Cancer drugs Flashcards

1
Q

methotrexate moa

A

folic acid analog that inhibits DHFR, decreasing DNA and protein synthesis

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2
Q

methotrexate toxicity

A

myelosuppression, reversible with leucovorin; macro vesicular fatty change in liver; mucositis, teratogenic

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3
Q

5-FU moa

A

pyrimidine analog bioactivated to 5F-dUMP, which covalently complexes folic acid; this inhibits thymidylate synthetase; decreasing DNA and protein synthesis

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4
Q

cytarabine moa

A

pyrimidien analog that inhibits DNA polymerase

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5
Q

5-FU toxicity

A

myelosuppression and photosensitivity; tx overdose with uridine;

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6
Q

cytarabine toxicity

A

leukopenia, thrombocytopenia, megaloblastic anemia,

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7
Q

azathioprine, 6-MP, and 6-TG moa

A

purine analogs; decrease de novo purine synthesis; activated by HGPRT and metabolized by xanthine oxidase

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8
Q

azathioprine, 6-MP, and 6-TG toxicity

A

bone marrow suppression, GI, and liver toxicity; increased toxicity with allopurinol

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9
Q

dactinomycin moa

A

intercalates in DNA

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10
Q

doxorubicin and daunorubicin moa

A

generation of free radicals, DNA intercalation

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11
Q

doxorubicin and daunorubicin toxicity

A

dilated cardiomyopathy; dexrazoxane used to prevent cardiotoxicity

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12
Q

belomycin moa

A

induces free radical formation which causes breaks in DNA strands

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13
Q

bleomycin toxicity

A

pulmonary fibrosis, skin changes, mucositis

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14
Q

cyclophosphamide and ifosfamide moa

A

covalently X-link (inter strand) DNA at guanine N-7; require bioactivation by liver

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15
Q

cyclophosphamide and ifosfamide toxicity

A

hemorrhagic cystitis; partially prevented by meson (binds to toxic metabs)

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16
Q

nitrosoureas (carmustine, lomustine, semustine, streptozocin) moa

A

cross link DNA
cross the BBB
require bioactivation

17
Q

nitrosoureas (carmustine, lomustine, semustine, streptozocin)

A

CNS toxicity - convulsions, dizziness, ataxia

18
Q

busulfan moa

A

cross links DNA

19
Q

busulfan toxicity

A

severe myelosuppression; pulmonary fibrosis, hyperpigmentation

20
Q

vinca alkaloids moa

A

bind beta-tubulin and inhibit polymerization of microtubules (M-phase cycle arrest)

21
Q

paclitaxel moa

A

hyperstabilize polymerized microtubules in M phase so that mitotic spindle cannot break down

22
Q

cisplatin, carboplatin moa

A

cross link DNA

23
Q

vinca alkaloids toxicty

A

peripheral neuritis

24
Q

cisplatin and carboplatin toxicity

A

nephrotoxicity and acoustic nerve damage; prevent nephrotoxicity with amifostine (free radical scavenger)

25
Q

etoposide and teniposide moa

A

inhibits topoisomerase II and increases DNA degradation (cannot relieve supercoils)

26
Q

irinotecan, topotecan moa

A

inhibit toposiomerase I and prevent DNA unwinding and replication

27
Q

hydroxyurea moa

A

inhibits ribonucleotide reductase, decreasing DNA synthesis (S-phase specific)

28
Q

prednisone moa

A

triggers apoptosis in cancer cells

29
Q

tamoxifen raloxifene moa

A

selective estrogen receptor modulators; antagonists in breast and agonists in bone;

30
Q

tamoxifen toxicity

A

partial agonist in endometrium which increases the risk of endometrial cancer; hot flashes

31
Q

trastuzumab moa

A

mAB to HER-2 (erbB2)

32
Q

trastuzumab toxicity

A

cardiotoxicity

33
Q

imatinib moa

A

tyrosine kinase inhibitor of BCR-ABL

34
Q

rituximab moa

A

mAB to CD20

35
Q

vermurafenib moa

A

small molecule inhibitor of forms of the braf kinase with v600E mutation

36
Q

Bevacizumab moa

A

mAB against VEGF; inhibits agiogenesis

37
Q

S-phase specific

A

etoposide and antimetabolites (MTX, 5-FU, cytarabine, axathioprine, 6-MP, 6-TG)

38
Q

M-phase specific

A

vinca alkaloids and taxanes

39
Q

G2 phase specific

A

bleomycin and etoposide