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Fibrinolytic drugs.
Fibrinolytic drugs.
Presented by A. Gowtham Sashtha 1st M.pharm
Department of pharmacology
K.M College of pharmacy.
Madurai - 623 501.
Introduction:
> Thrombosis :
> ➜Thrombosis occurs when blood clots block
veins or arteries.
> ➜Complications of thrombosis can producing
such as a stroke or heart attack.
> Symptoms
> ➜Pain and swelling in one leg, chest pain, or
numbness on one side of the body.
Causes of Thrombosis :
→Endothelial injury
→Abnormal blood flow
→Hypercoagulability
Fibrinolytics (Thrombolytics)
Fibrinolytics(or) Thrombolytic is a agent to
treatment fo dissolve dangerous clots in blood
vessels, improve blood flow, and prevent damage to
tissues.
Normal Regulations of platelet aggregation:
Activation of
platelet
aggregation:
Formation of Fibrin :
Natures of Thrombus:
Fibrinolytics Drugs:
Plasminogen Activators:
I) 1st Generation:
→Streptokinase
→Urokinase
II) 2nd Generation:
→Anistreplase
→Alteplase
→Reteplase (analogue of Alteplase)
→Tenecteplas.
Mechanism of action of Fibrinolytics drugs:
Plasminogen Activators:
I) 1st Generation:
➜ Streptokinase:
Source:
→Streptokinase is a protein extracted from
cultures of beta hemolytic streptococci.
→It activates plasminogen
→No intrinsic enzymatic activity.
Mechanism of action:
➜ It combines with pro activators Plasminogen to
form a complex.
➜ This complex catalyst the conversation of
plasminogen to active plasmin.
➜So rapid lysis of the clot by plasmin.
➜ This streptokinase plasminogen complex in not
inhibited by natural a2-antiplastin.
➜ t1/2 - less than 20 mins
Adverse e ect:
➜ Hemorrhage
➜ Not used to steptococcal infections (Have anti
steptococcal antibodies may develop Hypersensitivity
reactions).
➜ Hypersensitivity due to antigenicity (rash, fever,
allergic reaction).
➜ Hypotension.
➜ Urokinase:
Source:
➜It is an enzyme isolated from human urine but
commercially prepared from cultured human kidney
cells.
MAO:
➜It is not clot specific:
➜so can create a generalized lytic state when
administered I.V
ADR:
➜ Bleeding,
➜ Decreased hematocrit
➜ Chest pain,
➜ Increased heart rate,
➜ Fever,
➜ Chills,
➜ Nausea, vomiting,
➜ Anaphylaxis reactions.
II) 2nd Generation:
Anistreplase:
➜ It is a prodrug.
➜Anisolyated plasminogen Streptokinase
Activators Complex (APSAC).
MOA:
➜ In de-acylated in circulation into the
plasminogen-Steptokinase complex.
➜ t1/3 - 70-120 mins.
Advantages of Anistreplase:
➜ Longer duration of action than streptokinase
➜ More Thrombolytics activities than streptokinase.
➜ Greater clot selectively than Streptokinase.
Alteplase: (Recombinant tissue plasminogen activators
-(rt-PA) ).
Source:
➜It is isolated from recombinant DNA technology
from human tissue culture.
MAO:
➜ It is moderately specific for fibrin bound
Plasminogen.
➜ It is directly inactivated by Plasminogen activator
inhibitors - 1 (PAI-1).
ADR:
➜ Nausea,
➜ Mild hypotension,
➜ Fever may occur,
Reteplase:
➜ It is a modified from of rt-PA that is longer
duration of action.
➜ Same mechanism of Alteplase
Tenecteplase:
➜ It is another genetically modified human t-PA.
➜ And also prepared from recombinant DNA
technology.
➜ It is more fibrin specific & long duration than
alteplase.
➜ It has half life of more than 30 mins.
➜ It only approved for use in acute myocardial
Infarction.
Therapeutic uses of Fibrinolytics drugs:
1)Acute myocardial Infarction:
➜ Fibrinolytics are an alternative first line approach to
emergency percutaneous coronary intervention (PCI) with
stent placement.
➜ Both 1st and 2nd generation drugs are used.
2)Deep vein thrombosis:
➜In leg, pelvis, shoulder.
➜Up to 60% patients can be successfully treated.
➜The Fibrinolytics drugs are decrease the pain and
swelling. Streptokinase,urokinase, alteplase.
3) Pulmonary embolism:
➜ Fibrinolytics therapy is indicated in life saving
drugs of Pulmonary Embolism.
➜ The Fibrinolytics drugs lung function is better
preserved.
➜ The Fibrinolytics recanalise 40% of lumb artery
occlusion, especially those treated within 72 hr.
5) Stroke:
➜ Thrombolytics therapy of ischaemic stroke
contraversial.
➜ Possibility of improved neurological outcome is
to be balanced with risk of intra cranial haemorrhage.
➜ Now alteplase is approved for use in ischaemic
strock
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Fibrinolytics drugs.

