Thrombolytics Flashcards

1
Q

How does plasmin circulate

A

in inactive form

inactivated by a2 antiplasmin

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2
Q

tPA is a ____ that cleaves ______ to activate plasmin

A

serine protease

arg-val bond

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3
Q

tPA is inhibited by

A

PAI-1 & PAI-2

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4
Q

___ forms activator complex with plasminogen

A

streptokinase

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5
Q

These catalyze conversion of plasminogen to plasmin

A

Alteplase, Reteplase, Urokinase

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6
Q

_____ inhibits plasminogen –> plasmin

A

aminocaproic acid

(derivative and analog of lysine)

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7
Q

Indications for thrombolytic therapy

A

AMI (asap)

Acute Ischemic Thrombotic stroke (within three hours)

PE

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8
Q

tPA’s

A
  • Alteplase
  • Reteplase (more potent, faster onset, NO FIBRIN SPECIFICITY b/c lacks binding domain
  • Tenecteplase (more fibrin specific than tPA, long half life)
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9
Q

Tenecteplase has point mutations in these domains.

Function of mutations?

A

Kringle, Protease

  • Increase T1/2
  • reduce inhibition by PAI
  • enhance activity at thrombus
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10
Q

These lack fibrin specificity

A

Reteplase, Streptokinase

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11
Q

tPA DOA, Clearance, AE’s

A

5-10 min

Liver & Kidney

Bleeding (internal or superficial)

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12
Q

Streptokinase forms __________

A

1:1 complex with plasminogen

to produce an active enzyme complex that catalyzes (plasminogen –> plasmin)

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13
Q

Urokinase Dosing, indications, AE’s

A

IV dose with 15-20 min half life

Massive PE

Bleeding and Allergic rxn (rare)

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14
Q

Anti-fibrinolytic agents used to…

A

to stop bleeding caused by thrombolytic drugs

Plasmin binds to fibrin through LYSINE site to activate fibrinolysis…. need drugs that act as lysine analogs

Aminocaproic acid, Tranexamic acid (10x more potent)

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15
Q

Clinical indications and AE’s for anti-fibrinolytics

A

Bleeding associated with thrombolytic therapy, adjunct therapy in hemophelia, rebleeding from intracranial aneurysms

Intravascular thrombosis (not easily lysed!)

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16
Q

Tranexamic acid and aminocaproic acid prevent…

A

binding of plasminogen and plasmin to fibrin, sparing clots and preventing hemorrhage