Clopidogrel Bisulfate (2 brand names, 1 dosage form, 1 route)
Available dosage forms: TABLET.
Routes of administration: ORAL.
Brand Names
- CLOPIDOGREL BISULFATE
- PLAVIX
Boxed Warning
The effectiveness of clopidogrel 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)]. Clopidogrel 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.
Adverse Reactions
The following serious adverse reactions are discussed below and elsewhere in the labeling: Bleeding [see Warnings and Precautions ( 5.2) ] ] Thrombotic thrombocytopenic purpura [see Warnings and Precautions (5.4) ]
Mechanism of Action
Clopidogrel is an inhibitor of platelet activation and aggregation through the irreversible binding of its active metabolite to the P2Y 12class of ADP receptors on platelets.
Overdosage
Platelet inhibition by clopidogrel is irreversible and will last for the life of the platelet. Overdose following clopidogrel administration may result in bleeding complications. A single oral dose of clopidogrel at 1500 or 2000 mg/kg was lethal to mice and to rats and at 3000 mg/kg to baboons. Symptoms of acute toxicity were vomiting, prostration, difficult breathing, and gastrointestinal hemorrhage in animals. Based on biological plausibility, platelet transfusion may restore clotting ability.