PLAVIX- clopidogrel bisulfate tablet, film coated
Bristol-Myers Squibb/Sanofi Pharmaceuticals Partnership
WARNING: DIMINISHED ANTIPLATELET EFFECT IN PATIENTS WITH TWO LOSS-OF-FUNCTION ALLELES OF THE CYP2C19 GENE
The effectiveness of Plavix results from its antiplatelet activity, which is dependent on its conversion to an active metabolite by the cytochrome P450 (CYP) system, principally CYP2C19 [see Warnings and Precautions (5.1), Clinical Pharmacology (12.3)]. Plavix at recommended doses forms less of the active metabolite and so has a reduced effect on platelet activity in patients who are homozygous for nonfunctional alleles of the CYP2C19 gene, (termed "CYP2C19 poor metabolizers"). Tests are available to identify patients who are CYP2C19 poor metabolizers [see Clinical Pharmacology (12.5)]. Consider use of another platelet P2Y12 inhibitor in patients identified as CYP2C19 poor metabolizers.
1 INDICATIONS AND USAGE
1.1 Acute Coronary Syndrome (ACS)
Plavix is indicated to reduce the rate of myocardial infarction and stroke (MI) in patients with non-ST-segment elevation ACS [unstable angina (UA)/non-ST-elevation myocardial infarction (NSTEMI)], including patients who are to be managed medically and those who are to be managed with coronary revascularization. Plavix should be administered in conjunction with aspirin.
Plavix is indicated to reduce the rate of myocardial infarction and stroke in patients with acute ST-elevation myocardial infarction (STEMI) who are to be managed medically. Plavix should be administered in conjunction with aspirin.
1.2 Recent MI, Recent Stroke, or Established Peripheral Arterial Disease
In patients with established peripheral arterial disease or with a history of recent myocardial infarction (MI) or recent stroke Plavix is indicated to reduce the rate of MI and stroke.
2 DOSAGE AND ADMINISTRATION
2.1 Acute Coronary Syndrome
In patients who need an antiplatelet effect within hours, initiate Plavix with a single 300-mg oral loading dose and then continue at 75 mg once daily. Initiating Plavix without a loading dose will delay establishment of an antiplatelet effect by several days [see Clinical Pharmacology (12.3) and Clinical Studies (14.1)].
2.2 Recent MI, Recent Stroke, or Established Peripheral Arterial Disease
75 mg once daily orally without a loading dose [see Clinical Pharmacology (12.3) and Clinical Studies (14.2)].
3 DOSAGE FORMS AND STRENGTHS
75 mg tablets: Pink, round, biconvex, film-coated tablets debossed with "75″ on one side and "1171″ on the other
300 mg tablets: Pink, oblong, film-coated tablets debossed with "300″ on one side and "1332″ on the other.
11 DESCRIPTION
Plavix (clopidogrel bisulfate) is a thienopyridine class inhibitor of P2Y12 ADP platelet receptors. Chemically it is methyl (+)-(S)-α-(2-chlorophenyl)-6,7-dihydrothieno[3,2-c]pyridine-5(4H)-acetate sulfate (1:1). The empirical formula of clopidogrel bisulfate is C16 H16 ClNO2 S�H2 SO4 and its molecular weight is 419.9.
12 CLINICAL PHARMACOLOGY
12.1 Mechanism of Action
Clopidogrel is an inhibitor of platelet activation and aggregation through the irreversible binding of its active metabolite to the P2Y12 class of ADP receptors on platelets.
