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BNF/Pre-Reg 2017-2018 > CV: Antiplatelet drugs > Flashcards

CV: Antiplatelet drugs Flashcards

1
Q

Why are antiplatelet drugs successful in preventing thrombus formation in the arterial circulation?

A

In the faster flowing vessels, thrombi are composed mainly of platelets with little fibrin (opposite in slower moving venus)

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2
Q

Aspirin is used in what? primary or secondary prevention?

A

The use of aspirin in primary prevention of cardiovascular events, in patients with or without diabetes, is of unproven benefit.

Long-term use of aspirin is of benefit in established cardiovascular disease (secondary prevention); unduly high blood pressure must be controlled before aspirin is given.

If high risk of GI bleeding, PPI can be used.

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3
Q

Before the initiation of aspirin for secondary prevention, uncontrolled what needs to be treated?

A

hypertension

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4
Q

What is the mechanism of action of aspirin?

A

Aspirin inhibits platelet cycloxygenase, a key enzyme in thromboxane A2 (TXA2) generation.

Thromboxane A2 triggers reactions that lead to platelet activation and aggregation, aspirin acts as a potent antiplatelet agent by inhibiting generation of this mediator.

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5
Q

Clopidogrel is licensed for the prevention of atherothrombotic events in patients with a history of symptomatic ischaemic disease.

Clopidogrel, in combination with low-dose what?, is also licensed for ACS without ST-segment elevation.

How long is this combination given for?

A

Clopidogrel is licensed for the prevention of atherothrombotic events in patients with a history of symptomatic ischaemic disease. Clopidogrel, in combination with low-dose aspirin, is also licensed for acute coronary syndrome without ST-segment elevation; in these circumstances the combination is given for up to 12 months (most benefit occurs during the first 3 months; there is no evidence of benefit beyond 12 months).

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6
Q

Clopidogrel, in combination with low-dose aspirin, is also licensed for acute myocardial infarction WITH ST-segment elevation. How does the length of treatment for STEMI differ to NSTEMI?

A

Clopidogrel, in combination with low-dose aspirin, is also licensed for acute myocardial infarction with ST-segment elevation; the combination is licensed for at least 4 weeks, but the optimum treatment duration has not been established.

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7
Q

When would clopidogrel, combination with low-dose aspirin, be used for the prevention of atherothrombotic and thromboemobolic events in patients with AF (and at least one risk factor for a vascular event)?

A

When warfarin sodium is unsuitable.

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8
Q

How does clopidogrel work?

A

The active metabolite of clopidogeel selectively inhibits the binding of adenosine diphosphate (ADP) to its platelet P2Y12 receptor and the subsequent ADP-mediated activation of the glycoprotein GPIIb/IIIa complex, thereby inhibiting platelet aggregation.

This action is irrerversible.

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9
Q

What is dipyridamole used by mouth as an adjunct to?

A

Dipyridamoleis used by mouth as an adjunct to oral anticoagulation for prophylaxis of thromboembolism associated with prosthetic heart valves. Modified-release preparations are licensed for secondary prevention of ischaemic stroke and transient ischaemic attacks.

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10
Q

Modified-release preparations of dipyridamole are licensed for what? (2)

A

Dipyridamoleis used by mouth as an adjunct to oral anticoagulation for prophylaxis of thromboembolism associated with prosthetic heart valves. Modified-release preparations are licensed for secondary prevention of ischaemic stroke and transient ischaemic attacks.

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11
Q

How does dipyridamole work?

A

Dipyridamole inhibits the phosphodiesterase enzymes that normally break down cAMP (increasing cAMP levels and blocking the platelet aggregation response to ADP) and/or cGMP.

(Also interacts with adenosine: inhibits the cellular reuptake of adenosine into platelets, red blood cells, and endothelial cells leading to increased extracellular concentrations of adenosine)

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12
Q

Prasugel, in combination with aspirin, is licensed for the prevention of atherothrombotic events in patients with acute coronary syndrome undergoing PCI; how long is the combination given for?

A

up to 12 months

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13
Q

Irreversible inhibitor of the binding of ADP to P2Y12 receptor

A

Clopidogrel

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14
Q

How does Prasugel work?

A

The same way to Clop, its active metabolite prevents the binding of ADP to its platelet receptor.

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15
Q

Ticagrelor, in combination with aspirin, is licensed for what?

