Clopidogrel

CLOPIDOGREL

Manufacturer: Amneal Pharmaceuticals LLC

Score: 148.0

Quick Summary

Clopidogrel is a P2Y12 platelet inhibitor used to reduce the rate of myocardial infarction and stroke in patients with acute coronary syndrome, recent myocardial infarction, recent stroke, or established peripheral arterial disease. It works by inhibiting platelet activation and aggregation through the irreversible binding of its active metabolite to the P2Y12 class of ADP receptors on platelets. The drug has several important safety considerations, including a warning about diminished antiplatelet effect in patients with two loss-of-function alleles of the CYP2C19 gene, contraindications for active pathological bleeding and hypersensitivity, and potential adverse reactions such as bleeding, thrombotic thrombocytopenic purpura, and gastrointestinal disorders. The recommended dosing is a 300 mg loading dose followed by 75 mg once daily, with considerations for special populations including pregnancy, nursing mothers, pediatric use, and geriatric use.

Key Clinical Findings and Indications

Reduces the rate of myocardial infarction and stroke in patients with acute coronary syndrome
Reduces the rate of myocardial infarction and stroke in patients with recent myocardial infarction, recent stroke, or established peripheral arterial disease
Inhibits platelet activation and aggregation through the irreversible binding of its active metabolite to the P2Y12 class of ADP receptors on platelets

Important Safety Information

Warning

Diminished antiplatelet effect in patients with two loss-of-function alleles of the CYP2C19 gene

Contraindications

Active pathological bleeding, such as peptic ulcer or intracranial hemorrhage
Hypersensitivity to clopidogrel or any component of the product

Adverse Reactions

Bleeding, including life-threatening and fatal bleeding
Thrombotic thrombocytopenic purpura
Gastrointestinal disorders, such as diarrhea, abdominal pain, and gastrointestinal hemorrhage

Dosing Recommendations

General Guidance

No dosage adjustment is necessary in elderly patients

Acute coronary syndrome

Adult Dose

300 mg loading dose followed by 75 mg once daily

Pediatric Dose

Not established

Recent myocardial infarction, recent stroke, or established peripheral arterial disease

Adult Dose

75 mg once daily

Pediatric Dose

Not established

Special Population Considerations

Pregnancy

Available data from cases reported in published literature and post-marketing surveillance have not identified any drug-associated risks for major birth defects or miscarriage
Therapy for the pregnant woman should not be withheld because of potential concerns regarding the effects of clopidogrel on the fetus

Nursing Mothers

No adverse effects on breastfed infants have been observed with maternal clopidogrel use during lactation in a small number of post-marketing cases
The developmental and health benefits of breastfeeding should be considered along with mother's clinical need for clopidogrel and any potential adverse effects on the breastfed infant from clopidogrel or from underlying maternal condition

Pediatric Use

Safety and effectiveness in pediatric populations have not been established
A randomized, placebo-controlled trial (CLARINET) did not demonstrate a clinical benefit of clopidogrel in neonates and infants with cyanotic congenital heart disease palliated with a systemic-to-pulmonary arterial shunt

Geriatric Use

Of the total number of subjects in the CAPRIE and CURE controlled clinical studies, approximately 50% of patients treated with clopidogrel were 65 years of age and older, and 15% were 75 years and older
No dosage adjustment is necessary in elderly patients