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The Last Pharm Exam > Lecture 2 - Cancer standard agents > Flashcards

Lecture 2 - Cancer standard agents Flashcards

1
Q

busulfan, cyclophasphamide, and the nitrosureas are all ______. they act when during the cell cycle?

A 
alkylating agents;
all times (cell cycle non specific)
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2
Q

alkylating agents in general do what to DNA?

A

form cross links –> prevent DNA replication/transcription –> apoptosis

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3
Q

name 3 nitrosureas

A

carmustine, lamustine, streptozocin

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4
Q

the nitrosureas require bioactivation via liver _______. they are very _______ and are used to treat what kind of tumors?

A

hydroxylation;

lipophillic, brain tumors (ie cross BBB)

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5
Q

main side effect of nitrosureas:

A

CNS toxicity –> convulsions, dizziness, etc

bone marrow suppression, hepatotoxic, and pulm toxic according to notes

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6
Q

cyclophosphamide:
activated or degraded by CYP450?
crosslink DNA at what specific molecule?

A

activated;

guanine N7

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7
Q

cyclophosphamide:

can cause _______ (heme thing), _____ ____ which is prevented by _____

A

myelosuppression, hemorrhagic cystitis, mesna (binds toxic metabolites)

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8
Q

cyclophosphamide:
what is its toxic metabolite?
other side effects include ____ ( a cancer), _____ (an endocrine thing), and _____ (reproductive thing)

A 
acrolein;
bladder cancer (TCC), SIADH, infertility
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9
Q

_______ is a slow acting nitrogen mustard that is the drug of choice for _____ lymphocytic leukemia

A

chlorambucil, chronic

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10
Q

busulfan:
mainly used to treat ____ and for bone marrow ablation. most important side effect = ____. also can cause pulm fibrosis and _____ changes

A

CML;
severe bm suppression;
skin (ie hyperpigmentation)

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11
Q

name 3 anti-tumor antibiotics

A

bleomycin, dactinomycin (actinomycin D), doxorubicin

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12
Q

doxorubicin:

mechanism of action = ______ and ______

A

generates free radicals;

intercalates DNA–>DNA strand breaks

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13
Q

doxorubin:

causes dose dependent ______ (most important toxicity) and _____ (heme thing)

A

cardiotoxicity (dilated cardiomyopathy);

myelosuppression

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14
Q

mitoxantrone:

_____ inhibitor that induces DNA double strand breaks. similar to doxorubicin

A

topoisomerase II

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15
Q

bleomycin:
mechanism of action =
when does it act in the cell cycle?

A

free radical formation –> DNA strand breaks;

G2 (also M phase)

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16
Q

bleomycin:
mainly used for what 2 cancers?
most imp side effect - _____ _____;
also causes _____ changes

A

testicular cancer, lymphomas;

pulmonary fibrosis, skin (ie hyperpigmentation, atrophic striae)

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17
Q

actinomycin D:
mechanism of action -
main side effect -

A

intercalates DNA;

myelosuppression

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18
Q

cisplatin, carboplatin, and oxaliplatin are all _____ derivatives. they work by _______

A

platinum;

cross-linking DNA

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19
Q

cisplatin is especially effective in ____ and _____ cancers.

A

testicular, ovarian

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20
Q

3 important toxicities for cisplatin:

A

nephrotoxic, neurotoxic, ototoxic

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21
Q

how to prevent nephrotoxicity of cisplatin?

what does carboplatin cause?

A

adequate hydration/saline diuresis (also diuretics);

myelosuppression

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22
Q

oxaliplatin is mainly used to treat _____

A

colorectal cancer

rade side effects

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23
Q

what cell cycle phase do the antimetabolites act in?

24
Q

methotrexate is a _____ analog that competitively inhibits _____ = decreased _____ synthesis and decreased DNA synthesis

A

folic acid;
dihydrofolate reductase, dTMP

used to treat lots of things

25
Q

MTX side effects:
mucositis ie _____;
_______ which is reversible with _____ rescue;
____ toxicity

A

mouth ulcers;
myelosuppression, leucovorin (folinic acid);
hepato

26
Q

MTX side effects:
pulmonary ______;
_____ anemia

A

fibrosis;

megaloblastic

27
Q

6 mercaptopurine is a _____ analog. it is the active metabolite of _____

A

purine;

azathioprine;

28
Q

6-mercaptopurine:
activated by ______ (an enzyme);
what other drug causes increased toxicity with 6-MP?

