Rx: RM CLOPIDOGREL 75MG TAB

PHARMACODYNAMICS / MECHANISM OF ACTION

Clopidogrel is an irreversible inhibitor of platelet aggregation. It acts by irreversibly modifying the platelet adenosine 5′-diphosphate (ADP) receptor, thus selectively inhibiting the binding of ADP to the platelet receptor and the subsequent activation of the glycoprotein GPIIb/IIIa complex, thereby inhibiting platelet aggregation. Consequently, platelets exposed to clopidogrel are affected for the remainder of their lifespan. Biotransformation of clopidogrel to its active metabolite is necessary to produce inhibition of platelet aggregation.

PHARMACOKINETICS

Clopidogrel is rapidly but incompletely absorbed after oral doses; absorption appears to be at least 50%. It is a prodrug and is extensively metabolized in the liver, mainly to the inactive carboxylic acid derivative; metabolism is mediated by the cytochrome P450 isoenzymes CYP3A4 and CYP2B6, and to a lesser extent by CYP1A2, CYP1A1, and CYP2C19. The active metabolite appears to be a lipid derivative but has not been identified in plasma.

Clopidogrel and the carboxylic acid derivative are highly protein bound. Clopidogrel and its metabolites are excreted in urine and feces; about 50% of an oral dose is recovered from the urine and about 46% from the feces.

INDICATIONS

For prevention of atherosclerotic events in patients with:

History of recent myocardial infarction (within a few days until less than 35 days from occurrence), recent ischemic stroke (from 7 days until less than 6 months) or established peripheral arterial disease.
Non-ST segment elevation acute coronary syndrome (unstable angina/non-Q-wave myocardial infarction) in patients who are managed medically with percutaneous coronary intervention (with or without stent) or coronary artery bypass graft (CABG).

It is given prophylactically as an alternative to aspirin in patients at risk of thromboembolic disorders such as myocardial infarction, peripheral arterial disease and stroke.

DOSAGE AND ADMINISTRATION

Recent MI or stroke, or established peripheral arterial disease
Recommended Dose: Orally, 75 mg once daily with or without food.

Prophylaxis of thromboembolic events.

Usual Dose: Orally, 75 mg once daily.

Unstable angina / Non-Q-wave acute coronary syndrome (unstable angina / non-Q-wave MI)

Initiate a single 300 mg loading dose and then continue at 75 mg once daily in combination with aspirin.
A higher bleeding risk was associated with combined use of clopidogrel and aspirin. It is recommended that physicians monitor their patients through clinical and laboratory evaluation.

Or, as prescribed by a physician.