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Pharmacology 2 > Cytotoxic Chemo > Flashcards

Cytotoxic Chemo Flashcards

1
Q

Growth Fraction

A

Proportion of cells in a tumor that are actively dividing

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2
Q

2 common toxicities of Topotecan/Irinotecan

A

Myelosuppression and Diarrhea

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3
Q

2 Purine Antimetabolites

A

6-MP and 6-GT

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4
Q

4 Plant Alkyloids

A

(1) Vin-‘s; (2) -side’s; (3) -can’s; (4) -taxel’s

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5
Q

5 Alkylating Agents

A

Cyclophosphamide, Mechlorethamine, Platinum Analogs, Procarbazine, Busulfan

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6
Q

5 Antibiotics for Chemotherapy

A

(1) Doxorubicin/Daunorubicin; (2) Bleomycin; (3) Dactinomycin; (4) Mitomycin

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7
Q

6 Antimetabolites

A

Methotrexate, 6-MP and 6-TG, 5-FU, Cytarabine, Gemcitabine

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8
Q

Acrolein is breakdown product of what

A

Cyclosphosphamide

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9
Q

Administration of Vinca Alkyloids

A

Parenterally

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10
Q

Alkylating agents: CCNS or CCS?

A

CCNS

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11
Q

Anthracyclines

A

Doxorubicin, Daunorubicin

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12
Q

Anthracyclines (-rubicin): CCS or CCNS?

A

CCNS

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13
Q

Anticancer drugs kill a fixed proportion of tumor cell populatino

A

Log-Kill Hypothesis

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14
Q

Antimetabolites: CCNS or CCS?

A

CCS, primarily S phase

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15
Q

Binds to dsDNA and inhibits DNA-dependent RNA synthesis

A

MOA of Dactinomycin

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16
Q

Bleomycin toxicities

A

Pneumoitis, Pulmonary Fibrosis, Alopecia

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17
Q

Bleomycin: CCS or CCNS?

A

CCS: G2 phase

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18
Q

Block formation of mitotic spindle by preventing assembly of tubulin dimers into microtubules

A

MOA of Vinca Alkyloids

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19
Q

Cisplatin toxcitities

A

Nephrotoxicity, Ototoxicity, Myelosuppression

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20
Q

Class with Cardiotoxicity

A

Anthracyclines (-rubicins)

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21
Q

Clearance of Vinca Alkyloids

A

Bililary Excretion

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22
Q

Concurrent Agent for 5-FU

A

Leucovorin (Enhanced action)

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23
Q

Concurrent Agent for 6-MP

A

Allopurinol (increases toxicity!)

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24
Q

Concurrent Agent for Anthracyclines

A

Dexroxazone (Fe chelator, reduced cardiotoxicity)

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25
Q

Concurrent Agent for Cisplatin

A

Amifostine (Cytoprotection)

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26
Q

Concurrent Agent for Cyclophosphamide

A

Mesna (protect against Acrolein production)

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27
Q

Concurrent Agent for MTX

A

Luecovorin (Metabolic rescue)

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28
Q

Concurrent Agent for Tumor Lysis Syndrome

A

Allopurinol

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29
Q

Concurrent Agents for Bone Mets

A

Pamidronate, Zoledronate (reduced bone pain and fractures)

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30
Q

Dactinomycin: CCS or CCNS?

A

CCNS

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31
Q

Deoxycytidine analog that inhibits ribonucleotide reductase –> Diminishes pool of deoxyribonucleoside triphosphates for DNA synthesis

A

MOA of Gemcitabine

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32
Q

Distinctive adverse effect of Anthracyclines

A

Cardiotoxicity

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33
Q

Dose Limiting Toxicity of 6-MP and 6-GT

A

Bone Marrow Suppression

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34
Q

Drug that causes blisters on contact with tissues

A

Vesicant

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35
Q

Elimination of Etoposide

A

Renal

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36
Q

First-Order Kinetics

A

A given dose kills a constant proportion of a cell population rather than a constant number of cells

37
Q

Forms H2O2, which generates free radicals and causes DNA strand scission

A

Procarbazine

38
Q

General MOA of Cyclophosphamide

A

Alkylating Agent

39
Q

General MOA of Mechlorethamine

A

Alkylating Agent

40
Q

General MOA of Platinum Agents

A

Alkylating Agents

41
Q

How can you reduce toxicity of Methotrexate

A

Folinic Acid (Leucovorin)