  • 1. Fibrinolytic drugs. Fibrinolytic drugs. Presented by A. Gowtham Sashtha 1st M.pharm Department of pharmacology K.M College of pharmacy. Madurai - 623 501.
  • 2. Introduction: > Thrombosis : > ➜Thrombosis occurs when blood clots block veins or arteries. > ➜Complications of thrombosis can producing such as a stroke or heart attack. > Symptoms > ➜Pain and swelling in one leg, chest pain, or numbness on one side of the body.
  • 3. Causes of Thrombosis : →Endothelial injury →Abnormal blood flow →Hypercoagulability Fibrinolytics (Thrombolytics) Fibrinolytics(or) Thrombolytic is a agent to treatment fo dissolve dangerous clots in blood vessels, improve blood flow, and prevent damage to tissues.
  • 4. Normal Regulations of platelet aggregation:
  • 8. Fibrinolytics Drugs: Plasminogen Activators: I) 1st Generation: →Streptokinase →Urokinase II) 2nd Generation: →Anistreplase →Alteplase →Reteplase (analogue of Alteplase) →Tenecteplas.
  • 9. Mechanism of action of Fibrinolytics drugs:
  • 10. Plasminogen Activators: I) 1st Generation: ➜ Streptokinase: Source: →Streptokinase is a protein extracted from cultures of beta hemolytic streptococci. →It activates plasminogen →No intrinsic enzymatic activity.
  • 11. Mechanism of action: ➜ It combines with pro activators Plasminogen to form a complex. ➜ This complex catalyst the conversation of plasminogen to active plasmin. ➜So rapid lysis of the clot by plasmin. ➜ This streptokinase plasminogen complex in not inhibited by natural a2-antiplastin. ➜ t1/2 - less than 20 mins
  • 12. Adverse e ect: ➜ Hemorrhage ➜ Not used to steptococcal infections (Have anti steptococcal antibodies may develop Hypersensitivity reactions). ➜ Hypersensitivity due to antigenicity (rash, fever, allergic reaction). ➜ Hypotension.
  • 13. ➜ Urokinase: Source: ➜It is an enzyme isolated from human urine but commercially prepared from cultured human kidney cells. MAO: ➜It is not clot specific: ➜so can create a generalized lytic state when administered I.V
  • 14. ADR: ➜ Bleeding, ➜ Decreased hematocrit ➜ Chest pain, ➜ Increased heart rate, ➜ Fever, ➜ Chills, ➜ Nausea, vomiting, ➜ Anaphylaxis reactions.
  • 15. II) 2nd Generation: Anistreplase: ➜ It is a prodrug. ➜Anisolyated plasminogen Streptokinase Activators Complex (APSAC). MOA: ➜ In de-acylated in circulation into the plasminogen-Steptokinase complex. ➜ t1/3 - 70-120 mins.
  • 16. Advantages of Anistreplase: ➜ Longer duration of action than streptokinase ➜ More Thrombolytics activities than streptokinase. ➜ Greater clot selectively than Streptokinase.
  • 17. Alteplase: (Recombinant tissue plasminogen activators -(rt-PA) ). Source: ➜It is isolated from recombinant DNA technology from human tissue culture. MAO: ➜ It is moderately specific for fibrin bound Plasminogen. ➜ It is directly inactivated by Plasminogen activator inhibitors - 1 (PAI-1).
  • 18. ADR: ➜ Nausea, ➜ Mild hypotension, ➜ Fever may occur, Reteplase: ➜ It is a modified from of rt-PA that is longer duration of action. ➜ Same mechanism of Alteplase
  • 19. Tenecteplase: ➜ It is another genetically modified human t-PA. ➜ And also prepared from recombinant DNA technology. ➜ It is more fibrin specific & long duration than alteplase. ➜ It has half life of more than 30 mins. ➜ It only approved for use in acute myocardial Infarction.
  • 20. Therapeutic uses of Fibrinolytics drugs: 1)Acute myocardial Infarction: ➜ Fibrinolytics are an alternative first line approach to emergency percutaneous coronary intervention (PCI) with stent placement. ➜ Both 1st and 2nd generation drugs are used. 2)Deep vein thrombosis: ➜In leg, pelvis, shoulder. ➜Up to 60% patients can be successfully treated. ➜The Fibrinolytics drugs are decrease the pain and swelling. Streptokinase,urokinase, alteplase.
  • 21. 3) Pulmonary embolism: ➜ Fibrinolytics therapy is indicated in life saving drugs of Pulmonary Embolism. ➜ The Fibrinolytics drugs lung function is better preserved. ➜ The Fibrinolytics recanalise 40% of lumb artery occlusion, especially those treated within 72 hr.
  • 22. 5) Stroke: ➜ Thrombolytics therapy of ischaemic stroke contraversial. ➜ Possibility of improved neurological outcome is to be balanced with risk of intra cranial haemorrhage. ➜ Now alteplase is approved for use in ischaemic strock
  • 23.
  • 25. Zoho Show To create beautiful presentations, download Zoho Show from Play Store https://zoho.to/cy7 Fibrinolytics drugs.pdf (This PDF has been generated using Zoho Show)