Clopidogrel

CLOPIDOGREL

( Anti-platelet )

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GROUP MEMBERS

Wajid Hanif Butt dp 305-060

Afzal Ali Shah dp 305-040

Khizar Nabeel Ali dp 305-026


Clopidogrel

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. I


Structure


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


http://en.wikipedia.org/wiki/Carbon

http://en.wikipedia.org/wiki/Hydrogen

http://en.wikipedia.org/wiki/Chlorine

http://en.wikipedia.org/wiki/Nitrogen

http://en.wikipedia.org/wiki/Oxygen

http://en.wikipedia.org/wiki/Sulfur

Brand name

Brands available in Pakistan

Lowplat 75 mg Pharmevo -(PVT) Clopid 75 mg Ferozsons (LAB LTD) Noclot 75 mg CCL Pharmaceutical

(PVT) Ogrel Plus-81

75 mg Bosch Pharmaceutical LTD


Dosage forms and administration

Clopidogrel bisulfate (clopidogrel hydrogen sulfate), most commonly under the trade names Plavix, as 75 mg oral tablets.


http://images.google.com.pk/imgres?imgurl=http://baguiar.com/sa/plavix.jpg&imgrefurl=http://baguiar.com/sa/bmameds.php&usg=__m4BWShAYj1Ra9YmgXEL4GlREQEc=&h=216&w=288&sz=33&hl=en&start=20&tbnid=vrFwINIwvQOgoM:&tbnh=86&tbnw=115&prev=/images%3Fq%3Dclopidogrel%26gbv%3D2%26hl%3Den%26sa%3DG

History

It 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%)


Graph


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 Rapidly absorb after oral administration

MetabolismHighly metabolized in liver & Rapidly

hydrolyzed into its carboxylic acid derivatives

Distribution Distribute through out the body with peak plasma level 3 mg/L

Elimination 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, the

concomitant administration of warfarin with Plavix should be undertaken with caution


Contra indication

Hypersensitivity to the drug substance or any component of the product

Active pathological bleeding such as peptic ulcer or intracranial hemorrhage

Pregnancy


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Healthcare

Clopidogrel