Kerns part 2 Fibrinolytic, Coagulants and antiplatelet

Different types of Antithrombotic drugs

• Anticoagulants

• Fibrinolytic agents

• Antiplatelet agents

Anticoagulants MOA

attenuate fibrin clot formation by blocking fibrin crosslinking

Fibrinolytic agents MOA

breakdown fibrin clots

Antiplatelet agents

• Inhibit activation of platelets

• Inhibit aggregation of platelets

What is Fibrinolysis

Bodys natural way to break down a clot

What converts plasminogen to plasmin

t-PA

What breaks down fibrin

Plasmin

What is Fibrin?

Insoluble strands that cross link to from a clot

What converts fibrinogen to fibrin

Thrombin (FIIa) (factor 2 A)

What inactivates t-PA

PAI-1

PAI-2

Thrombolytic drugs MOA

rapidly dissolve blood clots by proteolytic cleavage

Thrombolytic Agent medications

• Urokinase (abbokinase)

• Strptokinase (streptase)

Urokinase (abbokinase) MOA

protease that directly activates plasminogen to plasmin to degrade fibrin (NO t-PA NEEDED)

Streptokinase MOA

thrombolytic enzyme that promotes proteolytic degradation of fibrin by activating plasminogen to plasmin

• can cause hypersensitivity

• Made from bacterial proteins

What are the Tissue Plasminogen Activator medication

• Alteplase

• Tenectaplase

• Reteplase

What can reverse activity of tPA

Coagulants that block lysine binding site of plasmin

How does plasmin bind to fibrin

Lysine binding

• plasmin has 5 binding sites

What class is aminocaproic acid and TXA

Coagulants

What is Emicizumab used for?

treat hemophila (genetic bleeding factor)

• Binds to 9a and xa to activate the natural coagulation cascade and restore the natural coagulation cascade

What are the roles of GPVI and GPIb in platelets

receptors that bind to collagen and allow them to adhere to damaged blood vessels

What type of drug is ASA

antiplatelet drug

Is ASA MOA reversible

Irreversible inhabitation of platelet aggregation through COX-1

What is the turnover of all the platelets in the human body

7-10 days

What COX-1 inhibitor is reversible

Indobufen

Medications that inhibit platelet aggregation

• Dipyridamole (Persantine)

• Cilostazol (Pletal)

Cilostazol and Dipyridamole MOA

Increase cAMP which inhibits platelet aggregation and promotes vasodilation

Medications that Covalent inhibit P2Y12 receptors (thienopyridines)

Clopidogrel, Ticlopidine and Prasugrel

Clopidogrel MOA

Blocks ADP activation of platelets and blocks binding.

What must happen for all medications in the Covalent Inhibitors of P2Y12 receptors

require metabolic conversion to an active metabolite (P450 metabolic activation)

Is Plavix binding to platelets reversible

No (irreversible)

What medication are the reversible inhibitors of P2Y12 receptors

• Brilinta (Ticagrelor)

• Cangrelor (Kengreal)

Why might a provider like Brilinta better than Plavix

• Reversible

• Does not require metabolic activation

• More rapid onset and offset of action

• More predictable