Coagulation Disorder Drugs Flashcards

1
Q

ASPIRIN

A

irreversible COX inhibitor (acetylation); reduces TxA2
preferentially targets platelets: endothelial cells can produce new prostacyclin; platelet has no nucleus to produce more TXA2
AE: GI, allergy (bronchospasm)
Use: secondary prevention of CV events
overdose: hepatic and renal toxicity

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2
Q

ibuprofen

A

COX inhibitor

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3
Q

CLOPIDOGREL

A

oral: prodrug
irreversible ADP receptor (P2Y12) inhibitor
poor 2C19 metabolizers have reduced response
use: post-MI, stroke, PAD (peripheral artery disease), PCI (percutaneous coronary intervention)
*ischemic heart disease

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4
Q

TICLOPIDINE

A

oral: metabolite more potent
irreversible ADP receptor (P2Y12) inhibitor
BB: agranulocytosis, neutropenia, thrombocytopenia, TTP, anemia
use: secondline due to AE

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5
Q

prasugrel

A

oral: prodrug
irreversible ADP receptor (P2Y12) inhibitor
use: acute MI, arterial thromboembolism, prophylaxis, PCI, unstable angina

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6
Q

dipyridamole

A

Oral/IV
phosphodiesterase (PDE) inhibitors
1. prostacyclin released-> increase adenylate cyclase-> cAMP increases: AA acid not released: decrease TXA2
2. adenosine accumulates (vasodilation)
3. decreases cAMP breakdown
use: prophylaxis of thrombosis for prosthetic heart valve (with warfarin)
CI: hypotension, asthma
hepatic glucoronidation; fecal elimination

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7
Q

ABCIXIMAB

A

IV
non-competitive, irreversible GPIIb/IIIa inhibitor
persists for 2 weeks after stopping administration
AE: bleeding, thrombocytopenia, anaphylaxis
Use: unstable angina, percutaneous transcutaneous coronary angioplasty

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8
Q

EFTIFIBATIDE

A

IV
reversible GPIIb/IIIa inhibitor
only persists 4 hrs
AE: bleeding, thrombocytopenia (less), anaphylaxis
Use: unstable angina, percutaneous transcutaneous coronary angioplasty

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9
Q

tirofiban

A

IV
reversible GPIIb/IIIa inhibitor
only persists 4 hrs
AE: bleeding, thrombocytopenia, anaphylaxis
Use: unstable angina, percutaneous transcutaneous coronary angioplasty

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10
Q

vorapaxar

A

PAR-1 inhibitor: blocks thrombin induced platelet aggregation
slower onset than for GPIIb/IIIa inhibitors
T1/2: 8 days
persists: 4 weeks
CYP3A4 metabolism
AE: bleeding

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11
Q

HEPARIN

A
IV/SC: rapid onset
ONLY for inpatient use
indirect thrombin inhibitor: accelerates AT3 binding coagulation factors (2, 10)
monitor: aPTT (want 1.5-2.5x normal)
SE: bleeding, antigenic (from animals and easy to get) anaphylaxis, thrombocytopenia
acts in blood, rapid onset, use is acute
need to monitor
short T1/2
80 u/kg bolus followed by 18 u/kg/hr
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12
Q

PROTAMINE SULFATE

A

IV
heparin antidote (v. basic): binds up heparin
incompletely neutralizes LMWH; does not reverse fondaparinux
SE: allergy to fish/DMT2: protamine rxn, too much is anticoagulative

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13
Q

DABIGATRAN

A

oral
direct thrombin inhibitor
Tx/prophylaxis: DVT, PE; stroke prophylaxis and HIT
Tox: bleeding (no antidote)

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14
Q

bivalirudin

A

IV
direct thrombin inhibitor
Tx/prophylaxis: DVT, PE; stroke prophylaxis and HIT
Tox: bleeding (no antidote)

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15
Q

lepirudin

A

IV
direct thrombin inhibitorTx/prophylaxis: DVT, PE; stroke prophylaxis and HIT
Tox: bleeding (no antidote)

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16
Q

ENOXAPARIN

A

indirect factor Xa inhibitor (thru ATIII): low MW heparin
compared to heparin: lower incidence of drug induced thrombocytopenia; bleeding may not change
injection
SE: bleeding, anaphylaxis
less impact on aPTT than heparin

