Clopidogrel
Mechanism :
The active metabolite of clopidogrel prevents binding of adenosine diphosphate (ADP) to its platelet receptor, impairing the ADP-mediated activation of the glycoprotein GPIIb/IIIa complex. It is proposed that the inhibition involves a defect in the mobilization from the storage sites of the platelet granules to the outer membrane. he drugs specifically and irreversibly inhibits the P2Y12 subtype of ADP receptor, which is important in aggregation of platelets and cross-linking by the protein fibrin. No direct interference occurs with the GPIIb/IIIa receptor. As the glycoprotein GPIIb/IIIa complex is the major receptor for fibrinogen, its impaired activation prevents fibrinogen binding to platelets and inhibits platelet aggregation. By blocking the amplification of platelet activation by released ADP, platelet aggregation induced by agonists other than ADP is also inhibited by the active metabolite of clopidogrel.
Indication :
Contraindications :
Hypersensitivity
Active pathologic bleeding (e.g., peptic ulcer, intracranial hemorrhage)
Dosing :
0.2-1 mg/kg PO OD.
Max: 75 mg/day.
Adverse Effect :
Agranulocytosis, aplastic anemia/pancytopenia, thrombotic thrombocytopenic purpura (TTP), acquired hemophilia A, hemorrhage, abnormal liver function test, hypersensitivity reactions, anaphylactoid reactions, serum sickness, headache, bronchospasm, interstitial pneumonitis, vasculitis, hypotension.
Interaction :
Abciximab: May increase the risk of bleeding.
Aspirin: May increase the risk of bleeding.
Armodafinil: May decrease clopidogrel efficacy.
Renal Dose :
Dose in Renal Impairment GFR (mL/min)
20-50 | Dose as in normal renal function |
10-20 | Dose as in normal renal function |
<10 | Dose as in normal renal function |
Dose in Patients undergoing Renal Replacement Therapies
CAPD | Unlikely to be dialysed. Dose as in normal renal function |
HD | Unlikely to be dialysed. Dose as in normal renal function |
HDF/High flux | Unknown dialysability. Dose as in normal renal function |
CAV/VVHD | Unlikely to be dialysed. Dose as in normal renal function |
Hepatic Dose :
No dosage adjustments are recommended.