Indications

In patients with non-ST-segment elevation ACS [unstable angina (UA)/non-ST-elevation myocardial infarction (NSTEMI)], it is suggested to lower the incidence 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 suggested to lower the incidence of MI and stroke in patients with established peripheral arterial disease or a history of recent myocardial infarction (MI) or recent stroke.

Pharmaceutical Name

Eskayef Pharmaceuticals Ltd.

Pharmacology

Clopidogrel is a prodrug that is used to treat blood clots. The irreversible binding of its active metabolite to the P2Y12 family 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 reduce ADP-induced platelet aggregation, and inhibition achieves a stable state between Days 3 and 7.

Dosage & Administration

• Acute Coronary Syndrome: Start Noclog with a single 300 mg (4 tablet) oral loading dose and then continue at 75 mg once day in individuals who need an antiplatelet effect within hours. It will take several days to establish an antiplatelet effect if you start it without a loading dosage.
• 75 mg once day orally without a loading dose for recent MI, recent stroke, or established peripheral arterial disease.
• It’s taken by mouth, with or without meals.

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): Noclog should not be used with Repaglinide since it raises Repaglinide plasma level.

Contraindications

Hypersensitivity to the medication ingredient or any component of the product is a contraindication to taking clopidogrel. Peptic ulcer or cerebral hemorrhage are examples of active pathological bleeding.

Side Effect

• Noclog is a medication that is typically well-tolerated.
• Bleeding, diarrhea, gastrointestinal pain, hemorrhage, and skin responses are all common adverse effects.
• Acquired hemophilia, anemia, angioedema, arthralgia, arthritis, and bone marrow abnormalities are all rare adverse effects.

Pregnancy & Lactation

In pregnant women, there are no appropriate and well-controlled trials. It should only be taken during pregnancy if absolutely necessary. Clopidogrel is not known to be excreted in human breast milk. Considering the medication’s value to the mother, a choice should be taken whether to cease breastfeeding or discontinue the drug.

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.
• Discontinuation of Clopidogrel increases the risk of cardiovascular events. Discontinue 5 days prior to elective surgery that has a major risk of bleeding. Resume Clopidogrel as soon as hemostasis is achieved.
• Thrombotic Thrombocytopenic Purpura (TTP) has been reported that requires urgent treatment including plasmapheresis (plasma exchange).
• Hypersensitivity including rash, angioedema, or hematologic reaction has been reported in patients receiving clopidogrel or a history of hypersensitivity to other thienopyridines.

Therapeutic Class

Following clopidogrel treatment, an overdose might result in bleeding problems. Platelet transfusion may restore clotting capacity based on biological plausibility.

Storage Conditions

Keep below 30°C temperature in a dry place. Protected from light. Do not freeze. Keep out of reach of children.

Generic

Clopidogrel Bisulphate