fibrinolytic agents

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revision material for fibrinolytics phar2102
jenny schneider
Flashcards by jenny schneider, updated more than 1 year ago
jenny schneider
Created by jenny schneider over 9 years ago
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Question Answer
True or False Fibrinolytic agents are used to lyse blood clots True
which of the following is not a fibrinolytic? enoxaparin streptokinase alteplase reteplase tenecteplase enoxaparin- this is a LMWH anticoagulant
True or False: fibrinolytic agents can be classed as fibrin specific agents and non-fibrin specific agents True
True or False Plasma is produced when plasminogen is activated. Plasmin is a proteolytic enzyme which breaks down fibrin that provides structural support for a clot True
which of the following fibrinolytics is non-fibrin specific? alteplase reteplase tenecteplase streptokinase streptokinase
True or False Fibrin specific agents produce limited plasminogen conversion in absence of fibrin True
True or False non-fibrin specific agents catalyse systemic fibrinolysis and cannot distinguish between fibrin bound palsminogen and circulating plasminogen True
True or False activaiton of circulating plasminogen by non-fibrin specific agents can produce a systemic lytic state TRUE
True or False Fibrin specific agents are based on naturally occurring tissue plasminogen activator (tPA) which acts by binding to surface of clot and activating fibrin bound plasminogen, plasmin is cleaved from the plasminogen associated with the fibrin and the fibrin is broken apart by plasmin to dissolve clot True
True or False streptokinase is not a protease. It works by forming a complex with plasminogen which induces a conformational change in plasminogen that exposes its active site. the complex then serves as an activator of additional plasminogen molecules True
What was the first fibrinolytic agent developed? strepotkinase
Where does streptokinase come from? it is isolated from broth cultures of certain streptococcal bacteria (beta haemolytic streptococci)
what is a disadvantage of streptokinase? patients may develop antibodies to the drug which can lead to allergic reaction if patient needs further doses; also antibodies can neutralise subsequent doses and can persist for at least 4y in up to 50% of patients
what is an example of a second generation fibrinolytic? alteplase
explain what alteplase is and how it is made alteplase is identical to native tPA. It is made by recombinant technology.
what are two examples of third generation fibrinolytics? reteplase and tenecteplase
How does reteplase differ in chemical structure from alteplase? reteplase is a synthetic tPA which contains 355 of the 527 amino acids in tPA (while alteplase is recombinant technology produced tPA)
How does the third generation fibrinolytic reteplase differ from alteplase in terms of half-life? reteplase has a longer half-life than alteplase (13-16min compared to 4-6min). This allows for bolus administration as opposed to alteplase which is administered as a bolus followed by IV infusion
Do alteplase and reteplase have the antibody problem seen with streptokinase? No
How does tenecteplase differ in chemical structure from alteplase and how is it made? tenecteplase is made using recombinant DNA technology. it is a 527 amino acid glycoprotein like tPA but there are structural modifications which make it different from tPA- substitution of asparagine for threonine 103 and glutamine for asparagine 117 and other changes at amino acids 296-299
How does half-life of tenecteplase differ from alteplase and reteplase? longer half-life (ranging from 20-24min to 130min)
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