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Therapeutics II > Antiplatelet Drugs Hockerman > Flashcards

Antiplatelet Drugs Hockerman Flashcards

1
Q

What is hemostasis?

A

Arrest of bleeding from a damaged blood vessel

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2
Q

Phases of hemostasis

A

-Vasospasm
-Platelet plug formation
-Fibrin clot formation
-Fibrinolysis

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3
Q

Why is it important that platelets do not have nuclei?

A

They cannot replace proteins that have been irreversibly inhibited

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4
Q

What does GP Ia bind to?

A

Collagen

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5
Q

What does GP Ib bind to?

A

von Willebrand Factor bridged to collagen

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6
Q

What do endothelial cells secrete?

A

PGI2 (prostacyclin) which inhibits thrombogenesis

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7
Q

Why does the disruption of the endothelial layer cause platelet aggregation?

A

Exposes collagen and van Willebrand factor to the clotting factors

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8
Q

What granules are secreted by the platelet through degranulation?

A

-ADP
-TXA2
-5-HT

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9
Q

What do the granules released by the platelet during degranulation do?

A

-ADP, 5-HT, and TXA2 activate and recruit other platelets
-TXA2 and 5-HT are also potent vasoconstrictors

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10
Q

What do GPIIb/IIIa receptors bind to?

A

These receptors bind to fibrinogen after ADP, 5-HT and TXA2 activation

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11
Q

How do platelets recruit other platelets during platelet aggregation?

A

-Platelets are cross-linked by fibrinogen which is a bivalent molecule
-Platelets then contract to form an irreversibly fused mass called a fibrin which stabilizes and anchors aggregated platelets

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12
Q

What are the COX-1 inhibitors?

A

Aspirin

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13
Q

COX-1 inhibitor mechanism of action

A

Irreversible inhibition by acetylation of COX-1 leading to a permanent loss of platelet COX-1 activity (decrease in TXA2)

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14
Q

At what dose is aspirin maximally effective?

A

AT 50-320mg per day

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15
Q

Why is it important to not go too high in dosing of aspirin?

A

PGI2 production in tissue inhibited by higher doses

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16
Q

What are the indications for aspirin?

A

“prophylaxis and treatment of arterial thromboembolic disorders”
-Prevent coronary thrombosis in unstable angina
-Adjunct to thrombolytic therapy
-Reducing recurrence of thrombotic stroke

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17
Q

What are two key clinical actions for aspirin?

A

-Prolong bleeding time, but no increase in prothrombin time
-Hemostasis returns to normal after 36 hours after last dose

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18
Q

Side effects of aspirin

A

-Upper GI bleed (risk increases with age, concurrent use of NSAIDs and/or alcohol)
-Acute aspirin overdose (above 150 mg/kg)

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19
Q

At what dose of aspirin can be fatal?

A

Over 500 mg/kg

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20
Q

Symptoms of acute aspirin overdose

A

-Nausea
-Vomiting
-Diarrhea
-Fever
-Coma

21
Q

What are the two ADP receptors involved in activating platelets?

A

-P2Y1
-P2Y12
-Activation of both is required for platelet activation by ADP

22
Q

What are the ADP receptor inhibitors?

A

-Clopidogrel (Plavix)
-Ticlopidine (Ticlid) (Not on the market anymore so probably not on exam)
-Prasugrel (Effient)
-Ticagrelor (Brilinta)
-Cangrelor (Kangreal)

23
Q

What is the pharmacophore for ADP receptor inhibitors?

A

Thienopyridine group

24
Q

Clopidogrel mechanism of action

A

-Irreversibly block ADP receptor on platelet and subsequent activation of GPIIb/IIIa complex
-Action lasts for several days

25
Q

What is the only ADP receptor inhibitor not given orally?

A

Cangrelor is given IV

26
Q

Use of Clopidogrel

A

-Acute coronary syndrome
-Recent MI
-Stroke
-Established peripheral vascular disease
-Coronary stent procedures

27
Q

Why does Prasugrel work more dependably in more people compared to Clopidogrel?

A

Clopidogrel is activated by the enzyme CYP2C19 while Prasugrel is activated by esterase and CYP3A4/CYP2B6

28
Q

What is a warning to consider in Prasugrel?

A

High risk of bleeding so it is not recommended in the elderly or before CABG

29
Q

What is Prasugrel approved for treating?

A

-Acute coronary syndrome
-Percutaneous coronary intervention (PCI)

30
Q

What is Ticagrelor used to treat?

A

-Acute coronary syndrome
-PCI

31
Q

What is a warning to consider in Ticagrelor?

A

Risk of bleeding- do not use immediately before a CABG

32
Q

What is Cangrelor used for?

A

An adjunct to PCI

33
Q

Which ADP receptor inhibitors are prodrugs?

A

-Clopidogrel
-Pasugrel

34
Q

Which ADP receptor inhibitors are not prodrugs?

A

-Ticagrelor
-Cangrelor

35
Q

Which ADP receptor inhibitors are reversible?

A

-Ticagrelor
-Cangrelor

36
Q

Which ADP receptor inhibitors are irreversible?

A

-Clopidogrel
-Prasugrel

37
Q

What are the GPIIb/IIIa receptor inhibitors?

A

-Abciximab
-Eptifibatide
-Tirofiban

38
Q

What is the same motif that is present in eptifibatide that is also present in the GPIIb/IIIa receptors?

A

-Arginine
-Glycine
-Aspartic acid

39
Q

How are GPIIb/IIIa receptor inhibitors given?

A

Through IV

40
Q

Which GPIIb/IIIa receptor inhibitor has the longest duration of action?

A

Abciximab which means it has an increased risk of bleeding

41
Q

Which GPIIb/IIIa receptor inhibitor has the shortest onset?

A

Tirofiban inhibits over 90% of platelet aggregation after just 30 minutes of infusion

42
Q

What is Eptifibatide used for?

A

To prevent thromboembolism in unstable angina and angioplastic coronary procedures

43
Q

Is Tirofiban reversible or irreversible?

A

Reversible

44
Q

What is Tirofiban used for?

A

Combined with heparin to treat acute coronary syndrome

45
Q

What is Abciximab used for?

A

-Prevent thromboembolism in coronary angioplasty
-Combined with t-PA for early treatment of acute MI

46
Q

Is Abciximab reversible or irreversible?

A

Reversible but it binds very tightly giving it a long half-life

47
Q

Use of Dipyridamole

A

-Combined with warfarin to prevent embolization from prosthetic heart valves
-Used with ASA to prevent cerebrovascular ischemia

48
Q

Use of Cilostazol

A

Intermittent claudication

Therapeutics II (33 decks)

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