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Pharm II > Heme > Flashcards

Heme Flashcards

1
Q

Asprin

A

Analgesic, antipyretic, anti-inflammatory, anti-platelet

MOA:
Irreversible COX 1&2 inhibitor by covalent acetylation
Plts cant synth new COX
Increased Bleeding time,
Reduced TXA2 and PGs
No effect PT and PTT

Toxicity:
Gastric ulceration, CNVIII
Chronic use -> acute renal failure, interstitial nephritis, upper GI bleed
Reye syndrome w/ virus in peds
OD -> resp alkalosis and then superimposed metabolic acidosis

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2
Q

ibuprofen

A 
Analgesic
MOA:
reversible COX inhibitors
half-life ~2h
hold 1-2 days preop
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3
Q

Naproxen

A 
Analgesic
reversible cox inhibitor
Tmax 1-2h
half life 12-17h
Hold several days preop
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4
Q

Clopidogrel

A

ADP receptor inhibitor
MOA:
Inhibits plt aggregation; irreversibly blocks ADP receptors

Clinical:
ACS, Coronary Stenting, prophylactic for thrombotic stroke

Tox: TTP/HUS

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5
Q

Prasugrel

A

ADP receptor inhibitor
MOA:
Inhibits plt aggregation; irreversibly blocks ADP receptors

Clinical:
ACS, Coronary Stenting, prophylactic for thrombotic stroke

Tox: TTP/HUS

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6
Q

Ticagrelor

A

ADP receptor inhibitor
MOA:
Inhibits plt aggregation; irreversibly blocks ADP receptors

Clinical:
ACS, Coronary Stenting, prophylactic for thrombotic stroke

Tox: TTP/HUS

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7
Q

Heparin

A

Anticoagulant

MOA:
cofactor for activation of antithrombin. Reduces thrombin, Factor Xa and IIa
short half life

Clinical use:
imediate anticoagulation for PE, ACS, MI DVT.
used during pregnancy (wont cross placenta)
Follow PTT

Tox:
Bleeding, thrombocytopenia(HIT)
osteoporosis, DDI,
Reversal = protamine sulfate

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8
Q

Enoxaparin

A

Anti-coagulant
LMWH

MOA:
LMWH acts more on Factor Xa are cofactor for activation of antithrombin. Reduces thrombin,
longer half life

Clinical use:
imediate anticoagulation for PE, ACS, MI DVT.
used during pregnancy (wont cross placenta)
SC administration
No lab monitoring

Not easily reversible

Tox:
Bleeding, thrombocytopenia(HIT)
osteoporosis, DDI,

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9
Q

Dalteparin

A

Anti-coagulant
LMWH

MOA:
LMWH acts more on Factor Xa are cofactor for activation of antithrombin. Reduces thrombin,
longer half life

Clinical use:
imediate anticoagulation for PE, ACS, MI DVT.
used during pregnancy (wont cross placenta)
SC administration
No lab monitoring

Not easily reversible

Tox:
Bleeding, thrombocytopenia(HIT)
osteoporosis, DDI,

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10
Q

Tinzaparin

A

Anti-coagulant
LMWH

MOA:
LMWH acts more on Factor Xa are cofactor for activation of antithrombin. Reduces thrombin,
longer half life

Clinical use:
imediate anticoagulation for PE, ACS, MI DVT.
used during pregnancy (wont cross placenta)
SC administration
No lab monitoring

Not easily reversible

Tox:
Bleeding, thrombocytopenia(HIT)
osteoporosis, DDI,

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11
Q

Fondaparinux

A

Anti-coagulant
LMWH

MOA:
LMWH acts more on Factor Xa are cofactor for activation of antithrombin. Reduces thrombin,
longer half life

Clinical use:
immediate anticoagulation for PE, ACS, MI DVT.
used during pregnancy (wont cross placenta)
SC administration
No lab monitoring

Not easily reversible

Tox:
Bleeding, thrombocytopenia(HIT)
osteoporosis, DDI,

No reversal agent!!

