Plavix: Full Drug Profile

Plavix - General Information

Plavix, 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.

Pharmacology of Plavix

Plavix, 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.

Plavix for patients

Patients should be told that they may bleed more easily and it may take them longer than usual to stop bleeding when they take Plavix or Plavix combined with aspirin, and that they should report any unusual bleeding to their physician. Patients should inform physicians and dentists that they are taking Plavix and/or any other product known to affect bleeding before any surgery is scheduled and before any new drug is taken.

Plavix Interactions

Aspirin, warfarin, heparin, NSAIDs

Plavix 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.

Additional information about Plavix

Plavix Indication

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

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.

Food Interactions

Take without regard to meals.

Generic Name

Clopidogrel

Drug Category

Antiplatelet Agents; Platelet Aggregation Inhibitors; Fibrinolytic Agents

Drug Type

Small Molecule; Approved

Other Brand Names containing Clopidogrel

Clopidogrel sulfate; Clopidogrel [Ban:Inn]; Plavix;

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 (Overdose)

Symptoms of acute toxicity include vomiting (in baboons), prostration, difficult breathing, and gastrointestinal hemorrhage.

Protein Binding

98%

Biotransformation

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.

Half Life

Carboxylic acid derivative: 8 hours (after single and multiple doses). Covalent binding to platelets has accounted for 2% of radiolabeled clopidogrel with a half-life of 11 days.

Dosage Forms of Plavix

Tablet Oral

Chemical IUPAC Name

methyl (2S)-2-(2-chlorophenyl)-2-(6,7-dihydro-4H-thieno[3,2-c]pyridin-5-yl)acetate

Chemical Formula

C16H16ClNO2S

Clopidogrel on Wikipedia

https://en.wikipedia.org/wiki/Clopidogrel

Organisms Affected

Humans and other mammals