FA HemeOnc Pharm

Question 1

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

Answer 1

Heparin

Question 2

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

Answer 2

Argatroban, bivalirudin

Question 3

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

Answer 3

Warfarin

Question 4

Bind and directly inhibit Factor Xa

Answer 4

Direct factor Xa inhibitors

Apixaban, rivaroxaban

Question 5

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

Answer 5

Thrombolytics

Question 6

Irreversible inhibits COX by covalent acetylation

Answer 6

ASA

Question 7

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

Answer 7

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

Question 8

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

Answer 8

Cilostazole, dipyridamole

Question 9

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

Answer 9

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

Question 10

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

Answer 10

Methotrexate

Question 11

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

Answer 11

5-FU

Question 12

Pyrimadine analog –> inhibition of DNA polymerase

Answer 12

Cytarabine

Question 13

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

Answer 13

Azathioprine, 6-MP, 6-TG

Question 14

Antitumor antibiotic that intercalates in DNA

Answer 14

Dactinomycin

Question 15

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

Answer 15

Doxorubicin, daunorubicin

Question 16

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

Answer 16

Bleomycin

Question 17

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

Answer 17

Busulfan

Question 18

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

Answer 18

Cyclophophamide, ifosfaminde

Question 19

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

Answer 19

Nitrosoureas (carmustine, lomustine, semustine, streptozocin)

Question 20

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

Answer 20

Vincristine, vinblastine

Question 21

Microtubule inhibitor

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

Answer 21

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

Question 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)

Answer 22

Cisplatin, carboplatin

Question 23

Inhibit topoisomerase II –> DNA degradation

Answer 23

Etoposide, teniposide

Question 24

Inhibit topoisomerase I and prevent DNA unwinding and replication

Answer 24

Irinotecan, topotecan

Question 25

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

Answer 25

Hydroxyurea

Question 26

Glucocorticoids used in cancer chemotherapy; may trigger apoptosis

Answer 26

Prednisone, prednisolone

Question 27

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

Answer 27

Tamoxifen (partial endometrial agonist) | raloxifene (endometrial antagonist)

Question 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

Answer 28

Trastuzumab

Question 29

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

Answer 29

Gleevac

Question 30

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

Answer 30

Rituximab

Question 31

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

Answer 31

Vemurafenib

Question 32

Monoclonal antibody against VEGF. Inhibits angiogensis

Answer 32

Bevacizumab

Question 33

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

Answer 33

Tamoxifen

Question 34

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

Answer 34

Raloxifene

Question 35

Ex: abciximab, eptifibatide, tirofiban

Answer 35

GP IIb/IIIa inhibitors

Question 36

Ex: clopidogrel, ticlopidine, prasugrel, ticagrelor

Answer 36

ADP receptor blockers

Question 37

Ex: Apixaban, rivaroxaban

Answer 37

Direct factor Xa inhibitors

Question 38

Reverse MTX myelosuppression with

Answer 38

leukovorin

Question 39

Treat 5FU overdose with

Answer 39

uridine

Question 40

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

Answer 40

Azathioprine, 6-MP

Question 41

Prevent doxorubicin/daunorubicin cardiotoxicity with

Answer 41

dexrazoxane

Question 42

Prevent cyclophosphamide/ifosfamide hemorrhagic cystitis with

Answer 42

mesna (thiol group of mesa binds toxic metabolites)

Question 43

Prevent cisplatin/carboplatin nephrotoxicity with

Answer 43

amifostine (free radical scavenger) and chloride diuresis

Question 44

SE cisplatin/carboplatin

Answer 44

acoustic nerve damage and nephrotoxicity

Question 45

SE vincristine

Answer 45

peripheral neuropathy

Question 46

SE bleomycin and busulfan

Answer 46

pulmonary fibrosis

Question 47

SE doxorubicin

Answer 47

cardiotoxicity

Question 48

SE trastuzumab

Answer 48

cardiotoxicity

Question 49

SE cyclophophamide

Answer 49

Hemorrhagic cystitis

Question 50

SE: 5FU, 6MP, MTX

Answer 50

myelosuppression

Question 51

Ex: enoxaparin, dalteparin

Answer 51

LMWH