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Pharm BMED 575
Thrombolytics
Question | Answer |
---|---|
Plasmin is the activated form of? | plasminogen |
Plasmin acts on what and produces what? | Acts on fibrin to degrade it |
What is the action of thrombolytic agents? | Converts plasminogen to plasmin |
Fibrinolytics can be used to treat severe pulmonary embolism | TRUE |
DVT cannot be treated with fibrinolytics | FALSE |
Arterial thrombosis are resistant to treatment by fibrinolystics | FALSE |
There are no cautions when treated strokes with fibrinolytics | FALSE |
Fibrinolytics can be used for AMI | TRUE |
Historically, what was used to treat coronary occlusion? | Thrombolytics |
What is PCI | percutneous coronary intervention (the placement of drug eluting stents) |
If thrombolytic agents are used, percent reduction in mortality is seen? | 20% |
What time frame must thrombolytics be administered? | within 6 hours |
What ECG waveforms are not as treated with thrombolytics? | non-Q wave |
What ECG patterns are most benefited by thrombolytic therapy? | ST-segment elevation or bundle branch block |
What adjunct treatments are used to treat MI with thrombolytics? | aspirin, beta blockers and ACE inhibitors |
Does heparin improve or make worse the response to t-PA? | improve |
Name four thrombolytic agents | tissue plasminogen activator, streptokinase, urokinase, and anistreplase |
What is the MOA of thrombolytics? | They all work to activate the fibrinolytic enzyme plasminogen |
Where is endogenous t-PA produced? | The endothelial cells |
What are rt-PA, Alteplase, Activase? | commercially produced recombinant t-PA |
How are the artificial t-PAs given? | As an IV infusion or bolus |
Which of the thrombolytics is able to activate "clot-bound" plasminogen? ie, get to plasminogen that is hidden by existing fibrin | rt-PA, Alteplase, Activase |
rt-PA, Alteplase, Activase have a higher risk of stroke, but what action are they most effective at? | establishing coronary re-perfusion |
Which thrombolytic is thousands of dollars per treatment? | rt-PA, Alteplase, Activase |
What are some of the side effects of Streptokinase? | Allergic response, anaphylaxis, and pyrexia |
Where does Streptkinase work? | complexes with proactivator and activates plasminogen |
Which thrombolytic is more systematic, rt-PA or streptokinase | Streptokinase. It is not as fibrin specific as rt-PA but acts more systematically |
If used with aspirin, which thrombolytic is as effective as other fibrinolytics? | Streptokinase |
What thrombolytic loses efficacy after the first treatment due to antibody formation? | streptokinase |
Where is endogenous urokinase produced? | the kidney |
What is the MOA of urokinase? | Urokinase directly activates plasminogen to plasmin |
How is urokinase dosed? | IV loading dose followed by 12 hour infusion |
What is APSAC? | anisoylated plasminogen streptokinase activator complex |
What are the constituents of anistreplase (Eminase) | an inert mixture of plasminogen and streptokinase |
What does anistreplase (Eminase) do once injected? | The acly group hydrolyzed once in the blood and it becomes fibrinolytic |
Which of the thrombolytics has a long duration of action? | anistreplase (Eminase) |
Which now discontinued thrombolytic is more clot selective than streptokinase but not as expensive as rt-PA? | anistreplase (Eminase) |
What was some of the reasons anistreplase was pulled from the market? | caused considerable fibrinogenolysis and is antigenic |
What is the MOA of aminocaproic acid (Amicar)? | it inhibits fibrinolysis and reversed the action of other fibrinolytic drugs |
What fibronlytic compound does aminocaproic acid (Amicar) act on? | it completely inhibits the formation of plasminogen |
What two patients groups would Amicar be used on? | hemophiliacs and those suffering from fibrinolytic therapy overdose |
How is Amicar used as a prophylactic? | To prevent re-bleeding in intracranial aneurysms. |
What chemical is aminocaproic acid (Amicar) similar to? | Lysine |
What is the MOA of transexamic acid (Cyklokapron)? | it inhibits the activation of plasminogen |
What inhibitor of fibrinolysis is useful is upper GI bleeds? | transexamic acid (Cyklokapron) |
What two inhibitors of fibrinolysis can cause intravascular thrombosis? | aminocaproic acid and transexamic acid |
Hypotension and myopathy are two adverse side effects of the inhibitors of fibrinolysis. | TRUE |
GI discomfort and nasal stuffiness are not an issue with aminocaproic acid and transexamic acid because they don't effect the parasympathetic nervous system | FALSE |
What is the MOA of aprotinin (Trasylol) | it is serine protease inhibitor |
While aminocaproic acid inhibits the formation of plasminogen and transexamic acid inhibits the activation of plasminogen, how does aprotinin (Trayslol) work? | It inhibits fibronolysis by free plasmin |
What is a side effect of aprotinin (Trasylol)? | may cause anaphylaxis |