Clopidogrel
(Anti platelet)
Introduction:
Clopidogrel is a potent oral antiplatelet agent often used in
the treatment of coronary artery disease, peripheral vascular
disease, and cerebrovascular disease.
 Clopidogrel is used for: Reducing the risk of stroke or heart
attack in patients who have already had a heart attack or
stroke, or have other circulatory problems due to narrowing
and hardening of the arteries
Systematic (IUPAC) name:
Methyl 2-(2-chlorophenyl)-2-(6,7-
dihydrothieno[3,2-c]pyridin-5(4H)-
yl)acetate
 Formula C16H16ClNO2S
 Mol. Mass 321.82 g/mol
Brand name:
Brands available in Pakistan
• Lowplat 75 mg Pharmevo -(PVT)
• Clopid 75 mg Ferozsons (LAB LTD)
• Noclot 75 mg CCL Pharmaceutical
• Ogrel Plus-81 75mg Bosch Pharmaceutical
LTD
Dosage forms and administration:
Clopidogrel bisulfate (clopidogrel hydrogen
sulfate), most commonly under the trade names
Plavix, as 75 mg oral tablets.
History:
is marketed by Bristol-Myers Squibb and Sanofi-
Aventis under the trade names Iscover and Plavix
respectively, by Sun Pharmaceuticals under the
trade name Clopilet and by Ranbaxy Laboratories
under the trade name Ceruvin. It works by
blocking a receptor called P2Y12.
Clinical trials:
 Recent Myocardial Infarction (MI), Recent Stroke or
Established Peripheral Arterial Disease
Plavix Aspirin
• Patients 9599 9586
• IS (fatal or not) 438 (4.6%) 461 (4.8%)
• MI (fatal or not) 275 (2.9%) 333 (3.5%)
• Other vascular death 226 (2.4%) 226 (2.4%)
• Total 939 (9.8%) 1020 (10.6%)
Clinical pharmacology:
Mechanism of Action
 Clopidogrel is an inhibitor of platelet aggregation.
Clopidogrel selectively inhibits the binding of adenosine
diphosphate (ADP) to its platelet receptor and the
subsequent ADP-mediated activation of the glycoprotein
GPIIb/IIIa complex, thereby inhibiting platelet
aggregation.
Pharmacokinetics and Metabolism:
Absorption
Metabolism
Distribution
elimination
Rapidly absorb after oral administration
Highly metabolized in liver & Rapidly
hydrolyzed into its carboxylic acid
derivatives.
Distribute through out the body with peak
plasma level 3 mg/l
Through urine
Adverse reaction:
Chest Pain
Fatigue
Edema
Hypertension
Dyspepsia
Neutropenia
Epistaxis
Bronchitis
Drug interaction:
 Aspirin
Plavix potentiated the effect of aspirin on collagen
induced platelet aggregation.
 Heparin
Coadministration of heparin had no effect on inhibition of
platelet aggregation
 Warfarin
Because of the increased risk of bleeding, its
administration should be undertaken with caution

Clopidogrel

  • 1.
  • 2.
    Introduction: Clopidogrel is apotent oral antiplatelet agent often used in the treatment of coronary artery disease, peripheral vascular disease, and cerebrovascular disease.  Clopidogrel is used for: Reducing the risk of stroke or heart attack in patients who have already had a heart attack or stroke, or have other circulatory problems due to narrowing and hardening of the arteries
  • 3.
    Systematic (IUPAC) name: Methyl2-(2-chlorophenyl)-2-(6,7- dihydrothieno[3,2-c]pyridin-5(4H)- yl)acetate  Formula C16H16ClNO2S  Mol. Mass 321.82 g/mol
  • 4.
    Brand name: Brands availablein Pakistan • Lowplat 75 mg Pharmevo -(PVT) • Clopid 75 mg Ferozsons (LAB LTD) • Noclot 75 mg CCL Pharmaceutical • Ogrel Plus-81 75mg Bosch Pharmaceutical LTD
  • 5.
    Dosage forms andadministration: Clopidogrel bisulfate (clopidogrel hydrogen sulfate), most commonly under the trade names Plavix, as 75 mg oral tablets.
  • 6.
    History: is marketed byBristol-Myers Squibb and Sanofi- Aventis under the trade names Iscover and Plavix respectively, by Sun Pharmaceuticals under the trade name Clopilet and by Ranbaxy Laboratories under the trade name Ceruvin. It works by blocking a receptor called P2Y12.
  • 7.
    Clinical trials:  RecentMyocardial Infarction (MI), Recent Stroke or Established Peripheral Arterial Disease Plavix Aspirin • Patients 9599 9586 • IS (fatal or not) 438 (4.6%) 461 (4.8%) • MI (fatal or not) 275 (2.9%) 333 (3.5%) • Other vascular death 226 (2.4%) 226 (2.4%) • Total 939 (9.8%) 1020 (10.6%)
  • 8.
    Clinical pharmacology: Mechanism ofAction  Clopidogrel is an inhibitor of platelet aggregation. Clopidogrel selectively inhibits the binding of adenosine diphosphate (ADP) to its platelet receptor and the subsequent ADP-mediated activation of the glycoprotein GPIIb/IIIa complex, thereby inhibiting platelet aggregation.
  • 9.
    Pharmacokinetics and Metabolism: Absorption Metabolism Distribution elimination Rapidlyabsorb after oral administration Highly metabolized in liver & Rapidly hydrolyzed into its carboxylic acid derivatives. Distribute through out the body with peak plasma level 3 mg/l Through urine
  • 10.
  • 11.
    Drug interaction:  Aspirin Plavixpotentiated the effect of aspirin on collagen induced platelet aggregation.  Heparin Coadministration of heparin had no effect on inhibition of platelet aggregation  Warfarin Because of the increased risk of bleeding, its administration should be undertaken with caution