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12
Q

Protamine sulfate

A

basic protein binds negatively charged heparins

Heparin reversal agent

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13
Q

warfarin

A 
Anticoagulant
MOA:
interferes w. gamma carboxylation of vit K dependent clotting factors II, VII, IX, X; proteins C&S
CYP450 metabolism
Extrinsic pathway 
Elevates PT
Long half-life

Clinical:
chronic anticoagulation (STEMI, venous thromboembolism prophylaxis, A.fib.
Not used in pregnancy
Follow PT/INR

Tox:
bleeding, teratogenic, skin/tissue necrosis

Reversal:
Vitamin K, Fresh Frozen Plasma

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14
Q

Argatroban

A

Anticoagulant

Hirudin derivative (leeches)
Direct thrombin inhibitor

heparin contraindications (HIT)

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15
Q

Bivalirudin

A

Anticoagulant

Hirudin derivative (leeches)
Direct thrombin inhibitor

heparin contraindications (HIT)

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16
Q

Dabigatran

A

Oral anticoagulant
Direct thrombin inhibitor
IIa inhibitor

Heparin contraindications (HIT)

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17
Q

Rivaroxaban

A

Anticoagulant
MOA:
Direct factor Xa inhibitor

Clinical:
Treatment/prophylaxis of DVT/PE, Afib(stroke)
Oral
no monitoring

Tox:
bleeding
no reversal agents

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18
Q

Apixaban

A

Anticoagulant
MOA:
Direct factor Xa inhibitor

Clinical:
Treatment/prophylaxis of DVT, Afib(stroke)
Oral
no monitoring

Tox:
bleeding
no reversal agents

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19
Q

tPA

A

Thrombolytics
MOA:
directly/indirectly aid conversion of plasminogen -> plasmin; cleaves thrombin and fibrin clots
^^PT, ^^PTT

Clinical:
Early MI, early ischemic stroke, direct thrombolysis of severe PE

Tox:
bleeding
Contraindicated in actively bleeding, hx of intracranial bleed, recent surgery, known bleeding diathesis, severe HTN

Reversal:
fibrinolysis inhibitor = aminocaproic acid
FFP/cryoprecipitate to correct factor deficiences

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20
Q

Urokinase Plasminogen

A 
Fibrinolytic
Thrombolytics
MOA:
directly/indirectly aid conversion of plasminogen -> plasmin; cleaves thrombin and fibrin clots
^^PT, ^^PTT

Clinical:
Early MI, early ischemic stroke, direct thrombolysis of severe PE

Tox:
bleeding
Contraindicated in actively bleeding, hx of intracranial bleed, recent surgery, known bleeding diathesis, severe HTN

Reversal:
fibrinolysis inhibitor = aminocaproic acid
FFP/cryoprecipitate to correct factor deficiences

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21
Q

streptokinase

A 
fibrinolytic
Thrombolytics
MOA:
Binds plasminogen cleaves fibrin clots
^^PT, ^^PTT

Clinical:
Early MI, early ischemic stroke, direct thrombolysis of severe PE

Tox:
bleeding
Contraindicated in actively bleeding, hx of intracranial bleed, recent surgery, known bleeding diathesis, severe HTN

Reversal:
fibrinolysis inhibitor = aminocaproic acid
FFP/cryoprecipitate to correct factor deficiences

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22
Q

Herbal clotting inhibitors

A

eg Ginko

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23
Q

cyclophosphamide

A

Alkylating agent

Commonly used

MOA:
covalently crosslink DNA at Guanine N-7; requires hepatic bioactivation.

