Thrombolytic Drugs Flashcards

1
Q

What classes of drugs are antiplatelet?

A

Aspirin, ADP receptor antagonists, GpIIb-GpIIIa receptor inhibitors

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2
Q

How does Aspirin (acetylsalicylic acid) work?

A

irreversible COX-I inhibitor

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3
Q

What is the general mechanism for ADP receptor antagonists?

A

irreversibly bind ADP receptor and prevent activation of platelets

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4
Q

What drugs are ADP receptor antagonists?

A

Ticlopidine, Clopidogrel, Prasugrel

-used in stents for ppl that don’t tolerate aspirin

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5
Q

What is the mechanism of Dipyridamole?

A

increases cAMP by blocking phosphodiesterase 3 –> inhibits platelet activation

  • little benefit on own
  • use with warfarin/aspirin
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6
Q

What drugs are GpIIb-GpIIIa receptor inhibitors?

A

Abiciximab, Eptifibatide, Tirofiban

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7
Q

What is the MOA for GpIIb-GpIIIa?

A

prevent binding of adhesive glycoproteins (fibrinogen/vWF) to activated platelets –> inhibits common pathway

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8
Q

What is specific about GpIIb-GpIIIa use?

A

IV admin.

used during angioplasty with heparin and aspirin

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9
Q

What drugs are the anti-coagulants?

A

Heparin (and derivatives), Dabigatran etexylate, Fondaparinux
-inhibit thrombin

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10
Q

What is the action of heparin?

A

binds to thrombin and DIRECTLY inhibits the enzyme from converting fibrinogen –> fibrin

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11
Q

What drugs are heparin derivatives?

A

lepirudin, bivalirudin, argatroban

also dabigatran etexylate (oral)

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12
Q

What is unique about admin. heparin and its derivatives?

A

must be admin. via IV

-Dabigatran etexylate is oral

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13
Q

What are the indirect inhibitors of thrombin (indirect anti-coags)?

A

unfractionated heparin (HMW), LMWH, Fondaparinux

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14
Q

What is the action of indirect anti-coag drugs?

A

enhance action of Antithrombin III to inhibit Factor Xa (results in no thrombin)

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15
Q

What is unique about Unfractionated Heparin and LMWH?

A

can bind antithrombin and thrombin to cause thrombin inhibition
-Fondaparinux cannot bind thrombin

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16
Q

What test is used to monitor heparin dosing?

A

partial thromboplastin time (PTT)

-LMWH doesn’t need to be monitored

17
Q

What is the action of protamine?

A

heparin antidote

18
Q

What is the mechanism of protamine?

A

basic, + charged molecule binds - charged heparin to form stable complex that isn’t active

19
Q

What is the action of Warfarin?

A

inhibits conversion of oxidized Vitamin K epoxide to reduced Vitamin K hydroquinone

20
Q

What is Vitamin K needed for in coagulation?

A

needed for gamma carboxylation of factors II, VII, IX, X, and Protein C and S

21
Q

Why is a patient on Warfarin initially hypercoagulable?

A

warfarin inhibits Protein C and S first that inhibit clotting; takes a few days before all of reduced Vit. K can be used up
-must admin another drug to bridge patient

22
Q

How is warfarin monitored?

A

INR (PT) - looks at Factor VII, which is the first to be affected

23
Q

What causes people to require different doses of Warfarin?

A

polymorphisms in VKOR1 gene

24
Q

What is the major issue with Warfarin?

A

low Tx index and tons of drug interactions

25
Q

What drugs are direct Factor Xa inhibitors?

A

Rivaroxaban, Apixaban, Exodaban

26
Q

What is the antidote for Warfarin?

A

Phytonadione (Vitamin K) - competes with Warfarin activity to cause coagulation

27
Q

What drugs are fibrinolytics?

A

tPAs, Streptokinase, Urokinase

28
Q

What drug is a fibrinolytic inhibitor?

A

Aminocaproic acid - blocks interaction of plasmin with fibrin –> reduces bleeding

29
Q

What drugs are tPAs?

A

Alteplase, Reteplase, Tenecteplase

30
Q

What is the MOA for the tPAs?

A

Selectively activate plasminogen that is bound to fibrin –> confines thrombus
tPA = tissue plasminogen activator

31
Q

What are the uses for tPAs?

A

given IV after ischemic stroke

pharmacologic conc. of tPA can induce systemic lytic state

32
Q

What is the action of Streptokinase?

A

complexes with plasminogen WHEREVER it is and helps formation of plasmin - not specific for clot site

33
Q

What is the action of Urokinase?

A

kidney enzyme that directly converts plasminogen to plasmin - promotes fibrinolysis