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pharmacology cardiovascular > Antiplatelet and fibrinolytic drugs > Flashcards

Antiplatelet and fibrinolytic drugs Flashcards

1
Q

What are antiplatelet drugs primarily used for

A

Arterial thrombosis

  • Acute myocardial infarction
  • In patients with risk of myocardial infarction
  • Following coronary bypass
  • Unstable coronary syndromes
  • Following coronary artery angioplasty
  • Transient cerebral ischaemic attack or thrombotic stroke
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2
Q

Give an example of an COX inhibitor that is an antiplatelet

A

Asprin

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3
Q

what is the mechanism of action of asprin

A
  • It irreversibly inactivates COX 1/ 2 (cyclooxygenase) resulting in decreased levels of TXA2 and consequentially inhibition of vasoconstriction and platelet aggregation
  • Platelets then take 7-10 days to replace COX but endothelial cells can replace it immediately
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4
Q

Describe the different dosages of asprin and what they are used for

A
  • Low dose (180mg/day) → effective in preventing a mini storke
  • 335mg/day → reduce risk of heart attack
  • > 1000mg/day → no effect die to great inhibiton of endothelial COX
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5
Q

What is the clinical use of asprin

A

•In acute myocardial infarction in combination with fibrinolytic drugs

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6
Q

Give examples of antiplatelet drugs that are ADP receptor antagonists

A

Ticlopidine
Clopidogrel
Prasugrel
Ticagrelor

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7
Q

What is the mechanism of action of Ticlopidine,

Clopidogrel and Prasugrel

A
  • Irreversible antagonist at the ADP receptor thereby reducing the release of ADP
  • This prevents the expressing of glycoprotein IIBb/IIIa receptors and consequentially reduces platelet aggregation
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8
Q

what is the mechanism of action of Ticagrelor

A
  • Reversible antagonist at the ADP receptor thereby reducing the release of ADP
  • This prevents the expressing of glycoprotein IIBb/IIIa receptors and consequentially reduces platelet aggregation
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9
Q

what is the onset of action of Ticlopidine

A

•Slow onset of 3-7 days

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10
Q

What is the clinical use of Ticlopidine

A

•Reducing the risk of stroke

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11
Q

What are the side effects of Ticlopidine (which consequentially limit the use of the drug)

A
  • Rash
  • Dirrhoea
  • Neutropenia
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12
Q

How is Clopidogrel administrated

A

• Prodrug, oral administration

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13
Q

What is the clinical use of Clopidogrel

A
  • In combination with asprin

* It reduces the risk of ischaemic stroke, myocardial infarction and vascular death

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14
Q

What are the side effects of Clopidogrel

A

•Less side effects than Ticlopidine especially neutropenia

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15
Q

What is the onset of Prasugrel

A
  • Faster onset than clopidogrel

* Hours

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16
Q

What are the side effects of Prasugrel

A

•More efficacious than clopidogrel so greater chance of bleeding

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17
Q

what is the efficacy of Ticagrelor

A

•Similar efficacy to prasugrel and clopidogrel

18
Q

what is the clinical use of Ticagrelor

A

•Its reversibility is an asset in certain clinical scenarios

19
Q

give examples of antiplatelet drugs that are IIb/IIIa receptor antagonists

A

Abciximab/ Tirfiban

Tirofiban/ Eptifibatide

20
Q

what is the mechanism of action of Abciximab and Tirfiban

A

•It is an antibody fragment directed at inhibiting the GP IIb/IIIa receptor and consequentially inhibiting platelet aggregation

21
Q

What is the clinical use of Abciximab and Tirfiban

A

•Used by IV infusion in high risk coronary angioplasty patients with heparin and asparin

22
Q

Why can Abciximab and Tirfiban only be administered once

A

•Its immunogenicity limits the use to a single administration

23
Q

What is the platelet recovery time following Abciximab or Tirfiban use

A

•Platelet function is recovered in days

24
Q

What is the mechanism of action of Tirofiban and Eptifibatide

A

•Cyclic peptides which lesemble IIb/IIIa ligands

25
Q

How ar Tirofiban and Eptifibatide administrated

A

•IV

26
Q

What is the platelet recovery time following Tirofiban or Eptifibatide use

A

•hours

27
Q

give an example of an antiplatelet drug that is a Prostaglandin agonist

A

Epoprostenol

28
Q

How is Epoprostenol given

A

IV

29
Q

When is Epoprostenol given (clinical use)

A

Administered in patients undergoing haemodialysis where heparin contraindicated

30
Q

Give an example of an antiplatelet drug that is a Phosphodiesterase inhibitor

A

Dipyridamole

31
Q

what is the mechanism of action of Dipyridamole

A

•Inhibits phosphodiesterase and increase platelet camp levels

32
Q

When is Dipyridamole used?

A

•In conjunction with asparin

33
Q

Give examples of fibrinolytic agents

A 
streptokinase 
Recombinant tPA (tissue plasminogen activator)
34
Q

What is the mechanism of action of streptokinase

A

•It binds and activates plasminogen so that the clot is then broken down

35
Q

What is the pharmacokinetics of streptokinase and how often can it be given

A
  • Action is blocked by antistreptococcal antibodies after 4 days
  • Therefore you must wait one year before it can be administrated again
36
Q

Give examples of Recombinant tPA (tissue plasminogen activator) and the administrtation/half life

A

Alteplase → Short half life so IV infusion
Duteplase→Short half life so IV infusion
Reteplase→ longer half-life so can give as IV bolus

37
Q

what is the mechanism of action of Recombinant tPA (tissue plasminogen activator)

A

Converts plasminogen to plasmin which breaks down the clots

It is more acitive at fibrin bound plasminogen so it is ‘clot’ specific

38
Q

what are the Absolute containidictions of fibrinolytic agents

A

Active or recent internal bleeding
•Recent cerebrovascular accident
•Invasive procedures where haemostasis is important

39
Q

what are the Relative containidictions of fibrinolytic agents

A
  • Pregnancy
  • Cardiopulmonary resuscitation
  • Trauma
  • Bacterial endocarditis
40
Q

what are the Unwanted effects of fibrinolytic agents

A
  • GI haemorrhage / stroke (treat with tranexamic acid)
  • Low grade allergic reactions / fever
  • Burst of plasmin generated by steptokinase can generate kinins thereby causing hypotension
41
Q

what are the Clinical uses of fibrinolytic agents

A
  • In acute myocardial infarction (within 12 hrs of onset, sooner the better)
  • Acute thrombotic stroke
  • Clearing thrombosed shunts / cannulae
  • Acute arterial thromboembolism

pharmacology cardiovascular (9 decks)

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