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Hemostasis Pharmacology
Anti-coagulants, anti-platelet, and Thrombolytic Drugs
25
Pharmacology
Graduate
11/12/2010

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Cards

Term
Hemostasis stages
Definition
Stage 1- Platelet Plug Formation

Stage 2- Coagulation
Term
Stage 1
Definition
-Platelets adhere to collagen in damaged vessel

-activated-massive aggregation of platelets through granule release of
TXA2 and ADP
Term
Stage 2
Definition
-fibrin cross linking of platelet formation
Term
Arterial Thrombosis
Definition
-Vascular injury at site of action

-Growth: Due to platelet adhesion

-Blood flow stops, coagulation takes place, and local tissue injury via loss blood flow
Term
Venous Thrombosis
Definition
-vascular injury not evident at site of initiation

-growth due to coagulation**

-source of DVT's***
Term
Anti-platelet drugs
Definition
-Prevention of arterial thrombosis
-Prevention of MI
-Prevention of stroke w/hx of TIA
-GPIIb/IIIa antagonists
*unstable angina
*stent intervention
Term
Anti-platelet drugs (ex.s)
Definition
COX inhibitors
-aspirin, indometh, ibuprofen,
cAMP modulators
-dipyridamole
ADP receptor antagonist
-clopidogrel
Glycoprotein IIb/IIIa receptor antagonis
-Abciximab
Term
Feedback inhibition of AA Cascade
Definition
-PGE and PGD exit platelet and attach to surface receptor
-receptor increases level of cAMP
-Phospholipase to AA is dampened
Term
NSAIDS
Definition
-block COX in platelets
-COX 1 predominant form in platelets
Term
Dypyridamole
Definition
-increases cAMP
-dampens production of AA from Phospholipase A
Term
COX 2 NSAID
Definition
-blocks PGI in endothelial cells
-lower PGI lead to decreased cAMP
-therefore AA is increased leading to more aggregation
Term
Anticoagulants: Parenteral
Definition
-Heparin drug of choice
-iv or sc admin
-fast acting
-plasma levels highly variable**
-Intensive monitoring required
-CAN be used in pregnancy
Term
Anticoagulants: Oral
Definition
-Warfarin drug of choice
-oral admin, slow onset of activity
-antagonizes vitamin K
-CANNOT be used in pregnancy
-Drug interactions serious concern
Term
Coagulation cascade: Vit. K inhibitors vs. Heparin
Definition
Vit K.: Factor VII, IX, X, and prothrombin

Heparin: XIa, IXa, Xa, and thrombin
Term
Heparin MOA
Definition
-heparin binds to anithrombin
-this complex binds to and inhibits thrombin
-there no aggregation is possible
Term
low MW heparin vs. heparin
Definition
-Low MW only cuases destruction of Factor Xa

-Heparin will destroy both thrombin and factor Xa
Term
Heparin: Tx
Definition
-pulmonary embolism
-evolving stroke
-massive deep vein thrombosis
-low dose for post-op venous thrombosis and combo with thrombolytic activity with MI
Term
Heparin: AE
Definition
-Hemorrhage
-Heparin-induced thrombocytopenia
-Allergy
Term
Heparin Antidote?

Warfarin Antidote?
Definition
-Protamine inactivates heparin

-Vitamin K reverses effects of coumadin
Term
Warfarin: Tx
Definition
-Acute MI
-Atrial Fib
-Pulmonary embolism
-Heart valve disease and replacement
Term
Direct thrombin inhibitor
Definition
-bind to freely circulating and clot-bound thrombin

-Lipirudin is parenteral DTI for HITs
Term
Thrombolytics
Definition
-dissolve existing blood clots

-plasmin degrades fibrin matrix of clots

-most effective: given within 4-6 hours of onset
Term
TPA
Definition
-Tissue plasminogen activator

-Converts plasminogen to plasmin only at site of clot
Term
Streptokinase
Definition
-derived from bacteria

-forms stable complex with plasminogen

-cheap

-**foreign protein-->can only be used once**
Term
Tissue Plasminogen Activator
Definition
-released from endothelial cells

-binds to fibrin and converts plasminogen to plasmin

-CLOT SPECIFIC: site of action is limited, less likely for hemorrhage

-expensive
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