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Antiplatelets & Fibrinolytics
HARSHIT SHETH
Thrombosis
• Arterial Thrombosis :
– Adherence of platelets to arterial walls -
White in color - Often associated with MI,
stroke and ischemia
• Venous Thrombosis :
– Develops in areas of stagnated blood flow
(deep vein thrombosis), Red in color-
Associated with Congestive Heart Failure,
Cancer, Surgery.
HOW PLAQUES ARE FORMED?
Antiplatelets, & fibrinolytics
Basic concepts
• PGI2- inhibit platelet aggregation
• TXA2- platelet aggregation
• Elevated c-AMP- inhibit platelet
aggregation & vice versa
• ADP receptors(P2Y1,P2Y2)-changes
shape & platelet aggregation
• GPIIb/IIIa receptors- binds fibrinogen
& platelets
• 5-HT-vasocostriction
• Collagen,Thrombin- platelet
aggregation agonist
Antiplatelets, & fibrinolytics
ANTIPLATELETS:
Classification
• Aspirin
• Phospodiesterase inhibitors-
Dipyridamol, - Cilostazole
• ADP antagonist-
Clopidogrel,Ticlopidine
• GPIIb/IIIa Antagonist-
Abciximab,Eptifibatide,Tirofiban ,
Lamifiban
• Synthetic PGI2- Epoprostenol
Aspirin(ASA):Mechanism
 Vascular endothelial cells can
synthesize new PGI2 but
platelets cannot synthesize
new TXA2.
 Thus action of aspirin on
platelet is permanent lasting for
the lifetime of platelet i.e. 7-10
days.
 Balance between TXA2
(promoter of aggregation) &
PGI2 ( inhibitor of aggregation)
As higher doses of aspirin are
needed to inhibit COX in
vascular endothelium than in
platelets, antiplatelet effect can
be achieved at low doses ( 75-
150 mg per day orally)
 Other NSAIDs are reversible
inhibitors.
Limitations of Aspirin
•Multiple pathways of platelet activation in
vivo
Thrombin, collagen, high shear stress
activate
platelets via non-cyclooxygenase pathways
Catecholamines can overcome antiplatelet
effect
Platelet adhesion and thrombus formation
not
blocked
Prothrombotic effect at higher doses
Inhibition of vascular prostacyclin
generation
Inhibition of tPA (at doses >300 mg)
Antiplatelets, & fibrinolytics
Adverse effects
• At lower dose mainly GIT adv. Effect:
A)GI mucosa damage
B)High risk of bleeding
C)Suppression of GI protective
action of PGs
Phosphodiaster Inhibitors:
• Dipyridamol:
• It inhibits Phosphodiasterase &
blocks uptake of adenosine to
increase cAMP which potentiate PGI2
& interfere with aggregation
• Dipyridamol+Aspirin-used in TIA
ADP antagonist:
Clopidogrel
• Pro Drug
• Slow onset of action
• Fewer side effects than
Ticlodipine
• Dose dependent action –
within 5 hrs of oral loading
dose 80% of platelet activity
inhibited.
• Duration of antiplatelet effect 7-
10 days.
Ticlodipine
• Pro Drug
• 8-11 days to show maximal effect.
• Nausea, vomiting, diarrhoea.
• Thrombocytopenia
• Neutropenia
• Thrombotic Thrombocytopenic
Purpura – rare.
• Due to distinct MOA combo with
aspirin has additive or synergistic
effect.
• Used for sec. prevention of stroke
GPIIb/IIIa Antagonist
Abciximab
• Human murine chimeric
monoclonal antibody Fab
fragment
• Binds with high affinity and
slow dissociation rate.
• Immediate and profound
inhibition of platelet activity
extending for 12-36 hrs after
termination of infusion.
• 0.25mg/kg bolus followed by
0.125μg/kgper min for 12hrs
Eptifibatide/ Tirofiban
• • Prevent binding of fibrinogen to
• the receptor complex
• • Used to treat unstable angina
• • Used for angioplastic coronary
• interventions.
