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Flashcards in Copy of Oncology - Copy of Onc Deck (35):
1

Methotrexate (MTX)

1) CA: leukemia, lymphoma, choriocarcinoma, sarcoma; non-CA: abortion, ectopic preg, rheumatoid arthritis, psoriasis
2) folate analog: inhibits DHFR --> decr dTMP --> decr DNA + protein syn
3) myelosuppression (reverse w/ leucovorin); macrovesicular fatty liver change; mucositis; teratogenic
4) S-phase specific

2

5-fluorouracil (5-FU)

1) colon CA, basal cell carcinoma (topical)
2) pyrimidine analog bioactivated to 5F-dUMP (covalently complexes folate) --> complex inhibits thymidylate synthase --> decr dTMP --> decr DNA + protein syn
3) myelosuppression (not reversible w/ leucovorin); OD rescue w/ thymidine; photosensitivity
4) S-phase specific

3

Cytarabine (arabinofuranosyl cytidine)

1) leukemia, lymphoma
2) pyrimidine analog --> inhibit DNA polymerase
3) leukopenia, thrombocytopenia, megaloblastic anemia
4) S-phase specific

4

Azathioprine

1) leukemias
2) purine (thiol) analog --> decr de novo purine syn
3) BM, GI, liver; metabolized by xanthine oxidase so incr toxicity w/ allopurinol
4) S-phase specific; activated by HGPRT

5

6-mercaptopurine (6-MP)

1) leukemias
2) purine (thiol) analog --> decr de novo purine syn
3) BM, GI, liver; metabolized by xanthine oxidase so incr toxicity w/ allopurinol
4) S-phase specific; activated by HGPRT

6

6-thioguanine (6-TG)

1) leukemias
2) purine (thiol) analog --> decr de novo purine syn
3) BM, GI, liver; metabolized by xanthine oxidase so incr toxicity w/ allopurinol
4) S-phase specific; activated by HGPRT

7

Dactinomycin (actinomycin D)

1) Wilm's tumor, Ewin's sarcoma, rhabdomyosarcoma; peds tumors
2) intercalates in DNA
3) myelosuppression
4) N/A

8

Doxorubicin (Adriamycin)

1) solid tumors, leukemias, lymphomas
2) makes ROS; non-covalently intercalate in DNA --> breaks DNA --> decr replication
3) cardiotoxicity* (dilated cardiomyopathy; use dexrazoxane, Fe chelator, to prevent), myelosuppression, alopecia; toxic to tissues following extravasation
4) N/A

9

Daunorubicin

1) solid tumors, leukemias, lymphomas
2) makes ROS; non-covalently intercalate in DNA --> breaks DNA --> decr replication
3) cardiotoxicity* (dilated cardiomyopathy; use dexrazoxane, Fe chelator, to prevent), myelosuppression, alopecia; toxic to tissues following extravasation
4) N/A

10

Bleomycin

1) testicular CA, Hodgkin's lymphoma
2) ROS formation --> causes breaks in DNA strands
3) pulm fibrosis*, skin changes; minimal myelosuppression
4) N/A

11

Cyclophosphamide

1) solid tumors, leukemia, lymphoma, some brain CAs
2) alkylating agent: covalently X-link DNA at guanine N-7
3) myelosuppression; hemorrhagic cystitis (partly prevent w/ mesna, thiol grp of mesna binds toxic metabolite)
4) need liver bioactivation

12

Ifosfamide

1) solid tumors, leukemia, lymphoma, some brain CAs
2) alkylating agent: covalently X-link DNA at guanine N-7
3) myelosuppression; hemorrhagic cystitis (partly prevent w/ mesna, thiol grp of mesna binds toxic metabolite)
4) need liver bioactivation

13

Carmustine

1) brain tumors (incl glioblastoma multiforme)
2) alkylating agent: nitrosourea
3) CNS toxicity: dizziness, ataxia
4) needs bioactivation; X's BBB --> CNS

14

Lomustine

1) brain tumors (incl glioblastoma multiforme)
2) alkylating agent: nitrosourea
3) CNS toxicity: dizziness, ataxia
4) needs bioactivation; X's BBB --> CNS

15

Semustine

1) brain tumors (incl glioblastoma multiforme)
2) alkylating agent: nitrosourea
3) CNS toxicity: dizziness, ataxia
4) needs bioactivation; X's BBB --> CNS

16

Streptozocin

1) brain tumors (incl glioblastoma multiforme)
2) alkylating agent: nitrosourea
3) CNS toxicity: dizziness, ataxia
4) needs bioactivation; X's BBB --> CNS

