explanation of fibrinolytics or thrombolytics also explanation of antifibrinolytics......

1. Fibrinolytic or Thrombolytic
NOIDA INSTITUTION ENGINEERING AND TECHNOLOGY
(PHARMACY INSTITUTION )
GREATER NOIDA
Presented by:
Sanskriti
M.Pharm (Pharmacology)
Advance Pharmacology
Under Guidance:
Mrs.Bhawani Pentela
Assistant Professor
NIET (Pharmacy
Institute)
Greater Noida

2. Fibrinolytic or Thrombolytic
 Definition
 Thrombolytics are the drugs used to lyse clot to recanalize occluded blood vessels(
mainly coronary artery).
 They act by activating natural fibrinolytic system.
• Fibrin : - Clot in the blood.
 Lysis :- Breakdown.
 Fibrinolysis :- Breakdown of fibrin clot.
 Fibrinolytic drug, also called thrombolytic drug, any agent that is capable of
stimulating the dissolution of a blood clot (thrombus) . Fibrinolytic drugs work by
work by activating the so-called fibrinolytic pathway. they occur in coronary,
cerebral or pulmonary vessels, they can be immediately life-threatening coronary
coronary thrombi are the cause of myocardial infarctions, cerebrovascular thrombi
thrombi ,produce strokes, and pulmonary thrombus emboli can lead to respiratory
respiratory and cardiac failure. Therefore, it is important to rapidly diagnose and
and treat blood clots

4. Mechanism of fibrinolytic
 Plasminogen is the inactive precursor present in plasma.
 It is converted to Plasmin by an Activator Substance present in blood and tissues.
 Plasmin can break down clots.
Plasminogen Plasmin Clot Dissolution.
 All fibrinolytic agents currently in use act directly or indirectly as plasminogen activators.
 They produce lyses of an already formed clot.
 So they are curative rather than prophylactic.
They can be injected ->
1)Intraarterially close to thrombus for a localized effect.
2)Intravenously for a generalized effect in multiple
Thrombi.

5. Fibrinolytic Drugs
 First Generation
Streptokinase and Urokinase
 Second Generation
Prourokinase
Atlepase
Reteplase
Tenecteplase
Anistreplase

6. Streptokinase
• It is a fibrinolytic agent obtained from beta haemolytic Streptococci.
• It acts as a plasminogen activator leading to fibrinolysis.
• It binds with circulating plasminogen to form complex that activates
plasminogen to Plasmin.
 Plasma half life: t1/2 40-80 min.
• Anistreplase (Eminase®) is a complex of SK and plasminogen. It has more
fibrin specificity and has a longer activity than natural SK; however, it causes
considerable fibrinogenolysis.

7. Streptokinase
 Therapeutic uses:
Acute myocardial infarction
Acute pulmonary embolism
Deep-vein thrombosis
Arterial thrombosis [PVD]
 Adverse effects
Bleeding, hypotension, allergic reactions, fever, arrhythmias
 Contraindications
Recent trauma, surgery, abortion, stroke, severe hypertension, peptic ulcer, bleeding disorders

8. Urokinase
• It is an Enzyme prepared from human urine.
• It is now prepared from cultured human kidney cells.
• Unlike Streptokinase It is :-
1. Non – Antigenic
2. Non- Pyrogenic
3. Does not produce Allergic reactions.
4. It is Expensive.
• Directly acts on plasminogen
• Adverse action profile same as Streptokinase

9. Alteplase
• Alteplase (tPA)originally derived from cultured human melanoma cells-now
recombinant DNA technology.
• Mechanism of action : It has low affinity for free plasminogen in the
plasma-rapidly activates plasminogen that is bound to fibrin in a thrombus
or a hemostatic plug.
• Fibrin selective: At low doses, it has the advantage of lysing only fibrin,
without unwanted degradation of other proteins- fibrinogen

10. Reteplase & Tenectaplase
• It is fibrin-specific human t-PA prepared by recombinant mutation
technology.
• It has longer duration than alteplase.
Tenecteplase: –
 Genetically engineered mutant form of alteplase .
 Higher fibrin selectivity and longer half life – 2 hrs
 Single bolus dose 0.5 mg/kg sufficient
 Very expensive

11. Anistreplase
• Anisoylated plasminogen activator complex.
• Anistreplase is a preformed complex of streptokinase and plasminogen
and it is considered to be a prodrug.
Advantages: Rapid IV injection may be given Greater clot selectivity. More
thrombolytic activity.

12. Mechanism of activators and inhibitors of fibrinolytic

13. USES of fibrinolytics
 Acute Myocardial infraction
 Deep vein thrombosis
 Pulmonary embolism
 Ischemic stroke
 Peripheral atrial occlusion

14. Contraindicated to thrombolytic
therapy
 Intracranial haemorrhage.
 Head injury/major surgery in past 3 months
 Intracranial tumours/vascular abnormality/aneurysms
 Active bleeding/bleeding disorders
 Peptic ulcer
 Any wound or recent fracture or tooth extraction
 Severe Hypertension

15. Antifibrinolytics
 Antifibrinolytics are a class of medication that are inhibitors of fibrinolysis.
 Aminocaproic acid and Tranexamic acid
 These lysine-like drugs interfere with the formation of the fibrinolytic enzyme plasmin from
its precursor plasminogen by plasminogen activators (primarily t-PA and u-PA) which takes
place mainly in lysine rich areas on the surface of fibrin .
 These drugs block the binding sites of the enzymes or plasminogen respectively and thus
stop plasmin formation.
 They are used in menorrhagia and bleeding tendency due to various causes

16. References
 Rathnaj Sreya”slide share of Fibrinolytic”2020 march 12.
 Sharma Dr.Lokendra “slide share of Thrombolytic and Fibrinolytic”2007 may
16.