17
Q

APIXABAN

A
oral
direct factor Xa inhibitor: leads to thrombin inhibition
Use: prophylaxis: DVT, PE, stroke
Tox: bleed without antidote
CYP3A4 metabolism
18
Q

RIVAROXABAN

A
oral
direct factor Xa inhibitor leads to thrombin inhibition
Use: prophylaxis: DVT, PE, stroke
Tox: bleed without antidote
CYP3A4 metabolism
19
Q

fondaparinux

A

IV/SC
LMWH: indirect factor Xa inhibitor: binds ATIII-> inhibits factor Xa
Use: prophylaxis: DVT, PE
Tox: bleeding without antidote

20
Q

WARFARIN

A

oral
clotting factor synthesis inhibitors: blocks vitamin K epoxide reductase (VKORC1): 2, 7, 9, 10, C, S
CYP2C9 important for metabolism (other CYPs too)
SE: hypercoaguability initially due to inhibition of certain factors quicker than others (skin necrosis: protein C and S have shorter T1/2); cholesterol embolism
monitor: PT, INR
teratogen
slow onset, acts on liver, for chronic use
issues: Vit. K consumption is constant, acetaminophen can increase INR, liver disease, skin necrosis: protein C and S have shorter T1/2 than heparin
desired INR: Tx and prophylaxis DVT 2.5; protection of mechanical heart valve 3

21
Q

PROTHROMBIN COMPLEX concentrate

A

warfarin antidote
factors 2, 7, 9, 10 and protein C and S
contraindication: angina, MI, PVD, stroke, thromboembolism

22
Q

phytonadione

A

vitamin K1

warfarin antidote

23
Q

ALTEPLASE

A

IV
(t-PA): thrombolytic
fibrin specific plasminogen activator
SE: anaphylaxis

24
Q

reteplase

A
IV
(rPA): thrombolytic
fibrin specific plasminogen activator
longer T1/2 than alteplase
SE: anaphylaxis
25
Q

tenectoplase

A
IV
(TNK-tPA): thrombolytic
fibrin specific plasminogen activator
longer T1/2 than alteplase
SE: anaphylaxis
26
Q

streptokinase

A

IV
thrombolytic
non-specific plasminogen activator (no affinity for fibrin bound plasminogen)
SE: anaphylaxis

27
Q

aminocaproic acid

A

fibrinolysis inhibitor: blocks plasminogen to plasmin
Use: hemorrhage, hyperfibronlysis
CI: DIC, clotting without heparin
monitor: hypotension, bradycardia

28
Q

cimetidine

A

CYP inhibitor: can inhibit hepatic metabolism metabolism

29
Q

PDE

A

catalyzes hydrolysis of cAMP and cGMP

30
Q

ginkgo biloba

A

antiplatelet properties

31
Q

garlic

A

antiplatelet properties

32
Q

ginger

A

inhibits thromboxane synthetase

33
Q

protamine reaction

A

shaking, flushing, chills, back/chest/flank pain, vasomotor collapse
Tx: morphine, meperidine, diphenhydramine, saline, support low BP

34
Q

vitamin K rich foods

A

asparagus, basil, beef or pork liver, black eyed peas, broccoli, brussel sprouts, cabbage, chick peas, cucumber peel, green onions, green tea, okra, parsley, green leafy veggies

35
Q

Factors that increase PT time warfarin patients

A

Kinetic: amiodarone, cimetidine, disulfarim, fluconazole, metronidazole, phenylbutazone, sulfinpyrazone, trimethoprim-sulfamethoxazole

dynamic: aspirin (high dose), cephalosporins (gen. 3), heparin, argatroban, dabigatran, revaroxaban, apixaban
body: liver disease, hyperthyroidism

36
Q

factors that decrease PT time

A

kinetic: barbiturates, cholestyramine, rifampin
dynamic: vit. K
body: hereditary resistance, hypothyroidism

37
Q

What drug is often given with thromoblytic drugs and why?

A

aspirin or heparin to prevent local thrombi as clot dissolves

38
Q

Use of thrombolytics

A
early MI, early ischemic stroke. PE
AE: bleeding
CI: bleeding, HTN, a-fib, arrhythmia 
DI: platelet inhibitors, anticoags, NSAIDs, antineoplastics, antithymocyte glogulin, aminocaproic acid, cephalosporins
Heparin ok
39
Q

FFP

A

can reverse the effect of warfarin