Clinical:
Solid tumors, leukemia, lymphomas, some brain

Tox:
myelosuppression, **hemorrhagic cystitis, partially prevented w. **mesna (binds toxic metabolites)

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24
Q

Cisplatin

A

bifunctional alkylating agent
MOA:
crosslinks DNA

Clinical:
testicular, bladder, ovary, lung carcinomas

Tox:
nephrotox, CNVIII damage
prevent nephrotox w/ amifostine (free radical scavenger) chloride diuresis

Renal insufficiency

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25
Q

Ondanestron

A 
Antiemetic
MOA:
5-HT3 central antagonist
decreases vagal stim
powerful central acting anti-emetic

Clinical:
antiemetic; post op and chemo

Tox:
Headache, constipation

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26
Q

Aprepitant

A

Antiemetic
Neurokinin 1 antagonist

CYP3A4 metabolism

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27
Q

Methotrexate

A

anti-metabolite

MOA:
folic acid analogue inhibits dihydrofolate reductase
–v dTMP –> –v DNA and –v protein synth

Leucovorin Rescue for bone marrow

Clinical:
cancers, leukemia, lymphomas, choriocarcinomas, sarcomas, Non-neoplastic: abortion, ectopic pregnancy, rheumatoid arthritis, psoriasis, IBD

TOX:
myelosuppression, reversible w/ leucovorin “rescue”
Macrovesicular fatty liver
mucositis, teratogenic

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28
Q

5-flurouricil

A

Nucleoside analogue
MOA:
pyrimidine analog, bioactivated to 5fF-dUMP, covalently complexes folic acid:
complex inhibits thymidylate synthase –>–vdTMP–>–vDNA and protein synth

Clinical:
colon cancer, pancreatic cancer, basal cell carcinoma

Tox:
myelosuppression, 
***leucovorin potentiates
OD rescue w/ uridine
photosensitivity
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29
Q

Leucovorin

A

*Methotrexate myelosuppression rescue

30
Q

Cytarabine (Ara-C

A

nucleoside analogue
arabinofuranosyl cytidine

MOA: pyrmadine analog; Inhibits DNA pol
S-phase specifric

Clinical:
Leukemias, lymphomas

Tox:
leukopenia, thrombocytopenia, megaloblastic anemia
pancytopenia

31
Q

Daunorubicin

A

Anthracycline antibiotic
MOA:
Generates free radicals that intercalate into DNA; breaks DNA and –v replication

Clinical:
solid tumors, leukemias, lymphomas

Tox:
cardiotox (dilated cardiomyopathy)
myelosuppression, alopecia, tissue tox from extravisation

Dexrasoxane prevents cardiotox (iron chelator)

32
Q

Doxorubicin

A

Anthracycline antibiotic
MOA:
Generates free radicals that intercalate into DNA; breaks DNA and –v replication

Clinical:
solid tumors, leukemias, lymphomas

Tox:
cardiotox (dilated cardiomyopathy)
myelosuppression, alopecia, tissue tox from extravisation

Dexrasoxane prevents cardiotox (iron chelator)

33
Q

Etoposide

A

MOA:
inhibits Topo II
–^ DNA degredation

Clinical:
solid tumors, leukemias, lymphomas

Tox:
myelosuppression, GI, alopecia

34
Q

Topotecan

A

MOA:
inhibits topo I
prevents DNA unwinding and replication

Clinical:
ovarian and SCLCs

Tox:
severe myelosuppression

35
Q

Irinotecan

A

MOA:
inhibits topo I
prevents DNA unwinding and replication

Clinical:
Colon cancers

Tox:
severe myelosuppression

36
Q

Bortezomib/Carfilzomib

A

Chemo; Multiple myeloma and Mantle Cell lymphoma

37
Q

Thalidomide

A

Oral immuno suppression

Multiple Myeloma
GVHD, leprosy

38
Q

Lenalidomide and Pomalidomide

A

Oral immune suppression
newer better thalidomide

mess up protein processing
Relapsed and refractory Multiple myeloma

39
Q

Vinblastine

A

Microtubule inhibitor
MOA:
Vinca alkaloid binds B-tubulin; inhibits polymerization; prevents mitotic spindle formation

Clinical:
solid tumors, leukemias, lymphomas,

Tox:
marrow suppression

40
Q

Vincristine

A

Microtubule inhibitor
MOA:
Vinca alkaloid binds B-tubulin; inhibits polymerization; prevents mitotic spindle formation

Clinical:
solid tumors, leukemias, lymphomas,

Tox:
neurotoxicity

41
Q

Paclitaxel and Taxols

A

Taxol
MOA:
hyperstabilizes polymerized microtubules in M-phase; mitotic spindle can not break down; anaphase doesnt occur.

