Cancer drugs Flashcards

(77 cards)

1
Q

Methotrexate- mechanism

A

dihydrofolate reductase inhibitor

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2
Q

Methotrexate- uses

A

Cancer- ALL, AML, breast cancer

Uterine pathology- ectopic pregnancy, abortion, choriocarcinoma, hydatiform mole

Immunosuppression: RA, psoriasis

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3
Q

Methotrexate- toxicity

A

bone marrow suppression- reversible with leucovorin (folin acid analog)

pulmonic fibrosis (methotrexate lung)

hepatotoxicity

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4
Q

5-Fluorouracil-mechanism

A

pyrimidine analog bioactivated to 5F-dUMP, which complexes covalently with folic acid. This complex inhibits thymidylate synthase, which then inhibits DNA synthesis.

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5
Q

5FU uses

A

colon cancer
topical use for actinic keratosis
pancreatic cancer
basal cell carcinoma

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6
Q

5FU side effects

A

Myelosuppression, not reversible with leucovorin

Uridine is a possible rescue agent

photosensitivity

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7
Q

Azathioprine, which is bioactivated to 6MP

MOA

A

purine analog, inhibits PRPP imidotransferase

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8
Q

6MP (azathioprine) uses

A

prevents organ rejection, RA, IBD, SLE

use to wean patients off steroids in chronic disease

use to treat steroid- refractory chronic disease

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9
Q

6MP (azathioprine) toxicity

A

myelosuppression
hepatotoxicity

increased toxicity with allopurinol or febuxostat which are also metabolized by xanthine oxidase enzyme

6TG is metabolized by a different enzyme, so it can be combined with azathioprine

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10
Q

cyclophosphamide/ ifosfamide MOA

A

bioactivated by the liver, then acts as an alkylating agent, cross- links DNA at guanine N7

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11
Q

cyclophosphamide uses

A

cancer: solid tumors, leukemia, lymphomas
immunosuppresant: lupus nephritis, polyarteritis nodosa

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12
Q

ifosfamide uses

A

testicular cancer. Ifosfamide is not used for testicular cancer

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13
Q

cyclofosfamide/ifosfamide toxicity

A

both drugs can lead to myelosuppression.
These alkylating agents form a toxic metabolic Acrolein, which can induce hepatotoxicity. For this reason, administer cyclofosfamide/ifosfamide with Mesna, which binds the Acrolein up and makes cyclophosphamide/ifosfamide safer

Both drugs are also associated with increased rates of transitional cell bladder cancer

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14
Q

Nitrosoureas: MOA

A

bioactivated alkylating agent that cross- links DNA in the CNS

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15
Q

Nitrosoureas- uses

A

brain tumors (including glioblastoma multiforme)

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16
Q

nitrosoureas- toxicity

A

CNS toxicity (convulsions, dizziness, ataxia)

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17
Q

Busulfan- MOA, uses, toxicity

A

alkylating agent that cross- links DNA

used for CML, ablation of bone marrow before bone marrow transplantation

toxicity: PULMONARY FIBROSIS
hyperpigmentation

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18
Q

Doxorubicin, daunorubicin: MOA, uses, toxicity

What drug is used to prevent toxicity?

A
  1. intercalates into DNA so that it can’t unwind
  2. generates free radicals

used to treat lymphoma, leukemia, solid tumors

toxicity: cardiotoxicity (dilated cardiomyopathy)
myelosuppression
alopecia

note: heart muscle relatively deficient in SOD

Dexrazoxane is an iron chelating agent that is used to prevent cardiotoxicity

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19
Q

Dactinomycin

A
intercalates DNA, 
used for children's tumors
-Wilm's tumor
-Ewing sarcoma
-Rhabdomyosarcoma
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20
Q

generates free radicals and intercalates DNA

A

Daunorubicin/doxorubicin

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21
Q

inhibits dihydrofolate reductase

A

Methotrexate

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22
Q

inhibits thymidylate synthase

A

5-FU

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23
Q

inhibits PRPP amidotransferase

A

6MP

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24
Q

inhibits DNA polymerase

A

Cytarabine (pyrimidine analog)