• • ADRs
• - Haemorrage
• - Thrombocytopenia
Antiplatelets, & fibrinolytics
Clinical uses of antiplatelet drugs
 The main drug is aspirin. Other
drugs with distinct actions (e.g.
dipyridamole, clopidogrel) can have
additive effects, or be used in
patients who are intolerant of aspirin.
 Uses of antiplatelet drugs relate
mainly to arterial thrombosis and
include uses in:
 acute myocardial infarction
high risk of myocardial infarction, including
a history of myocardial infarction, angina
– unstable Angina (clopidogrel is added to
aspirin)
following coronary artery bypass
grafting
– following coronary artery angioplasty
(PCI) – abciximab(I.V), are used in some
patients in addition to aspirin)
– transient cerebral ischaemic attack
('ministrokes') or thrombotic stroke, to
prevent recurrence (dipyridamole can be
added to aspirin)
– atrial fibrillation, if oral anticoagulation is
contraindicated.
• epoprostenol [PGI2]; have
specialised clinical applications in
haemodialysis or haemofiltration in
cases in which heparin is
FIBRINOLYTICS
• These drugs dissolve the Thrombi in
blood vessel(mainly coronary artery)
by activating fibrinolytic system
Fibrinolytics Agents
1st
GEN:
• Streptokinase
• Urokinase
2nd
GEN
• Alteplase
3rd
GEN
• Reteplase
• Tenecteplase
Streptokinase :1st
GEN:
• Streptokinase is a protein
• synthesized by streptococci that
• combines with proactivator
• plasminogen. Caution in patients
• with previous history of fibrinolytic
• therapy due to formation of
• antibodies.
• • Streptokinase- loading dose of
• 250,000 units followed by
• 100,000 units/hr for 24-72 hrs.
• • It is antigenic & can cause
hypersensitivity rxn when used
Urokinase
• Urokinase is a human enzyme
synthesized by the kidney that
directly converts plasminogen to
plasmin.
• Plasminogen can be activated
endogenously by t-PA.
Preferentially activate plasminogen
bound to fibrin
 Non-antigenic
Indicated in pts. With sensitivity to
strepokinase
FIBRINOLYTICS
• 2ND
GEN: ALTEPLASE (TPA)
– Cleaves plasminogen plasmin
fibrinolysis
– Specific activity in thrombus, less
systemic fibrinolysis
– Weight-based IV infusion over 60-90min
– Half-life<5 min
– Heparin commonly administered shortly
after
• 2ND
GEN: ALTEPLASE (TPA)
– Cleaves plasminogen plasmin
fibrinolysis
– Specific activity in thrombus, less
systemic fibrinolysis
– Weight-based IV infusion over 60-90min
– Half-life<5 min
– Heparin commonly administered shortly
after
 DOSE- 60 mg i.v.
over the first hour followed by
40 mg at a rate of 20 mg/hr.
Adv.Of alteplase in TIA(mini
stroke)
Comparision
FIBRINOLYTICS
• 3RD
GEN: modifications of TPA
– RETEPLASE
• Half-life= 18 min
• Double bolus regimen
– TENECTEPLASE (TNK)
• Half life= 20 min
• Single-weight tiered bolus dosing over 5-10s
*bolus-doses fewer med errors
* No absol mortality benefit in AMI
FIBRINOLYTICS: Clinical uses
• The main use is in acute myocardial
infarction, with ST segment elevation
on the ECG within 12 hours of onset
(the earlier the better!)
• Other uses include:
– acute thrombotic stroke within 3 hours of
onset (tPA), in selected patients
– clearing thrombosed shunts and
cannulae
– acute arterial thromboembolism
– life-threatening deep vein thrombosis
and pulmonary embolism (streptokinase,
given promptly).
Adv. Effect : These agents do not
distinguish b/w pathological thrombi &
fibrin deposit at site of vascular injury
Books To Be Referred:
• Lippincott
• F.s.k Barar
• Rang & Dale
• Goodman & Gillman
• K D Tripathi
• H L Sharma
• R K Goyal
• Photographs from Medical books
• Internet
Antiplatelets, & fibrinolytics
Good ideas are not adopted automatically.
