HemOnc--Pharmacology Flashcards

1
Q

heparin moa?

A

cofactor for atIII, decreases thrombin and factor Xa

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2
Q

direct thrombin inhibitors

A

argatroban, bivalirudin–derivatives of hirudin

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3
Q

in HIT, what to use for anticoagulation?

A

argatroban or bivalirudin

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4
Q

warfarin moa?

A

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

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5
Q

how to follow warfarin effect?

A

extrinsic pathway–use PT/INR to monitor

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6
Q

warfarin tox?

A

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

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7
Q

Direct factor Xa inhibitors?

A

apixaban, rivaroxaban;

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8
Q

aspirin overdose? A/B derrangement

A

initially a respiratory alkalosis then superimposed by metabolic acidosis

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9
Q

ADP receptor inhibitors? moa?

A

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

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10
Q

ADP receptor inhibitor that can cause neutropenia?

A

ticlopidine

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11
Q

ADP receptor inhibitors can cause..?

A

TTP or HUS

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12
Q

cilostazol, dipyradamole?

A

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

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13
Q

GP IIb/IIIa inhibitors?

A

abciximab,eptifibatide, tirofiban; can cause thrombocytopenia

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14
Q

Cell cycle effect: vinca alkaloids and taxols

A

inhibit M phase

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15
Q

Cell cycle effect: antimetabolites

A

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

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16
Q

Cell cycle effect: etoposide

A

S and G2 phase

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17
Q

Cell cycle effect: bleomycin

A

G2 phase

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18
Q

methotrexate moa?

A

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

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19
Q

methotrexate tox?

A

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

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20
Q

5-FU moa?

A

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

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21
Q

5FU tox?

A

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

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22
Q

cytarabine moa?

A

pyrimidine analog–>inhibits DNA polymerase;

23
Q

cytarabine tox?

A

pancytopenia

24
Q

azathioprine, 6MP, 6TG moa? tox?

A

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

25
Q

do not mix azathioprine or 6MP with…?

A

allopurinol (XO inhibitor)

26
Q

dactinomycin moa? tox? use?

A

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

27
Q

doxorubicin, daunorubicin moa? tox?

A

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

28
Q

treat doxorubicin tox?

A

dexrazoxane (iron chelating agent) used to prevent cardiotoxicity

29
Q

Bleomycin moa? tox?

A

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

30
Q

which antitumor antibiotic has minimal myelosuppresion?

A

bleomycin

31
Q

what are some alkylating agents?

A

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

32
Q

cyclophosphamide, ifosfamide moa?

A

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

33
Q

cyclophosphamide tox?

A

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

34
Q

nitrosuoureas moa? tox?

A

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

35
Q

what type of tumors is nitrosoureas specially used for?

A

CNS tumors including glioblastoma multiforme because it can penetrate BBB

36
Q

busulfan is used for?

A

CML; and to ablate bone marrow before transplant

37
Q

busulfan tox?

A

severe myelosuppression, pulmonary fibrosis, hyperpigmentation

38
Q

what are some microtubule inhibitors?

A

vincristine, vinblastine, paclitaxols and other -taxols

39
Q

vincristine, vinblastine moa? use?

A

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

40
Q

vincristine tox?

A

neurotoxicity (areflexia, peripheral neuritis, paralytic ileus)

41
Q

vinblastine tox?

A

bone marrow supression

42
Q

paclitaxol moa?

A

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

43
Q

paclitaxel tox?

A

myelosuppression, alopecia, hypersensitivity

44
Q

cisplatin, carboplatin moa? use?

A

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

45
Q

cisplatin/carboplatin tox?

A

nephrotoxic, acoustic nerve damage

46
Q

prevent nephrotox of cisplatin?

A

amifostine (free radical scavenger) and chloride diuresis

47
Q

etoposide, teniposide moa? tox?

A

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

48
Q

irinotecan, topotecan moa? tox?

A

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

49
Q

hydroxyurea moa? tox?

A

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

50
Q

hydroxyurea use?

A

melanoma, CML, sickle cell disease (increased HbF)

51
Q

traztuzumab tox?

A

cardiotoxic

52
Q

imatinib moa? tox?

A

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

53
Q

test before giving rituximab?

A

increased risk of PML, test for JC virus