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Myelotoxicity of Thienopyridines
Platelet aggregation <ul><li>Platelets , or  thrombocytes  precursor megakaryocytes </li></ul><ul><li>They circulate in th...
Platelet aggregation mechanism
 
Thienopyridines <ul><li>A class of ADP receptor </li></ul><ul><li>P2Y12 inhibitors  </li></ul><ul><li>Used for anti-platel...
Thienopyridines Ticlopidine (1 st  generation) N F O S O O C H 3 Clopidogrel (2 nd  generation) Prasugrel (CS-747) (LY6403...
Clopidogrel <ul><li>Generic: clopidogrel  </li></ul><ul><li>Class: ADP-receptor antagonist </li></ul>
Mode of Action of Clopidogrel COX (cyclo-oxygenase) ADP (adenosine diphosphate) TXA 2  (thromboxane A 2 ) Jarvis B, Simpso...
Pharmacology of Clopidogrel <ul><li>Absorption (oral): rapid,  </li></ul><ul><li>Metabolism: rapid and extensive hepatic m...
Activation of clopidogrel
Activation of clopidogrel
Side effects <ul><li>Severe neutropenia </li></ul><ul><li>Agranulocytosis </li></ul><ul><li>Toxic effects are seen on Haem...
Question <ul><li>Whether clopidogrel is activated directly in myelon? </li></ul><ul><li>How it activation takes place? </l...
 
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Swarna Maseneni

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platelet mechanism and clopidogrel metabolism

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Swarna Maseneni

  1. 1. Myelotoxicity of Thienopyridines
  2. 2. Platelet aggregation <ul><li>Platelets , or thrombocytes precursor megakaryocytes </li></ul><ul><li>They circulate in the blood of mammals </li></ul><ul><li>Involved in hemostasis, leading to the formation of blood clots . </li></ul>
  3. 3. Platelet aggregation mechanism
  4. 5. Thienopyridines <ul><li>A class of ADP receptor </li></ul><ul><li>P2Y12 inhibitors </li></ul><ul><li>Used for anti-platelet activity </li></ul><ul><li>These drugs include: </li></ul><ul><ul><ul><ul><li>Ticlopidine, </li></ul></ul></ul></ul><ul><ul><ul><ul><li>Clopidogrel </li></ul></ul></ul></ul><ul><ul><ul><ul><li>Prasugrel </li></ul></ul></ul></ul>
  5. 6. Thienopyridines Ticlopidine (1 st generation) N F O S O O C H 3 Clopidogrel (2 nd generation) Prasugrel (CS-747) (LY640315) (3 rd generation) N S Cl N S Cl COOCH 3
  6. 7. Clopidogrel <ul><li>Generic: clopidogrel </li></ul><ul><li>Class: ADP-receptor antagonist </li></ul>
  7. 8. Mode of Action of Clopidogrel COX (cyclo-oxygenase) ADP (adenosine diphosphate) TXA 2 (thromboxane A 2 ) Jarvis B, Simpson K. Drugs 2000; 60: 347–77. CLOPIDOGREL ASA COX ADP ADP C GPllb/llla (Fibrinogen receptor) Collagen thrombin TXA 2 Activation TXA 2
  8. 9. Pharmacology of Clopidogrel <ul><li>Absorption (oral): rapid, </li></ul><ul><li>Metabolism: rapid and extensive hepatic metabolism </li></ul><ul><li>Excretion: 50% in urine and 46% in faeces, after 5 days </li></ul><ul><li>Standard dosing: 75 mg once daily </li></ul>
  9. 10. Activation of clopidogrel
  10. 11. Activation of clopidogrel
  11. 12. Side effects <ul><li>Severe neutropenia </li></ul><ul><li>Agranulocytosis </li></ul><ul><li>Toxic effects are seen on Haematopoietic stem cells in the myelon and not from the peripheral destruction of leukocytes </li></ul>
  12. 13. Question <ul><li>Whether clopidogrel is activated directly in myelon? </li></ul><ul><li>How it activation takes place? </li></ul>

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