Anti-platelet agents Flashcards

1
Q

Aspirin - Mechanism

A

Inhibits COX-1 synthesis of thromboxane A2

Low dose (81mg) is specific for anti-platelet activity - reaches highest concentrations in the portal vein, thus greater effect on circulating platelet COX-1 relative to tissue endothelial cell COX-2 (prostacyclin synthesis)

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2
Q

Aspirin - Pharmacokinetics

A

Once daily oral dosing

Hepatic elimination

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3
Q

Aspirin - Uses

A

Secondary prevention of MI and ischemic stroke

Acute MI & Unstable Angina (ACS)

Percutaneous Coronary Intervention

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4
Q

Aspirin - Adverse Reactions & DDIs

A

Dyspepsia
Nausea
Vomiting
GI bleeding

Increased bleeding risk with anticoagulants

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5
Q

Clopidrogel & Prasugrel - Mechanism

A

Platelet ADP P2Y12 receptor antagonist; interferes with ADP-induced platelet aggregation via irreversible receptor inhibition

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6
Q

Clopidrogel - Adverse Reactions & DDIs

A

Bleeding (P & T > C)
Dyspepsia
Gastritis
Headache

Use of proton pump inhibitors may decrease efficacy

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7
Q

Dipyridamole - Mechanism

A

Phosphodiesterase inhibitor; blocks degradation of cAMP - elevated cAMP levels potentiate prostacyclin’s anti-aggretory action

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8
Q

Aggrenox

A

Aspirin + Dipyridamole

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9
Q

Dipyridamole - Adverse Reactions

A

GI upset
Dizziness
Headache
Nausea

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10
Q

Abciximab - Mechanism

A

Fab fragment of humanized monoclonal antibody to IIb/IIIa receptors on platelets; prevents fibrinogen binding and subsequent platelet aggregation

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11
Q

Abciximab - Pharmacokinetics

A

Administered by continuous IV infusion

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12
Q

Ticagrelor - Mechanism

A

Reversible inhibition of platelet ADP (P2Y12) receptor; interferes with ADP-induced platelet aggregation

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13
Q

Clopidogrel, Prasugrel & Ticagrelor - Pharmacokinetics

A

Clopidogrel & Prasugrel - Once daily oral administration, hepatic metabolism to active metabolite via CYP450, renal/fecal elimination

Ticagrelor - Twice daily oral administration, hepatic metabolism to active metabolite

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14
Q

Ticagrelor - Adverse Reactions

A

Bleeding (P & T > C)
Dyspnea
Bradyarrhythmias

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15
Q

Clopidogrel, Prasugrel, and Ticagrelor - Uses

A

Acute MI & Unstable Angina (ACS)

Percutaneous Coronary Intervention

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16
Q

Eptifibatide

A

Cyclic peptide inhibitor platelet GIIb/IIIa receptor; prevents fibrinogen binding and subsequent platelet aggregation

Administered by IV infusion
Renal elimination

AR: Bleeeding

Use: Percutaneous Coronary Intervention

17
Q

Dipyridamole - Uses

A

Secondary prevention of MI & Stroke

18
Q

Tirofiban

A

Non-peptide inhibitor of Platelet IIb/IIIa receptor; prevents fibrinogen binding and subsequent platelet aggregation

Administered by IV infusion, renal elimination

AR: Bleeding

Use: Percutaneous Coronary Intervention