Fibrinolytics Flashcards
what is the role of plasminogen/plasmin in the process of blood clotting?
to digest fibrinogen to fibrin
what is the mechanism for the conversion of plasminogen to active plasmin?
tPA (tissue plasminogen activator)
- t-PA is inhibited by PAI-2 and PAI-1
what drugs are used to dissolve clots?
alteplase, tenecteplase, reteplase
what is alteplase?
- recomb human tPA-527 aa residue
- bind fibrin
what is reteplase?
- recomb human tPA with deletion of aa (355/527)
- more potent, faster onset
- lack fibrin binding domain, less fibrin specific
what is tenecteplase?
- recomb mutant form of tPA
- longer t1/2 by IV bolus
- more fibrin specific than tPA
what are the indications for thrombolytic therapy?
- acute MI
- acute ischemic thrombotic stroke
- PE
what are the different mechanisms for these tPA factors?
- alteplase & tenecteplase - have plasminogen goes into clots by tPA and binds to clot, activating plasmin which then chews up the clot
- Reteplase
- Plasminogen quickly uses tPA to activate plasmin that then dec. fibrinogen and fibrin clots very rapidly
what are the three anti- fibrinolytic agents
Aminocaproic acid, Tranexamic acid, lysine
what are the anti-fibrinolytic agents used for?
used to stop bleeding cause by thrombolytic drugs
what anti-fibrinolytic is more potent than others?
tranexamic acid is 10x more potent than aminocaproic acid
what are some clinical uses with anti-fibrinolytic?
- treat bleeding from thrombolytic therapy
- adj. therapy in hemophilia
- re-bleeding from intracranial aneurms
what are some major risks with anti-fibrinolytic?
- intravascular thrombosis as result of fibrinolysis inhibition
- thrombi formed during therapy arent equally lysed.
what does structure is this?
aminocaproic acid
what structure is this?
lysine
what structure is this?
tranexamic acid