They must be driven into practice with
courageous patience.
--Hyman Rickover
US Admiral(1900-1986)
37

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Antiplatelets, & fibrinolytics

  • 2. Thrombosis • Arterial Thrombosis : – Adherence of platelets to arterial walls - White in color - Often associated with MI, stroke and ischemia • Venous Thrombosis : – Develops in areas of stagnated blood flow (deep vein thrombosis), Red in color- Associated with Congestive Heart Failure, Cancer, Surgery.
  • 3. HOW PLAQUES ARE FORMED?
  • 5. Basic concepts • PGI2- inhibit platelet aggregation • TXA2- platelet aggregation • Elevated c-AMP- inhibit platelet aggregation & vice versa • ADP receptors(P2Y1,P2Y2)-changes shape & platelet aggregation • GPIIb/IIIa receptors- binds fibrinogen & platelets • 5-HT-vasocostriction • Collagen,Thrombin- platelet aggregation agonist
  • 7. ANTIPLATELETS: Classification • Aspirin • Phospodiesterase inhibitors- Dipyridamol, - Cilostazole • ADP antagonist- Clopidogrel,Ticlopidine • GPIIb/IIIa Antagonist- Abciximab,Eptifibatide,Tirofiban , Lamifiban • Synthetic PGI2- Epoprostenol
  • 9.  Vascular endothelial cells can synthesize new PGI2 but platelets cannot synthesize new TXA2.  Thus action of aspirin on platelet is permanent lasting for the lifetime of platelet i.e. 7-10 days.  Balance between TXA2 (promoter of aggregation) & PGI2 ( inhibitor of aggregation)
  • 10. As higher doses of aspirin are needed to inhibit COX in vascular endothelium than in platelets, antiplatelet effect can be achieved at low doses ( 75- 150 mg per day orally)  Other NSAIDs are reversible inhibitors.
  • 11. Limitations of Aspirin •Multiple pathways of platelet activation in vivo Thrombin, collagen, high shear stress activate platelets via non-cyclooxygenase pathways Catecholamines can overcome antiplatelet effect Platelet adhesion and thrombus formation not blocked Prothrombotic effect at higher doses Inhibition of vascular prostacyclin generation Inhibition of tPA (at doses >300 mg)
  • 13. Adverse effects • At lower dose mainly GIT adv. Effect: A)GI mucosa damage B)High risk of bleeding C)Suppression of GI protective action of PGs
  • 14. Phosphodiaster Inhibitors: • Dipyridamol: • It inhibits Phosphodiasterase & blocks uptake of adenosine to increase cAMP which potentiate PGI2 & interfere with aggregation • Dipyridamol+Aspirin-used in TIA
  • 16. Clopidogrel • Pro Drug • Slow onset of action • Fewer side effects than Ticlodipine • Dose dependent action – within 5 hrs of oral loading dose 80% of platelet activity inhibited. • Duration of antiplatelet effect 7- 10 days.
