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Flashcards in Antiplatelet and Antithrombotics Deck (8)
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Aspirin- MOA, Onset of Action, Administration Route, Elimination, Adverse Effects, Safety in Pregnancy, DDIs, Uses

Lose dose (81mg) "selective" inhibition of platelet COX-1 (irreversible), can be rapid, oral-once daily, hepatic, gastric upset, bleeding, pregnancy category C/D (3rd), increase in bleeding risk with anticoagulants, acute MI-Unstable angina (ACS), PCI-2ndary prevention MI-stroke.

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Ticegrelor, Clopidogrel, Prasugrel- MOA, Onset of Action, Administration Route, Elimination, Adverse Effects, Safety in Pregnancy, DDIs, Uses

MOA: Inhibition of platelet ADP, (P2Y12) receptor, [C,P] irreversible, [T] reversible, Efficacy (P-T >C). OOA: Onset -2hrs; peak 2-5 hrs if loading dose is used, otherwise 3-7 days. (C-P) oral prodrug-once daily, T- oral-twice daily. C: activated by CYP2C19, then renal and fecal excretion. P: activated by CYP34A/2B6. T: CYP3A4 metabolism to active metabolite. Bleeding (P-T >C). C: Pregnancy category B. P-T: Pregnancy Category C. C: PPIs may block activation of prodrug by CYP2C19. No DDI with [P]+ PPIs. Acute MI- Unstable angina, PCI.

2

Dipyridamole- MOA, Onset of Action, Administration Route, Elimination, Adverse Effects, Safety in Pregnancy, DDIs, Uses

Inhibits PDE in platelets -> increase cAMP -> increase PGI2, anti-aggregation effect. Oral. Hepatic: phase II conjugation. Dizziness, HA, nausea, GI upset. Pregnancy category B. 2ndary prevention, MI-stroke.

3

Abciximab [A]- Eptifibatide [E], Tirofiban [T]: MOA, Onset of Action, Administration Route, Elimination, Adverse Effects, Safety in Pregnancy, DDIs, Uses

Blocks platelet GIIb/IIIa receptor preventing fibrinogen binding and platelet aggregation. A: monoclonal Ab. E: cyclic peptide. T: non-peptide. Rapid onset. Parental infusion. A: renal, t1/2- 30 min. E: renal, t1/2- 2.5 hours, T: renal, t1/2 2 hrs. Bleeding. A: PC C. E: PC B. T: PC B. PCI.

4

Heparin UFH: MOA, Onset of Action, Administration Route, Elimination, Monitoring Lab Test, Adverse Effects, Safety in Pregnancy, DDIs, Overdose Tx, Uses

Binds ATIII -> inactivates IIa and Xa. Rapid (minutes if IV w/ LD). Parenteral (IC/SC). Dose dependent t1/2 cleared by RES. aPTT (can use anti-factor Xa prn). Bleeding/ thrombocytopenia. Safe. Antiplatelet agents. Protamine. ACS/ VTE.

5

LMWH (Enoxaparin-Dalteparin): MOA, Onset of Action, Administration Route, Elimination, Monitoring Lab Test, Adverse Effects, Safety in Pregnancy, DDIs, Overdose Tx, Uses

Binds ATIII -> inactivates Xa. 3-5 hours SC. Parenteral (IV/SC). Renal clearance (decrease dose in renal failure). Not needed, action predictable. Dosed on mg/kg basis (can use anti-factor Xa prn). Bleeding/ thrombocytopenia. Safe. Antiplatelet agents. Protamine. ACS/ VTE.

6

Warfarin: MOA, Onset of Action, Administration Route, Elimination, Monitoring Lab Test, Adverse Effects, Safety in Pregnancy, DDIs, Overdose Tx, Uses

Inhibits liver synthesis of Vit K dep factors (II, VII, IX, and X). Delayed (hours to days). Oral. Hepatic metabolism- CYP2C9. INR (from PT). Bleeding, skin necrosis. NOT safe -> category X. Increase effect: CYP450-inhibitors, abx, decrease effect: CYP450inducers dietary Vit K. Phytonadione (Vit K1)- FFP. A fib/ VTE prophylaxis.

7

Dabigatran, Rivaroxaban, Apixaban: MOA, Onset of Action, Administration Route, Elimination, Monitoring Lab Test, Adverse Effects, Safety in Pregnancy, DDIs, Overdose Tx, Uses

D: direct thrombin IIa inhibitor. R,A: direct factor Xa inhibitor. D: peak 1-2 h, 2-3 d to steady state, R,A: peak action 2.5-4h. D: oral-administered as prodrug. R,A: hepatic CYP3A, A: BID. D,R: not routinely monitored. D: Bleeding, gastritis symptoms. R: Bleeding DRA: Category C- not studied. Decrease effect: DRA P-glycoprotein inducers (rifampin, dronedarone). Increase effect (DRA) P-glycoprotein inhibitors; R CYP3A4 inhibitors. DRA: no specific antidote.
All A-fib. D: VTE (non-FDA approved). R: DVT-PE prevention after total hip or knee replacement.