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Flashcards in antineoplastics Deck (26):
1

Methotrexate

folic acid analog, competitively inhibits dihydrofolate reductase -> dec. thymidine synthesis. Tx: CA, abortion, RA, psoriasis, IBD, vasculitis. Tx: myelosuppresion (reversible w/folate), hepatotox, mucositis, pulm fibrosis.

2

5-FU

pyrimidine analog: inhibits thymidylate synthase -> dec. thymidine synthesis. Tx: colon pancreatic, basal cell CA (topical). tox: myelosuppression (irreversible)

3

6-MP

dec. de novo purine synthesis

4

hydroxyurea

inhibits ribonucleotide reductase -> dec. DNA synthesis. Tx: melanoma, CML, HbSS. tox: severe myelosupp, GI upset

5

alkylating agents

cross-links DNA

6

cisplatin, carboplatin

cross-links DNA. Tx: testicular, bladder, ovary, lung CA. tox: nephrotox (prevent w/amifostine (free rad scavenger) and chloride diuresis), ototox

7

bleomycin

induces free radical damage -> DNA strand breakage. Tx: testicular CA, Hodgkins. tox: pulm. fibrosis, inc. skin pigment, mucositis. minimal myelosupp.

8

dactinomycin

DNA intercalator. Tx: wilms, ewing, rhabdomyosarcoma = CHILDHOOD tumors. tox: myelosupp.

9

doxorubicin

DNA intercalator + generates free radicals -> DNA breaks. Tx: solid tumors, leukemia, lymphoma. tox: cardiotoxic (dilated. prevent w/Fe chelator dexrazoxane), myelosupp. alopecia. toxic if extravasates.

10

etoposide, teniposide

inhibits topoisomerase II (makes DNA strand breaks to edit DNA) - like fluoroquinolones. Tx: solid tumors (testicular, small cell lung), leukemias, lymphomas. tox: myelosupp, GI upset, alopecia.

11

irinotecan, topotecan

inhibits topoisomerase I and prevents DNA unwinding + replication. Tx: colon Ca (irino), ovarian and small cell lung (topo). tox: severe myelosupp, diarrhea.

12

vinca alkaloids (vincristine, vinblastine)

inhibit microtubule formation (M phase arrest). Tx: solid tumors, leukemias, Hodgkins (blastine), nonH lymphoma (cristine). tox: cristine: neurotox. blastine: blasts bone marrow (myelosupp).

13

paclitaxel, other taxols

inhibits microtubule disassembly (stuck in M phase, no anaphase). Tx: ovarian and breast CA. tox: myelosupp, alopecia, hypersensitivity.

14

azathioprene

= purine (thiol) analog. metabolized into 6-MP. dec. de novo purine synthesis. metabolized by xanthine oxidase

15

cladribine

purine analog. many MoAs: inhibits DNA polymerase, -> DNA strand breaks, etc. Tx: hairy cell leukemia. tox: myelosuppression, nephrotox, neurotox.

16

cytarabine

pyrimidine analog: inhibits DNA polymerase. Tx: AML, lymphomas. tox: leukopenia, dec. plts, megaloblastic anemia.

17

busulfan

cross-links DNA. Tx: CML, pre-transplant BM ablation. tox: severe myelosupp, pulm fibrosis, hyperpigmentation

18

cyclophosphamide

crosslinks DNA at guanine N-7. requires activation in liver. Tx: solid tumors, leukemia, lymphoma. tox: myelosupp., hemorrhagic cystitis. prevent (partially) w/mesna: binds toxic metabolites

19

nitrosoureas (carmustine, lomustine, semustine, streptozocin)

crosslinks DNA. requires activation. crosses BBB. Tx: brain tumors (inc. glioblastoma). tox: CNS Sx

20

bevacizumab

monoclonal Ab against VEGF. Tx: solid tumors (colon, renal cell). tox: hemorrhage, blood clots, dec. wound healing.

21

erlotinib

EGFR TK inhibitor. Tx: NSC lung CA. tox: rash

22

imatinib

TK inhibitor of BCR-ABL and c-kit (GI stromal tumors). tox: fluid retention

23

rituximab

monoclonal Ab against CD20. Tx: NH lymphoma, CLL, IBD, RA. tox: inc. risk of PML

24

tamoxifen, raloxifene

SERM: breast antagonist, bone agonist. tox: tamox: endometrial agonist.

25

trastuzumab

monoclonal Ab against HER-2 (TK receptor). Tx: HER-2+ breast and gastric CA. tox: cardiotox

26

vemurafenib

BRAF inhibitor. Tx: BRAF+ melanoma.