Pharmacokinetics: Clopidogrel is rapidly but incompletely absorbed after oral doses; absorption appears to be at least 50%. It is a prodrug and is extensively metabolized in the liver, following absorption, mainly to the inactive carboxylic acid derivative. The active metabolite appears to be a thiol derivative but has not been identified in the plasma. Clopidogrel and the carboxylic acid derivative are highly protein bound. Clopidogrel and its metabolites are excreted in the urine and feces; after oral administration, 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 adenosine diphosphate-mediated platelet aggregation. It is given prophylactically as an alternative to aspirin in patients at risk of thromboembolic disorders eg, myocardial infarction, peripheral arterial disease and stroke. Clopidogrel is also used with aspirin in the management of patients with unstable angina, as an adjunct to medical or interventional management.
Prophylaxis of Thromboembolic Events: 75 mg once daily.
Management of Acute Coronary Syndrome including Unstable Angina and Non-Q Wave Myocardial Infarction: 300 mg as a single loading dose, followed by 75 mg once daily.
Hypersensitivity to clopidogrel or any component of Timiflo.
Severe hepatic impairment; active pathological bleeding eg, peptic ulcer or intracranial hemorrhage.
Use in lactation: The use of clopidogrel is contraindicated in breastfeeding.
Thrombotic Thrombocytopenia Purpura (TTP): Thrombotic thrombocytopenia purpura has been reported rarely following use of clopidogrel, sometimes after a short exposure (<2 weeks). It is a serious condition and requires urgent referral to a hematologist for prompt treatment. It is characterized by thrombocytopenia, microangiopathic hemolytic anemia [schistocytes (fragmented RBCs) seen on peripheral smear], neurological findings, renal dysfunction and fever.
Use with caution in patients at risk of increased bleeding from trauma, surgery or other pathological condition, patients who have lesions with a propensity to bleed (eg, ulcer) and hepatic impairment.
Discontinue clopidogrel 7 days prior to surgery or any event when a normal platelet effect is needed.
Use with caution in patients taking medication that increased the risk of bleeding eg, nonsteroidal anti-inflammatory drugs (NSAIDs) or aspirin.
Use in pregnancy: Use in pregnancy only if it is clearly indicated.
Use in children: Clopidogrel is not approved for use in children.
The incidence of adverse effects, particularly blood dyscrasias, is lower with clopidogrel, although fatalities have been reported. Other adverse effects reported rarely includes serum sickness, interstitial pneumonitis, erythema multiforme, Stevens-Johnson syndrome, lichen planus and myalgia.
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 P-450 isoenzyme CYP2C9 and interactions with drugs metabolized by this isoenzyme are theoretically possible. It may also inhibit CYP2B6.
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.