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Each caplet contains : Clopidogrel bisulphate equivalent to clopidogrel. 75 mg PHARMACOLOGY Clopidogrel selectively inhibits the binding of adenosine diphosphate (ADP) to its platelet receptor and the subsequent ADP- medicated activation of the GPIIa/IIIa complex, thereby inhibiting platelet agregation. Biotransformation of Clopidogrel is necessary to produce inhibiton of platetel agregation. Clopidogrel also inhibits platelets agregation induced by other agonist by blocking the amplification of platelet activation by released ADP. Clopidogrel acts by irreversible modifiying the platelet ADP receptor. Consequently, platelets exposed to Clopidogrel are effected for the remainder of their lifespan and recovery of normal platelet function occurs at a rate consistent with platelet turnover. Clopidogrel is extensively metabolized by the liver and the main metabolite, which is inactive, is the carboxylic acid derivative, which represents about 85% of the circulating compound in plasma. Clopidogrel is prodrug. The active metabolite, a thiol derivative, is formed by oxidation of Clopidogrel to 2-oxo-Clopidogrel and subsequent hydrolysis. The oxidation step is regulated primary by cythocrome P450 isoenzyms WB6 and 3A4 and to a lesser extent by 1A1, 1A2 and 2C19. The active thiol metabolite has not been detected in plasma. INDICATIONS Myocardial infarction (from few days until less than 35 days) Ischaemic stroke (from 7 days until less than 6 months) Established peripheral arterial disease Non-ST segment elevation acute coronary syndrome (unstable angina or non-Q-wave myocardial infarction) in combination with ASA. CONTRA – INDICATIONS Hypersensitivity to any component of this drug Active pathological bleeding Severe liver impairment, lactation, active pathological bleeding such as peptic ulcer or intracranial hemorrhage. DOSAGES Adults and elderly: Clopidogrel should be given as single daily dose of 75 mg with or without food. In patients suffering from acute coronary syndrome. Clopidogrel should be given as single daily dose of 75 mg with or without food. In patients suffering from acute coronary syndrome. Non-ST segment elevation (unstable angina or non-Q-wave myocardial infarction) : Clopidogrel treatment should be initiated with a single 300 mg loading dose and then continued at 75 mg once a day (with acetyl salicylic acid (ASA) 75 mg-325 mg daily). Since higher doses of ASA were associated with higherbleeding risk it is recommended that the dose of ASA should not be higher than 100 mg. The optimal duration of treatment has not been formally establish. Children and adolescents : There is no experience in children. WARNINGS AND PRECAUTIONS Should be used with caution in patients who may be at risk of increased bleeding from trauma, surgery or other pathological conditions, and in patients receiving treatment with ASA, nonsteroid anti-inflamatory drugs, including COX 2-inhibitors, heparin, or glycoprotein IIb/ IIIa inhibitors. Clopidogrel prolongs bleeding time and should be used with caution in patients who have lesions with a propensity to bleed (particularly gastrointestinal and intraocular) Clopidogrel should be used with caution in hepatically and renally impaired patients. Patients should be informed of any of the following: During the course of therapy with clopidogrel alone or in combination with aspirin, patients can be more easily injured and / or bleed, also takes more than normal time for cessation of bleeding. patients should inform the doctor if abnormal bleeding occur. Patients should inform the doctor or dentist about Clopidogrel therapy before surgery is taken or the use of new drugs. The efficacy and safety in children have not been established. Pregnancy and lactation : it is preferable not to use Clopidogrel during pregnancy as a precautionary measure. Clopidogrel should not be administered in nursing mother. Due to the risk of bleeding and haematological undesireble effects, blood cell count determination and/or other appropriate testing should be promptly considered whenever clinical symptoms suggestive of bleeding arise during the course of treatment. Patients should be followed carefully for any signs of bleeding including occult bleeding, especially during the first weeks of treatment and/or after invasive cardiac procedures or surgery. Patients should be told that it might take longer than usual to stop bleeding when they take Clopidogrel (alone or in combination with ASA), and that they should report any unusual bleeding (site or duration) to their physician. Patients should inform physicians and dentist that they are taking Clopidogrel before any surgery is scheduled and before any new drug is taken. Thrombotic Thrombocytopenic