Plagerine

Plagerine

clopidogrel

Manufacturer:

Micro Labs

Distributor:

Zizawa Healthcare
Full Prescribing Info
Contents
Clopidogrel bisulphate.
Description
Each tablet contains clopidogrel bisulphate equivalent to clopidogrel 75 mg.
Clopidogrel bisulphate is methyl(+)-(S)-(2-chlorophenyl)-6,7-dihydrothieno[3,2-c] pyridine-5(4H)-acetatesulfate (1:1).
Action
Antiplatelet agent.
Pharmacology: Clopidogrel is an inhibitor of platelet aggregation. A variety of drugs that inhibit platelet function have been shown to decrease morbid events in people with established atherosclerotic cardiovascular disease as evidenced by stroke or transient ischemic attacks, myocardial infarction, or need for bypass or angioplasty. This indicates that platelets participate in the initiation and/or evolution of these events and that inhibiting them can reduce the event rate.
Pharmacodynamics: Clopidogrel selectively inhibits the binding of adenosine diphosphate (ADP) to its platelet receptor and the subsequent A.P.-mediated activation of the glycoprotein GPIIb/IIIa complex, thereby inhibiting platelet aggregation. Biotransformation of clopidogrel is necessary to produce inhibition of platelet aggregation, but an active metabolite responsible for the activity of the drug has not been isolated. It also inhibits platelet aggregation induced by agonists other than ADP by blocking the amplification of platelet activation by released A.P. Clopidogrel does not inhibit phosphodiesterase activity.
Pharmacokinetics: Clopidogrel is extensively metabolized by the liver. The main circulating metabolite is the carboxylic acid derivative and it too has no effect on platelet aggregation. It represents about 85% of the circulating drug-related compounds in plasma.
The elimination half-life of the main circulating metabolite was 8 hrs after single and repeated administration. Covalent binding to platelets accounted for 2% of radiolabel with a half-life of 11 days. Clopidogrel is rapidly absorbed after oral administration of repeated doses of 75 mg clopidogrel (base), with peak plasma levels (~/=3 mg/L) of the main circulating metabolite occurring approximately 1 hr after dosing. The pharmacokinetics of the main circulating metabolite is linear (plasma concentrations increased in proportion to dose) in the dose range of 50-150 mg of clopidogrel. Absorption is at least 50% based on urinary excretion of clopidogrel-related metabolites.
Clopidogrel undergoes rapid hydrolysis into its carboxylic acid derivative.
Indications/Uses
For the reduction of atherosclerotic events (myocardial infarction, stroke and vascular death) in patients with atherosclerosis documented by recent stroke, recent myocardial infarction or established peripheral arterial disease.
Dosage/Direction for Use
Hypertension: Recommended Dose: 75 mg once daily, with or without food.
No dosage adjustment is necessary for elderly patients or patients with renal disease.
Overdosage
One case of deliberate overdosage with clopidogrel was reported in the large, controlled clinical study. A 34-year old woman took a single 1,050-mg dose of clopidogrel (equivalent to 14 standard 75-mg tablets). There were no associated adverse events. No special therapy was instituted and she recovered without sequelae. Based on biological plausibility, platelet transfusion may be appropriate to reverse the pharmacological effects of clopidogrel if quick reversal is required.
Contraindications
Patients with hypersensitivity to any of the components of Plagerine; active pathological bleeding eg, peptic ulcer or intracranial hemorrhage.
Special Precautions
As with other antiplatelet agents, clopidogrel should be used with caution in patients who may be at risk of increased bleeding from trauma, surgery or other pathological conditions. If a patient is to undergo elective surgery and an antiplatelet effect is not desired, clopidogrel should be discontinued 7 days prior to surgery.
Use in pregnancy & lactation: There are no adequate and well-controlled studies in pregnant women. Clopidogrel should be used during pregnancy only if clearly needed.
It is not known whether clopidogrel is excreted in human milk. Because many drugs are excreted in human milk and because of the potential for serious adverse reactions in nursing infants, a decision should be made whether to discontinue nursing or to discontinue clopidogrel, taking into account the importance of the drug to the nursing woman.
Use In Pregnancy & Lactation
There are no adequate and well-controlled studies in pregnant women. Clopidogrel should be used during pregnancy only if clearly needed.
It is not known whether clopidogrel is excreted in human milk. Because many drugs are excreted in human milk and because of the potential for serious adverse reactions in nursing infants, a decision should be made whether to discontinue nursing or to discontinue clopidogrel, taking into account the importance of the drug to the nursing woman.
Adverse Reactions
Body as a Whole (General disorders): Chest pain, accidental injury, influenza-like symptoms, pain, fatigue.
Cardiovascular Disorders (General): Edema, hypertension.
Central and Peripheral Nervous System Disorders: Headache, dizziness.
Gastrointestinal System Disorders: Abdominal pain, dyspepsia, diarrhea, nausea.
Metabolic and Nutritional Disorders: Hypercholesterolemia.
Musculoskeletal System Disorders: Arthralgia, back pain.
Platelet, Bleeding and Clotting Disorders: Purpura, epistaxis.
Psychiatric Disorders: Depression.
Respiratory System Disorders: Upper respiratory tract infection, dyspnoea, rhinitis, bronchitis, coughing.
Skin & Appendage Disorders: Rash, prorates.
Urinary System Disorders: Urinary tract infection.
Drug Interactions
Aspirin did not modify the clopidogrel-mediated inhibition of A.P.-induced platelet aggregation. Co-administration of heparin had no effect on inhibition of platelet aggregation induced by clopidogrel.
Clopidogrel should be co-administered with caution in NSAIDs.
Storage
Store in a cool, dry place.
MIMS Class
Anticoagulants, Antiplatelets & Fibrinolytics (Thrombolytics)
ATC Classification
B01AC04 - clopidogrel ; Belongs to the class of platelet aggregation inhibitors excluding heparin. Used in the treatment of thrombosis.
Presentation/Packing
FC tab 75 mg x 3 x 10's.
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