Exam 5: Anti platelet Flashcards

1
Q

Name the platelet formation cascade of events.

A
  1. GPIb/Ia/IIa binds (collagen + vWF)
  2. PLA2 up-regulation
  3. AA (COX-1)
  4. PGH2
  5. TS~ TxA2 (TP-R receptor = autocoid)
  6. PS~ PGI2 (IP-R receptor = autocoid)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

Name Gi + Gq function in platelet formation.

A

Gi~ decrease AC ~ decrease cAMP ~ increase Ca+
PDE turns cAMP into AMP ~ increase Ca+

Gq~ increase PLC ~ increase IP3 + DAG ~ increase in Ca+

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

Gi + Gq lead to what 3 things?

A
  • platelets release granules
  • platelets change shape + increase surface area
  • GIIb/IIIa expression (mesh formation via cross-linking w/ fibrin or vWF)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

What other receptors are located on platelet that are effected by anti-platelet drugs?

A

ADP (P2Y12) + P2Y1

platelets express PGY12 (Gi) + PGY1 (Gq)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

T/F? PGY1 + PGY12 must both be activated in order to participate in platelet formation.

A

True

PGY12 (Gi coupled)- ADP receptor is effected by drugs

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

What do does the expression of GIIb/IIIa allow for?

A

cause platelets to bind to one another cross-linking w/ Fibrogen or vWF

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

What normally acts on PAR-1 receptors? What drug blocks PAR-1 receptors Vorapaxar

A

Thrombin

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

Name the drugs: COX-1 inhibitors

A

ASA

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

Name the drugs: PAR-1 (thrombiin) inhibitory

A

VoRAPraxar (Zontivity)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

Name the drugs: GIIb/IIIa inhibitors (TEA)

A

Tirofiban
Epitfibatide
Abciximab (monoclonal antibody)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

Name the drugs: PDE inhibitors

A

Cilostazol

ASA + Dip (Aggrenox)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

Name the drugs: ADP inhibitors (CYP/CTP)

A

Cangrelor (Kengreal)
*TICAgrelor (Brilinta)- parent+ prodrug (active metabolite)
Prasugrel (Effient)
Plavix (clopidogrel)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

Which ADP drugs are prodrugs (2)?
IV?
active parent + metabolite?

A
  • Plavix + (Prasugrel) Effient (irreversible)
    Cangrelor (Kengreal)
    Ticagrelor (Brilinta) -BID
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

ADP irreversible drug? (2)

A

Plavix

Effient

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

ADP reversible drugs? (1)

A

CANgrelor (KENgrel) - IV

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

What drug is most commonly used in STROKE patients?

A

Aggrenox + Cilostazol

PDE (inhibition) leads to INCREASE cAMP leads to MLCK inhibition (vasodilation)

17
Q

Which GIIb/IIIa inhibitors is a monoclonal antiboby?

A

Abciximab

18
Q

Which GIIb/IIIa inhibitors are renally cleared?

all are IV admin

A

Tirofiban (synthetic non-petide)
Epitfibatide (peptide)
selective for GPIIb/IIIa

19
Q

Why does Abciximab have the longest duration?

A

non-renal impaired