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Pharmacology II - CP > Anticoagulants , Antiplatelets, Thrombolytics > Flashcards

Anticoagulants , Antiplatelets, Thrombolytics Flashcards

1
Q

anticoagulants definition

A

PREVENT clot formation or extension of existing clots

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2
Q

antiplatelets definition

A

reduce platelet aggregation on the surface of the platelet

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3
Q

thrombolytics definition

A

converts endogenous plasminogen to the fibrinolytic enzyme plasmin to dissolve newly formed blood clots

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4
Q

Four major counter regulatory pathways

A

fibrinolysis, tissue factor plasminogen inhibitor, protein c system, serine protease inhibitors

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5
Q

things that can prevent coagulation

A

endogenous anticoagulation factors, siliconized containers, heparin (CPB or dialysis), citrate ion

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6
Q

tissue factor plasminogen inhibitor action

A

inhibits extrinsic pathway by inhibiting TF-VIIa complex

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7
Q

coagulation propagation is inhibited by the

A

protein c pathway

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8
Q

4 key elements of the protein c pathway

A

protein c
thrombomodulin
endothelial protein c receptor
protein s

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9
Q

protein c

A

activated by thrombin to form activated protein c and inhibits activated factors V and VIII
is a potent anticoagulant, profibrinolytic, and anti-inflammatory

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10
Q

what is a cofactor to APC (activated protein C) in the inactivation of factor Va and VIIIa?

A

protein S

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11
Q

serpin/antithrombin

A

binds and inactivates thrombin, factor IIa, IXa, Xa, XIa, and XIIa

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12
Q

the enzymatic activity of antithrombin is enhanced

A

in the presence of heparin

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13
Q

any substance that deionizes the blood calcium will ___

A

prevent coagulation

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14
Q

____ charged citrate ion combines with ___ charged calcium in the blood to cause ___

A

negatively ; positively; unionized calcium compound

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15
Q

what can depress Calcium levels?

A

liver damage or massive transfusion where citrate ion can’t be removed quickly enough

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16
Q

Warfarin (coumadin) MOA

A

inhibits vitamin K resulting in defective factor II, VII, IX, X

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17
Q

what is coumadin contraindicated in?

A

pregnant women (crosses placenta)

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18
Q

what can we give to a parturient who has a clot?

A

heparin

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19
Q

coumadin pharmacokinetics

A

2.5-10mg dose varies depending on INR, onset 3-4 days, DOA 2-4 days

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20
Q

which processes have an INR goal of 2-3 on coumadin

A

afib, vte, pe, prevention of vte, tissue heart valves

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21
Q

which processes have an INR goal of 2.5-3.5 on coumadin?

A

mechanical heart valve, prevention of recurrent MI, history of vte

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22
Q

when to discontinue coumadin for minor surgery?

A

1-5 days for PT 20% within baseline

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23
Q

coumadin reversal with immediate surgery or active bleeding

A

vitamin k

2.5-20mg orally or 1-5 mg IV at rate of 1mg/min

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24
Q

emergency surgery coumadin reversal

A

FFP or 4-factor concentrate (Kcentra)

