Fibrinolytics Flashcards

1
Q

What are the synthetic tPA drugs?

A

Alteplase
Reteplase
Tenecteplase

shortest to longest duration <5 minutes thru 20-25 minutes.

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2
Q

What is alteplase

A

recombinant tPA -activates plasminogen to plasmin

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3
Q

What is Reteplase

A

Recombinant tPA with the fibrin binding domain removed.

Acts more rapidly and lasts about 15 minutes instead of 5.

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4
Q

What is Tenecteplase

A

Recombinant tPA that is PAI-1 resistant.

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5
Q

What are the antidotes to the fibrinolytics

A

Aminocaproic Acid - competitive inhibitor of plasminogen activator proteins. Competes with plasminogen for binding site.

Aprotinin - plasmin, trypsin, kallekrein, general serine protease inhibitor

Fresh Frozen Plasma
Cryoprecipitate
Coagulation factor concentrates

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6
Q

What are the non-tPA fibrinolytics?

A

Streptokinase
Anistreplase
Staphylokinase
Urokinase

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7
Q

What is Anistreplase

A

A bound complex of streptokinase and plasminogen together

Also acts to activate endogenous plasminogen

half life 1.5 hours

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8
Q

What is the half life of streptokiase?

A

30 minutes. given i.v. (all thrombolytics are given i.v.)

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9
Q

What is Staphylokinase

A

Same effects and mech as streptokinase but slightly less effective and less antigenic

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10
Q

What is Urokinase

A

Human enzyme isolated from urine.

Not immunogenic,

half life 15 minutes.

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11
Q

What are the indications for fibrinolytic treatment

A

Acute MI if PCI is unnavailable within 2 hours

Severe DVT of PE with hemodynamic instability

Ischemic stroke, within 4.5 hours of symptom onset.

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12
Q

Contraindications for fibrinolytis

A

Any active internal bleeds

Significant trauma or surgery within the past 10 days, especially head trauma

Significant GI or Cranial bleeding within the past 3 months

Severe hypertension

Aortic dissection or Aortic pericarditis.

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13
Q

Fibrinolytic SEs

A

Bleeding, especially intracranial bleeding.

  • Bleeding complications as high as 15% of patients.
  • Lethal bleeding in 0.5%

Allergic and anaphylactic reactions possible to Streptokinase, Anistreplase, and Staphylokinase

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14
Q

Drugs used in bleeding disorders

A

Local:

  • Vasoconstrictors, Epinephrine, NE, Desmopressin
  • Collagen, Gelatin, Fibrin meshes
  • Injections/sclerotherapy to vericose veins/hemorrhoids

Systemic:

  • Vitamin K orally
  • Fresh Frozen plasma
  • Cryoprecipitates of concentrated cotting factors
  • Aminocaproid acid and its derivatives
    antidote for fibrinolytics
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15
Q

When is amiocaproic acid used?

A

In fibrinolytic overdose

Prophylactic therapy for hemophilia

Post-surgical bleeding

Prophylaxis for intracranial aneurysm rebleeding.

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16
Q

What is Aprotinin

A

bovine pancreatic trypsin inhibitor (BPTI),

an antifibrinolytic molecule that inhibits trypsin and related proteolytic enzymes.

inhibits plasmin, trypsin, kallikrein, chymotrypsin

only administered i.v.

17
Q

What is Aprotinin’s indications

SEs

A

Bleeding from thrombolytics

Used in devices for extracorporeal circulation

SEs:
Allergic, anaphylctic reactions

Reversible liver damage and decreased kidney function.