CTLA4 on T cells
Ipilimumab (yervoy) | *CTLA4 = cyctotoxic t lymphocyte associated protein 4
26
Uses for ipilimumab (yervoy)
Melanoma NSCLC Hodgkins lymphoma
27
Checkpoint inhibitor that is an MAB against PD-1 on some NK cells
Nivolumab (opdivo) | PD-1=programmed death receptor
28
Drug that can cause significant incidence of secondary leukemias
Etoposide and teniposide
29
Toxicity from checkpoint inhibitors prominently includes
Autoimmunity
30
Chimeric antigen receptor (CAR) T cell can be used for
Cancer and autoimmune | Subsets of treatment resistand cancers
31
Uses for angiogenesis inhibitors - thalidomide and lanalidomide
Causes direct growth arrest in multiple myeloma cells
32
Side effects of thalidomide
Teratogenic | Peripheral neuropathy
33
Side effects of lanalidomide
Teratogenic Peripheral neuropathy Neutropenia Thromboembolism
34
Boron containing 26S proteasome inhibitor
Boretezamib
35
Bortezamib mechanism
Disregulates turnover of proteins mediating cell cycle (cyclins, p53) ER stress -> apoptosis
36
Metabolism of bortezamib
CYP3A4
37
Uses of bortezamib (velcade)
Mutliple myeloma and mantle cell lymphoma
38
What is dose limiting toxicity of bortezamib (velcade)
Peripheral neuropathy
39
Drug that has extremely low therapeutic index ~1
Bortezamib (velcade)
40
Mechlorethamine mechanism
Alkylating agent | Form covalent adducts across DNA strands
41
Administration of mechlorethamine (alkylating agent)
Iv infusion near tumor site
42
Administration of cyclophosphamide (alkylating agent)
Oral -> wide distribution
43
Elimination of cyclophosphamide (alkylating agent)
Urine (active alkylator and metabolites)
44
Toxicities of cyclophosphamide
Classical toxicities + myocarditis and hemorrhagic cystitis
45
Use of cyclophosphamide (alkylating agent)
Hematogenous tumors
46
Administration of actinomycin d
IV
47
Elimination of actinomycin d
Bile and urine - unchanged
48
Uses of actinomycin d
Choriocarcinoma, wilms tumor, testicular tumors, karposis sarcoma
49
Administration and distribution of adriamycin
IV; wide except CNS
50
Elimination of adriamycin
Bile
51
Metabolism of adriamycin
Liver
52
Toxicities of adriamycin
Classical toxicities + adriamycin cardiotoxicity
53
Administration of bleomycin
Iv or IM
54
Use of bleomycin
Lymphoma, germ cell cancers, head/neck cancer
55
Folic acid analog
Methotrexate
56
Inhibits dihydrofolate reductase
Methotrexate
57
What cant be synthesiaed due to methotrexate
Thymidine | Tetrahydrofolate
58
Dose limiting toxicity of purine analogs (ie 6-MP)
Myelosuppression
59
6-MP blocks synthesis of
ATP and GTP
60
Metabolism of 6-MP (purine analog)
Tissue xanthine oxidase and thiopurine methyltransferase
61
6-MP has a reaction with
Allopurinol
62
5-FU inhibits
Thymidylate synthetase
63
Effects of 5-FU enhanced by
Leukovorin
64
Drug that can be used topically for basal cell carcinoma
5-FU
65
Toxicities of 5-FU
Classical toxicities + CNS (ataxia, confusion)
66
Drugs that bind to tubulin and disaggregate mitotic spindles -> metaphase arrest
Vinca alkaloids: vincristine, vinblastine
67
Drug that binds tubulin and stabilized microtubules -> metaphase arrest
Taxol (paclitaxel)
68
Estrogen agonist
Estradiol
69
Estrogen antagonist
Tamoxifen
70
Androgen agonist
Danazol
71
Androgen antagonist
Flutamide
72
GnRH agonist
Leuprolide
73
GnRH antagonist
Degarelix
74
Drugs that can be used for reversible chemical orchiectomy or oophorectomy
Leuprolide (GnRH agonist) | Degarelix (antagonist)
75
Aromatase inhibitors
Anastrazole, letrozole, vorozole
76
Mechanism of aromatase inhibitors
Prevent generation of estrogens from androgens | More effective than tamoxifen

Concepts in Pathology and Tissue Morphology (10 decks)

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