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25
unfractionated heparin is ____ unpredictable than LMWH
more
26
heparin is a
naturally occurring polysaccharide that inhibits coagulation and enhances antithrombin
27
when unfractionated heparin binds to antithrombin it inactivates which coagulation enzymes?
thrombin IIa, factors IX, Xa, XI, XII
28
heparin must contain at least ____ units/mL
120 UPS
29
100 units/kg of heparin IV elimination half time
56 minutes
30
400 units/kg of Heparin IV elimination half time
152 minutes
31
a ____ in temperature prolongs the elimination half time of heparin
decrease
32
ACT monitoring with unfractionated heparin
get a baseline, 3-5 minutes post administration, then 30 minute - 1 hour intervals post administration
33
Clinical uses of unfractionated heparin
VTE SQ, PE prophylaxis, warfarin bridge, vascular or non-CPB (ACT 200-300s), interventional aneurysm clipping/coiling (>250s), CPB (>400-480s)
34
Dosing of unfractionated heparin for prophylaxis
5,000 units SQ q8-12h
35
Dosing of unfractionated heparin for treatment of thromboembolism
5,000 units IV, then continuous infusion for goal PTT 1.5-2.5 times control value
36
Dosing of unfractionated heparin for cardiopulmonary bypass
400 units/kg IV
37
Dosing of unfractionated heparin for vascular interventions
100 - 150 units/kg IV
38
Heparin side effects
hemorrhage, hematomas, thrombocytopenia (HIT), allergic reaction, hypotension, altered protein binding
39
Considerations for IV heparin and neuraxial anesthesia
1 hour delay between needle placement and heparin admin catheter should be removed 1 hour before heparin admin and 2-4 hours after last heparin dose monitor PTT or ACT
40
Mild or type I HIT
30-40% cases non-immune mediated plt count < 100,000 3-15 days after initiation of therapy
41
Severe of type II HIT
immune mediated plt count < 50,000 6-10 days after initiation of therapy
42
patients with antithrombin deficiency will have a resistance to ____
heparin
43
estrogen containing contraceptives decrease antithrombin's ability to ____
inhibit Xa
44
treatment for antithrombin deficiency with heparin resistance
2-4 units of FFP in adults | antithrombin concentrate
45
heparin reversal
protamine | 1 - 1.5 mg for each 100 units of heparin administered
46
low molecular weight heparin differences from unfractionated heparin
less protein binding, elimination half life 24 hours, one daily dosing
47
enoxaparin (lovenox) action
binds to and accelerates antithrombin | inhibits factor Xa and IIa so there is decreased thrombin activity and prevention of fibrin clot formation
48
enoxaparin dose example for DVT prophylaxis
30 mg SQ every 12 hours
49
advantages of LMWH/lovenox
reduced dosing frequency, more predictable, fewer effects on platelet function, reduced risk for HIT
50
disadvantages of LMWH/lovenox
expensive, delay surgery for 12 hours after last dose, protamine not as effective in reversal
51
What may be a better reversal for lovenox?
FFP
52
advantages of direct oral anticoagulants
alternative to warfarin, rapid onset with peak effect in 2-4 hours, predictable, minimal drug interactions, no routine labs
53
direct thrombin (IIa) inhibitor
dabigatran (pradaxa)
54
Dabigatran (Pradaxa) pharmacokinetics
renal elimination 1/2 life = 12 hours reversal: Idarucizumab (praxbind)
55
Direct Factor Xa inhibitors
rivaroxaban (xarelto), apixaban (eliquis), edoxaban (savaysa)
56
how are direct factor Xa inhibitors metabolized?
hepatic metabolism
57
When to stop direct oral anticoagulants for low bleeding risk procedures?
24 hours prior
58
When to stop direct oral anticoagulants for high bleeding risk procedures?
48 hours prior
59
antiplatelet agents
cyclooxygenase inhibitors (ASA, NSAIDs), P2Y12 receptor antagonists, glycoprotein IIb/IIIa inhibitors
60
antiplatelet MOA
suppress platelet function (inhibit platelet aggregation) for prevention of thrombosis
61
Aspirin MOA
antithrombotic effects by inhibiting platelet aggregation, inhibits thromboxane A2 synthesis IRREVERSIBLE, lasts life of a platelet
62
Aspirin dosing
81-325 mg
63
NSAIDs MOA
same as ASA except they reversibly depress thromboxane A2 production by platelets often held prior to surgery
64
primary prophylaxis should be ___ in perioperative period
continued but may be discontinued
65
secondary prophylaxis should be ____ in perioperative period
continued
66
Hold ASA in these circumstances:
intracranial, middle ear, posterior eye or intramedullary spine surgery, prostate surgery
67
Clopidogrel MOA
P2Y12 - ADP receptor antagonist | pro-drug that is metabolized by CYP450 enzymes and inhibits platelet aggregation
68
Ticagrelor
does not need hepatic activation | must be d/c'd 7 days prior to surgery
69
What is useful in emergency surgery for someone who is taking clopidogrel or ticagrelor?
platelet transfusion
70
indications for P2Y12 receptor antagonists
secondary prevention for MI, CVA, coronary artery stenting, acute coronary syndrome, peripheral artery disease
71
withdrawal of ASA in patients with CAD is associated with
a 2-4 fold increase in death/MI
72
patients with stents are at high risk of _____
thrombotic events especially in the first 3 months after insertion
73
platelet glycoprotein IIb/IIIa antagonists MOA
act at fibrinogen receptors that are important for platelet aggregation blocks fibrinogen
74
platelet glycoprotein IIb/IIIa antagonists
abciximab (reopro), tirofiban (aggrastat), eptifibatide (integrilin)
75
what ACT level do we want for people on platelet glycoprotein IIb/IIIa antagonists
between 200-400 seconds
76
what are the 3 herbal agents that inhibit platelet aggregation?
garlic, ginkgo, ginseng
77
how long should you discontinue garlic?
7 days
78
how long should you discontinue ginkgo?
36 hours
79
how long should you discontinue ginseng?
preferably 7 days but definitely 24 hours
80
what else should does ginseng do besides inhibit platelet aggregation?
lowers blood glucose
81
fibrin specific thrombolytics
alteplase, reteplase, tenecteplase
82
non fibrin specific thrombolytic
streptokinase
83
thrombolytics MOA
possess inherent fibrinolytic effects or enhances body's fibrinolytic system by converting plasminogen to plasmin breaking down newly formed clots
84
when are thrombolytics contraindicated?
trauma, severe HTN, active bleeding, pregnancy
85
alteplase considerations
synthesized by endothelial cells limited to use in first 3-6hours of ischemic stroke short 1/2 life (5 minutes) - give as bolus then infusion
86
thrombolytic efficacy
depends on the age of the clot | older clots have more cross linking and more compact = difficult to dissolve
87
anticoagulants in general
delay or prevent clotting and have no effect after the clot is formed
88
antithrombotics in general
influence the formation of clot by inhibiting platelet activity

Pharmacology II - CP (12 decks)

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