ANTINEOPLASTIC AGENT Flashcards

1
Q

ADR: Alopecia

A

Doxorubicin, Carboplatin

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2
Q

ADR: Neutrotoxic can go to BBB

A

Nitrosurea: Carmustine & Lomustine

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3
Q

ADR: H/A and Peripheral neuropathy

A

Vinka alkaloids: vincristine & vinblastine

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4
Q

ADR: Change in visual quality / corneal opacity

A

Tamoxifen

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5
Q

ADR: Epistaxis (nosebleed)

A

Plicamycin

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6
Q

ADR: Cardiotoxicity/ Bone marrow depression

A

Doxorubicin, Daunorubicin

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7
Q

ADR: Pulmonary fibrosis

A

Bleomycin, Busulfan

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8
Q

ADR: Liver toxicity

A

Methotrexate

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9
Q

ADR: Nephrotoxic

A

Cisplatin, Carboplatin

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10
Q

ADR: Myelosuppression

A

Methotrexate, 5-Flurouracil

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11
Q

ADR: Hemorrhagic Cystitis

A

Cyclophosphamide

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12
Q

ADR: Muscle pain, Malaise, Fever

A

Cytarabine

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13
Q

New or unusual growth of tissue or tumor
may be benign or malignant cancer

A

Neoplasms

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14
Q

uncontrollable growth and spread of abnormal

A

Neoplasia

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15
Q

any cancer that arises form epithelium

A

Carcinoma

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16
Q

cancer of connective tissue

A

Sarcoma

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17
Q

cancer of the lymph nodes

A

Lymphoma

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18
Q

Any abnormal swelling in or on body part

A

Tumor

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19
Q

a tumor that does not invade and destroy the tissue in which it originates or spread to the distant sites in the body

A

Benign

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20
Q

a tumor that does invade and destroys the tissue in which it originates and can spread to other sites in the body via the bloodstream and lymphatic system.

A

Malignant

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21
Q

The distant spread of tumor from its site origin

A

Metastasis

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22
Q

aka mutation: exposure to chemicals or unusual element that cause cancer and step 1

A

Initiation

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23
Q

a promotor that increases mutation of the cell, can be specific or non-specific and step 2

A

Promotion

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24
Q

INc. the growth -> activate tumor cell to spread
aggressive and inc malignant

A

Progression

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25
Q

Chemicals
Excess energy or macronutrients especially unsaturated fats
virus
radiation
limited antioxidant and other nutrients

A

causes of cancer

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26
Q

Curative
Palliative
Adjuvant therapy
salvage chemotherapy
neoadjuvant

A

Goals for the cancer

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27
Q

total eradication of cancer cells
lower tumor cell burden at which level host
immunological defenses may keep the cells in control

A

Curative

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28
Q

Alleviation of symptoms, decrease tumor size, control growth
avoidance of life-threatening toxicity
inc. survival and improved quality of life

A

Palliative

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29
Q

attempt to eradicate microscopic cancer after surgery

A

Adjuvant therapy

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30
Q

an attempt to get a patient into remission, after previous therapies have failed

A

salvage chemotherapy

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31
Q

chemotherapy is given to decrease the tumor burden before definitive therapy (surgery, radiation)

A

neoadjuvant

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32
Q

oncologists prefer to use the term complete response or remission to indicate a patient with no evidence of disease after treatment

A

remission

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33
Q

chemotherapeutic agents kill a constant fraction of cells (1st order kinetics), rather than specific number of cells after each dose

A

Log Kill hypothesis

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34
Q

significance weight ____ that indicates positive to a tumor

A

1 gram

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35
Q

Antimetabolites
Bleomycin
Podophyllin Alkaloids
Plant alkaloids

A

Cell cycle specific agent

36
Q

Alkylating Agents
antibiotics
cisplatin
nitrosoureas

A

Cell cycle non-specific agent

37
Q

guardian of the cell
tumor suppressor

A

p53

38
Q

the ability of some cells to synthesize their own growth factors

A

Autocrine signaling

39
Q

the programmed cell death

A

apoptosis

40
Q

INB. cell division thru alkylation of DNA

A

Alkylating Agents

41
Q

Nitrogen mustard
ethyleneimines
alkyl sulfonate
nitrosoureas
triazenes

A

Alkylating Agents

42
Q

Prodrugs under nitrogen mustard

A

mechlorethamine, cyclophosphamide

43
Q

a too-reactive agent
a vesicant
only in IV form
intermediate product: aziridine

A

mechlorethamine

44
Q

Antidote for mechlorethamine toxicity

A

Na thiosulfate

45
Q

use in chronic lymphocytic leukemia
acute lymphoblastic leukemia
toxic metabolite: Acrolein
hydroxylation in the liver

A

cyclophosphamide

46
Q

active part of cyclophosphamide

A

phospharamide mustard

47
Q

a chemical added to cyclophosphamide
concentrates the electrophilic substance in the kidney and conjugates acrolein

A

MESNA (2-mercaptoethansesulfonate)

48
Q

be taken orally
least toxic nitro mustard
it slows down the reaction in the formation of
aziridine, making oral administration possible for them

A

chlorambucil and melfalan

49
Q

use in bladder cancer, ovarian cancer, breast cancer
moa: desulfuration
IM: aziridine
reactive in low ph

