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Pharmacology > Fibrinolytics > Flashcards

Fibrinolytics Flashcards

1
Q

What is haemostasis?

A

Cessation of blood loss from a damaged vessel.

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2
Q

What is thrombosis?

A

A pathological condition resulting from inappropriate activation of haemostatic mechanisms.

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3
Q

What characterizes venous thrombosis?

A

Usually associated with stasis of blood; small platelet component and large component of fibrin.

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4
Q

What characterizes arterial thrombosis?

A

Usually associated with atherosclerosis; large platelet component.

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5
Q

Define thrombus.

A

A blood clot formed in situ within the vascular system, impeding blood flow.

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6
Q

What is the role of thrombin in blood clotting?

A

Converts soluble fibrinogen to an insoluble meshwork of fibrin.

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7
Q

What are the two limbs of the clotting cascade?

A

In vivo (extrinsic) pathway - Rapid; in vitro (intrinsic) pathway - Slow.

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8
Q

What is the function of calcium ions in coagulation?

A

Essential for activation of factors IXa, VIIa, and Xa.

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9
Q

What is haemophilia A caused by?

A

Lack of factor VIII.

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10
Q

What is the primary use of antithrombotic drugs?

A

To treat thrombosis.

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11
Q

What are the three classifications of antithrombotic drugs?

A
  • Antiplatelet drugs
  • Anticoagulants
  • Fibrinolytic agents
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12
Q

What is the action of heparin?

A

Inhibits plasma antithrombin III.

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13
Q

What are common adverse effects of heparin?

A
  • Bleeding
  • Thrombocytopaenia
  • Hypersensitivity reactions
  • Osteoporosis
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14
Q

What is the mechanism of action of low molecular weight heparins?

A

Accelerates action of antithrombin III, increasing inactivation of factor Xa.

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15
Q

What is the main use of direct thrombin inhibitors?

A

Directly inhibit thrombin without relying on antithrombin III.

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16
Q

What is dabigatran used for?

A

Prevention of venous thromboembolism and stroke in atrial fibrillation.

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17
Q

What is the mechanism of action of warfarin?

A

Inhibits the reduction of vitamin K, preventing carboxylation of factors II, VII, IX, and X.

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18
Q

What is streptokinase and its primary use?

A

A plasminogen activating protein used to reduce mortality in acute myocardial infarction.

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19
Q

What are the adverse effects of streptokinase?

A
  • Nausea
  • Headache
  • Dizziness
  • Low blood pressure
  • Mild fever
  • Bleeding
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20
Q

What is epsilon amino-caproic acid (EACA)?

A

A lysine analogue that inhibits plasminogen activation and is used to check fibrinolysis associated bleeding.

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21
Q

What is the treatment for overdose of heparin?

A

Protamine sulfate.

22
Q

Fill in the blank: The drug _______ is a recombinant tissue plasminogen activator.

A

Alteplase

23
Q

True or False: Direct thrombin inhibitors require monitoring of activated partial thromboplastin time (aPTT).

A

False

24
Q

What is the primary indication for using antifibrinolytic drugs?

A

To counteract the effect of fibrinolytic agents and bleeding due to their use.

25
Q

What can rapid intravenous injection of certain drugs cause?

A

Hypotension, bradycardia, and possible arrhythmias.

26
Q

What is a limitation of the large dose needed for specific treatments?

A

Tranexamic acid is mostly preferred.

27
Q

What is the initial priming dose of tranexamic acid?

A

5 g oral/i.v., followed by 1 g hourly till bleeding stops (max. 30 g in 24 hrs).

28
Q

What is the mechanism of action of tranexamic acid?

A

Inhibits plasminogen activation and thus prevents fibrinolysis.

29
Q

List some clinical uses of tranexamic acid.

A
  • Treat bleeding or risk of bleeding following prostatectomy or dental extraction
  • Menorrhagia (excessive menstrual blood loss)
  • Life-threatening bleeding following thrombolytic drug administration.
30
Q

How much more potent is tranexamic acid compared to EACA?

A

7 times more potent.

31
Q

What are the main side effects of tranexamic acid?

A
  • Nausea
  • Diarrhoea.
32
Q

What can occur infrequently as a side effect of tranexamic acid?

A
  • Thromboembolic events
  • Disturbed colour vision
  • Allergic reactions.
33
Q

What is the typical dosage range for tranexamic acid?

A

10–15 mg/kg 2–3 times a day or 1–1.5 g TDS oral, 0.5–1 g TDS by slow i.v. infusion.

34
Q

What are antiplatelet drugs used for?

A

Interfere with platelet function and are useful in the prophylaxis of thromboembolic disorders.

35
Q

What receptors do platelets express on their surface?

A

Several glycoprotein (GP) integrin receptors.

36
Q

What happens when reactive proteins like collagen react with platelet receptors?

A

Platelet activation and release of pro-aggregatory and vasoconstrictor mediators.

37
Q

What forms a ‘platelet plug’ in arteries?

A

The binding of fibrinogen and von Willebrand factor (vWF) to platelet GPIIb/IIIa receptors.

38
Q

In which type of thrombosis are antiplatelet drugs more useful?

A

Arterial thrombosis.

39
Q

Which substance synthesized in the intima of blood vessels inhibits platelet aggregation?

A

Prostacyclin (PGI2).

40
Q

What is the role of platelets in atherogenesis?

A

They play a role in atherosclerotic plaque formation leading to coronary artery heart disease.

41
Q

What is the mechanism of action of aspirin as an antiplatelet drug?

A

Inhibits cyclo-oxygenase irreversibly and inhibits platelet thromboxane (TX)A2 synthesis.

42
Q

What are the gastrointestinal side effects of aspirin?

A

Irritation of the stomach lining, gastrointestinal upset, ulcers, and bleeding.

43
Q

What is clopidogrel and how does it function?

A

A prodrug that irreversibly inhibits P2Y12 receptors and inhibits platelet aggregation.

44
Q

What is the clinical effect of clopidogrel in relation to aspirin?

A

Its clinical effect is additive with aspirin.

45
Q

What is prasugrel used for?

A

Acute coronary syndrome (ACS).

46
Q

How does ticagrelor differ from other antiplatelet drugs?

A

It is reversible but non-competitive.

47
Q

What do antagonists of GPIIb/IIIa receptors do?

A

Inhibit diverse agonists activating GPIIb/IIIa receptors.

48
Q

What is dipyridamole used for?

A

As a vasodilator for angina pectoris and in addition to aspirin for stroke or transient ischemic attack.

49
Q

List some clinical uses of antiplatelet drugs.

A
  • Acute myocardial infarction
  • Prevention of myocardial infarction in patients at high risk
  • Cerebral ischemic attack (ministrokes) or thrombotic stroke
  • Prevent recurrence in atrial fibrillation.
50
Q

What is the primary action of antiplatelet drugs?

A

To prevent arterial thrombosis.

Pharmacology (18 decks)

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