A

HGPRT;

allopurinol (inhibits XO)

29
Q

6-MP:
mainly used to treat what cancer?
side effects = _____ (heme), _____ (a GI thing), and ____ toxicity

A

acute leukemia
bm suppression/pancytopenia;
pancreatitis;
liver

30
Q

clofarabine is a _____ analog that inhibits ______ and ribonucleotide reductase. used to treat ______

A

purine;
DNA polymerase;
acute leukemia

31
Q

5-FU and cytarabine are _____ analogues

A

pyrimidine

32
Q

5FU:

bioactivated to _____ which inhibits ______. _______ is a pro-drug with similar activity.

A

5-FdUMP; thymidylate synthase;

capecitabine

33
Q

5-FU:

mainly used to treat _____ and _____ cancer and topically, _______

A

colon, pancreatic;

basal cell

34
Q

5-FU:

side effects = _____ (heme thing). severe _____ (GI), and ______ (Skin)

A

bm suppression; diarrhea;
palmar-plantar erythrodyesthesia

also photosensitivity

35
Q

cytarabine inhbibits ________. mainly used to treat _____ and ______.

A

DNA polymerase;

leukemia, lymphoma

36
Q

cytarabine:

side effect = _____

A

bm suppression, pancytopenia

37
Q

raltitrexexd and pemetrexed inhibit _____. can be used to treat malignant _______

A

thymidylate synthetase;

mesothelioma

38
Q

gemcitabine:
_______ analog that inhibits DNA polymerase and also ____ ____;
main side effect is ______

A

pyrimidine;
ribonucleotide reductase;
myelosuppression

39
Q

etoposide/teniposide:
inhibit ______;
active when during the cell cycle?

A

topoisomerase II;

S and G2

40
Q

etoposide/teniposide:
mainly used to treat _____ and _______ (Solid tumors) + heme tumors;
2 side effects

A

testicular, small cell lung cancer;

myelosuppression, alopecia

41
Q

hydroxyurea:

inhibits _______. acts during what phase of the cell cycle?

A

ribonucleotide reductase;

s-phase

42
Q

hydroxyurea:

used to treat ______ disorders, _____ _____ anemia, and melanoma

A

myeloproliferate (ie CML); sickle cell

43
Q

hydroxyurea can cause severe ______

A

myelosuppression

44
Q

microtubule inhibitors include what 2 drugs?

when are they active?

A

paclitaxel/other taxols;
vincristine/vinblastine;

M phase (mitosis)

45
Q

vincristine and vinblastine bind _____ and effect polymerization how?

A

beta tubulin;

inhibit polymerization into microtubules

46
Q

vinblastine is used to treat _____ cancer and _____ lymphoma

A

testicular;

hodgkin

47
Q

vincristine is used to treat solid tumors, ____ lymphoma, and leukemias;

main side effect =

A

non-hodgkin;

neurotoxic–peripheral neuropathy, constipation

48
Q

vinblastine is less neurotoxic but causes _____

A

bone marrow suppression

49
Q

______ is used in advanced breast cancer and is first line treatment for advanced nonsmall cell lung cancer

A

vinorelbine

50
Q

taxanes (taxol) mechanism of action?

A

hyperstabilize polymerized microtubules (ie prevent depolymerization)

51
Q

taxols are used to treat what 2 types of cancer?

A

breast, ovarian

52
Q

taxols can cause _____ and _____

A

myelosuppression, peripheral neuropathy

53
Q

L-asparginase:

used to treat _____ mainly.

54
Q

mitotane:

intereferes with synthesis of adrenocortical steroids and is used to treat tumors of the _____

A

adrenal cortex

55
Q

irinotecan and topotecan are camptothecins that inhibit _____. they are active when during the cell cycle?

A

topoisomerase 1;

S phase and G2

56
Q

irinotecan is mainly used to treat ____ cancer. topotecan treats _____ and _____ cancer

A

colon;

ovarian, small cell lung cancer

The Last Pharm Exam (10 decks)

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