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Effient

Effient, a thienopyridine derivative, is a platelet activation and aggregation inhibitor structurally and pharmacologically related to clopidogrel and ticlopidine. Similar to clopidogrel, effient is a prodrug that requires enzymatic transformation in the liver to its active metabolite, R-138727. R-138727 irreversibly binds to P2Y12 type ADP receptors on platelets thus preventing activation of the GPIIb/IIIa receptor complex. As a result, inhibition of ADP -mediated platelet activation and aggregation occurs. Effient was developed by Daiichi Sankyo Co. and is currently marketed in the United States and Canada in cooperation with Eli Lilly and Company for acute coronary syndromes planned for percutaneous coronary intervention (PCI ). FDA approved in 2009.

Effient is a member of the thienopyridine class of ADP receptor inhibitors, like ticlopidine (trade name Ticlid) and clopidogrel (trade name Plavix). These agents reduce the aggregation (“clumping”) of platelets by irreversibly binding to P2Y12 receptors. Compared to clopidogrel, effient inhibits adenosine diphosphate–induced platelet aggregation more rapidly, more consistently, and to a greater extent than do standard and higher doses of clopidogrel in healthy volunteers and in patients with coronary artery disease, including those undergoing PCI. The increased potency of effient appears to be due to more efficient conversion to its active metabolite. However, it carries a higher risk of bleed compared to clopidogrel, which may be a result of its higher potency. Effient produces inhibition of platelet aggregation to 20 μM or 5 μM ADP, as measured by light transmission aggregometry.

LD50 (rat) 1,000 – 2,000 mg/kg; LD50 (rabbit) > 1,000 mg/kg

Imprints


Drug: Effient
Strength: 10 Mg
Pill Imprint: 10 MG 4759
Color: Beige
Shape: Six-sided

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Drug: Effient
Strength: 10 Mg
Pill Imprint: 10 5123
Color: Beige
Shape: Six-sided

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Drug: Effient
Strength: 5 Mg
Pill Imprint: 5 MG 4760
Color: Yellow
Shape: Six-sided

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Drug: Effient
Strength: 5 Mg
Pill Imprint: 5 5121
Color: Yellow
Shape: Six-sided

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