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pharm exam 2 > Topic 14 Platelet Blockers > Flashcards

Topic 14 Platelet Blockers Flashcards

(68 cards)

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1
Q

Aspirin &/or called?

A

Acetylsalicylic Acid

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2
Q

Many functions are mediated by aspirin’s ability to irreversibly bind (and inactivate) what enzyme ?

A

enzyme cyclooxygenase-1 (COX-1) and modify the activities of COX-2.
This inhibition lasts for the entire life of the platelet!!!

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3
Q

once COX-2 has been modified by aspirin it produces what?

A

lipoxins

Lipoxins are anti-inflammatory

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4
Q

Lipoxins are what?

A

anti-inflammatory

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5
Q

Aspirin inhibits platelets ability to do what?

A

–Platelets’ release of ADP is inhibited

–Platelets’ ability to synthesize Thromboxane A₂ and Prostaglandin E₂ from Arachadonic Acid is inhibited.

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6
Q

Thromboxanes produced by platelets tend to help what?

A

help induce clot formation while the Prostaglandins tend to be pro-inflammatory

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7
Q

Prostaglandins tend to be what?

A

Pro-inflammatory

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8
Q

Aspirin function - With Thromboxanes

blocked, platelets won’t aggregate for how long

A

for the life of the platelet

–a good thing in places like coronary or carotid arteries!

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9
Q

RBCs live how long?

A

100 days

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10
Q

Platelets live how long?

A

8-9 days

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11
Q

four major clinical applications for aspirin

A

fever
inflammation
joint pain
platelet aggregation/clot/thrombosis

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12
Q

when aspirin is given – platelets cant aggregate what 4 things can be prevented?

A

Thrombotic stroke
Deep MI
Pulmonary Emboli
Venous emboli

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13
Q

Aspirin side effects

A

bleeding
COMPLETE PLATELET ACTIVATION -occurs at a dose of 160mg
GI (like gastric ulcers)
Kidney damage

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14
Q

Aspirin dose that causes complete platelet activation

A

160mg

this has big variability/ not true but use

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15
Q

Aspirin GI side effects (like ulcers) are caused how (cellularly)?

A

-PGI₂ prevents gastric parietal cells from secreting HCL
-PGE₂ and PGF₂-alpha cause the stomach and SI to creative surface-protective mucus.
*This happens on a cellular biochemical level,
therefore things like “coated” and “enteric”
aspirin don’t actually accomplish much

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16
Q

PGF2 alpha also causes what in animals and can be ppl?

A

pus filled uterus

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17
Q

How does Aspirin cause kidney damage ?

A

Prostaglandins are largely responsible for maintaining adequate renal blood flow.
-By blocking Prostaglandin synthesis, salts and fluid start to be retained, potassium
isn’t excreted properly, and the kidneys are “scarred” (interstitial nephritis.)

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18
Q

Prostaglandins are largely responsible for what in the kindeys?

A

for maintaining adequate RBF

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19
Q

Aspirin Clearance where? T1/2

A

Conjugated by the liver, cleared by the kidneys so the half-life is 3.5 hours

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20
Q

The conjugated stage of Aspirin in the liver is very saturable. what does this mean for T1/2?

A

so at higher doses over several days the half-life increases 4-5X

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21
Q

Ticlopidine

A

(Ticlid)

Thienopyidines (pts coming fromcath lab will be on these prob)
Like aspirin: Block platelet aggregation
Unlike aspirin: Different M.O.A

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22
Q

Clopidogrel

A

(Plavix)

Thienopyidines (pts coming fromcath lab will be on these prob)
Like aspirin: Block platelet aggregation
Unlike aspirin: Different M.O.A

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23
Q

Prasugrel

A

Effient

Thienopyidines (pts coming fromcath lab will be on these prob)
Like aspirin: Block platelet aggregation
Unlike aspirin: Different M.O.A

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24
Q

Thienopyidines - what do they inhibit/block ?

A

act by irreversibly inhibiting the ADP pathway of platelets…
•This blocks platelets’ GPIIb/IIIa receptors.
•Consequently, affected platelets can’t bind to each other or to fibrinogen