A

The prevention of atherothrombotic events in patients with ACS; the combination is usually given for up to 12 months.

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16
Q

How does Ticagrelor work?

A

REVERSIBLE inhibitor of P2Y12ADP receptor on platelets.

17
Q

Phosphodiesterase inhibitor that leads to increased cellular cAMP levels and blocked platelet aggregation response to ADP

A

Dipyridamole inhibits the phosphodiesterase enzymes that normally break down cAMP (increasing cAMP levels and blocking the platelet aggregation response to ADP) and/or cGMP.

(Also interacts with adenosine: inhibits the cellular reuptake of adenosine into platelets, red blood cells, and endothelial cells leading to increased extracellular concentrations of adenosine)

18
Q

With regards to coronary stents, in what circumstances is clopidogrel given for 12 months vs 1 month following placement?

A

. Clopidogrel is recommended for 1 month following elective percutaneous coronary intervention with placement of a bare-metal stent, and for 12 months if percutaneous coronary intervention with placement of a bare-metal stent was for an acute coronary syndrome; clopidogrel should be given for 12 months following placement of a drug-eluting stent.

19
Q

Glycoprotein IIb/IIIa inhibitors work how?

A

They prevent platelet aggregation by blocking the binding of fibrinogen to receptors on platelets.

20
Q

Abcimiximab is a monoclonal antibody which binds to glycoprotein IIb/IIIa receptors and to other related sites; it is licensed as an adjunct to what in what circumstances?

A

Abciximab is a monoclonal antibody which binds to glycoprotein IIb/IIIa receptors and to other related sites; it is licensed as an adjunct to heparin (unfractionated) and aspirin for the prevention of ischaemic complications in high-risk patients undergoing percutaneous transluminal coronary intervention.

21
Q

How often should the monoclonal antibody abcimiximab be used? Why?

A

Abcimiximab should be used once daily (to avoid the additional risk of thrombocytopenia).

22
Q

Eptifibatide (in combination with heparin and aspirin) inhibits glycoprotein IIb/IIIa receptors and is licensed in what?

A

Eptifibatide is licensed for use to prevent early myocardial infarction in patients with unstable angina OR non-ST-segment-elevation MI.

23
Q

Tirofiban is another glycoprotein IIb/IIIa inhibitor which is licensed both for the prevention of early MI in patients with UA or NSTEMI and for the reduction of major CV events in patients with STEMI intended for PCI. What must it be used in combination with?

A

Tirofiban is always used with aspirin, clopidogrel and unfract heparin.

24
Q

When is epoprostenol used?

A

It is used to inhibit platelet aggregation during renal dialysis when heparins are unsuitable or contra-indicated.

25
Q

How does epoprostenol work?

A

Epoprostenol (prostacyclin) is a member of the eicosanoid family of lipid molecules.

It causes decreased Thromboxane-A2 and PDGF.

Also see iloprost a synthetic prostacylin analogue used as a vasodilator in severe raynauds phenomenon or ischiemia of limb; pulmonary hypertension and primary pulmonary hypertension.

26
Q

Phosphodiesterase inhibitor

A

Dipyridamole PDE5

27
Q

ADP receptor antagonists (3)

A

Clopidogrel
Prasugrel
Ticagrelor - reversible

28
Q

COX inhibitor

A

Aspirin irrerversibly inhibits COX-1, thereby blocking the formation of thromboxane A2

29
Q

Glycoprotein IIb/IIIa receptor antagonists (3)

A

Abciximab - irrerversible
Tirofiban - reversibly
Eptifibatide

30
Q

What type of drug is Cilostazol?

A

PDE3 inhibitor.
It is used to treat intermittent claudication. (See peripheral vascular disease deck).

Similar drug to dipyridamole.

31
Q

Glycoprotein IIb/IIIa receptor antagonists are most commonly used when?

A

Deployed during the surgical procedure (PCI) where stents are placed into narrowed vessels. They work by antagonising these receptors on the surface of platelets, with abciximab binding irrerversibly and tirofiban binding reversibly.

32
Q

What side effects can abciximab cause?

A 
Bleeding
Thrombocytopenia
Nausea 
Vomiting
HYPOTENSION
Headache
33
Q

Which of the following is NOT a prodrug?

Clopidogrel
Prasugel
Ticagrelor

A

Ticagrelor is not a pro drug.

BNF/Pre-Reg 2017-2018 (144 decks)

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