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Flashcards in HemOnc--Pharmacology Deck (53):
1

heparin moa?

cofactor for atIII, decreases thrombin and factor Xa

2

direct thrombin inhibitors

argatroban, bivalirudin--derivatives of hirudin

3

in HIT, what to use for anticoagulation?

argatroban or bivalirudin

4

warfarin moa?

interferes with synthesis and gamma-carboxlyation of vitamin K dependent clotting factors (2, 7, 9, 10 and proteins C and S)

5

how to follow warfarin effect?

extrinsic pathway--use PT/INR to monitor

6

warfarin tox?

bleeding, teratogenic (do not use in preg); skin/tissue necrosis esp if patient has genetic protein C/S deficiency; drug-drug interactions

7

Direct factor Xa inhibitors?

apixaban, rivaroxaban;

8

aspirin overdose? A/B derrangement

initially a respiratory alkalosis then superimposed by metabolic acidosis

9

ADP receptor inhibitors? moa?

clopidogrel, ticlopidine, prasugrel, ticagrelor; inhibits platelet aggregation by irreversibly blocking ADP receptors and prevents GPIIb/IIIa receptor expression, preventing fibrinogen binding

10

ADP receptor inhibitor that can cause neutropenia?

ticlopidine

11

ADP receptor inhibitors can cause..?

TTP or HUS

12

cilostazol, dipyradamole?

PDEIII inhibitors, increase cAMP in platelets-->inhibiting platelet aggregation; also vasodilates

13

GP IIb/IIIa inhibitors?

abciximab,eptifibatide, tirofiban; can cause thrombocytopenia

14

Cell cycle effect: vinca alkaloids and taxols

inhibit M phase

15

Cell cycle effect: antimetabolites

S phase; eg MTX, 5-FU, cytarabine, 6MP, 6TG, hdroxyurea

16

Cell cycle effect: etoposide

S and G2 phase

17

Cell cycle effect: bleomycin

G2 phase

18

methotrexate moa?

folic acid analog that inhibits DHF reductase-->decreases dTMP-->decreases DNA and protein synthesis

19

methotrexate tox?

myelosuppression (reverse with folinic acid); macrovesicular fatty change in liver, mucositis, teratogen

20

5-FU moa?

pyrimide analog bioactivated to 5F-dUMP which covalently complexes folic acid to inhibit thymidylate synthase-->decrease dTMP-->decrease DNA and protein synthesis

21

5FU tox?

myelosupression which cannot be reversed with folinic acid; overdose rescue with uridine; photosensitivty

22

cytarabine moa?

pyrimidine analog-->inhibits DNA polymerase;

23

cytarabine tox?

pancytopenia

24

azathioprine, 6MP, 6TG moa? tox?

purine (thiol) analogs-->decrease de novo purine synthesis; activated by HGPRT; tox to bone marrow/GI/liver

25

do not mix azathioprine or 6MP with...?

allopurinol (XO inhibitor)

26

dactinomycin moa? tox? use?

intercalates DNA; myelosuppresion; used in wilms tumor, ewing sarcoma, rhabomyosarcoma; childhood tumors

27

doxorubicin, daunorubicin moa? tox?

generate free radicals-->intercalate in DNA-->breaks DNA->decr replication; used in solid tumors, leukemias, lymphomas; cardiotoxic (dilated CM), myelosuppresion, alopecia

28

treat doxorubicin tox?

dexrazoxane (iron chelating agent) used to prevent cardiotoxicity

29

Bleomycin moa? tox?

induces free radical formation-->DNA strand breaks; pulmonary fibrosis, skin changes, mucositis; hyperpigmentation; use in testicular cancer/hodgkins

30

which antitumor antibiotic has minimal myelosuppresion?

bleomycin

31

what are some alkylating agents?

cyclophosphamide, ifosfamide, nitrosoureas, busulfan; all cross link DNA

32

cyclophosphamide, ifosfamide moa?

covalently x-link (interstrand) DNA at guanine N-7; requires bioactivation by liver

33

cyclophosphamide tox?

myelosuppresion; hemorrhagic cystitis that can be prevented with mesna (thiol group bind toxic metabolites)

34

nitrosuoureas moa? tox?

requires bioactivation and cross links DNA; CNS tox (convulsions/dizziness/ataxia)

35

what type of tumors is nitrosoureas specially used for?

CNS tumors including glioblastoma multiforme because it can penetrate BBB

36

busulfan is used for?

CML; and to ablate bone marrow before transplant

37

busulfan tox?

severe myelosuppression, pulmonary fibrosis, hyperpigmentation

38

what are some microtubule inhibitors?

vincristine, vinblastine, paclitaxols and other -taxols

39

vincristine, vinblastine moa? use?

vinca alkaloids that bind B-tubulin, inhibit polymerization and prevent mitotic spindle formation (M phase arrest); use in solid tumors/leukemia/lymphomas

40

vincristine tox?

neurotoxicity (areflexia, peripheral neuritis, paralytic ileus)

41

vinblastine tox?

bone marrow supression

42

paclitaxol moa?

hyperstabilize polymerized mtubules in M phase so that mitotic spindle cannot break down; use in ovarian and breast carcinomas

43

paclitaxel tox?

myelosuppression, alopecia, hypersensitivity

44

cisplatin, carboplatin moa? use?

cross links DNA; testicular/bladder/ovary/lung carcinoma

45

cisplatin/carboplatin tox?

nephrotoxic, acoustic nerve damage

46

prevent nephrotox of cisplatin?

amifostine (free radical scavenger) and chloride diuresis

47

etoposide, teniposide moa? tox?

inhibits topoisomerase II-->increase DNA degradation; myelosuppresion, GI irritation, alopecia

48

irinotecan, topotecan moa? tox?

topoisomerase I inhibition and prevents DNA unwinding and replication; severe myelosuppresion and diarrhea

49

hydroxyurea moa? tox?

inhibits ribonucleotide reductase-->decreases dna synthesis (S phase specific); bone marrow suppression, GI upset

50

hydroxyurea use?

melanoma, CML, sickle cell disease (increased HbF)

51

traztuzumab tox?

cardiotoxic

52

imatinib moa? tox?

tyrosine kinase inhibitor of bcr-abl (CML) and c-kit (GI and stromal tumors); fluid retention

53

test before giving rituximab?

increased risk of PML, test for JC virus