Cancer drugs

Question 1

methotrexate moa

Answer 1

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

Question 2

methotrexate toxicity

Answer 2

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

Question 3

5-FU moa

Answer 3

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

Question 4

cytarabine moa

Answer 4

pyrimidien analog that inhibits DNA polymerase

Question 5

5-FU toxicity

Answer 5

myelosuppression and photosensitivity; tx overdose with uridine;

Question 6

cytarabine toxicity

Answer 6

leukopenia, thrombocytopenia, megaloblastic anemia,

Question 7

azathioprine, 6-MP, and 6-TG moa

Answer 7

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

Question 8

azathioprine, 6-MP, and 6-TG toxicity

Answer 8

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

Question 9

dactinomycin moa

Answer 9

intercalates in DNA

Question 10

doxorubicin and daunorubicin moa

Answer 10

generation of free radicals, DNA intercalation

Question 11

doxorubicin and daunorubicin toxicity

Answer 11

dilated cardiomyopathy; dexrazoxane used to prevent cardiotoxicity

Question 12

belomycin moa

Answer 12

induces free radical formation which causes breaks in DNA strands

Question 13

bleomycin toxicity

Answer 13

pulmonary fibrosis, skin changes, mucositis

Question 14

cyclophosphamide and ifosfamide moa

Answer 14

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

Question 15

cyclophosphamide and ifosfamide toxicity

Answer 15

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

Question 16

nitrosoureas (carmustine, lomustine, semustine, streptozocin) moa

Answer 16

cross link DNA
cross the BBB
require bioactivation

Question 17

nitrosoureas (carmustine, lomustine, semustine, streptozocin)

Answer 17

CNS toxicity - convulsions, dizziness, ataxia

Question 18

busulfan moa

Answer 18

cross links DNA

Question 19

busulfan toxicity

Answer 19

severe myelosuppression; pulmonary fibrosis, hyperpigmentation

Question 20

vinca alkaloids moa

Answer 20

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

Question 21

paclitaxel moa

Answer 21

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

Question 22

cisplatin, carboplatin moa

Answer 22

cross link DNA

Question 23

vinca alkaloids toxicty

Answer 23

peripheral neuritis

Question 24

cisplatin and carboplatin toxicity

Answer 24

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

Question 25

etoposide and teniposide moa

Answer 25

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

Question 26

irinotecan, topotecan moa

Answer 26

inhibit toposiomerase I and prevent DNA unwinding and replication

Question 27

hydroxyurea moa

Answer 27

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

Question 28

prednisone moa

Answer 28

triggers apoptosis in cancer cells

Question 29

tamoxifen raloxifene moa

Answer 29

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

Question 30

tamoxifen toxicity

Answer 30

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

Question 31

trastuzumab moa

Answer 31

mAB to HER-2 (erbB2)

Question 32

trastuzumab toxicity

Answer 32

cardiotoxicity

Question 33

imatinib moa

Answer 33

tyrosine kinase inhibitor of BCR-ABL

Question 34

rituximab moa

Answer 34

mAB to CD20

Question 35

vermurafenib moa

Answer 35

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

Question 36

Bevacizumab moa

Answer 36

mAB against VEGF; inhibits agiogenesis

Question 37

S-phase specific

Answer 37

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

Question 38

M-phase specific

Answer 38

vinca alkaloids and taxanes

Question 39

G2 phase specific

Answer 39

bleomycin and etoposide