hem/onc Flashcards

1
Q

heparin MOA?

A

activates antithrombin –> decreased thrombin and Xa

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2
Q

LMWH vs heparin?

A

LMWH (enoxaparin, dalteparin) and fondaparinux = FXa inhib

  • more Xa action
  • better bioavail
  • longer T1/2
  • don’t need monitoring
  • less easily reversible
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3
Q

how to reverse heparin?

A

protamine sulfate ( + charge –> binds heparin)

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4
Q

HIT?

A

IgG against heparin-bound platelet factor 4 (PF4)

Ab-heparin-PF4 complex –> platelet activation –> thrombosis and TCP

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5
Q

direct thrombin inhibitors?

A

argatroban
bivalirudin
dabigatran

** alternatives to heparin in pts with HIT

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6
Q

warfarin MOA?

A

blocks gamma-carboxylation of vit K dependent factors
metabolism affected by polymorphisms in VKORC1 gene (vit K epoxide reductase complex)

** affects extrinsic pathway, PT/INR

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7
Q

mechanism of warfarin-induced tissue necrosis?

A

small vessel microthromboses

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8
Q

direct F Xa inhibitors?

A

apixaban, rivaroxaban

uses: tx and ppx for DVT/PE, stroke ppx in afib

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9
Q

how to tx thrombolytic tox?

A

aminocaproic acid (inhibits fibrinolysis)

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10
Q

aspirin MOA?

A

irreversible COX1/2 inhib via acetylation
increases bleeding time, decreases TXA2 and PGs

** no effect on PT or PTT

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11
Q

ADP receptor inhibitors/

A

clopidogrel, prasugrel, ticagrelor, ticlopidine
irreversible block of ADP receptor –> prevent expression of GPIIb/IIIa –> inhibit platelet agg

    • ticagrelor = reversible
    • ticlopidine –> neutropenia
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12
Q

cilostazol, dipyramidole?

A

PDEIII inhib –> increased cAMP in platelets –> inhib of aggregation; vasodilation

    • used in intermittent claudication, coronary syndromes
    • tox: nausea, HA, flushing, hypoT, abd pain
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13
Q

GP IIb/IIIa inhibs?

A

abciximab, eptifibatide, tirofiban
used for unstable angina, PTCA

** tox: bleeding, TCP

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14
Q

antimetabolites that are purine analogs?

A

6MP
azathioprine
cladribine

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15
Q

azathioprine/6MP MOA?

A

purine analogs, activated by HGPRT

inhibit de novo purine synth

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16
Q

azathioprine/6MP uses?

A

rejection ppx, RA, IBD, SLE

weaning pts off steroids in chronic dz

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17
Q

azathioprine/6MP toxicity?

A

myelosuppression
GI
liver

** increased toxicity with allopurinol and febuxostat (metab by XO)

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18
Q

cladribine MOA?

A

purine analog

multiple mechanisms: DNA pol inhib, DNA breaks

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19
Q

cladribine uses?

A

hairy cell leukemia

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20
Q

cladribine toxicity?

A

myelosuppresssion
nephrotoxicity
neurotoxicity

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21
Q

antimetabolites that inhibit pyrimidine synthesis?

A

cytarabine
5FU
methotrexate

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22
Q

cytarabine MOA?

A

pyrimidine analog

inhibit DNA pol

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23
Q

cytarabine uses?

A

leukemia - AML

lymphomas

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24
Q

cytarabine toxicity?

