Brands, Medical Use, Clinical Data
Drug Category
- Antiplatelet Agents
- Platelet Aggregation Inhibitors
- Fibrinolytic Agents
Dosage Forms
- Tablet (round, biconvex, film-coated)
Brands / Synonyms
Clopidogrel sulfate; Clopidogrel [Ban:Inn]; Plavix; Plavix
Indications
For the reduction of atherosclerotic events (myocardial infarction, stroke, and vascular death) in patients with atherosclerosis documented by recent stroke, recent myocardial infarction, or established peripheral arterial disease
Pharmacology
Clopidogrel, an antiplatelet agent structurally and pharmacologically similar to ticlopidine, is used to reduce atherosclerotic events such as myocardial infarction, stroke, and vascular death in patients who have had a recent stroke, recent MI, or have established peripheral vascular disease.
Mechanism of Action
The active metabolite of clopidogrel prevents binding of adenosine diphosphate (ADP) to its platelet receptor, impairing the ADP-mediated activation of the glycoprotein GPIIb/IIIa complex. It is proposed that the inhibition involves a defect in the mobilization from the storage sites of the platelet granules to the outer membrane. No direct interference occurs with the GPIIb/IIIa receptor. As the glycoprotein GPIIb/IIIa complex is the major receptor for fibrinogen, its impaired activation prevents fibrinogen binding to platelets and inhibits platelet aggregation. By blocking the amplification of platelet activation by released ADP, platelet aggregation induced by agonists other than ADP is also inhibited by the active metabolite of clopidogrel.
Absorption
Absorption is at least 50% based on urinary excretion of clopidogrel-related metabolites. Bioavailability has not been found to be affected by food.
Toxicity
Symptoms of acute toxicity include vomiting (in baboons), prostration, difficult breathing, and gastrointestinal hemorrhage.
Biotrnasformation / Drug Metabolism
Hepatic, extensive and rapid, by hydrolysis to the main circulating metabolite, a carboxylic acid derivative, which accounts for approximately 85% of the circulating drug-related compounds. A glucuronic acid derivative of the carboxylic acid derivative has also been found in plasma and urine. Neither the parent compound nor the carboxylic acid derivative has a platelet inhibiting effect.
Contraindications
The use of Plavix is contraindicated in the following conditions:
· Hypersensitivity to the drug substance or any component of the product.
· Active pathological bleeding such as peptic ulcer or intracranial hemorrhage.
Drug Interactions
Aspirin, warfarin, heparin, NSAIDs
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