A

Thiotepa

50
Q

use in chronic myelogenous leukemia
intermediate metabolite: 3-hydroxysulfolane
tetrahydrothiophene 1-oxide
sulfalene

A

Busulfan

51
Q

____optimal for antineoplastic activity of busulfan

A

4-5 alkyl substituents

52
Q

undergo spontaneous non-enzymatic degradation with formation of the 2-chloroethyl carbonium ion from diazohydroxide formed

liberates isocynate that attach carbomoyl grp to the lysine residue of protein inactive DNA

A

nitrosoureas

53
Q

alkylating agent that pass thru BBB
use in brain tumor
myelosuppression is the dose-limiting effect

A

Nitrosurea: Carmustine & Lomustine

54
Q

BCNU/ Bis-chloroethyl nitrosourea

A

Carmustine

55
Q

CCNUU/ chloroethyl- Cyclohexyl nitrosourea

A

Lomustine

56
Q

undergoes N-demethylation (liver cyp450)
forms diazomethane
can inb mao and aldehyde dehydrogenase

A

Dacarbazine/procarbazine

57
Q

purine analogs
pyrimidine analogs
folic acid analogs

myelosuppression is the dose-limiting toxicity for all drugs in this class
prodrugs
target: S phase of the cell division

A

antimetabolite

58
Q

mercaptopurine
thioguanine
Azathioprine
pentostatin
hypoxanthine and quanine
DNA

A

purine analogs

59
Q

____convert to T-GMP (6-thioguanine mono phosphate)
_____convert T-IMP (6-thioinosine mono phosphate)

A

Thioguanine, mercaptopurine

60
Q

T-GMP AND T-IMP CONVERTS INTO HGPRT BY enzyme called _____

A

Guanylyl kinase

61
Q

HGPRT means

A

Hypoxanthine guanine phosphoribosyl transferase

62
Q

the accumulation cases inhibition in inosinate oxygenase

A

HGPRT

63
Q

used an immunosuppressive agent
and a derivative of 6 mercaptopurine

A

Azathioprine

64
Q

mercaptopurine + ____will make it more toxic

A

Allopurinol

65
Q

D-arabinose form D-ribose DNA polymerase inb

A

Vidarabine

66
Q

addition of fluorine in D-ribose
arabirosyl- 7- fluroadenine Triphosphate
DNA polymerase inb

A

Fludarabine

67
Q

chlorine incorporated in the adenine
2-chlorodeoxy adenosine triphosphate
DNA polymerase inb

A

Cladribine

68
Q

Fluorouracil
Floxuridine
Cytarabine
Gemcitabine
RNA

A

Pyrimidine Analogs

69
Q

1st choice for colon cancer
inb thymidtlate synthase
converted ito a fraudulent nucleotide
FDUMP
IM: 5-fluorodeoxyuridine monophosphate
5-fluorouridine triphosphate

A

5-Fluorouracil

70
Q

FDUMP means

A

Fluorodeoxyuridine monophosphate

71
Q

Prodrugs of 5-Fu
to reduce the catabolic inactivation of 5-FU by DPD
inb DPD

A

capecitabine, tegafur

72
Q

DPD means

A

Dihydropyrimidine dehydrogenase

73
Q

discovered in Europe 1960 approved by FDA june 1969
Cytosine arabinoside
1 beta-arabinofuranosylcytosine
rapid conversion into cytosine arabinoside triphosphate, which damage DNA when cell cycle holds in “S-phase”

A

Cytarabine

74
Q

Cytarabine +____+____= use to treat acute nonlymphocytic leukemia

A

daunorubicin, thioguanine

75
Q

replaces cytidine, during DNA replication
1st line for small lung cancer (iV)
Fluorination sugar moiety

A

Gemcitabine

76
Q

Moa: blocks DNA synthesis through inb enzyme dihydrofolate reductase
pseudo irreversibile (highgher ph)
folate acid inb kills cells in the s-phase

A

Methotrexate

77
Q

___is given to prevent toxicity in cells. Given 6-24 hours after treatment w/ MTX

A

Leucovorin

78
Q

Daunorubicin
Doxorubicin
Dactinomycin
Idarubicin
valrubicin
bleomycin
mitomycin
Plicamycin
Streptozocin

A

Cytotoxic Antibiotic

79
Q

disrupt DNA function and cell division
streptomyces
MOA: intercalation
inb topoisomerase
alkylation
strand breakage

A

Cytotoxic Antibiotic

80
Q

isolated streptomyces verticillius
naturally occurring as Cu-chelates
intercalates between G-C base pairs
ROS formation from bleo-iron complex

A

Bleomycin

81
Q

isolated streptomyces parvulus
inb topisomerase II
g-c base pairs
G1 and S phase
3-phenoxazone, 9-dicarboxylic acid

A

dactionomycin

82
Q

a toxic anthracycline
planar oxidized anthracene nucleus fused to a cyclohexane ring that is subsequently connected to an amino sugar

A

doxorubicin, daunorubicin

83
Q

a derivative of daunorubicin that is less toxic
4-demetoxy analog

A

idarubicin

84
Q

an epimer derivative of doxorubicin

A

epirubicin

85
Q

isolated in streptomyces peucetius
it intercalates into DNA and decreased synthesis of both DNA & RNA

A

Anthracycline