A

pancytopenia, megaloblastic anemia

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25
5FU MOA?
pyrimidine analog, activated to 5F-dUMP --> covalently complexes folate complex inhibits thymidylate synthase --> decreased dTMP --> decreased DNA synthesis
26
5FU uses?
colon cancer pancreatic cancer topical --> basal cell carcinoma
27
5FU toxicity?
myelosuppresion ** NOT reversible with leucovorin (folinic acid)
28
MTX MOA?
folic acid analog | competitive inhibition of DHFR --> decreased dTMP --> decreased DNA synthesis
29
MTX uses?
cancer: ALL, lymphoma, choriocarcinoma, sarcoma | non-cancer: ectopic preg/abortion, RA, psoriasis, IBD, vasculitis
30
MTX toxicity?
myelosuppression hepatotoxicity mucositis pulmonary fibrosis ** myelosuppresion REVERSIBLE with leucovorin (folinic acid) - contrast to 5FU
31
bleomycin MOA?
free radical formation --> DNA strand breaks
32
bleomycin uses?
testicular cancer | Hodgkin lymphoma
33
bleomycin toxicity?
pulmonary fibrosis skin pigmentation mucositis
34
dactinomycin MOA?
intercalates in DNA
35
dactinomycin uses?
childhood tumors! | Wilms, Ewing, rhabdomyo
36
dactinomycin toxicity?
myelosuppression
37
doxo/daunorubicin MOA?
free radicals, intercalates in DNA | DNA breaks --> decreased replication
38
doxo/daunorubicin uses?
solid tumors leukemias lymphomas
39
doxo/daunorubicin toxicity?
dilated cardiomyopathy myelosuppression alopecia ** DEXRAZOXANE prevents cardiomyopathy
40
busulfan MOA?
DNA crosslinking
41
busulfan uses?
CML | BM ablation prior to txp
42
busulfan toxicity?
SEVERE myelosuppression pulmonary fibrosis skin pigmentation
43
cyclophosphamide, ifosfamide MOA?
cross link DNA at guanine-N7 | need bioactivation in liver
44
cyclophosphamide/ifosfamide uses?
solid tumors leukemia lymphomas
45
cyclophos/ifos toxicity?
myelosuppression hemorrhagic cystitis ** MESNA partially prevents hemorrhagic cystitis
46
nitrosureas MOA?
(carmustine, lomustin, semustine, streptoxocin) need bioactivation cross BBB --> CNS cross link DNA
47
nitrosureas use?
brain tumors - GBM, etc
48
nitrosureas toxicity?
CNS - convulsions, dizziness, ataxias
49
taxol MOA?
hyperstabilize microtubules in M phase --> prevent progression to anaphase
50
taxol uses?
ovarian and breast ca
51
taxol toxicity?
myelosuppression alopecia hypersensitivity
52
vincristine/blastine MOA?
bind beta-tubulin --> inhibit polymerization into micrtubules --> prevent spindle formation - M phase arrest
53
vincristine/blastine uses?
solid tumors leukemias Hodgkin - vinblastine non-Hodgkin - vincristine
54
vincristine toxicity?
neurotoxicity - areflexia, peripheral neuritis, paralytic ileus
55
vinblastine toxicity?
myelosuppression
56
cisplatin/carboplatin?
cross link DNA used in testicular, bladder, ovary, lung carcinomas tox: nephro, oto ** AMIFOSTINE and saline diuresis prevent nephrotoxicity
57
Etoposide/teniposide?
inhibit topo II --> increased DNA degradation used in solid tumors (esp testicular and SCLC), leuk, lymph tox: myelosuppression, GI, alopecia
58
irinotecan/topotecan?
inhibit topo I --> prevent DNA unwinding/replication irinotecan --> colon cancer topotecan --> ovarian and SCLC tox: SEVERE myelosuppression, diarrhea
59
hydroxyurea?
inhibits ribonucleotide reductase --> decreased DNA synth used in melanoma, CML, sickle cell tox: SEVERE myelosuppression, diarrhea
60
prednisone used in which cancers?
CLL | non-Hodgkin
61
bevacizumab?
VEGF monoclonal Ab use: CRC, RCC tox: hemorrhage, clots, impaired wound healing
62
erlotinib?
EGFR tyr kinase inhib used: non small cell lung ca tox: rash
63
imatinib?
tyr kinase inhibition of BCR-ABL and c-kit used in CML, GI stromal tumors tox: fluid retention
64
rituximab?
anti-CD20 monoclonal Ab used in Non-Hodgkin, CLL, IBD, RA tox: increased risk of PML
65
tamoxifen/raloxifene?
SERMS tamoxifen: brca tx raloxifene: osteoporosis ppx tamoxifen tox: increased risk of endo ca, hot flashes raloxifene: no increase in endo ca
66
trastuzumab?
HER2 monoclonal Ab (tyr kinase) used in br ca and gastric ca tox: CARDIAC
67
vemurafenib?
small molecule inhib of BRAF oncogene + melanoma | used in metastatic melanoma