Pharmacology: Mechanism of Action: Clopidogrel bisulfate is an inhibitor of ADP-induced platelet aggregation acting by direct inhibition of adenosine diphosphate (ADP) binding to its receptor and of the subsequent ADP-mediated activation of the glycoprotein GPIIb/IIIa complex.
Pharmacokinetics: Clopidogrel is rapidly but incompletely absorbed after oral dose; absorption appears to be at least 50%. It is a prodrug and is extensively metabolized in the liver, mainly to the inactive carboxylic acid derivative. The active metabolite appears to be a thiol derivative but has not been identified in plasma. Clopidogrel and the carboxylic acid derivative are highly protein bound. Clopidogrel and its metabolites are excreted in urine and feces; about 50% of an oral dose is recovered from the urine and about 46% from the feces.
Clopidogrel is a thienopyridine antiplatelet drug used in thromboembolic disorders. It is an analogue of ticlopidine and acts by inhibiting ADP-mediated platelet aggregation. It is given prophylactically as an alternative to aspirin in patients with atherosclerosis who are at risk of thromboembolic disorders eg, myocardial infarction, peripheral arterial disease and stroke. It is also used with aspirin in patients with unstable angina, as an adjunct to medical or interventional management.
Prophylaxis of Thromboembolic Events: Usual Dose: 75 mg once daily.
Management of Acute Coronary Syndromes (including Unstable Angina and Non-Q Wave Myocardial Infarction): Single 300-mg loading dose, followed by 75 mg once daily.
Overdosage following clopidogrel administration may lead to prolonged bleeding time and subsequent bleeding complications. Appropriate therapy should be considered is bleeding is observed or suspected.
No antidote to the pharmacological activity of clopidogrel has been found. Platelet transfusion may be used to reverse the pharmacological effects of clopidogrel when quick reversal is required.
Hypersensitivity to clopidogrel or any of the ingredients in the formulation or components of Clopidra.
Active bleeding eg, peptic ulcer and intracranial hemorrhage.
Significant liver impairment or cholestatic jaundice.
As with other antiplatelet agents, when considering prescribing clopidogrel, physicians should inquire whether the patient has a history of bleeding. Clopidogrel should be used with caution in patients who may be at risk of increased bleeding from recent trauma, surgery or other pathological condition/s. Because of the increase risk of bleeding, the concomitant administration of warfarin with clopidogrel should be undertaken with caution.
In patients with recent transient ischemic attack (TIA) or stroke who are at high risk of recurrent ischemic events, the combination of aspirin and clopidogrel has not been shown to be more effective then clopidogrel alone, but the combination has been shown to increase major bleeding.
If a patient is to undergo elective surgery, consideration should be given to discontinue clopidogrel 5-7 days prior to surgery to allow for the reversal of the effect.
Clopidogrel prolongs bleeding time. Although it has shown a lower incidence of gastrointestinal bleeding compared to acetylsalicylic acid (ASA) in a large, controlled clinical trial (CAPRIE), clopidogrel should not be used in patients who have lesions with a propensity to bleed. In CURE, the incidence of major gastrointestinal bleeding was 1.3% versus 0.7% (clopidogrel + ASA vs placebo + ASA, respectively). In patients taking clopidogrel, drugs that might induce GI lesions should be used in caution.
The most frequent adverse drug reactions (≥1%) with clopidogrel (with or without associated ASA) in controlled clinical trials were hemorrhage and bleeding disorders including purpura, any rash, dyspepsia, abdominal pain and diarrhea.
The most serious adverse drug reactions from controlled clinical trials rarely reported (<1%) were bleeding and clotting disorders including gastrointestinal hemorrhage, hemorrhagic ulcer and hemothorax.
Bleeding Disorders: Agranulocytosis/granulocytopenia, aplastic anemia, neutropenia and thrombocytopenia.
Gastrointestinal System Disorders: Duodenal, gastric or peptic ulcer, gastritis.
Skin Disorders: Any rash and bullous eruption.
Clopidogrel should be used with caution in patients receiving other drugs that increase the risk of bleeding, including anticoagulants, other antiplatelets and NSAIDs. Clopidogrel may inhibit the cytochrome P450 isoenzyme CYP2C9 and interactions with drugs metabolized by this isoenzyme are theoretically possible; it may also inhibit CYP2B6 as was observed with the reduced conversion of bupropion to its active metabolite.
Store at temperatures not exceeding 30°C.
B01AC04 - clopidogrel ; Belongs to the class of platelet aggregation inhibitors excluding heparin. Used in the treatment of thrombosis.
Clopidra FC tab 75 mg
100's (P29/film-coated tab, P2,900/box)
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