Clinical:
ovariann, breast carcinomas

Tox:
myelosuppression, alopecia, hypersensitivity.

42
Q

G-CSF

A

shortens time that pt is neutropenis, minimizes infection risk
Neutropenia

43
Q

GM-CSF

A

Neutropenia
Granulocyte-macrophage colony stimulating factor

Stimulates production of granulocytes and monocytes

44
Q

Erythropoietin

A

Anemia
erythrocyte production

for chronic renal failure, ACD, MDS, AIDS, chemo

45
Q

IL-11

A

Thrombocytopenia

46
Q

Thrombopoeitin

A

Thrombocytopenia

47
Q

Darbepoietin alpha

A

Anemia

48
Q

IL-2

A

Stimulates anti tumor response

Growth factor fo T-cells and NK

Renal cell carcinoma

49
Q

Interferons

A

Stimulates anti tumor response

SC admin

50
Q

Rituximab

A

Monoclonal Ab
MOA:
monoclonal Ab vs. CD20
(found in most B-cell neoplasms)

Clinical:
lymphoma
rheumatoid arthritis (w/ MTX)
ITP

Tox:
–^ risk of progressive multifocal leukoencephalopathy

51
Q

5-Azacytidine

A

epigenetic Chemotherapeutic

cant be methylated
incorporated and tunr on genes that cancer cells have methylated/shut off

52
Q

Suberoylanilide Hydroxamic acid

A

Chemotherapeutic

53
Q

Nivolumab

A

Monoclonal Ab

unresectible or metastatic melanoma; squamous NSCLC

54
Q

Pembrolizumab

A

monoclonal Ab

unresectable or metastatic melanoma; metastatic NSCLC

55
Q

Trastuzumab

A

Mab
Her2/neu receptor

Her2+ breast cancer

ADR
Cardiac tox
dyspnea
allergy

56
Q

Imatinib mesylate

A

RTK inhibitor
MOA:
Tyrosine kinase inhibitor or bcr-abl and c-kit
CYP3A4

Clinical:
CML, GI stromal tumors

Tox:
fluid retention
Cardiac

57
Q

Erlotinib

A

Chemotherapeutic
Tarceva
EGFR inhibitor

58
Q

Bevacizumab

A

MOA:
monoclonal Ab vs VEGF; inhibits angiogenesis

Clinical:
solid tumors

Tox:
hemorrhage and impaired wound healing

59
Q

Abciximab

A

Fab fragment against GPIIb/IIIa

prevention of acute clotting/vessel closure in PCI

2x major bleed

60
Q

Eptifibatide

A

GPIIb/IIIa inhibitor

Rarely used

thrombocytopenia

61
Q

Tirofiban

A

GPIIb/IIIa inhibitor

Rarely used

thrombocytopenia

62
Q

Alkylating agents

A

reactive organic moleucles
alkylate DNA
Phase non-specific
linear dose-response

ADR:
nausea, marrow suppression, mutagenesis, secondary carcinomas

63
Q

Methchlorethamine

A

Nitrogen mustard Alkylating agent
First chemo agent

no longer used

64
Q

Melphalan

A

Nitrogen mustard alkylating agent

commonly used

few side effects

65
Q

ifosphamide

A

Nitrogen mustard alkylating agent

commonly used

few side effects

66
Q

chlorambucil

A

Nitrogen mustard alkylating agent

commonly used

few side effects

67
Q

Gemtuzumab

A

monoclonal Ab
carries toxin to CD33 cells

AML

68
Q

Tiuxetan

A

MAB
anti CD20
radioactivity

69
Q

cetuximab

A

MAB

EGFR target

70
Q

Vemurafenib

A

protein kinase inhibitor
B-Raf mutation

Oral for metastatic melanoma

Pharm II (3 decks)

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