42
Q

In what phase to Vinca Alkyloids work

A

M Phase

43
Q

Increases degradation of DNA and inhibits mitochondrial ETC

A

MOA of Etoposide/Teniposide

44
Q

Inhibit Topo 1

A

MOA of Topotecan/Irinotecan

45
Q

Inhibits Thymidylate Synthase and leads to “thymineless death” of cells

A

5-FU

46
Q

Kinetics of Cytotoxic drugs

A

First-Order Kinetics

47
Q

Leucovorin Rescue

A

Reduce toxic effects of Methotrexate by administration of Folinic Acid (Leucovorin)

48
Q

Log-Kill Hypothesis

A

Anticancer drugs kill a fixed proportion of tumor cell populatino

49
Q

Main toxicity of Gemcitabine

A

Myelosuppression

50
Q

Main use of Daunorubicin

A

Acute Leukemias

51
Q

Methotrexate clearance is dependent on

A

Renal function

52
Q

Mitomycin: CCS or CCNS?

A

CCNS

53
Q

MOA of 5-FU

A

Inhibits Thymidylate Synthase and leads to “thymineless death” of cells

54
Q

MOA of 6-GT

A

Purine Antimetabolite

55
Q

MOA of 6-MP

A

Purine Antimetabolite

56
Q

MOA of Bleomycin

A

Generates free radicals

57
Q

MOA of Cytarabine (ARA-C)

A

Pyrimidine antimetabolite

58
Q

MOA of Dactinomycin

A

Binds to dsDNA and inhibits DNA-dependent RNA synthesis

59
Q

MOA of Doxorubicin/Daunorubicin

A

Intercalate b/t base pairs, Inhibit Topo 2, Generate free radicals

60
Q

MOA of Etoposide/Teniposide

A

Increases degradation of DNA and inhibits mitochondrial ETC

61
Q

MOA of Gemcitabine

A

Deoxycytidine analog that inhibits ribonucleotide reductase –> Diminishes pool of deoxyribonucleoside triphosphates for DNA synthesis

62
Q

MOA of Mitomycin

A

Alkylating agent that cross-links DNA

63
Q

MOA of Paclitaxel/Docetaxel (Taxanes)

A

Prevent microtubule disassembly in mitotic spindle

64
Q

MOA of Procarbazine

A

Forms H2O2, which generates free radicals and causes DNA strand scission

65
Q

MOA of Topotecan/Irinotecan

A

Inhibit Topo 1

66
Q

MOA of Vinca Alkyloids

A

Block formation of mitotic spindle by preventing assembly of tubulin dimers into microtubules

67
Q

Of all the antimetabolites, __ is most specific for S phase

A

Cytarabine

68
Q

Prevent microtubule disassembly in mitotic spindle

A

MOA of Paclitaxel/Docetaxel

69
Q

Primary use of Procarbazine

A

Hodgkin’s Lymphoma

70
Q

Proportion of cells in a tumor that are actively dividing

A

Growth Fraction

71
Q

Purine antimetabolites are used mainly in

A

Acute Leukemias and Chronic Myelocyte Leukemia

72
Q

Pyrimidine antimetabolite

A

Cytarabine

73
Q

Resistance to 5-FU

A

Decreased activation of 5-FU, Increased Thymidylate Synthase activity, Reduced drug sensitivity

74
Q

Resistance to 6-MP and 6-GT

A

Decreased HGPRTase activity (activating enzyme) or increase production of Alkaline Phosphatases

75
Q

Resistance to Alkylating agents

A

Increased DNA repair; Decreased drug permeability; Production of trapping agents (thiols)

76
Q

Resistance to Vinca Alkyloids

A

Increased efflux

77
Q

Special cyclophosphamide toxicity

A

Hemorrhage Cystitis

78
Q

The metabolism of 6-MP by Xanthine Oxidase is inhibited by

A

Allopurinol

79
Q

Use of Mechlorethamine

A

Hodgkin’s Lymphoma

80
Q

Use of Taxanes

A

Advanced Breast and Ovarian cancers

81
Q

Uses of Dactinomycin

A

Melanoma and Wilms tumor

82
Q

Vesicant

A

Drug that causes blisters on contact with tissues

83
Q

Vincristine toxicities

A

Peripheral neuropathy, Paralytic Ileus

84
Q

What is needed for Cyclophosphamide antitumor activity

A

Hepatic CYP450 biotransformation

85
Q

What may protect against cardiotoxicity from Anthracyclines

A

Dexrazoxane

86
Q

When to give Allopurinol

A

Tumor Lysis Syndrome, 6-MP

87
Q

When to give Amifostine

A

Cisplatin (cytoprotection)

88
Q

When to give Leucovorin

A

MTX, 5-FU

89
Q

When to give Mesna as concurrent agent

A

Cyclophasphamide (protect against Acrolein production)

Pharmacology 2 (8 decks)

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