Trade Names:Plavix- Tablet 75 mg (as base)
Clopidogrel is a thienopyridine derivative, chemically related to ticlopidine, which inhibits platelet aggregation. It acts by irreversibly modifying the platelet adenosine diphosphate (ADP) receptor. Therefore, platelet aggregation is inhibited for both ADP-mediated and ADP-amplified (by other agonists) platelet activation. Consequently, platelets exposed to clopidogrel are affected for the remainder of their lifespan.
Rapidly absorbed. T max is about 1 h. C max is about 3 mg/L.
98% reversibly bound to plasma proteins; active metabolite is 94% reversibly bound to plasma proteins.
Extensively metabolized in the liver; undergoes rapid hydrolysis to carboxylic acid derivative (active).
50% excreted in urine; 46% excreted in feces. The t ½ of active metabolite is 8 h.
3 to 7 days.
About 5 days.
Reduction of atherosclerotic events (eg, MI, stroke, vascular death) in patients with atherosclerosis documented by recent stroke, recent MI, or established peripheral arterial disease; treatment of acute coronary syndrome (unstable angina/non–Q-wave MI), including patients managed medically and those managed with percutaneous coronary intervention (with or without stent) or coronary artery bypass graft; treatment of acute coronary syndrome in patients with ST-segment elevation acute MI; as a loading dose regimen of clopidogrel with aspirin to prevent cardiac adverse reactions in patients undergoing coronary stent implantation.
Hypersensitivity to any component of the product; active pathological bleeding such as peptic ulcer or intracranial hemorrhage.
PO Start with a 300 mg loading dose, then continue at 75 mg once daily, initiating and continuing aspirin (75 to 325 mg/day) in combination with clopidogrel.Recent MI, Recent Stroke, or Established Peripheral Arterial Disease
PO 75 mg once daily with or without food.Acute Coronary Syndrome (ST-Segment Elevation Acute MI)Adults
PO 75 mg once daily in combination with aspirin, with or without thrombolytic agents. Treatment may be initiated with or without a loading dose.
Administer prescribed dose daily without regard to meals. Administer with food if GI upset occurs.
Store at controlled room temperature (59° to 86°F).
Clopidogrel inhibits CYP-450 2C9. Accordingly, clopidogrel may interfere with the metabolism of phenytoin, tamoxifen, tolbutamide, warfarin (prolongs bleeding time), torsemide, fluvastatin, and many NSAIDs, but there are no data with which to predict the magnitude of these interactions. Use caution when administering clopidogrel with any of these drugs.Bupropion
Plasma levels may be elevated by clopidogrel, increasing the risk of adverse reactions.Macrolide and related antibiotics (eg, erythromycin, telithromycin)
May inhibit the antiplatelet effects of clopidogrel.NSAIDs
Risk of hemorrhage may be increased.Rifamycins (eg, rifampin)
Antiplatelet effect of clopidogrel may be enhanced.
None well documented.
Edema, hypertension (4%); hypotension, vasculitis (postmarketing).
Headache (8%); dizziness (6%); depression (4%); confusion, hallucinations (postmarketing).
Rash (4%); pruritus (3%); angioedema, erythema multiforme, lichen planus, Stevens-Johnson syndrome, toxic epidermal necrolysis (postmarketing).
Conjunctival, ocular, and retinal bleeding (postmarketing).
Abdominal pain (6%); diarrhea, dyspepsia (5%); nausea (3%); colitis (including ulcerative or lymphocytic), pancreatitis, stomatitis, taste disorders (postmarketing).
UTI (3%); glomerulopathy, increased creatinine levels (postmarketing).
Purpura/bruise (5%); epistaxis (3%); agranulocytosis, aplastic anemia/pancytopenia, bleeding (including intracranial, GI, and retroperitoneal hemorrhage), thrombotic thrombocytopenic purpura (postmarketing).
Abnormal LFTs, acute liver failure, hepatitis (postmarketing).
Arthralgia, back pain (6%); myalgia, vasculitis (postmarketing).
Upper respiratory tract infection (9%); dyspnea (5%); bronchitis, rhinitis (4%); coughing (3%); bronchospasm, interstitial pneumonitis (postmarketing).
Accidental injury, chest pain, influenza-like symptoms (8%); pain (6%); fatigue (3%); anaphylactoid reactions, hypersensitivity reactions, serum sickness (postmarketing).
Monitor patient for bleeding or unusual bruising, and report to health care provider if noted.
Category B .
Safety and efficacy not established.
Use with caution.
Use with caution in patients with severe hepatic disease who may have bleeding diathesis.
Use with caution in patients with increased bleeding from trauma, surgery, or other pathological conditions. If undergoing surgery and antiplatelet effect is not desired, discontinue clopidogrel 5 days prior.
Clopidogrel prolongs bleeding time. Use with caution in patients who have lesions with a propensity to bleed (eg, ulcers). Cautiously use drugs that might increase such lesions (eg, aspirin, NSAIDs).
May occur, sometimes after short-term exposure (less than 2 wk).
Prolonged bleeding with subsequent bleeding complications.
Copyright © 2009 Wolters Kluwer Health.