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Flashcards in FA HemeOnc Pharm Deck (51):
1

Cofactor for the activation of antithrombin, dec thrombin and dec factor Xa; short half-life

Heparin

2

Derivatives of hirudin, the anticoagulant used by leeches; inhibits thrombin directly. Used instead of heparin for anti coagulating patients with HIT.

Argatroban, bivalirudin

3

Interferes with normal synthesis and gamma-carboxylation of vitamin K-dependent clotting factors 2, 7, 9, and 10.

Warfarin

4

Bind and directly inhibit Factor Xa

Direct factor Xa inhibitors
(Apixaban, rivaroxaban)

5

Directly or indirectly aid conversion of plasminogen to plasmin, which cleaves thrombin and fibrin clots.

Thrombolytics

6

Irreversible inhibits COX by covalent acetylation

ASA

7

Inhibit platelet aggregation by irreversibly blocking ADP receptors. Inhibit fibrinogen binding by preventing GP IIb/IIIa from binding to fibrinogen.

ADP receptor blockers (clopidogrel, ticlopidine, prasugrel, ticagrelor)

8

Phosphodiesterase III inhibitor; increase cAMP in platelets, thus inhibit platelet aggregation; vasodilators

Cilostazole, dipyridamole

9

Bind to GP IIb/IIIa receptor on activated platelets, preventing aggregation.

GP IIb/IIIa inhibitors (abciximab, eptifibatide, tirofiban)

10

Folic acid analog that inhibits DHF --. dec dTMP --> dec DNA and protein synthesis

Methotrexate

11

Pyrimidine analog bioactivated to 5F-dUMP, which covalently complexes folic acid; complex inhids thymidylate synthase --> dec dTMP --> dec DNA and protein synthesis

5-FU

12

Pyrimadine analog --> inhibition of DNA polymerase

Cytarabine

13

Purine (thiol analogs) --> decreased de novo purine synthesis, activated by HGPRT

Azathioprine, 6-MP, 6-TG

14

Antitumor antibiotic that intercalates in DNA

Dactinomycin

15

Antitumor antibiotic that generates free radicals; intercalate in DNA --> DNA breaks --> decreased replication

Doxorubicin, daunorubicin

16

Antitumor antibiotic that induces free radical formation, which causes breaks in DNA strands

Bleomycin

17

Alkylating agent that cross-links DNA (used for CML)

Busulfan

18

Alkylating agent that covalently cross-links (interstrand) DNA at guanine N-7; requires bioactivation by liver

Cyclophophamide, ifosfaminde

19

Alkylating agent that cross-links DNA; requires biactivation; crosses BBB to CNS (so used for brain tumors, including glioblastoma multiforme)

Nitrosoureas (carmustine, lomustine, semustine, streptozocin)

20

Microtubule inhibitor
Vinca alkaloids that bind beta-tubulin, inhibit its polymerization into mircotubules, thereby preventing mitotic spindle formation (M-phase arrest)

Vincristine, vinblastine

21

Microtubule inhibitor
Hyperstabilize polymerized microtubules in M phase so that mitotic spindle cannot break down (anaphase cannot occur).

Paclitaxel, other taxols (it is taxing to stay polymerized!)

22

Platinum-containing chemotherapy drugs that cross-link DNA; SEs include acoustic nerve damage and nephrotoxicity (prevent w/ amigostine (free radical scavenger) and chloride diuresis)

Cisplatin, carboplatin

23

Inhibit topoisomerase II --> DNA degradation

Etoposide, teniposide

24

Inhibit topoisomerase I and prevent DNA unwinding and replication

Irinotecan, topotecan

25

Inhibits ribonuclease reductase --> decreased DNA synthesis (s-phase specific); also increases HbF

Hydroxyurea

26

Glucocorticoids used in cancer chemotherapy; may trigger apoptosis

Prednisone, prednisolone

27

SERMs - receptor antagonists in breast and agonists in bone. Block the binding of estrogen to ER+ cells

Tamoxifen (partial endometrial agonist)
raloxifene (endometrial antagonist)

28

Monoclonal antibody against HER-2 (c-erbB2), a tyrosine kinase receptor. Helps kill breast cancer cells that over express HER-2 through inhibition of HER2-initiated cellular signaling and antibody-dependent cytotoxicity

Trastuzumab

29

Tyrosine kinase inhibitor of bcr-abl (Ph chromosome fusion gene in CML) and c-Kit (common in GI stromal tumors)

Gleevac

30

Monoclonal antibody against CD20, which is found on most B-cell neoplasms

Rituximab

31

Small molecule inhibitor of forms of the B-raf kinase with the V600E mutation

Vemurafenib

32

Monoclonal antibody against VEGF. Inhibits angiogensis

Bevacizumab

33

SERM - antagonist in breast, agonist in bone and partial agonist in endometrium (used for ER+ breast cancer)

Tamoxifen

34

SERM - antagonist in breast and endometrium, agonist in bone (used for osteoporosis)

Raloxifene

35

Ex: abciximab, eptifibatide, tirofiban

GP IIb/IIIa inhibitors

36

Ex: clopidogrel, ticlopidine, prasugrel, ticagrelor

ADP receptor blockers

37

Ex: Apixaban, rivaroxaban

Direct factor Xa inhibitors

38

Reverse MTX myelosuppression with

leukovorin

39

Treat 5FU overdose with

uridine

40

Two drugs that are metabolized by xanthine oxidase and thus have increased toxicity with allopurinol

Azathioprine, 6-MP

41

Prevent doxorubicin/daunorubicin cardiotoxicity with

dexrazoxane

42

Prevent cyclophosphamide/ifosfamide hemorrhagic cystitis with

mesna (thiol group of mesa binds toxic metabolites)

43

Prevent cisplatin/carboplatin nephrotoxicity with

amifostine (free radical scavenger) and chloride diuresis

44

SE cisplatin/carboplatin

acoustic nerve damage and nephrotoxicity

45

SE vincristine

peripheral neuropathy

46

SE bleomycin and busulfan

pulmonary fibrosis

47

SE doxorubicin

cardiotoxicity

48

SE trastuzumab

cardiotoxicity

49

SE cyclophophamide

Hemorrhagic cystitis

50

SE: 5FU, 6MP, MTX

myelosuppression

51

Ex: enoxaparin, dalteparin

LMWH