Generic

Clopidogrel Bisulphate

Indications

In patients with non-ST-segment elevation ACS [unstable angina (UA)/non-ST-elevation myocardial infarction (NSTEMI)], it is advised to reduce the rate of myocardial infarction (MI) and stroke. In individuals with acute ST-elevation myocardial infarction, it is used to lower the risk of myocardial infarction and stroke (STEMI).

Recent MI, recent Stroke, or existing Peripheral Artery Disease: It is advised to lower the rate of MI and stroke in patients with established peripheral arterial disease or a history of recent myocardial infarction (MI) or recent stroke.

Pharmacology

Clopidogrel is a prodrug that is used to treat blood clots. The irreversible binding of its active metabolite to the P2Y12 class of ADP receptors on platelets suppresses platelet activation and aggregation. Platelet aggregation inhibition is dose-dependent and visible 2 hours after single oral dosages. On the first day, repeated 75 mg doses decrease ADP-induced platelet aggregation, and inhibition achieves a stable state between Days 3 and 7.

Dosage & Administration

Acute Coronary Syndrome: In patients who need an antiplatelet effect within hours, initiate Odrel with a single 300 mg (4 tablets) oral loading dose and then continue at 75 mg once daily. Initiating it without a loading dose will delay establishment of an antiplatelet effect by several days.

Recent MI, Recent Stroke, or Established Peripheral Arterial Disease: 75 mg once daily orally without a loading dose.

It is given orally with or without food.

Interaction

• NSAIDs, warfarin, and selective serotonin and serotonin norepinephrine reuptake inhibitors (SSRIs, SNRIs): NSAIDs, warfarin, and selective serotonin and serotonin norepinephrine reuptake inhibitors (SSRIs, SNRIs): CYP2C19 inhibitors (omeprazole or esomeprazole): Increases the risk of bleeding. Avoid taking omeprazole or esomeprazole at the same time.
• Repaglinide (substrates for CYP2C8): Clopidogrel should not be taken with Repaglinide since it raises Repaglinide plasma level.

Contraindications

Odrel should not be used if you have any of the following conditions: Hypersensitivity to the medicine or any of the product’s components. Peptic ulcer or cerebral hemorrhage are examples of active pathological bleeding.

Side Effects

• Odrel is a generally well-tolerated drug.
• Common side effects: Bleeding, Diarrhoea, gastrointestinal discomfort, hemorrhage, Skin reactions.
• Rare side effects: Acquired hemophilia, anemia, angioedema, arthralgia, arthritis, bone marrow disorders.

Pregnancy & Lactation

There are no adequate and well-controlled studies on pregnant women. It should be used during pregnancy only if clearly needed. It is unknown whether Odrel is excreted in human breast milk. A decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.

Precautions & Warnings

• As it is a prodrug, so metabolism to its active metabolite is impaired by genetic variations in CYP2C19 (poor metabolizer) and by the drugs that inhibit CYP2C19 such as Omeprazole and Esomeprazole. Concomitant use with these drugs and in CYP2C19 poor metabolizer may reduce the antiplatelet activity of Clopidogrel.
• As it inhibits platelet aggregation for the lifetime of the platelet (7-10 days), the risk of bleeding may increase. To restore hemostasis, platelet transfusions within 4 hours of the loading dose or 2 hours of the maintenance dose may be less effective.

Therapeutic Class

Anti-platelet drugs

Storage Conditions

Protect from light and moisture by storing in a cool, dry place below 30°C. Keep out of children’s reach.

Pharmaceutical Name

Beximco Pharmaceuticals Ltd.