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Drugs, Supplies and Delivery
Clopidogrel (Plavix)
Clopidogrel, commonly known by its brand name Plavix, is a widely used antiplatelet medication. While it is not primarily an antihypertensive drug, it plays a critical role in the management of cardiovascular diseases, particularly in patients with hypertension who are at risk of thrombotic events. This article synthesizes information from the British National Formulary (BNF), Lippincott Textbook of Pharmacology, and Lange Basic & Clinical Pharmacology to provide a detailed overview of clopidogrel, including its mechanism, uses, dosing, side effects, precautions, and drug interactions.
Clopidogrel is a thienopyridine derivative that irreversibly inhibits the P2Y12 subtype of adenosine diphosphate (ADP) receptors on platelets. By blocking these receptors, clopidogrel prevents ADP-mediated activation of the glycoprotein IIb/IIIa complex, which is essential for platelet aggregation. This inhibition reduces the formation of arterial blood clots, making it effective in preventing thrombotic events (Lippincott, Lange).
Clopidogrel is a prodrug that requires hepatic activation via cytochrome P450 enzymes (primarily CYP2C19). Genetic polymorphisms in CYP2C19 can affect its efficacy, leading to the concept of "clopidogrel resistance" in some patients (BNF).
- Acute Coronary Syndrome (ACS):
- Used in combination with aspirin for the management of unstable angina, non-ST-segment elevation myocardial infarction (NSTEMI), and ST-segment elevation myocardial infarction (STEMI) (BNF).
- Percutaneous Coronary Intervention (PCI):
- Administered to prevent stent thrombosis in patients undergoing PCI with stent placement (Lippincott).
- Secondary Prevention of Cardiovascular Events:
- Reduces the risk of myocardial infarction (MI), stroke, and cardiovascular death in patients with a history of recent MI, stroke, or established peripheral arterial disease (PAD) (Lange).
- Acute Coronary Syndrome (ACS):
- Loading dose: 300–600 mg once (for faster onset of action).
- Maintenance dose: 75 mg once daily (BNF).
- Percutaneous Coronary Intervention (PCI):
- Loading dose: 600 mg once (preferably before the procedure).
- Maintenance dose: 75 mg once daily for up to 12 months (or longer, depending on stent type and clinical judgment) (Lippincott).
- Secondary Prevention:
- Maintenance dose: 75 mg once daily indefinitely or as recommended by guidelines (Lange).
Administration:
- Can be taken with or without food.
- Compliance is critical, as discontinuation increases the risk of thrombotic events (BNF).
- Common: Bleeding (e.g., gastrointestinal, intracranial), bruising, diarrhea, and rash (Lippincott).
- Serious: Severe bleeding (e.g., hemorrhagic stroke, gastrointestinal hemorrhage), thrombotic thrombocytopenic purpura (TTP), and neutropenia (BNF).
- Active Bleeding: Contraindicated in patients with active pathological bleeding (e.g., peptic ulcer, intracranial hemorrhage) (Lange).
- Surgery: Discontinue 5–7 days before elective surgery to reduce bleeding risk (BNF).
- Liver Impairment: Use with caution in patients with severe hepatic impairment (Lippincott).
- Pregnancy and Lactation: Use only if benefits outweigh risks; limited data available (Lange).
- Proton Pump Inhibitors (PPIs): Omeprazole and esomeprazole (CYP2C19 inhibitors) may reduce clopidogrel’s efficacy. Use pantoprazole or H2 blockers if acid suppression is needed (BNF).
- Other Anticoagulants/Antiplatelets: Increased risk of bleeding when combined with aspirin, heparin, or warfarin (Lippincott).
- CYP2C19 Inhibitors: Fluconazole, fluoxetine, and cimetidine may reduce clopidogrel’s activation (Lange).
- Rifampin: May enhance clopidogrel’s antiplatelet effects by inducing CYP2C19 (BNF).
Clopidogrel is the generic name for this medication. It is marketed under the brand name Plavix®, but generic versions are widely available, making it an affordable option for patients.
