Drugs Used In Coagulation Disorders III: Fibrinolytic Drugs. Drugs Used In Bleeding Disorders. Flashcards

1
Q

What is fibrinolysis?

A

The conversion of plasminogen to plasmin which then hydrolysis fibrin

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2
Q

What type of enzyme is plasmin?

A

Serine protease

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3
Q

Name the fibrinolytic drugs

A
Streptokinase
Anistreplase
Staphylokinase
Urokinase
Tissue plasminogen activator (tPA) 
Reteplase
Tenecteplase
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4
Q

What are the clinical indications of fibrinolytic drugs?

A

Multiple PE
Central DVT
Stroke
AMI

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5
Q

When is streptokinase active?

A

Enzymatically it is not active by itself, it must be bound to plasminogen in a 1:1 complex

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6
Q

What is the action of the streptokinase:plasminogen complex?

A

The complex can convert plasminogen to plasmin — then there is hydrolysis of fibrin plugs + the degradation of fibrinogen, V and VII

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7
Q

What is the half life of Streptokinase?

A

20-40mins

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8
Q

How is Streptokinase administered?

A

IV infusion

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9
Q

What is the half life of Anistreplase?

A

1.5h

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10
Q

What is the half life of Urokinase?

A

15m

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11
Q

What is the half life of Reteplase?

A

15-18 mins

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12
Q

What is the benefit of Reteplase over Alteplase?

A

Longer half life

Less expensive

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13
Q

How is Reteplase administered?

A

IV: 2 bolus separated by 30 mins

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14
Q

How is Tenecteplase administered?

A

IV: only 1 injection

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15
Q

What type of enzyme is tPA?

A

Serine protease

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16
Q

What is the mechanism of action of tPA?

A

Converts plasminogen to plasmin directly

17
Q

What type of enzyme is Urokinase?

A

Serine protease

18
Q

What is the mechanism of action of Urokinase?

A

Converts plasminogen to plasmin directly

19
Q

What are the contraindications of the fibrinolytic drugs?

A
Active bleeding 
Serious GI or cerebral bleeding within 3 months
Surgery
Severe trauma within 10 days 
Severe HTN
Aortic dissection
Acute pericarditis
20
Q

What are the major adverse effects of the fibrinolytic drugs?

A

Bleeding: incidence: 15%, lethal: 0.5%

Staphylokinase, streptokinase and Anistreplase may cause hypersensitivity reactions