Exam 5: Anti platelet Flashcards
Name the platelet formation cascade of events.
- GPIb/Ia/IIa binds (collagen + vWF)
- PLA2 up-regulation
- AA (COX-1)
- PGH2
- TS~ TxA2 (TP-R receptor = autocoid)
- PS~ PGI2 (IP-R receptor = autocoid)
Name Gi + Gq function in platelet formation.
Gi~ decrease AC ~ decrease cAMP ~ increase Ca+
PDE turns cAMP into AMP ~ increase Ca+
Gq~ increase PLC ~ increase IP3 + DAG ~ increase in Ca+
Gi + Gq lead to what 3 things?
- platelets release granules
- platelets change shape + increase surface area
- GIIb/IIIa expression (mesh formation via cross-linking w/ fibrin or vWF)
What other receptors are located on platelet that are effected by anti-platelet drugs?
ADP (P2Y12) + P2Y1
platelets express PGY12 (Gi) + PGY1 (Gq)
T/F? PGY1 + PGY12 must both be activated in order to participate in platelet formation.
True
PGY12 (Gi coupled)- ADP receptor is effected by drugs
What do does the expression of GIIb/IIIa allow for?
cause platelets to bind to one another cross-linking w/ Fibrogen or vWF
What normally acts on PAR-1 receptors? What drug blocks PAR-1 receptors Vorapaxar
Thrombin
Name the drugs: COX-1 inhibitors
ASA
Name the drugs: PAR-1 (thrombiin) inhibitory
VoRAPraxar (Zontivity)
Name the drugs: GIIb/IIIa inhibitors (TEA)
Tirofiban
Epitfibatide
Abciximab (monoclonal antibody)
Name the drugs: PDE inhibitors
Cilostazol
ASA + Dip (Aggrenox)
Name the drugs: ADP inhibitors (CYP/CTP)
Cangrelor (Kengreal)
*TICAgrelor (Brilinta)- parent+ prodrug (active metabolite)
Prasugrel (Effient)
Plavix (clopidogrel)
Which ADP drugs are prodrugs (2)?
IV?
active parent + metabolite?
- Plavix + (Prasugrel) Effient (irreversible)
Cangrelor (Kengreal)
Ticagrelor (Brilinta) -BID
ADP irreversible drug? (2)
Plavix
Effient
ADP reversible drugs? (1)
CANgrelor (KENgrel) - IV
