this ppt about the thrombolytic agents and its mechanism of action, uses, adverse effects and contraindications. this will help to the medical students to understand about the fibrinolytic drugs easily
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Fibrinolytics.pptx
1. A 58 year old male came to the emergency
department with complaints of left sided chest pain
radiates to the back and left arm and increased
sweating, difficulty in breathing since 4 a.m today.
He is a known hypertensive and diabetic for past 10
years under regular treatment,
what is your diagnosis ?
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4. By the end of the session will be able to
Understand what is Fibrinolytic system
Describe the fibrinolytic drugs & its mechanism
Enlist its Uses & Adverse effects
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5. Checks and balances the clotting system
Dissolves the clot at the site of damage, once
damage is repaired
Activators : tPA, Factor XIIa & Kallikrein
Inhibitors : α2 anti plasmin, α2 macroglobulin
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6. Plasmin :
○ Enzyme responsible for fibrin degradation
○ Generated from plasminogen by tPA (tissue
plasminogen activator)
Plasminogen :
○ Inactive form of plasmin
○ Present in circulation as well as bound to fibrin
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7. tPA (tissue Plasminogen Activator) :
○ Produced by vascular endothelium
○ Selectively activates fibrin bound plasminogen
into plasmin
Anti plasmin :
○ Present in circulation and inactivates the leaked
plasmin & prevents premature lysis of fibrin
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10. Obtained from β hemolytic streptococci
MOA :
Forms 1:1 complex with plasminogen
Catalyses
1. Plasminogen(Inactive) Plasmin(active) Fibrinolysis
2. Breakdown of fibrinogen
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11. Non fibrin specific
Half life : 60 – 80 mins
Use : Myocardial infarction, Deep vein thrombosis &
Pulmonary embolism
Advantages :
Least expensive ; still used in resource poor areas
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12. Disadvantages :
Antigenic ; can cause hypersensitivity
Anti streptococcal antibodies – reduce its efficacy
Cannot be repeated
Fever, Hypotension, arrhythmia
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13. Cultured from human kidney cells
Direct plasminogen activator
Can degrade both fibrin & fibrinogen
T1/2 : 20 mins
Use :
Patients whom streptokinase cannot be repeated
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14. Advantages :
Mild fibrin specific
Non antigenic ; Non pyrogenic ; does not produce
hypotension
Pro urokinase : recombinant form ; more fibrin
specific
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15. Recombinant tissue plasminogen activator
Produced by recombinant DNA technology from
human tissue culture
More fibrin specific ; hydrolyze fibrin only (not
fibrinogen)
Rapidly activates plasminogen ; t1/2 is 5–10 mins
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16. Advantages :
Non antigenic
Superior in dissolving old clots
Disadvantages :
Higher incidence of reocclusion ; needs I.V heparin
co administration
Fever, Nausea, mild hypotension
Quite expensive
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17. Modified recombinant tissue plasminogen activator
Less specific for fibrin bound plasminogen
Long acting ; t1/2 is 15 – 20 mins
Dose : 10 mg over 10 min repeated after 30 min
A/E : fever, hypotension
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18. Genetically engineered mutant form of native rt-PA
IV single bolus dose 50mg over 10 seconds
Advantages :
High fibrin selectivity
Long acting ; t1/2 is 2hours
Resistance to PAI –1 (plasminogen activator inhibitor 1)
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20. Anisolyated plasminogen streptokinase activator
complex
Consists of purified human plasminogen with
bacterial streptokinase in which the active site of
plasminogen has been protected by anisoylation (a
process of acetylation)
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22. Advantages :
Synthesized to improve the pharmacokinetics of
streptokinase-proactivator complex
More fibrin specificity
Long acting (t1/2 > 90mins)
A/E : Hypersensitivity, Hypotension, Bleeding etc.
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24. Intracranial haemorrhage /
Intracranial tumour
Ischemic stroke / Head injury
in past 3 months
Vascular abnormalities
Bleeding disorders
Peptic ulcer
Esophageal varices
Any wound or recent fracture
Tooth extraction
Major surgery within 3 weeks
Uncontrolled hypertension
Pregnancy
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25. tPA – main activator of fibrinolytic system
Streptokinase – antigenic ; non specific
Urokinase – fibrin specific ; less side effects
Alteplase – very short acting ; risk of reocclusion
Reteplase – less fibrin specific ; long acting
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26. Tenecteplase : High fibrin selectivity ; long acting ;
resistance to PAI 1
Antistreplase : modified anisolyated streptokinase
to improve pharmacokinetics
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