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25
Give dexrazoxane with ... for...
dexrazoxan with daunorubicin/doxorubicin | for cardiotocity
26
Give leucovorin with ... for...
leucovorin with methotrexate for myelosuppression rescue
27
give mesna with... for...
cyclophosphamide and ifosfamide for toxic acrolein metabolite, which causes hemorrhagic cystitis
28
give uridine with... for...
uridine is a rescue agent for 5FU myelosuppression
29
Bleomycin
generates free radicals leading to DNA damage. use for testicular cancer (along with etoposide and cisplatin), Hodgkin lymphoma toxicity: pulmonary fibrosis lance can't take bleomycin because he races
30
pulmonary fibrosis
methotrexate (antimetabolite) lung busulfan alkylating agent bleomycin antitumor antibiotic
31
folic acid analog that inhbits dihydrofolate reductase
methotrexate
32
pyrimidine analog that inhibits thymidylate synthase
5-FU
33
how does the body metabolize 6MP?
xanthine oxidase
34
which cancer drug is often used in rheumatoid diseases and ectopic pregnancy?
methotrexate
35
alkylates DNA, toxicity includes pulmonary fibrosis
Busulfan
36
fragments DNA, toxicity includes pulmonary fibrosis
bleomycin
37
blocks purine synthesis, metabolized by xanthine oxidase
azathioprine (6MP)
38
nitrogen mustard, alkylates DNA
nitrosoureas
39
folic acid analog that inhibits dihydrofolate reductase
methotrexate
40
intercalates DNA, produces oxygen free radicals, cardiotoxic
doxorubicin, daunorubicin
41
DNA alkylating agents used in brain cancer
nitrosoureas
42
applied topically for actinic keratoses and basal cell cancers
topical 5FU
43
treatment for childhood tumors (Ewing sarcoma, Wilms tumor, rhabdomyosarcoma)
dactinomycin
44
side effect of hemorrhagic cystitis
cyclophosphamide and ifosfamide
45
cisplatin, carboplatin, oxaliplatin
cross-link DNA GU treatments include ovarian cancer, bladder, cancer, testicular cancer, lung carcinoma toxicity includes nephrotoxicity, ototoxicity prevent nephrotoxicity with amifostine (free radical scavenger), and chloride (saline) diuresis
46
Etoposide, teniposide
etoposide inhibits topoismerase II, enhancing DNA degradation by super-coiling use for solid tumors (particularly testicular and small cell lung cancer), prostate cancer leukemias, lymphomas toxicity includes myelosuppression
47
testicular cancer regimen | Eradicate Ball Cancer
etoposide, bleomycin (or ifosfamide), cisplatin
48
irinotecan and topotecan
these inhibit topoisomerase I irinotecan is used for metastatic colon cancer topotecan is used for small cell lung cancer, ovarian cancer, cervical cancer
49
Vincristine
blocks polymerization of microtubules used to treat hodgkin lymphoma, Wilms tumor, Ewing sarcoma, choriocarcinoma side effects: neurotoxicity peripheral neuritis
50
Vinblastine
blocks mictotubule polymerization indications are also similar to vincristine WT, choriocarcinoma, Ewing sarcoma, Hodgkin lymphoma toxicity: myelosuppression Vinblastine blasts bone marrow
51
Paclitaxel
hyperstabilizes polymerized microtubules in M phase, so that mitotic spindle cannot break down (anaphase cannot occur) used for ovarian and breast carcinomas toxicity: hypersensitivity
52
drugs that work on microtubules
``` vincristine vinblastine paclitaxel mebendazole albendazole griseofulvin colchicine ```
53
hydroxyurea
inhibits ribonucleotide reductase, thereby inhibiting DNA synthesis (S-phase specific) used for melanoma, CML, sickle cell disease (increased HbF) toxicity: severe myelosuppression, GI upset
54
Prednisone
triggers apoptosis in lymphoid tumors like CLL and Hodgkin lymphoma
55
BAM CUSHINGOID
buffalo hump amenorrhea moon facies ``` crazy ulcers skin changes htn infection necrotic femoral head glaucoma osteoporosis immunosuppression diabetes ```
56
Selective estrogen receptor modulators (SERMs) | Tamoxifen
ER antagonist at breast ER agonist in bone ER partial agonist in endometrium use for ER+ breast cancer prevent cancer in patients with BRCA mutation tox: increased risk of endometrial carcinoma via overstimulation of endometrial tissue in women with endometrial cancer, tamoxifen can be used for treatment
57
Raloxifene SERM
used to treat osteoporosis ER antagonist - breast -endometrium ER agonist -bone
58
Trastuxumab
monoclonal antibody against HER2 receptor (TKR), which helps to kill cancers that overexpress HER2. Useful only for HER-2+ breast cancer and gastric cancer (tras2zumab) Cardiotoxicity- HER2 Heartceptin hurts the heart
59
inhibits microtubule formation
vincristine
60
inhibits microtubule disassembly
paclitaxel
61
inhibits ribunucleutide reductase
hydroxyurea
62
inhibits topoisomerase II
etoposide
63
inhibits topoisomerase I
topotecan
64
Cardiotoxicity
trastuzumab (herceptin)
65
hypersensitivity reactions
paclitaxel
66
increased risk of endometrial cancer
tamoxifen
67
nephrotoxicity and ototoxicity
cisplatin
68
peripheral neuropathy
vincristine
69
Rituximab
``` antibody against CD20 used for lymphomas, leukemias RA vasculitis pemphigus vulgaris ITP ``` tox: increases risk of progressive multifiocal leukencephalopathy
70
Bevacizumab
monoclonal antibody against VEGF, inhibits angiogenesis cancers need new blood vessels or they will die treat metastatic colon cancer metastatic cervical cancer certain types of lung cancer metastatic renal cell carcinoma side effects: impaired wound healing, severe hemorrhage (hemoptysis, GI bleeding, epistaxis)
71
Imatinib
enzyme inhibitor targets BCR-Abl TKR, produced by t(9;22) Philadelphia chromosome CML ALL AML
72
cross-links DNA, nephrotoxic, ototoxic
cisplatin carboplatin oxaliplatin
73
prevents tubulin disassm
Paclitaxel
74
inhibits ribonucleotide reductase
hydroxyurea
75
inhibitor of the mutated tyrosine kinase produced by the Philadelphia chromozome
imatinib
76
monoclonal antibody against HER2
trastuzumab
77
SERM that does not increase the risk of endometrial cancer
raloxifene