Anti cancer Flashcards

1
Q

agents that donate an alkyl group - DNA crosslinks @ position N-7 guanine

A

alkylating agents

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2
Q

is activated by hepatic cytochrome P450

A

Cyclophosphamide

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3
Q

treats hematologic and solid malignancies (leukemia’s, lymphomas, breast cancer, ovarian cancer)

A

Cyclophosphamide

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4
Q

ADR: BM depression, hemorrhagic cystitis, increases risk of bladder cancer, hyponatremia due to SIADH, infertility and premature menopause

A

Cyclophosphamide

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5
Q

MOA: increase DNA repair, decrease drug permeability, production of trapping agents (thiols)

A

Alkylating agents

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6
Q

causes cystitis

A

acrolein

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7
Q

binds and inactivates acrolein and hydration

A

MESNA

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8
Q

active form of Cyclophosphamide

A

phosphoramide mustard

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9
Q

nitrosoureas

A

temozolomide - most used
carmustine
lomustine
streptozotocin

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10
Q

cross BBB and treat brain tumors and cause ADR of neurotoxicity

A

nitrosoureas

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11
Q

treats insulinoma and induces type 1 diabetes

A

streptozotocin

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12
Q

MOA: same as Cyclophosphamide, but also forms hydrogen peroxide, which generates free radicals that cause DNA damage

A

procarbazine

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13
Q

Treats Hodgkins lymphoma

ADR: disulfiram like reaction after drinking alcohol & secondary cancers (acute leukemia - years after)

A

procarbazine

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14
Q

analogs that bind DNA and form intra strand and inter strand cross links

A

Platinum analogs

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15
Q

treats solid malignancies - specifically testicular cancer;
Is marrow sparing;
same MOA as Cyclophosphamide

A

cisplatin

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16
Q

ADR: ototoxicity, neurotoxicity and nephrotoxicity

A

cisplatin

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17
Q

what drug can prevent nephrotoxicity

A

amifostine

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18
Q

similar to cisplatin but ADR less renal toxicity, but increase BM depression

A

carboplatin

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19
Q

inhibit microtubule production and mitotic spindle assembly; acts on M phase

A

vincristine

vinblastine

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20
Q

resistance: increase efflux of drug from tumor cells (p glycoprotein)

A

plant alkaloids

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21
Q

Treats: Hodgkins, breast cancer, testicular cancer

A

vinblastine

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22
Q

toxicity: BM suppression, anorexia, nausea, vomiting, diarrhea, alopecia

A

vinblastine

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23
Q

treats: childhood leukemias, childhood wilms tumor, neuroblastoma, Hodgkins

A

vincristine

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24
Q

toxicity: peripheral neuritis with paresthesia, SIADH, muscle weakness
muscle sparing effect!

A

vincristine

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25
Q

enhance microtubule production and prevent their degradation - improper mitotic spindle function

A

paclitaxel

docetaxel

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26
Q

ADR: neutropenia, peripheral neuropathy, hypersensitivity reactions, alopecia

A

paclitaxel

docetaxel

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27
Q

topoisomerase 2 inhibitors

active in late S and early G2 phase

A

etoposide

teniposide

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28
Q

treats testicular and prostate cancer and small cell lung cancer

A

etoposide

teniposide

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29
Q

topoisomerase 1 inhibitors

A

topotecan

irinotecan

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30
Q

treats ovarian cancer and small cell lung cancer

A

topotecan

irinotecan

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31
Q

pyrimidine analog and is only active against hematologic malignancies (AML, Non-Hodgkins)

A

cytarabine

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32
Q

acts in S phase

converted to 5’ (ara-CMP) then converted to dCMP kinase converted to ara CTP (active)

A

cytarabine

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33
Q

inhibits DNA poly

incorporates into DNA and RNA

A

cytarabine

34
Q

ADR: neurotoxicity, hand - foot syndrome, BM depression, corneal toxicity, keratoconjunctivitis

A

cytarabine

35
Q

need HGPRT to activate
blocks synthesis of IMP
inhibits DNA synthesis
blocks S phase

A

6-MP

6-TG

36
Q

inhibits IMP to AMP and guanine

A

6-MP

37
Q

inhibits guanine synthesis from IMP

A

6-TG

38
Q

XO inhibitor

A

allopurinol

39
Q

inhibition of XO increases level of purine analogs (6-MP) and cause toxicity/effects

A

allopurinol

40
Q

Resistance: cancer cells having decrease activity of HGPRT; also increases alkaline phosphatase that inactivates toxic nucleotides

A

6-MP

6-TG

41
Q

cytotoxic folate analog, preventing conversion of DHF to THF; inhibits dihydrofolate reducatase

A

methotrexate

42
Q

causes build up of DHF
stop DNA and RNA synthesis in rapidly dividing cells
affects S phase
does not cross BBB

A

methotrexate

43
Q

Treats

1) antineoplastic cancers
2) w/ misoprostol used as abortifacient and ectopic pregnancy
3) invasive molar pregnancy, trophoblastic tumors
4) choriocarcinoma
5) psoriasis
6) first line in RA

A

methotrexate

44
Q

mech. of resistance
1) decrease drug transport
2) decrease polyglutamate
3) altered DHFR
4) increase levels of DHFR