17

Busulfan

1) CML; also to ablate BM before BMT
2) alkylating agent
3) pulm fibrosis*; hyperpigmentation

18

Vincristine

1) solid tumors, leukemias, lymphomas
2) microtubule inhibitor: alkaloid that binds to tubulin in M phase + blocks polymerization so mitotic spindle can't form
3) neurotoxicity: areflexia, periph neuritis; paralytic ileus

19

Vinblastine

1) solid tumors, leukemias, lymphomas
2) microtubule inhibitor: alkaloid that binds to tubulin in M phase + blocks polymerization so mitotic spindle can't form
3) BM suppression (VinBLASTine BLASTS Bone Marrow)

20

Paclitaxel

1) ovarian + breast carcinomas
2) microtubule inhibitor: hyperstabilizes polymerized microtubules in M phase so mitotic spindle can't break down (blocks anaphase)
3) myelosuppression, hypersensitivity
4) N/A

21

Cisplatin

1) testicular, bladder, ovary, lung carcinomas
2) X-links DNA
3) nephrotoxicity (prevent w/ amifostine/ROS scavenger and chloride diuresis), acoustic nerve damage
4) N/A

22

Carboplatin

1) testicular, bladder, ovary, lung carcinomas
2) X-links DNA
3) nephrotoxicity (prevent w/ amifostine/ROS scavenger and chloride diuresis), acoustic nerve damage

23

Etoposide

1) solid tumors, leukemias, lymphomas
2) topo II inhibitor --> incr DNA degradation
3) myelosuppression, GI irritation, alopecia
4) N/A

24

Teniposide

1) solid tumors, leukemias, lymphomas
2) topo II inhibitor --> incr DNA degradation
3) myelosuppression, GI irritation, alopecia
4) N/A

25

Hydroxyurea

1) melanoma, CML, sickle cell dz (incr HbF)
2) inhibits ribonucleotide reductase --> decr DNA syn (S-phase specific)
3) BM suppression, upset GI
4) N/A

26

Prednisone

1) CA chemotx: CLL, non-Hodgkin's lymphomas; immunosuppressant (autoimmune dz)
2) glucocorticoid; may trigger apoptosis; may work on non-dividing cells
3) Cushing-like sx's; immunosuppression, cataracts*, acne, osteoporosis, HTN, peptic ulcers*, hyperglycemia, psychosis*
4) N/A

27

Prednisolone

1) CA chemotx: CLL, non-Hodgkin's lymphomas; immunosuppressant (autoimmune dz)
2) glucocorticoid; may trigger apoptosis; may work on non-dividing cells
3) Cushing-like sx's; immunosuppression, cataracts*, acne, osteoporosis, HTN, peptic ulcers*, hyperglycemia, psychosis
4) N/A

28

Tamoxifen

1) breast CA tx + prophylaxis; prevent osteoporosis
2) SERM: R antagonist in breast + agonist in bone; block estrogen binding to ER+ cells
3) partial agonist in endometrium --> incr endometrial CA risk; "hot falshes"
4) compare toxicity to raloxifene

29

Raloxifene

1) breast CA tx + prophylaxis; prevent osteoporosis
2) SERM: R antagonist in breast + agonist in bone; block estrogen binding to ER+ cells
3) no incr in endometrial carcinoma b/c it's an endometrial antagonist
4) compare toxicity to tamoxifen

30

Trastuzumab (Herceptin)

1) HER-2 (+) breast CA
2) monoclonal ab against HER-2 (c-erbB2), a tyrosine kinase --> kill breast CA cells taht overexpress HER-2 (ab-dependent cytotoxicity)
3) cardiotoxicity
4) N/A

31

Imatinib (Gleevec)

1) CML, GI stromal tumors
2) Ph chr bcr-abl tyroxine kinase inhibitor
3) fluid retention
4) N/A

32

Rituximab

1) non-Hodgkin's lymphoma, rheumatoid arthritis (w/ MTX)
2) monoclonal ab against CD20 (found on most B-cell neoplasms)
3) N/A
4) N/A

33

Vemurafenib

1) metastatic melanoma
2) small molec inhibitor of B-Raf kinases that have V600E mute
3) N/A
4) N/A

34

Bevacizumab

1) solid tumors
2) monoclonal ab against VEGF --> inhibits angiogenesis
3) N/A
4) N/A

35

Cladribine

1) Hairy Cell Leukemia*
2) Adenosine analog, resistant to Adenosine Deaminase*. thus Cladribine is able to achieve really high intracellular concentrations -> incorporated into DNA --> DNA breaks.
4) penetrates the CNS