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Drug Action I > Block 2 - Antiplatelets Med Chem > Flashcards

Block 2 - Antiplatelets Med Chem Flashcards

(45 cards)

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1
Q

What are the anti platelet drugs?

A
  1. Aspirin
  2. Glycoprotein IIb/IIIa inhibitors
  3. ADP inhibitors (clopidogrel)
  4. PDE/adenosine uptake inhibitors
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2
Q

Describe how platelet aggregation occurs?

A
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3
Q

Understand platelet aggregation cascade Slides 5-8

A
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4
Q

What is the MOA of COX1 inhibitors?

A

Block the synthesis of thromboxane A2

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5
Q

What is thromboxane A2?

A

key inducer of platelet aggregation → a potent vasoconstrictors at high concentration

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6
Q

Describe the effects of acetylsalicylic acid?

A

Aspirin is an Irreversible inhibitor of COX-1

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7
Q

What gives aspirin is lasting aggregation effect?

A

Lifetime of the platelet and platelets can replicate

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8
Q

What are PDE inhibitors do?

A

Leads to increased cAMP leads to negative effect on intracellular calcium levels → drug inhibits → Low intracellular calcium levels inhibit aggregation

Promotes the conversion of cAMP → AMP

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9
Q

What are the PDE3 inhibitors for platelet aggregation?

A
  1. Dipyridamole
  2. Cilostazol (more selective)
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10
Q

What do PDE3 inhibitors need to mimic?

A

cAMP

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11
Q

What is the MOA of P2Y purinergic receptor?

A

Targets P2Y12 that promotes ADP binding → intracellular Ca2+

Antagonists → slow activation GP IIb/IIIa receptors → prevents aggregation

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12
Q

What is the SAR of P2Y antagonists?

A

ADP mimicry

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13
Q

What are the ADP binding sites on platelets? Function?

A

Px1, P2Y1, P2Y12

Increases intracellular Ca2+

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14
Q

What are P2Y antagonists? Which are prodrugs?

A
  1. Ticlopidine
  2. Clopidogrel
  3. Prasugrel
  4. Ticagrelor (Not prodrug)
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15
Q

What P2Y antagonists are metabolized by CYP?

A
  1. Clopidogrel
  2. Ticagrelor
  3. Ticlopidine

CYP2C19

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16
Q

Brand name Ticagrelor

A

Brilinta

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17
Q

What are the newest anti platelet aggregators?

A

Glycoprotein IIb/IIIa Receptor Antagonists

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18
Q

MOA of Glycoprotein IIb/IIIa Receptor Antagonists?

A
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19
Q

What are the benefits of using Glycoprotein IIb/IIIa Receptor Antagonists?

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A

provides anti-aggregation regardless of the source of thrombus

20
Q

What are the peptide sequences of Glycoprotein IIb/IIIa Receptor Antagonists?

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A

Arg-Gly-Asp
Lys-Gly-Asp

21
Q

What does Glycoprotein IIb/IIIa Receptor Antagonists mimic?

22
Q

What is abciximab? ADR?

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A
  1. Chimeric murine antibody (contains Arg-Gly-Asp)
  2. Long DOA
  3. Peptide

Thrombocytopenia

23
Q

What is Eptifibatide? ADRs?

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A

Cylic heptapeptide containing Lys-Gly-Asp

Highly specific with low binding affinity (peptide)

Advantage b/c highly reversible = less thrombocytopenia

24
Q

What is tirofiban

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A
  1. Disimalr to disinterring (isolated from snake venom)
  2. Peptidomimetic (COOH and NH mimic the Arg-Gly-Asp of disintegrin)

Better bioavailability

25
What is desmopressin (DDVAP)?
1. Vasopressin analogue 2. Increase the release of Von Willebrand factor → increase platelet adhesion 3. Same indication as vasopressin
26
Why does vasopressin have to be given as an injection?
Peptide
27
What are the indications of vasopressin?
central diabetes insipidus: extreme urination, thirst, bed-wetting Better than desmopressin
28
MOA of vasopressin?
Increases release of von Willebrand factor
29
Why is DDAVP have better PO bioavailability the vasopressin?
Formas a more acid stable structure → deaminated Cys and altered stereochemistry in Arg
30
What is von Willebrand factor?
Increases the amount of stickiness of platelets → Increases platelet binding
31
What are classes of thrombolytics?
1. t-Pa derivatives 2. Streptokinase
32
What is the MOA of thrombolytics?
1. Dissolves clots that have formed 2. Activates plasminogen to plasmin conversion → Degradation of fibrin
33
Describe the conversion of plasminogen to plasmin
34
What is the exception of urokinase?
1. Plasminogen to plasmin conversion 2. Degrades fibrin directly
35
What are thrombolytics IV?
1. peptidic in nature 2. Based on tPA 3. Occurs naturally in body, regulated by tPA1 and tPA2
36
What is streptokinase?
1. No activity until bound to plasminogen (1:1) 2. breaks down fibrinogen, factor V, VII 3. Drug of choice (cheap and effective)
37
What is the ADR of streptase?
Activates immune system Comes from streptococcus
38
MOA of urokinase?
Kinlytic 1. isolated from urine (hence the name) but now from cultured human fetal kidney cells 2. Same MOA + breaks down fibrin directly 3. Short half-life 4. No hypersensitivity
39
What is alteplase?
Low affinity for free plasminogen, high affinity for plasminogen bound to fibrin in a thrombus Ultra short DOA From isolated human melanoma cells Expensive
40
What are the types of thrombolytics?
1. Streptase (Streptokinase) 2. Kinlytic (Urokinase) 3. Activase (Alteplase) 4. Retevase (Reteplase) 5. TNKase (Tenecteplase)
41
What is Retevase (Reteplase)?
525 amino acid sequence of Alteplase w/o the first 172 amino acids Same MOA but more specific than Alteplase
42
How does Tenecteplase differ from Alteprase?
1. 3 point mutation 2. 15x more specific 3. 80x more potent
43
What are the plasminogen-based reversal agents?
Lysteda (tranexamic acid)
44
MOA of Lysteda?
1. Inhibitor of fibrinolysis (“anti-fibrinolytic” or “anti-thrombolytic”) 2. Synthetic lysine analogue 3. Same MOA for aminocaproic acid
45
Indications of Lysteda?
1. Does not increase clotting, but rather stabilizes existing clots 2. Denistry 3. CO formulated with mefanamic acid (NSAID) for decrease of pain and blood loss with menorrhagia

Drug Action I (32 decks)

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