A

methotrexate

45
Q

ADR:

1) folate def
2) megaloblastic anemia
3) myelosuppression
4) pancytopenia
5) renal toxicity
6) lung fibrosis
7) mucositis
8) baldness
9) hepatotoxicity
10) immunosuppressed have increased risk of infection

A

methotrexate

46
Q

antidote for methotrexate
give after methotrexate
only works in normal cells

A

leucovorin (folonic acid)

47
Q

complexes with THF and inhibits thymidylate synthase to block thymidine production; increase dUMP; interferes with mRNA translation and inhibits DNA synthesis

A

5-FU

48
Q

ADR: diarrhea, photosensitivity, rash, myelosuppression , infection, hyperpigmentation, hand foot syndrome, neurologic deficits

A

5-FU

49
Q

resistance due to decrease activation of 5-FU, decrease thymidylate synthesis activity

A

5-FU

50
Q

uses: carcinomas - breast, GIT, hepatoma, ovary, cervix, urinary, bladder, prostate, pancreas, colon, oropharyngeal

A

5-FU

51
Q

antidote for overdose of 5-FU

A

uridine triacetate

52
Q

ribonucleotide reductase inhibitor

blocks thymidine synthesis

A

hydroxyurea

53
Q

treats sickle cell and CML; increases HbF - protection against HbS
ADR: myelosupression and increased infection side effect

A

hydroxyurea

54
Q

binds DNA and produces free radicals; free radicals produced cause single and double strand breaks in DNA

A

bleomycin

55
Q

blocks the G2 phase of cell cycle

A

bleomycin

56
Q

treats hematologic and solid malignancies and acts as sclerosing agent - (tx varicose veins)

A

bleomycin

57
Q

cures pulmonary toxicity - pulmonary fibrosis

A

bleomycin

58
Q

CCNS drugs
produce free radicals
intercalate in DNA - block DNA and RNA synthesis
inhibit topoisomerase 2

A

doxorubicin

daunorubicin

59
Q

treats a broad range of solid and hematologic malignancies and lymphomas

A

doxorubicin

daunorubicin

60
Q

causes cardio toxicity - dilated cardiomyopathy
myelosupression
alopecia

A

doxorubicin

daunorubicin

61
Q

prevents anthracycline induced cardiomyopathy

A

dexrazoxane

62
Q

erythema and desquamation of skin observed at sites of prior radiation therapy

A

radiation recall reaction

63
Q

intercalates in DNA - block DNA and RNA synthesis

A

actinomycin D

64
Q

treats choriocarcinoma if no response to MTX

A

actinomycin D

65
Q

used in childhood acute lymphoblastic leukemia
ADR: hypersensitivity and pancreatitis
Note: increase S amylase/ S lipase levels clue

A

asparaginase

66
Q

Immunosuppressant; breaks down lymphocytes

ADR: compromised immune system

A

prednisone

67
Q

resistance; MDR 1 coded efflux pump

A

anticancer antibiotics

68
Q

small molecule kinase inhibitors

A
imatinib 
erlotinib
sorafenib
sunitinib
vemurafenib
gefitinib
pazopanib
69
Q

treats CML - 1st line
blocks tyrosine kinase domain of the BCR/ABL fusion protein
blocks the c kit tyrosine kinase (GIST)
can cause fluid retention - ankle and periorbital edema

A

imatinib

70
Q

translocation between chromosomes 9 and 22 - BCR/ABL oncogene on chromosome 22

A

Philadelphia chromosome - imatinib

71
Q

blocks the epidermal growth factor receptor (EGFR) tyrosine kinase
tumors with EGFR over expression (non small cell lung and pancreatic cancer)

A

erlotinib

gefitinib

72
Q

inhibits the vascular endothelial growth factor receptor (VEGFR) tyrosine kinase
treat renal cell carcinoma

A

sorafenib
sunitinib
pazopanib

73
Q

treat hairy cell leukemia, CML, AIDS related capos sarcoma

A

interferon alpha 2a

74
Q

treats hairy cell leukemia, melanoma, follicular lymphoma, AIDS related capos sarcoma

A

interferon alpha 2b

75
Q

cyclin dependent kinase inhibitor

used: CDK 4/6 inhibitor for postmenopausal women with ER +, but HER 2 - breast cancer

A

palbociclib

76
Q
  • depletes B cells
  • binds CD20 on B cells
  • treats chronic lymphocytic leukemia, RA and non Hodgkin lymph
  • immunosuppression and increased risk infection
A

rituximab

77
Q

SE: headache, fever, skin rash, pruritus, dyspnea, hypotension, can cause serum sickness (arthralgia within 7-10 days)

A

rituximab

78
Q
  • binds the epidermal growth factor receptor (EGFR)
  • treat colorectal cancer
  • SE: can cause papulopustular acneiformrash
A

cetuximab

panitumab

79
Q
  • binds VEGF
  • inhibits growth of blood vessels in tumors
  • treats metastatic tumors (colorectal cancer, ovarian), retinopathy, RCC, NSCLC and wet macular degeneration
A

bevacizumab

80
Q
  • against HER 2 receptor
  • binds epidermal growth factor receptor 2 (HER2, c-erbB2)
  • treats HER2 + breast cancer
  • can cause cardiotoxicity
A

trastuzumab