Purpura (TTP) has been reported very rarely following the use of Clopidogrel, sometimes after a short exposure. It is characterised by thrombocytopenia and microangiopathic hemolytic anemia associated with either neurological findings, renal dysfunction or fever. TTP is a potentialy fatal condition requiring prompt treatment including plasmapheresis. In view of the lack of data, Clopidogrel cannot be recommended in acute ischaemic stroke (less than 7 days). Patient with rare herditary problems of galactose intolerance, the lapp lactase deficiencies or glucose galactose malabsorption should not taken this medicine. SIDE EFFECTS Hemorrhagic disorders : Bleeding, gastrointestinal bleeding, purpura/bruising/haematoma and epstaxis. Haematuria and eye bleeding (mainly conjuntival), intracranial bleeding. Haematological disorders : severe neutropenia, a plastic anaemia, severe thrombocytopenia. Central and peripheral nervous system disorders : Headache, vertigo, dizziness and paraesthesia. Gastrointestinal system disorders : Dyspepsia, abdominal pain and diarrhoea Nausea, gastritis, flatulence, constipation, vomiting, gastric ulcer and duodenal ulcer. Colitis (including ulcerative or lymphocytic colitis), pancreatitis Skin and appendage disorders : rash and pruritus, angiodema, bullous dermatitis (erythema multiforme, rash erythematous, urticaria, exzema and lichen planus. Blood and lymphatic system disorders : Thrombotic Thrombocytopenic Purpura (TTP) severe thrombocytopenia, granulocytopenia, agranulocytosis, anaemia dan aplastic anaemia/pancytopenia. Platelet, bleeding and clotting disorders : bleeding time increased and platelets decreased. Bleeding : some cases were reported with fatal outcome (especially intracranial, gastrointestinal and retroperitoneal hemorrhage); serious cases of skin bleeding (purpura), musculoskeletal bleeding (haemarthrosis, haematomal), eye bleeding (conjunctival ocular, retina), epistaxis, respiratory tract bleeding (haemoptysis, pulmonary haemorrhage), haematuria and haemorrhage of operative wound have been reported; cases of serious haemorrhage have been reported in patients taking Clopidogrel concomitanly with acetylsalicylic acid or Clopidogrel with acetylsalicylic acid and heparin. White cell and RES disorders : Leucopenia, neutrophils decreased and eosinophilia. Immune system disorders : Anaphylactoid reaction. Psychiatric disorders : confusion, hallucinations. Nervous system disorders : taste disturbance. Vascular disorders : Vasculitis, hypotension. Respiratory, thoracic, and mediatinal disorders : Bronchospasm. Hepato-biliary disorders : Hepatitis. Musculoskeletal, connective tissue and bone disorders : Arthralgia, arthritis. Renal and urinary disorders : Glomerulonephritis. General disorders and administration site conditions : Fever. Investigations : Abnormal liver function test, blood creatinine increase. OVERDOSAGES Overdose following Clopidogrel administration may lead to prolonged bleeding time and subsequent bleeding complications. Appropriate therapy should be considered if bleeding are observed. No antidote to the pharmacological activity Clopidogrel has been found. If prompt correction of prolonged bleeding time is required, platelet transfusion may reverse the effects of Clopidogrel. DRUG INTERACTIONS Aspirin does not influence the inhibition of platelet aggregation by clopidogrel It should be used with caution when concomitantly administered with non steroidal anti inflammatory drugs. It should be used with caution when administered concomitantly with warfarin. Glycoprotein IIb/IIIa inhibitor : Clopidogrel should be used with caution in patients who may be at risk of increased bleeding from trauma, surgery or other pathological conditions that receive concomitant glycoprotein IIb/IIIa inhibitors. Thrombolytics : the safety of the concomitant administration of Clopidogrel, rt-PA and heparin was assessed in patients with recent myocardial infarction. The incidence of clinically significant bleeding was similar to that observed when rt-PA and heparin are co-administered with ASA. The safety of the concomitant adiministration of Clopidogrel with other thrombolytic agents has not been formally established and should be undertaken with caution. Heparin : concomitant use with Clopidogrel does not alter heparin dosage or coagulation effects and does not causes Clopidogrel-induced inhibition of platelet aggregation. A pharmacodynamic interaction between Clopidogrel and heparin is possible, leading to increased risk of bleeding. Concomitant use should be undertaken with caution. Presentation : Box, 5 strips @ 6 caplets ON MEDICAL PRESCRIPTION ONLY Storage : store at a cool (15-25C) and dry place, protected from light. |
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