  • 17. Ticlodipine • Pro Drug • 8-11 days to show maximal effect. • Nausea, vomiting, diarrhoea. • Thrombocytopenia • Neutropenia • Thrombotic Thrombocytopenic Purpura – rare. • Due to distinct MOA combo with aspirin has additive or synergistic effect. • Used for sec. prevention of stroke
  • 19. Abciximab • Human murine chimeric monoclonal antibody Fab fragment • Binds with high affinity and slow dissociation rate. • Immediate and profound inhibition of platelet activity extending for 12-36 hrs after termination of infusion. • 0.25mg/kg bolus followed by 0.125μg/kgper min for 12hrs
  • 20. Eptifibatide/ Tirofiban • • Prevent binding of fibrinogen to • the receptor complex • • Used to treat unstable angina • • Used for angioplastic coronary • interventions. • • ADRs • - Haemorrage • - Thrombocytopenia
  • 22. Clinical uses of antiplatelet drugs  The main drug is aspirin. Other drugs with distinct actions (e.g. dipyridamole, clopidogrel) can have additive effects, or be used in patients who are intolerant of aspirin.  Uses of antiplatelet drugs relate mainly to arterial thrombosis and include uses in:  acute myocardial infarction high risk of myocardial infarction, including a history of myocardial infarction, angina – unstable Angina (clopidogrel is added to aspirin)
  • 23. following coronary artery bypass grafting
  • 24. – following coronary artery angioplasty (PCI) – abciximab(I.V), are used in some patients in addition to aspirin) – transient cerebral ischaemic attack ('ministrokes') or thrombotic stroke, to prevent recurrence (dipyridamole can be added to aspirin) – atrial fibrillation, if oral anticoagulation is contraindicated. • epoprostenol [PGI2]; have specialised clinical applications in haemodialysis or haemofiltration in cases in which heparin is
  • 25. FIBRINOLYTICS • These drugs dissolve the Thrombi in blood vessel(mainly coronary artery) by activating fibrinolytic system
  • 26. Fibrinolytics Agents 1st GEN: • Streptokinase • Urokinase 2nd GEN • Alteplase 3rd GEN • Reteplase • Tenecteplase
  • 27. Streptokinase :1st GEN: • Streptokinase is a protein • synthesized by streptococci that • combines with proactivator • plasminogen. Caution in patients • with previous history of fibrinolytic • therapy due to formation of • antibodies. • • Streptokinase- loading dose of • 250,000 units followed by • 100,000 units/hr for 24-72 hrs. • • It is antigenic & can cause hypersensitivity rxn when used
  • 28. Urokinase • Urokinase is a human enzyme synthesized by the kidney that directly converts plasminogen to plasmin. • Plasminogen can be activated endogenously by t-PA. Preferentially activate plasminogen bound to fibrin  Non-antigenic Indicated in pts. With sensitivity to strepokinase
  • 29. FIBRINOLYTICS • 2ND GEN: ALTEPLASE (TPA) – Cleaves plasminogen plasmin fibrinolysis – Specific activity in thrombus, less systemic fibrinolysis – Weight-based IV infusion over 60-90min – Half-life<5 min – Heparin commonly administered shortly after • 2ND GEN: ALTEPLASE (TPA) – Cleaves plasminogen plasmin fibrinolysis – Specific activity in thrombus, less systemic fibrinolysis – Weight-based IV infusion over 60-90min – Half-life<5 min – Heparin commonly administered shortly after  DOSE- 60 mg i.v. over the first hour followed by 40 mg at a rate of 20 mg/hr.
  • 30. Adv.Of alteplase in TIA(mini stroke)
  • 32. FIBRINOLYTICS • 3RD GEN: modifications of TPA – RETEPLASE • Half-life= 18 min • Double bolus regimen – TENECTEPLASE (TNK) • Half life= 20 min • Single-weight tiered bolus dosing over 5-10s *bolus-doses fewer med errors * No absol mortality benefit in AMI
  • 33. FIBRINOLYTICS: Clinical uses • The main use is in acute myocardial infarction, with ST segment elevation on the ECG within 12 hours of onset (the earlier the better!) • Other uses include: – acute thrombotic stroke within 3 hours of onset (tPA), in selected patients – clearing thrombosed shunts and cannulae – acute arterial thromboembolism – life-threatening deep vein thrombosis and pulmonary embolism (streptokinase, given promptly).
  • 34. Adv. Effect : These agents do not distinguish b/w pathological thrombi & fibrin deposit at site of vascular injury
  • 35. Books To Be Referred: • Lippincott • F.s.k Barar • Rang & Dale • Goodman & Gillman • K D Tripathi • H L Sharma • R K Goyal • Photographs from Medical books • Internet
  • 37. Good ideas are not adopted automatically. They must be driven into practice with courageous patience. --Hyman Rickover US Admiral(1900-1986) 37