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25
Which Thienopyidine is Approved for use in the prevention of TIAs and strokes and for use with aspirin post-stent placement to prevent thrombi formation
Ticlopidine (Ticlid)
26
Ticlopidine (Ticlid) has what kind of warnings?
Black Box Warnings for hematological disorders - Aplastic anemia (not producing more cells) - Neutropenia - Thrombotic Thrombocytopenia Purpura (low levels of platelets bc you get these little clots that use up all the platelets and you get purple splotches)
27
what is Neutropenia
the presence of abnormally few neutrophils in the blood, leading to increased susceptibility to infection.
28
Clopidogrel (Plavix) is used more for what as compared to Ticlopidine
Used more for cardiac “issues” (MI prevention, ACS, post-PTCA etc.) than Ticlopidine
29
Prasugrel’s (Effient) is more effective in treating what events than other thienopyridines!?
thrombotic-related events
30
Prasugrel (effient) Black Box Warning?
for hemorrhagic stroke, excessive hemorrage and negative sequelae (a condition that is the consequence of a previous disease) resulting from sudden discontinuation
31
Glycoprotein IIb/IIIa Blockers (3)
Abciximab (Reopro) Eptifibatide (Integrilin) Tirofiban (aggrastat)
32
Abciximab
Reopro Glycoprotein IIb/IIIa Blockers
33
Reopro
Abciximab Glycoprotein IIb/IIIa Blockers
34
Epitifibatide
Integrilin Glycoprotein IIb/IIIa Blockers
35
Tirofiban
Aggrastat Glycoprotein IIb/IIIa Blockers
36
Integrilin
Eptifibatide Glycoprotein IIb/IIIa Blockers
37
Aggrastat
Tirofiban Glycoprotein IIb/IIIa Blockers
38
Glycoprotein IIb/IIIa Blockers are all used extensively for what?
All used extensively for ACS and in cath labs to make your life more miserable when they finally decide to send the patient to surgery
39
Dipyridamole
Persantine primarily a coronary vasodilator
40
Persantine
Dipyridamile primarily a coronary vasodilator
41
Dipryidamole (Persantine) how is it used?
Rarely (if ever) used by itself. -Typically used as an adjunct with warfarin or aspirin for anticoagulation post-prosthetic heart valve implantation or for a-fib
42
Dextrans what are they?
glucose based polymers - can be made positive or negative
43
Dextrans - what are they used as? why
used as a volume expander | BC - One gram of dextran binds 20-25 ml of H2O (same effect as albumin)
44
Two kinds of Dextrans?
- Dextran 70 (Macrodex) - Dextran 40 (Rheomacrodex) May be used as part of pump prime Both mostly excreted by the kidneys over several hours and the rest metabolized
45
Dextran -- do what to RBCs? and do what to clots?
Bind RBCs, platelets, and vascular endothelium making them all less “sticky”. •Decreases Factor V, VIII, and IX functionality. •Clots formed in the presence of dextrans are “less sturdy” and more easily lysed.
46
Dextran side effects ? (3) - (#2 is the most important)
``` #1) Intra-op and post-op bleeding. #2) Volume overload, particularly in heart failure and anuric renal failure patients. #3) Anaphylaxis is not uncommon and occurs within minutes of administration ```
47
Dextrans Typical MAX Dosage to put in prime
2g/kg (20ml/kg)
48
Hespan is made with what?
a mixture of starch polymers (instead of glucose polymers - like dextrans)
49
Hespan does waht?
volume expander | sig reduces FVIII causing elevated aPTT
50
Hespan side effects?
Acute renal failure, coagulopathies and anaphylaxis
51
Hespan MAX daily dosage
20ml/kg
52
Alteplase/tPA
Activase Thrombolytics
53
Reteplase
Retevase Thrombolytics
54
Streptokinase
Streptase Thrombolytics Approved for pulmonary emboli, DVTs, aMIs, and thrombosed shunts
55
Urokinase
Kinlytic Thrombolytics Approved for use in pulmonary emboli
56
Thrombolytics - when will you give these? | Alteplase, Reteplase, Streptokinase, Urokinase
YOU WILL NEVER GIVE THESE! ESP NEVER ON BYPASS
57
Thrombolytics end in what ?
ase
58
What do Thrombolytics do?
they actually dissolve "lyse" clots that are already present. cant put in your reservoir
59
Streptokinase (streptase) attaches to what ? to convert what?
attaches to plasminogen and this complex acts to convert plasminogen into plasmin. •This complex also destroys fibrinogen and Factors V and VII
60
Urokinase (kinlytic) converts what to do what?
Directly converts plasminogen into plasmin to dissolve clots
61
Altepase/tPA (activase) used for?
Used for aMIs, thombotic strokes, and pulmonary embolism
62
Antithrombin III works with what to effect anticoagulation?
AT III works with heparin to effect anticoagulation | effect is multiplied by thousands to millions of times when combined with heparin
63
ATIII is made where?
liver (its a small protein)
64
Thrombate
Is a type of ATIII | Made from pooled human plasma
65
Atryn
Is a type of ATIII | Made from the milk of genetically modified goats
66
Differences btwn the two types of ATIII - Atryn and Thrombate?
Atryn 40% cheaper to use than Thrombate. - Atryn’s half-life is ~9 hours vs. Thrombate’s ~3 days. - Atryn must be refrigerated, Thrombate’s stored at room temperature
67
Which ATIII do we use?
Recent perfusion trend is away from Thrombate use towards Atryn
68
When do we administer ATIII?
AT III is used in the treatment of acquired or congenital AT III deficiency

pharm exam 2 (9 decks)

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