Clovel
Clopidogrel
Indication
Clopidogrel is used to prevent atherothrombosis, which can lead to atherothrombotic events (such as heart attack,recent myocardial infarction, recent stroke or established peripheral arterial disease).
Clopidogrel is used with aspirin for prevention of arterothrombotic and thromboembolic events in patients with atrial fibrillations (irregular heartbeat).
Dosage and Administration
Recent myocardial infarction, recent stroke or established peripheral arterial disease 75 mg once daily. Non-ST segment elevation acute coronary syndrome (unstable angina/ non-Q wave myocardial infarction). Initially 300 mg loading dose and then continued at 75 mg once daily. Aspirin (75 mg - 325 mg...
Composition
Each film-coated tablet contains:
Clopidogrel Bisulfate USP equivalent to Clopidogrel 75 mg.
Description
Clopidogrel bisulfate, an antiplatelet, is a thienopyridine class inhibitor of P2Yl 2ADP platelet receptors. Chemically, it is thieno [3,2-c] pyridine-5(4H)-acetic acid, a-(2-chloroph enyl)-6, 7-dihydro-, methyl ester, (S)-, sulfate (1:1) or methyl (+)-(S)-a-(o-chlorophenyl)-6, 7-dihydrothieno [3, ...
Clinical Pharmacology
Clopidogrel is metabolized by CYP450 enzyme to produce the active metabolite that inhibits platelet aggregation. The active metabolite of clopidogrel selectively inhibits the binding of adenosine diphosphate (ADP) to its platelet P2Y 12 receptor and the subsequent ADP-mediated activation of the glyc...
Pharmacokinetics
Clopidogrel is rapidly but incompletely absorbed from GI tract (approximately 50%). Time to peak plasma concentration is approximately 30 - 60 minutes. Clopidogrel is a primary and has extensive first-pass metabolism in liver. Tt is extensively metabolized by two main metabolic pathways: one mediate...
Inhibition of platelet aggregation detected 2 hours after 300 mg administered; after second day of treatment with 50 - 100 mg/day.
Excretion is approximately 50% in urine, approximately 46% in faeces, both as metabolites and unchanged drugs. Administration of clopidogrel with meals or by prior antiplatelets ingestion did not significantly modify the bioavailability of clopidogrel.
Contraindication
Hypersensitivity to clopidogrel or any component of the formulation.
Active pathological bleeding such as peptic ulcer or intracranial haemorrhage.
Coagulation disorders.
Precaution
Clopidogrel should be used with caution in cases of thrombotic thrombocytopenic purpura (TTP); patients receiving anticoagulants or other antiplatelet drugs concurrently; liver disease; hypertension; renal impairment; patients having a previous hypersensitivity or other untoward effects related to t...
Adverse Effects
As clopidogrel affects hemostasis, bleeding is associated, and hemorrhage may occur at virtually any site.
>10% GI: Abdominal pain, vomiting, dyspepsia, gastritis and constipation.
3% to 10% CVS: Chest pain, oedema, hypertension. CNS: Headache, dizziness, depression, fatigue, general pain.
Respiratory: Dyspnea, rhinitis, bronchitis, coughing, upper respiratory infection.
Other: Rash, pruritus,hypercholesterolemia, diarrhea, nausea, UTT, purpura, liver function test abnormalities, arthralgia, back pain, flu-like syndrome.
<l% Life threatening: Agranulocytosis, allergic reaction, angioedema, aplastic anaemia, thrombocytopenia, hepatitis, haemorrhage.
Drug Interaction
Cytochrome P450 effect: Substrate of CYP I A2, 3A4, inhibits CYP2C8/9.
Increased Effect/ Toxicity: At high concentration, clopidogrel may interfere with the metabolism of amiodarone, cisapride, cyclosporine, diltiazem, fluvastatin, irbesartan, losartan, oral hypoglycemic, paclitaxel, phenytoin, quinidine, sildenafil, tamoxifen, torsemide, verapamil and some NSAIDs whic...
Clopidogrel and naproxen resulted in an increase of GI occult blood loss.
Anticoagulants (warfarin, thrombolytics) or other anti-platelet agents may increase the risk of bleeding.
Storage
Store below 30°C in cool and dry place. Protect from light and moisture. Keep out of reach and sight of children.
Presentation
3 x 10's Alu-Alu Blisters.